U.S. BRAND NAMES — Excedrin® Extra Strength [OTC]; Excedrin® Migraine [OTC]; Fem-Prin® [OTC]; Genaced™ [OTC]; Goody's® Extra Strength Headache Powder [OTC]; Goody's® Extra Strength Pain Relief [OTC]; Pain-Off [OTC]; Vanquish® Extra Strength Pain Reliever [OTC]
PHARMACOLOGIC CATEGORY Analgesic, Miscellaneous
DOSING: ADULTS Pain management: Based on acetaminophen component: Mild-to-moderate pain: Oral: 325-650 mg every 4-6 hours as needed; do not exceed 4 g/day Mild-to-moderate pain associated with migraine headache: Oral: 500 mg/dose (in combination with 500 mg aspirin and 130 mg caffeine) every 6 hours while symptoms persist; do not use for longer than 48 hours Based on aspirin component: Mild-to-moderate pain: Oral: 325-650 mg every 4-6 hours as needed; do not exceed 4 g/day Mild-to-moderate pain associated with migraine headache: Oral: 500 mg/dose (in combination with 500 mg acetaminophen and 130 mg caffeine) every 6 hours; do not use for longer than 48 hours
Product labeling:
Excedrin® Extra Strength, Excedrin® Migraine: Oral: 2 doses every 6 hours (maximum: 8 doses/24 hours) Note: When used for migraine, do not use for longer than 48 hours
Goody's® Extra Strength Headache Powder: Oral: 1 powder, placed on tongue or dissolved in water, every 4-6 hours (maximum: 4 powders/24 hours)
Goody's® Extra Strength Pain Relief Tablets: Oral: 2 tablets every 4-6 hours (maximum: 8 tablets/24 hours)
Vanquish® Extra Strength Pain Reliever: Oral: 2 tablets every 4 hours (maximum: 12 tablets/24 hours)
DOSING: PEDIATRIC Product labeling:
Excedrin® Extra Strength, Excedrin® Migraine: Oral: Children >12 years: Refer to adult dosing
Goody's® Extra Strength Headache Powder: Oral: Children >12 years: Refer to adult dosing
Goody's® Extra Strength Pain Relief Tablets: Oral: Children >12 years: Refer to adult dosing
Vanquish® Extra Strength Pain Reliever: Oral: Children >12 years: Refer to adult dosing
DOSING: ELDERLY — Refer to adult dosing.
DOSING: HEPATIC IMPAIRMENT — Use with caution. Limited, low-dose therapy usually well tolerated in hepatic disease/cirrhosis. However, cases of hepatotoxicity at daily acetaminophen dosages <4 g/day have been reported. Avoid chronic use in hepatic impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Caplet: Excedrin® Extra Strength, Excedrin® Migraine: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg Vanquish® Extra Strength Pain Reliever: Acetaminophen 194 mg, aspirin 227 mg, and caffeine 33 mg
Geltab (Excedrin® Extra Strength, Excedrin® Migraine): Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg
Powder (Goody's® Extra Strength Headache Powder): Acetaminophen 260 mg, aspirin 520 mg, and caffeine 32.5 mg [contains lactose]
Tablet: Excedrin® Extra Strength, Excedrin® Migraine, Genaced™, Pain-Off: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg Fem-Prin®: Acetaminophen 194.4 mg, aspirin 226.8 mg, and caffeine 32.4 mg Goody's® Extra Strength Pain Relief: Acetaminophen 130 mg, aspirin 260 mg, and caffeine 16.25 mg
DOSAGE FORMS: CONCISE Caplet: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg; acetaminophen 194 mg, aspirin 227 mg, and caffeine 33 mg Excedrin® Extra Strength [OTC], Excedrin® Migraine [OTC]: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg Vanquish® Extra Strength Pain Reliever [OTC]: Acetaminophen 194 mg, aspirin 227 mg, and caffeine 33 mg
Geltab: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg Excedrin® Extra Strength [OTC], Excedrin® Migraine [OTC]: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg
Powder: Acetaminophen 260 mg, aspirin 520 mg, and caffeine 32.5 mg Goody's® Extra Strength Headache Powder [OTC]: Acetaminophen 260 mg, aspirin 520 mg, and caffeine 32.5 mg
Tablet: Excedrin® Extra Strength [OTC], Excedrin® Migraine [OTC], Genaced™ [OTC], Pain-Off [OTC]: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg Fem-Prin® [OTC]: Acetaminophen 194.4 mg, aspirin 226.8 mg, and caffeine 32.4 mg Goody's® Extra Strength Pain Relief [OTC]: Acetaminophen 130 mg, aspirin 260 mg, and caffeine 16.25 mg
GENERIC EQUIVALENT AVAILABLE — Yes
USE — Relief of mild-to-moderate pain; mild-to-moderate pain associated with migraine headache
ADVERSE REACTIONS SIGNIFICANT — See individual agents.
CONTRAINDICATIONS — Hypersensitivity to acetaminophen, aspirin, salicylates, caffeine, or any component of the formulation; pregnancy
DRUG INTERACTIONS Acetaminophen: Substrate (minor) of CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A4; Inhibits CYP3A4 (weak)
Aspirin: Substrate (minor) of CYP2C9
Caffeine: Substrate of CYP1A2 (major), 2C9 (minor), 2D6 (minor), 2E1 (minor), 3A4 (minor); Inhibits CYP1A2 (weak), 3A4 (moderate)
Also see individual agents.
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Excessive intake of ethanol may increase the risk of acetaminophen-induced hepatotoxicity. Avoid ethanol or limit to <3 drinks/day.
PREGNANCY RISK FACTOR — D (show table)
PHARMACODYNAMICS / KINETICS — See individual agents.
Wednesday, January 23, 2008
Sunday, January 20, 2008
Acetaminophen, aspirin, and caffeine
U.S. BRAND NAMES — Excedrin® Extra Strength [OTC]; Excedrin® Migraine [OTC]; Fem-Prin® [OTC]; Genaced™ [OTC]; Goody's® Extra Strength Headache Powder [OTC]; Goody's® Extra Strength Pain Relief [OTC]; Pain-Off [OTC]; Vanquish® Extra Strength Pain Reliever [OTC]
PHARMACOLOGIC CATEGORY Analgesic, Miscellaneous
DOSING: ADULTS Pain management: Based on acetaminophen component: Mild-to-moderate pain: Oral: 325-650 mg every 4-6 hours as needed; do not exceed 4 g/day Mild-to-moderate pain associated with migraine headache: Oral: 500 mg/dose (in combination with 500 mg aspirin and 130 mg caffeine) every 6 hours while symptoms persist; do not use for longer than 48 hours Based on aspirin component: Mild-to-moderate pain: Oral: 325-650 mg every 4-6 hours as needed; do not exceed 4 g/day Mild-to-moderate pain associated with migraine headache: Oral: 500 mg/dose (in combination with 500 mg acetaminophen and 130 mg caffeine) every 6 hours; do not use for longer than 48 hours
Product labeling:
Excedrin® Extra Strength, Excedrin® Migraine: Oral: 2 doses every 6 hours (maximum: 8 doses/24 hours) Note: When used for migraine, do not use for longer than 48 hours
Goody's® Extra Strength Headache Powder: Oral: 1 powder, placed on tongue or dissolved in water, every 4-6 hours (maximum: 4 powders/24 hours)
Goody's® Extra Strength Pain Relief Tablets: Oral: 2 tablets every 4-6 hours (maximum: 8 tablets/24 hours)
Vanquish® Extra Strength Pain Reliever: Oral: 2 tablets every 4 hours (maximum: 12 tablets/24 hours)
DOSING: PEDIATRIC Product labeling:
Excedrin® Extra Strength, Excedrin® Migraine: Oral: Children >12 years: Refer to adult dosing
Goody's® Extra Strength Headache Powder: Oral: Children >12 years: Refer to adult dosing
Goody's® Extra Strength Pain Relief Tablets: Oral: Children >12 years: Refer to adult dosing
Vanquish® Extra Strength Pain Reliever: Oral: Children >12 years: Refer to adult dosing
DOSING: ELDERLY — Refer to adult dosing.
DOSING: HEPATIC IMPAIRMENT — Use with caution. Limited, low-dose therapy usually well tolerated in hepatic disease/cirrhosis. However, cases of hepatotoxicity at daily acetaminophen dosages <4 g/day have been reported. Avoid chronic use in hepatic impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Caplet: Excedrin® Extra Strength, Excedrin® Migraine: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg Vanquish® Extra Strength Pain Reliever: Acetaminophen 194 mg, aspirin 227 mg, and caffeine 33 mg
Geltab (Excedrin® Extra Strength, Excedrin® Migraine): Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg
Powder (Goody's® Extra Strength Headache Powder): Acetaminophen 260 mg, aspirin 520 mg, and caffeine 32.5 mg [contains lactose]
Tablet: Excedrin® Extra Strength, Excedrin® Migraine, Genaced™, Pain-Off: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg Fem-Prin®: Acetaminophen 194.4 mg, aspirin 226.8 mg, and caffeine 32.4 mg Goody's® Extra Strength Pain Relief: Acetaminophen 130 mg, aspirin 260 mg, and caffeine 16.25 mg
DOSAGE FORMS: CONCISE Caplet: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg; acetaminophen 194 mg, aspirin 227 mg, and caffeine 33 mg Excedrin® Extra Strength [OTC], Excedrin® Migraine [OTC]: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg Vanquish® Extra Strength Pain Reliever [OTC]: Acetaminophen 194 mg, aspirin 227 mg, and caffeine 33 mg
Geltab: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg Excedrin® Extra Strength [OTC], Excedrin® Migraine [OTC]: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg
Powder: Acetaminophen 260 mg, aspirin 520 mg, and caffeine 32.5 mg Goody's® Extra Strength Headache Powder [OTC]: Acetaminophen 260 mg, aspirin 520 mg, and caffeine 32.5 mg
Tablet: Excedrin® Extra Strength [OTC], Excedrin® Migraine [OTC], Genaced™ [OTC], Pain-Off [OTC]: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg Fem-Prin® [OTC]: Acetaminophen 194.4 mg, aspirin 226.8 mg, and caffeine 32.4 mg Goody's® Extra Strength Pain Relief [OTC]: Acetaminophen 130 mg, aspirin 260 mg, and caffeine 16.25 mg
GENERIC EQUIVALENT AVAILABLE — Yes
USE — Relief of mild-to-moderate pain; mild-to-moderate pain associated with migraine headache
ADVERSE REACTIONS SIGNIFICANT — See individual agents.
CONTRAINDICATIONS — Hypersensitivity to acetaminophen, aspirin, salicylates, caffeine, or any component of the formulation; pregnancy
DRUG INTERACTIONS Acetaminophen: Substrate (minor) of CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A4; Inhibits CYP3A4 (weak)
Aspirin: Substrate (minor) of CYP2C9
Caffeine: Substrate of CYP1A2 (major), 2C9 (minor), 2D6 (minor), 2E1 (minor), 3A4 (minor); Inhibits CYP1A2 (weak), 3A4 (moderate)
Also see individual agents.
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Excessive intake of ethanol may increase the risk of acetaminophen-induced hepatotoxicity. Avoid ethanol or limit to <3 drinks/day.
PREGNANCY RISK FACTOR — D (show table)
PHARMACODYNAMICS / KINETICS — See individual agents.
PHARMACOLOGIC CATEGORY Analgesic, Miscellaneous
DOSING: ADULTS Pain management: Based on acetaminophen component: Mild-to-moderate pain: Oral: 325-650 mg every 4-6 hours as needed; do not exceed 4 g/day Mild-to-moderate pain associated with migraine headache: Oral: 500 mg/dose (in combination with 500 mg aspirin and 130 mg caffeine) every 6 hours while symptoms persist; do not use for longer than 48 hours Based on aspirin component: Mild-to-moderate pain: Oral: 325-650 mg every 4-6 hours as needed; do not exceed 4 g/day Mild-to-moderate pain associated with migraine headache: Oral: 500 mg/dose (in combination with 500 mg acetaminophen and 130 mg caffeine) every 6 hours; do not use for longer than 48 hours
Product labeling:
Excedrin® Extra Strength, Excedrin® Migraine: Oral: 2 doses every 6 hours (maximum: 8 doses/24 hours) Note: When used for migraine, do not use for longer than 48 hours
Goody's® Extra Strength Headache Powder: Oral: 1 powder, placed on tongue or dissolved in water, every 4-6 hours (maximum: 4 powders/24 hours)
Goody's® Extra Strength Pain Relief Tablets: Oral: 2 tablets every 4-6 hours (maximum: 8 tablets/24 hours)
Vanquish® Extra Strength Pain Reliever: Oral: 2 tablets every 4 hours (maximum: 12 tablets/24 hours)
DOSING: PEDIATRIC Product labeling:
Excedrin® Extra Strength, Excedrin® Migraine: Oral: Children >12 years: Refer to adult dosing
Goody's® Extra Strength Headache Powder: Oral: Children >12 years: Refer to adult dosing
Goody's® Extra Strength Pain Relief Tablets: Oral: Children >12 years: Refer to adult dosing
Vanquish® Extra Strength Pain Reliever: Oral: Children >12 years: Refer to adult dosing
DOSING: ELDERLY — Refer to adult dosing.
DOSING: HEPATIC IMPAIRMENT — Use with caution. Limited, low-dose therapy usually well tolerated in hepatic disease/cirrhosis. However, cases of hepatotoxicity at daily acetaminophen dosages <4 g/day have been reported. Avoid chronic use in hepatic impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Caplet: Excedrin® Extra Strength, Excedrin® Migraine: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg Vanquish® Extra Strength Pain Reliever: Acetaminophen 194 mg, aspirin 227 mg, and caffeine 33 mg
Geltab (Excedrin® Extra Strength, Excedrin® Migraine): Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg
Powder (Goody's® Extra Strength Headache Powder): Acetaminophen 260 mg, aspirin 520 mg, and caffeine 32.5 mg [contains lactose]
Tablet: Excedrin® Extra Strength, Excedrin® Migraine, Genaced™, Pain-Off: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg Fem-Prin®: Acetaminophen 194.4 mg, aspirin 226.8 mg, and caffeine 32.4 mg Goody's® Extra Strength Pain Relief: Acetaminophen 130 mg, aspirin 260 mg, and caffeine 16.25 mg
DOSAGE FORMS: CONCISE Caplet: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg; acetaminophen 194 mg, aspirin 227 mg, and caffeine 33 mg Excedrin® Extra Strength [OTC], Excedrin® Migraine [OTC]: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg Vanquish® Extra Strength Pain Reliever [OTC]: Acetaminophen 194 mg, aspirin 227 mg, and caffeine 33 mg
Geltab: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg Excedrin® Extra Strength [OTC], Excedrin® Migraine [OTC]: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg
Powder: Acetaminophen 260 mg, aspirin 520 mg, and caffeine 32.5 mg Goody's® Extra Strength Headache Powder [OTC]: Acetaminophen 260 mg, aspirin 520 mg, and caffeine 32.5 mg
Tablet: Excedrin® Extra Strength [OTC], Excedrin® Migraine [OTC], Genaced™ [OTC], Pain-Off [OTC]: Acetaminophen 250 mg, aspirin 250 mg, and caffeine 65 mg Fem-Prin® [OTC]: Acetaminophen 194.4 mg, aspirin 226.8 mg, and caffeine 32.4 mg Goody's® Extra Strength Pain Relief [OTC]: Acetaminophen 130 mg, aspirin 260 mg, and caffeine 16.25 mg
GENERIC EQUIVALENT AVAILABLE — Yes
USE — Relief of mild-to-moderate pain; mild-to-moderate pain associated with migraine headache
ADVERSE REACTIONS SIGNIFICANT — See individual agents.
CONTRAINDICATIONS — Hypersensitivity to acetaminophen, aspirin, salicylates, caffeine, or any component of the formulation; pregnancy
DRUG INTERACTIONS Acetaminophen: Substrate (minor) of CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A4; Inhibits CYP3A4 (weak)
Aspirin: Substrate (minor) of CYP2C9
Caffeine: Substrate of CYP1A2 (major), 2C9 (minor), 2D6 (minor), 2E1 (minor), 3A4 (minor); Inhibits CYP1A2 (weak), 3A4 (moderate)
Also see individual agents.
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Excessive intake of ethanol may increase the risk of acetaminophen-induced hepatotoxicity. Avoid ethanol or limit to <3 drinks/day.
PREGNANCY RISK FACTOR — D (show table)
PHARMACODYNAMICS / KINETICS — See individual agents.
Acetaminophen and pseudoephedrine
SPECIAL ALERTS Infant Deaths Associated with Cough and Cold Medications - January 2007
The Centers for Disease Control and Prevention (CDC) has released a report concerning the use of cough and cold medications in children <2 years of age. Products containing nasal decongestants (eg, pseudoephedrine), antihistamines (eg, carbinoxamine), cough suppressants (eg, dextromethorphan), and expectorants are often used in this age group. The CDC notes that during 2004 and 2005, ~ 1519 children <2 years of age were seen in emergency departments for adverse effects, including overdose, associated with these medications.
During this time period, 3 infants <6 months of age died. All 3 had postmortem blood levels of pseudoephedrine, ranging from 4743-7100 ng/mL (therapeutic levels for children 2-12 years: 180-500 ng/mL). In one case, the infant received both a prescription product containing pseudoephedrine and an over-the-counter (OTC) product, also containing pseudoephedrine. Alternatives to nasal decongestants in this age group may be softening nasal secretions with saline drops or a cool-mist humidifier and/or the removal of nasal secretions with the use of rubber suction bulb.
Safety and efficacy for the use of cough and cold products in children <2 years of age is limited. The Food and Drug Administration (FDA) notes that there are no approved OTC uses for these products in children <2 years of age. Clinicians are reminded to ask caregivers about the use of OTC products in order to avoid exposure to multiple medications containing the same ingredient. Caregivers are reminded that OTC cough and cold products should not be used in children <2 years of age except under specific direction by their healthcare provider.
For additional information, refer to the following CDC website: http://www.cdc.gov/mmwr/preview/mmwrhtml/mm5601a1.htm, Centers for Disease Control, "Infant Deaths Associated with Cough and Cold Medications - Two States, 2005,"MMWR Morb Mortal Wkly Rep, 2007, 56(01):1-4.
U.S. BRAND NAMES — Allerest® Allergy and Sinus Relief [OTC]; Genapap™ Sinus Maximum Strength [OTC]; Mapap Sinus Maximum Strength [OTC]; Medi-Synal [OTC]; Oranyl Plus [OTC]; Ornex® Maximum Strength [OTC]; Ornex® [OTC]; Sinus-Relief [OTC] [DSC]; Sudafed® Multi-Symptom Sinus and Cold [OTC]; Tylenol® Cold Daytime, Children's [OTC]; Tylenol® Cold, Infants [OTC]; Tylenol® Sinus Daytime [OTC]
PHARMACOLOGIC CATEGORY Alpha/Beta AgonistAnalgesic, Miscellaneous
DOSING: ADULTS Pain (Analgesic): Oral; Based on acetaminophen component: 325-650 mg every 4-6 hours as needed; do not exceed 4 g/day
Decongestant: Oral: Based on pseudoephedrine component: 60 mg every 4 hours; do not exceed 360 mg/day
Product labeling: Sudafed® Multi-Symptom Sinus and Cold: 2 capsules every 4-6 hours (maximum: 8 capsules/24 hours) Tylenol® Sinus Daytime: 2 caplets or gelcaps every 4-6 hours (maximum: 8 caplets or gelcaps/24 hours)
DOSING: PEDIATRIC Analgesic: Based on acetaminophen component: Oral: Children: 10-15 mg/kg/dose every 4-6 hours as needed; do not exceed 5 doses in 24 hours
Decongestant: Based on pseudoephedrine component: Oral: Children: 2-6 years: 15 mg every 4 hours; do not exceed 90 mg/day 6-12 years: 30 mg every 4 hours; do not exceed 180 mg/day Children >12 years and Adults: Refer to adult dosing.
Product labeling:
Children's Tylenol® Cold Daytime: Children: 2-5 years (24-47 lb): 1 teaspoonful every 4-6 hours (maximum: 4 doses/24 hours) 6-11 years (48-95 lb): 2 teaspoonfuls every 4-6 hours (maximum: 4 doses/24 hours)
Infants' Tylenol® Cold: Children 2-3 years (24-35 lb): 1.6 mL every 4-6 hours (maximum: 4 doses/24 hours)
Sudafed® Multi-Symptom Sinus and Cold, Tylenol® Sinus Daytime: Children 12 years: Refer to adult dosing.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: HEPATIC IMPAIRMENT — Use with caution. Limited, low-dose therapy usually well tolerated in hepatic disease/cirrhosis; however, cases of hepatotoxicity at daily acetaminophen dosages <4 g/day have been reported. Avoid chronic use in hepatic impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Caplet: Allerest® Allergy and Sinus Relief, Ornex®: Acetaminophen 325 mg and pseudoephedrine hydrochloride 30 mg Genapap™ Sinus Maximum Strength, Mapap Sinus Maximum Strength, Ornex® Maximum Strength, Tylenol® Sinus Daytime: Acetaminophen 500 mg and pseudoephedrine hydrochloride 30 mg
Capsule, liquid: Sudafed® Multi-Symptom Sinus and Cold: Acetaminophen 325 mg and pseudoephedrine hydrochloride 30 mg [contains sodium 16 mg]
Gelcap: Tylenol® Sinus Daytime: Acetaminophen 500 mg and pseudoephedrine hydrochloride 30 mg
Liquid: Childrens Tylenol® Cold Daytime: Acetaminophen 160 mg and pseudoephedrine hydrochloride 15 mg per 5 mL (120 mL) [contains sodium benzoate; fruit flavor]
Liquid, oral [drops]: Infants Tylenol® Cold: Acetaminophen 80 mg and pseudoephedrine 7.5 mg per 0.8 mL [contains sodium benzoate; bubble gum flavor]
Tablet: Medi-Synal, Sinus-Relief [DSC]: Acetaminophen 325 mg and pseudoephedrine hydrochloride 30 mg Oranyl Plus: Acetaminophen 500 mg and pseudoephedrine hydrochloride 30 mg
DOSAGE FORMS: CONCISE Caplet: Allerest® Allergy and Sinus Relief, Ornex®: Acetaminophen 325 mg and pseudoephedrine hydrochloride 30 mg Genapap™ Sinus Maximum Strength, Mapap Sinus Maximum Strength, Ornex® Maximum Strength, Tylenol® Sinus Daytime: Acetaminophen 500 mg and pseudoephedrine hydrochloride 30 mg
Capsule, liquid: Sudafed® Multi-Symptom Sinus and Cold: Acetaminophen 325 mg and pseudoephedrine hydrochloride 30 mg
Gelcap: Tylenol® Sinus Daytime: Acetaminophen 500 mg and pseudoephedrine hydrochloride 30 mg
Liquid: Childrens Tylenol® Cold Daytime: Acetaminophen 160 mg and pseudoephedrine hydrochloride 15 mg per 5 mL
Liquid, oral [drops]: Infants Tylenol® Cold: Acetaminophen 80 mg and pseudoephedrine 7.5 mg per 0.8 mL
Tablet: Medi-Synal: Acetaminophen 325 mg and pseudoephedrine hydrochloride 30 mg Oranyl Plus: Acetaminophen 500 mg and pseudoephedrine hydrochloride 30 mg
GENERIC EQUIVALENT AVAILABLE — Yes
USE — Relief of mild-to-moderate pain; relief of congestion
ADVERSE REACTIONS SIGNIFICANT — See individual agents.
DRUG INTERACTIONS — Acetaminophen: Substrate (minor) of CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A4; Inhibits CYP3A4 (weak)
Also see individual agents.
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Excessive intake of ethanol may increase the risk of acetaminophen-induced hepatotoxicity. Avoid ethanol or limit to <3 drinks/day.
DIETARY CONSIDERATIONS Sudafed® Multi-Symptom Sinus and Cold capsule contains acetaminophen 325 mg, pseudoephedrine hydrochloride 30 mg, and sodium 16 mg.
CANADIAN BRAND NAMES — Contac® Cold and Sore Throat, Non Drowsy, Extra Strength; Dristan® N.D., Extra Strength; Dristan® N.D.; Sinutab® Non Drowsy; Sudafed® Head Cold and Sinus Extra Strength; Tylenol® Decongestant; Tylenol® Sinus
INTERNATIONAL BRAND NAMES — Contac Cold and Sore Throat, Non Drowsy, Extra Strength (CA); Dristan N.D. (CA); Dristan N.D., Extra Strength (CA); Sinutab Non Drowsy (CA); Sudafed Head Cold and Sinus Extra Strength (CA); Tylenol Decongestant (CA); Tylenol Sinus (CA)
PHARMACODYNAMICS / KINETICS — See individual agents.
The Centers for Disease Control and Prevention (CDC) has released a report concerning the use of cough and cold medications in children <2 years of age. Products containing nasal decongestants (eg, pseudoephedrine), antihistamines (eg, carbinoxamine), cough suppressants (eg, dextromethorphan), and expectorants are often used in this age group. The CDC notes that during 2004 and 2005, ~ 1519 children <2 years of age were seen in emergency departments for adverse effects, including overdose, associated with these medications.
During this time period, 3 infants <6 months of age died. All 3 had postmortem blood levels of pseudoephedrine, ranging from 4743-7100 ng/mL (therapeutic levels for children 2-12 years: 180-500 ng/mL). In one case, the infant received both a prescription product containing pseudoephedrine and an over-the-counter (OTC) product, also containing pseudoephedrine. Alternatives to nasal decongestants in this age group may be softening nasal secretions with saline drops or a cool-mist humidifier and/or the removal of nasal secretions with the use of rubber suction bulb.
Safety and efficacy for the use of cough and cold products in children <2 years of age is limited. The Food and Drug Administration (FDA) notes that there are no approved OTC uses for these products in children <2 years of age. Clinicians are reminded to ask caregivers about the use of OTC products in order to avoid exposure to multiple medications containing the same ingredient. Caregivers are reminded that OTC cough and cold products should not be used in children <2 years of age except under specific direction by their healthcare provider.
For additional information, refer to the following CDC website: http://www.cdc.gov/mmwr/preview/mmwrhtml/mm5601a1.htm, Centers for Disease Control, "Infant Deaths Associated with Cough and Cold Medications - Two States, 2005,"MMWR Morb Mortal Wkly Rep, 2007, 56(01):1-4.
U.S. BRAND NAMES — Allerest® Allergy and Sinus Relief [OTC]; Genapap™ Sinus Maximum Strength [OTC]; Mapap Sinus Maximum Strength [OTC]; Medi-Synal [OTC]; Oranyl Plus [OTC]; Ornex® Maximum Strength [OTC]; Ornex® [OTC]; Sinus-Relief [OTC] [DSC]; Sudafed® Multi-Symptom Sinus and Cold [OTC]; Tylenol® Cold Daytime, Children's [OTC]; Tylenol® Cold, Infants [OTC]; Tylenol® Sinus Daytime [OTC]
PHARMACOLOGIC CATEGORY Alpha/Beta AgonistAnalgesic, Miscellaneous
DOSING: ADULTS Pain (Analgesic): Oral; Based on acetaminophen component: 325-650 mg every 4-6 hours as needed; do not exceed 4 g/day
Decongestant: Oral: Based on pseudoephedrine component: 60 mg every 4 hours; do not exceed 360 mg/day
Product labeling: Sudafed® Multi-Symptom Sinus and Cold: 2 capsules every 4-6 hours (maximum: 8 capsules/24 hours) Tylenol® Sinus Daytime: 2 caplets or gelcaps every 4-6 hours (maximum: 8 caplets or gelcaps/24 hours)
DOSING: PEDIATRIC Analgesic: Based on acetaminophen component: Oral: Children: 10-15 mg/kg/dose every 4-6 hours as needed; do not exceed 5 doses in 24 hours
Decongestant: Based on pseudoephedrine component: Oral: Children: 2-6 years: 15 mg every 4 hours; do not exceed 90 mg/day 6-12 years: 30 mg every 4 hours; do not exceed 180 mg/day Children >12 years and Adults: Refer to adult dosing.
Product labeling:
Children's Tylenol® Cold Daytime: Children: 2-5 years (24-47 lb): 1 teaspoonful every 4-6 hours (maximum: 4 doses/24 hours) 6-11 years (48-95 lb): 2 teaspoonfuls every 4-6 hours (maximum: 4 doses/24 hours)
Infants' Tylenol® Cold: Children 2-3 years (24-35 lb): 1.6 mL every 4-6 hours (maximum: 4 doses/24 hours)
Sudafed® Multi-Symptom Sinus and Cold, Tylenol® Sinus Daytime: Children 12 years: Refer to adult dosing.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: HEPATIC IMPAIRMENT — Use with caution. Limited, low-dose therapy usually well tolerated in hepatic disease/cirrhosis; however, cases of hepatotoxicity at daily acetaminophen dosages <4 g/day have been reported. Avoid chronic use in hepatic impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Caplet: Allerest® Allergy and Sinus Relief, Ornex®: Acetaminophen 325 mg and pseudoephedrine hydrochloride 30 mg Genapap™ Sinus Maximum Strength, Mapap Sinus Maximum Strength, Ornex® Maximum Strength, Tylenol® Sinus Daytime: Acetaminophen 500 mg and pseudoephedrine hydrochloride 30 mg
Capsule, liquid: Sudafed® Multi-Symptom Sinus and Cold: Acetaminophen 325 mg and pseudoephedrine hydrochloride 30 mg [contains sodium 16 mg]
Gelcap: Tylenol® Sinus Daytime: Acetaminophen 500 mg and pseudoephedrine hydrochloride 30 mg
Liquid: Childrens Tylenol® Cold Daytime: Acetaminophen 160 mg and pseudoephedrine hydrochloride 15 mg per 5 mL (120 mL) [contains sodium benzoate; fruit flavor]
Liquid, oral [drops]: Infants Tylenol® Cold: Acetaminophen 80 mg and pseudoephedrine 7.5 mg per 0.8 mL [contains sodium benzoate; bubble gum flavor]
Tablet: Medi-Synal, Sinus-Relief [DSC]: Acetaminophen 325 mg and pseudoephedrine hydrochloride 30 mg Oranyl Plus: Acetaminophen 500 mg and pseudoephedrine hydrochloride 30 mg
DOSAGE FORMS: CONCISE Caplet: Allerest® Allergy and Sinus Relief, Ornex®: Acetaminophen 325 mg and pseudoephedrine hydrochloride 30 mg Genapap™ Sinus Maximum Strength, Mapap Sinus Maximum Strength, Ornex® Maximum Strength, Tylenol® Sinus Daytime: Acetaminophen 500 mg and pseudoephedrine hydrochloride 30 mg
Capsule, liquid: Sudafed® Multi-Symptom Sinus and Cold: Acetaminophen 325 mg and pseudoephedrine hydrochloride 30 mg
Gelcap: Tylenol® Sinus Daytime: Acetaminophen 500 mg and pseudoephedrine hydrochloride 30 mg
Liquid: Childrens Tylenol® Cold Daytime: Acetaminophen 160 mg and pseudoephedrine hydrochloride 15 mg per 5 mL
Liquid, oral [drops]: Infants Tylenol® Cold: Acetaminophen 80 mg and pseudoephedrine 7.5 mg per 0.8 mL
Tablet: Medi-Synal: Acetaminophen 325 mg and pseudoephedrine hydrochloride 30 mg Oranyl Plus: Acetaminophen 500 mg and pseudoephedrine hydrochloride 30 mg
GENERIC EQUIVALENT AVAILABLE — Yes
USE — Relief of mild-to-moderate pain; relief of congestion
ADVERSE REACTIONS SIGNIFICANT — See individual agents.
DRUG INTERACTIONS — Acetaminophen: Substrate (minor) of CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A4; Inhibits CYP3A4 (weak)
Also see individual agents.
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Excessive intake of ethanol may increase the risk of acetaminophen-induced hepatotoxicity. Avoid ethanol or limit to <3 drinks/day.
DIETARY CONSIDERATIONS Sudafed® Multi-Symptom Sinus and Cold capsule contains acetaminophen 325 mg, pseudoephedrine hydrochloride 30 mg, and sodium 16 mg.
CANADIAN BRAND NAMES — Contac® Cold and Sore Throat, Non Drowsy, Extra Strength; Dristan® N.D., Extra Strength; Dristan® N.D.; Sinutab® Non Drowsy; Sudafed® Head Cold and Sinus Extra Strength; Tylenol® Decongestant; Tylenol® Sinus
INTERNATIONAL BRAND NAMES — Contac Cold and Sore Throat, Non Drowsy, Extra Strength (CA); Dristan N.D. (CA); Dristan N.D., Extra Strength (CA); Sinutab Non Drowsy (CA); Sudafed Head Cold and Sinus Extra Strength (CA); Tylenol Decongestant (CA); Tylenol Sinus (CA)
PHARMACODYNAMICS / KINETICS — See individual agents.
Acetaminophen and phenyltoloxamine
U.S. BRAND NAMES — Aceta-Gesic [OTC]; Alpain; Dologesic®; Flextra 650; Flextra-DS; Genasec™ [OTC]; Hyflex-DS®; Lagesic™; Percogesic® [OTC]; Phenagesic [OTC]; Phenylgesic [OTC]; RhinoFlex 650; RhinoFlex™; Staflex
PHARMACOLOGIC CATEGORY Analgesic, Miscellaneous
DOSING: ADULTS Pain (Analgesic): Oral: Based on acetaminophen component: 325-650 mg every 4-6 hours as needed (maximum: 4 g/day)
Product-specific labeling: Oral: Flextra-650: 1/2-1 tablet every 6 hours (maximum: 4 tablets/day) Flextra-DS, Hyflex-DS®, RhinoFlex™, RhinoFlex™-650:1/2-1 tablet every 4 hours (maximum: 5 tablets/day) Percogesic®: 1-2 tablets every 4 hours (maximum: 8 tablets/24 hours)
DOSING: PEDIATRIC Analgesic: Oral: Based on acetaminophen component: 10-15 mg/kg/dose every 4-6 hours as needed (maximum: 5 doses/24 hours)
Product-specific labeling: Oral: Flextra-650: Children 6 to <12 years: 1/2 tablet every 6 hours (maximum: 2 tablets/day) Children 12 years: Refer to adults dosing. Flextra-DS, Hyflex-DS®, RhinoFlex™, RhinoFlex™-650: Children 6 to <12 years: 1/2 tablet every 4 hours (maximum: 2.5 tablets/day) Children 12 years : Refer to adults dosing. Percogesic®: Children 6-12 years: 1 tablet every 4 hours (maximum: 4 tablets/24 hours)
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT Specific dosing adjustment not available. Monitor renal function with severe impairment.
DOSING: HEPATIC IMPAIRMENT — Use with caution. Limited, low-dose therapy is usually well tolerated in hepatic disease/cirrhosis; however, cases of hepatotoxicity at daily acetaminophen dosages <4 g/day have been reported. Avoid chronic use in hepatic impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Caplet: Alpain: Acetaminophen 500 mg and phenyltoloxamine citrate 60 mg Dologesic®: Acetaminophen 500 mg and phenyltoloxamine citrate 30 mg Staflex: Acetaminophen 500 mg and phenyltoloxamine citrate 55 mg
Caplet, extended release [scored]: Lagesic™: Acetaminphen 600 mg and phenyltoloxamine citrate 66 mg
Capsule: Dologesic®: Acetaminophen 500 mg and phenyltoloxamine citrate 30 mg
Liquid: Dologesic®: Acetaminophen 500 mg and phenyltoloxamine citrate 30 mg per 15 mL (180 mL)
Tablet: Acetaminophen 325 mg and phenyltoloxamine citrate 30 mg Aceta-Gesic, Genasec™, Percogesic®, Phenagesic, Phenylgesic: Acetaminophen 325 mg and phenyltoloxamine citrate 30 mg Flextra-650: Acetaminophen 650 mg and phenyltoloxamine citrate 60 mg Flextra-DS, Hyflex-DS®, RhinoFlex™: Acetaminophen 500 mg and phenyltoloxamine citrate 50 mg RhinoFlex™-650: Acetaminophen 650 mg and phenyltoloxamine citrate 50 mg
DOSAGE FORMS: CONCISE Caplet: Alpain: Acetaminophen 500 mg and phenyltoloxamine citrate 60 mg Dologesic®: Acetaminophen 500 mg and phenyltoloxamine citrate 30 mg Staflex: Acetaminophen 500 mg and phenyltoloxamine citrate 55 mg
Caplet, extended release [scored]: Lagesic™: Acetaminphen 600 mg and phenyltoloxamine citrate 66 mg
Capsule: Dologesic®: Acetaminophen 500 mg and phenyltoloxamine citrate 30 mg
Liquid: Dologesic®: Acetaminophen 500 mg and phenyltoloxamine citrate 30 mg per 15 mg
Tablet: Acetaminophen 325 mg and phenyltoloxamine citrate 30 mg Aceta-Gesic [OTC], Genasec™ [OTC], Percogesic® [OTC], Phenagesic [OTC], Phenylgesic [OTC]: Acetaminophen 325 mg and phenyltoloxamine citrate 30 mg Flextra-650: Acetaminophen 650 mg and phenyltoloxamine citrate 60 mg Flextra-DS, Hyflex-DS®, RhinoFlex™: Acetaminophen 500 mg and phenyltoloxamine citrate 50 mg RhinoFlex™-650: Acetaminophen 650 mg and phenyltoloxamine citrate 50 mg
GENERIC EQUIVALENT AVAILABLE — Yes: Tablet
USE — Relief of mild pain
CONTRAINDICATIONS — Hypersensitivity to acetaminophen, phenyltoloxamine, or any component of the formulation
WARNINGS / PRECAUTIONS Concerns related to adverse effects: CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). Hepatotoxicity: May cause severe hepatic toxicity on acute overdose; in addition, chronic daily dosing in adults has resulted in liver damage in some patients.
Disease-related concerns: Ethanol use: Use with caution in patients with alcoholic liver disease; consuming 3 alcoholic drinks/day may increase the risk of liver damage. G6PD deficiency: Use with caution in patients with known G6PD deficiency. Glaucoma: Use with caution in patients with glaucoma. Hepatic impairment: Use with caution in patients with hepatic impairment. Prostatic hyperplasia/urinary stricture: Use with caution in patients with prostatic hyperplasia and/or urinary stricture. Renal impairment: Use with caution in patients with renal impairment. Respiratory disease: Use with caution in patients with pre-existing respiratory compromise (hypoxia and/or hypercapnia), COPD or other obstructive pulmonary disease, and kyphoscoliosis or other skeletal disorder which may alter respiratory function; critical respiratory depression may occur, even at therapeutic dosages.
Special populations: Pediatrics: Safety and efficacy have not been established in children <6 years of age.
Other warnings/precautions: Dosage limit: Limit acetaminophen dose to <4>3 days or for pain lasting >10 days in adults or >5 days in children.
DRUG INTERACTIONS — Acetaminophen: Substrate (minor) of CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A4; Inhibits CYP3A4 (weak)
Refer to Acetaminophen monograph.
ETHANOL / NUTRITION / HERB INTERACTIONS Ethanol: Excessive intake of ethanol may increase the risk of acetaminophen-induced hepatotoxicity. Avoid ethanol or limit to <3 drinks/day.
Food: Rate of absorption may be decreased when given with food.
PREGNANCY RISK FACTOR — C (show table)
PRICING — (data from drugstore.com)Tablets (Flextra DS) 50-500 mg (30): $22.35
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Refer to Acetaminophen monograph.
MECHANISM OF ACTION — Acetaminophen inhibits the synthesis of prostaglandins in the central nervous system and peripherally blocks pain impulse generation; produces antipyresis from inhibition of hypothalamic heat-regulating center. Phenyltoloxamine is an antihistamine (H1-blocking agent) which acts primarily to inhibit secretions in the nose, mouth, and pharynx, as well as causing CNS depression.
PHARMACOLOGIC CATEGORY Analgesic, Miscellaneous
DOSING: ADULTS Pain (Analgesic): Oral: Based on acetaminophen component: 325-650 mg every 4-6 hours as needed (maximum: 4 g/day)
Product-specific labeling: Oral: Flextra-650: 1/2-1 tablet every 6 hours (maximum: 4 tablets/day) Flextra-DS, Hyflex-DS®, RhinoFlex™, RhinoFlex™-650:1/2-1 tablet every 4 hours (maximum: 5 tablets/day) Percogesic®: 1-2 tablets every 4 hours (maximum: 8 tablets/24 hours)
DOSING: PEDIATRIC Analgesic: Oral: Based on acetaminophen component: 10-15 mg/kg/dose every 4-6 hours as needed (maximum: 5 doses/24 hours)
Product-specific labeling: Oral: Flextra-650: Children 6 to <12 years: 1/2 tablet every 6 hours (maximum: 2 tablets/day) Children 12 years: Refer to adults dosing. Flextra-DS, Hyflex-DS®, RhinoFlex™, RhinoFlex™-650: Children 6 to <12 years: 1/2 tablet every 4 hours (maximum: 2.5 tablets/day) Children 12 years : Refer to adults dosing. Percogesic®: Children 6-12 years: 1 tablet every 4 hours (maximum: 4 tablets/24 hours)
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT Specific dosing adjustment not available. Monitor renal function with severe impairment.
DOSING: HEPATIC IMPAIRMENT — Use with caution. Limited, low-dose therapy is usually well tolerated in hepatic disease/cirrhosis; however, cases of hepatotoxicity at daily acetaminophen dosages <4 g/day have been reported. Avoid chronic use in hepatic impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Caplet: Alpain: Acetaminophen 500 mg and phenyltoloxamine citrate 60 mg Dologesic®: Acetaminophen 500 mg and phenyltoloxamine citrate 30 mg Staflex: Acetaminophen 500 mg and phenyltoloxamine citrate 55 mg
Caplet, extended release [scored]: Lagesic™: Acetaminphen 600 mg and phenyltoloxamine citrate 66 mg
Capsule: Dologesic®: Acetaminophen 500 mg and phenyltoloxamine citrate 30 mg
Liquid: Dologesic®: Acetaminophen 500 mg and phenyltoloxamine citrate 30 mg per 15 mL (180 mL)
Tablet: Acetaminophen 325 mg and phenyltoloxamine citrate 30 mg Aceta-Gesic, Genasec™, Percogesic®, Phenagesic, Phenylgesic: Acetaminophen 325 mg and phenyltoloxamine citrate 30 mg Flextra-650: Acetaminophen 650 mg and phenyltoloxamine citrate 60 mg Flextra-DS, Hyflex-DS®, RhinoFlex™: Acetaminophen 500 mg and phenyltoloxamine citrate 50 mg RhinoFlex™-650: Acetaminophen 650 mg and phenyltoloxamine citrate 50 mg
DOSAGE FORMS: CONCISE Caplet: Alpain: Acetaminophen 500 mg and phenyltoloxamine citrate 60 mg Dologesic®: Acetaminophen 500 mg and phenyltoloxamine citrate 30 mg Staflex: Acetaminophen 500 mg and phenyltoloxamine citrate 55 mg
Caplet, extended release [scored]: Lagesic™: Acetaminphen 600 mg and phenyltoloxamine citrate 66 mg
Capsule: Dologesic®: Acetaminophen 500 mg and phenyltoloxamine citrate 30 mg
Liquid: Dologesic®: Acetaminophen 500 mg and phenyltoloxamine citrate 30 mg per 15 mg
Tablet: Acetaminophen 325 mg and phenyltoloxamine citrate 30 mg Aceta-Gesic [OTC], Genasec™ [OTC], Percogesic® [OTC], Phenagesic [OTC], Phenylgesic [OTC]: Acetaminophen 325 mg and phenyltoloxamine citrate 30 mg Flextra-650: Acetaminophen 650 mg and phenyltoloxamine citrate 60 mg Flextra-DS, Hyflex-DS®, RhinoFlex™: Acetaminophen 500 mg and phenyltoloxamine citrate 50 mg RhinoFlex™-650: Acetaminophen 650 mg and phenyltoloxamine citrate 50 mg
GENERIC EQUIVALENT AVAILABLE — Yes: Tablet
USE — Relief of mild pain
CONTRAINDICATIONS — Hypersensitivity to acetaminophen, phenyltoloxamine, or any component of the formulation
WARNINGS / PRECAUTIONS Concerns related to adverse effects: CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). Hepatotoxicity: May cause severe hepatic toxicity on acute overdose; in addition, chronic daily dosing in adults has resulted in liver damage in some patients.
Disease-related concerns: Ethanol use: Use with caution in patients with alcoholic liver disease; consuming 3 alcoholic drinks/day may increase the risk of liver damage. G6PD deficiency: Use with caution in patients with known G6PD deficiency. Glaucoma: Use with caution in patients with glaucoma. Hepatic impairment: Use with caution in patients with hepatic impairment. Prostatic hyperplasia/urinary stricture: Use with caution in patients with prostatic hyperplasia and/or urinary stricture. Renal impairment: Use with caution in patients with renal impairment. Respiratory disease: Use with caution in patients with pre-existing respiratory compromise (hypoxia and/or hypercapnia), COPD or other obstructive pulmonary disease, and kyphoscoliosis or other skeletal disorder which may alter respiratory function; critical respiratory depression may occur, even at therapeutic dosages.
Special populations: Pediatrics: Safety and efficacy have not been established in children <6 years of age.
Other warnings/precautions: Dosage limit: Limit acetaminophen dose to <4>3 days or for pain lasting >10 days in adults or >5 days in children.
DRUG INTERACTIONS — Acetaminophen: Substrate (minor) of CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A4; Inhibits CYP3A4 (weak)
Refer to Acetaminophen monograph.
ETHANOL / NUTRITION / HERB INTERACTIONS Ethanol: Excessive intake of ethanol may increase the risk of acetaminophen-induced hepatotoxicity. Avoid ethanol or limit to <3 drinks/day.
Food: Rate of absorption may be decreased when given with food.
PREGNANCY RISK FACTOR — C (show table)
PRICING — (data from drugstore.com)Tablets (Flextra DS) 50-500 mg (30): $22.35
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Refer to Acetaminophen monograph.
MECHANISM OF ACTION — Acetaminophen inhibits the synthesis of prostaglandins in the central nervous system and peripherally blocks pain impulse generation; produces antipyresis from inhibition of hypothalamic heat-regulating center. Phenyltoloxamine is an antihistamine (H1-blocking agent) which acts primarily to inhibit secretions in the nose, mouth, and pharynx, as well as causing CNS depression.
Acetaminophen and diphenhydramine
U.S. BRAND NAMES — Excedrin® P.M. [OTC]; Goody's PM® [OTC]; Legatrin PM® [OTC]; Percogesic® Extra Strength [OTC]; Tylenol® PM [OTC]; Tylenol® Severe Allergy [OTC]
PHARMACOLOGIC CATEGORY Analgesic, Miscellaneous
DOSING: ADULTS — Insomnia and pain: Oral: Adults: 50 mg of diphenhydramine HCl (76 mg diphenhydramine citrate) at bedtime or as directed by physician; do not exceed recommended dosage
DOSING: PEDIATRIC — Not for use in children <12 years of age.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: HEPATIC IMPAIRMENT — Use with caution. Limited, low-dose therapy is usually well tolerated in hepatic disease/cirrhosis; however, cases of hepatotoxicity at daily acetaminophen dosages <4 g/day have been reported. Avoid chronic use in hepatic impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Caplet: Acetaminophen 500 mg and diphenhydramine hydrochloride 25 mg Excedrin® P.M.: Acetaminophen 500 mg and diphenhydramine citrate 38 mg Legatrin PM®: Acetaminophen 500 mg and diphenhydramine hydrochloride 50 mg Percogesic® Extra Strength: Acetaminophen 500 mg and diphenhydramine hydrochloride 25 mg Tylenol® PM: Acetaminophen 500 mg and diphenhydramine hydrochloride 25 mg [also available in vanilla caplets] Tylenol® Severe Allergy: Acetaminophen 500 mg and diphenhydramine hydrochloride 12.5 mg
Gelcap: Tylenol® PM: Acetaminophen 500 mg and diphenhydramine hydrochloride 25 mg
Geltab: Acetaminophen 500 mg and diphenhydramine hydrochloride 25 mg Excedrin® P.M.: Acetaminophen 500 mg and diphenhydramine citrate 38 mg Tylenol® PM: Acetaminophen 500 mg and diphenhydramine hydrochloride 25 mg
Liquid: Tylenol® PM: Acetaminophen 500 mg and diphenhydramine hydrochloride 25 mg per 15 mL (240 mL) [contains sodium benzoate; vanilla flavor]
Powder for oral solution: Goody's PM®: Acetaminophen 500 mg and diphenhydramine citrate 38 mg [contains potassium 41.9 mg and sodium 3.15 mg per powder]
Tablet: Acetaminophen 500 mg and diphenhydramine hydrochloride 25 mg Excedrin® P.M.: Acetaminophen 500 mg and diphenhydramine citrate 38 mg
DOSAGE FORMS: CONCISE Caplet: Acetaminophen 500 mg and diphenhydramine 25 mg Excedrin® P.M. [OTC]: Acetaminophen 500 mg and diphenhydramine 38 mg Legatrin PM® [OTC]: Acetaminophen 500 mg and diphenhydramine 50 mg Percogesic® Extra Strength [OTC], Tylenol® PM [OTC]: Acetaminophen 500 mg and diphenhydramine 25 mg Tylenol® Severe Allergy [OTC]: Acetaminophen 500 mg and diphenhydramine 12.5 mg
Gelcap: Tylenol® PM [OTC]: Acetaminophen 500 mg and diphenhydramine 25 mg
Geltab: Acetaminophen 500 mg and diphenhydramine 25 mg Excedrin® P.M. [OTC]: Acetaminophen 500 mg and diphenhydramine 38 mg Tylenol® PM [OTC]: Acetaminophen 500 mg and diphenhydramine 25 mg
Liquid: Tylenol® PM [OTC]: Acetaminophen 500 mg and diphenhydramine 25 mg per 15 mL
Powder for oral solution: Goody's PM® [OTC]: Acetaminophen 500 mg and diphenhydramine 38 mg
Tablet: Acetaminophen 500 mg and diphenhydramine 25 mg Excedrin® P.M. [OTC]: Acetaminophen 500 mg and diphenhydramine 38 mg
GENERIC EQUIVALENT AVAILABLE — Yes: Excludes gelcap, powder, and liquid
USE — Aid in the relief of insomnia accompanied by minor pain
ADVERSE REACTIONS SIGNIFICANT — See individual agents.
DRUG INTERACTIONS Acetaminophen: Substrate (minor) of CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A4; Inhibits CYP3A4 (weak)
Diphenhydramine: Inhibits CYP2D6 (moderate)
Also see individual agents.
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Excessive intake of ethanol may increase the risk of acetaminophen-induced hepatotoxicity. Avoid ethanol or limit to <3 drinks/day.
PHARMACODYNAMICS / KINETICS — See individual agents.
PHARMACOLOGIC CATEGORY Analgesic, Miscellaneous
DOSING: ADULTS — Insomnia and pain: Oral: Adults: 50 mg of diphenhydramine HCl (76 mg diphenhydramine citrate) at bedtime or as directed by physician; do not exceed recommended dosage
DOSING: PEDIATRIC — Not for use in children <12 years of age.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: HEPATIC IMPAIRMENT — Use with caution. Limited, low-dose therapy is usually well tolerated in hepatic disease/cirrhosis; however, cases of hepatotoxicity at daily acetaminophen dosages <4 g/day have been reported. Avoid chronic use in hepatic impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Caplet: Acetaminophen 500 mg and diphenhydramine hydrochloride 25 mg Excedrin® P.M.: Acetaminophen 500 mg and diphenhydramine citrate 38 mg Legatrin PM®: Acetaminophen 500 mg and diphenhydramine hydrochloride 50 mg Percogesic® Extra Strength: Acetaminophen 500 mg and diphenhydramine hydrochloride 25 mg Tylenol® PM: Acetaminophen 500 mg and diphenhydramine hydrochloride 25 mg [also available in vanilla caplets] Tylenol® Severe Allergy: Acetaminophen 500 mg and diphenhydramine hydrochloride 12.5 mg
Gelcap: Tylenol® PM: Acetaminophen 500 mg and diphenhydramine hydrochloride 25 mg
Geltab: Acetaminophen 500 mg and diphenhydramine hydrochloride 25 mg Excedrin® P.M.: Acetaminophen 500 mg and diphenhydramine citrate 38 mg Tylenol® PM: Acetaminophen 500 mg and diphenhydramine hydrochloride 25 mg
Liquid: Tylenol® PM: Acetaminophen 500 mg and diphenhydramine hydrochloride 25 mg per 15 mL (240 mL) [contains sodium benzoate; vanilla flavor]
Powder for oral solution: Goody's PM®: Acetaminophen 500 mg and diphenhydramine citrate 38 mg [contains potassium 41.9 mg and sodium 3.15 mg per powder]
Tablet: Acetaminophen 500 mg and diphenhydramine hydrochloride 25 mg Excedrin® P.M.: Acetaminophen 500 mg and diphenhydramine citrate 38 mg
DOSAGE FORMS: CONCISE Caplet: Acetaminophen 500 mg and diphenhydramine 25 mg Excedrin® P.M. [OTC]: Acetaminophen 500 mg and diphenhydramine 38 mg Legatrin PM® [OTC]: Acetaminophen 500 mg and diphenhydramine 50 mg Percogesic® Extra Strength [OTC], Tylenol® PM [OTC]: Acetaminophen 500 mg and diphenhydramine 25 mg Tylenol® Severe Allergy [OTC]: Acetaminophen 500 mg and diphenhydramine 12.5 mg
Gelcap: Tylenol® PM [OTC]: Acetaminophen 500 mg and diphenhydramine 25 mg
Geltab: Acetaminophen 500 mg and diphenhydramine 25 mg Excedrin® P.M. [OTC]: Acetaminophen 500 mg and diphenhydramine 38 mg Tylenol® PM [OTC]: Acetaminophen 500 mg and diphenhydramine 25 mg
Liquid: Tylenol® PM [OTC]: Acetaminophen 500 mg and diphenhydramine 25 mg per 15 mL
Powder for oral solution: Goody's PM® [OTC]: Acetaminophen 500 mg and diphenhydramine 38 mg
Tablet: Acetaminophen 500 mg and diphenhydramine 25 mg Excedrin® P.M. [OTC]: Acetaminophen 500 mg and diphenhydramine 38 mg
GENERIC EQUIVALENT AVAILABLE — Yes: Excludes gelcap, powder, and liquid
USE — Aid in the relief of insomnia accompanied by minor pain
ADVERSE REACTIONS SIGNIFICANT — See individual agents.
DRUG INTERACTIONS Acetaminophen: Substrate (minor) of CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A4; Inhibits CYP3A4 (weak)
Diphenhydramine: Inhibits CYP2D6 (moderate)
Also see individual agents.
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Excessive intake of ethanol may increase the risk of acetaminophen-induced hepatotoxicity. Avoid ethanol or limit to <3 drinks/day.
PHARMACODYNAMICS / KINETICS — See individual agents.
Acetaminophen and codeine
U.S. BRAND NAMES — Capital® and Codeine; Tylenol® With Codeine
PHARMACOLOGIC CATEGORY Analgesic, Opioid
DOSING: ADULTS — Doses should be adjusted according to severity of pain and response of the patient. Adult doses 60 mg codeine fail to give commensurate relief of pain but merely prolong analgesia and are associated with an appreciably increased incidence of side effects.
Cough (Antitussive): Oral: Based on codeine (15-30 mg/dose) every 4-6 hours (maximum: 360 mg/24 hours based on codeine component)
Pain (Analgesic): Oral: Based on codeine (30-60 mg/dose) every 4-6 hours (maximum: 4000 mg/24 hours based on acetaminophen component) 1-2 tablets every 4 hours to a maximum of 12 tablets/24 hours
DOSING: PEDIATRIC
(For additional information see "Acetaminophen and codeine: Pediatric drug information")Analgesic: Oral: Codeine: 0.5-1 mg codeine/kg/dose every 4-6 hours Acetaminophen: 10-15 mg/kg/dose every 4 hours up to a maximum of 2.6 g/24 hours for children <12>12 years: 15 mL every 4 hours as needed of elixir
DOSING: ELDERLY — Doses should be titrated to appropriate analgesic effect.
1 Tylenol® [#3] or 2 Tylenol® [#2] tablets every 4 hours; do not exceed 4 g/day acetaminophen.
DOSING: RENAL IMPAIRMENT — See individual agents.
DOSING: HEPATIC IMPAIRMENT — Use with caution. Limited, low-dose therapy is usually well tolerated in hepatic disease/cirrhosis; however, cases of hepatotoxicity at daily acetaminophen dosages <4 g/day have been reported. Avoid chronic use in hepatic impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product; [CAN] = Canadian brand name
Caplet: ratio-Lenoltec No. 1 [CAN], Tylenol No. 1 [CAN]: Acetaminophen 300 mg, codeine phosphate 8 mg, and caffeine 15 mg [not available in the U.S.] Tylenol No. 1 Forte [CAN]: Acetaminophen 500 mg, codeine phosphate 8 mg, and caffeine 15 mg [not available in the U.S.]
Elixir, oral [C-V]: Acetaminophen 120 mg and codeine phosphate 12 mg per 5 mL (5 mL, 10 mL, 12.5 mL, 15 mL, 120 mL, 480 mL) [contains alcohol 7%] Tylenol® with Codeine [DSC]: Acetaminophen 120 mg and codeine phosphate 12 mg per 5 mL (480 mL) [contains alcohol 7%; cherry flavor] Tylenol Elixir with Codeine [CAN]: Acetaminophen 160 mg and codeine phosphate 8 mg per 5 mL (500 mL) [contains alcohol 7%, sucrose 31%; cherry flavor; not available in the U.S.]
Suspension, oral [C-V] (Capital® and Codeine): Acetaminophen 120 mg and codeine phosphate 12 mg per 5 mL (480 mL) [alcohol free; fruit punch flavor]
Tablet [C-III]: Acetaminophen 300 mg and codeine phosphate 15 mg; acetaminophen 300 mg and codeine phosphate 30 mg; acetaminophen 300 mg and codeine phosphate 60 mg ratio-Emtec [CAN], Triatec-30 [CAN]: Acetaminophen 300 mg and codeine phosphate 30 mg [not available in the U.S.] ratio-Lenoltec No. 1 [CAN]: Acetaminophen 300 mg, codeine phosphate 8 mg, and caffeine 15 mg [not available in the U.S.] ratio-Lenoltec No. 2 [CAN], Tylenol No. 2 with Codeine [CAN]: Acetaminophen 300 mg, codeine phosphate 15 mg, and caffeine 15 mg [not available in the U.S.] ratio-Lenoltec No. 3 [CAN], Tylenol No. 3 with Codeine [CAN]: Acetaminophen 300 mg, codeine phosphate 30 mg, and caffeine 15 mg [not available in the U.S.] ratio-Lenoltec No. 4 [CAN], Tylenol No. 4 with Codeine [CAN]: Acetaminophen 300 mg and codeine phosphate 60 mg [not available in the U.S.] Triatec-8 [CAN]: Acetaminophen 325 mg, codeine phosphate 8 mg, and caffeine 30 mg [not available in the U.S.] Triatec-8 Strong [CAN]: Acetaminophen 500 mg, codeine phosphate 8 mg, and caffeine 30 mg [not available in the U.S.] Tylenol® with Codeine No. 3: Acetaminophen 300 mg and codeine phosphate 30 mg [contains sodium metabisulfite] Tylenol® with Codeine No. 4: Acetaminophen 300 mg and codeine phosphate 60 mg [contains sodium metabisulfite]
DOSAGE FORMS: CONCISE — [CAN] = Canadian brand name
Caplet: ratio-Lenoltec No. 1 [CAN], Tylenol No. 1 [CAN]: Acetaminophen 300 mg, codeine 8 mg, and caffeine 15 mg [not available in the U.S.] Tylenol No. 1 Forte [CAN]: Acetaminophen 500 mg, codeine 8 mg, and caffeine 15 mg [not available in the U.S.]
Elixir, oral [C-V]: Acetaminophen 120 mg and codeine 12 mg per 5 mL Tylenol Elixir with Codeine [CAN]: Acetaminophen 160 mg and codeine 8 mg per 5 mL [not available in the U.S.]
Suspension, oral [C-V]: Acetaminophen 120 mg and codeine 12 mg per 5 mL Capital® and Codeine [C-V]: Acetaminophen 120 mg and codeine 12 mg per 5 mL
Tablet [C-III]: Acetaminophen 300 mg and codeine 15 mg; acetaminophen 300 mg and codeine 30 mg; acetaminophen 300 mg and codeine 60 mg ratio-Emtec [CAN], Triatec-30 [CAN]: Acetaminophen 300 mg and codeine 30 mg [not available in the U.S.] ratio-Lenoltec No. 1 [CAN]: Acetaminophen 300 mg, codeine 8 mg, and caffeine 15 mg [not available in the U.S.] ratio-Lenoltec No. 2 [CAN], Tylenol No. 2 with Codeine [CAN]: Acetaminophen 300 mg, codeine 15 mg, and caffeine 15 mg [not available in the U.S.] ratio-Lenoltec No. 3 [CAN], Tylenol No. 3 with Codeine [CAN]: Acetaminophen 300 mg, codeine 30 mg, and caffeine 15 mg [not available in the U.S.] ratio-Lenoltec No. 4 [CAN], Tylenol No. 4 with Codeine [CAN]: Acetaminophen 300 mg and codeine 60 mg [not available in the U.S.] Triatec-8 [CAN]: Acetaminophen 325 mg, codeine 8 mg, and caffeine 30 mg [not available in the U.S.] Triatec-8 Strong [CAN]: Acetaminophen 500 mg, codeine 8 mg, and caffeine 30 mg [not available in the U.S.] Tylenol® with Codeine No. 3: Acetaminophen 300 mg and codeine 30 mg Tylenol® with Codeine No. 4: Acetaminophen 300 mg and codeine 60 mg
GENERIC EQUIVALENT AVAILABLE — Yes
USE — Relief of mild-to-moderate pain
ADVERSE REACTIONS SIGNIFICANT >10%: Central nervous system: Lightheadedness, dizziness, sedation Gastrointestinal: Nausea, vomiting Respiratory: Dyspnea
1% to 10%: Central nervous system: Euphoria, dysphoria Dermatologic: Pruritus Gastrointestinal: Constipation, abdominal pain Miscellaneous: Histamine release
<1% (Limited to important or life-threatening): Antidiuretic hormone release, biliary tract spasm, bradycardia, hypotension, intracranial pressure increased, physical and psychological dependence, respiratory depression, urinary retention
CONTRAINDICATIONS — Hypersensitivity to acetaminophen, codeine, or any component of the formulation; significant respiratory depression (in unmonitored settings); acute or severe bronchial asthma; hypercapnia; paralytic ileus
WARNINGS / PRECAUTIONS Concerns related to adverse effects: CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). Hepatotoxicity: May cause severe hepatic toxicity on acute overdose; in addition, chronic daily dosing in adults has resulted in liver damage in some patients. Hypotension: May cause hypotension; use with caution in patients with hypovolemia, cardiovascular disease (including acute MI), or drugs which may exaggerate hypotensive effects (including phenothiazines or general anesthetics). Phenanthrene hypersensitivity: Use with caution in patients with hypersensitivity reactions to other phenanthrene-derivative opioid agonists (hydrocodone, hydromorphone, levorphanol, oxycodone, oxymorphone).
Disease-related concerns: Abdominal conditions: May obscure diagnosis or clinical course of patients with acute abdominal conditions. Adrenal insufficiency: Use with caution in patients with adrenal insufficiency, including Addison's disease. CNS depression/coma: Use with caution in patients with CNS depression or coma. Drug abuse: Use with caution in patients with a history of drug abuse or acute alcoholism; potential for drug dependency exists. Tolerance, psychological and physical dependence may occur with prolonged use. Ethanol use: Use with caution in patients with alcoholic liver disease; consuming 3 alcoholic drinks/day may increase the risk of liver damage. G6PD deficiency: Use with caution in patients with known G6PD deficiency. Head trauma: Use with extreme caution in patients with head injury, intracranial lesions, or elevated intracranial pressure; exaggerated elevation of ICP may occur. Hepatic impairment: Use with caution in patients with severe hepatic impairment. Prostatic hyperplasia/urinary stricture: Use with caution in patients with prostatic hyperplasia and/or urinary stricture. Renal impairment: Use with caution in patients with renal impairment. Respiratory disease: Use with caution in patients with pre-existing respiratory compromise (hypoxia and/or hypercapnia), COPD or other obstructive pulmonary disease, and kyphoscoliosis or other skeletal disorder which may alter respiratory function; critical respiratory depression may occur, even at therapeutic dosages. Seizure disorder: Use with caution in patients with a history of seizure disorder. Thyroid dysfunction: Use with caution in patients with thyroid dysfunction.
Concurrent drug therapy issues: Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.
Special populations: Debilitated patients: Use with caution in debilitated patients; there is a greater potential for critical respiratory depression, even at therapeutic dosages. Elderly: Use with caution in the elderly; may be more sensitive to adverse effects. Decrease initial dose.
Dosage form specific issues: Metabisulfite: Tablets contain metabisulfite which may cause allergic reactions. Non-U.S. formulations: Some non-U.S. formulations (including most Canadian formulations) may contain caffeine as an additional ingredient. Caffeine may cause CNS and cardiovascular stimulation, as well as GI irritation in high doses. Use with caution in patients with a history of peptic ulcer or GERD; avoid in patients with symptomatic cardiac arrhythmias.
Other warnings/precautions: Dosage limit: Limit total acetaminophen dose to <4 g/day. Withdrawal: Concurrent use of agonist/antagonist analgesics may precipitate withdrawal symptoms and/or reduced analgesic efficacy in patients following prolonged therapy with mu opioid agonists. Abrupt discontinuation following prolonged use may also lead to withdrawal symptoms.
RESTRICTIONS — C-III; C-V
Note: In countries outside of the U.S., some formulations of Tylenol® with Codeine (eg, Tylenol® No. 3) include caffeine.
DRUG INTERACTIONS — Acetaminophen: Substrate (minor) of CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A4; Inhibits CYP3A4 (weak)
Increased toxicity: CNS depressants, phenothiazines, tricyclic antidepressants, guanabenz, MAO inhibitors (may also decrease blood pressure); effect of warfarin may be enhanced.
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Excessive intake of ethanol may increase the risk of acetaminophen-induced hepatotoxicity. Avoid ethanol or limit to <3 drinks/day.
PREGNANCY RISK FACTOR — C (show table)
LACTATION — Enters breast milk/use caution
DIETARY CONSIDERATIONS — May be taken with food.
PRICING — (data from drugstore.com)Solution (Acetaminophen-Codeine) 120-12 mg/5 mL (118): $8.99 120-12 mg/5 mL (240): $8.98
Tablets (Acetaminophen-Codeine #2) 300-15 mg (30): $7.99
Tablets (Acetaminophen-Codeine #3) 300-30 mg (30): $7.99
Tablets (Acetaminophen-Codeine #4) 300-60 mg (30): $11.99
Tablets (Tylenol/Codeine #3) 300-30 mg (30): $17.69
Tablets (Tylenol/Codeine #4) 300-60 mg (30): $30.54
MONITORING PARAMETERS — Relief of pain, respiratory and mental status, blood pressure, bowel function
TOXICOLOGY / OVERDOSE COMPREHENSIVE Symptoms include hepatic necrosis, blood dyscrasias, respiratory depression.
Acetylcysteine 140 mg/kg orally (loading) followed by 70 mg/kg every 4 hours for 17 doses; therapy should be initiated based upon laboratory analysis suggesting high probability of hepatotoxic potential.
Naloxone 2 mg I.V. (0.01 mg/kg for children) with repeat administration as necessary up to a total of 10 mg; can also be used to reverse the toxic effects of the opiate.
Activated charcoal is effective at binding certain chemicals, and this is especially true for acetaminophen (use within 2 hours of ingestion).
CANADIAN BRAND NAMES — ratio-Emtec; ratio-Lenoltec; Triatec-30; Triatec-8 Strong; Triatec-8; Tylenol Elixir with Codeine; Tylenol No. 1 Forte; Tylenol No. 1; Tylenol No. 2 with Codeine; Tylenol No. 3 with Codeine; Tylenol No. 4 with Codeine
INTERNATIONAL BRAND NAMES — Algesidal (FR); Algimide (CO); Algimide F (CO); Chemists Own Dolased Day Pain Relief (AU); Claradol Codeine (FR); Co-Cadamol (SG); Cod-Acamol Forte (IL); Codabrol (IL); Codalgin (AU, NZ); Codapane (AU); Codeidol (CO); Codeidol F (CO); Codeipar (CL); Codicet (TH); Codilprane Enfant (FR); Codipar (GB, IE); Coditam (ID); Codoliprane (FR); Codoliprane Enfant (FR); Codral Pain Relief (AU); Dafalgan Codeine (FR); Dolorol Forte (ZA); Dymadon Co (AU, NZ); Dymadon Forte (AU); Efferalgan Codeine (PY); Febricod (AU); Liquigesic Co (AU); Maxadol (ZA); Nasa w/codeine (TH); Paceco (MY, SG); Panadeine (AN, AU, BB, BM, BS, BZ, CZ, GY, HK, HU, JM, MY, NZ, SR, TT); Panadeine Co (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Panadeine Forte (AU); Panadiene (AN, AU, BB, BM, BS, BZ, CZ, GY, HK, HU, JM, JP, MY, NZ, SR, TT); Panado-Co Caplets (ZA); Panadol Ultra (HK); Panamax (AU); Paracodol (ZA); Paradine (MY); Paramax (EE); Parcono (TH); Parcoten (HK); Perdolan codeine (BE); Prodeine Forte (AU); Prodeine-15 (AU); ratio-Emtec (CA); ratio-Lenoltec (CA); Rokamol Plus (IL); Solpadeine (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Solpadol (GB, IE); Triatec-30 (CA); Triatec-8 (CA); Triatec-8 Strong (CA); TWC 30 (IN); Tylenol Elixir with Codeine (CA); Tylenol No. 1 (CA); Tylenol No. 1 Forte (CA); Tylenol No. 2 with Codeine (CA); Tylenol No. 3 with Codeine (CA); Tylenol No. 4 with Codeine (CA); Tylex CD (CR, DO, GT, HN, MX, NI, PA, SV); Winadol Forte (CO); Zapain (GB, IE)
MECHANISM OF ACTION — Inhibits the synthesis of prostaglandins in the central nervous system and peripherally blocks pain impulse generation; produces antipyresis from inhibition of hypothalamic heat-regulating center; binds to opiate receptors in the CNS, causing inhibition of ascending pain pathways, altering the perception of and response to pain; causes cough supression by direct central action in the medulla; produces generalized CNS depression. Caffeine (contained in some non-U.S. formulations) is a CNS stimulant; use with acetaminophen and codeine increases the level of analgesia provided by each agent.
PHARMACODYNAMICS / KINETICS — See individual agents.
PHARMACOLOGIC CATEGORY Analgesic, Opioid
DOSING: ADULTS — Doses should be adjusted according to severity of pain and response of the patient. Adult doses 60 mg codeine fail to give commensurate relief of pain but merely prolong analgesia and are associated with an appreciably increased incidence of side effects.
Cough (Antitussive): Oral: Based on codeine (15-30 mg/dose) every 4-6 hours (maximum: 360 mg/24 hours based on codeine component)
Pain (Analgesic): Oral: Based on codeine (30-60 mg/dose) every 4-6 hours (maximum: 4000 mg/24 hours based on acetaminophen component) 1-2 tablets every 4 hours to a maximum of 12 tablets/24 hours
DOSING: PEDIATRIC
(For additional information see "Acetaminophen and codeine: Pediatric drug information")Analgesic: Oral: Codeine: 0.5-1 mg codeine/kg/dose every 4-6 hours Acetaminophen: 10-15 mg/kg/dose every 4 hours up to a maximum of 2.6 g/24 hours for children <12>12 years: 15 mL every 4 hours as needed of elixir
DOSING: ELDERLY — Doses should be titrated to appropriate analgesic effect.
1 Tylenol® [#3] or 2 Tylenol® [#2] tablets every 4 hours; do not exceed 4 g/day acetaminophen.
DOSING: RENAL IMPAIRMENT — See individual agents.
DOSING: HEPATIC IMPAIRMENT — Use with caution. Limited, low-dose therapy is usually well tolerated in hepatic disease/cirrhosis; however, cases of hepatotoxicity at daily acetaminophen dosages <4 g/day have been reported. Avoid chronic use in hepatic impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product; [CAN] = Canadian brand name
Caplet: ratio-Lenoltec No. 1 [CAN], Tylenol No. 1 [CAN]: Acetaminophen 300 mg, codeine phosphate 8 mg, and caffeine 15 mg [not available in the U.S.] Tylenol No. 1 Forte [CAN]: Acetaminophen 500 mg, codeine phosphate 8 mg, and caffeine 15 mg [not available in the U.S.]
Elixir, oral [C-V]: Acetaminophen 120 mg and codeine phosphate 12 mg per 5 mL (5 mL, 10 mL, 12.5 mL, 15 mL, 120 mL, 480 mL) [contains alcohol 7%] Tylenol® with Codeine [DSC]: Acetaminophen 120 mg and codeine phosphate 12 mg per 5 mL (480 mL) [contains alcohol 7%; cherry flavor] Tylenol Elixir with Codeine [CAN]: Acetaminophen 160 mg and codeine phosphate 8 mg per 5 mL (500 mL) [contains alcohol 7%, sucrose 31%; cherry flavor; not available in the U.S.]
Suspension, oral [C-V] (Capital® and Codeine): Acetaminophen 120 mg and codeine phosphate 12 mg per 5 mL (480 mL) [alcohol free; fruit punch flavor]
Tablet [C-III]: Acetaminophen 300 mg and codeine phosphate 15 mg; acetaminophen 300 mg and codeine phosphate 30 mg; acetaminophen 300 mg and codeine phosphate 60 mg ratio-Emtec [CAN], Triatec-30 [CAN]: Acetaminophen 300 mg and codeine phosphate 30 mg [not available in the U.S.] ratio-Lenoltec No. 1 [CAN]: Acetaminophen 300 mg, codeine phosphate 8 mg, and caffeine 15 mg [not available in the U.S.] ratio-Lenoltec No. 2 [CAN], Tylenol No. 2 with Codeine [CAN]: Acetaminophen 300 mg, codeine phosphate 15 mg, and caffeine 15 mg [not available in the U.S.] ratio-Lenoltec No. 3 [CAN], Tylenol No. 3 with Codeine [CAN]: Acetaminophen 300 mg, codeine phosphate 30 mg, and caffeine 15 mg [not available in the U.S.] ratio-Lenoltec No. 4 [CAN], Tylenol No. 4 with Codeine [CAN]: Acetaminophen 300 mg and codeine phosphate 60 mg [not available in the U.S.] Triatec-8 [CAN]: Acetaminophen 325 mg, codeine phosphate 8 mg, and caffeine 30 mg [not available in the U.S.] Triatec-8 Strong [CAN]: Acetaminophen 500 mg, codeine phosphate 8 mg, and caffeine 30 mg [not available in the U.S.] Tylenol® with Codeine No. 3: Acetaminophen 300 mg and codeine phosphate 30 mg [contains sodium metabisulfite] Tylenol® with Codeine No. 4: Acetaminophen 300 mg and codeine phosphate 60 mg [contains sodium metabisulfite]
DOSAGE FORMS: CONCISE — [CAN] = Canadian brand name
Caplet: ratio-Lenoltec No. 1 [CAN], Tylenol No. 1 [CAN]: Acetaminophen 300 mg, codeine 8 mg, and caffeine 15 mg [not available in the U.S.] Tylenol No. 1 Forte [CAN]: Acetaminophen 500 mg, codeine 8 mg, and caffeine 15 mg [not available in the U.S.]
Elixir, oral [C-V]: Acetaminophen 120 mg and codeine 12 mg per 5 mL Tylenol Elixir with Codeine [CAN]: Acetaminophen 160 mg and codeine 8 mg per 5 mL [not available in the U.S.]
Suspension, oral [C-V]: Acetaminophen 120 mg and codeine 12 mg per 5 mL Capital® and Codeine [C-V]: Acetaminophen 120 mg and codeine 12 mg per 5 mL
Tablet [C-III]: Acetaminophen 300 mg and codeine 15 mg; acetaminophen 300 mg and codeine 30 mg; acetaminophen 300 mg and codeine 60 mg ratio-Emtec [CAN], Triatec-30 [CAN]: Acetaminophen 300 mg and codeine 30 mg [not available in the U.S.] ratio-Lenoltec No. 1 [CAN]: Acetaminophen 300 mg, codeine 8 mg, and caffeine 15 mg [not available in the U.S.] ratio-Lenoltec No. 2 [CAN], Tylenol No. 2 with Codeine [CAN]: Acetaminophen 300 mg, codeine 15 mg, and caffeine 15 mg [not available in the U.S.] ratio-Lenoltec No. 3 [CAN], Tylenol No. 3 with Codeine [CAN]: Acetaminophen 300 mg, codeine 30 mg, and caffeine 15 mg [not available in the U.S.] ratio-Lenoltec No. 4 [CAN], Tylenol No. 4 with Codeine [CAN]: Acetaminophen 300 mg and codeine 60 mg [not available in the U.S.] Triatec-8 [CAN]: Acetaminophen 325 mg, codeine 8 mg, and caffeine 30 mg [not available in the U.S.] Triatec-8 Strong [CAN]: Acetaminophen 500 mg, codeine 8 mg, and caffeine 30 mg [not available in the U.S.] Tylenol® with Codeine No. 3: Acetaminophen 300 mg and codeine 30 mg Tylenol® with Codeine No. 4: Acetaminophen 300 mg and codeine 60 mg
GENERIC EQUIVALENT AVAILABLE — Yes
USE — Relief of mild-to-moderate pain
ADVERSE REACTIONS SIGNIFICANT >10%: Central nervous system: Lightheadedness, dizziness, sedation Gastrointestinal: Nausea, vomiting Respiratory: Dyspnea
1% to 10%: Central nervous system: Euphoria, dysphoria Dermatologic: Pruritus Gastrointestinal: Constipation, abdominal pain Miscellaneous: Histamine release
<1% (Limited to important or life-threatening): Antidiuretic hormone release, biliary tract spasm, bradycardia, hypotension, intracranial pressure increased, physical and psychological dependence, respiratory depression, urinary retention
CONTRAINDICATIONS — Hypersensitivity to acetaminophen, codeine, or any component of the formulation; significant respiratory depression (in unmonitored settings); acute or severe bronchial asthma; hypercapnia; paralytic ileus
WARNINGS / PRECAUTIONS Concerns related to adverse effects: CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). Hepatotoxicity: May cause severe hepatic toxicity on acute overdose; in addition, chronic daily dosing in adults has resulted in liver damage in some patients. Hypotension: May cause hypotension; use with caution in patients with hypovolemia, cardiovascular disease (including acute MI), or drugs which may exaggerate hypotensive effects (including phenothiazines or general anesthetics). Phenanthrene hypersensitivity: Use with caution in patients with hypersensitivity reactions to other phenanthrene-derivative opioid agonists (hydrocodone, hydromorphone, levorphanol, oxycodone, oxymorphone).
Disease-related concerns: Abdominal conditions: May obscure diagnosis or clinical course of patients with acute abdominal conditions. Adrenal insufficiency: Use with caution in patients with adrenal insufficiency, including Addison's disease. CNS depression/coma: Use with caution in patients with CNS depression or coma. Drug abuse: Use with caution in patients with a history of drug abuse or acute alcoholism; potential for drug dependency exists. Tolerance, psychological and physical dependence may occur with prolonged use. Ethanol use: Use with caution in patients with alcoholic liver disease; consuming 3 alcoholic drinks/day may increase the risk of liver damage. G6PD deficiency: Use with caution in patients with known G6PD deficiency. Head trauma: Use with extreme caution in patients with head injury, intracranial lesions, or elevated intracranial pressure; exaggerated elevation of ICP may occur. Hepatic impairment: Use with caution in patients with severe hepatic impairment. Prostatic hyperplasia/urinary stricture: Use with caution in patients with prostatic hyperplasia and/or urinary stricture. Renal impairment: Use with caution in patients with renal impairment. Respiratory disease: Use with caution in patients with pre-existing respiratory compromise (hypoxia and/or hypercapnia), COPD or other obstructive pulmonary disease, and kyphoscoliosis or other skeletal disorder which may alter respiratory function; critical respiratory depression may occur, even at therapeutic dosages. Seizure disorder: Use with caution in patients with a history of seizure disorder. Thyroid dysfunction: Use with caution in patients with thyroid dysfunction.
Concurrent drug therapy issues: Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.
Special populations: Debilitated patients: Use with caution in debilitated patients; there is a greater potential for critical respiratory depression, even at therapeutic dosages. Elderly: Use with caution in the elderly; may be more sensitive to adverse effects. Decrease initial dose.
Dosage form specific issues: Metabisulfite: Tablets contain metabisulfite which may cause allergic reactions. Non-U.S. formulations: Some non-U.S. formulations (including most Canadian formulations) may contain caffeine as an additional ingredient. Caffeine may cause CNS and cardiovascular stimulation, as well as GI irritation in high doses. Use with caution in patients with a history of peptic ulcer or GERD; avoid in patients with symptomatic cardiac arrhythmias.
Other warnings/precautions: Dosage limit: Limit total acetaminophen dose to <4 g/day. Withdrawal: Concurrent use of agonist/antagonist analgesics may precipitate withdrawal symptoms and/or reduced analgesic efficacy in patients following prolonged therapy with mu opioid agonists. Abrupt discontinuation following prolonged use may also lead to withdrawal symptoms.
RESTRICTIONS — C-III; C-V
Note: In countries outside of the U.S., some formulations of Tylenol® with Codeine (eg, Tylenol® No. 3) include caffeine.
DRUG INTERACTIONS — Acetaminophen: Substrate (minor) of CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A4; Inhibits CYP3A4 (weak)
Increased toxicity: CNS depressants, phenothiazines, tricyclic antidepressants, guanabenz, MAO inhibitors (may also decrease blood pressure); effect of warfarin may be enhanced.
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Excessive intake of ethanol may increase the risk of acetaminophen-induced hepatotoxicity. Avoid ethanol or limit to <3 drinks/day.
PREGNANCY RISK FACTOR — C (show table)
LACTATION — Enters breast milk/use caution
DIETARY CONSIDERATIONS — May be taken with food.
PRICING — (data from drugstore.com)Solution (Acetaminophen-Codeine) 120-12 mg/5 mL (118): $8.99 120-12 mg/5 mL (240): $8.98
Tablets (Acetaminophen-Codeine #2) 300-15 mg (30): $7.99
Tablets (Acetaminophen-Codeine #3) 300-30 mg (30): $7.99
Tablets (Acetaminophen-Codeine #4) 300-60 mg (30): $11.99
Tablets (Tylenol/Codeine #3) 300-30 mg (30): $17.69
Tablets (Tylenol/Codeine #4) 300-60 mg (30): $30.54
MONITORING PARAMETERS — Relief of pain, respiratory and mental status, blood pressure, bowel function
TOXICOLOGY / OVERDOSE COMPREHENSIVE Symptoms include hepatic necrosis, blood dyscrasias, respiratory depression.
Acetylcysteine 140 mg/kg orally (loading) followed by 70 mg/kg every 4 hours for 17 doses; therapy should be initiated based upon laboratory analysis suggesting high probability of hepatotoxic potential.
Naloxone 2 mg I.V. (0.01 mg/kg for children) with repeat administration as necessary up to a total of 10 mg; can also be used to reverse the toxic effects of the opiate.
Activated charcoal is effective at binding certain chemicals, and this is especially true for acetaminophen (use within 2 hours of ingestion).
CANADIAN BRAND NAMES — ratio-Emtec; ratio-Lenoltec; Triatec-30; Triatec-8 Strong; Triatec-8; Tylenol Elixir with Codeine; Tylenol No. 1 Forte; Tylenol No. 1; Tylenol No. 2 with Codeine; Tylenol No. 3 with Codeine; Tylenol No. 4 with Codeine
INTERNATIONAL BRAND NAMES — Algesidal (FR); Algimide (CO); Algimide F (CO); Chemists Own Dolased Day Pain Relief (AU); Claradol Codeine (FR); Co-Cadamol (SG); Cod-Acamol Forte (IL); Codabrol (IL); Codalgin (AU, NZ); Codapane (AU); Codeidol (CO); Codeidol F (CO); Codeipar (CL); Codicet (TH); Codilprane Enfant (FR); Codipar (GB, IE); Coditam (ID); Codoliprane (FR); Codoliprane Enfant (FR); Codral Pain Relief (AU); Dafalgan Codeine (FR); Dolorol Forte (ZA); Dymadon Co (AU, NZ); Dymadon Forte (AU); Efferalgan Codeine (PY); Febricod (AU); Liquigesic Co (AU); Maxadol (ZA); Nasa w/codeine (TH); Paceco (MY, SG); Panadeine (AN, AU, BB, BM, BS, BZ, CZ, GY, HK, HU, JM, MY, NZ, SR, TT); Panadeine Co (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Panadeine Forte (AU); Panadiene (AN, AU, BB, BM, BS, BZ, CZ, GY, HK, HU, JM, JP, MY, NZ, SR, TT); Panado-Co Caplets (ZA); Panadol Ultra (HK); Panamax (AU); Paracodol (ZA); Paradine (MY); Paramax (EE); Parcono (TH); Parcoten (HK); Perdolan codeine (BE); Prodeine Forte (AU); Prodeine-15 (AU); ratio-Emtec (CA); ratio-Lenoltec (CA); Rokamol Plus (IL); Solpadeine (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Solpadol (GB, IE); Triatec-30 (CA); Triatec-8 (CA); Triatec-8 Strong (CA); TWC 30 (IN); Tylenol Elixir with Codeine (CA); Tylenol No. 1 (CA); Tylenol No. 1 Forte (CA); Tylenol No. 2 with Codeine (CA); Tylenol No. 3 with Codeine (CA); Tylenol No. 4 with Codeine (CA); Tylex CD (CR, DO, GT, HN, MX, NI, PA, SV); Winadol Forte (CO); Zapain (GB, IE)
MECHANISM OF ACTION — Inhibits the synthesis of prostaglandins in the central nervous system and peripherally blocks pain impulse generation; produces antipyresis from inhibition of hypothalamic heat-regulating center; binds to opiate receptors in the CNS, causing inhibition of ascending pain pathways, altering the perception of and response to pain; causes cough supression by direct central action in the medulla; produces generalized CNS depression. Caffeine (contained in some non-U.S. formulations) is a CNS stimulant; use with acetaminophen and codeine increases the level of analgesia provided by each agent.
PHARMACODYNAMICS / KINETICS — See individual agents.
Acetaminophen
(For additional information see "Acetaminophen: Patient drug information" and see "Acetaminophen: Pediatric drug information")
U.S. BRAND NAMES — Acephen™ [OTC]; Apra Children's [OTC]; Aspirin Free Anacin® Maximum Strength [OTC]; Cetafen Extra® [OTC]; Cetafen® [OTC]; Comtrex® Sore Throat Maximum Strength [OTC]; FeverALL® [OTC]; Genapap™ Children [OTC]; Genapap™ Extra Strength [OTC]; Genapap™ Infant [OTC]; Genapap™ [OTC]; Genebs Extra Strength [OTC]; Genebs [OTC]; Infantaire [OTC]; Mapap Children's [OTC]; Mapap Extra Strength [OTC]; Mapap Infants [OTC]; Mapap [OTC]; Nortemp Children's [OTC]; Pain Eze [OTC]; Silapap® Children's [OTC]; Silapap® Infants [OTC]; Tycolene Maximum Strength [OTC]; Tycolene [OTC]; Tylenol® 8 Hour [OTC]; Tylenol® Arthritis Pain [OTC]; Tylenol® Children's with Flavor Creator [OTC]; Tylenol® Children's [OTC]; Tylenol® Extra Strength [OTC]; Tylenol® Infants [OTC]; Tylenol® Junior [OTC]; Tylenol® [OTC]; Valorin Extra [OTC]; Valorin [OTC]
PHARMACOLOGIC CATEGORY Analgesic, Miscellaneous
DOSING: ADULTS — Pain or fever: Oral, rectal: 325-650 mg every 4-6 hours or 1000 mg 3-4 times/day; do not exceed 4 g/day.
DOSING: PEDIATRIC — Pain or fever: Oral, rectal: Children <12 years: 10-15 mg/kg/dose every 4-6 hours as needed; do not exceed 5 doses (2.6 g) in 24 hours; alternatively, the following doses may be used; see table.
(For additional information see "Acetaminophen: Pediatric drug information")
Acetaminophen Dosing 0-3 months: 40 mg 4-11 months: 80 mg 1-2 years: 120 mg 2-3 years: 160 mg 4-5 years: 240 mg 6-8 years: 320 mg 9-10 years: 400 mg 11 years: 480 mg
Note: Higher rectal doses have been studied for use in preoperative pain control in children. However, specific guidelines are not available and dosing may be product dependent. The safety and efficacy of alternating acetaminophen and ibuprofen dosing has not been established.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT Clcr 10-50 mL/minute: Administer every 6 hours.
Clcr <10 mL/minute: Administer every 8 hours (metabolites accumulate).
Moderately dialyzable (20% to 50%)
DOSING: HEPATIC IMPAIRMENT — Use with caution. Limited, low-dose therapy is usually well tolerated in hepatic disease/cirrhosis. However, cases of hepatotoxicity at daily acetaminophen dosages <4 g/day have been reported. Avoid chronic use in hepatic impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Caplet: 500 mg Cetafen Extra® Strength, Genapap™ Extra Strength, Genebs Extra Strength, Mapap Extra Strength, Tycolene Maximum Strength, Tylenol® Extra Strength: 500 mg
Caplet, extended release: Tylenol® 8 Hour, Tylenol® Arthritis Pain: 650 mg
Capsule: 500 mg
Elixir: 160 mg/5 mL (120 mL, 480 mL, 3780 mL) Apra Children's: 160 mg/5 mL (120 mL, 480 mL, 3780 mL) [alcohol free; contains benzoic acid; cherry and grape flavors] Mapap Children's: 160 mg/5 mL (120 mL) [alcohol free; contains benzoic acid and sodium benzoate; cherry flavor]
Gelcap: Mapap Extra Strength, Tylenol® Extra Strength: 500 mg
Geltab: Tylenol® Extra Strength: 500 mg
Geltab, extended release: Tylenol® 8 Hour: 650 mg [DSC]
Liquid, oral: 500 mg/15 mL (240 mL) Comtrex® Sore Throat Maximum Strength: 500 mg/15 mL (240 mL) [contains sodium benzoate; honey lemon flavor] Genapap™ Children: 160 mg/5 mL (120 mL) [contains sodium benzoate; cherry and grape flavors] Silapap®: 160 mg/5 mL (120 mL, 240 mL, 480 mL) [sugar free; contains sodium benzoate; cherry flavor] Tylenol® Extra Strength: 500 mg/15 mL (240 mL) [contains sodium benzoate; cherry flavor]
Solution, oral: 160 mg/5 mL (120 mL, 480 mL)
Solution, oral [drops]: 80 mg/0.8 mL (15 mL) [droppers are marked at 0.4 mL (40 mg) and at 0.8 mL (80 mg)] Genapap™ Infant: 80 mg/0.8 mL (15 mL) [fruit flavor] Infantaire: 80 mg/0.8mL (15 mL, 30 mL) Silapap® Infant's: 80 mg/0.8 mL (15 mL, 30 mL) [contains sodium benzoate; cherry flavor]
Suppository, rectal: 120 mg, 325 mg, 650 mg Acephen™: 120 mg, 325 mg, 650 mg FeverALL®: 80 mg, 120 mg, 325 mg, 650 mg Mapap: 125 mg, 650 mg
Suspension, oral: Mapap Children's: 160 mg/5 mL (120 mL) [contains sodium benzoate; cherry flavor] Nortemp Children's: 160 mg/5 mL (120 mL) [alcohol free; contains sodium benzoate; cotton candy flavor] Tylenol® Children's: 160 mg/5 mL (120 mL, 240 mL) [contains sodium benzoate; bubble gum yum, cherry blast, dye free cherry, grape splash, and very berry strawberry flavors] Tylenol® Children's with Flavor Creator: 160 mg/5 mL (120 mL) [contains sodium 2 mg/5 mL and sodium benzoate; cherry blast flavor; packaged with apple (4), bubblegum (8), chocolate (4), & strawberry (4) sugar free flavor packets]
Suspension, oral [drops]: Mapap Infants: 80 mg/0.8 mL (15 mL, 30 mL) [contains sodium benzoate; cherry flavor] Tylenol® Infants: 80 mg/0.8 mL (15 mL, 30 mL) [contains sodium benzoate; cherry, dye free cherry, and grape flavors]
Tablet: 325 mg, 500 mg Aspirin Free Anacin® Extra Strength, Genapap™ Extra Strength, Genebs Extra Strength, Mapap Extra Strength, Pain Eze, Tylenol® Extra Strength, Valorin Extra: 500 mg Cetafen®, Genapap™, Genebs, Mapap, Tycolene, Tylenol®, Valorin: 325 mg
Tablet, chewable: 80 mg Genapap™ Children: 80 mg [contains phenylalanine 6 mg/tablet; fruit and grape flavors] Mapap Children's: 80 mg [contains phenylalanine 3 mg/tablet; bubble gum, fruit, and grape flavors] Mapap Junior Strength: 160 mg [contains phenylalanine 12 mg/tablet; grape flavor]
Tablet, orally disintegrating: 80 mg, 160 mg Tylenol® Children's Meltaways: 80 mg [bubble gum, grape, and watermelon flavors] Tylenol® Junior Meltaways: 160 mg [bubble gum and grape flavors]
DOSAGE FORMS: CONCISE Caplet: 500 mg Cetafen Extra® Strength [OTC], Genapap™ Extra Strength [OTC], Genebs Extra Strength [OTC], Mapap Extra Strength [OTC], Tycolene Maximum Strength [OTC], Tylenol® Extra Strength [OTC]: 500 mg
Caplet, extended release: Tylenol® 8 Hour [OTC], Tylenol® Arthritis Pain [OTC]: 650 mg
Capsule: 500 mg
Elixir: 160 mg/5 mL Apra Children's [OTC]: 160 mg/5 mL Mapap Children's [OTC]: 160 mg/5 mL
Gelcap: 500 mg Mapap Extra Strength [OTC], Tylenol® Extra Strength [OTC]: 500 mg
Geltab: 500 mg Tylenol® Extra Strength [OTC]: 500 mg
Liquid, oral: 500 mg/15 mL Comtrex® Sore Throat Maximum Strength [OTC], Tylenol® Extra Strength [OTC]: 500 mg/15 mL Genapap™ Children [OTC], Silapap® [OTC]: 160 mg/5 mL
Solution, oral: 160 mg/5 mL
Solution, oral [drops]: 80 mg/0.8 mL Genapap™ Infant [OTC], Infantaire [OTC], Silapap® Infant's [OTC]: 80 mg/0.8 mL
Suppository, rectal: 120 mg, 325 mg, 650 mg Acephen® [OTC]: 120 mg, 325 mg, 650 mg FeverALL® [OTC]: 80 mg, 120 mg, 325 mg, 650 mg Mapap [OTC]: 125 mg, 650 mg
Suspension, oral: 160 mg/5 mL Mapap Children's [OTC], Nortemp Children's [OTC], Tylenol® Children's [OTC], Tylenol® Children's with Flavor Creator [OTC]: 160 mg/5 mL
Suspension, oral [drops]: 80 mg/0.8 mL Mapap Infants [OTC], Tylenol® Infants [OTC]: 80 mg/0.8 mL
Tablet: 325 mg, 500 mg Aspirin Free Anacin® Extra Strength [OTC], Genapap™ Extra Strength [OTC], Genebs Extra Strength [OTC], Mapap Extra Strength [OTC], Redutemp® [OTC], Tylenol® Extra Strength [OTC], Valorin Extra [OTC]: 500 mg Cetafen® [OTC], Genapap™ [OTC], Genebs [OTC], Mapap [OTC], Tylenol® [OTC], Valorin [OTC]: 325 mg
Tablet, chewable: 80 mg Genapap™ Children [OTC], Mapap Children's [OTC]: 80 mg Mapap Junior Strength [OTC]: 160 mg
Tablet, orally disintegrating: 80 mg, 160 mg Tylenol® Children's Meltaways [OTC]: 80 mg Tylenol® Junior Meltaways [OTC]: 160 mg
GENERIC EQUIVALENT AVAILABLE — Yes: Excludes extended release products
ADMINISTRATION Suppositories: Do not freeze.
Suspension, oral: Shake well before pouring a dose.
USE — Treatment of mild-to-moderate pain and fever (antipyretic/analgesic); does not have antirheumatic or anti-inflammatory effects
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Dermatologic: Rash
Endocrine & metabolic: May increase chloride, uric acid, glucose; may decrease sodium, bicarbonate, calcium
Hematologic: Anemia, blood dyscrasias (neutropenia, pancytopenia, leukopenia)
Hepatic: Bilirubin increased, alkaline phosphatase increased
Renal: Ammonia increased, nephrotoxicity with chronic overdose, analgesic nephropathy
Miscellaneous: Hypersensitivity reactions (rare)
CONTRAINDICATIONS — Hypersensitivity to acetaminophen or any component of the formulation
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Hepatotoxicity: May cause severe hepatic toxicity on acute overdose; in addition, chronic daily dosing in adults has resulted in liver damage in some patients.
Disease-related concerns: Ethanol use: Use with caution in patients with alcoholic liver disease; consuming 3 alcoholic drinks/day may increase the risk of liver damage. G6PD deficiency: Use with caution in patients with known G6PD deficiency.
Other warnings/precautions: Dosage limit: Limit dose to <4>3 days or for pain lasting >10 days in adults or >5 days in children.
DRUG INTERACTIONS — Substrate (minor) of CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A4; Inhibits CYP3A4 (weak)
Decreased effect: Barbiturates, carbamazepine, hydantoins, rifampin, sulfinpyrazone may decrease the analgesic effect of acetaminophen. Cholestyramine may decrease acetaminophen absorption (separate dosing by at least 1 hour).
Increased toxicity: Barbiturates, carbamazepine, hydantoins, isoniazid, rifampin, sulfinpyrazone may increase the hepatotoxic potential of acetaminophen. Chronic ethanol abuse increases risk for acetaminophen toxicity; effect of warfarin may be enhanced.
ETHANOL / NUTRITION / HERB INTERACTIONS Ethanol: Excessive intake of ethanol may increase the risk of acetaminophen-induced hepatotoxicity. Avoid ethanol or limit to <3 drinks/day.
Food: Rate of absorption may be decreased when given with food.
Herb/Nutraceutical: St John's wort may decrease acetaminophen levels.
PREGNANCY RISK FACTOR — B (show table)
LACTATION — Enters breast milk/compatible
DIETARY CONSIDERATIONS — Chewable tablets may contain phenylalanine (amount varies, ranges between 3-12 mg/tablet); consult individual product labeling.
PRICING — (data from drugstore.com)Tablets (Tylenol) 325 mg (30): $7.99 500 mg (30): $7.99
MONITORING PARAMETERS — Relief of pain or fever
REFERENCE RANGE Therapeutic concentration (analgesic/antipyretic): 10-30 mcg/mL
Toxic concentration (acute ingestion) with probable hepatotoxicity: >200 mcg/mL at 4 hours or 50 mcg/mL at 12 hours after ingestion
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include hepatic necrosis, transient azotemia, renal tubular necrosis with acute toxicity, anemia, and GI disturbances with chronic toxicity. Acetylcysteine 140 mg/kg orally (loading) followed by 70 mg/kg every 4 hours for 17 doses. Therapy should be initiated based upon laboratory analysis suggesting high probability of hepatotoxic potential. Activated charcoal is very effective at binding acetaminophen.
CANADIAN BRAND NAMES — Abenol®; Apo-Acetaminophen®; Atasol®; Novo-Gesic; Pediatrix; Tempra®; Tylenol®
INTERNATIONAL BRAND NAMES — A-Mol (TH); Abenol (CA); Acamol (CL, IL); Acamoli Baby (IL); Acamoli Forte suppositories for Kids (IL); Acenol (PL); Acet (MY, PH); ACET suppositories (SG); Acetalgin (CH); Acetamol (IT); Adorem (CO); Afebrin (HK, ID); Alvedon (SE); Amol (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Anadin (PL); Anadin dla dzieci (PL); Analgiser (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Antidol (PL); APAP (PL); Apo-Acetaminophen (CA); Arfen (BF, BJ, CI, ET, GH, GM, GN, KE, LR, MA, ML, MR, MU, MW, MY, NE, NG, SC, SD, SL, SN, TZ, UG, ZM, ZW); Atamel (PE); Atasol (CA); Ben-U-Ron (PT); Benuron (JP, PL); Biogesic (ID, PH, TH); Biogesic Suspension (HK); Bodrex (ID); Calapol (ID); Calodol (PH); Calpol (AE, AN, BB, BF, BH, BJ, BM, BS, BZ, CI, CY, EG, ET, GH, GM, GN, GY, IE, IN, IQ, IR, JM, JO, JP, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, NE, NG, OM, PL, QA, SA, SC, SD, SL, SN, SR, SY, TH, TT, TZ, UG, YE, ZM, ZW); Causalon (AR); Cemol (TH); Christamol (HK); Claradol (MA); Codipar (PL); Crocin (IN); Dafalgan (PL); Daga (TH); Denamol (TH); Dirox (AR); Dismifen (MX); Dolex (UY); Doliprane (FR, MA, PL); Dolitabs (FR); Dolofen (CO); Dolomol (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Dolorol (ZA); Dolotemp (MX); Dymadon (AU); Efferalgan (PL); Efferalgan 500 (CR, DO, EE, GT, HN, NI, PA, SV); Efferalganodis (FR); Eraldor (EC); Etoran (PL); Europain (HK); Expandol (FR); Febridol (AU); Fepril (MY); Fervex (BR); Fortolin (CN); Gelocatil (ES); Geluprane 500 (FR); Grippostad (PL); Gunaceta (ID); Itamol (ID); Itamol Forte (ID); Kamolas (ID); Kyofen (CO); Lekadol (HR, PL); Lemgrip (BE); Lexalgin (PH); Lotemp (TH); Lupocet (HR); Maganol (ID); Malidens (IN); Mebinol (PE); Medgenol (PH); Metagesic (PH); Mexalen (AT, CZ, HU); Milidon 500 (SG); Minopan (KR); Mypara (TH); Nalgesik (ID); Napamol (ZA); Naprex (ID); NEBS (JP); Nektol 500 (PH); Nilapur (ID); Novo-Gesic (CA, PL); Pacimol (IN); Pamol (DK, NZ); Panadol (AE, AU, BE, BF, BG, BH, BJ, CH, CI, CL, CY, EE, EG, ET, FI, FR, GB, GH, GM, GN, GR, HK, ID, IE, IL, IQ, IR, JO, KE, KR, KW, LB, LR, LY, MA, ML, MR, MU, MW, NE, NG, NL, NZ, OM, PK, PL, QA, SA, SC, SD, SL, SN, SY, TH, TW, TZ, UG, UY, YE, ZM, ZW); Panadol Actifast (MY, SG); Panadon (HR); Panamax (AU); Panodil (DK, NO, SE); Paracemol (PL); Paracenol (PL); Paracet (NO); Paracetamol (HR, PL); Parageniol (PY); Paragin (TH); Paralief (IE); Paramidol (PE); Paramol (IL, PL, TW); Parapaed (DE); Parapaed Junior (NZ); Parapaed Six Plus (NZ); Paratabs (NZ); Parcemol (HK); Parcemol Forte (HK); Parvid (PH); Paximol (SG); Pediatrix (CA); Pedipan (KR); Penral-Night (KR); Perfalgan (PL); Pinex (NO); Plicet (HR, PL); Poro (MY); Puernol (IT); Raperon (KR); Rapidol (CL); Reliv (SE); Remedol (AN, BB, BM, BS, BZ, GY, JM, SR, TT); Revanin (BF, BJ, CI, ET, GH, GM, GN, KE, LR, MA, ML, MR, MU, MW, NE, NG, SC, SD, SL, SN, TZ, UG, ZM, ZW); Rhinapen elixir (KR); Salzone (BF, BJ, CI, ET, GH, GM, GN, KE, LR, MA, ML, MR, MU, MW, NE, NG, SC, SD, SL, SN, TZ, UG, ZM, ZW); Saridon (CO); Sensamol (IL); Serimol (HK); Sinedol (DO); Stone (TW); Suspen ER (KR); Tabcin (PL); Tamifen (EC); Tazamol (PL); Tempra (BE, CA, EC, ES, GR, ID, JP, TH); Tempte (TW); Temzzard (MX); Turpan (ID); Tylenol (AT, AU, BG, BR, CA, CH, CN, DE, ES, FR, JP, KR, MX, PH, PT, TH, VE); Tylenol Extra Fuerte (PY); Tylenol Forte (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, PL, QA, SA, SY, YE); Tylex (CR, DO, GT, HN, NI, PA, SV); Winadol (CO, VE); Xebramol (TH); Zydinol (PH)
MECHANISM OF ACTION — Inhibits the synthesis of prostaglandins in the central nervous system and peripherally blocks pain impulse generation; produces antipyresis from inhibition of hypothalamic heat-regulating center
PHARMACODYNAMICS / KINETICS Onset of action: <1 hour
Duration: 4-6 hours
Absorption: Incomplete; varies by dosage form
Protein binding: 8% to 43% at toxic doses
Metabolism: At normal therapeutic dosages, hepatic to sulfate and glucuronide metabolites, while a small amount is metabolized by CYP to a highly reactive intermediate (acetylimidoquinone) which is conjugated with glutathione and inactivated; at toxic doses (as little as 4 g daily) glutathione conjugation becomes insufficient to meet the metabolic demand causing an increase in acetylimidoquinone concentration, which may cause hepatic cell necrosis
Half-life elimination: Prolonged following toxic doses Neonates: 2-5 hours Adults: 1-3 hours (may be increased in elderly; however, this should not affect dosing)
Time to peak, serum: Oral: 10-60 minutes; may be delayed in acute overdoses
Excretion: Urine (2% to 5% unchanged; 55% as glucuronide metabolites; 30% as sulphate metabolites)
U.S. BRAND NAMES — Acephen™ [OTC]; Apra Children's [OTC]; Aspirin Free Anacin® Maximum Strength [OTC]; Cetafen Extra® [OTC]; Cetafen® [OTC]; Comtrex® Sore Throat Maximum Strength [OTC]; FeverALL® [OTC]; Genapap™ Children [OTC]; Genapap™ Extra Strength [OTC]; Genapap™ Infant [OTC]; Genapap™ [OTC]; Genebs Extra Strength [OTC]; Genebs [OTC]; Infantaire [OTC]; Mapap Children's [OTC]; Mapap Extra Strength [OTC]; Mapap Infants [OTC]; Mapap [OTC]; Nortemp Children's [OTC]; Pain Eze [OTC]; Silapap® Children's [OTC]; Silapap® Infants [OTC]; Tycolene Maximum Strength [OTC]; Tycolene [OTC]; Tylenol® 8 Hour [OTC]; Tylenol® Arthritis Pain [OTC]; Tylenol® Children's with Flavor Creator [OTC]; Tylenol® Children's [OTC]; Tylenol® Extra Strength [OTC]; Tylenol® Infants [OTC]; Tylenol® Junior [OTC]; Tylenol® [OTC]; Valorin Extra [OTC]; Valorin [OTC]
PHARMACOLOGIC CATEGORY Analgesic, Miscellaneous
DOSING: ADULTS — Pain or fever: Oral, rectal: 325-650 mg every 4-6 hours or 1000 mg 3-4 times/day; do not exceed 4 g/day.
DOSING: PEDIATRIC — Pain or fever: Oral, rectal: Children <12 years: 10-15 mg/kg/dose every 4-6 hours as needed; do not exceed 5 doses (2.6 g) in 24 hours; alternatively, the following doses may be used; see table.
(For additional information see "Acetaminophen: Pediatric drug information")
Acetaminophen Dosing 0-3 months: 40 mg 4-11 months: 80 mg 1-2 years: 120 mg 2-3 years: 160 mg 4-5 years: 240 mg 6-8 years: 320 mg 9-10 years: 400 mg 11 years: 480 mg
Note: Higher rectal doses have been studied for use in preoperative pain control in children. However, specific guidelines are not available and dosing may be product dependent. The safety and efficacy of alternating acetaminophen and ibuprofen dosing has not been established.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT Clcr 10-50 mL/minute: Administer every 6 hours.
Clcr <10 mL/minute: Administer every 8 hours (metabolites accumulate).
Moderately dialyzable (20% to 50%)
DOSING: HEPATIC IMPAIRMENT — Use with caution. Limited, low-dose therapy is usually well tolerated in hepatic disease/cirrhosis. However, cases of hepatotoxicity at daily acetaminophen dosages <4 g/day have been reported. Avoid chronic use in hepatic impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Caplet: 500 mg Cetafen Extra® Strength, Genapap™ Extra Strength, Genebs Extra Strength, Mapap Extra Strength, Tycolene Maximum Strength, Tylenol® Extra Strength: 500 mg
Caplet, extended release: Tylenol® 8 Hour, Tylenol® Arthritis Pain: 650 mg
Capsule: 500 mg
Elixir: 160 mg/5 mL (120 mL, 480 mL, 3780 mL) Apra Children's: 160 mg/5 mL (120 mL, 480 mL, 3780 mL) [alcohol free; contains benzoic acid; cherry and grape flavors] Mapap Children's: 160 mg/5 mL (120 mL) [alcohol free; contains benzoic acid and sodium benzoate; cherry flavor]
Gelcap: Mapap Extra Strength, Tylenol® Extra Strength: 500 mg
Geltab: Tylenol® Extra Strength: 500 mg
Geltab, extended release: Tylenol® 8 Hour: 650 mg [DSC]
Liquid, oral: 500 mg/15 mL (240 mL) Comtrex® Sore Throat Maximum Strength: 500 mg/15 mL (240 mL) [contains sodium benzoate; honey lemon flavor] Genapap™ Children: 160 mg/5 mL (120 mL) [contains sodium benzoate; cherry and grape flavors] Silapap®: 160 mg/5 mL (120 mL, 240 mL, 480 mL) [sugar free; contains sodium benzoate; cherry flavor] Tylenol® Extra Strength: 500 mg/15 mL (240 mL) [contains sodium benzoate; cherry flavor]
Solution, oral: 160 mg/5 mL (120 mL, 480 mL)
Solution, oral [drops]: 80 mg/0.8 mL (15 mL) [droppers are marked at 0.4 mL (40 mg) and at 0.8 mL (80 mg)] Genapap™ Infant: 80 mg/0.8 mL (15 mL) [fruit flavor] Infantaire: 80 mg/0.8mL (15 mL, 30 mL) Silapap® Infant's: 80 mg/0.8 mL (15 mL, 30 mL) [contains sodium benzoate; cherry flavor]
Suppository, rectal: 120 mg, 325 mg, 650 mg Acephen™: 120 mg, 325 mg, 650 mg FeverALL®: 80 mg, 120 mg, 325 mg, 650 mg Mapap: 125 mg, 650 mg
Suspension, oral: Mapap Children's: 160 mg/5 mL (120 mL) [contains sodium benzoate; cherry flavor] Nortemp Children's: 160 mg/5 mL (120 mL) [alcohol free; contains sodium benzoate; cotton candy flavor] Tylenol® Children's: 160 mg/5 mL (120 mL, 240 mL) [contains sodium benzoate; bubble gum yum, cherry blast, dye free cherry, grape splash, and very berry strawberry flavors] Tylenol® Children's with Flavor Creator: 160 mg/5 mL (120 mL) [contains sodium 2 mg/5 mL and sodium benzoate; cherry blast flavor; packaged with apple (4), bubblegum (8), chocolate (4), & strawberry (4) sugar free flavor packets]
Suspension, oral [drops]: Mapap Infants: 80 mg/0.8 mL (15 mL, 30 mL) [contains sodium benzoate; cherry flavor] Tylenol® Infants: 80 mg/0.8 mL (15 mL, 30 mL) [contains sodium benzoate; cherry, dye free cherry, and grape flavors]
Tablet: 325 mg, 500 mg Aspirin Free Anacin® Extra Strength, Genapap™ Extra Strength, Genebs Extra Strength, Mapap Extra Strength, Pain Eze, Tylenol® Extra Strength, Valorin Extra: 500 mg Cetafen®, Genapap™, Genebs, Mapap, Tycolene, Tylenol®, Valorin: 325 mg
Tablet, chewable: 80 mg Genapap™ Children: 80 mg [contains phenylalanine 6 mg/tablet; fruit and grape flavors] Mapap Children's: 80 mg [contains phenylalanine 3 mg/tablet; bubble gum, fruit, and grape flavors] Mapap Junior Strength: 160 mg [contains phenylalanine 12 mg/tablet; grape flavor]
Tablet, orally disintegrating: 80 mg, 160 mg Tylenol® Children's Meltaways: 80 mg [bubble gum, grape, and watermelon flavors] Tylenol® Junior Meltaways: 160 mg [bubble gum and grape flavors]
DOSAGE FORMS: CONCISE Caplet: 500 mg Cetafen Extra® Strength [OTC], Genapap™ Extra Strength [OTC], Genebs Extra Strength [OTC], Mapap Extra Strength [OTC], Tycolene Maximum Strength [OTC], Tylenol® Extra Strength [OTC]: 500 mg
Caplet, extended release: Tylenol® 8 Hour [OTC], Tylenol® Arthritis Pain [OTC]: 650 mg
Capsule: 500 mg
Elixir: 160 mg/5 mL Apra Children's [OTC]: 160 mg/5 mL Mapap Children's [OTC]: 160 mg/5 mL
Gelcap: 500 mg Mapap Extra Strength [OTC], Tylenol® Extra Strength [OTC]: 500 mg
Geltab: 500 mg Tylenol® Extra Strength [OTC]: 500 mg
Liquid, oral: 500 mg/15 mL Comtrex® Sore Throat Maximum Strength [OTC], Tylenol® Extra Strength [OTC]: 500 mg/15 mL Genapap™ Children [OTC], Silapap® [OTC]: 160 mg/5 mL
Solution, oral: 160 mg/5 mL
Solution, oral [drops]: 80 mg/0.8 mL Genapap™ Infant [OTC], Infantaire [OTC], Silapap® Infant's [OTC]: 80 mg/0.8 mL
Suppository, rectal: 120 mg, 325 mg, 650 mg Acephen® [OTC]: 120 mg, 325 mg, 650 mg FeverALL® [OTC]: 80 mg, 120 mg, 325 mg, 650 mg Mapap [OTC]: 125 mg, 650 mg
Suspension, oral: 160 mg/5 mL Mapap Children's [OTC], Nortemp Children's [OTC], Tylenol® Children's [OTC], Tylenol® Children's with Flavor Creator [OTC]: 160 mg/5 mL
Suspension, oral [drops]: 80 mg/0.8 mL Mapap Infants [OTC], Tylenol® Infants [OTC]: 80 mg/0.8 mL
Tablet: 325 mg, 500 mg Aspirin Free Anacin® Extra Strength [OTC], Genapap™ Extra Strength [OTC], Genebs Extra Strength [OTC], Mapap Extra Strength [OTC], Redutemp® [OTC], Tylenol® Extra Strength [OTC], Valorin Extra [OTC]: 500 mg Cetafen® [OTC], Genapap™ [OTC], Genebs [OTC], Mapap [OTC], Tylenol® [OTC], Valorin [OTC]: 325 mg
Tablet, chewable: 80 mg Genapap™ Children [OTC], Mapap Children's [OTC]: 80 mg Mapap Junior Strength [OTC]: 160 mg
Tablet, orally disintegrating: 80 mg, 160 mg Tylenol® Children's Meltaways [OTC]: 80 mg Tylenol® Junior Meltaways [OTC]: 160 mg
GENERIC EQUIVALENT AVAILABLE — Yes: Excludes extended release products
ADMINISTRATION Suppositories: Do not freeze.
Suspension, oral: Shake well before pouring a dose.
USE — Treatment of mild-to-moderate pain and fever (antipyretic/analgesic); does not have antirheumatic or anti-inflammatory effects
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Dermatologic: Rash
Endocrine & metabolic: May increase chloride, uric acid, glucose; may decrease sodium, bicarbonate, calcium
Hematologic: Anemia, blood dyscrasias (neutropenia, pancytopenia, leukopenia)
Hepatic: Bilirubin increased, alkaline phosphatase increased
Renal: Ammonia increased, nephrotoxicity with chronic overdose, analgesic nephropathy
Miscellaneous: Hypersensitivity reactions (rare)
CONTRAINDICATIONS — Hypersensitivity to acetaminophen or any component of the formulation
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Hepatotoxicity: May cause severe hepatic toxicity on acute overdose; in addition, chronic daily dosing in adults has resulted in liver damage in some patients.
Disease-related concerns: Ethanol use: Use with caution in patients with alcoholic liver disease; consuming 3 alcoholic drinks/day may increase the risk of liver damage. G6PD deficiency: Use with caution in patients with known G6PD deficiency.
Other warnings/precautions: Dosage limit: Limit dose to <4>3 days or for pain lasting >10 days in adults or >5 days in children.
DRUG INTERACTIONS — Substrate (minor) of CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A4; Inhibits CYP3A4 (weak)
Decreased effect: Barbiturates, carbamazepine, hydantoins, rifampin, sulfinpyrazone may decrease the analgesic effect of acetaminophen. Cholestyramine may decrease acetaminophen absorption (separate dosing by at least 1 hour).
Increased toxicity: Barbiturates, carbamazepine, hydantoins, isoniazid, rifampin, sulfinpyrazone may increase the hepatotoxic potential of acetaminophen. Chronic ethanol abuse increases risk for acetaminophen toxicity; effect of warfarin may be enhanced.
ETHANOL / NUTRITION / HERB INTERACTIONS Ethanol: Excessive intake of ethanol may increase the risk of acetaminophen-induced hepatotoxicity. Avoid ethanol or limit to <3 drinks/day.
Food: Rate of absorption may be decreased when given with food.
Herb/Nutraceutical: St John's wort may decrease acetaminophen levels.
PREGNANCY RISK FACTOR — B (show table)
LACTATION — Enters breast milk/compatible
DIETARY CONSIDERATIONS — Chewable tablets may contain phenylalanine (amount varies, ranges between 3-12 mg/tablet); consult individual product labeling.
PRICING — (data from drugstore.com)Tablets (Tylenol) 325 mg (30): $7.99 500 mg (30): $7.99
MONITORING PARAMETERS — Relief of pain or fever
REFERENCE RANGE Therapeutic concentration (analgesic/antipyretic): 10-30 mcg/mL
Toxic concentration (acute ingestion) with probable hepatotoxicity: >200 mcg/mL at 4 hours or 50 mcg/mL at 12 hours after ingestion
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include hepatic necrosis, transient azotemia, renal tubular necrosis with acute toxicity, anemia, and GI disturbances with chronic toxicity. Acetylcysteine 140 mg/kg orally (loading) followed by 70 mg/kg every 4 hours for 17 doses. Therapy should be initiated based upon laboratory analysis suggesting high probability of hepatotoxic potential. Activated charcoal is very effective at binding acetaminophen.
CANADIAN BRAND NAMES — Abenol®; Apo-Acetaminophen®; Atasol®; Novo-Gesic; Pediatrix; Tempra®; Tylenol®
INTERNATIONAL BRAND NAMES — A-Mol (TH); Abenol (CA); Acamol (CL, IL); Acamoli Baby (IL); Acamoli Forte suppositories for Kids (IL); Acenol (PL); Acet (MY, PH); ACET suppositories (SG); Acetalgin (CH); Acetamol (IT); Adorem (CO); Afebrin (HK, ID); Alvedon (SE); Amol (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Anadin (PL); Anadin dla dzieci (PL); Analgiser (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Antidol (PL); APAP (PL); Apo-Acetaminophen (CA); Arfen (BF, BJ, CI, ET, GH, GM, GN, KE, LR, MA, ML, MR, MU, MW, MY, NE, NG, SC, SD, SL, SN, TZ, UG, ZM, ZW); Atamel (PE); Atasol (CA); Ben-U-Ron (PT); Benuron (JP, PL); Biogesic (ID, PH, TH); Biogesic Suspension (HK); Bodrex (ID); Calapol (ID); Calodol (PH); Calpol (AE, AN, BB, BF, BH, BJ, BM, BS, BZ, CI, CY, EG, ET, GH, GM, GN, GY, IE, IN, IQ, IR, JM, JO, JP, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, NE, NG, OM, PL, QA, SA, SC, SD, SL, SN, SR, SY, TH, TT, TZ, UG, YE, ZM, ZW); Causalon (AR); Cemol (TH); Christamol (HK); Claradol (MA); Codipar (PL); Crocin (IN); Dafalgan (PL); Daga (TH); Denamol (TH); Dirox (AR); Dismifen (MX); Dolex (UY); Doliprane (FR, MA, PL); Dolitabs (FR); Dolofen (CO); Dolomol (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Dolorol (ZA); Dolotemp (MX); Dymadon (AU); Efferalgan (PL); Efferalgan 500 (CR, DO, EE, GT, HN, NI, PA, SV); Efferalganodis (FR); Eraldor (EC); Etoran (PL); Europain (HK); Expandol (FR); Febridol (AU); Fepril (MY); Fervex (BR); Fortolin (CN); Gelocatil (ES); Geluprane 500 (FR); Grippostad (PL); Gunaceta (ID); Itamol (ID); Itamol Forte (ID); Kamolas (ID); Kyofen (CO); Lekadol (HR, PL); Lemgrip (BE); Lexalgin (PH); Lotemp (TH); Lupocet (HR); Maganol (ID); Malidens (IN); Mebinol (PE); Medgenol (PH); Metagesic (PH); Mexalen (AT, CZ, HU); Milidon 500 (SG); Minopan (KR); Mypara (TH); Nalgesik (ID); Napamol (ZA); Naprex (ID); NEBS (JP); Nektol 500 (PH); Nilapur (ID); Novo-Gesic (CA, PL); Pacimol (IN); Pamol (DK, NZ); Panadol (AE, AU, BE, BF, BG, BH, BJ, CH, CI, CL, CY, EE, EG, ET, FI, FR, GB, GH, GM, GN, GR, HK, ID, IE, IL, IQ, IR, JO, KE, KR, KW, LB, LR, LY, MA, ML, MR, MU, MW, NE, NG, NL, NZ, OM, PK, PL, QA, SA, SC, SD, SL, SN, SY, TH, TW, TZ, UG, UY, YE, ZM, ZW); Panadol Actifast (MY, SG); Panadon (HR); Panamax (AU); Panodil (DK, NO, SE); Paracemol (PL); Paracenol (PL); Paracet (NO); Paracetamol (HR, PL); Parageniol (PY); Paragin (TH); Paralief (IE); Paramidol (PE); Paramol (IL, PL, TW); Parapaed (DE); Parapaed Junior (NZ); Parapaed Six Plus (NZ); Paratabs (NZ); Parcemol (HK); Parcemol Forte (HK); Parvid (PH); Paximol (SG); Pediatrix (CA); Pedipan (KR); Penral-Night (KR); Perfalgan (PL); Pinex (NO); Plicet (HR, PL); Poro (MY); Puernol (IT); Raperon (KR); Rapidol (CL); Reliv (SE); Remedol (AN, BB, BM, BS, BZ, GY, JM, SR, TT); Revanin (BF, BJ, CI, ET, GH, GM, GN, KE, LR, MA, ML, MR, MU, MW, NE, NG, SC, SD, SL, SN, TZ, UG, ZM, ZW); Rhinapen elixir (KR); Salzone (BF, BJ, CI, ET, GH, GM, GN, KE, LR, MA, ML, MR, MU, MW, NE, NG, SC, SD, SL, SN, TZ, UG, ZM, ZW); Saridon (CO); Sensamol (IL); Serimol (HK); Sinedol (DO); Stone (TW); Suspen ER (KR); Tabcin (PL); Tamifen (EC); Tazamol (PL); Tempra (BE, CA, EC, ES, GR, ID, JP, TH); Tempte (TW); Temzzard (MX); Turpan (ID); Tylenol (AT, AU, BG, BR, CA, CH, CN, DE, ES, FR, JP, KR, MX, PH, PT, TH, VE); Tylenol Extra Fuerte (PY); Tylenol Forte (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, PL, QA, SA, SY, YE); Tylex (CR, DO, GT, HN, NI, PA, SV); Winadol (CO, VE); Xebramol (TH); Zydinol (PH)
MECHANISM OF ACTION — Inhibits the synthesis of prostaglandins in the central nervous system and peripherally blocks pain impulse generation; produces antipyresis from inhibition of hypothalamic heat-regulating center
PHARMACODYNAMICS / KINETICS Onset of action: <1 hour
Duration: 4-6 hours
Absorption: Incomplete; varies by dosage form
Protein binding: 8% to 43% at toxic doses
Metabolism: At normal therapeutic dosages, hepatic to sulfate and glucuronide metabolites, while a small amount is metabolized by CYP to a highly reactive intermediate (acetylimidoquinone) which is conjugated with glutathione and inactivated; at toxic doses (as little as 4 g daily) glutathione conjugation becomes insufficient to meet the metabolic demand causing an increase in acetylimidoquinone concentration, which may cause hepatic cell necrosis
Half-life elimination: Prolonged following toxic doses Neonates: 2-5 hours Adults: 1-3 hours (may be increased in elderly; however, this should not affect dosing)
Time to peak, serum: Oral: 10-60 minutes; may be delayed in acute overdoses
Excretion: Urine (2% to 5% unchanged; 55% as glucuronide metabolites; 30% as sulphate metabolites)
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