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.