U.S. BRAND NAMES — Zovirax®
PHARMACOLOGIC CATEGORY Antiviral Agent
DOSING: ADULTS — Note: Obese patients should be dosed using ideal body weight
Genital HSV: I.V.: Immunocompetent: Initial episode, severe: 5 mg/kg every 8 hours for 5-7 days Oral: Initial episode: 200 mg every 4 hours while awake (5 times/day) for 10 days (per manufacturer's labeling); 400 mg 3 times/day for 5-10 days has also been reported Recurrence: 200 mg every 4 hours while awake (5 times/day) for 5 days (per manufacturer's labeling; begin at earliest signs of disease); 400 mg 3 times/day for 5 days has also been reported Chronic suppression: 400 mg twice daily or 200 mg 3-5 times/day, for up to 12 months followed by re-evaluation (per manufacturer's labeling); 400-1200 mg/day in 2-3 divided doses has also been reported Topical: Immunocompromised: Ointment: Initial episode: 1/2" ribbon of ointment for a 4" square surface area every 3 hours (6 times/day) for 7 days
Herpes labialis (cold sores): Topical: Apply 5 times/day for 4 days
Herpes zoster (shingles): Oral: Immunocompetent: 800 mg every 4 hours (5 times/day) for 7-10 days I.V.: Immunocompromised: 10 mg/kg/dose or 500 mg/m2/dose every 8 hours for 7 days
HSV encephalitis: I.V.: 10 mg/kg/dose every 8 hours for 10 days (per manufacturer's labeling); 10-15 mg/kg/dose every 8 hours for 14-21 days also reported
Mucocutaneous HSV: I.V.: Immunocompromised: 5 mg/kg/dose every 8 hours for 7 days (per manufacturer's labeling); dosing for up to 14 days also reported Oral: Immunocompromised (unlabeled use): 400 mg 5 times a day for 7-14 days Topical: Ointment: Nonlife-threatening, immunocompromised: 1/2" ribbon of ointment for a 4" square surface area every 3 hours (6 times/day) for 7 days
Varicella-zoster (chickenpox): Begin treatment within the first 24 hours of rash onset: Oral: >40 kg (immunocompetent): 800 mg/dose 4 times a day for 5 days I.V.: Immunocompromised (unlabeled use): 1500 mg/m2/day divided every 8 hours or 10 mg/kg/dose every 8 hours for 7-10 days
Prevention of HSV reactivation in HIV-positive patients, for use only when recurrences are frequent or severe (unlabeled use): Oral: 200 mg 3 times/day or 400 mg 2 times/day
Prevention of HSV reactivation in HSCT (unlabeled use): Note: Start at the beginning of conditioning therapy and continue until engraftment or until mucositis resolves (~30 days) Oral: 200 mg 3 times/day I.V.: 250 mg/m2/dose every 12 hours
Bone marrow transplant recipients (unlabeled use): I.V.: Allogeneic patients who are HSV and CMV seropositive: 500 mg/m2/dose (10 mg/kg) every 8 hours; for clinically-symptomatic CMV infection, consider replacing acyclovir with ganciclovir
DOSING: PEDIATRIC — Note: Obese patients should be dosed using ideal body weight
(For additional information see "Acyclovir: Pediatric drug information")
Genital HSV: I.V.: Children 12 years: Refer to adult dosing. Oral: Initial episode (unlabeled use): 40-80 mg/kg/day divided into 3-4 doses for 5-10 days (maximum: 1 g/day) Chronic suppression (unlabeled use; limited data): 80 mg/kg/day in 3 divided doses (maximum: 1 g/day), re-evaluate after 12 months of treatment
Herpes labialis (cold sores): Topical: Children 12 years: Refer to adult dosing.
Herpes zoster (shingles): I.V.: Children <12 years (immunocompromised): 20 mg/kg/dose every 8 hours for 7 days Children 12 years: Refer to adult dosing.
HSV encephalitis: I.V.: Children 3 months to 12 years: 20 mg/kg/dose every 8 hours for 10 days (per manufacturer's labeling); dosing for 14-21 days also reported Children 12 years: Refer to adult dosing.
Mucocutaneous HSV: I.V.: Children <12 years (immunocompromised): 10 mg/kg/dose every 8 hours for 7 days Children 12 years: Refer to adult dosing.
Neonatal HSV: I.V.: Neonate: Birth to 3 months: 10 mg/kg/dose every 8 hours for 10 days (manufacturer's labeling); 15 mg/kg/dose or 20 mg/kg/dose every 8 hours for 14-21 days has also been reported
Varicella-zoster (chickenpox): Begin treatment within the first 24 hours of rash onset: Oral: Children 2 years and 40 kg (immunocompetent): 20 mg/kg/dose (up to 800 mg/dose) 4 times/day for 5 days Children >40 kg: Refer to adult dosing. I.V.: Children <1 year (immunocompromised, unlabeled use): 10 mg/kg/dose every 8 hours for 7-10 days Children 1 year: Refer to adult dosing.
Prevention of HSV reactivation in HIV-positive patients, for use only when recurrences are frequent or severe (unlabeled use): Oral: 80 mg/kg/day in 3-4 divided doses
Prevention of HSV reactivation in HSCT (unlabeled use): Note: Start at the beginning of conditioning therapy and continue until engraftment or until mucositis resolves (~30 days): I.V.: 250 mg/m2/dose every 8 hours or 125 mg/m2/dose every 6 hours
Bone marrow transplant recipients (unlabeled use): I.V.: Refer to adult dosing.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT Oral: Clcr 10-25 mL/minute/1.73 m2: Normal dosing regimen 800 mg every 4 hours: Administer 800 mg every 8 hours Clcr <10 mL/minute/1.73 m2: Normal dosing regimen 200 mg every 4 hours, 200 mg every 8 hours, or 400 mg every 12 hours: Administer 200 mg every 12 hours Normal dosing regimen 800 mg every 4 hours: Administer 800 mg every 12 hours
I.V.: Clcr 25-50 mL/minute/1.73 m2: Administer recommended dose every 12 hours Clcr 10-25 mL/minute/1.73 m2: Administer recommended dose every 24 hours Clcr <10 mL/minute/1.73 m2: Administer 50% of recommended dose every 24 hours
Hemodialysis: Administer dose after dialysis
Peritoneal dialysis: No supplemental dose needed
CAVH: 3.5 mg/kg/day
CVVHD/CVVH: Adjust dose based upon Clcr 30 mL/minute
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Capsule: 200 mg Zovirax®: 200 mg
Cream, topical: Zovirax®: 5% (2 g, 5 g)
Injection, powder for reconstitution, as sodium: 500 mg, 1000 mg Zovirax®: 500 mg [DSC]
Injection, solution, as sodium [preservative free]: 25 mg/mL (20 mL, 40 mL); 50 mg/mL (10 mL, 20 mL)
Ointment, topical: Zovirax®: 5% (15 g)
Suspension, oral: 200 mg/5 mL (480 mL) Zovirax®: 200 mg/5 mL (480 mL) [banana flavor]
Tablet: 400 mg, 800 mg Zovirax®: 400 mg, 800 mg
DOSAGE FORMS: CONCISE Capsule: 200 mg Zovirax®: 200 mg
Cream, topical: Zovirax®: 5% (2 g, 5 g)
Injection, powder for reconstitution: 500 mg, 1000 mg
Injection, solution [preservative free]: 25 mg/mL (20 mL, 40 mL); 50 mg/mL (10 mL, 20 mL)
Ointment, topical: Zovirax®: 5% (15 g)
Suspension, oral: 200 mg/5 mL Zovirax®: 200 mg/5 mL
Tablet: 400 mg, 800 mg Zovirax®: 400 mg, 800 mg
GENERIC EQUIVALENT AVAILABLE — Yes: Excludes cream, ointment
ADMINISTRATION Oral: May be administered with or without food.
I.V.: Avoid rapid infusion; infuse over 1 hour to prevent renal damage; maintain adequate hydration of patient; check for phlebitis and rotate infusion sites
Topical: Not for use in the eye. Apply using a finger cot or rubber glove to avoid transmission to other parts of the body or to other persons.
COMPATIBILITY — Stable in D5W, D5NS, D51/4NS, D51/2NS, LR, NS.
Incompatible with blood products and protein-containing solutions.
Y-site administration: Compatible: Allopurinol, amikacin, amphotericin B cholesteryl sulfate complex, ampicillin, cefamandole, cefazolin, cefoperazone, cefotaxime, cefoxitin, ceftazidime, ceftizoxime, ceftriaxone, cefuroxime, chloramphenicol, cimetidine, clindamycin, co-trimoxazole, dexamethasone, dimenhydrinate, diphenhydramine, docetaxel, doxorubicin liposome, doxycycline, erythromycin lactobionate, etoposide, famotidine, filgrastim, fluconazole, gatifloxacin, gentamicin, granisetron, heparin, hydrocortisone sodium succinate, hydromorphone, imipenem/cilastatin, linezolid, lorazepam, magnesium sulfate, melphalan, methylprednisolone sodium succinate, metoclopramide, metronidazole, multivitamins, nafcillin, oxacillin, paclitaxel, penicillin G potassium, pentobarbital, perphenazine, piperacillin, potassium chloride, propofol, ranitidine, remifentanil, sodium bicarbonate, tacrolimus, teniposide, theophylline, thiotepa, ticarcillin, tobramycin, vancomycin, zidovudine. Incompatible: Amifostine, amsacrine, aztreonam, cefepime, dobutamine, dopamine, fludarabine, foscarnet, gemcitabine, idarubicin, levofloxacin, ondansetron, piperacillin/tazobactam, sargramostim, vinorelbine. Variable (consult detailed reference): Cisatracurium, diltiazem, meperidine, meropenem, morphine, TPN.
Compatibility when admixed: Compatible: Fluconazole. Incompatible: Dobutamine, dopamine. Variable (consult detailed reference): Meropenem.
USE — Treatment of genital herpes simplex virus (HSV), herpes labialis (cold sores), herpes zoster (shingles), HSV encephalitis, neonatal HSV, mucocutaneous HSV in immunocompromised patients, varicella-zoster (chickenpox)
USE - UNLABELED / INVESTIGATIONAL — Prevention of HSV reactivation in HIV-positive patients; prevention of HSV reactivation in hematopoietic stem-cell transplant (HSCT); prevention of HSV reactivation during periods of neutropenia in patients with acute leukemia
ADVERSE REACTIONS SIGNIFICANT Systemic: Oral:
>10%: Central nervous system: Malaise (12%)
1% to 10%: Central nervous system: Headache (2%) Gastrointestinal: Nausea (2% to 5%), vomiting (3%), diarrhea (2% to 3%)
Systemic: Parenteral:
1% to 10%: Dermatologic: Hives (2%), itching (2%), rash (2%) Gastrointestinal: Nausea/vomiting (7%) Hepatic: Liver function tests increased (1% to 2%) Local: Inflammation at injection site or phlebitis (9%) Renal: BUN increased (5% to 10%), creatinine increased (5% to 10%), acute renal failure
Topical:
>10%: Dermatologic: Mild pain, burning, or stinging (ointment 30%)
1% to 10%: Dermatologic: Pruritus (ointment 4%), itching
All forms: <1% (Limited to important or life-threatening): Abdominal pain, aggression, agitation, alopecia, anaphylaxis, anemia, angioedema, anorexia, ataxia, coma, confusion, consciousness decreased, delirium, desquamation, diarrhea, disseminated intravascular coagulopathy (DIC), dizziness, dry lips, dysarthria, encephalopathy, erythema multiforme, fatigue, fever, gastrointestinal distress, hallucinations, hematuria, hemolysis, hepatitis, hyperbilirubinemia, hypotension, insomnia, jaundice, leukocytoclastic vasculitis, leukocytosis, leukopenia, local tissue necrosis (following extravasation), lymphadenopathy, mental depression, myalgia, neutrophilia, paresthesia, peripheral edema, photosensitization, pruritus, psychosis, renal failure, seizure, somnolence, sore throat, Stevens-Johnson syndrome, thrombocytopenia, thrombocytopenic purpura/hemolytic uremic syndrome (TTP/HUS), thrombocytosis, toxic epidermal necrolysis, tremor, urticaria, visual disturbances
CONTRAINDICATIONS — Hypersensitivity to acyclovir, valacyclovir, or any component of the formulation
WARNINGS / PRECAUTIONS — Use with caution in immunocompromised patients; thrombocytopenic purpura/hemolytic uremic syndrome (TTP/HUS) has been reported. Use caution in the elderly, pre-existing renal disease, or in those receiving other nephrotoxic drugs. Maintain adequate hydration during oral or intravenous therapy. Use I.V. preparation with caution in patients with underlying neurologic abnormalities, serious hepatic or electrolyte abnormalities, or substantial hypoxia.
Safety and efficacy of oral formulations have not been established in pediatric patients <2 years of age.
Chickenpox: Treatment should begin within 24 hours of appearance of rash; oral route not recommended for routine use in otherwise healthy children with varicella, but may be effective in patients at increased risk of moderate to severe infection (>12 years of age, chronic cutaneous or pulmonary disorders, long-term salicylate therapy, corticosteroid therapy).
Genital herpes: Physical contact should be avoided when lesions are present; transmission may also occur in the absence of symptoms. Treatment should begin with the first signs or symptoms.
Herpes labialis: For external use only to the lips and face; do not apply to eye or inside the mouth or nose. Treatment should begin with the first signs or symptoms.
Herpes zoster: Acyclovir should be started within 72 hours of appearance of rash to be effective.
ETHANOL / NUTRITION / HERB INTERACTIONS — Food: Does not affect absorption of oral acyclovir.
PREGNANCY RISK FACTOR — B (show table)
PREGNANCY IMPLICATIONS — Teratogenic effects were not observed in animal studies. Acyclovir has been shown to cross the human placenta. There are no adequate and well-controlled studies in pregnant women. Results from a pregnancy registry, established in 1984 and closed in 1999, did not find an increase in the number of birth defects with exposure to acyclovir when compared to those expected in the general population. However, due to the small size of the registry and lack of long-term data, the manufacturer recommends using during pregnancy with caution and only when clearly needed. Data from the pregnancy registry may be obtained from GlaxoSmithKline.
LACTATION — Enters breast milk/use with caution (AAP rates "compatible")
BREAST-FEEDING CONSIDERATIONS — Nursing mothers with herpetic lesions near or on the breast should avoid breast-feeding. Limited data suggest exposure to the nursing infant of ~0.3 mg/kg/day following oral administration of acyclovir to the mother.
DIETARY CONSIDERATIONS — May be taken with or without food. Acyclovir 500 mg injection contains sodium ~50 mg (~2 mEq).
PRICING — (data from drugstore.com)Capsules (Acyclovir) 200 mg (30): $12.99
Capsules (Zovirax) 200 mg (30): $66.50
Cream (Zovirax) 5% (2): $42.53 5% (5): $94.81
Ointment (Zovirax) 5% (15): $105.18
Suspension (Acyclovir) 200 mg/5 mL (473): $82.68
Suspension (Zovirax) 200 mg/5 mL (473): $183.41
Tablets (Acyclovir) 400 mg (60): $28.99 800 mg (30): $24.99
Tablets (Zovirax) 400 mg (60): $242.78 800 mg (30): $236.13
MONITORING PARAMETERS — Urinalysis, BUN, serum creatinine, liver enzymes, CBC
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Overdoses of up to 20 g have been reported. Symptoms of overdose include agitation, seizures, somnolence, confusion, elevated serum creatinine, and renal failure. In the event of overdose, sufficient urine flow must be maintained to avoid drug precipitation within renal tubules. Hemodialysis has resulted in up to 60% reduction in serum acyclovir levels.
CANADIAN BRAND NAMES — Apo-Acyclovir®; Gen-Acyclovir; Nu-Acyclovir; ratio-Acyclovir; Zovirax®
INTERNATIONAL BRAND NAMES — Abbovir (PL); ACERPES (DE); Acic Creme (DE); Acicloftal (IT); Aciclor (VE); Aciclosina (PE); Aciclovir (PL); Aciclovir-BC IV (AU); Acihexal (AU); Acivir Cream (IL, IN); Acivir Eye (IN); Acix (PL); Aclova (KR); Aclovir (HR, TH, TW); Aclovirax (HK); ACS (KR); Activir (FR); Acyclo-V (AU, BH); Acyclostad (PL); Acyclovir (PL); Acyclovir Stada (PL); Acyklowir (PL); Acylene (MY); Acyrova (KR); Acyvir (EC, HK, IT); Aias (KR); Antivir (PL); Apicol (CO); Apo-Acyclovir (CA, PL); Avorax (HK, MY, SG); Avorax Cream (MY); Awirol (PL); Azovir (ID); Bearax (SG); Cicloferon (MX); Cicloviral (CO); Clinovir (ID, TH); Clovicin (TW); Clovir (BR); Cloviran (CL); Colsor (TH); Cusiviral (ES, HK, MY, PL, SG); Cyclivex (ZA); Cyclomed (IL); Cyclorax (HK); Cyclostad (PH); Cyclovir (BF, BJ, CI, ET, GH, GM, GN, KE, LR, MA, ML, MR, MU, MW, NE, NG, SC, SD, SL, SN, TZ, UG, ZM, ZW); Cyllanvir (PH); Danovir (SG); Deherp (TH, TW); Dravyr (SG); Duvimex (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Entir (SG, TH); Erlvirax (SG); Euroclovir (HK); Eurovir (PY); Exavir (BR); Expit (UY); Gen-Acyclovir (CA); Hascovir (PL); Herpefug (DE); Herpesin (PL); Herpex (BH, IN, PL); Herpoviric (DE); Herpoviric Rp Creme (DE); Heviran (PL); Inmerax (CL); Juviral (DE); Laciken (MX); Lermex (TH); Libravir (EC); Lisovyr (AR, CL); Lovir (AU, HK, MY, NZ, SG); Lovire (ZA); Marvir (TH); Matrovir (ID); Maynor (ES); Medovir (AE, BF, BG, BH, BJ, CI, CY, EG, ET, GH, GM, GN, IQ, IR, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, MY, NE, NG, OM, QA, SA, SC, SD, SG, SL, SN, SY, TZ, UG, YE, ZM, ZW); Nevirz (ID); Norum (TH); Nu-Acyclovir (CA); Olvit (MX); Oppvir (TH, TW); Opthavir (MX); Poviral (EC); Proviral (AR); Qualiclovir (HK); Quavir (ID); Ranvir (TH); Ranviran (PL); ratio-Acyclovir (CA); Skirax (TW); Supra-Vir (IL); Supraviran (DE, PL); Supraviran Creme (AE, BH, CY, DE, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Syntovir (HK); Vacrax (MY); Vermis (TH); Vicorax (TH, TW); Viraban (NZ); Viracir (PL); Viralex-DS (PH); Virax (KR); Vircella (ID); Virest (MY, SG); Virex (CO); Virless (CN, TW); Viroclear (HK); Virogon (TH); Virolan (TW); Virolex (HR, PL); Viromed (TH); Virucid (HK); Virules (HK); Vivir (KR); Warviron (HK); Zetavir (MX); Zeven Cream (MY); Zevin (HK, TH); Zoral (HK, SG); Zoral Cream (MY); Zorax (SG); Zorel (ID); Zoter (ID); Zovir (DK); Zovirax [tabs./susp./ungt.] (PL); Zovirax (AE, AN, AR, AT, AU, BB, BD, BE, BF, BG, BH, BJ, BM, BO, BR, BS, BZ, CA, CH, CI, CL, CN, CR, CY, CZ, DE, DK, DO, EG, ES, ET, FI, FR, GB, GH, GM, GN, GR, GT, GY, HK, HN, HR, HU, ID, IE, IL, IN, IQ, IR, IT, JM, JO, JP, KE, KR, KW, LB, LR, LY, MA, ML, MR, MU, MW, MX, MY, NE, NG, NI, NL, NO, NZ, OM, PA, PE, PH, PK, PR, PT, PY, QA, RU, SA, SC, SD, SE, SL, SN, SR, SV, SY, TR, TT, TW, TZ, UG, UY, YE, ZA, ZM, ZW); Zumasid (ID); Zyclir (AU); Zyclorax (ID); Zyvir (KE)
MECHANISM OF ACTION — Acyclovir is converted to acyclovir monophosphate by virus-specific thymidine kinase then further converted to acyclovir triphosphate by other cellular enzymes. Acyclovir triphosphate inhibits DNA synthesis and viral replication by competing with deoxyguanosine triphosphate for viral DNA polymerase and being incorporated into viral DNA.
PHARMACODYNAMICS / KINETICS Absorption: Oral: 15% to 30%
Distribution: Vd: 0.8 L/kg (63.6 L): Widely (eg, brain, kidney, lungs, liver, spleen, muscle, uterus, vagina, CSF)
Protein binding: 9% to 33%
Metabolism: Converted by viral enzymes to acyclovir monophosphate, and further converted to diphosphate then triphosphate (active form) by cellular enzymes
Bioavailability: Oral: 10% to 20% with normal renal function (bioavailability decreases with increased dose)
Half-life elimination: Terminal: Neonates: 4 hours; Children 1-12 years: 2-3 hours; Adults: 3 hours
Time to peak, serum: Oral: Within 1.5-2 hours
Excretion: Urine (62% to 90% as unchanged drug and metabolite)
PATIENT INFORMATION — This is not a cure for herpes (recurrences tend to continually reappear every 3-6 months after original infection), nor will this medication reduce the risk of transmission to others when lesions are present; avoid sexual intercourse when visible lesions are present. Take as directed for full course of therapy; do not discontinue even if feeling better. Oral doses may be taken with food.
(For additional information see "Acyclovir: Patient drug information"
Wednesday, January 23, 2008
Acrivastine and pseudoephedrine
U.S. BRAND NAMES — Semprex®-D
PHARMACOLOGIC CATEGORY Antihistamine
DOSING: ADULTS — Rhinitis, nasal congestion, allergic symptoms: Oral: 1 capsule 3-4 times/day
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Do not use.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule: Acrivastine 8 mg and pseudoephedrine hydrochloride 60 mg
DOSAGE FORMS: CONCISE Capsule: Semprex®-D: Acrivastine 8 mg and pseudoephedrine 60 mg
GENERIC EQUIVALENT AVAILABLE — No
USE — Temporary relief of nasal congestion, decongest sinus openings, running nose, itching of nose or throat, and itchy, watery eyes due to hay fever or other upper respiratory allergies
ADVERSE REACTIONS SIGNIFICANT >10%: Central nervous system: Drowsiness, headache
1% to 10%: Cardiovascular: Tachycardia, palpitation Central nervous system: Nervousness, dizziness, insomnia, vertigo, lightheadedness, fatigue Gastrointestinal: Nausea, vomiting, xerostomia, diarrhea Genitourinary: Dysuria Neuromuscular & skeletal: Weakness Respiratory: Pharyngitis, cough increased Miscellaneous: Diaphoresis
CONTRAINDICATIONS — Hypersensitivity to pseudoephedrine, acrivastine (or other alkylamine antihistamines), or any component of the formulation; MAO inhibitor therapy within 14 days of initiating therapy; severe hypertension, severe coronary artery disease; renal impairment (Clcr 48 mL/minute)
WARNINGS / PRECAUTIONS Disease-related concerns: Asthma: Use with caution in patients with asthma. Cardiovascular disease: Use with caution in patients with high blood pressure and/or ischemic heart disease. Diabetes: Use with caution in patients with diabetes mellitus. GI obstruction: Use with caution in patients with GI obstruction. Increased intraocular pressure: Use with caution in patients with increased intraocular pressure. Prostatic hyperplasia/urinary obstruction: Use with caution in patients with prostatic hyperplasia and/or GU obstruction. Thyroid dysfunction: Use with caution in patients with thyroid dysfunction.
Special populations: Elderly: Use with caution in patients >60 years of age. Pediatrics: Not recommended for use in children.
DRUG INTERACTIONS Decreased effect of guanethidine, reserpine, methyldopa, and beta-blockers
Increased toxicity with MAO inhibitors (hypertensive crisis), sympathomimetics, CNS depressants, ethanol (sedation)
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Avoid ethanol (may increase sedation)
PREGNANCY RISK FACTOR — B (show table)
LACTATION — Enters breast milk/contraindicated
PRICING — (data from drugstore.com)Capsules (Semprex-D) 8-60 mg (30): $37.47
MECHANISM OF ACTION — Refer to Pseudoephedrine; acrivastine is an analogue of triprolidine and it is considered to be relatively less sedating than traditional antihistamines; believed to involve competitive blockade of H1-receptor sites resulting in the inability of histamine to combine with its receptor sites and exert its usual effects on target cells
PHARMACODYNAMICS / KINETICS Pseudoephedrine: See Pseudoephedrine.
Acrivastine: Metabolism: Minimally hepatic Time to peak: ~1.1 hours Excretion: Urine (84%); feces (13%)
PHARMACOLOGIC CATEGORY Antihistamine
DOSING: ADULTS — Rhinitis, nasal congestion, allergic symptoms: Oral: 1 capsule 3-4 times/day
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Do not use.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule: Acrivastine 8 mg and pseudoephedrine hydrochloride 60 mg
DOSAGE FORMS: CONCISE Capsule: Semprex®-D: Acrivastine 8 mg and pseudoephedrine 60 mg
GENERIC EQUIVALENT AVAILABLE — No
USE — Temporary relief of nasal congestion, decongest sinus openings, running nose, itching of nose or throat, and itchy, watery eyes due to hay fever or other upper respiratory allergies
ADVERSE REACTIONS SIGNIFICANT >10%: Central nervous system: Drowsiness, headache
1% to 10%: Cardiovascular: Tachycardia, palpitation Central nervous system: Nervousness, dizziness, insomnia, vertigo, lightheadedness, fatigue Gastrointestinal: Nausea, vomiting, xerostomia, diarrhea Genitourinary: Dysuria Neuromuscular & skeletal: Weakness Respiratory: Pharyngitis, cough increased Miscellaneous: Diaphoresis
CONTRAINDICATIONS — Hypersensitivity to pseudoephedrine, acrivastine (or other alkylamine antihistamines), or any component of the formulation; MAO inhibitor therapy within 14 days of initiating therapy; severe hypertension, severe coronary artery disease; renal impairment (Clcr 48 mL/minute)
WARNINGS / PRECAUTIONS Disease-related concerns: Asthma: Use with caution in patients with asthma. Cardiovascular disease: Use with caution in patients with high blood pressure and/or ischemic heart disease. Diabetes: Use with caution in patients with diabetes mellitus. GI obstruction: Use with caution in patients with GI obstruction. Increased intraocular pressure: Use with caution in patients with increased intraocular pressure. Prostatic hyperplasia/urinary obstruction: Use with caution in patients with prostatic hyperplasia and/or GU obstruction. Thyroid dysfunction: Use with caution in patients with thyroid dysfunction.
Special populations: Elderly: Use with caution in patients >60 years of age. Pediatrics: Not recommended for use in children.
DRUG INTERACTIONS Decreased effect of guanethidine, reserpine, methyldopa, and beta-blockers
Increased toxicity with MAO inhibitors (hypertensive crisis), sympathomimetics, CNS depressants, ethanol (sedation)
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Avoid ethanol (may increase sedation)
PREGNANCY RISK FACTOR — B (show table)
LACTATION — Enters breast milk/contraindicated
PRICING — (data from drugstore.com)Capsules (Semprex-D) 8-60 mg (30): $37.47
MECHANISM OF ACTION — Refer to Pseudoephedrine; acrivastine is an analogue of triprolidine and it is considered to be relatively less sedating than traditional antihistamines; believed to involve competitive blockade of H1-receptor sites resulting in the inability of histamine to combine with its receptor sites and exert its usual effects on target cells
PHARMACODYNAMICS / KINETICS Pseudoephedrine: See Pseudoephedrine.
Acrivastine: Metabolism: Minimally hepatic Time to peak: ~1.1 hours Excretion: Urine (84%); feces (13%)
Acitretin:
U.S. BRAND NAMES — Soriatane®
PHARMACOLOGIC CATEGORY Retinoid-Like Compound
DOSING: ADULTS Psoriasis: Oral: Individualization of dosage is required to achieve maximum therapeutic response while minimizing side effects Initial therapy: Therapy should be initiated at 25-50 mg/day, given as a single dose with the main meal Maintenance: Doses of 25-50 mg/day may be given after initial response to treatment; the maintenance dose should be based on clinical efficacy and tolerability
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule: 10 mg, 25 mg
DOSAGE FORMS: CONCISE Capsule: Soriatane®: 10 mg, 25 mg
GENERIC EQUIVALENT AVAILABLE — No
USE — Treatment of severe psoriasis
ADVERSE REACTIONS SIGNIFICANT >10%: Central nervous system: Hyperesthesia (10% to 25%) Dermatologic: Cheilitis (>75%), alopecia (50% to 75%), skin peeling (50% to 75%), dry skin (25% to 50%), nail disorder (25% to 50%), pruritus (25% to 50%), erythematous rash (10% to 25%), skin atrophy (10% to 25%), sticky skin (10% to 25%), paronychia (10% to 25%) Endocrine & metabolic: Hypercholesterolemia (25% to 50%), hypertriglyceridemia (50% to 75%), HDL decreased (25% to 50%), phosphorus increased (10% to 25%), potassium increased (10% to 25%), sodium increased (10% to 25%), magnesium increased/decreased (10% to 25%), fasting blood sugar increased (25% to 50%), fasting blood sugar decreased (10% to 25%) Gastrointestinal: Xerostomia (10% to 25%) Hematologic: Reticulocytes increased (25% to 50%), hematocrit decreased (10% to 25%), hemoglobin decreased (10% to 25%), WBC increased/decreased (10% to 25%), haptoglobin increased (10% to 25%), neutrophils increased (10% to 25%) Hepatic: Liver function tests increased (25% to 50%), alkaline phosphatase increased (10% to 25%), direct bilirubin increased (10% to 25%), GGTP increased (10% to 25%) Neuromuscular & skeletal: Paresthesia (10% to 25%), arthralgia (10% to 25%), rigors (10% to 25%), CPK increased (25% to 50%), spinal hyperostosis progression (10% to 25%) Ocular: Xerophthalmia (10% to 25%), Renal: Uric acid increased (10% to 25%), acetonuria (10% to 25%), hematuria (10% to 25%), RBC in urine (10% to 25%) Respiratory: Rhinitis (25% to 50%), epistaxis (10% to 25%)
1% to 10%: Cardiovascular: Flushing, edema Central nervous system: Headache, pain, depression, insomnia, somnolence, fatigue Dermatologic: Skin odor, hair texture change, bullous eruption, dermatitis, diaphoresis increased, psoriasiform rash, purpura, pyogenic granuloma, rash, seborrhea, ulcers, fissures, sunburn Endocrine & metabolic: Hot flashes, potassium decreased, phosphorus decreased, sodium decreased, calcium increased or decreased, chloride increased or decreased Gastrointestinal: Gingival bleeding, gingivitis, saliva increased, stomatitis, thirst, ulcerative stomatitis, abdominal pain, diarrhea, nausea, taste disturbance, anorexia, appetite increased, tongue disorder Hepatic: Total bilirubin increased Neuromuscular & skeletal: Arthritis, back pain, hypertonia, myalgia, osteodynia, peripheral joint hyperostosis, Bell's palsy Ocular: Blurred vision, blepharitis, conjunctivitis, night blindness, photophobia, corneal epithelial abnormality, eye pain, eyebrow or eyelash loss, diplopia, cataract Otic: Earache, tinnitus Renal: BUN increased, creatinine increased, glycosuria, proteinuria Respiratory: Sinusitis
<1% (Limited to important or life-threatening): Anxiety, bleeding time increased, chest pain, cirrhosis, conjunctival hemorrhage, constipation, corneal ulceration, cyanosis, deafness, diplopia, dizziness, dyspepsia, dysphonia, dysuria, eczema, esophagitis, fever, furunculosis, gastritis, glossitis, gum hyperplasia, hair discoloration, healing impaired, hemorrhage, hepatic dysfunction, hepatitis, hyperkeratosis, hypertrichosis, hypoesthesia, intermittent claudication, itchy eyes, jaundice, leukorrhea, malaise, melena, MI, moniliasis, myopathy, nervousness, neuritis, pancreatitis, papilledema, peripheral ischemia, photosensitivity, pseudotumor cerebri, scleroderma, skin fragility or thinning, spinal hyperostosis (new lesion), stroke, taste loss, tendonitis, thromboembolism
CONTRAINDICATIONS — Hypersensitivity to acitretin, other retinoids, or any component of the formulation; patients who are pregnant or intend on becoming pregnant; ethanol ingestion; severe hepatic or renal dysfunction; chronically-elevated blood lipid levels; concomitant use with methotrexate or tetracycline
Acitretin is contraindicated in females of childbearing potential unless all of the following conditions apply. 1) Patient has severe psoriasis unresponsive to other therapy or if clinical condition contraindicates other treatments. 2) Patient must have two negative urine or serum pregnancy tests prior to therapy. 3) Patient must commit to using two effective forms of birth control starting 1 month prior to acitretin treatment and for 3 years after discontinuation. 4) Patient is reliable in understanding and carrying out instructions. 5) Patient has received, and acknowledged, understanding of a careful oral and printed explanation of the hazards of fetal exposure to acitretin and the risk of possible contraception failure; this explanation may include showing a line drawing to the patient of an infant with the characteristic external deformities resulting from retinoid exposure during pregnancy. Patient must sign an agreement/informed consent document stating that she understands these risks and that she should not consume ethanol during therapy or for 2 months after discontinuation. 6) All patients (male and female) should not donate blood during and for 3 years following treatment with acitretin.
WARNINGS / PRECAUTIONS Box warnings: Blood donation: See "Other warnings/precautions" below. Ethanol use: See "Concurrent drug therapy issues" below. Medication guide: See "Other warnings/precautions" below. Pregnancy: See "Special populations" below.
Concerns related to adverse effects: Hepatotoxicity: Monitor for hepatotoxicity; discontinue if elevations of liver enzymes occur. Use with caution in patients at risk of hypertriglyceridemias. Pseudotumor cerebri: Rarely associated with pseudotumor cerebri. Visual disturbances: May cause a decrease in night vision or decreased tolerance to contact lenses; discontinue if visual changes occur.
Concurrent drug therapy issues: Ethanol use: [U.S. Boxed Warning]: All patients (male and female) should abstain from ethanol or ethanol-containing products during therapy and for 2 months after discontinuation.
Special populations: Pediatrics: Safety and efficacy have not been established in children; growth potential may be affected. Pregnancy: [U.S. Boxed Warning]: Not for use by women who want to become pregnant; patient should not get pregnant for at least 3 years after discontinuation.
Other warnings/precautions: Blood donation: [U.S. Boxed Warning]: All patients should be advised not to donate blood during therapy or for 3 years following completion of therapy. Medication guide: [U.S. Boxed Warning]: All patients must be provided with a medication guide each time acitretin is dispensed. Female patients must also sign an informed consent prior to therapy.
RESTRICTIONS — An FDA-approved medication guide must be distributed when dispensing an outpatient prescription (new or refill) where this medication is to be used without direct supervision of a healthcare provider. Medication guides are available at http://www.fda.gov/cder/Offices/ODS/medication_guides.htm.
DRUG INTERACTIONS Ethanol: Etretinate (a retinoid with a much longer half-life) can be formed with concurrent use; contraindicated.
Methotrexate: The concomitant administration of methotrexate and etretinate has been associated with hepatitis, a similar increased hepatitis risk may be expected with the combined use of acitretin and methotrexate; concomitant use is contraindicated.
Progestins: Decreased contraceptive effect with concurrent use; use of "mini-pill" preparations are not recommended. Interactions with other progestational agents or hormonal contraceptives have not been established.
Sulfonylureas: Glucose-lowering effect may be potentiated. Effect seen with glibenclamide.
Tetracycline: Acitretin and tetracyclines may both cause increased intracranial pressure; concomitant use is contraindicated.
Vitamin A: Concomitant administration of vitamin A and other systemic retinoids must be avoided due to the risk of possible additive toxic effects.
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Use leads to formation of etretinate, a teratogenic metabolite with a prolonged half-life; concomitant use of ethanol or ethanol-containing products is contraindicated.
PREGNANCY RISK FACTOR — X (show table)
PREGNANCY IMPLICATIONS — Acitretin is teratogenic in humans. Severe birth defects have been reported when conception occurred during treatment or after therapy was complete. Not for use by women who want to become pregnant; patient should not get pregnant for at least 3 years after discontinuation. In addition, because ethanol forms a teratogenic metabolite and would increase the duration of teratogenic potential, ethanol should not be consumed during treatment or for 2 months after discontinuation. Limited amounts of acitretin are found in seminal fluid; although it appears this poses little risk to a fetus, the actual risk of teratogenicity is not known. Any pregnancy which occurs during treatment, or within 3 years after treatment is discontinued, should be reported to the manufacturer at 1-888-500-3376 or to the FDA at 1-800-FDA-1088.
LACTATION — Enters breast milk/not recommended
BREAST-FEEDING CONSIDERATIONS — Acitretin should not be given prior to or during nursing due to the potential for adverse effects in the nursing infant.
DIETARY CONSIDERATIONS — Administer with food. Avoid ingestion of additional sources of exogenous vitamin A (in excess of RDA); use of ethanol and ethanol-containing products is contraindicated.
PRICING — (data from drugstore.com)Capsules (Soriatane) 10 mg (30): $451.54 25 mg (30): $573.49
MONITORING PARAMETERS — Lipid profile (baseline and at 1- to 2-week intervals for 4-8 weeks); liver function tests (baseline, and at 1- to 2-week intervals until stable, then as clinically indicated); blood glucose in patients with diabetes; bone abnormalities (with long-term use)
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms of acute hypervitaminosis A (headache, vertigo) would be expected; vomiting has also been reported. Pregnancy test for women of childbearing age; counseling regarding potential for birth defects and appropriate contraceptive use.
CANADIAN BRAND NAMES — Soriatane®
INTERNATIONAL BRAND NAMES — Neo-Tigason (TH); Neotigason (AN, AR, AT, AU, BB, BE, BF, BG, BJ, BM, BR, BS, BZ, CH, CI, CL, CN, CO, CZ, DE, DK, EC, EE, EG, ES, ET, FI, GB, GH, GM, GN, GY, HU, IE, IL, IT, JM, KE, KR, LR, MA, ML, MR, MU, MW, MX, NE, NG, NL, NO, NZ, PE, PH, PL, PT, PY, SC, SD, SE, SL, SN, SR, TT, TW, TZ, UG, UY, VE, ZA, ZM, ZW); Soriatane (CA, FR)
PHARMACODYNAMICS / KINETICS — Etretinate has been detected in serum for up to 3 years following therapy, possibly due to storage in adipose tissue.
Onset: May take 2-3 months for full effect; improvement may be seen within 8 weeks.
Absorption: Oral: ~72% absorbed when given with food
Protein binding: >99% bound, primarily to albumin
Metabolism: Metabolized to cis-acitretin; both compounds are further metabolized. Concomitant ethanol use leads to the formation of etretinate (active).
Half-life elimination: Acitretin: 49 hours (range: 33-96); cis-acitretin: 63 hours (range: 28-157); etretinate: 120 days (range: 84-168 days)
Excretion: Feces (34% to 54%); urine (16% to 53%)
PATIENT INFORMATION — Take with food. Do not drink alcohol during therapy and for 2 months after discontinuation. Use contraception for 1 month before, during, and for 3 years after discontinuation. You may not be able to tolerate contact lenses during treatment. Do not donate blood during treatment and for 3 years after discontinuation (male and female patients). Avoid exposure to sunlight. Wear protective clothing and sunscreens. Avoid use of other vitamin A products. Females: Use two effective forms of birth control. If you have had your tubes tied, then use an additional form of birth control. If you become pregnant, contact your prescriber immediately.
PHARMACOLOGIC CATEGORY Retinoid-Like Compound
DOSING: ADULTS Psoriasis: Oral: Individualization of dosage is required to achieve maximum therapeutic response while minimizing side effects Initial therapy: Therapy should be initiated at 25-50 mg/day, given as a single dose with the main meal Maintenance: Doses of 25-50 mg/day may be given after initial response to treatment; the maintenance dose should be based on clinical efficacy and tolerability
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule: 10 mg, 25 mg
DOSAGE FORMS: CONCISE Capsule: Soriatane®: 10 mg, 25 mg
GENERIC EQUIVALENT AVAILABLE — No
USE — Treatment of severe psoriasis
ADVERSE REACTIONS SIGNIFICANT >10%: Central nervous system: Hyperesthesia (10% to 25%) Dermatologic: Cheilitis (>75%), alopecia (50% to 75%), skin peeling (50% to 75%), dry skin (25% to 50%), nail disorder (25% to 50%), pruritus (25% to 50%), erythematous rash (10% to 25%), skin atrophy (10% to 25%), sticky skin (10% to 25%), paronychia (10% to 25%) Endocrine & metabolic: Hypercholesterolemia (25% to 50%), hypertriglyceridemia (50% to 75%), HDL decreased (25% to 50%), phosphorus increased (10% to 25%), potassium increased (10% to 25%), sodium increased (10% to 25%), magnesium increased/decreased (10% to 25%), fasting blood sugar increased (25% to 50%), fasting blood sugar decreased (10% to 25%) Gastrointestinal: Xerostomia (10% to 25%) Hematologic: Reticulocytes increased (25% to 50%), hematocrit decreased (10% to 25%), hemoglobin decreased (10% to 25%), WBC increased/decreased (10% to 25%), haptoglobin increased (10% to 25%), neutrophils increased (10% to 25%) Hepatic: Liver function tests increased (25% to 50%), alkaline phosphatase increased (10% to 25%), direct bilirubin increased (10% to 25%), GGTP increased (10% to 25%) Neuromuscular & skeletal: Paresthesia (10% to 25%), arthralgia (10% to 25%), rigors (10% to 25%), CPK increased (25% to 50%), spinal hyperostosis progression (10% to 25%) Ocular: Xerophthalmia (10% to 25%), Renal: Uric acid increased (10% to 25%), acetonuria (10% to 25%), hematuria (10% to 25%), RBC in urine (10% to 25%) Respiratory: Rhinitis (25% to 50%), epistaxis (10% to 25%)
1% to 10%: Cardiovascular: Flushing, edema Central nervous system: Headache, pain, depression, insomnia, somnolence, fatigue Dermatologic: Skin odor, hair texture change, bullous eruption, dermatitis, diaphoresis increased, psoriasiform rash, purpura, pyogenic granuloma, rash, seborrhea, ulcers, fissures, sunburn Endocrine & metabolic: Hot flashes, potassium decreased, phosphorus decreased, sodium decreased, calcium increased or decreased, chloride increased or decreased Gastrointestinal: Gingival bleeding, gingivitis, saliva increased, stomatitis, thirst, ulcerative stomatitis, abdominal pain, diarrhea, nausea, taste disturbance, anorexia, appetite increased, tongue disorder Hepatic: Total bilirubin increased Neuromuscular & skeletal: Arthritis, back pain, hypertonia, myalgia, osteodynia, peripheral joint hyperostosis, Bell's palsy Ocular: Blurred vision, blepharitis, conjunctivitis, night blindness, photophobia, corneal epithelial abnormality, eye pain, eyebrow or eyelash loss, diplopia, cataract Otic: Earache, tinnitus Renal: BUN increased, creatinine increased, glycosuria, proteinuria Respiratory: Sinusitis
<1% (Limited to important or life-threatening): Anxiety, bleeding time increased, chest pain, cirrhosis, conjunctival hemorrhage, constipation, corneal ulceration, cyanosis, deafness, diplopia, dizziness, dyspepsia, dysphonia, dysuria, eczema, esophagitis, fever, furunculosis, gastritis, glossitis, gum hyperplasia, hair discoloration, healing impaired, hemorrhage, hepatic dysfunction, hepatitis, hyperkeratosis, hypertrichosis, hypoesthesia, intermittent claudication, itchy eyes, jaundice, leukorrhea, malaise, melena, MI, moniliasis, myopathy, nervousness, neuritis, pancreatitis, papilledema, peripheral ischemia, photosensitivity, pseudotumor cerebri, scleroderma, skin fragility or thinning, spinal hyperostosis (new lesion), stroke, taste loss, tendonitis, thromboembolism
CONTRAINDICATIONS — Hypersensitivity to acitretin, other retinoids, or any component of the formulation; patients who are pregnant or intend on becoming pregnant; ethanol ingestion; severe hepatic or renal dysfunction; chronically-elevated blood lipid levels; concomitant use with methotrexate or tetracycline
Acitretin is contraindicated in females of childbearing potential unless all of the following conditions apply. 1) Patient has severe psoriasis unresponsive to other therapy or if clinical condition contraindicates other treatments. 2) Patient must have two negative urine or serum pregnancy tests prior to therapy. 3) Patient must commit to using two effective forms of birth control starting 1 month prior to acitretin treatment and for 3 years after discontinuation. 4) Patient is reliable in understanding and carrying out instructions. 5) Patient has received, and acknowledged, understanding of a careful oral and printed explanation of the hazards of fetal exposure to acitretin and the risk of possible contraception failure; this explanation may include showing a line drawing to the patient of an infant with the characteristic external deformities resulting from retinoid exposure during pregnancy. Patient must sign an agreement/informed consent document stating that she understands these risks and that she should not consume ethanol during therapy or for 2 months after discontinuation. 6) All patients (male and female) should not donate blood during and for 3 years following treatment with acitretin.
WARNINGS / PRECAUTIONS Box warnings: Blood donation: See "Other warnings/precautions" below. Ethanol use: See "Concurrent drug therapy issues" below. Medication guide: See "Other warnings/precautions" below. Pregnancy: See "Special populations" below.
Concerns related to adverse effects: Hepatotoxicity: Monitor for hepatotoxicity; discontinue if elevations of liver enzymes occur. Use with caution in patients at risk of hypertriglyceridemias. Pseudotumor cerebri: Rarely associated with pseudotumor cerebri. Visual disturbances: May cause a decrease in night vision or decreased tolerance to contact lenses; discontinue if visual changes occur.
Concurrent drug therapy issues: Ethanol use: [U.S. Boxed Warning]: All patients (male and female) should abstain from ethanol or ethanol-containing products during therapy and for 2 months after discontinuation.
Special populations: Pediatrics: Safety and efficacy have not been established in children; growth potential may be affected. Pregnancy: [U.S. Boxed Warning]: Not for use by women who want to become pregnant; patient should not get pregnant for at least 3 years after discontinuation.
Other warnings/precautions: Blood donation: [U.S. Boxed Warning]: All patients should be advised not to donate blood during therapy or for 3 years following completion of therapy. Medication guide: [U.S. Boxed Warning]: All patients must be provided with a medication guide each time acitretin is dispensed. Female patients must also sign an informed consent prior to therapy.
RESTRICTIONS — An FDA-approved medication guide must be distributed when dispensing an outpatient prescription (new or refill) where this medication is to be used without direct supervision of a healthcare provider. Medication guides are available at http://www.fda.gov/cder/Offices/ODS/medication_guides.htm.
DRUG INTERACTIONS Ethanol: Etretinate (a retinoid with a much longer half-life) can be formed with concurrent use; contraindicated.
Methotrexate: The concomitant administration of methotrexate and etretinate has been associated with hepatitis, a similar increased hepatitis risk may be expected with the combined use of acitretin and methotrexate; concomitant use is contraindicated.
Progestins: Decreased contraceptive effect with concurrent use; use of "mini-pill" preparations are not recommended. Interactions with other progestational agents or hormonal contraceptives have not been established.
Sulfonylureas: Glucose-lowering effect may be potentiated. Effect seen with glibenclamide.
Tetracycline: Acitretin and tetracyclines may both cause increased intracranial pressure; concomitant use is contraindicated.
Vitamin A: Concomitant administration of vitamin A and other systemic retinoids must be avoided due to the risk of possible additive toxic effects.
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Use leads to formation of etretinate, a teratogenic metabolite with a prolonged half-life; concomitant use of ethanol or ethanol-containing products is contraindicated.
PREGNANCY RISK FACTOR — X (show table)
PREGNANCY IMPLICATIONS — Acitretin is teratogenic in humans. Severe birth defects have been reported when conception occurred during treatment or after therapy was complete. Not for use by women who want to become pregnant; patient should not get pregnant for at least 3 years after discontinuation. In addition, because ethanol forms a teratogenic metabolite and would increase the duration of teratogenic potential, ethanol should not be consumed during treatment or for 2 months after discontinuation. Limited amounts of acitretin are found in seminal fluid; although it appears this poses little risk to a fetus, the actual risk of teratogenicity is not known. Any pregnancy which occurs during treatment, or within 3 years after treatment is discontinued, should be reported to the manufacturer at 1-888-500-3376 or to the FDA at 1-800-FDA-1088.
LACTATION — Enters breast milk/not recommended
BREAST-FEEDING CONSIDERATIONS — Acitretin should not be given prior to or during nursing due to the potential for adverse effects in the nursing infant.
DIETARY CONSIDERATIONS — Administer with food. Avoid ingestion of additional sources of exogenous vitamin A (in excess of RDA); use of ethanol and ethanol-containing products is contraindicated.
PRICING — (data from drugstore.com)Capsules (Soriatane) 10 mg (30): $451.54 25 mg (30): $573.49
MONITORING PARAMETERS — Lipid profile (baseline and at 1- to 2-week intervals for 4-8 weeks); liver function tests (baseline, and at 1- to 2-week intervals until stable, then as clinically indicated); blood glucose in patients with diabetes; bone abnormalities (with long-term use)
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms of acute hypervitaminosis A (headache, vertigo) would be expected; vomiting has also been reported. Pregnancy test for women of childbearing age; counseling regarding potential for birth defects and appropriate contraceptive use.
CANADIAN BRAND NAMES — Soriatane®
INTERNATIONAL BRAND NAMES — Neo-Tigason (TH); Neotigason (AN, AR, AT, AU, BB, BE, BF, BG, BJ, BM, BR, BS, BZ, CH, CI, CL, CN, CO, CZ, DE, DK, EC, EE, EG, ES, ET, FI, GB, GH, GM, GN, GY, HU, IE, IL, IT, JM, KE, KR, LR, MA, ML, MR, MU, MW, MX, NE, NG, NL, NO, NZ, PE, PH, PL, PT, PY, SC, SD, SE, SL, SN, SR, TT, TW, TZ, UG, UY, VE, ZA, ZM, ZW); Soriatane (CA, FR)
PHARMACODYNAMICS / KINETICS — Etretinate has been detected in serum for up to 3 years following therapy, possibly due to storage in adipose tissue.
Onset: May take 2-3 months for full effect; improvement may be seen within 8 weeks.
Absorption: Oral: ~72% absorbed when given with food
Protein binding: >99% bound, primarily to albumin
Metabolism: Metabolized to cis-acitretin; both compounds are further metabolized. Concomitant ethanol use leads to the formation of etretinate (active).
Half-life elimination: Acitretin: 49 hours (range: 33-96); cis-acitretin: 63 hours (range: 28-157); etretinate: 120 days (range: 84-168 days)
Excretion: Feces (34% to 54%); urine (16% to 53%)
PATIENT INFORMATION — Take with food. Do not drink alcohol during therapy and for 2 months after discontinuation. Use contraception for 1 month before, during, and for 3 years after discontinuation. You may not be able to tolerate contact lenses during treatment. Do not donate blood during treatment and for 3 years after discontinuation (male and female patients). Avoid exposure to sunlight. Wear protective clothing and sunscreens. Avoid use of other vitamin A products. Females: Use two effective forms of birth control. If you have had your tubes tied, then use an additional form of birth control. If you become pregnant, contact your prescriber immediately.
Acetylcysteine
U.S. BRAND NAMES — Acetadote®
PHARMACOLOGIC CATEGORY AntidoteMucolytic Agent
DOSING: ADULTS Acetaminophen poisoning: Oral: 140 mg/kg; followed by 17 doses of 70 mg/kg every 4 hours; repeat dose if emesis occurs within 1 hour of administration; therapy should continue until acetaminophen levels are undetectable and there is no evidence of hepatotoxicity. I.V. (Acetadote®): Loading dose: 150 mg/kg over 60 minutes; Note: Extended infusion time recommended by manufacturer as of February, 2006. Loading dose is followed by 2 additional infusions: Initial maintenance dose of 50 mg/kg infused over 4 hours, followed by a second maintenance dose of 100 mg/kg infused over 16 hours. Total dosage: 300 mg/kg administered over 21 hours. Patients <40 kg: Reduce fluid volume according to the following table.
Acetadote® Dosing / Fluid Volume Guidelines for Patients <40 kg
Body weight 30 kg: Loading dose (150 mg/kg over 1 hour): Acetadote® 22.5 mL in D5W 100 mL Second dose (50 mg/kg over 4 hours): Acetadote® 7.5 mL in D5W 250 mL Third dose (100 mg/kg over 16 hours): Acetadote® 15 mL in D5W 500 mL
Body weight 25 kg: Loading dose (150 mg/kg over 1 hour): Acetadote® 18.75 mL in D5W 100 mL Second dose (50 mg/kg over 4 hours): Acetadote® 6.25 mL in D5W 250 mL Third dose (100 mg/kg over 16 hours): Acetadote® 12.5 mL in D5W 500 mL
Body weight 20 kg: Loading dose (150 mg/kg over 1 hour): Acetadote® 15 mL in D5W 60 mL Second dose (50 mg/kg over 4 hours): Acetadote® 5 mL in D5W 140 mL Third dose (100 mg/kg over 16 hours): Acetadote® 10 mL in D5W 280 mL
Body weight 15 kg: Loading dose (150 mg/kg over 1 hour): Acetadote® 11.25 mL in D5W 45 mL Second dose (50 mg/kg over 4 hours): Acetadote® 3.75 mL in D5W 105 mL Third dose (100 mg/kg over 16 hours): Acetadote® 7.5 mL in D5W 210 mL
Body weight 10 kg: Loading dose (150 mg/kg over 1 hour): Acetadote® 7.5 mL in D5W 130 mL Second dose (50 mg/kg over 4 hours): Acetadote® 2.5 mL in D5W 70 mL Third dose (100 mg/kg over 16 hours): Acetadote® 5 mL in D5W 140 mL Note: If commercial I.V. form is unavailable, the following dose has been reported using solution for oral inhalation (unlabeled): Loading dose: 140 mg/kg, followed by 70 mg/kg every 4 hours, for a total of 13 doses (loading dose and 48 hours of treatment); infuse each dose over 1 hour through a 0.2 micron Millipore filter (in-line). Experts suggest that the duration of acetylcysteine administration may vary depending upon serial acetaminophen levels and liver function tests obtained during treatment. In general, patients without measurable acetaminophen levels and without significant LFT elevations (>3 times the ULN) can safely stop acetylcysteine after 24 hours of treatment. The patients who still have detectable levels of acetaminophen, and/or LFT elevations (>1000 units/L) continue to benefit from additional acetylcysteine administration.
Adjuvant therapy in respiratory conditions: Note: Patients should receive bronchodilator 15 minutes prior to dose. Inhalation, nebulization (face mask, mouth piece, tracheostomy): Acetylcysteine 10% and 20% solution (dilute 20% solution with sodium chloride or sterile water for inhalation); 10% solution may be used undiluted: 3-5 mL of 20% solution or 6-10 mL of 10% solution until nebulized given 3-4 times/day; dosing range: 1-10 mL of 20% solution or 2-20 mL of 10% solution every 2-6 hours Inhalation, nebulization (tent, croupette): Dose must be individualized; may require up to 300 mL solution/treatment Direct instillation: Into tracheostomy: 1-2 mL of 10% to 20% solution every 1-4 hours Through percutaneous intratracheal catheter: 1-2 mL of 20% or 2-4 mL of 10% solution every 1-4 hours via syringe attached to catheter
Diagnostic bronchogram: Nebulization or intratracheal: 1-2 mL of 20% solution or 2-4 mL of 10% solution administered 2-3 times prior to procedure
Prevention of radiocontrast-induced renal dysfunction (unlabeled use): Oral: 600 mg twice daily for 2 days (beginning the day before the procedure); may be given as powder in capsules, some centers use solution (diluted in cola beverage or juice). Hydrate patient with saline concurrently.
DOSING: PEDIATRIC
(For additional information see "Acetylcysteine: Pediatric drug information")Acetaminophen poisoning: Refer to adult dosing.
Adjuvant therapy in respiratory conditions: Note: Patients should receive an aerosolized bronchodilator 10-15 minutes prior to acetylcysteine Inhalation, nebulization (face mask, mouth piece, tracheostomy): Acetylcysteine 10% and 20% solution (dilute 20% solution with sodium chloride or sterile water for inhalation); 10% solution may be used undiluted. Infants: 1-2 mL of 20% solution or 2-4 mL 10% solution until nebulized given 3-4 times/day Children: Refer to adult dosing. Inhalation, nebulization (tent, croupette): Children: Refer to adult dosing.
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution: Acetadote®: 20% [200 mg/mL] (30 mL) [contains disodium edetate]
Solution, inhalation/oral: 10% [100 mg/mL] (4 mL, 10 mL, 30 mL); 20% [200 mg/mL] (4 mL, 10 mL, 30 mL)
DOSAGE FORMS: CONCISE Injection, solution: Acetadote®: 20% [200 mg/mL] (30 mL)
Solution, inhalation/oral: 10% [100 mg/mL]; 20% [200 mg/mL]
GENERIC EQUIVALENT AVAILABLE — Yes: Solution for inhalation
ADMINISTRATION Inhalation: Acetylcysteine is incompatible with tetracyclines, erythromycin, amphotericin B, iodized oil, chymotrypsin, trypsin, and hydrogen peroxide. Administer separately. Intermittent aerosol treatments are commonly given when patient arises, before meals, and just before retiring at bedtime.
Oral: For treatment of acetaminophen overdosage, administer orally as a 5% solution. Dilute the 20% solution 1:3 with a cola, orange juice, or other soft drink. Use within 1 hour of preparation. Unpleasant odor becomes less noticeable as treatment progresses. If patient vomits within 1 hour of dose, readminister.
I.V.: Intravenous formulation (Acetadote®): Administer loading dose of 150 mg/kg over 60 minutes (see "Note"), followed by 2 separate maintenance infusions: 50 mg/kg over 4 hours followed by 100 mg/kg over 16 hours. If not using commercially available I.V. formulation, use a 0.2-ยต millipore filter (in-line). Note: Extended infusion time recommended by manufacturer as of February, 2006.
COMPATIBILITY Inhalation: Incompatible with rubber and metals (particularly iron, copper, and nickel); do not mix with ampicillin, tetracycline, oxytetracycline, erythromycin.
Intravenous: Compatible with D5W, 1/2NS, SWFI. Incompatible with rubber and metals (particularly iron, copper, and nickel).
USE — Adjunctive mucolytic therapy in patients with abnormal or viscid mucous secretions in acute and chronic bronchopulmonary diseases; pulmonary complications of surgery and cystic fibrosis; diagnostic bronchial studies; antidote for acute acetaminophen toxicity
USE - UNLABELED / INVESTIGATIONAL — Prevention of radiocontrast-induced renal dysfunction (oral, I.V.); distal intestinal obstruction syndrome (DIOS, previously referred to as meconium ileus equivalent)
ADVERSE REACTIONS SIGNIFICANT Inhalation: Frequency not defined. Central nervous system: Drowsiness, chills, fever Gastrointestinal: Vomiting, nausea, stomatitis Local: Irritation, stickiness on face following nebulization Respiratory: Bronchospasm, rhinorrhea, hemoptysis Miscellaneous: Acquired sensitization (rare), clamminess, unpleasant odor during administration
Intravenous:
>10%: Miscellaneous: Anaphylactoid reaction (~17%; reported as severe in 1% or moderate in 10% of patients within 15 minutes of first infusion; severe in 1% or mild to moderate in 6% to 7% of patients after 60-minute infusion)
1% to 10%: Cardiovascular: Angioedema (2% to 8%), vasodilation (1% to 6%), hypotension (1% to 4%), tachycardia (1% to 4%), syncope (1% to 3%), chest tightness (1%), flushing (1%) Central nervous system: Dysphoria (<1% to 2%) Dermatologic: Urticaria (2% to 7%), rash (1% to 5%), facial erythema (1%), palmar erythema (1%), pruritus (1% to 3%), pruritus with rash and vasodilation (2% to 9%) Gastrointestinal: Vomiting (<1% to 10%), nausea (1% to 10%), dyspepsia (1%) Neuromuscular & skeletal: Gait disturbance (<1% to 2%) Ocular: Eye pain (<1% to 3%) Otic: Ear pain (1%) Respiratory: Bronchospasm (1% to 6%), cough (1% to 4%), dyspnea (<1% to 3%), pharyngitis (1%), rhinorrhea (1%), rhonchi (1%), throat tightness (1%) Miscellaneous: Diaphoresis (1%)
CONTRAINDICATIONS — Hypersensitivity to acetylcysteine or any component of the formulation
WARNINGS / PRECAUTIONS Disease-related concerns: Acetaminophen overdose: Appropriate use: The modified Rumack-Matthew nomogram allows for stratification of patients into risk categories based on the relationship between the serum acetaminophen level and time after ingestion. There are several situations where the nomogram is of limited use. Serum acetaminophen levels obtained prior to 4-hour postingestion are not interpretable; patients presenting late may have undetectable serum concentrations, but have received a lethal dose. The nomogram is less predictive in a chronic ingestion or in an overdose with an extended release product. Acetylcysteine should be administered for any signs of hepatotoxicity even if acetaminophen serum level is low or undetectable. The nomogram also does not take into account patients at higher risk of acetaminophen toxicity (eg, alcoholics, malnourished patients).
Dosage form specific issues: Inhalation: Since increased bronchial secretions may develop after inhalation, percussion, postural drainage, and suctioning should follow. If bronchospasm occurs, administer a bronchodilator; discontinue acetylcysteine if bronchospasm progresses. Intravenous: Acute flushing and erythema have been reported; usually occurs within 30-60 minutes and may resolve spontaneously. Serious anaphylactoid reactions have also been reported. Acetylcysteine infusion may be interrupted until treatment of allergic symptoms is initiated; the infusion can then be carefully restarted. Treatment for anaphylactic reactions should be immediately available. Use caution with asthma or history of bronchospasm.
DRUG INTERACTIONS — Adsorbed by activated charcoal; clinical significance is minimal, though, once a pure acetaminophen ingestion requiring N-acetylcysteine is established; further charcoal dosing is unnecessary once the appropriate initial charcoal dose is achieved (5-10 g:g acetaminophen)
PREGNANCY RISK FACTOR — B (show table)
PREGNANCY IMPLICATIONS — Based on limited reports using acetylcysteine to treat acetaminophen overdose in pregnant women, acetylcysteine has been shown to cross the placenta and may provide protective levels in the fetus.
LACTATION — Excretion in breast milk unknown/use caution
PRICING — (data from drugstore.com)Solution (Acetylcysteine) 10% (30): $19.56 20% (4): $7.99 20% (10): $14.99
Solution (Mucomyst) 20% (30): $18.99
Solution (Mucomyst-10) 10% (10): $11.74 10% (30): $18.99
MONITORING PARAMETERS — Acetaminophen overdose: AST, ALT, bilirubin, PT, serum creatinine, BUN, serum glucose, and electrolytes. Acetaminophen levels at ~4 hours postingestion (every 4-6 hours if extended release acetaminophen; plot on the nomogram) and every 4-6 hours to assess serum levels, and LFTs for possible hepatotoxicity. Assess patient for nausea, vomiting, and skin rash following oral administration for treatment of acetaminophen poisoning. If administered I.V., monitor for anaphylaxis/anaphylactoid reactions.
REFERENCE RANGE — Determine acetaminophen level as soon as possible, but no sooner than 4 hours after ingestion (to ensure peak levels have been obtained); administer for acetaminophen level >150 mcg/mL at 4 hours following ingestion; toxic concentration with probable hepatotoxicity: >200 mcg/mL at 4 hours or 50 mcg at 12 hours
TOXICOLOGY / OVERDOSE COMPREHENSIVE — The treatment of acetylcysteine toxicity is usually aimed at reversing anaphylactoid symptoms or controlling nausea and vomiting. The use of epinephrine, antihistamines, and steroids may be beneficial.
CANADIAN BRAND NAMES — Acetylcysteine Solution; Mucomyst®; Parvolex®
INTERNATIONAL BRAND NAMES — ACC (MX, PL); ACC 200 (EE, HU); Acetain (KR); Acetylcysteine Solution (CA); Acypront (HK, PL); Alveolex (IE); Bromuc (BR); Drenaflen (EC); Ecomucyl (CH); Eloamin (CZ); Exomuc (FR, HK); Fabrol (AT, GR); Flemex AC (TH); Fluimicil (CH); Fluimucil (BR, CN, CO, EC, HK, ID, MA, NL, PE, PL, SG, TH, TW); Fluimucil A (MY, PK); Fluimukan (HR); Flutafin (TW); Hidonac (ID, PH, TH); Libramucil (EC); Menaxol (CR, DO, GT, HN, NI, PA, SV); Mucofillin (JP); Mucolator (MY); Mucolitico (CL); Mucomiste (PT); Mucomyst (AT, AU, BE, CA, DK, FI, FR, KR, NL); Mucoserin (KR); Mucosof (CN); Mucosten (KR); Mucosys (IN); Mucoza (TH); Mukolit (ID); Muteran (KR); Parvolex (CA, GB, IE, NZ, PH); Parvolex DBL (MY); Reolin (IL); Simucin (TH); Siran 200 (IL); Solmucol (SG); Spatam (SG); Stecin (KR); Syntemucol (PL); Tussicom (PL); Zifluvis (CO)
MECHANISM OF ACTION — Exerts mucolytic action through its free sulfhydryl group which opens up the disulfide bonds in the mucoproteins thus lowering mucous viscosity. The exact mechanism of action in acetaminophen toxicity is unknown; thought to act by providing substrate for conjugation with the toxic metabolite.
PHARMACODYNAMICS / KINETICS Onset of action: Inhalation: 5-10 minutes
Duration: Inhalation: >1 hour
Distribution: 0.47 L/kg
Protein binding, plasma: 83%
Half-life elimination: Reduced acetylcysteine: 2 hours Total acetylcysteine: Adults: 5.5 hours; Newborns: 11 hours
Time to peak, plasma: Oral: 1-2 hours
Excretion: Urine
PATIENT INFORMATION — Clear airway by coughing deeply before using aerosol.
(For additional information see "Acetylcysteine: Patient drug information")
PHARMACOLOGIC CATEGORY AntidoteMucolytic Agent
DOSING: ADULTS Acetaminophen poisoning: Oral: 140 mg/kg; followed by 17 doses of 70 mg/kg every 4 hours; repeat dose if emesis occurs within 1 hour of administration; therapy should continue until acetaminophen levels are undetectable and there is no evidence of hepatotoxicity. I.V. (Acetadote®): Loading dose: 150 mg/kg over 60 minutes; Note: Extended infusion time recommended by manufacturer as of February, 2006. Loading dose is followed by 2 additional infusions: Initial maintenance dose of 50 mg/kg infused over 4 hours, followed by a second maintenance dose of 100 mg/kg infused over 16 hours. Total dosage: 300 mg/kg administered over 21 hours. Patients <40 kg: Reduce fluid volume according to the following table.
Acetadote® Dosing / Fluid Volume Guidelines for Patients <40 kg
Body weight 30 kg: Loading dose (150 mg/kg over 1 hour): Acetadote® 22.5 mL in D5W 100 mL Second dose (50 mg/kg over 4 hours): Acetadote® 7.5 mL in D5W 250 mL Third dose (100 mg/kg over 16 hours): Acetadote® 15 mL in D5W 500 mL
Body weight 25 kg: Loading dose (150 mg/kg over 1 hour): Acetadote® 18.75 mL in D5W 100 mL Second dose (50 mg/kg over 4 hours): Acetadote® 6.25 mL in D5W 250 mL Third dose (100 mg/kg over 16 hours): Acetadote® 12.5 mL in D5W 500 mL
Body weight 20 kg: Loading dose (150 mg/kg over 1 hour): Acetadote® 15 mL in D5W 60 mL Second dose (50 mg/kg over 4 hours): Acetadote® 5 mL in D5W 140 mL Third dose (100 mg/kg over 16 hours): Acetadote® 10 mL in D5W 280 mL
Body weight 15 kg: Loading dose (150 mg/kg over 1 hour): Acetadote® 11.25 mL in D5W 45 mL Second dose (50 mg/kg over 4 hours): Acetadote® 3.75 mL in D5W 105 mL Third dose (100 mg/kg over 16 hours): Acetadote® 7.5 mL in D5W 210 mL
Body weight 10 kg: Loading dose (150 mg/kg over 1 hour): Acetadote® 7.5 mL in D5W 130 mL Second dose (50 mg/kg over 4 hours): Acetadote® 2.5 mL in D5W 70 mL Third dose (100 mg/kg over 16 hours): Acetadote® 5 mL in D5W 140 mL Note: If commercial I.V. form is unavailable, the following dose has been reported using solution for oral inhalation (unlabeled): Loading dose: 140 mg/kg, followed by 70 mg/kg every 4 hours, for a total of 13 doses (loading dose and 48 hours of treatment); infuse each dose over 1 hour through a 0.2 micron Millipore filter (in-line). Experts suggest that the duration of acetylcysteine administration may vary depending upon serial acetaminophen levels and liver function tests obtained during treatment. In general, patients without measurable acetaminophen levels and without significant LFT elevations (>3 times the ULN) can safely stop acetylcysteine after 24 hours of treatment. The patients who still have detectable levels of acetaminophen, and/or LFT elevations (>1000 units/L) continue to benefit from additional acetylcysteine administration.
Adjuvant therapy in respiratory conditions: Note: Patients should receive bronchodilator 15 minutes prior to dose. Inhalation, nebulization (face mask, mouth piece, tracheostomy): Acetylcysteine 10% and 20% solution (dilute 20% solution with sodium chloride or sterile water for inhalation); 10% solution may be used undiluted: 3-5 mL of 20% solution or 6-10 mL of 10% solution until nebulized given 3-4 times/day; dosing range: 1-10 mL of 20% solution or 2-20 mL of 10% solution every 2-6 hours Inhalation, nebulization (tent, croupette): Dose must be individualized; may require up to 300 mL solution/treatment Direct instillation: Into tracheostomy: 1-2 mL of 10% to 20% solution every 1-4 hours Through percutaneous intratracheal catheter: 1-2 mL of 20% or 2-4 mL of 10% solution every 1-4 hours via syringe attached to catheter
Diagnostic bronchogram: Nebulization or intratracheal: 1-2 mL of 20% solution or 2-4 mL of 10% solution administered 2-3 times prior to procedure
Prevention of radiocontrast-induced renal dysfunction (unlabeled use): Oral: 600 mg twice daily for 2 days (beginning the day before the procedure); may be given as powder in capsules, some centers use solution (diluted in cola beverage or juice). Hydrate patient with saline concurrently.
DOSING: PEDIATRIC
(For additional information see "Acetylcysteine: Pediatric drug information")Acetaminophen poisoning: Refer to adult dosing.
Adjuvant therapy in respiratory conditions: Note: Patients should receive an aerosolized bronchodilator 10-15 minutes prior to acetylcysteine Inhalation, nebulization (face mask, mouth piece, tracheostomy): Acetylcysteine 10% and 20% solution (dilute 20% solution with sodium chloride or sterile water for inhalation); 10% solution may be used undiluted. Infants: 1-2 mL of 20% solution or 2-4 mL 10% solution until nebulized given 3-4 times/day Children: Refer to adult dosing. Inhalation, nebulization (tent, croupette): Children: Refer to adult dosing.
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution: Acetadote®: 20% [200 mg/mL] (30 mL) [contains disodium edetate]
Solution, inhalation/oral: 10% [100 mg/mL] (4 mL, 10 mL, 30 mL); 20% [200 mg/mL] (4 mL, 10 mL, 30 mL)
DOSAGE FORMS: CONCISE Injection, solution: Acetadote®: 20% [200 mg/mL] (30 mL)
Solution, inhalation/oral: 10% [100 mg/mL]; 20% [200 mg/mL]
GENERIC EQUIVALENT AVAILABLE — Yes: Solution for inhalation
ADMINISTRATION Inhalation: Acetylcysteine is incompatible with tetracyclines, erythromycin, amphotericin B, iodized oil, chymotrypsin, trypsin, and hydrogen peroxide. Administer separately. Intermittent aerosol treatments are commonly given when patient arises, before meals, and just before retiring at bedtime.
Oral: For treatment of acetaminophen overdosage, administer orally as a 5% solution. Dilute the 20% solution 1:3 with a cola, orange juice, or other soft drink. Use within 1 hour of preparation. Unpleasant odor becomes less noticeable as treatment progresses. If patient vomits within 1 hour of dose, readminister.
I.V.: Intravenous formulation (Acetadote®): Administer loading dose of 150 mg/kg over 60 minutes (see "Note"), followed by 2 separate maintenance infusions: 50 mg/kg over 4 hours followed by 100 mg/kg over 16 hours. If not using commercially available I.V. formulation, use a 0.2-ยต millipore filter (in-line). Note: Extended infusion time recommended by manufacturer as of February, 2006.
COMPATIBILITY Inhalation: Incompatible with rubber and metals (particularly iron, copper, and nickel); do not mix with ampicillin, tetracycline, oxytetracycline, erythromycin.
Intravenous: Compatible with D5W, 1/2NS, SWFI. Incompatible with rubber and metals (particularly iron, copper, and nickel).
USE — Adjunctive mucolytic therapy in patients with abnormal or viscid mucous secretions in acute and chronic bronchopulmonary diseases; pulmonary complications of surgery and cystic fibrosis; diagnostic bronchial studies; antidote for acute acetaminophen toxicity
USE - UNLABELED / INVESTIGATIONAL — Prevention of radiocontrast-induced renal dysfunction (oral, I.V.); distal intestinal obstruction syndrome (DIOS, previously referred to as meconium ileus equivalent)
ADVERSE REACTIONS SIGNIFICANT Inhalation: Frequency not defined. Central nervous system: Drowsiness, chills, fever Gastrointestinal: Vomiting, nausea, stomatitis Local: Irritation, stickiness on face following nebulization Respiratory: Bronchospasm, rhinorrhea, hemoptysis Miscellaneous: Acquired sensitization (rare), clamminess, unpleasant odor during administration
Intravenous:
>10%: Miscellaneous: Anaphylactoid reaction (~17%; reported as severe in 1% or moderate in 10% of patients within 15 minutes of first infusion; severe in 1% or mild to moderate in 6% to 7% of patients after 60-minute infusion)
1% to 10%: Cardiovascular: Angioedema (2% to 8%), vasodilation (1% to 6%), hypotension (1% to 4%), tachycardia (1% to 4%), syncope (1% to 3%), chest tightness (1%), flushing (1%) Central nervous system: Dysphoria (<1% to 2%) Dermatologic: Urticaria (2% to 7%), rash (1% to 5%), facial erythema (1%), palmar erythema (1%), pruritus (1% to 3%), pruritus with rash and vasodilation (2% to 9%) Gastrointestinal: Vomiting (<1% to 10%), nausea (1% to 10%), dyspepsia (1%) Neuromuscular & skeletal: Gait disturbance (<1% to 2%) Ocular: Eye pain (<1% to 3%) Otic: Ear pain (1%) Respiratory: Bronchospasm (1% to 6%), cough (1% to 4%), dyspnea (<1% to 3%), pharyngitis (1%), rhinorrhea (1%), rhonchi (1%), throat tightness (1%) Miscellaneous: Diaphoresis (1%)
CONTRAINDICATIONS — Hypersensitivity to acetylcysteine or any component of the formulation
WARNINGS / PRECAUTIONS Disease-related concerns: Acetaminophen overdose: Appropriate use: The modified Rumack-Matthew nomogram allows for stratification of patients into risk categories based on the relationship between the serum acetaminophen level and time after ingestion. There are several situations where the nomogram is of limited use. Serum acetaminophen levels obtained prior to 4-hour postingestion are not interpretable; patients presenting late may have undetectable serum concentrations, but have received a lethal dose. The nomogram is less predictive in a chronic ingestion or in an overdose with an extended release product. Acetylcysteine should be administered for any signs of hepatotoxicity even if acetaminophen serum level is low or undetectable. The nomogram also does not take into account patients at higher risk of acetaminophen toxicity (eg, alcoholics, malnourished patients).
Dosage form specific issues: Inhalation: Since increased bronchial secretions may develop after inhalation, percussion, postural drainage, and suctioning should follow. If bronchospasm occurs, administer a bronchodilator; discontinue acetylcysteine if bronchospasm progresses. Intravenous: Acute flushing and erythema have been reported; usually occurs within 30-60 minutes and may resolve spontaneously. Serious anaphylactoid reactions have also been reported. Acetylcysteine infusion may be interrupted until treatment of allergic symptoms is initiated; the infusion can then be carefully restarted. Treatment for anaphylactic reactions should be immediately available. Use caution with asthma or history of bronchospasm.
DRUG INTERACTIONS — Adsorbed by activated charcoal; clinical significance is minimal, though, once a pure acetaminophen ingestion requiring N-acetylcysteine is established; further charcoal dosing is unnecessary once the appropriate initial charcoal dose is achieved (5-10 g:g acetaminophen)
PREGNANCY RISK FACTOR — B (show table)
PREGNANCY IMPLICATIONS — Based on limited reports using acetylcysteine to treat acetaminophen overdose in pregnant women, acetylcysteine has been shown to cross the placenta and may provide protective levels in the fetus.
LACTATION — Excretion in breast milk unknown/use caution
PRICING — (data from drugstore.com)Solution (Acetylcysteine) 10% (30): $19.56 20% (4): $7.99 20% (10): $14.99
Solution (Mucomyst) 20% (30): $18.99
Solution (Mucomyst-10) 10% (10): $11.74 10% (30): $18.99
MONITORING PARAMETERS — Acetaminophen overdose: AST, ALT, bilirubin, PT, serum creatinine, BUN, serum glucose, and electrolytes. Acetaminophen levels at ~4 hours postingestion (every 4-6 hours if extended release acetaminophen; plot on the nomogram) and every 4-6 hours to assess serum levels, and LFTs for possible hepatotoxicity. Assess patient for nausea, vomiting, and skin rash following oral administration for treatment of acetaminophen poisoning. If administered I.V., monitor for anaphylaxis/anaphylactoid reactions.
REFERENCE RANGE — Determine acetaminophen level as soon as possible, but no sooner than 4 hours after ingestion (to ensure peak levels have been obtained); administer for acetaminophen level >150 mcg/mL at 4 hours following ingestion; toxic concentration with probable hepatotoxicity: >200 mcg/mL at 4 hours or 50 mcg at 12 hours
TOXICOLOGY / OVERDOSE COMPREHENSIVE — The treatment of acetylcysteine toxicity is usually aimed at reversing anaphylactoid symptoms or controlling nausea and vomiting. The use of epinephrine, antihistamines, and steroids may be beneficial.
CANADIAN BRAND NAMES — Acetylcysteine Solution; Mucomyst®; Parvolex®
INTERNATIONAL BRAND NAMES — ACC (MX, PL); ACC 200 (EE, HU); Acetain (KR); Acetylcysteine Solution (CA); Acypront (HK, PL); Alveolex (IE); Bromuc (BR); Drenaflen (EC); Ecomucyl (CH); Eloamin (CZ); Exomuc (FR, HK); Fabrol (AT, GR); Flemex AC (TH); Fluimicil (CH); Fluimucil (BR, CN, CO, EC, HK, ID, MA, NL, PE, PL, SG, TH, TW); Fluimucil A (MY, PK); Fluimukan (HR); Flutafin (TW); Hidonac (ID, PH, TH); Libramucil (EC); Menaxol (CR, DO, GT, HN, NI, PA, SV); Mucofillin (JP); Mucolator (MY); Mucolitico (CL); Mucomiste (PT); Mucomyst (AT, AU, BE, CA, DK, FI, FR, KR, NL); Mucoserin (KR); Mucosof (CN); Mucosten (KR); Mucosys (IN); Mucoza (TH); Mukolit (ID); Muteran (KR); Parvolex (CA, GB, IE, NZ, PH); Parvolex DBL (MY); Reolin (IL); Simucin (TH); Siran 200 (IL); Solmucol (SG); Spatam (SG); Stecin (KR); Syntemucol (PL); Tussicom (PL); Zifluvis (CO)
MECHANISM OF ACTION — Exerts mucolytic action through its free sulfhydryl group which opens up the disulfide bonds in the mucoproteins thus lowering mucous viscosity. The exact mechanism of action in acetaminophen toxicity is unknown; thought to act by providing substrate for conjugation with the toxic metabolite.
PHARMACODYNAMICS / KINETICS Onset of action: Inhalation: 5-10 minutes
Duration: Inhalation: >1 hour
Distribution: 0.47 L/kg
Protein binding, plasma: 83%
Half-life elimination: Reduced acetylcysteine: 2 hours Total acetylcysteine: Adults: 5.5 hours; Newborns: 11 hours
Time to peak, plasma: Oral: 1-2 hours
Excretion: Urine
PATIENT INFORMATION — Clear airway by coughing deeply before using aerosol.
(For additional information see "Acetylcysteine: Patient drug information")
Acetylcholine
U.S. BRAND NAMES — Miochol®-E
PHARMACOLOGIC CATEGORY Cholinergic AgonistOphthalmic Agent, Miotic
DOSING: ADULTS — To produce miosis: Intraocular: 0.5-2 mL of 1% injection (5-20 mg) instilled into anterior chamber before or after securing one or more sutures
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Powder for solution, intraocular, as chloride: Miochol®-E: 1:100 [20 mg; packaged with diluent (2 mL)]
DOSAGE FORMS: CONCISE Powder for intraocular solution: Miochol®-E: 1:100 [20 mg; packaged with diluent (2 mL)]
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Open under aseptic conditions only. Attach filter before irrigating eye.
USE — Produces complete miosis in cataract surgery, keratoplasty, iridectomy, and other anterior segment surgery where rapid miosis is required
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Cardiovascular: Bradycardia, flushing, hypotension
Central nervous system: Headache
Ocular: Clouding, corneal edema, decompensation
Respiratory: Dyspnea
Miscellaneous: Diaphoresis
CONTRAINDICATIONS — Hypersensitivity to acetylcholine chloride or any component of the formulation; acute iritis and acute inflammatory disease of the anterior chamber
WARNINGS / PRECAUTIONS — During cataract surgery, use only after lens is in place. Systemic effects rarely occur but can cause problems for patients with acute cardiac failure, bronchial asthma, peptic ulcer, hyperthyroidism, GI spasm, urinary tract obstruction, and Parkinson's disease; open under aseptic conditions only.
DRUG INTERACTIONS Decreased effect possible with flurbiprofen and suprofen, ophthalmic.
Increased effect may be prolonged or enhanced in patients receiving tacrine.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Acetylcholine is used primarily in the eye and there are no reports of its use in pregnancy. Because it is ionized at physiologic pH, transplacental passage would not be expected.
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Treatment includes flushing eyes with water or normal saline and supportive measures. If accidentally ingested, induce emesis or perform gastric lavage.
CANADIAN BRAND NAMES — Miochol®-E
INTERNATIONAL BRAND NAMES — Miochol (AU, BE, FI, NL, NZ); Miochol-E (AU, CA, CL, DE, GB, HK, ID, IE, IL, KR, NL, NZ, SG)
MECHANISM OF ACTION — Causes contraction of the sphincter muscles of the iris, resulting in miosis and contraction of the ciliary muscle, leading to accommodation spasm
PHARMACODYNAMICS / KINETICS Onset of action: Rapid
Duration: ~10 minutes
PATIENT INFORMATION — Do not touch dropper to eye. May sting on instillation. Use caution while driving at night or performing hazardous tasks.
(For additional information see "Acetylcholine: Patient drug information")
PHARMACOLOGIC CATEGORY Cholinergic AgonistOphthalmic Agent, Miotic
DOSING: ADULTS — To produce miosis: Intraocular: 0.5-2 mL of 1% injection (5-20 mg) instilled into anterior chamber before or after securing one or more sutures
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Powder for solution, intraocular, as chloride: Miochol®-E: 1:100 [20 mg; packaged with diluent (2 mL)]
DOSAGE FORMS: CONCISE Powder for intraocular solution: Miochol®-E: 1:100 [20 mg; packaged with diluent (2 mL)]
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Open under aseptic conditions only. Attach filter before irrigating eye.
USE — Produces complete miosis in cataract surgery, keratoplasty, iridectomy, and other anterior segment surgery where rapid miosis is required
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Cardiovascular: Bradycardia, flushing, hypotension
Central nervous system: Headache
Ocular: Clouding, corneal edema, decompensation
Respiratory: Dyspnea
Miscellaneous: Diaphoresis
CONTRAINDICATIONS — Hypersensitivity to acetylcholine chloride or any component of the formulation; acute iritis and acute inflammatory disease of the anterior chamber
WARNINGS / PRECAUTIONS — During cataract surgery, use only after lens is in place. Systemic effects rarely occur but can cause problems for patients with acute cardiac failure, bronchial asthma, peptic ulcer, hyperthyroidism, GI spasm, urinary tract obstruction, and Parkinson's disease; open under aseptic conditions only.
DRUG INTERACTIONS Decreased effect possible with flurbiprofen and suprofen, ophthalmic.
Increased effect may be prolonged or enhanced in patients receiving tacrine.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Acetylcholine is used primarily in the eye and there are no reports of its use in pregnancy. Because it is ionized at physiologic pH, transplacental passage would not be expected.
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Treatment includes flushing eyes with water or normal saline and supportive measures. If accidentally ingested, induce emesis or perform gastric lavage.
CANADIAN BRAND NAMES — Miochol®-E
INTERNATIONAL BRAND NAMES — Miochol (AU, BE, FI, NL, NZ); Miochol-E (AU, CA, CL, DE, GB, HK, ID, IE, IL, KR, NL, NZ, SG)
MECHANISM OF ACTION — Causes contraction of the sphincter muscles of the iris, resulting in miosis and contraction of the ciliary muscle, leading to accommodation spasm
PHARMACODYNAMICS / KINETICS Onset of action: Rapid
Duration: ~10 minutes
PATIENT INFORMATION — Do not touch dropper to eye. May sting on instillation. Use caution while driving at night or performing hazardous tasks.
(For additional information see "Acetylcholine: Patient drug information")
Acetohydroxamic acid:
U.S. BRAND NAMES — Lithostat®
PHARMACOLOGIC CATEGORY Urinary Tract Product
DOSING: ADULTS — Susceptible infections: Oral: 250 mg 3-4 times/day for a total daily dose of 10-15 mg/kg/day
DOSING: PEDIATRIC — Susceptible infections: Oral: Initial: 10 mg/kg/day
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Not recommended for use in significant renal impairment (Srcr >2.5 mg/dL).
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet: 250 mg
DOSAGE FORMS: CONCISE Tablet: Lithostat®: 250 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Should be administered on an empty stomach.
USE — Adjunctive therapy in chronic urea-splitting urinary infection
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Cardiovascular: Deep vein thrombosis (rare), embolism, palpitation, phlebitis
Central nervous system: Anorexia, anxiety, depression, headache, malaise, nervousness, tremor
Dermatologic: Flushing (with ethanol consumption), rash (nonpruritic, macular)
Gastrointestinal: Nausea, vomiting
Hematologic: Hemolytic anemia (15% with laboratory evidence; ~3% severe requiring discontinuation; may be accompanied by GI symptoms or systemic complaints of malaise and/or fatigue); hyperbilirubinemia
Respiratory: Pulmonary embolism (rare)
CONTRAINDICATIONS — Hypersensitivity to acetohydroxamic acid or any component of the formulation; pregnancy
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Bone marrow suppression: May suppress bone marrow function; use with caution in patients with prior bone marrow depression. Close monitoring of hematologic function is recommended. Hemolytic anemia: Has been associated with hemolytic anemia (Coombs' negative), which may be associated with gastrointestinal distress and systemic symptoms; use with caution in patients with anemia. Monitor hematologic parameters during extended therapy. Hepatotoxicity: May cause hepatic injury; close monitoring of hepatic function is recommended.
Disease-related concerns: Psychiatric disorders: Use with caution in patients with pre-existing psychiatric disorders; may be associated with nervousness, anxiety, and/or depression.
DRUG INTERACTIONS Calcium and/or magnesium products: Acetohydroxamic acid may chelate divalent metals, decreasing the absorption of both agents; avoid concurrent use.
Iron: Orally-administered iron may be chelated by acetohydroxamic acid, decreasing the absorption of both agents. To treat hypochromic anemia, parenteral iron should be used.
ETHANOL / NUTRITION / HERB INTERACTIONS Ethanol: Avoid ethanol (may increase incidence of rash and/or flushing).
Food: May decrease absorption of acetohydroxamic acid.
PREGNANCY RISK FACTOR — X (show table)
LACTATION — Excretion in breast milk unknown/not recommended
DIETARY CONSIDERATIONS — Should be taken on an empty stomach, 1 hour before or 2 hours after meals.
PRICING — (data from drugstore.com)Tablets (Lithostat) 250 mg (100): $143.36
MONITORING PARAMETERS — In patients receiving therapy >2 weeks, monitor CBC with reticulocytes at 3-month intervals during the duration of treatment.
CANADIAN BRAND NAMES — Lithostat®
INTERNATIONAL BRAND NAMES — Lithostat (CA)
MECHANISM OF ACTION — Acetohydroxamic acid inhibits bacterial urease enzymes, decreasing the formation of ammonia in the urine by urea-splitting organisms. A reduction in urinary ammonia may increase the antibacterial activity of some antibiotic agents.
PHARMACOLOGIC CATEGORY Urinary Tract Product
DOSING: ADULTS — Susceptible infections: Oral: 250 mg 3-4 times/day for a total daily dose of 10-15 mg/kg/day
DOSING: PEDIATRIC — Susceptible infections: Oral: Initial: 10 mg/kg/day
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Not recommended for use in significant renal impairment (Srcr >2.5 mg/dL).
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet: 250 mg
DOSAGE FORMS: CONCISE Tablet: Lithostat®: 250 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Should be administered on an empty stomach.
USE — Adjunctive therapy in chronic urea-splitting urinary infection
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Cardiovascular: Deep vein thrombosis (rare), embolism, palpitation, phlebitis
Central nervous system: Anorexia, anxiety, depression, headache, malaise, nervousness, tremor
Dermatologic: Flushing (with ethanol consumption), rash (nonpruritic, macular)
Gastrointestinal: Nausea, vomiting
Hematologic: Hemolytic anemia (15% with laboratory evidence; ~3% severe requiring discontinuation; may be accompanied by GI symptoms or systemic complaints of malaise and/or fatigue); hyperbilirubinemia
Respiratory: Pulmonary embolism (rare)
CONTRAINDICATIONS — Hypersensitivity to acetohydroxamic acid or any component of the formulation; pregnancy
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Bone marrow suppression: May suppress bone marrow function; use with caution in patients with prior bone marrow depression. Close monitoring of hematologic function is recommended. Hemolytic anemia: Has been associated with hemolytic anemia (Coombs' negative), which may be associated with gastrointestinal distress and systemic symptoms; use with caution in patients with anemia. Monitor hematologic parameters during extended therapy. Hepatotoxicity: May cause hepatic injury; close monitoring of hepatic function is recommended.
Disease-related concerns: Psychiatric disorders: Use with caution in patients with pre-existing psychiatric disorders; may be associated with nervousness, anxiety, and/or depression.
DRUG INTERACTIONS Calcium and/or magnesium products: Acetohydroxamic acid may chelate divalent metals, decreasing the absorption of both agents; avoid concurrent use.
Iron: Orally-administered iron may be chelated by acetohydroxamic acid, decreasing the absorption of both agents. To treat hypochromic anemia, parenteral iron should be used.
ETHANOL / NUTRITION / HERB INTERACTIONS Ethanol: Avoid ethanol (may increase incidence of rash and/or flushing).
Food: May decrease absorption of acetohydroxamic acid.
PREGNANCY RISK FACTOR — X (show table)
LACTATION — Excretion in breast milk unknown/not recommended
DIETARY CONSIDERATIONS — Should be taken on an empty stomach, 1 hour before or 2 hours after meals.
PRICING — (data from drugstore.com)Tablets (Lithostat) 250 mg (100): $143.36
MONITORING PARAMETERS — In patients receiving therapy >2 weeks, monitor CBC with reticulocytes at 3-month intervals during the duration of treatment.
CANADIAN BRAND NAMES — Lithostat®
INTERNATIONAL BRAND NAMES — Lithostat (CA)
MECHANISM OF ACTION — Acetohydroxamic acid inhibits bacterial urease enzymes, decreasing the formation of ammonia in the urine by urea-splitting organisms. A reduction in urinary ammonia may increase the antibacterial activity of some antibiotic agents.
Acetic acid, propylene glycol diacetate, and hydrocortisone
U.S. BRAND NAMES — Acetasol® HC; VoSol® HC
PHARMACOLOGIC CATEGORY Otic Agent, Anti-infective
DOSING: ADULTS — Otitis externa (superficial): Otic: Instill 3-5 drops in ear(s) every 4-6 hours
DOSING: PEDIATRIC — Children 3 years: Refer to adult dosing.
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, otic drops: Acetic acid 2%, propylene glycol diacetate 3%, and hydrocortisone 1% (10 mL)
DOSAGE FORMS: CONCISE Solution, otic drops: Acetic acid 2%, propylene glycol diacetate 3%, and hydrocortisone 1% (10 mL) Acetasol® HC, VoSol® HC: Acetic acid 2%, propylene glycol diacetate 3%, and hydrocortisone 1% (10 mL)
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — After removing cerumen and debris, solution may be applied by inserting a cotton wick into the ear canal and saturating with the solution. Wick may remain in place for 24 hours and then removed; however, drops should continue to be instilled into ear canal as long as indicated.
USE — Treatment of superficial infections of the external auditory canal caused by organisms susceptible to the action of the antimicrobial, complicated by swelling
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined: Otic: Transient burning or stinging may be noticed occasionally when the solution is first instilled into the acutely inflamed ear
CONTRAINDICATIONS — Hypersensitivity to acetic acid, propylene glycol, hydrocortisone, or any component of the formulation; perforated tympanic membrane; herpes simplex; vaccinia, and varicella
DRUG INTERACTIONS — Hydrocortisone: Substrate of CYP3A4 (minor); Induces CYP3A4 (weak)
PRICING — (data from drugstore.com)Solution (Acetasol HC) 2-1% (10): $16.07
PATIENT INFORMATION — See individual agents for Acetic Acid and Hydrocortisone.
(For additional information see "Acetic acid, propylene glycol diacetate, and hydrocortisone: Patient drug information")
PHARMACOLOGIC CATEGORY Otic Agent, Anti-infective
DOSING: ADULTS — Otitis externa (superficial): Otic: Instill 3-5 drops in ear(s) every 4-6 hours
DOSING: PEDIATRIC — Children 3 years: Refer to adult dosing.
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, otic drops: Acetic acid 2%, propylene glycol diacetate 3%, and hydrocortisone 1% (10 mL)
DOSAGE FORMS: CONCISE Solution, otic drops: Acetic acid 2%, propylene glycol diacetate 3%, and hydrocortisone 1% (10 mL) Acetasol® HC, VoSol® HC: Acetic acid 2%, propylene glycol diacetate 3%, and hydrocortisone 1% (10 mL)
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — After removing cerumen and debris, solution may be applied by inserting a cotton wick into the ear canal and saturating with the solution. Wick may remain in place for 24 hours and then removed; however, drops should continue to be instilled into ear canal as long as indicated.
USE — Treatment of superficial infections of the external auditory canal caused by organisms susceptible to the action of the antimicrobial, complicated by swelling
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined: Otic: Transient burning or stinging may be noticed occasionally when the solution is first instilled into the acutely inflamed ear
CONTRAINDICATIONS — Hypersensitivity to acetic acid, propylene glycol, hydrocortisone, or any component of the formulation; perforated tympanic membrane; herpes simplex; vaccinia, and varicella
DRUG INTERACTIONS — Hydrocortisone: Substrate of CYP3A4 (minor); Induces CYP3A4 (weak)
PRICING — (data from drugstore.com)Solution (Acetasol HC) 2-1% (10): $16.07
PATIENT INFORMATION — See individual agents for Acetic Acid and Hydrocortisone.
(For additional information see "Acetic acid, propylene glycol diacetate, and hydrocortisone: Patient drug information")
Subscribe to:
Posts (Atom)