Amprenavir


Concise Prescribing Info
Indications/Uses
HIV infection.
Dosage/Direction for Use
Adult : PO Combined w/ other antiretrovirals: As cap: 1.2 g twice daily, w/ ritonavir: 600 mg twice daily; soln: 17 mg/kg 3 times/day. Max: 2.8 g/day.
Dosage Details
Oral
HIV infection
Adult: Combined with other antiretrovirals: Capsule: 1,200 mg bid (600 mg bid when used with ritonavir); solution: 17 mg/kg tid. Max: 2.8 g/day.
Child: Combined with other antiretrovirals: Capsule: 4-12 yr and <50 kg: 20 mg/kg bid or 15 mg/kg tid (max: 2.4 g/day); Oral solution: 4-12 yr and <50 kg: 22.5 mg/kg bid or 17 mg/kg tid (max: 2.8 g/day).
Hepatic Impairment
Do not use oral solution. Capsules: moderate impairment (Child-Pugh score 5-8): 450 mg bid and severe impairment (Child-Pugh score 9-12): 300 mg bid.
Administration
May be taken with or without food. Do not take w/ high fat meal.
Contraindications
Hypersensitivity; sulfonamide allergy. Oral solution: Infants, child <4 yr old; renal or hepatic failure; concomitant metronidazole or disulfiram therapy. Pregnancy and lactation.
Special Precautions
Elderly; renal impairment, hepatic impairment, DM, haemophilia; sensitivity to sulfonamides; use of sildenafil, vitamin E supplements. Always use with other antiretroviral agents in HIV treatment. Use oral solution only when capsule and other protease inhibitors are not therapeutic options. Capsule and oral solution not interchangeable on a mg-per-mg basis. Monitor for propylene glycol-associated adverse effect when oral solution is admin.
Adverse Reactions
Tremors, oral or perioral paraesthesia; mood disorders, dyslipidaemia, redistribution of body fat causing "protease paunch", buffalo hump, facial atrophy and breast enlargement; rash; GI effects e.g. nausea, vomiting and diarrhoea.
Potentially Fatal: Hypersensitivity, Stevens-Johnson syndrome and acute haemolytic anaemia.
Overdosage
Monitor patient and institute supportive care as necessary.
Drug Interactions
Clorazepate, alprazolam, diazepam, erythromycin and midazolam increase risk of prolonged sedation and respiratory depression. Plasma concentrations of cilostazol, rifabutin, sertindole and terfenadine (risk of ventricular arrhythmias), sildenafil, antiarrhythmics may be increased. May increase warfarin effects. St. John's wort. Ethanol. Oestrogens; dexamethasone; delavirdine; efavirenz and veriparine; methadone.
Potentially Fatal: Drugs with narrow therapeutic index e.g. cisapride and terfenadine, pimozide, guanidine and rifampicin. Ergot alkaloids; lovastatin and simvastatin.
Food Interaction
High fat meals increase amprenavir levels by about 6-folds.
Action
Description: Amprenavir, a selective, competitive, reversible inhibitor of HIV-1 protease, inhibits the cleavage of viral polyprotein precursors into individual functional proteins found, thus forming immature, noninfectious viral particles.
Pharmacokinetics:
Absorption: Rapidly absorbed. Takes about 1-2 hr to reach peak plasma concentrations after an oral dose.
Distribution: 90% bound to plasma proteins.
Metabolism: Metabolised by liver cytochrome CYP3A4.
Excretion: Elimination half-life: about 7.1-10.6 hr. Mainly excreted as metabolites in faeces (about 75%).
Storage
Store at 25°C.
MIMS Class
Disclaimer: This information is independently developed by MIMS based on Amprenavir from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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