amprenavir (Agenerase)
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Introduction
Tradename: Agenerase.
Indications
Dosage
Capsules: 50 & 150 mg.
Each 150 mg capsule of Agenerase contains 109 IU of vitamin E
Solution: 15 mg/mL, containing 46 IU of vitamin E/mL
Pharmacokinetics
- rapidly absorbed after oral administration
- peak serum concentration 1-2 hours after oral administration
- may be taken with or without food, avoid high fat meals
- wide volume of distribution (430L)
- 90% bound to serum proteins
- high affinity for alpha-1 acid glycoprotein
- metabolized in the liver by cyt P450 3A4
- eliminated in urine
- 1/2life 7.1-10.6 hours
elimination via liver
Monitor
Adverse effects
- common (> 5%)
- nausea/vomiting (73%)
- diarrhea (33%)
- rash (25%)
- perioral paresthesias (26%)
- peripheral paresthesias (8%)
- taste disorder (10%)
- depression (15%)
- uncommon (< 5%)
- drug adverse effects of antiretroviral protease inhibitors
- drug adverse effects of antiretroviral agents
Drug interactions
- contradindicated due to potentially serious events
- agents which lower plasma concentration of amprenavir:
- rifampin lowers plasma concentration of amprenavir by 90%
- rifabutin lowers plasma concentration of amprenavir by 15%
- phenobarbital
- phenytoin
- carbamazepine
- amprenavir increases plasma concentration of:
- any drug, including amprenavir itself, that inhibits cyt P450 3A4 may increase levels of amprenavir
- any drug that induces cyt P450 3A4 may diminish levels of amprenavir
- drug interaction(s) of fluticasone with HIV1 protease inhibitors
- drug interaction(s) of antiretroviral protease inhibitor in combination with ritonavir
- drug interaction(s) of statins with antiviral protease inhibitors
- drug interaction(s) of antibiotics with warfarin
Mechanism of action
- inhibits HIV-1 protease
- binds to active site of HIV-1 protease
- prevents processing of gag & gag-pol precursors
- results in formation of immature, non-infectious viral particles
More general terms
Additional terms
- cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)
- fosamprenavir (Lexiva)
References
- ↑ GlaxoWellcome package insert
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, Update 9/99
- ↑ Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220233&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Department of Veterans Affairs, VA National Formulary
- ↑ 5.0 5.1 5.2 Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260704&pb=PRL (subscription needed) http://www.prescribersletter.com