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amprenavir |
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Detailed Prescribing Information |
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October 2005 |
| Amprenavir = Agenerase | |
| Dosing Forms | 50mg, 150 mg soft gel caps; also liquid form available 15 mg/cc |
| Dosing |
Without boosting: 8x150 mg soft gel caps twice
a day With boosting: 6x150 caps + 1x100 mg ritonavir, both twice a day, or 8x150 caps + 2x100 mg ritonavir both once a day Dose adjustment is required for hepatic insufficiency. |
| Food Dependence | Amprenavir may be taken with or without food, but it should not be taken with a high fat meal. |
| Adverse Effects |
Mainly GI disturbance
including nausea, abdominal pain, diarrhea Also perioral paresthesia, hepatitis, fat redistribution, hyperlipidemia, Type 2 diabetes Possible cross-hypersensitivity to sulfonamides 1% incidence of Stevens-Johnson: discontinue amprenavir for moderate rash, progression of rash, and/or systemic symptoms. Due to vitamin E contained in the formulation, vitamin E supplementation by patients should be avoided. |
| Interactions |
Methadone levels are decreased and
amprenavir levels are decreased: protease inhibitor alternatives should be
considered. Rifampin decreases amprenavir levels significantly. St John's Wort decreases amprenavir levels. Amprenavir increases sildenafil levels Take amprenavir at least one hour before or one hour after antacids Anticonvulsants phenytoin, phenobarbital, carbamazepine all decrease amprenavir levels Use lowest possible dose of atorvastatin Dexamethasone should be used with
caution due to lowering of amprenavir levels |
| Suggested laboratory evaluations |
Liver profile and glucose monthly x 3
months, then every 3-4 months Lipid profile q3-4 months |
| Contraindications |
Ergot derivatives, cisapride, pimozide,
triazolam, midazolam Rifampin,
oral contraceptives, delavirdine |
| Warnings |
Use cautiously in patients
with a history of sulfonamide hypersensitivity Liquid form should be used in children less than 4 years of age due to excess amounts of propylene glycol contained in the excipient. Concomitant use of amprenavir liquid and ritonavir is contraindicated due to interference with the metabolism of propylene glycol by ritonavir. This same issue is relevant to patients with hepatic failure: amprenavir liquid should not be used. Rifampin should not be used with amprenavir: rifabutin at reduced dosage may be substituted. St John's Wort should not be used. Lovastatin and simvastatin should not be used due to high levels of these drugs and possible toxicity. |
| Usage Suggestions |
This drug may be largely supplanted by
fosamprenavir
which is a prodrug of amprenavir. Fosamprenavir has a lower pill
burden and dosing frequency when boosted with ritonavir (see
PI boosting below).
Additionally fosamprenavir may be better tolerated and less likely to cause dyslipidemia. However, fosamprenavir may not be combined with lopinavir/ritonavir at least until further interaction data is known. |
| Full Prescribing Information | http://www.gsk.com/products/agenerase_us.htm |
| Links to Antiretroviral Sections (click on anything) |
| Nucleoside & Nucleotide Reverse Transcriptase Inhibitors (NRTI) |
| AZT | ddC | ddI | d4T | 3TC | ABC | FTC | TDF | Combivir | Trizivir | Epzicom | Truvada |
| Nonnucleoside Reverse Transcriptase Inhibitors (NNRTI) |
| efavirenz | nevirapine | delavirdine |
| Protease Inhibitors (PI) | Boosted Protease Inhibitors |
| saquinavir | indinavir | ritonavir | nelfinavir | amprenavir | lopinavir + ritonavir | atazanavir | fosamprenavir | tipranavir |
| Fusion Inhibitors |
| enfuvirtide |
Updated 10.25.2005
