|
nelfinavir |
|
Detailed Prescribing Information |
| Nelfinavir = Viracept | |
| Dosing Forms | Coated 250 mg tablets; 625 mg tablets; oral powder 50 mg/g |
| Dosing |
2 x 625 mg twice a day
or 5 x 250 mg twice a day or 3 x 250 three times a day,
All nelfinavir regimens should be taken with food,
preferably a meal |
| Hepatic insufficiency: No data | |
| Renal insufficiency: No adjustment needed | |
| Food dependence | Nelfinavir should be taken with food at every dose. Food increases absorption. |
| Adverse Effects |
Soft stools or diarrhea (50%),
hepatitis, hyperlipidemia, diabetes, fat redistribution Diarrhea: consider Imodium, calcium supplement (Tums, Rolaids, Ca carbonate 500 twice a day) or psyllium fiber twice a day |
| Interactions |
Efavirenz decreases
nelfinavir levels (increase nelfinavir to 6x250 twice a day)
Nevirapine decreases nelfinavir levels (increase
nelfinavir to 6x250 twice a day) |
|
Effects of nelfinavir on other drug levels: Mild increase in indinavir AUC 200-400% increase in saquinavir AUC and Cmax Significant increase in rifabutin levels: decrease rifabutin to 150 mg daily 100% increase in single dose azithromycin AUC and Cmax 100% increase in atorvastatin AUC and Cmax 500% increase in simvastatin AUC 20-50% reductions in levels of OCPs, methadone, phenytoin |
|
|
Drugs that increase nelfinavir levels: Indinavir: 83% increase in AUC and 31% increase in Cmax Ritonavir 500 mg q12hours: 152% increase in AUC, 44% increase in Cmax Saquinavir: slight increase Efavirenz: slight increase Delavirdine: approx 100% increase in AUC, Cmax, Cmin Ketoconazole: 15-35% increase |
|
|
Drugs that decrease nelfinavir levels: Nevirapine: 32% decrease in Cmin Rifabutin 150 mg daily: approx 20% decrease Rifabutin 300 mg daily: approx 25-50% decrease Carbamazepine Rifampin 600 mg daily: 75-92% decrease St John's wort |
|
| No data: atazanavir, fosamprenavir, amprenavir | |
| Contraindications |
Antiarrhythmics: amiodarone, quinidine Ergot derivatives: dihydroergotamine, ergonovine, ergotamine, methylergonovine Neuroleptics: pimozide Sedatives/hypnotics: midazolam, triazolam
Statins other than atorvastatin, pravastatin |
| Suggested laboratory evaluations | Liver profile and glucose monthly x 3 months, then every 3-4 months; lipid profile q3-4 months |
| Warnings |
Carbamazepine decreases nelfinavir levels Monitor levels of cyclosporine, tacrolimus, sirolimus, phenytoin Additional contraception should be employed in addition to oral contraceptives Use reduced doses of drugs for erectile dysfunction |
| Full Prescribing Information | http://www.viracept.com |
| 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 | Atripla |
| Nonnucleoside Reverse Transcriptase Inhibitors (NNRTI) |
| efavirenz | nevirapine | delavirdine | etravirine |
| Protease Inhibitors (PI) | Boosted Protease Inhibitors |
| saquinavir | indinavir | ritonavir | nelfinavir | amprenavir | lopinavir + ritonavir | atazanavir | fosamprenavir | tipranavir |
| Fusion Inhibitors |
| enfuvirtide |
| Co-Receptor Inhibitors |
| maraviroc |
| Integrase inhibitors |
| raltegravir |
Updated 10.17.2007
