Nelfinavir information from DrugsUpdate
P - Caution when used during pregnancy
L - Contraindicated in lactation
FI - Food *
Nelfinavir (Viracept) is an antiretroviral drug used in the treatment of the human immunodeficiency virus (HIV). Nelfinavir belongs to the class of drugs known as protease inhibitors (PIs) and like other PIs is generally used in combination with other antiretroviral drugs.
Nelfinavir mesylate (Viracept, formally AG1343) is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2nM) and is being widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection.
Pharmacodynamics
Pharmacokinetics
Nelfinavir is a selective, competitive, reversible HIV protease inhibitor. It inhibits HIV-1 protease preventing the cleavage of the gag-pol polyprotein resulting in the production of noninfectious virus.
Absorption
Absorbed from the GI tract. Peak plasma levels in 2-4 hours. Absorption increased with food.
Distribution
Extensively bound to plasma proteins (98%). Enters breast milk.
Metabolism
Hepatic via oxidation.
Excretion
Mainly via faeces (as metabolites); via urine (about 1-2%). Terminal half-life: 3.5-5 hours.
Nelfinavir Indications / Nelfinavir Uses
Information Not Available
Nelfinavir Adverse Reactions / Nelfinavir Side Effects
Hyperglycaemia, dyslipidaemia and redistribution of body fat (protease paunch, buffalo hump, facial atrophy and heart engorgement); hypertriglyceridaemia, hypercholesterolaemia. Diarrhoea, rash, nausea, flatulence, decreased lymphocytes, decreased neutrophils, decreased haemoglobin, increased creatine kinase, increased transaminases.
Precautions
Information Not Available
Special Precautions
Pregnancy. Hepatic and renal impairment; haemophilia A or B; diabetes. Monitor for signs of lipodystrophy.
Other Drug Interactions
Reduced levels/effects with antacids, phenobarbital, carbamazepine, aminoglutethimide, phenytoin, rifampicin, nafcillin, nevirapine, omeprazole, nevirapine. Increased serum levels/effects with azole antifungal agents, cimetidine, efavirenz. Increased serum levels/effects of azithromycin, calcium channel blockers, clarithromycin, corticosteroids (e.g. fluticasone), mirtazapine, nateglinide, nefazodone, ciclosporin, sirolimus, tacrolimus, venlafaxine, eplerinone, fentanyl, atorvastatin, phosphodiesterase-5 (PDE-5) inhibitors, rifabutin, trazodone, TCAs. Reduced serum levels/effects of hormonal contraceptives, methadone, theophylline derivatives.
Potentially Fatal: Increased serum levels/toxicity of amiodarone, cisapride, pimozide, midazolam, triazolam, ergot alkaloids, lovastatin, simvastatin, quinidine.
Other Interactions
Food Interaction
Combination with acidic food or juice may produce bitter taste. Plasma concentration time curve (AUC) increased by 2- to 3-fold with food. Reduced serum levels with St John's wort.
Dosage
Oral
HIV infection
Adult: Combined with other antiretrovirals: 1.25 g bid or 0.75 g tid.
Child: Combined with other antiretrovirals: 2-13 yr: 45-55 mg/kg bid or 25-35 mg/kg tid.
Max Dosage: Child: 0.75 g tid.
Hepatic impairment: Dose reduction may be required.
Food(before/after)
Should be taken with food
List of Contraindications
Nelfinavir and Pregnancy
Caution when used during pregnancy
Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).
Nelfinavir and Lactation
Contraindicated in lactation
Nelfinavir and Children
Safety and efficacy not established for children younger than 2 years of age.
Nelfinavir and Geriatic
Information Not Available
Nelfinavir and Other Contraindications
Hypersensitivity; lactation
Storage
Oral
Store at 15-30° (59-86°F)
Lab interference
Oral
Store at 15-30° (59-86°F)
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