Nelfinavir

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; ≥13 yr Same as adult dose.
Max Dosage: Child: 0.75 g tid.
Hepatic impairment: Dose reduction may be required.

Should be taken with food.

Hypersensitivity; lactation.

Pregnancy. Hepatic and renal impairment; haemophilia A or B; diabetes. Monitor for signs of lipodystrophy.

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.

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.

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.

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 hr. 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 hr.

Oral: Store at 15-30° (59-86°F).

Antivirals

J05AE04 - nelfinavir ; Belongs to the class of protease inhibitors. Used in the systemic treatment of viral infections.