Nelfinavir

Indications

Nelfinavir is used for: HIV infection

Adult Dose

Oral HIV infection Adult: Combined with other antiretrovirals: 1.25 g bid or 0.75 g tid. Hepatic Impairment Mild impairment (Child-Pugh class A): Dose adjustment not necessary Severe impairment (Child-Pugh Class B or C): Not recommended

Child Dose

Oral HIV infection Child: Combined with other antiretrovirals: 2-13 yr: 45-55 mg/kg bid or 25-35 mg/kg tid. Max: 0.75 g tid. Max Dosage: Child: 0.75 g tid.

Renal Dose

Renal Impairment Dose adjustment not necessary

Administration

Should be taken with food.

Contra Indications

Hypersensitivity; lactation.

Precautions

Pregnancy. Hepatic and renal impairment; haemophilia A or B; diabetes. Monitor for signs of lipodystrophy. Lactation: HIV+ women are advised not to breastfeed

Pregnancy-Lactation

Pregnancy Category: B Lactation: HIV+ women are advised not to breastfeed

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.

Side Effects

Side effects of Nelfinavir : >10% Diarrhea (14-20%) 1-10% Nausea (3-7%), Flatulence (1-5%), Abdominal pain (1%), Anemia (1%), Allergic reaction (1%), Impaired concentration (1%), Lipodystrophy (1%), Metabolic acidosis (1%), Rash (1-3%), Leukopenia (1%), Thrombocytopenia (1%), Weakness (1%) <1% QTc prolongation, Torsades de pointes, Diabetes mellitus, new onset and exacerbation, Hyperglycemia

Mode of Action

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.