Nelfinavir

Indications
 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.

Special Populations: When administered in combination with ritonavir: Nefinavir 500-750 mg bid plus ritonavir 400 mg bid.
Contraindications
 Hypersensitivity; lactation.
Warnings / Precautions
 Pregnancy. Hepatic and renal impairment; haemophilia A or B; diabetes. Monitor for signs of lipodystrophy.
Adverse Reactions
 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.
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.
See Below for More nelfinavir Drug Interactions
Food Interactions
 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.
Mechanism of Actions
 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.
Administration
 Should be taken with food.
Storage Conditions
 Oral: Store at 15-30° (59-86°F).
ATC Classification
 J05AE04 - nelfinavir ; Belongs to the class of protease inhibitors. Used in the systemic treatment of viral infections.
Storage
 Oral: Store at 15-30° (59-86°F).
Available As
  • Nelfinavir 250 mg
  • Nelfinavir 625 mg

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