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Indications and 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; ≥13 yr Same as adult dose. |
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Hepatic Impairment
Dose reduction may be required.
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Administration
Should be taken with food.
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Contraindications
Hypersensitivity; lactation.
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Special Precautions
Pregnancy. Hepatic and renal impairment; haemophilia A or B; diabetes. Monitor for signs of lipodystrophy.
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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.
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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. |
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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.
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Action
Description:
Mechanism 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. Pharmacokinetics: 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. |
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Storage
Store at 15-30° (59-86°F).
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MIMS Class
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