Nelfinavir


Concise Prescribing Info
Indications/Uses
HIV infection.
Dosage/Direction for Use
Adult : PO Combined with other antiretrovirals: 1.25 g bid or 0.75 g tid.
Dosage Details
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.
Hepatic Impairment
Dose reduction may be required.
Administration
Should be taken with food.
Contraindications
Hypersensitivity; lactation.
Special 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.
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.
Action
Description: 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.
Storage
Store at 15-30° (59-86°F).
MIMS Class
Disclaimer: This information is independently developed by MIMS based on Nelfinavir from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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