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ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Protease inhibitors
nelfinavir
J05AE04
Forms & Strengths
- Oral powder: 50 mg per 1 g
- Tablets: 250 mg
Adult Dosing
- 1250 mg orally twice daily with food
- 750 mg orally three times daily with food
Pediatric Dosing
- Neonates (birth to 2 months): 40 mg/kg orally twice daily or 30 mg/kg orally three times daily
- Children (2 to 13 years): 45 to 55 mg/kg orally twice daily (maximum 2500 mg/day) or 25 to 30 mg/kg orally three times daily (maximum 750 mg/dose)
Indications
- Treatment of HIV-1 infection in combination with other antiretroviral agents
Mechanism of Action
- HIV-1 protease inhibitor that binds to the protease active site, preventing cleavage of Gag-Pol polyproteins, resulting in the production of immature, non-infectious viral particles
Contraindications
- Hypersensitivity to nelfinavir or any of its components
- Co-administration with drugs highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious/life-threatening events (e.g., amiodarone, lovastatin, simvastatin, rifampin, triazolam, midazolam)
Adverse Reactions
- Diarrhea
- Nausea
- Fatigue
- Rash
- Flatulence
- Hyperglycemia
- Dyslipidemia
- Fat redistribution (lipodystrophy)
Drug Interactions
- CYP3A4 substrates: May increase plasma concentrations of certain drugs (e.g., sildenafil, statins, immunosuppressants)
- CYP3A4 inducers: Rifampin and St. John's wort significantly decrease nelfinavir concentrations
- CYP2C19 substrates: Nelfinavir inhibits CYP2C19, potentially increasing concentrations of drugs like omeprazole
- Oral contraceptives: May decrease concentrations of ethinyl estradiol and norethindrone, requiring alternative contraception
Curated Content: Needs Vetting Before Put to Clinical Use