Trade Names:Viracept- Tablets 250 mg- Powder 50 mg/g
Inhibits human immunodeficiency virus (HIV) protease, the enzyme required to form functional proteins in HIV-infected cells.
Food increased maximum plasma concentration and AUC by 2- to 3-fold. T max was 2 to 4 h and C max was 3 to 4 h.
Nelfinavir's Vd is 2 to 7 L/kg and protein binding is greater than 98%.
Nelfinavir is metabolized by multiple CYP-450 isoforms, including CYP3A. Major metabolite has activity comparable with parent drug.
The t ½ is 3.5 to 5 h; 87% excreted in feces (78% metabolites, 22% unchanged) and 1% to 2% in urine (unchanged).
Treatment of HIV infection in combination with other antiretroviral agents.
Hypersensitivity to nelfinavir or any component of the product. Concomitant therapy with amiodarone, ergot derivatives, quinidine, lovastatin, midazolam, pimozide, simvastatin, and triazolam.
PO 1,250 mg twice daily or 750 mg 3 times daily in combination with nucleoside analogs.Children (2 to 13 yr of age)
PO 20 to 30 mg/kg/dose 3 times daily.
Store tablets and powder at controlled room temperature (59° to 86°F).
Nelfinavir may increase blood levels of these drugs, which may produce extreme sedation and respiratory depression. Do not coadminister.Amiodarone, cisapride, cyclosporine, lovastatin, pimozide, quinidine, rifabutin, sildenafil, simvastatin, sirolimus, tacrolimus
Nelfinavir may elevate blood levels of these drugs, which may increase the risk of arrhythmias or other potential serious adverse reactions.Carbamazepine, phenobarbital, St. John's wort
May decrease nelfinavir plasma concentrations.Indinavir
Nelfinavir may increase indinavir blood levels.Indinavir, ritonavir
May increase nelfinavir plasma concentrations.Methadone
May decrease methadone concentration.Oral contraceptives
Concentrations of ethinyl estradiol, a component of oral contraceptives, may be reduced.Phenytoin
Nelfinavir may decrease blood levels of phenytoin.Rifabutin
May increase rifabutin concentration and decrease nelfinavir concentration.Rifampin
May decrease plasma concentrations of nelfinavir.
None well documented.
Headache; paresthesia; dizziness; insomnia; somnolence; anxiety; depression; seizures; emotional lability; hyperkinesia; migraine; sleep disorder.
Rash (2%); pruritus; sweating; urticaria; dermatitis folliculitis.
Pharyngitis; rhinitis; sinusitis; acute iritis; eye disorder.
Anorexia; diarrhea (20%); dyspepsia; flatulence; nausea (3%); vomiting; abdominal pain; pancreatitis; bleeding; mouth ulcerations.
Sexual dysfunction; kidney calculus; urine abnormality.
Anemia; leukopenia; thrombocytopenia.
Increased alkaline phosphatase; LFTs; CPK; hyperlipidemia; amylase; lactic dehydrogenase; hyperuricemia; hyperglycemia; hypoglycemia; dehydration; gamma glutamyl transpeptidase.
Asthenia; fever; myalgia; back pain; malaise; arthralgia; myasthenia; myopathy; accidental injury; allergic reaction; arthralgia; cramps.
Category B .
Undetermined. HIV-infected mothers should not breast-feed their infants.
Safety and efficacy not established for children younger than 2 yr of age.
Use caution in patients with hepatic function impairment; decreased nelfinavir Cl may occur.
New onset diabetes and exacerbation of pre-existing diabetes mellitus has been reported in postmarking surveillance.
Redistribution/accumulation of body fat has been observed in patients receiving antiretroviral therapy.
There have been reports of increased bleeding, including skin hematomas and hemarthrosis in patients with hemophilia type A and B treated with protease inhibitors. A causal relationship not established.
Nelfinavir powder contains 11.2 mg phenylalanine/g of powder.
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