Nelfinavir mesylate
Nelfinavir mesylate (Viracept)
Nelfinavir mesylate
(nel- FIN-ah-veer)
Pregnancy Category: B Viracept (Rx)

Classification: Antiviral, protease inhibitor

See Also: See also Antiviral Drugs.

Action/Kinetics: HIV-1 protease inhibitor, resulting in prevention of cleavage of gagpol polyprotein resulting in production of immature, non-infectious viruses. Activity is increased when used with didanosine, lamivudine, stavudine, zalcitabine, or zidovudine. Peak plasma levels: 2-4 hr. Steady-state plasma levels: 3-4 mcg/mL. Food increases plasma levels 2-3 fold. t 1/2 terminal: 3.5-5 hr. Metabolites (one of which is as active as parent compound) and unchanged drug excreted mainly in feces.

Uses: Treat HIV infection when antiretroviral therapy is required.

Contraindications: Administration with astemizole, cisapride, midazolam, rifampin, terfenadine, or triazolam.

Special Concerns: Use with caution with hepatic impairment. Safety and efficacy have not been determined in children less than 2 years of age.

Side Effects: Side effects were determined when used in combination with other antiviral drugs. GI: N&V;, diarrhea, flatulence, abdominal pain, anorexia, dyspepsia, epigastric pain, GI bleeding, hepatitis, mouth ulcers, pancreatitis. CNS: Anxiety, depression, dizziness, emotional lability, hyperkinesia, insomnia, migraine, paresthesia, seizures sleep disorder, somnolence, suicide ideation. Hematologic: Anemia, leukopenia, thrombocytopenia. Respiratory: Dyspnea, rhinitis, sinusitis, pharyngitis. GU: Kidney calculus, sexual dysfunction, urine abnormality. Ophthalmic: Eye disorder, acute iritis. Musculoskeletal: Arthralgia, arthritis, cramps, myalgia, myasthenia, myopathy. Dermatologic: Dermatitis, folliculitis, fungal dermatitis, maculopapular rash, pruritus, urticaria, sweating. Miscellaneous: Asthenia, dehydration, allergic reaction, back pain, fever, headache, malaise, pain, accidental injury.

Laboratory Test Alterations: ALT, AST, creatine phosphokinase, alkaline phosphatase, amylase, lactic dehydrogenase, GGT. Hyperlipidemia, hyperuricemia, hypoglycemia. Abnormal LFTs.

Overdose Management: Symptoms: See side effects. Treatment: Emesis or gastric lavage, followed by activated charcoal.

Drug Interactions: Anticonvulsants / Possible nelfinavir plasma levels Didanosine / Absorption of nelfinavir Indinavir / Significant in nelfinavir levels Oral contraceptives / Drug effects; use alternative contraceptive measures Rifabutin / Rifabutin levels; reduce rifabutin dose one-half Rifampin / Significant in nelfinavir levels; do not coadminister

How Supplied: Powder for Reconstitution: 50 mg/1 g; Suspension: 50 mg/5 mL; Tablets: 250 mg

Dosage
?Powder, Tablets HIV.
Adults: 750 mg (i.e., 3-250 mg tablets) t.i.d. in combination with nucleoside analogs. Children, 2 to 13 years: 20-30 mg/kg/dose t.i.d.