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Action/Kinetics:
By binding tightly to reverse transcriptase, nevirapine prevents viral RNA from being converted into DNA. In combination with a nucleoside analogue, it reduces the amount of virus circulating in the body and increases CD4+ cell counts. Readily absorbed, with peak plasma levels occurring 4 hr after a 200-mg dose. Extensively metabolized in the liver. Excreted through both the urine (about 90%) and the feces (about 10%). Induces its own metabolism; following chronic use the half-life decreases from about 45 hr following a single dose to 25 to 30 hr following multiple dosing with 200 or 400 mg daily.
Uses:
In combination with nucleoside analogues (e.g., AZT, lamivudine, didanosine, zalcitabine) or protease inhibitors (e.g., saquinavir, indinavir, nelfinavir, aritonavir) for the treatment of HIV-1 infections in adults and children 2 months or older who have experienced clinical and immunologic deterioration. Always use in combination with at least one other antiretroviral agent, as resistant viruses emerge rapidly when nevirapine is used alone.
Contraindications:
Lactation.
Special Concerns:
The duration of benefit from therapy may be limited. Is not a cure for HIV infections; clients may continue to experience illnesses associated with HIV infections, including opportunistic infections. Has not been shown to reduce the risk of transmitting HIV to others through sexual contact or blood contamination. Use with caution in impaired renal or hepatic function.
Side Effects:
GI: Nausea, diarrhea, abdominal pain, ulcerative stomatitis, hepatitis.
CNS: Headache, fatigue, paresthesia.
Hematologic: Decreased hemoglobin, decreased platelets, decreased neutrophils, granulocytopenia (occurs more in children).
Miscellaneous:
Rash (may be severe and life-threatening) fever, peripheral neuropathy, myalgia.
Laboratory Test Alterations:
ALT, AST, GGT, total bilirubin. Abnormal LFTs.
Drug Interactions:
-
Ketoconazole / Significant
plasma ketoconacole levels; do not use together
-
Methadone /
Plasma methadone levels;
methadone dose
-
Oral contraceptives /
OC plasma levels
effect
-
Protease inhibitors /
Plasma levels of protease inhibitors
-
Rifabutin /
Nevirapine trough concentrations
-
Rifampin /
Nevirapine trough concentrations
How Supplied:
Suspension: 50 mg/5 mL;
Tablet: 200 mg
Dosage
?Suspension, Tablets
HIV-1 infections.
Adults, initial: 200 mg/day for 14 days.
Maintenance: 200 mg b.i.d. (e.g., 7:00 a.m. and 7:00 p.m.) in combination with a nucleoside analogue antiretroviral agent.
Children, 2 months-8 years: 4 mg/kg once daily for 14 days followed by 7 mg/kg b.i.d.
Children, 8 years and older: 4 mg/kg once daily for 14 days followed by 4 mg/kg once daily. Do not exceed a total daily dose of 400 mg for any client.
