NEVIRAPINE TABLETS FOR ORAL SUSPENSION
Clinical safety rating: safe
Induces CYP3A4 decreasing levels of many drugs Can cause severe skin reactions and hepatotoxicity.
Non-nucleoside reverse transcriptase inhibitor (NNRTI) that binds directly to HIV-1 reverse transcriptase, causing a conformational change and inhibiting RNA-dependent and DNA-dependent DNA polymerase activity.
| Metabolism | Extensively metabolized by cytochrome P450 (CYP) 3A4 and other CYP isozymes, with major metabolites being hydroxynevirapine and glucuronide conjugates. |
| Excretion | Renal (approx. 80% as glucuronidated metabolites, <5% unchanged), fecal (approx. 10%) |
| Half-life | Terminal elimination half-life is approximately 25-30 hours after single dose; decreases to 20-22 hours after multiple dosing due to autoinduction of CYP3A4 and CYP2B6. |
| Protein binding | Approximately 60% bound to plasma proteins (mainly albumin). |
| Volume of Distribution | 1.2-1.4 L/kg (suggests extensive distribution into tissues, including CSF and brain). |
| Bioavailability | Oral: >90% (absolute bioavailability not formally determined; based on urinary recovery and comparison with IV data in similar NNRTIs). |
| Onset of Action | Oral: Clinical effect onset occurs within 2-4 weeks (reduction in HIV-1 RNA) but steady-state concentrations achieved by 2-4 weeks. |
| Duration of Action | Duration of antiviral effect is continuous with twice-daily dosing; trough concentrations should be maintained above therapeutic threshold (approximately 3,000 ng/mL). |
200 mg orally once daily for 14 days, then 200 mg orally twice daily.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for GFR ≥20 mL/min; contraindicated for GFR <20 mL/min or in hemodialysis. |
| Liver impairment | Child-Pugh A: 200 mg orally once daily for 14 days, then 200 mg orally twice daily if tolerated. Child-Pugh B: 200 mg orally once daily; do not escalate to twice daily. Child-Pugh C: contraindicated. |
| Pediatric use | For patients ≥2 years: 150 mg/m² orally once daily for 14 days, then 150 mg/m² orally twice daily; maximum 400 mg/day. For patients <2 years: not recommended. |
| Geriatric use | No specific dose adjustment required; monitor for hepatic and renal function, increased risk of adverse effects due to comorbid conditions. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Induces CYP3A4 decreasing levels of many drugs Can cause severe skin reactions and hepatotoxicity.
| FDA category | Animal |
| Breastfeeding | Nevirapine is excreted into human breast milk; the milk-to-plasma ratio is approximately 0.6. Breastfeeding is not recommended for HIV-infected mothers in developed countries due to risk of HIV transmission. In settings where breastfeeding is advised, nevirapine may be used but the infant should be monitored for adverse effects such as rash and hepatotoxicity. |
| Teratogenic Risk |
■ FDA Black Box Warning
Severe, life-threatening hepatotoxicity, including fatal hepatic events, has occurred in patients with or without pre-existing hepatic impairment. Severe, life-threatening skin reactions, including Stevens-Johnson syndrome, toxic epidermal necrolysis, and hypersensitivity reactions, have occurred.
| Common Effects | Rash |
| Serious Effects |
Patients with moderate to severe hepatic impairment (Child-Pugh B or C). Concomitant use with certain drugs (e.g., rifampin, St. John's wort). Do not use as a single agent for treatment or prophylaxis.
| Precautions | Monitor hepatic function and skin reactions closely; discontinue if severe rash or hepatotoxicity occurs. Do not restart after severe events. Use with caution in patients with hepatic impairment or co-infection with hepatitis B/C. Monitor immune reconstitution syndrome and drug interactions. |
Loading safety data…
| Nevirapine is classified as FDA Pregnancy Category B. Animal studies have not demonstrated fetal harm, but adequate human studies in pregnant women are lacking. There is no known risk of teratogenicity based on available data, but caution is advised. Placental transfer occurs, and nevirapine is used in pregnancy for prevention of mother-to-child transmission of HIV. First trimester exposure does not appear to increase major birth defects, but data are limited. |
| Fetal Monitoring | Monitor maternal liver function tests (AST, ALT) at baseline and frequently during therapy due to risk of hepatotoxicity, especially in women with CD4 counts >250 cells/μL. Monitor for rash, which may be a precursor to severe skin reactions. In pregnancy, monitor HIV viral load and CD4 count; infant should be tested for HIV status after birth. |
| Fertility Effects | No significant effects on fertility have been reported in animal studies or human data. Nevirapine is not known to impair male or female reproductive function. |