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). |
| Molecular Weight | 266.298 |
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 | Use only if benefit outweighs risk. Studies show increased risk of hepatotoxicity and rash; teratogenicity not clearly established. |
| 2nd trimester | Use with caution; monitor liver function. Limited data but no major teratogenic signals. May be preferred over certain other antiretrovirals. |
| 3rd trimester | Use with caution; monitor liver function. Risk of hepatotoxicity may be higher postpartum. Consider alternative if hepatic impairment. |
Clinical note
Induces CYP3A4 decreasing levels of many drugs Can cause severe skin reactions and hepatotoxicity.
| FDA category | Animal |
| Placental transfer | Nevirapine crosses the placenta readily; cord blood concentrations approximate maternal plasma levels. Used in perinatal prophylaxis for HIV. |
■ 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 |
Hypersensitivity to nevirapine or any excipientSevere hepatic impairment (Child-Pugh Class B or C)Concomitant use with rifampicin or St. John's wortBaseline AST or ALT >5 times upper limit of normal (unless due to HIV)Previous severe rash or hypersensitivity reaction to nevirapine
| 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. |
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| Breastfeeding |
| Nevirapine is excreted into breast milk in concentrations similar to maternal plasma. In HIV-positive mothers, breastfeeding is not recommended due to risk of HIV transmission. For other indications, potential benefits must be weighed against risk of infant exposure; limited data on long-term effects. |
| Lactation Rating | L4 (Possibly Hazardous) |
| Teratogenic Risk | 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. |
| Food/Dietary |
| No significant food interactions. Nevirapine can be taken with or without food, as food does not affect absorption. Avoid St. John’s wort, which can reduce nevirapine levels via CYP induction. No specific dietary restrictions. |
| Clinical Pearls | Nevirapine is associated with severe, life-threatening hepatotoxicity and skin reactions (including Stevens-Johnson syndrome) particularly in the first 18 weeks of therapy. A 14-day lead-in dose of 200 mg once daily is mandatory to reduce rash risk. Monitor hepatic enzymes at baseline and frequently during therapy. Do not restart nevirapine after a severe rash or symptomatic hepatic events. Nevirapine induces its own metabolism via CYP3A4, so no dose adjustment needed for mild-to-moderate hepatic impairment but contraindicated in Child-Pugh Class B or C. Pregnancy category B; however, avoid use in women with CD4 >250 cells/mm³ unless benefit outweighs risk due to increased hepatotoxicity. Male patients with CD4 >400 cells/mm³ also have increased risk. Always assess baseline CD4 and transaminases. |
| Patient Advice | Take nevirapine exactly as prescribed; do not change dose or stop without consulting your doctor. · A lower dose (200 mg once daily) is given for the first 14 days to reduce the risk of serious rash; after 14 days, the dose increases to 200 mg twice daily. · Report any skin rash, hives, mouth sores, or blistering immediately—these can be signs of a severe allergic reaction. · Watch for symptoms of liver problems: dark urine, pale stools, yellowing of skin/eyes, abdominal pain, nausea, or unexplained fatigue. Seek medical help right away if these occur. · Do not stop nevirapine even if you feel better; stopping can lead to drug resistance. · Nevirapine does not cure HIV or prevent transmission; continue to use barrier protection and avoid sharing needles. · Inform your doctor about all other medicines, including over-the-counter drugs, supplements, and herbal products (e.g., St. John’s wort). · If you miss a dose, take it as soon as you remember unless it is near the time of the next dose. Do not double the dose. |