Dosing & Uses
Dosage Forms & Strengths
oral suspension
- 10mg/mL
tablet, immediate-release
- 200mg
tablet, extended-release
- 100mg
- 400mg
HIV Infection
Indicated for treatment of HIV-1 infection in combination with other antiretrovirals; also used for prevention of maternal-fetal HIV transmission in women with no prior antiretroviral treatment
200 mg PO qDay x 14 days, THEN
If no rash, increase to 200 mg q12hr; if rash occurs wait until it is resolved before increasing
Prevention of maternal-fetal HIV transmission: 200 mg PO as a single dose at onset of labor, in combination with IV zidovudine
Extended-release tablets
- Initial therapy: When initiating therapy, give immediate-release tablet 200 mg PO qDay for 14 days, then extended-release tablet 400 mg PO qDay thereafter
- Switch from immediate-release: If already taking immediate-release regimen, may switch to extended-release 400 mg PO qDay without 14-day lead-in period of immediate-release nevirapine
Dosing Considerations
Based on serious and life-threatening hepatotoxicity observed in controlled and uncontrolled trials, nevirapine should not be initiated in adult females with CD4+ cell counts >250 cells/mm³ or in adult males with CD4+ cell counts >400 cells/mm³ unless the benefit outweighs the risk
The 14-day lead-in period with immediate-release dosing must be strictly followed; it has been demonstrated to reduce the frequency of rash
If nevirapine extended-release interrupted >7 days, restart with lead-in dosing with immediate-release nevirapine
If mild-to-moderate rash (without constitutional symptoms) occurs during 14-day lead-in period, do not increase immediate-release dose or initiate extended-release regimen until the rash has resolved; duration of the lead-in dosing should not exceed 28 days, at which point an alternative regimen should be chosen; discontinue also if severe rash develops or rash with elevated hepatic transaminases or with constitutional symptoms occur
Dosage Forms & Strengths
oral suspension
- 10mg/mL
tablet, immediate-release
- 200mg
tablet, extended-release
- 100mg
- 400mg
HIV Infection
Indicated for treatment of HIV-1 infection in combination with other antiretrovirals
Immediate-release
- <15 days: Safety and efficacy not established
- ≥15 days to 16 years: 150 mg/m² PO qDay for 2 wk; if no rash, then increase to 150 mg/m² q12hr; not to exceed 200 mg/dose
- >16 years: As adults; 200 mg PO qDay for 2 wk; if no rash or untoward effect occurs, then increase to 200 mg PO q12h
Extended-release
- <6 years: Safety and efficacy not established
6-18 years
- Switch from immediate-release tabs: If already taking immediate-release, may switch to extended- release without 14-day lead-in period of immediate-release nevirapine
- Initial therapy: Initiate with immediate-release 150 mg/m² PO qDay for 14 days (not to exceed 200 mg/day), THEN
- Extended-release dose based on BSA as follows:
- 0.58-0.83 m²: 200 mg PO qDay
- 0.84-1.16 m²: 300 mg PO qDay
- ≥1.17 m²: 400 mg PO qDay
Alternate dosing based on HIV treatment guidelines (March, 2016)
- Immediate-release and suspension formulations
<1 month (investigational dose)
- 34-37 weeks gestational age: 4 mg/kg/dose PO BID for 1 week, then increase to 6 mg/kg/dose BID thereafter
- ≥37 weeks gestational age: 6 mg/kg/dose PO BID
≥1 month
- ≥1 month to <8 years: 200 mg/m² PO BID
- ≥8 years: 120-150 mg/m² PO BID
- Not to exceed 200 mg BID
Prevention of Maternal-Fetal HIV Transmission in Neonates
Additional prophylaxis with nevirapine is needed for HIV-exposed infants of women who did not receive antepartum ART (NIH perinatal guidelines July 2012)
Birth weight 1.5-2 kg: 8 mg/dose PO
Birth weight >2 kg: 12 mg/dose PO
Administer 3 doses in the first week of life; 1st dose 48 hr after birth, give 2nd dose 48 hr after 1st dose, and 3rd dose 96 hr after 2nd dose
Recommended in combination with 6 weeks of zidovudine
Dosing Considerations
The 14-day lead-in period with immediate-release dosing must be strictly followed; it has been demonstrated to reduce the frequency of rash
If nevirapine extended-release interrupted >7 days, restart with lead-in dosing with immediate-release nevirapine
If mild-to-moderate rash (without constitutional symptoms) occurs during 14-day lead-in period, do not increase immediate-release dose or initiate extended-release regimen until the rash has resolved; duration of the lead-in dosing should not exceed 28 days, at which point an alternative regimen should be chosen
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse Effects
>10%
Diarrhea (15-20%)
Rash (15-20%)
Headache (11%)
Neutropenia (10-11%)
Fever (8-11%)
1-10%
Ulcerative stomatitis (4%)
Increased LFTs (2-4%)
Abdominal pain (2%)
Paresthesia (2%)
Nausea
Anemia
Peripheral neuropathy
Myalgia
Frequency Not Defined
Potentially fatal hepatotoxicity (fulminant hepatitis, cholestatic hepatitis, hepatic failure, hepatic necrosis)
Stevens-Johnson syndrome
Toxic epidermal necrolysis
Rhabdomyolysis
Postmarketing Reports
Body as a whole: Fever, somnolence, drug withdrawal, redistribution/accumulation of body fat
Gastrointestinal: Vomiting
Liver and biliary: Jaundice, fulminant and cholestatic hepatitis, hepatic necrosis, hepatic failure
Hematology: Anemia, eosinophilia, neutropenia Investigations: decreased serum phosphorus
Investigations: Decreased serum phosphorus
Musculoskeletal: Arthralgia, rhabdomyolysis associated with skin and/or liver reactions
Neurologic: Paraesthesia
Skin and appendages: Allergic reactions including anaphylaxis, angioedema, bullous eruptions, ulcerative stomatitis and urticaria have all been reported; hypersensitivity syndrome and hypersensitivity reactions with rash associated with constitutional findings (eg, fever, blistering, oral lesions, conjunctivitis, facial edema, muscle or joint aches, general malaise, fatigue, or significant hepatic abnormalities, drug reaction with eosinophilia and systemic symptoms [DRESS])
Warnings
Black Box Warnings
Monitoring during the first 18 wk of therapy essential; extra vigilance warranted during first 6 wk of therapy (period of greatest risk)
Fatal and nonfatal hepatotoxicity
- Discontinue immediately with signs or symptoms of hepatitis or increased transaminase levels combined with rash or other systemic symptoms
Fatal and nonfatal skin reactions
- Discontinue immediately if severe skin or hypersensitivity reactions occur or if any rash with systemic symptoms occurs
Contraindications
Hypersensitivity
Moderate or severe hepatic impairment (Child-Pugh class B or C)
Coadministration with drugs (eg, CYP inducers) where significant decreases in nevirapine plasma concentrations may occur, which may result in loss of virologic response and possible resistance and cross-resistance to other NNRTIs
Use as part of postexposure prophylaxis (PEP) regimens
Cautions
Do not restart therapy following severe skin rash, skin rash combined with increased transaminases or other symptoms, or hypersensitivity reaction
Risk of severe, life threatening skin reactions including Stevens-Johnson syndrome, toxic epidermal necrolysis, and hypersensitivity
Discontinue if severe rash or any rash accompanied by constitutional findings occurs
Risk of immune reconstitution syndrome if used in combination with other antiretroviral drugs
Redistribution/accumulation of body fat may occur (cushingoid appearance)
Limited human data are insufficient to determine risk of infertility in humans; based on results from animal fertility studies conducted in rats, therapy may reduce fertility in females of reproductive potential; not known if these effects on fertility are reversible
Risk of hepatotoxicity
- Rhabdomyolysis reported in some patients experiencing skin and/or liver reactions associated with therapy; hepatitis/hepatic failure may be associated with signs of hypersensitivity which can include severe rash or rash accompanied by fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, facial edema, eosinophilia, granulocytopenia, lymphadenopathy, or renal dysfunction; patients with signs or symptoms of hepatitis must be advised to discontinue therapy and immediately seek medical evaluation, which should include liver enzyme tests
- The first 18 weeks of therapy are a critical period during which intensive clinical and laboratory monitoring of patients is required to detect potentially life-threatening hepatic events; some experts recommend clinical and laboratory monitoring more often than once per month, and in particular, include monitoring of liver enzyme tests at baseline, prior to dose escalation and at two weeks post-dose escalation; after initial 18-week period, frequent clinical and laboratory monitoring should continue throughout treatment
- Hepatic injury may progress despite treatment discontinuation
- Female gender and higher CD4 are higher risk factors
Pregnancy & Lactation
Pregnancy
There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to nevirapine during pregnancy; healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263
Available data from the APR show no difference in risk of overall major birth defects for nevirapine compared with background rate for major birth defects of 2.7% in the U.S. reference population of the Metropolitan Atlanta Congenital Defects Program (MACDP); rate of miscarriage is not reported in the APR
Severe hepatic events, including fatalities, reported in pregnant women receiving chronic therapy as part of combination treatment of HIV-1 infection; regardless of pregnancy status, women with CD4+ cell counts greater than 250 cells/mm3 should not initiate therapy unless benefit outweighs risk; it is unclear if pregnancy augments risk observed in non-pregnant women
Lactation
The Centers for Disease Control and Prevention recommend that HIV-1 infected mothers in the United States not breastfeed infants to avoid risking postnatal transmission of HIV-1 infection; published data report that nevirapine is present in human milk; there are limited data on effects of nevirapine on breastfed infant; there is no information on effects of nevirapine on milk production; because of potential for (1) HIV-1 transmission (in HIV-negative infants), (2) developing viral resistance (in HIV-positive infants), and (3) serious adverse reactions in nursing infants, mothers should not breastfeed if they are receiving therapy; published literature indicates that rash and hyperbilirubinemia have been seen in infants exposed to nevirapine through breastmilk
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI); activity against HIV-1 by binding to reverse transcriptase, and thereby blocking RNA- and DNA-dependent DNA polymerase actions including HIV-1 replication
Does not require intracellular phosphorylation for activity
Absorption
Bioavailability: >90%
Peak Plasma: 2-4 hr
Distribution
Distributed widely; crosses placenta; enters breast milk; CSF penetration approximates 50% of plasma
Protein Bound: 50-60%
Vd: 1.2-1.4 L/kg
Metabolism
Extensively hepatic via CYP3A4 (hydroxylation to inactive compounds)
May undergo enterohepatic recycling
Elimination
Half-life: Decreases over 2-4 wk with chronic dosing due to autoinduction (ie, half-life initially 45 hr and decreases to 23 hr)
Excretion: Urine (~81% as metabolites, <3% as unchanged drug); feces (10%)
Administration
Oral Administration
Shake suspension gently and administer entire measured dose
5 mL or less: Use oral syringe
Extended-release tablets should be swallowed whole; do not chew, crush, or split
May take with or without food
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Patient Handout
Formulary
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