Nevirapine

Mechanism :

Nevirapine binds directly to reverse transcriptase (RT) and blocks the RNA-dependent and DNA-dependent DNA polymerase activities by causing a disruption of the enzyme's catalytic site. The activity of nevirapine does not compete with template or nucleoside triphosphates.

Indication :

• HIV-1 treatment as part of combination regimen

Contraindications :

Hypersensitivity, Post-exposure prophylaxis use, Baseline CD4 >250 (female pts), Baseline CD4 >400 (male pts), Caution if HBV or HCV co-infection.

Hepatic impairment, Child-Pugh Class B or C.

Dosing :

Adverse Effect :

Serious Reactions: Hypersensitivity reaction, severe anaphylaxis, Stevens-Johnson syndrome and toxic epidermal necrolysis, drug rash with eosinophilia, hepatotoxicity.

Common Reactions: Stomatitis, nausea, elevated ALT/AST, fatigue, headache, anemia, diarrhea, abdominal pain, hepatotoxicity, arthralgia/myalgia, lipodystrophy.

Interaction :

Acenocoumarol: Nevirapine may decrease the anticoagulant effect of acenocoumarol.
Anisindione: Nevirapine may decrease the anticoagulant effect of anisindione.
Atazanavir: Nevirapine, a strong CYP3A4 inducer, may decrease the serum concentration of atazanavir by increasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of atazanavir if nevirapine is initiated, discontinued or dose changed.
Atorvastatin: Nevirapine, a strong CYP3A4 inducer, may decrease the serum concentration of atorvastatin by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of atorvastatin if nevirapine is initiated, discontinued or dose changed.
Dicoumarol: Nevirapine may decrease the anticoagulant effect of dicumarol.
Estradiol valerate/Dienogest: Affects CYP3A4 metabolism, decreases or effects levels of Estradiol valerate/Dienogest.
Etravirine: Nevirapine may cause a significant decrease in plasma levels of etravirine and a loss of efficacy. Combination of two NNRTIs has not been demonstrated to be of benefit to HIV therapy.
Ketoconazole: Nevirapine, a strong CYP3A4 inducer, may decrease the serum concentration of ketoconazole by increasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of ketoconazole if nevirapine is initiated, discontinued or dose changed.
Lovastatin: The strong CYP3A4 inducer, nevirapine, may decrease the effect of lovastatin by increasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of lovastatin if nevirapine is initiated, discontinued or dose changed.
Methadone: The antiretroviral agent decreases the effect of methadone.
Nelfinavir: Nevirapine may decrease the effect of nelfinavir.
Quinupristin: This combination presents an increased risk of toxicity.
Roflumilast: Affects CYP3A4 metabolism, decreases level or effect of roflumilast.
Saquinavir: Decreases the effect of saquinavir.
Simvastatin: The strong CYP3A4 inducer, nevirapine, may decrease the effect of simvastatin by increasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of simvastatin if nevirapine is initiated, discontinued or dose changed.
St. John's Wort: St. John's Wort decreases nevirapine effect.
Telithromycin: Nevirapine may decrease the plasma concentration of Telithromycin. Consider alternate therapy.
Temsirolimus: Nevirapine may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Tipranavir: Nevirapine, a CYP3A4 inducer, may decrease the serum concentration of Tipranavir, a CYP3A4 substrate. Monitor for changes in Tipranavir effect if Nevirapine is initiated, discontinued or dose changed.
Tramadol: Nevirapine may decrease the effect of Tramadol by increasing Tramadol metabolism and clearance.
Trazodone: The CYP3A4 inducer, Nevirapine, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Nevirapine is initiated, discontinued or dose changed.
Vandetanib: Decreases levels of vandetanib by affecting CYP3A4 metabolism. Contraindicated.
Warfarin: Nevirapine may decrease the anticoagulant effect of warfarin by increasing metabolism of R-warfarin via CYP3A4.

Renal Dose :

Hepatic Dose :