Non-Nucleoside Reverse Transcriptase Inhibitors: Nevirapine
Contents Introduction Information card Pharmacokinetics Dosing Side effects Drug interactions

Introduction

The information represented on this drug does not necessarily correspond with the information that can be found in the Belgian scientific leaflet.
Nevirapine is a potent noncompetitive inhibitor of HIV-1 reverse transcriptase. It was approved the first FDA-approved Non-Nucleoside Reverse Transcriptase Inhibitor (1996). (100,106)

Abbreviation(s):  Generic name: Brand name: NVP nevirapine Viramune®		USA (FDA) Adult approval date: Pediatric approval date: June 21, 1996 September 11, 1998
Pharmaceutical co.: Boehringer Ingelheim		Belgium: Reimbursable since September 1998
	Active Ingredient	Dosage form; Route		Strength
	Nevirapine	Tablet; Oral		200MG

Pharmacokinetics

Nevirapine is readily absorbed after oral dosing (bioavailability of approximately 90%). Absorption is not dependent on a fed or fasting condition, thus allowing for more convenient dosing regimens. Nevirapine appears to induce its own metabolism via its activating effect of the P450 system. Nevirapine readily crosses the blood brain barrier. In a small study, the CSF concentration of nevirapine was approximately 50% of that in plasma (and similar to the protein-free plasma concentration). (106)

Dosing

Because nevirapine iduces its own metabolism, it may be dose escalated over the first 2 weeks of therapy. The current recommended schedule is 200 mg daily for 14 days, followed by 200 mg twice daily. (106)

Side effects

In general, nevirapine is safe and well tolerated. The most significant adverse reaction has been rash. The rash is typically a diffuse, maculopapular erythematous eruption involving the trunk, face, and extremities, sparing the hands and feet. When rash is severe, use of  nevirapine should be stopped; if rash is mild, symptomatic therapy should be  initiated. In some individuals, this rash has progressed to Stevens-Johnson syndrome. The incidence of rash is reduced by using a dose escalation. (100,106)
Other common mild to moderate adverse reactions reported with nevirapine use include fever, headaches, nausea, and possibly ulcerative stomatitis. (106)

Drug interactions

Nevirapine is an inducer of the hepatic cytochrome P450 CYP3A isoforms. The manufacturer recommends that nevirapine not be given concurrently with rifampin or rifabutin, and further recommends caution in using nevirapine with oral contraceptives. (106,114)
 
 

Interactions with other antiretroviral agents

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