Pharmacology · Non-nucleoside reverse transcriptase inhibitors (NNRTIs)

Nevirapine !

An old, cheap NNRTI. It can cause hepatitis and severe skin reactions in the first weeks, more often in people with high CD4 counts.

Updated 2026-11-01

Class: Non-nucleoside reverse transcriptase inhibitors (NNRTIs)
Enzyme: HIV-1 reverse transcriptase (NNRTI pocket)
ATC code: J05AG01
WHO Model List of Essential Medicines

Also called: NVP

HIV-1 reverse transcriptase (NNRTI pocket)Nevirapine

The figure shows nevirapine in the allosteric pocket of HIV-1 reverse transcriptase.

Target in 3D: HIV-1 reverse transcriptase (NNRTI pocket). PDB structure 1VRT (RCSB PDB, public domain). View the structure at RCSB PDB

Mechanism of action

Like other NNRTIs, it sits in the allosteric pocket of HIV-1 reverse transcriptase and locks the enzyme. Resistance appears quickly if used alone or added to a failing regimen.

It binds the allosteric pocket of reverse transcriptase
It blocks the enzyme's movement
Viral DNA synthesis stops

Pharmacokinetics

Metabolism: Liver, by CYP3A and CYP2B6; it induces these same enzymes and speeds its own metabolism

Indications

HIV-1 infection, combined with other antiretrovirals HIV infection and AIDS →

Adverse effects

Common

Rash
Nausea
Headache
Raised transaminases

Contraindications

Moderate or severe hepatic impairment
Post-exposure prophylaxis (occupational or non-occupational)

Key interactions

St John's wort: Greatly lowers nevirapine; not recommended
Methadone: Nevirapine lowers methadone (risk of withdrawal)
CYP3A and CYP2B6 substrates: Can lower their levels by induction

What is monitored

Close liver tests during the first 18 weeks
Skin: any rash, especially with fever or systemic symptoms
CD4 before starting

Administration and safety

By mouth
It starts with a two-week lead-in at lower exposure, which reduces rash; if stopped for more than a week, the lead-in is repeated
The dose is not stepped up while a rash is present

Nursing care

Teach to seek care at once for rash, fever, blisters, jaundice or abdominal pain
Check transaminases before and during the first weeks
Record the start date to track the lead-in period

Pregnancy and breastfeeding

Hepatotoxicity risk is higher in women with CD4 above 250 cells/mm³, so it is not started in them unless the benefit justifies it.

Test yourself

Think of the answer, then tap the question to see it.

Which two serious toxicities mark nevirapine use?

Hepatotoxicity and severe skin reactions (Stevens-Johnson), especially in the first weeks.

Who has a higher hepatotoxicity risk when starting nevirapine?

Women with CD4 above 250 cells/mm³ and men with CD4 above 400 cells/mm³.

What is the two-week lead-in for?

It reduces how often rash occurs; if rash appears, the dose is not stepped up until it resolves.

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HIV infection and AIDS

← Back to the class: Non-nucleoside reverse transcriptase inhibitors (NNRTIs)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: DailyMed - NEVIRAPINE tablet (DailyMed (U.S. National Library of Medicine), 2026); Nevirapine: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2025); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); eEML - Electronic Essential Medicines List (World Health Organization, 2025).

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Representative model, for educational purposes only.