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# Rilpivirine

A second-generation NNRTI. It is absorbed only with food and stomach acid; there is also a long-acting injectable form.

Updated 2026-11-01

- Class: [Non-nucleoside reverse transcriptase inhibitors (NNRTIs)](https://durgical.com/en/pharmacology/classes/non-nucleoside-reverse-transcriptase-inhibitors/)
- Enzyme: HIV-1 reverse transcriptase (NNRTI pocket)
- ATC code: J05AG05

Also called: RPV

✂**HIV-1 reverse transcriptase (NNRTI pocket)**Rilpivirine

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

**Target in 3D:** HIV-1 reverse transcriptase (NNRTI pocket). PDB structure 2ZD1 (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/2ZD1) · Drag to rotate · pinch to zoom

## Mechanism of action

A flexible NNRTI that fits the allosteric pocket of reverse transcriptase even when the pocket changes shape, so it keeps activity against some mutations that defeat efavirenz and nevirapine.

- It adapts to the allosteric pocket of reverse transcriptase
- It locks the enzyme
- Viral DNA synthesis stops

## Pharmacokinetics

**Absorption**
Needs food and an acidic stomach to be absorbed

**Metabolism**
Liver, by CYP3A

## Indications

- HIV-1 infection, combined with other antiretrovirals, in people without very high viral load [HIV infection and AIDS →](https://durgical.com/en/conditions/hiv-infection-and-aids/)
- As a long-acting injectable with cabotegravir to maintain viral suppression [HIV infection and AIDS →](https://durgical.com/en/conditions/hiv-infection-and-aids/)

## Adverse effects

### Common

- Headache
- Insomnia
- Rash
- Depressive symptoms

### Serious (rare, important)

- Severe depressive disorders
- Severe skin and hypersensitivity reactions
- QTc prolongation at high exposures
- Hepatotoxicity

## Contraindications

- Proton pump inhibitors
- Strong CYP3A inducers: rifampicin, carbamazepine, oxcarbazepine, phenytoin, St John's wort, among others

## Key interactions

**Proton pump inhibitors**
They raise gastric pH and rilpivirine is not absorbed: contraindicated

**Antacids and H2 blockers**
Reduce absorption; doses are separated in time

**QT-prolonging drugs**
Alternatives are preferred

## What is monitored

- Viral load and CD4
- Mood
- Liver tests

## Administration and safety

- By mouth, always with a meal
- Check the medication list for any proton pump inhibitor before starting
- The long-acting injectable is given intramuscularly by health staff

## Nursing care

- Teach to take it with food
- Ask about heartburn medicines, including over-the-counter ones
- Watch for depressive symptoms

## Pregnancy and breastfeeding

The label describes use in pregnant people already suppressed on rilpivirine; the treating team decides.

## Memory aid

'Rilpivirine wants a meal and acid': no proton pump inhibitors.

## Test yourself

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

## Why are proton pump inhibitors contraindicated with rilpivirine?

Because rilpivirine needs an acidic stomach to be absorbed; with high pH its levels fall and resistance appears.

## Which drug is long-acting injectable rilpivirine combined with?

With injectable cabotegravir.

## What structural advantage does rilpivirine have over efavirenz?

It is flexible and adapts to the mutated allosteric pocket, so it keeps activity against some mutations.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/rilpivirine/)

## Related drugs

- [Efavirenz](https://durgical.com/en/pharmacology/efavirenz/)
- [Doravirine](https://durgical.com/en/pharmacology/doravirine/)
- [Cabotegravir](https://durgical.com/en/pharmacology/cabotegravir/)

## Related conditions

- [HIV infection and AIDS](https://durgical.com/en/conditions/hiv-infection-and-aids/)

[← Back to the class: Non-nucleoside reverse transcriptase inhibitors (NNRTIs)](https://durgical.com/en/pharmacology/classes/non-nucleoside-reverse-transcriptase-inhibitors/)

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 - RILPIVIRINE tablet, film coated](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=dadbf50d-6b7d-4fb5-bd9f-7769b048e764) (DailyMed (U.S. National Library of Medicine), 2026); [Rilpivirine: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a611037.html) (MedlinePlus (U.S. National Library of Medicine), 2025); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=J05AG05) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/rilpivirine/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/rilpivirine/