Products
Rilpivirine has been commercially available in the EU and the United States since 2011 in tablet form (Edurant, combination products). In many countries, rilpivirine was approved in February 2013.
Structure and properties
Rilpivirine (C22H18N6, Mr = 366.4 g/mol) has a non-nucleoside structure. It is a diarylpyrimidine and is present in drugs as rilpivirine hydrochloride, a white powder that is practically insoluble in water.
Effects
Rilpivirine (ATC J05AG05) has antiviral properties against HIV-1, with effects based on inhibition of reverse transcriptase. The agent was developed as an alternative to efavirenz.
Indications
For treatment of infection with HIV-1 (combination antiretroviral therapy).
Dosage
According to the SmPC. The usual dose is 25 mg. Rilpivirine is taken once daily with a meal. Administration with meals is necessary because bioavailability is reduced by approximately 40% in the fasting state.
Contraindications
- Hypersensitivity
- Combination with certain drugs (see below)
Full details of precautions and interactions can be found in the drug label.
Interactions
Rilpivirine is metabolized by CYP3A. Combination with the CYP inducers carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifabutin, rifampin, rifapentine, and St. John’s wort is contraindicated because these agents may decrease plasma concentrations of rilpivirine. Also contraindicated is concomitant administration of proton pump inhibitors because they cause an increase in gastric pH and multiple doses of dexamethasone. Furthermore, combination with drugs that can prolong the QT interval and induce cardiac arrhythmias should be avoided.
Adverse effects
The most common possible adverse effects include depression, insomnia, headache, and skin rash. Rilpivirine may prolong the QT interval.
