rilpivirine

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Rilpivirine is a next-generation non-nucleoside drug developed by Tibotec Pharmaceuticals.

Like etravirine (TMC 125) also developed by Tibotec, rilpivirine has been designed to remain effective against HIV which has become resistant to first generation NNRTIs like nevirapine and efavirenz.

Update: Rilpivirine was listed on the PBS in Australia in April 2012 for adults with HIV-1 infection. It is intended for use in combination with other antiretroviral agents in initial therapy or for those requiring an alternative agent.

Approval followed its 2011 listing by the FDA in the US which was based primarily on 48-week results of 2 Phase III studies showing that previously untreated individuals who received rilpivirine + 2 nucleoside/nucleotide analogues (NRTIs) had rates of viral suppression and CD4 T-cell increases that were similar to those of individuals who received efavirenz + NRTIs.

Basic info


Generic name rilpivirine
Brand name Edurant
Also known as
Drug class Non-Nucleotide Reverse Transcriptase Inhibitors
Pediatric dosing? Available in doses suitable for children and/or young people.
Availability in Australia Available on the Pharmaceutical Benefits Scheme (PBS) through S100 prescribers since
This drug may be available through clinical trials in Australia.
You may be able to import this drug from overseas for your personal use.
Formulation
Links:


Taking it

Like most anti-HIV drugs, rilpivirine must be taken in combination with other drugs to be completely effective. Commonly, rilpivirine is combined with one other nucleoside (NRTI) drug and either a protease inhibitor or non-nucleoside, although other combinations are sometimes used. Your doctor will advise you on the right combination of drugs to suit your circumstances.



With or without food

rilpivirine must be taken with a high-fat meal

Side effect

All drugs can produce side effects in some people. These may be mild, moderate or severe, so you should be aware of potential side effects before starting any drug, and speak to your doctor if you experience side effects that concern you.


  • Common side effects may include Central Nervous System (CNS) related side effects including dizziness, difficulty with concentration, sleep disturbances, vivid dreams, agitation., nausea (upset stomach, feeling sick to the stomach), dizziness, sleep disturbances.
  • Less common side effects may include rash.
  • It's unlikely you will experience all of these side effects, and you may not experience any side effects at all. Before starting any new drug, ask your doctor about side effects you might experience and discuss strategies for dealing with side effects if they do occur. If you experience any significant side effect you should continue taking your medicine and see your doctor as soon as possible.

Interactions with other drugs

An acidic gastric environment is necessary for absorption of rilpivirine. Medications that increase gastric pH may substantially reduce serum rilpivirine concentrations. Proton pump inhibitors should not be given to persons taking rilpivirine. If H2 receptor antagonists are coadministered, they should be given at least 12 hours before or at least 4 hours after rilpivirine; antacids should be given at least 2 hours before or at least 4 hours after rilpivirine. Rilpivirine is a substrate of hepatic cytochrome P450 3A, so drugs that induce or inhibit the action of this isoenzyme may alter serum rilpivirine levels. In some cases, these interactions may be therapeutically significant. For example, rifamycins (eg, rifampin and rifabutin), certain anticonvulsants (eg, carbamazepine and phenytoin), and St. John's wort may substantially decrease rilpivirine concentrations and should not be given to persons taking rilpivirine.(2) Macrolides and azole antifungals may increase rilpivirine levels. Of the antiretrovirals, protease inhibitors may increase rilpivirine concentrations, whereas the NNRTIs efavirenz, etravirine, and nevirapine may decrease rilpivirine concentrations. The effect of efavirenz may be significant and prolonged, even after efavirenz is discontinued; the management of this interaction (eg, when discontinuing efavirenz and starting rilpivirine) has not been established.(5) Rilpivirine may affect the levels of other medications. For example, it decreases serum levels of ketoconazole and increases levels of atorvastatin.