Edurant (rilpivirine) - HIV Drug Information

Second-Generation Drug Offers Lower Side Effects, Longer Half Life

Courtesy Janssen Pharmaceuticals

Drug Classification

Edurant (rilpivirine) is classified as a non-nucleoside reverse transcriptase inhibitor (NNRTI) for use in the treatment of HIV. Edurant was approved by the U.S. Food and Drug Administration (FDA) in May 2011. In 2015 the FDA updated its treatment guidelines, recommending Edurant for patients 12 years of age of older who

  • weigh at least 77 lbs (33kg);
  • have a CD4 count over 200 cells/mL, and; 

Edurant is considered an advance over first-generation NNRTIs such as Sustiva (efavirenz) and Viramune (nevirapine), offering a lower pill burden, fewer side effects, a longer half life, and far superior drug resistance profile

The drug rilpivirine is also a component of the fixed dose combination drug Complera (rilpivirine + tenofovir + emtricitabine), allowing for a once-daily, all-in-one combination HIV therapy.

Drug Formulation

A white, round, film-coated, 25mg tablet embossed with "346" on one side and "TMC" on the other. The pill is very small, measuring 6.4mm in diameter (or approximately 0.04 inches).

Dosing Recommendations

One 25mg tablet taken orally, once daily as part of combination antiretroviral therapy (ART). Edurant must be taken with a meal, ideally one with high fat, to ensure optimal metabolism. Replacement meals or protein drinks should not be considered alternatives.

Edurant should be stored at room temperature between 68°F to 77°F (20°C to 25°C) and in the original container to avoid direct light exposure.

Common Side Effects

A number of drug side effects have been noted in clinical trial patients taking Edurant. The most common adverse events, reported in 2% or more of patients, are:

  • Abdominal pain
  • Fatigue
  • Headache
  • Depression
  • Insomnia
  • Abnormal dreams
  • Rash

Side effects were typically transient, resolving over the course of one to several weeks, with few patients discontinuing as a result of treatment intolerance.

Drug Contraindications

Edurant should not be taken with the following drugs or supplements:

  • Anti-seizure medications: Carbatrol, Equetro, Tegretol, Tegretol-XR, Teril, Epitol, Trileptal, Luminal, Dilantin, Dilantin-125, Phenytek
     
  • Rifampin-based anti-tuberculosis medications: Mycobutin, Rifater, Rifamate, Rimactane, Rifadin, Priftin
     
  • Proton pump inhibitors: Nexium, Vimovo, Prevacid, Prilosec, Zegerid, Protonix, Aciphex
     
  • More than one dose of the steroid dexamethasone or dexamethasone sodium phosphate
     
  • St. John's Wort

Treatment Considerations

Inform your doctor of any liver condition you may have before starting Edurant. There may be increased risk for liver problems in some, particularly for people with a hepatitis diagnosis or a pre-existing liver dysfunction. Liver enzymes should be regularly monitored as part of a person's routine blood tests when taking Edurant.

Advise your doctor if you have had any liver disease or disorder, of if you had either hepatitis B or hepatitis C.  

Additionally, advise your doctor if you have any mental health problems before starting Edurant as the drug may further complicate these conditions.

Antacids with aluminum, magnesium hydroxide, or calcium carbonate can prevent Edurant from being properly absorbed. If you're using an over-the counter antacid (like Rolaids or Tums), it is suggested that it be taken two hours before or four hours after a dose of Edurant.

H2-receptor antagonists used to block stomach acid (like Tagamet, Pepcid, Axid or Zantac) can also block absorption. It is suggested that these be taken twelve hours before or four hours after a dose of Edurant.

While Edurant is not contraindicated during pregnancy (with animal studies showing no adverse effect to fetal development, even when used in amounts 15-70 times that of humans), HIV-positive mothers should be advised not to breastfeed whether on Edurant or not.

Sources:

U.S. Food and Drug Administration (FDA). "FDA approves new HIV treatment." Silver Spring, Maryland; press release issued on May 20, 2011.

FDA. "EDURANT - Highlights of Prescribing Information." Accessed March 28, 2016

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