Rilpivirine

Information about Rilpivirine

Rilpivirine is a nonnucleoside reverse transcriptase inhibitor used in combination with other antiretroviral agents in the therapy of human immunodeficiency virus (HIV) infection.

Liver safety of Rilpivirine

Rilpivirine is associated with a low rate of transient serum aminotransferase elevations during therapy and has been implicated in rare cases of clinically apparent acute liver injury.

Mechanism of action of Rilpivirine

Rilpivirine (ril" pi vir' een) is an antiretroviral agent that acts by noncompetitive binding to, and inhibition of the HIV reverse transcriptase. Rilpivirine is a nonnucleoside reverse transcriptase inhibitor similar in action to nevirapine, efavirenz, delavirdine and etavirine. In several randomized controlled trials, rilpivirine was found to have similar efficacy to efavirenz when combined with at least two nucleoside analogues (typically tenofovir and emtricitabine). Rilpivirine was the fifth nonnucleoside reverse transcriptase inhibitor approved by the FDA [2011], and current indications are for the treatment of HIV infection in combination with other HIV medications.

Dosage and administration for Rilpivirine

Rilpivirine is available under the brand name Edurant in tablets of 25 mg. The recommended dose is 25 mg orally once daily with a meal. Rilpivirine is also available in a fixed dose combination (25 mg) once a day tablet with emtricitabine (200 mg) and tenofovir disoproxil fumarate (300 mg) under the brand name Complera [2011] and a similar combination with tenofovir alafenamide fumarate (25 mg) under the brand name Odefsey [2016]. Antiviral resistance can occur and resistance patterns are similar to, and cross react with those due to other nonnucleoside reverse transcription inhibitors.

Side effects of Rilpivirine

Common side effects include fatigue, dizziness, headache, insomnia, depression and skin rashes.

Antiviral agents

Drugs for HIV Infection, in the Subclass Antiretroviral Agents

• Fusion Inhibitors (HIV)
  • Enfuvirtide, Maraviroc

• Integrase Inhibitors (HIV)
  • Dolutegravir, Elvitegravir, Raltegravir

• Monoclonal Antibodies
  • Ibalizumab

• Nonnucleoside Reverse Transcriptase Inhibitors (HIV)
  • Delavirdine, Efavirenz, Etravirine, Nevirapine, Rilpivirine

• Nucleoside Analogues (HIV)
  • Abacavir, Didanosine, Emtricitabine, Lamivudine, Stavudine, Tenofovir, Zidovudine

• Protease Inhibitors (HIV)
  • Amprenavir, Atazanavir, Darunavir, Fosamprenavir, Indinavir, Lopinavir, Nelfinavir,Ritonavir, Saquinavir, Tipranavir

Drugs for Hepatitis B

• • Alpha Interferon, Adefovir, Emtricitabine, Entecavir, Lamivudine, Telbivudine, Tenofovir

Drugs for Hepatitis C

• Interferon Based Therapies
  • Alpha Interferon and Peginterferon, Ribavirin

HCV NS5A Inhibitors

• Daclatasvir, Elbasvir, Ledipasvir, Ombitasvir, Pibrentasvir, Velpatasvir

HCV NS5B (Polymerase) Inhibitors

• Dasabuvir, Sofosbuvir

HCV Protease Inhibitors

• Asunaprevir, Boceprevir, Glecaprevir, Grazoprevir, Paritaprevir, Simeprevir, Telaprevir, Voxilaprevir

Combination Therapies

• Epclusa, Harvoni, Mavyret, Technive, Viekira Pak, Vosevi, Zepatier

Drugs for Herpes Virus Infections (HSV, CMV, others)

• Acyclovir, Cidofovir, Famciclovir, Foscarnet, Ganciclovir, Valacyclovir, Valganciclovir

Drugs for Influenza

• Amantadine, Oseltamivir, Peramivir, Rimantadine, Zanamivir

• Dailymed label info on Rilpivirine
• FDA Rilpivirine

Rilpivirine

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  Rilpivirine
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  Rilpivirine 3D Structure
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  Rilpivirine Metabolism Example