Product: Complera

Company: Gilead Sciences

Pharmacologic class: Nucleoside analogue reverse transcriptase inhibitors + non-nucleoside reverse transcriptase inhibitor.

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Active ingredients: Emtricitabine 200 mg, tenofovir disoproxil fumarate 300 mg, rilpivirine 25 mg; tabs.

Indication: HIV-1 infection.

Pharmacology: Complera is a fixed-dose combination of the antiviral drugs emtricitabine, rilpivirine, and tenofovir disoproxil fumarate. 

Clinical trials: The efficacy of rilpivirine is based on the analyses of 48-week data from two trials (ECHO and THRIVE) in antiretroviral treatment-naïve adults. In ECHO, the background regimen (BR) was tenofovir DF + emtricitabine. In THRIVE, the BR consisted of one of the following: tenofovir DF + emtricitabine, or zidovudine + lamivudine, or abacavir + lamivudine. Subjects were randomized to receive either rilpivirine 25 mg once daily or efavirenz 600 mg once daily in addition to a BR.

Based on the pooled data from both trials at 48 weeks, the proportion of subjects with <50 HIV-1 RNA copies/mL receiving rilpivirine/tenofovir DF/emtricitabine (N=550) compared with subjects receiving efavirenz/tenofovir DF/emtricitabine (N=546) was 83% and 81%, respectively. The mean CD4+ cell count increase from baseline was 193 cells/mm3 for rilpivirine-treated subjects and 182 cells/mm3 for efavirenz-treated subjects. 

Adults: Take with a meal. One tablet once daily. Renal impairment (creatinine clearance [CrCl] <50 mL/min): not recommended.

Children: <18 years: not recommended.

Contraindications: Concomitant carba­mazepine, oxcarbazepine, phenobarbital, phenytoin, rifabutin, rifampin, rifapentine, esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole, systemic dexamethasone (more than single dose), St. John’s wort.

Warnings/Precautions: Suspend if lactic acidosis or hepatotoxicity occurs. Women, obesity, prolonged nucleoside exposure, other risk factors for hepatic dysfunction: increased risk of toxicity. Not for treating chronic hepatitis B; test for hepatitis B virus (HBV) before starting therapy and monitor patients coinfected with HIV-1 and HBV during and for several months after stopping treatment (discontinuing therapy may exacerbate HBV infection). Renal impairment: monitor CrCl and serum phosphorus. May prolong QTc interval with supratherapeutic doses. History or risk of fractures or osteopenia: monitor bone mineral density; consider vitamin D and calcium supplementation. Pregnancy (Cat. B). Nursing mothers: not recommended.

Interactions: Avoid concomitant drugs that contain emtricitabine, tenofovir, rilpivirine, lamivudine, or adefovir dipivoxil. Emtricitabine/tenofovir: Monitor drugs that reduce renal function or compete for renal tubular secretion (e.g., adefovir dipivoxil, cidofovir, acyclovir, valacyclovir, ganciclovir, valganciclovir). Avoid concomitant or recent use of nephrotoxic agents. Rilpivirine: Potentiated by CYP3A inhibitors. Antagonized by CYP3A inducers (see Contraindications). May antagonize azole antifungals (monitor for breakthrough infections), methadone (monitor). Separate antacids (by at least two hours before or at least four hours after) and H2-receptor antagonists (by at least 12 hours before or four hours after); drugs that increase gastric pH may result in decreased plasma concentrations. Caution with drugs with a known risk for torsades de pointes.

Adverse reactions: Insomnia, headache, GI upset, fatigue, dizziness, depression, abnormal dreams, rash; fat redistribution, immune reconstitution syndrome, lactic acidosis, severe hepatomegaly with steatosis (may be fatal).

How supplied: Tabs — 30

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