Emtricitabine, Rilpivirine And Tenofovir Disoproxil Fumarate

Brand Names: Emtricitabine, Rilpivirine And Tenofovir Disoproxil Fumarate

Drug Class: Human Immunodeficiency Virus Nucleoside Analog Reverse Transcriptase Inhibitor

Overview

11 DESCRIPTION Emtricitabine, rilpivirine and tenofovir disoproxil fumarate tablets are a fixed-dose combination tablet containing FTC, rilpivirine hydrochloride, and TDF. Emtricitabine, USP (FTC) is a synthetic nucleoside analog of cytidine. Rilpivirine (RPV) is a non-nucleoside reverse transcriptase inhibitor.

Mechanism of Action

12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Emtricitabine, rilpivirine and tenofovir disoproxil fumarate tablets are a fixed-dose combination of the antiretroviral drugs FTC, RPV, and TDF [see Microbiology (12.4) ]. 12.2 Pharmacodynamics Effects on Electrocardiogram The effect of RPV at the recommended dose of 25 mg once daily on the QTcF interval was evaluated in a randomized, placebo-, and active- (moxifloxacin 400 mg once daily) controlled crossover study in 60 healthy adults, with 13 measurements over 24 hours at steady state. The maximum mean time-matched (95% upper confidence bound) differences in QTcF interval from placebo after baseline correction was 2.0 (5.0) milliseconds (i.e., below the threshold of clinical concern).

Indications

  • 1 INDICATIONS AND USAGE Emtricitabine, rilpivirine and tenofovir disoproxil fumarate tablets are indicated as a complete regimen for the treatment of HIV-1 infection in adults and pediatric patients weighing at least 35 kg: • as initial therapy in those with no antiretroviral treatment history with HIV-1 RNA less than or equal to 100,000 copies/mL at the start of therapy or • to replace a stable antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA less than 50 copies/mL) on a stable antiretroviral regimen for at least 6 months with no treatment failure and no known...

Common Doses

  • 50 mL
  • 25 mg
  • 200 mg
  • 300 mg

Dosage

2 DOSAGE AND ADMINISTRATION • Testing: Prior to or when initiating emtricitabine, rilpivirine and tenofovir disoproxil fumarate tablets, test for hepatitis B virus infection. Prior to initiation and during treatment with emtricitabine, rilpivirine and tenofovir disoproxil fumarate tablets, on a clinically appropriate schedule, assess serum creatinine, estimated creatinine clearance, urine glucose, and urine protein in all patients. In patients with chronic kidney disease, also assess serum phosphorus. ( 2.

Black Box Warning

WARNING: POSTTREATMENT ACUTE EXACERBATION OF HEPATITIS B Severe acute exacerbations of hepatitis B virus (HBV) have been reported in patients who are coinfected with HBV and HIV-1 and have discontinued products containing emtricitabine (FTC) and/or tenofovir disoproxil fumarate (TDF), two of the components of emtricitabine, rilpivirine and tenofovir disoproxil fumarate tablets . Closely monitor hepatic function with both clinical and laboratory follow-up for at least several months in patients who are coinfected with HIV-1 and HBV and discontinue emtricitabine, rilpivirine and tenofovir...

Contraindications

  • 4 CONTRAINDICATIONS Emtricitabine, rilpivirine and tenofovir disoproxil fumarate tablets are contraindicated when coadministered with the following drugs; coadministration may result in loss of virologic response and possible resistance to emtricitabine, rilpivirine and tenofovir disoproxil fumarate tablets or to the class of NNRTIs [see Warnings and Precautions (5.7) , Drug Interactions (7) , and Clinical Pharmacology (12.

Side Effects

  • 6 ADVERSE REACTIONS The following adverse reactions are discussed in other sections of the labeling: • Severe Acute Exacerbations of Hepatitis B in Patients Coinfected with HIV-1 and HBV [see Warnings and Precautions (5.1) ]. • Skin and Hypersensitivity Reactions [see Warnings and Precautions (5.2) ]. • Hepatotoxicity [see Warnings and Precautions (5.3) ]. • Depressive Disorders [see Warnings and Precautions (5.4) ]. • New Onset or Worsening Renal Impairment [see Warnings and Precautions (5.5) ]. • Bone Loss and Mineralization Defects [see Warnings and Precautions (5.6) ].

Interactions

  • 7 DRUG INTERACTIONS • Emtricitabine, rilpivirine and tenofovir disoproxil fumarate tablets are a complete regimen for the treatment of HIV-1 infection; therefore, coadministration with other antiretroviral medications for treatment of HIV-1 infection is not recommended. ( 7.1 ) • Consult the Full Prescribing Information prior to and during treatment for important drug interactions. ( 4 , 5.7 , 7 ) 7.1 Not Recommended with Other Antiretroviral Medications Because emtricitabine, rilpivirine and tenofovir disoproxil fumarate tablets are a complete regimen, coadministration with other...