emtricitabine/rilpivirine/tenofovir DF (Rx)

Brand and Other Names:Complera
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Dosing & Uses

AdultPediatric

Dosing Forms & Strengths

emtricitabine/rilpivirine/tenofovir DF (ie, tenofovir disoproxil fumarate)

tablet

  • 200mg/25mg/300mg

HIV Infection

Indicated as a complete regimen for treatment of HIV-1 infection in treatment-naïve adults with HIV-1 RNA ≤100,000 copies/mL at start of therapy and in certain virologically suppressed (HIV-1 RNA <50 copies/mL) patients on a stable antiretroviral therapy (ART)

1 tablet (emtricitabine 200 mg/rilpivirine 25 mg/tenofovir 300 mg) PO qDay with a meal

Dosage Modifications

Coadministration with rifabutin

  • Add 1 tablet of rilpivirine 25 mg with Complera for the duration of rifabutin coadministration

Renal impairment

  • Mild (CrCl ≥50 mL/min): No dosage adjustment necessary
  • Moderate or severe (CrCl <50 mL/min): Not recommended

Hepatic impairment

  • Mild to moderate (Child-Pugh class A or B): No dosage adjustments necessary
  • Severe (Child-Pugh class C): Not studied

Dosing Considerations

Prior to initiation and during treatment

  • Test for hepatitis B virus (HBV) infection
  • Assess serum creatinine, estimated creatinine clearance, urine glucose, and urine protein in all patients
  • Assess serum phosphorus in chronic kidney disease patients

Limitation of use

  • Rilpivirine-treated patients who had >100,000 copies/mL HIV-1 RNA at the start of therapy experienced more virologic failure (HIV-1 RNA ≥50 copies/mL) compared with rilpivirine-treated patients with ≤100,000 copies/mL

Dosage Forms & Strengths

emtricitabine/rilpivirine/tenofovir DF (ie, tenofovir disoproxil fumarate)

tablet

  • 200mg/25mg/300mg

HIV Infection

Indicated as a complete regimen for treatment of HIV-1 infection in treatment-naïve adults and adolescents (≥12 yr who weigh ≥35 kg) with HIV-1 RNA ≤100,000 copies/mL and in certain virologically suppressed (HIV-1 RNA <50 copies/mL) patients on a stable ART regimen at start of therapy in order to replace their current ART regimen

<12 years: Safety and efficacy not established

≥12 years and weight ≥35 kg: 1 tablet (emtricitabine 200 mg/rilpivirine 25 mg/tenofovir 300 mg) PO qDay with a meal

Dosage Modifications

Coadministration with rifabutin

  • Add 1 tablet of rilpivirine 25 mg with Complera for the duration of rifabutin coadministration

Renal impairment

  • Mild (CrCl ≥50 mL/min): No dosage adjustment necessary
  • Moderate or severe (CrCl <50 mL/min): Not recommended

Hepatic impairment

  • Mild to moderate (Child-Pugh class A or B): No dosage adjustments necessary
  • Severe (Child-Pugh class C): Not studied

Dosing Considerations

Prior to initiation and during treatment

  • Test for HBV infection
  • Assess serum creatinine, estimated creatinine clearance, urine glucose, and urine protein in all patients
  • Assess serum phosphorus in chronic kidney disease patients

Limitation of use

  • Rilpivirine-treated patients who had >100,000 copies/mL HIV-1 RNA at the start of therapy experienced more virologic failure (HIV-1 RNA ≥50 copies/mL) compared with rilpivirine-treated patients with ≤100,000 copies/mL
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Interactions

Interaction Checker

and emtricitabine/rilpivirine/tenofovir DF

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    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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            Contraindicated (2)

            • elvitegravir/cobicistat/emtricitabine/tenofovir DF

              emtricitabine, elvitegravir/cobicistat/emtricitabine/tenofovir DF. Other (see comment). Contraindicated. Comment: Elvitegravir/cobicistat/emtricitabine/tenofovir is a complete regimen for HIV and should not be administered with other antiretrovirals.

            • lamivudine

              emtricitabine and lamivudine both increase risk of immune reconstitution syndrome. Contraindicated. Coadministration of emtricitabine containing products and lamivudine containing products should be avoided. Combination will result in therapeutic duplication.

              emtricitabine, lamivudine. Other (see comment). Contraindicated. Comment: Coadministration of emtricitabine containing products and lamivudine containing products should be avoided. Combination will result in therapeutic duplication.

            Serious - Use Alternative (1)

            • cabotegravir

              emtricitabine, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            Monitor Closely (42)

            • abacavir

              abacavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • acyclovir

              acyclovir increases levels of emtricitabine by Other (see comment). Use Caution/Monitor. Comment: Coadministration of emtricitabine with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of emtricitabine.

            • adefovir

              adefovir increases levels of emtricitabine by Other (see comment). Use Caution/Monitor. Comment: Coadministration of emtricitabine with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of emtricitabine.

            • atazanavir

              atazanavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • celecoxib

              emtricitabine, celecoxib. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • cidofovir

              cidofovir increases levels of emtricitabine by Other (see comment). Use Caution/Monitor. Comment: Coadministration of emtricitabine with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of emtricitabine.

            • diclofenac

              emtricitabine, diclofenac. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • diflunisal

              emtricitabine, diflunisal. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • efavirenz

              efavirenz and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • enfuvirtide

              emtricitabine and enfuvirtide both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • etodolac

              emtricitabine, etodolac. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • fenoprofen

              emtricitabine, fenoprofen. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • flurbiprofen

              emtricitabine, flurbiprofen. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • fosamprenavir

              fosamprenavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • ganciclovir

              ganciclovir, emtricitabine. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Use alternatives if available. Increased risk of hematologic toxicity.

              ganciclovir increases levels of emtricitabine by Other (see comment). Use Caution/Monitor. Comment: Coadministration of emtricitabine with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of emtricitabine.

            • ibuprofen

              emtricitabine, ibuprofen. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • ibuprofen IV

              emtricitabine, ibuprofen IV. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • indinavir

              indinavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • indomethacin

              emtricitabine, indomethacin. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • ketoprofen

              emtricitabine, ketoprofen. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • ketorolac

              emtricitabine, ketorolac. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • meclofenamate

              emtricitabine, meclofenamate. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • mefenamic acid

              emtricitabine, mefenamic acid. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • meloxicam

              emtricitabine, meloxicam. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • nabumetone

              emtricitabine, nabumetone. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • naproxen

              emtricitabine, naproxen. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • nelfinavir

              nelfinavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • nevirapine

              emtricitabine and nevirapine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • orlistat

              orlistat will decrease the level or effect of emtricitabine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Loss of virological control reported in HIV-infected patients taking orlistat concomitantly. Exact mechanism is unclear, but may include a drug-drug interaction that inhibits systemic absorption of the antiretroviral drug. Monitor HIV RNA levels frequently and if increased HIV viral load confirmed, discontinue orlistat.

            • oxaprozin

              emtricitabine, oxaprozin. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • piroxicam

              emtricitabine, piroxicam. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • ribavirin

              ribavirin increases toxicity of emtricitabine by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Use alternatives if available. Increased risk of lactic acidosis.

            • ritonavir

              ritonavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • saquinavir

              saquinavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • stavudine

              emtricitabine and stavudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • sulindac

              emtricitabine, sulindac. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • tenofovir DF

              emtricitabine and tenofovir DF both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • tipranavir

              tipranavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • tolmetin

              emtricitabine, tolmetin. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • valacyclovir

              valacyclovir increases levels of emtricitabine by Other (see comment). Use Caution/Monitor. Comment: Coadministration of emtricitabine with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of emtricitabine.

            • valganciclovir

              valganciclovir, emtricitabine. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Use alternatives if available. Increased risk of hematologic toxicity.

              valganciclovir increases levels of emtricitabine by Other (see comment). Use Caution/Monitor. Comment: Coadministration of emtricitabine with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of emtricitabine.

            • zidovudine

              emtricitabine and zidovudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            Minor (0)

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              Adverse Effects

              >10% (rilpivirine)

              Increased ALT (Grade 1: 16%)

              Increased AST (Grade 1: 13%)

              Increased total cholesterol (Grade 1: 13%)

              Increased LDL cholesterol (Grade 1: 11%)

              >10% (emtricitabine and tenofovir)

              Diarrhea

              Nausea

              Fatigue

              Headache

              Dizziness

              Depression

              Insomnia

              Abnormal dreams

              Rash

              1-10% (rilpivirine)

              Increased creatinine (5%)

              Increased total bilirubin (Grade 1: 5%)

              Headache (2%)

              Insomnia (2%)

              Dizziness (1%)

              Nausea (1%)

              Depressive disorder (1%)

              Abnormal dreams (1%)

              Rash (1%)

              1-10% (emtricitabine or tenofovir)

              Abdominal pain

              Dyspepsia

              Vomiting

              Fever

              Pain

              Nasopharyngitis

              Pneumonia

              Sinusitis

              Upper respiratory tract infection

              Arthralgia

              Back pain

              Myalgia

              Paresthesia

              Peripheral neuropathy (including peripheral neuritis and neuropathy)

              Anxiety

              Increased cough

              Rhinitis

              Skin discoloration (hyperpigmentation of palms/soles)

              Postmarketing Reports

              Rilpivirine

              • Renal and urinary disorders: Nephrotic syndrome
              • Skin and subcutaneous tissue disorders: Severe skin and hypersensitivity reactions including DRESS (Drug Reaction with Eosinophilia and Systemic Symptoms)

              Tenofovir

              • Immune system disorders: Allergic reaction, including angioedema
              • Metabolism and nutrition disorders: Lactic acidosis, hypokalemia, hypophosphatemia
              • Respiratory, thoracic, and mediastinal disorders: Dyspnea
              • Gastrointestinal disorders: Pancreatitis, increased amylase, abdominal pain
              • Hepatobiliary disorders: Hepatic steatosis, hepatitis, increased liver enzymes (most commonly AST, ALT gamma GT)
              • Skin and subcutaneous tissue disorders: Rash
              • Musculoskeletal and connective tissue disorders: Rhabdomyolysis, osteomalacia
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              Warnings

              Black Box Warnings

              Posttreatment acute exacerbation of hepatitis B

              • Severe acute exacerbations of hepatitis B reported with coinfection of HBV and HIV-1 and have discontinued emtricitabine (FTC) or tenofovir, which are components of Complera
              • Closely monitor hepatic function with both clinical and laboratory follow-up for at least several months after discontinuing treatment in patients who are coinfected with HIV-1 and HBV; if appropriate, initiation of antihepatitis B therapy may be warranted

              Contraindications

              Hypersensitivity

              Coadministration of the following drugs

              • Anticonvulsants (eg, carbamazepine, oxcarbazepine, phenobarbital, phenytoin)
              • Antimycobacterials (eg, rifabutin, rifampin, rifapentine)
              • Glucocorticoid systemic dexamethasone (more than a single dose)
              • St. John’s wort
              • Proton pump inhibitors (eg, esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole)

              Cautions

              Lactic acidosis/severe hepatomegaly with steatosis

              Coinfection with HIV-1 and HBV (see Black Box Warnings)

              Severe skin and hypersensitivity reactions reported, including cases of drug reaction with eosinophilia and systemic symptoms (DRESS) with rilpivirine (RPV)-containing regimens; discontinue therapy immediately if signs or symptoms of severe skin or hypersensitivity reactions develop, including but not limited to, severe rash or rash accompanied by fever, blisters, mucosal involvement, conjunctivitis, facial edema, angioedema, hepatitis, or eosinophilia; monitor and initiate appropriate therapy

              Hepatic adverse events reported in patients receiving an RPV-containing regimen; a few cases of hepatic toxicity reported in adults who had no preexisting hepatic disease or other identifiable risk factors

              Renal impairment, including cases of acute renal failure and Fanconi syndrome (renal tubular injury with severe hypophosphatemia), with tenofovir DF (TDF)

              Redistribution/accumulation of body fat observed in patients receiving antiretroviral therapy

              May increase risk for immune reconstitution syndrome; autoimmune disorders (such as Graves’ disease, polymyositis, Guillain-Barré syndrome, and autoimmune hepatitis) reported; however, the time to onset is more variable and can occur many months after initiation of treatment

              Severe depressive disorders reported; immediate medical evaluation recommended

              Bone effects of tenofovir DF

              • Bone mineral density may decrease
              • Osteomalacia associated with proximal renal tubulopathy, manifested as bone pain or pain in extremities and which may contribute to fractures, reported

              Drug interactions overview

              • Use of drugs that impair renal function or compete for active tubular secretion may increase serum concentrations of FTC, tenofovir, and/or other renally eliminated drugs
              • Limited information available on potential pharmacodynamic interactions between RPV and drugs that prolong QTc interval; consider alternatives to Complera when coadministered with a drug with a known risk of torsade de pointes
              • Complera is a complete regimen; coadministration with other antiretroviral medications for treatment of HIV-1 infection is not recommended
              • Rilpivirine
                • Rilpivirine is a CYP3A4 substrate
                • Coadministration with CYP3A inducers may decrease plasma levels of RPV and loss of virologic response and possible resistance to RPV or to the class of NNRTIs
                • Coadministration with CYP3A inhibitor may increase plasma levels of RPV
                • Coadministration with drugs that increase gastric pH may decrease plasma levels of RPV and cause loss of virologic response and possible resistance to RPV or to the class of NNRTIs
                • Also see Contraindications
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              Pregnancy & Lactation

              Pregnancy

              Pregnancy exposure registry monitors pregnancy outcomes in individuals exposed to treatment during pregnancy

              Register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263

              Available data from the APR show no increase in overall risk of major birth defects with first-trimester exposure for FTC, RPV, or TDF In a clinical trial, total RPV exposures were generally lower during pregnancy compared with the postpartum period

              Based on HIV-1-infected pregnant individuals who completed a clinical trial through postpartum period with an RPV-based regimen, no dose adjustments are required for pregnant patients who are already on a stable RPV-containing regimen prior to pregnancy and who are virologically suppressed (HIV-1 RNA <50 copies/mL)

              Closely monitor viral load; lower exposures of RPV were observed during pregnancy

              Lactation

              The Centers for Disease Control and Prevention recommends HIV infected mothers not breastfeed their infants to avoid risking postnatal transmission of HIV

              Based on published data, FTC and tenofovir reported to be present in human milk

              No data available on the presence of RPV in human milk; however has been shown to be present in rat milk

              Because of the potential for: HIV transmission (in HIV-negative infants); developing viral resistance (in HIV-positive infants); and adverse reactions in a breastfed infant similar to those seen in adults, instruct mothers not to breastfeed

              Pregnancy Categories

              A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

              B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

              C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

              D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

              X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

              NA: Information not available.

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              Pharmacology

              Mechanism of Action

              Emtricitabine: Nucleoside reverse transcriptase inhibitor (NRTI); following phosphorylation, interferes with HIV viral DNA polymerase and inhibits viral replication; cytosine analogue

              Rilpivirine: Antiviral agent; diarylpyrimidine non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1; inhibits HIV-1 replication by noncompetitive inhibition of HIV-1 reverse transcriptase

              Tenofovir: Nucleoside reverse transcriptase inhibitor (NRTI); following hydrolysis and phosphorylation, inhibits HIV-1 reverse transcriptase by competing with AMP as substrate

              Absorption

              Bioavailability

              • Emtricitabine: 93%
              • Rilpivirine: Exposure 25% higher with combined tablet compared with administration of separate agents; absolute bioavailability unknown
              • Tenofovir: <25% (fasting)

              Peak Plasma Time

              • Emtricitabine: 1-2 hr
              • Rilpivirine: 4-5 hr
              • Tenofovir: 1 hr

              Peak Plasma Concentration

              • Emtricitabine: 1.8 mcg/mL
              • Rilpivirine: 80 ng/mL
              • Tenofovir: 0.3 mcg/mL

              AUC

              • Emtricitabine: 10 mcg•hr/mL
              • Rilpivirine: 2.397 mcg•hr/mL
              • Tenofovir: 2.29 mcg•hr/mL

              Distribution

              Protein Bound

              • Emtricitabine: <4%
              • Rilpivirine: 99.7%
              • Tenofovir: <0.7%

              Metabolism

              Metabolized by

              • Rilpivirine: CYP3A

              Metabolites

              • Emtricitabine: 3′-sulfoxide diastereomers (approximately 9% of the dose) and the glucuronic acid conjugate (approximately 4% of the dose)

              Elimination

              Half-life

              • Emtricitabine: 10 hr
              • Rilpivirine: 50 hr
              • Tenofovir: 17 hr

              Renal clearance

              • Emtricitabine: 213 mL/min
              • Tenofovir: 243.5 mL/min

              Excretion

              • Emtricitabine: Urine 86%; feces 14%
              • Rilpivirine: Urine 6.1%; feces 85%
              • Tenofovir: Urine 70-80%
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              Administration

              Oral Administration

              Take with food

              Storage

              Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F)

              Keep container tightly closed

              Dispense only in original container

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              Patient Handout

              A Patient Handout is not currently available for this monograph.
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              Formulary

              FormularyPatient Discounts

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              The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

              Tier Description
              1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
              2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
              3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
              4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              NC NOT COVERED – Drugs that are not covered by the plan.
              Code Definition
              PA Prior Authorization
              Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
              QL Quantity Limits
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