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emtricitabine/rilpivirine/tenofovir

General

Pronunciation:
em-tri-si-ti-been/ril–pi-vir-een/te-noe-fo-veer


Trade Name(s)

  • Complera

Pregnancy Category
Category B

Ther. Class.
antiretrovirals

Pharm. Class.
nucleoside reverse transcriptase inhibitors
non nucleoside reverse transcriptase inhibitors

Indications

  • Management of HIV infection in treatment-naïve adults with HIV-1 RNA <100,000 copies/mL at the start of therapy (for use as a complete regiment)
  • Management of HIV infection in patients on a stable antiretroviral regimen with HIV-1 RNA <50 copies/mL (to replace their current antiretroviral regimen)

Action

  • Emtricitabine– Phosphorylated intracellularly where it inhibits HIV reverse transcriptase, resulting in viral DNA chain termination
  • Rilpivirine– Inhibits HIV-replication by noncompetitively inhibiting HIV reverse transcriptase
  • Tenofovir– Phosphorylated intracellularly where it inhibits HIV reverse transcriptase resulting in disruption of DNA synthesis

Therapeutic Effect(s):

Slowed progression of HIV infection and decreased occurrence of sequelae

Pharmacokinetics

emtricitabine

Absorption: Rapidly and extensively absorbed; 93% bioavailable

Distribution: Unknown

Metabolism and Excretion: Some metabolism, 86% renally excreted, 14% fecal excretion

Half-life: 10 hr

rilpivirine

Absorption: Well absorbed following oral administration

Distribution: Unknown

Protein Binding: 99.7%

Metabolism and Excretion: Mostly metabolized by the liver (CYP3A enzyme system); 25% excreted in feces unchanged, <1% excreted unchanged in urine

Half-life: 50 hr

tenofovir

Absorption: Tenofovir disoproxil fumarate is a prodrug, which is split into tenofovir, the active component

Distribution: Absorption is enhanced by food

Metabolism and Excretion: 70–80% excreted unchanged in urine by glomerular filtration and active tubular secretion

Half-life: Unknown

TIME/ACTION PROFILE (blood levels)

ROUTEONSETPEAKDURATION
emtricitabine POrapid1–2 hr 24 hr
rilpivirine POunknown4–5 hr24 hr
tenofovir POunknown2 hr*24 hr
* When taken with food.

Contraindication/Precautions

Contraindicated in:

  • Drugs that may significantly ↓ rilpivirine levels (may ↓ virologic response, ↑ risk of resistance and cross-resistance);
  • Concurrent use of other antiretrovirals;
  • Concurrent use of carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin, rifapentine, proton pump inhibitors, dexamethasone (>1 dose), or St. John's wort
  • Concurrent use of other products containing emtricitabine, rilpivirine (unless dose adjustment needed with rifabutin), tenofovir, lamivudine, or adefovir
  • CCr <50 mL/min
  • Lactation:HIV-infected patients should not breastfeed

Use Cautiously in:

  • History of suicidal ideation or depression
  • History of pathologic fractures/osteoporosis/bone loss
  • OB: Use during pregnancy only if potential benefit justifies potential fetal risk
  • Pedi: Safety and effectiveness not established.

Adverse Reactions/Side Effects

Combination

GI: HEPATOTOXICITY

GU: renal impairment

MS: ↓ bone density

Derm: DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS)

Misc: POST-TREATMENT ACUTE EXACERBATION OF HEPATITIS B, fat redistribution, immune reconstitution syndrome

rilpivirine

CNS: SUICIDAL THOUGHTS, depression, insomnia, headache

emtricitabine/tenofovir

CNS: abnormal dreams, depression, dizziness, fatigue, headache, insomnia

F and E: hypophosphatemia

GI: diarrhea, nausea

Derm: rash

GU: ACUTE RENAL FAILURE/FANCONI SYNDROME

MS: bone pain, ↓ bone mineral density, muscle pain, osteomalacia

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

  • May ↑ risk of nephrotoxicity with other nephrotoxic drugs; avoid if possible
  • Strong CYP3A4 inducers, including carbamazepine, oxcarbazepine, phenobarbital, phenytoin, dexamethasone (more than a single dose), rifabutin, rifampin, and rifapentine may ↓ levels and effectiveness; concurrent use contraindicated; .
  • Proton pump inhibitors including esomeprazole, lansoprazole, omeprazole, pantoprazole, and rabeprazole ↑ gastric pH and may ↓ blood levels and effectiveness; concurrent use contraindicated.
  • Antacids including aluminum hydroxide, magnesium hydroxide, and calcium carbonate ↑ gastric pH and may ↓ blood levels; administer at least 2 hr before or 4 hr after.
  • Blood levels and effectiveness may be ↓ by H2 -receptor antagonists including cimetidine, famotidine, nizatidine, and ranitidine; administer 12 hr after or 4 hr before.
  • Nephrotoxic agents, including NSAIDs ↑ risk of nephrotoxicity; avoid concurrent use
  • Concurrent use of other drugs that ↑ risk of torsade de pointes may ↑ risk of serious arrhythmias
  • May alter requirements for methadone maintenance.
  • Blood levels and risk of adverse effects may be ↑ by clarithromycin, erythromycin, and troleandomycin; consider azithromycin as an alternative

Drug-Natural Products:

St. John's wort may ↓ blood levels and effectiveness; concurrent use contraindicated.

Route/Dosage

PO: (Adults) One tablet once daily. Concurrent rifabutin therapy– Give an additional 25 mg of rilpivirine once daily.

Availability

Tablets: emtricitabine 200 mg/rilpivirine 25 mg/ tenofovir 300 mg

Assessment

  • Assess for change in severity of HIV symptoms and for symptoms of opportunistic infections during therapy.
  • Monitor closely for notable changes in behavior that could indicate the emergence or worsening of suicidal thoughts or behavior or depression.
  • Monitor bone mineral density in patients who have a history of pathologic bone fracture or are at risk for osteoporosis or bone loss.
  • Monitor for signs or symptoms of severe skin or hypersensitivity reactions (severe rash or rash accompanied by fever, blisters, mucosal involvement, conjunctivitis, facial edema, angioedema, hepatitis or eosinophilia). Discontinue Complera immediately if signs develop.
  • Monitor bone mineral density in patients who have a history of pathologic bone fracture or are at risk for osteoporosis or bone loss.

Lab Test Considerations: Monitor viral load and CD4 cell count regularly during therapy.

  • Assess for hepatitis B virus (HBV). Complera is not approved for administration in patients with HIV and HBV.
  • Monitor liver function tests before and periodically during therapy, especially in patients with underlying liver disease or marked ↑ transaminase. May cause ↑ serum creatinine, AST, ALT, total bilirubin, total cholesterol, LDL, and triglycerides. Lactic acidosis may occur with hepatic toxicity causing hepatic steatosis; may be fatal, especially in women.
  • Calculate creatinine clearance (CCr), urine glucose, and urine protein prior to therapy. CCr should be >70 mL/min before starting therapy. Monitor CCr, urine glucose, and urine protein in all patients periodically during therapy and serum phosphorous in patients at risk for renal impairment. Assess patients with persistent or worsening bone pain, pain in extremities, fractures and/or muscular pain or weakness for proximal renal tubulopathy; evaluate renal function promptly.

Potential Diagnoses

Implementation

  • PO: Administer once daily with food

Patient/Family Teaching

  • Emphasize the importance of taking Complera as directed, at the same time each day. Do not take more than prescribed amount and do not stop taking without consulting health care professional. Take missed doses with a meal if remembered <12 hr from the time it is usually taken, then return to regular schedule. If more than 12 hr from time dose is usually taken, omit dose and resume dosing schedule; do not double doses. Advise patient to read Patient Information prior to starting therapy and with each Rx refill in case of changes.
  • Advise patient to take antacids 2 hr before or 4 hr after and H2 -antagonists 12 hr before or 4 hr after Complera.
  • Instruct patient that Complera should not be shared with others.
  • Inform patient that Complera does not cure AIDS or prevent associated or opportunistic infections. Rilpivirine does not reduce the risk of transmission of HIV to others through sexual contact or blood contamination. Caution patient to use a condom and to avoid sharing needles or donating blood to prevent spreading the AIDS virus to others. Advise patient that the long-term effects of Complera are unknown at this time.
  • Advise patient to notify health care professional immediately if symptoms of lactic acidosis (nausea, vomiting, unusual or unexpected stomach discomfort, and weakness) occur.
  • Inform patients and families of risk of suicidal thoughts and behavior and advise that behavioral changes, emergency or worsening signs and symptoms of depression, unusual changes in mood, or emergence of suicidal thoughts, behavior, or thoughts of self-harm should be reported to health care professional immediately.
  • Immune reconstitution syndrome may trigger opportunistic infections or autoimmune disorders. Notify health care professional if symptoms occur.
  • May cause dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
  • Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications, especially St. John's wort.
  • Inform patient that changes in body fat (increased fat in upper back and neck, breast, and around back, chest, and stomach area, loss of fats from legs, arms, and face) may occur.
  • Rep: Advise patients to notify health care professional if pregnancy is planned or suspected. Advise patient to avoid breastfeeding during Complera therapy. Encourage women who become pregnant during Complera therapy to enroll in Antiviral Pregnancy Registry by calling 1-800-258-4263.
  • Emphasize the importance of regular follow-up exams and blood counts to determine progress and monitor for side effects.

Evaluation/Desired Outcomes

  • Delayed progression of AIDS and decreased opportunistic infections in patients with HIV.
  • Decrease in viral load and increase in CD4 cell counts.
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Citation

Quiring, Courtney, et al. "Emtricitabine/rilpivirine/tenofovir." Davis's Drug Guide, 16th ed., F.A. Davis Company, 2019. Medicine Central, im.unboundmedicine.com/medicine/view/Davis-Drug-Guide/110537/all/emtricitabine_rilpivirine_tenofovir.
Quiring C, Sanoski CA, Vallerand AH. Emtricitabine/rilpivirine/tenofovir. Davis's Drug Guide. 16th ed. F.A. Davis Company; 2019. https://im.unboundmedicine.com/medicine/view/Davis-Drug-Guide/110537/all/emtricitabine_rilpivirine_tenofovir. Accessed April 24, 2019.
Quiring, C., Sanoski, C. A., & Vallerand, A. H. (2019). Emtricitabine/rilpivirine/tenofovir. In Davis's Drug Guide. Available from https://im.unboundmedicine.com/medicine/view/Davis-Drug-Guide/110537/all/emtricitabine_rilpivirine_tenofovir
Quiring C, Sanoski CA, Vallerand AH. Emtricitabine/rilpivirine/tenofovir [Internet]. In: Davis's Drug Guide. F.A. Davis Company; 2019. [cited 2019 April 24]. Available from: https://im.unboundmedicine.com/medicine/view/Davis-Drug-Guide/110537/all/emtricitabine_rilpivirine_tenofovir.
* Article titles in AMA citation format should be in sentence-case
TY - ELEC T1 - emtricitabine/rilpivirine/tenofovir ID - 110537 A1 - Quiring,Courtney, AU - Sanoski,Cynthia A, AU - Vallerand,April Hazard, BT - Davis's Drug Guide UR - https://im.unboundmedicine.com/medicine/view/Davis-Drug-Guide/110537/all/emtricitabine_rilpivirine_tenofovir PB - F.A. Davis Company ET - 16 DB - Medicine Central DP - Unbound Medicine ER -