section name header

Pronunciation ⬇

em-tri-SYE-ti-been/te-NOE-fo-veer al-a-FEN-a-mide

Classifications ⬆ ⬇

Therapeutic Classification: antiretrovirals

Pharmacologic Classification: nucleoside reverse transcriptase inhibitors

Indications ⬆ ⬇

REMS

Action ⬆ ⬇

  • Emtricitabine and tenofovir alafenamide: Phosphorylated intracellularly, where they inhibit HIV reverse transcriptase, resulting in inhibition of viral replication.
Therapeutic effects:
  • Slowed progression of HIV infection and decreased occurrence of sequelae.
  • Reduction in risk of sexually acquired HIV infection in at-risk individuals.

Pharmacokinetics ⬆ ⬇

Emtricitabine

Absorption: Extent of absorption following oral administration unknown.

Distribution: Unknown.

Metabolism/Excretion: Undergoes some metabolism with 70% renally excreted and 14% excreted in feces as metabolites.

Half-Life: 10 hr.

Tenofovir Alafenamide

Absorption: Tenofovir alafenamide is a prodrug, which is hydrolyzed into tenofovir; absorption ↑ by high-fat meals.

Distribution: Unknown.

Metabolism/Excretion: Tenofovir is phosphorylated to tenofovir diphosphate (active metabolite); 32% excreted in feces, <1% in urine.

Half-Life: 0.51 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTEONSETPEAKDURATION
Emtricitabine POrapid3 hr24 hr
Tenofovir POrapid1 hr24 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects ⬆ ⬇

GI: abdominal pain, diarrhea, LACTIC ACIDOSIS/HEPATOMEGALY WITH STEATOSIS, nausea

GU: ACUTE RENAL FAILURE/FANCONI SYNDROME, renal impairment

MS: ↓bone mineral density

Neuro: headache

Misc: immune reconstitution syndrome

Interactions ⬆ ⬇

Drug-drug:

Drug-Natural Products:

Route/Dosage ⬆ ⬇

HIV-1 Infection

Renal Impairment

Renal Impairment

HIV-1 PrEP

Renal Impairment

Renal Impairment

Availability ⬆ ⬇

(Generic available)
  • Tablets: emtricitabine 200 mg/tenofovir alafenamide 25 mg; emtricitabine 120 mg/tenofovir alafenamide 15 mg

Assessment ⬆ ⬇

  • Assess for change in severity of HIV symptoms or new onset HIV symptoms, and for signs/symptoms of opportunistic infections during therapy.
  • Monitor for severe acute HBV exacerbation; may occur with discontinuation of therapy. If patient with HBV discontinues therapy, monitor clinically and with laboratories for several months after discontinuation; consider therapy for HBV as indicated.
  • Monitor for immune reconstitution syndrome (inflammatory response to opportunistic infection and development of autoimmune disorders) in patients with HIV-1, especially during therapy initiation.
  • Monitor for signs/symptoms of lactic acidosis and severe hepatomegaly with steatosis. If lactic acidosis suspected or hepatotoxicity, even in the absence of marked ↑ in transaminases, occurs, discontinue emtricitabine/tenofovir alafenamide.

Lab Test Considerations:

  • Prior to initiation for treatment of HIV infection, assess HBV status.
  • Prior to initiation and regularly during treatment of HIV infection, assess serum creatinine, estimated CCr, urine glucose, and urine protein. Additionally, monitor serum phosphorous in patients with chronic kidney disease. If clinically significant ↓ in renal function or Fanconi syndrome occurs, discontinue therapy.
  • Confirm negative HIV status prior to initiating PrEP. Screen for HIV-1 at least every 3 mo and upon diagnosis of other sexually transmitted infections during use for PrEP. If HIV-1 infection suspected, convert PrEP to an HIV treatment regimen until negative infection status confirmed.
  • Monitor liver function tests for at least several months in patients with HBV who discontinue emtricitabine/tenofovir/alafenamide.

Implementation ⬆ ⬇

  • Do not confuse emtricitabine, tenofovir alafenamide with emtricitabine, tenofovir disoproxil fumarate.
  • Encourage HBV negative patients to complete HBV vaccination.
  • PO: Administer once daily without regard to food.

Patient/Family Teaching ⬆ ⬇

  • Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy.
  • Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care provider before taking other medications.
  • Caution HIV-1 positive patient that missing doses may result in development of drug resistance.
  • Inform HIV-1 positive patient that emtricitabine/tenofovir alafenamide does not cure HIV but may ↓ risk of transmission; use a condom and avoid sharing needles or donating blood to prevent spreading HIV.
  • Counsel HIV-1 negative patient on the use of other HIV prevention measures (condom use, knowledge of partners’ HIV status, regular screening of sexually transmitted infections) and to strictly adhere to daily dosing schedule. Prevention effectiveness is strongly correlated with adherence.
  • Advise HIV-1 negative patient to immediately notify health care provider of suspected HIV-1 exposure and symptoms of acute HIV-1 infection (fever, headache, fatigue, arthralgia, vomiting, myalgia, diarrhea, pharyngitis, rash, night sweats, adenopathy).
  • Advise patient not to stop therapy without consulting health care provider; may lead to severe HBV exacerbation. Inform patient of importance of HBV testing and, if negative, vaccination before starting therapy.
  • Advise patient to notify health care provider immediately if signs/symptoms of lactic acidosis (nausea, vomiting, unusual stomach discomfort, weakness), hypersensitivity (swelling of face, eyes, lips, mouth, tongue, or throat; difficulty breathing), or liver disease (yellow skin or conjunctiva, dark urine, light-colored stool, loss of appetite, nausea, abdominal pain) occurs.
  • Inform patient that therapy may trigger reconstitution syndrome; advise patient to notify health care provider if signs/symptoms of opportunistic infections or autoimmune disorders occur.
  • Rep: Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected or if breastfeeding. Encourage patient/health care provider to register pregnancies in the Antiretroviral Pregnancy Registry: 1-800-258-4263. Inform HIV-1 positive patient of potential risks of breastfeeding, including transmission to HIV-1 negative infant, development of viral resistance in HIV-1 negative infant, and adverse reactions in infant similar to those of adults.

Evaluation/Desired Outcomes ⬆ ⬇

  • Slowed progression of HIV infection and ↓ occurrence of sequelae.
  • Reduction in risk of sexually acquired HIV infection in at-risk individuals.

US Brand Names ⬆ ⬇

Descovy

Code ⬆

NDC Code