Usual Adult Dose for HIV Infection

1 tablet orally once a day

Comments:

• Pregnant patients who were already taking this drug before pregnancy and who are virologically suppressed (HIV-1 RNA less than 50 copies/mL) may continue 1 tablet orally once a day; since lower rilpivirine exposures were seen during pregnancy, viral load should be monitored.

Use: As a complete regimen for the treatment of HIV-1 infection, as initial therapy in patients with no antiretroviral treatment history with HIV-1 RNA up to 100,000 copies/mL or to replace a stable antiretroviral regimen in patients who are virologically-suppressed (HIV-1 RNA less than 50 copies/mL) for at least 6 months with no history of treatment failure and no known substitutions associated with resistance to the individual components

Usual Pediatric Dose for HIV Infection

At least 35 kg: 1 tablet orally once a day

Comments:

• Pregnant patients who were already taking this drug before pregnancy and who are virologically suppressed (HIV-1 RNA less than 50 copies/mL) may continue 1 tablet orally once a day; since lower rilpivirine exposures were seen during pregnancy, viral load should be monitored.

Use: As a complete regimen for the treatment of HIV-1 infection, as initial therapy in patients with no antiretroviral treatment history with HIV-1 RNA up to 100,000 copies/mL or to replace a stable antiretroviral regimen in patients who are virologically-suppressed (HIV-1 RNA less than 50 copies/mL) for at least 6 months with no history of treatment failure and no known substitutions associated with resistance to the individual components

Renal Dose Adjustments

Emtricitabine/rilpivirine/tenofovir alafenamide:

• Estimated CrCl at least 30 mL/min: No adjustment recommended.
• Severe renal dysfunction (estimated CrCl 15 to less than 30 mL/min) or ESRD (estimated CrCl less than 15 mL/min) not receiving chronic hemodialysis: Not recommended.

Emtricitabine/rilpivirine/tenofovir disoproxil fumarate (DF):

• Estimated CrCl less than 50 mL/min: Not recommended.

Liver Dose Adjustments

Mild or moderate liver dysfunction (Child-Pugh A or B): No adjustment recommended.
Severe liver dysfunction (Child-Pugh C): Data not available

Dose Adjustments

Emtricitabine/rilpivirine/tenofovir DF:

• If used with rifabutin: An additional 25 mg/day of rilpivirine is recommended.

Precautions

US BOXED WARNING:

• POSTTREATMENT ACUTE EXACERBATION OF HEPATITIS B: Severe acute exacerbations of hepatitis B reported in patients coinfected with HIV-1 and HBV after stopping products containing emtricitabine and/or tenofovir DF, and may occur when tenofovir alafenamide-containing products are stopped. Hepatic function of HIV-1/HBV-coinfected patients should be closely monitored with clinical and laboratory follow-up for at least several months after stopping this drug. If appropriate, antihepatitis B therapy may be necessary.

CONTRAINDICATIONS:

• Coadministration with drugs that may cause loss of virologic response and possible resistance to this drug or to the class of NNRTIs; such drugs include carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin, rifapentine, systemic dexamethasone (more than a single dose), St. John's wort, proton pump inhibitors (e.g., dexlansoprazole, esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole)

Safety and efficacy have not been established in patients weighing less than 35 kg; this drug is not recommended for use in these patients.

Consult WARNINGS section for additional precautions.

Dialysis

Emtricitabine/rilpivirine/tenofovir alafenamide:

• ESRD (estimated CrCl less than 15 mL/min) receiving chronic hemodialysis: Caution recommended.

Emtricitabine/rilpivirine/tenofovir DF: Not recommended.

Comments (emtricitabine/rilpivirine/tenofovir alafenamide):

• Increased monitoring for rilpivirine-related side effects is recommended for ESRD patients receiving chronic hemodialysis.
• On hemodialysis days, dose should be administered after hemodialysis complete.

Other Comments

Administration advice:

• Test patients for HBV infection before/when starting this drug.
• In all patients, assess serum creatinine, estimated CrCl, urine glucose, and urine protein before/when starting this drug, and during therapy with this drug as clinically appropriate; in patients with chronic kidney disease, also assess serum phosphorus.
• Take emtricitabine/rilpivirine/tenofovir alafenamide with a meal.
• Take emtricitabine/rilpivirine/tenofovir DF with food; a protein drink is not a replacement for food.
• Administer antacids (e.g., aluminum/magnesium hydroxide, calcium carbonate) at least 2 hours before or at least 4 hours after this drug; administer H2-receptor antagonists at least 12 hours before or at least 4 hours after this drug.
• Consult the manufacturer product information regarding missed doses.

Storage requirements:

• Store in original bottle; keep bottle tightly closed.
• Emtricitabine/rilpivirine/tenofovir alafenamide: Store below 30C (86F).
• Emtricitabine/rilpivirine/tenofovir DF: Store at 25C (77F); excursions permitted to 15C to 30C (59F to 86F).

General:

• Emtricitabine/rilpivirine/tenofovir alafenamide: Each 3-drug fixed dose combination tablet contains emtricitabine 200 mg, rilpivirine 25 mg, and tenofovir alafenamide 25 mg.
• Emtricitabine/rilpivirine/tenofovir DF: Each 3-drug fixed dose combination tablet contains emtricitabine 200 mg, rilpivirine 25 mg, and tenofovir DF 300 mg.
• Limitations of Use: More rilpivirine-treated patients starting therapy with HIV-1 RNA greater than 100,000 copies/mL had virologic failure (HIV-1 RNA at least 50 copies/mL) compared to those with HIV-1 RNA up to 100,000 copies/mL.

Monitoring:

• General: Viral load in pregnant patients; for rilpivirine-related side effects in ESRD patients receiving chronic hemodialysis who use emtricitabine/rilpivirine/tenofovir alafenamide
• Hepatic: Appropriate laboratory tests (before starting therapy) and for hepatotoxicity (during therapy) in patients with underlying hepatic disease or marked baseline elevations in liver-associated tests; liver-associated tests in patients without preexisting liver dysfunction or other risk factors; hepatic function of HIV-1/HBV-coinfected patients with clinical and laboratory follow-up (for at least several months after stopping therapy)
• Infections/Infestations: For chronic HBV infection in all patients (before/when starting therapy)
• Metabolic: Serum phosphorus in patients with chronic kidney disease (before/when starting and as clinically appropriate during therapy)
• Musculoskeletal: Bone mineral density in patients using emtricitabine/rilpivirine/tenofovir DF with history of pathologic bone fracture or other risk factors for osteoporosis or bone loss
• Renal: Serum creatinine, estimated CrCl, urine glucose, and urine protein in all patients (before/when starting and as clinically appropriate during therapy)

Patient advice:

• Read the US FDA-approved patient labeling (Patient Information).
• If coinfected with HBV and HIV-1, do not stop this drug without first consulting healthcare provider.
• Contact healthcare provider at once if a rash develops. Stop this drug immediately and seek medical attention if rash with fever, blisters, mucosal involvement, eye inflammation (conjunctivitis), severe allergic reaction (swelling of the face, eyes, lips, mouth, tongue, or throat; difficulty swallowing or breathing), and/or any signs/symptoms of liver problems develop.
• Seek medical evaluation at once if depressive symptoms develop.
• Avoid taking this drug with concurrent/recent use of nephrotoxic agents.
• Stop this drug if clinical symptoms suggesting lactic acidosis or pronounced hepatotoxicity develop.
• Notify healthcare provider at once of any symptoms of infection.
• It is important to take this drug on a regular dosing schedule with food; avoid missing doses as it can lead to development of resistance.