• Management of HIV infection in patients who have no antiretroviral treatment history or in those on a stable antiretroviral regimen who are virologically suppression (with HIV-1 RNA <50 copies/mL) and no history of treatment failure or no known substitutions associated with resistance to the individual components of the medication (to replace their current antiretroviral regimen).

Contraindicated in:

• Concurrent use of dofetilide or rifampin
• Severe renal impairment (CCr 15–30 mL/min) or end-stage renal disease (CCr <15 mL/min) not receiving hemodialysis
• Patients with no antiretroviral treatment history and end-stage renal disease (CCr <15 mL/min) who are receiving chronic hemodialysis
• Severe hepatic impairment
• Lactation: Breast feeding not recommended in patients with HIV.

Use Cautiously in:

• Hepatitis B co-infection
• History of suicidal ideation or depression (↑ risk of suicidal thoughts)
• Renal impairment or receiving nephrotoxic medications (↑ risk of renal impairment)
• OB: Use during pregnancy only if potential benefit justifies potential fetal risk
• Pedi: Children weighing <14 kg (safety and effectiveness not established).

GI: ↑ amylase, ↑ liver enzymes, diarrhea, LACTIC ACIDOSIS/HEPATOMEGALY WITH STEATOSIS, nausea.

GU: ACUTE RENAL FAILURE/FANCONI SYNDROME.

Hemat: neutropenia.

Metab: hyperlipidemia.

MS: ↑ creatine kinase.

Neuro: abnormal dreams, dizziness, fatigue, headache, insomnia.

Misc: ACUTE EXACERBATION OF HEPATITIS B, immune reconstitution syndrome.

Drug-Drug:

• Bictegravir may ↑ dofetilide levels and the risk of torsades de pointes; concurrent use contraindicated.
• Rifampin may ↓ bictegravir levels and its effectiveness; concurrent use contraindicated.
• Medications that compete for active tubular secretion, including acyclovir, cidofovir, ganciclovir, valacyclovir, valganciclovir, or aminoglycosides may ↑ emtricitabine and tenofovir levels and toxicity.
• Nephrotoxic agents, including NSAIDs ↑ risk of nephrotoxicity with tenofovir; avoid concurrent use.
• Carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifabutin, and rifapentine may ↓ bictegravir and tenofovir levels and their effectiveness; avoid concurrent use.
• Administration with antacids, containing magnesium or aluminum ↓ absorption of bictegravir; take ≥2 hr before or ≥6 hr after magnesium- or aluminum-containing antacids.
• Administration with supplements or antacids containing calcium or iron↓ absorption of bictegravir; take at the same time as calcium or iron supplements with food (and not on an empty stomach).
• May ↑ metformin levels.

Drug-Natural Products:

• St. John's wort may ↓ bictegravir and tenofovir levels and their effectiveness; avoid concurrent use.

• Tablets: bictegravir 30 mg/emtricitabine 120 mg/tenofovir alafenamide 15 mg; bictegravir 50 mg/emtricitabine 200 mg/tenofovir alafenamide 25 mg;

• PO (Adults and Children ≥25 kg): 1 tablet (bictegravir 50 mg/emtricitabine 200 mg/tenofovir alafenamide 25 mg) once daily.
• PO (Children 14–24 kg): 1 tablet (bictegravir 30 mg/emtricitabine 120 mg/tenofovir alafenamide 15 mg) once daily.

Biktarvy

• Bictegravir: Inhibits HIV-1 integrase, which is required for viral replication; Emtricitabine: Phosphorylated intracellularly where it inhibits HIV reverse transcriptase, resulting in viral DNA chain termination; Tenofovir: Phosphorylated intracellularly where it inhibits HIV reverse transcriptase resulting in disruption of DNA synthesis.

• Slowed progression of HIV infection and decreased occurrence of sequelae.

Therapeutic Classification: antiretrovirals

Pharmacologic Classification: nucleoside reverse transcriptase inhibitors, integrase strand transfer inhibitors (INSTI)

Absorption: Bictegravir: Extent of absorption following oral administration unknown; Emtricitabine: Well absorbed (93%) following oral administration; Tenofovir: Tenofovir alafenamide is a prodrug, which is hydrolyzed into tenofovir, the active component; absorption enhanced by high-fat meals.

Distribution: Bictegravir, emtricitabine, and tenofovir: Unknown.

Protein Binding: Bictegravir: >99%.

Metabolism/Excretion: Bictegravir: Primarily metabolized by the CYP3A4 isoenzyme and UGT1A1 in the liver; 60% excreted in feces, 35% excreted in urine; Emtricitabine: Undergoes some metabolism, 70% excreted in urine, 14% excreted in feces; Tenofovir: Tenofovir is phosphorylated to tenofovir diphosphate (active metabolite); 32% excreted in feces, <1% excreted in urine.

Half-life: Bictegravir: 17.3 hr; Emtricitabine: 10.4 hr; Tenofovir alafenamide: 0.51 hr; Tenofovir diphosphate: 150–180 hr.

(plasma concentrations)

• Emphasize the importance of taking medication as directed. Do not take more than prescribed amount and do not stop taking without consulting health care professional. Take missed doses as soon as remembered, but not if almost time for next dose; do not double doses. Advise patient to read Patient Information before starting therapy and with each Rx refill in case of changes.
• Instruct patient that medication should not be shared with others.
• Inform patient that medication does not cure AIDS or prevent associated or opportunistic infections. Therapy may 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.
• Instruct patient to notify health care professional immediately if symptoms of lactic acidosis (tiredness or weakness, unusual muscle pain, trouble breathing, stomach pain with nausea and vomiting, cold especially in arms or legs, dizziness, fast or irregular heartbeat) or if signs of hepatotoxicity (yellow skin or whites of eyes, dark urine, light colored stools, lack of appetite for several days or longer, nausea, abdominal pain) occur.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications, especially St. John's wort.
• Advise patient to notify health care professional if signs and symptoms of immune reconstitution syndrome (signs and symptoms of an infection) occur.
• Rep: May cause fetal harm. Advise patient taking oral contraceptives to use a nonhormonal method of birth control during therapy. If pregnancy is suspected notify health care professional promptly. Inform pregnant women about the Antiretroviral Pregnancy Registry. Enroll patient by calling 1-800-258-4263. Advise female patient to avoid breast feeding.
• Emphasize the importance of regular follow-up exams and blood counts to determine progress and monitor for side effects.

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