Biktarvy Bictegravir Sodium Emtricitabine and Tenofovir Alafenamide Fumarate Tablets

1. Indications and Usage
Treatment of HIV-1 Infection:
Indicated for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults and pediatric patients weighing at least 25 kg.
Regimen Status:
A complete regimen; no other antiretroviral drugs are required when used as directed.
2. Dosage and Administration
Recommended Dosage:
Adults and Adolescents (≥12 years or ≥35 kg): One tablet (50 mg bictegravir, 200 mg emtricitabine, 25 mg tenofovir alafenamide) orally once daily.
Pediatric Patients (≥1 year and ≥14 kg to <25 kg): Oral tablet or granules once daily based on weight band.
Administration Instructions:
Can be taken with or without food.
Swallow the tablet whole; do not chew or crush.
Missed Dose:
If a dose is missed and it is less than 18 hours since the usual time of dosing, take the dose as soon as possible and resume the normal schedule.
If more than 18 hours have passed, skip the missed dose and resume the normal schedule.
3. Mechanism of Action
Fixed-Dose Combination:
Bictegravir: An HIV-1 integrase strand transfer inhibitor (INSTI) that blocks the integration of viral DNA into the host genome.
Emtricitabine: A nucleoside analog reverse transcriptase inhibitor (NRTI).
Tenofovir Alafenamide (TAF): A nucleotide analog reverse transcriptase inhibitor (NRTI).
Physiological Effect:
The combination inhibits HIV replication by blocking reverse transcription and integration steps, preventing the virus from infecting new cells.
4. Safety and Warnings
Hepatitis B Virus (HBV) Reactivation:
Severe acute exacerbations of hepatitis B have been reported in patients coinfected with HIV-1 and HBV who discontinue emtricitabine or tenofovir alafenamide. Monitor hepatic function closely for several months after stopping treatment.
Immune Reconstitution Syndrome:
May occur shortly after initiation of antiretroviral therapy.
Renal Impairment:
Avoid use with concurrent or recent use of a nephrotoxic agent (e.g., NSAIDs).
Drug Interactions:
Concomitant use with dofetilide is contraindicated.
5. Adverse Reactions
Most Common:
Diarrhea (6%), nausea (5%), headache (5%), and fatigue.
Laboratory Abnormalities:
Increases in creatine kinase, amylase, and lipase.
6. Drug Interactions
Magnesium- or Aluminum-Containing Antacids:
Separate dosing by at least 2 hours.
Multivalent Cation Supplements:
(e.g., Calcium, Iron, Magnesium) Do not administer concomitantly.
Dofetilide:
Contraindicated due to potential for serious or life-threatening reactions (e.g., QTc prolongation).
Rifampin:
Contraindicated as it significantly decreases bictegravir plasma concentrations.
7. Pharmaceutical Information
Chemical Name:
Bictegravir Sodium:
Sodium (1R,2S)-1-(4-{2-chloro-6-[(2,3,4-trifluorophenyl)carbamoyl]pyridin-3-yl}-2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepin-7-yl)-N-[(1S,2R)-1-hydroxy-1-(2-hydroxyphenyl)propan-2-yl]-2-methylazetidine-2-carboxamide
Emtricitabine:
4-Amino-5-fluoro-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2(1H)-one
Tenofovir Alafenamide Fumarate:
Isopropyl (((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)-L-alaninate hemifumarate