Drug Name - Biktarvy
Manufactured by - Gilead Sciences
Class: Integrase strand transfer inhibitor (INSTI) + 2 Nucleoside reverse transcriptase inhibitors (NRTIs)
Composition: Bictegravir (50 mg) + Emtricitabine (200 mg) +Tenofovir alafenamid (25 mg)
Mechanism of Action (MOA)
Bictegravir
Integrase Strand Transfer Inhibitor (INSTI)
Stops the insertion of virus DNA into your healthy immune cells’ DNA.
Emtricitabine and tenofovir alafenamide
Nucleoside Reverse Transcriptase Inhibitors (NRTIs)
Block virus conversion of RNA into DNA (replication).
Indication
Complete regimen
Treatment of human immunodeficiency virus (HIV-1) infections in adults and pediatrics weighing at least 25 kg.
Suppresses both HIV-1 + HBV coinfection
Suddenly stopping-------- life-threatening liver/HBV flares-up—
medical supervision is always required.
Clinical Uses
Who have no prior history of antiretroviral treatment.
To replace virologically suppressed (HIV-1 RNA < 50 copies per ml) current HIV-1 medication.
No known substitution-associated resistance to bictegravir and tenofovir.
Warning and Precaution
Patients with severe renal impairment (CrCl < 30 ml/min).
Patients with severe hepatic impairment.
Contraindication
Rifampin
As a metabolic enzyme (CYP450 3A4 and UGT1A1) inducer,
Bictarvy.
Triggers P-glycoprotein:
absorption
Dofetilide
Bictegravir blocks transport proteins (OCT2 and MATE1) --------
in Dofetilide levels in blood
prolonging QT intervals (Torsades de Points).
Drug Interaction
Metformin -
transfer protein (OCT2, MATE1) in kidney
Metformin
------- lactic acidosis, GI distress.
Antacids and polyvalent cations - binds
with Bictarvy -------- -
absorption
Anticonvulsants - carbamazepine, oxcarbazepine, phenobarbital, phenytoin
liver metabolic enzyme
--------
drug clearance
Renal medication - like NSAIDs (ibuprofen, naproxen) and Antivirals (acyclovir, valacyclovir, etc.) competes with Bictarvy for active tubular secretion--------
concentration (Bictarvy).
Common Adverse Reactions
Nausea, vomitting, diarrhoea, fatigue, headache, etc.
Severe adverse effects
Lactic acidosis--------- NRTIs
DNA polymerase the mitochondria cannot generaete ATP, body shifts to anaerobic metabolism.
Hepatomegali/ steatosis--------- mitochondrial dysfunction.
Worsen hepatitis B
Immune reconstitution syndrome
Clinical Pearls and Exam Essentials
Renal dosing - recommended only when CrCl > 30 mL/min.
Cations - Take Biktarvy on an empty stomach at least 2 or > 2 hours before administering an antacid.
Mineral supplements - If calcium and iron supplements are taken with food simultaneously, take Biktarvy.
Food interaction - can be taken with or without food.
First choice for initial HIV-1 infection.
MBH/PS
