Drug of the week series : Biktarvy

Drug Name - Biktarvy

Manufactured by - Gilead Sciences

Class: Integrase strand transfer inhibitor (INSTI) + 2 Nucleoside reverse transcriptase inhibitors (NRTIs)

:test_tube: Composition: Bictegravir (50 mg) + Emtricitabine (200 mg) +Tenofovir alafenamid (25 mg)

:round_pushpin: Mechanism of Action (MOA)

Bictegravir
:dna:Integrase Strand Transfer Inhibitor (INSTI) :right_arrow: Stops the insertion of virus DNA into your healthy immune cells’ DNA.

Emtricitabine and tenofovir alafenamide
:dna: Nucleoside Reverse Transcriptase Inhibitors (NRTIs) :right_arrow: Block virus conversion of RNA into DNA (replication).

:fire: Indication

:right_arrow: Complete regimen :backhand_index_pointing_right: Treatment of human immunodeficiency virus (HIV-1) infections in adults and pediatrics weighing at least 25 kg.

:right_arrow: Suppresses both HIV-1 + HBV coinfection :backhand_index_pointing_right: Suddenly stopping-------- life-threatening liver/HBV flares-up— :magnifying_glass_tilted_left: medical supervision is always required.

:stethoscope: Clinical Uses

:right_arrow: Who have no prior history of antiretroviral treatment.

:right_arrow: To replace virologically suppressed (HIV-1 RNA < 50 copies per ml) current HIV-1 medication.

:right_arrow: No known substitution-associated resistance to bictegravir and tenofovir.

:warning: Warning and Precaution

:right_arrow: Patients with severe renal impairment (CrCl < 30 ml/min).

:right_arrow: Patients with severe hepatic impairment.

:skull_and_crossbones: Contraindication

:cross_mark: Rifampin

:right_arrow: As a metabolic enzyme (CYP450 3A4 and UGT1A1) inducer, :right_arrow_curving_down: Bictarvy.

:right_arrow: Triggers P-glycoprotein: :right_arrow_curving_down: absorption

:cross_mark: Dofetilide

:right_arrow: Bictegravir blocks transport proteins (OCT2 and MATE1) -------- :right_arrow_curving_up: in Dofetilide levels in blood :backhand_index_pointing_right: prolonging QT intervals (Torsades de Points).

:pill: Drug Interaction

:syringe: Metformin - :cross_mark: transfer protein (OCT2, MATE1) in kidney :backhand_index_pointing_right: Metformin :right_arrow_curving_up: ------- lactic acidosis, GI distress.

:syringe: Antacids and polyvalent cations - binds :handshake: with Bictarvy -------- -:right_arrow_curving_down: absorption

:syringe: Anticonvulsants - carbamazepine, oxcarbazepine, phenobarbital, phenytoin :backhand_index_pointing_right: liver metabolic enzyme :right_arrow_curving_up: -------- :right_arrow_curving_up: drug clearance

:syringe: Renal medication - like NSAIDs (ibuprofen, naproxen) and Antivirals (acyclovir, valacyclovir, etc.) competes with Bictarvy for active tubular secretion-------- :right_arrow_curving_up: concentration (Bictarvy).

Common Adverse Reactions

:backhand_index_pointing_right: Nausea, vomitting, diarrhoea, fatigue, headache, etc.

:warning: Severe adverse effects

:right_arrow: Lactic acidosis--------- NRTIs :backhand_index_pointing_right: :cross_mark: DNA polymerase the mitochondria cannot generaete ATP, body shifts to anaerobic metabolism.
:right_arrow: Hepatomegali/ steatosis--------- mitochondrial dysfunction.
:right_arrow: Worsen hepatitis B
:right_arrow: Immune reconstitution syndrome

:bullseye: Clinical Pearls and Exam Essentials

:check_mark: Renal dosing - recommended only when CrCl > 30 mL/min.
:check_mark: Cations - Take Biktarvy on an empty stomach at least 2 or > 2 hours before administering an antacid.
:check_mark: Mineral supplements - If calcium and iron supplements are taken with food simultaneously, take Biktarvy.
:check_mark: Food interaction - can be taken with or without food.
:check_mark: First choice for initial HIV-1 infection.

MBH/PS

3 Likes

Detailed explanation. Very well covered.

1 Like

Thank you for sharing a detailed explanation of this drug. It was introduced around 2018 and has been in use ever since.

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Insightful

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Informative read

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Thank you for your kind words.

Glad you find the article informative.

Glad you find the article insightful.

1 Like

Yes!
Thank you for adding value to it.