Bictegravir: Uses, Dosage and Side Effects
Bictegravir is an antiretroviral agent used to treat HIV-1 infection. It belongs to the class of integrase strand transfer inhibitors and is used in combination with other active substances.
Things worth knowing about "Bictegravir"
Bictegravir is an antiretroviral agent used to treat HIV-1 infection. It belongs to the class of integrase strand transfer inhibitors and is used in combination with other active substances.
What is Bictegravir?
Bictegravir is an antiretroviral medication used in the treatment of Human Immunodeficiency Virus type 1 (HIV-1) infection. It belongs to the drug class of integrase strand transfer inhibitors (INSTIs). In clinical practice, bictegravir is exclusively available as a fixed-dose combination with tenofovir alafenamide (TAF) and emtricitabine (FTC), marketed under the brand name Biktarvy.
Mechanism of Action
HIV requires the enzyme integrase to insert its genetic material into the DNA of the human host cell. Bictegravir selectively blocks this step by inhibiting the catalytic activity of the integrase enzyme. This prevents the viral DNA from being permanently integrated into the host cell, thereby stopping the production of new virus copies. This mechanism is highly specific and has minimal impact on human cellular enzymes.
Indications
Bictegravir (as part of Biktarvy) is approved for use in:
- Adults with HIV-1 infection who have not previously received antiretroviral therapy (treatment-naive patients)
- Adults whose virus is stably suppressed and who are switching to a simplified regimen (virologically suppressed patients)
- Adolescents and children above a specified body weight threshold as per current approval
Dosage
The standard dose is one tablet (50 mg bictegravir / 200 mg emtricitabine / 25 mg tenofovir alafenamide) taken once daily, with or without food. The once-daily single-tablet regimen is designed to support medication adherence.
Side Effects
Bictegravir is generally well tolerated. Possible side effects include:
- Common: Headache, nausea, diarrhea, fatigue
- Uncommon: Sleep disturbances, abnormal dreams, dizziness, skin rash
- Rare: Elevated liver enzymes, renal function impairment
As with all antiretroviral medications, bictegravir can in rare cases cause lactic acidosis or worsening of pre-existing liver disease. Regular medical monitoring is recommended.
Drug Interactions
Bictegravir is primarily metabolized via the enzyme CYP3A4 and UGT1A1. Therefore, interactions may occur with the following substances:
- Rifampicin and other strong CYP3A4 inducers: may significantly reduce bictegravir plasma levels and diminish efficacy
- Antacids containing magnesium or aluminum hydroxide: may reduce bictegravir absorption (a time-separated intake is recommended)
- St. John's Wort (Hypericum perforatum): co-administration is contraindicated
Special Considerations
Bictegravir should not be discontinued without medical guidance, as uncontrolled cessation can lead to the development of viral resistance and a rebound in viral load. Use during pregnancy requires careful benefit-risk assessment. Bictegravir is excreted in breast milk; breastfeeding is generally not recommended for HIV-positive mothers.
References
- European Medicines Agency (EMA): Biktarvy - Summary of Product Characteristics. Approved 2018. Available at: https://www.ema.europa.eu
- Panel on Antiretroviral Guidelines for Adults and Adolescents - Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents with HIV. U.S. Department of Health and Human Services. Available at: https://clinicalinfo.hiv.gov
- Gallant J et al. - Bictegravir, Emtricitabine, and Tenofovir Alafenamide versus Dolutegravir, Abacavir, and Lamivudine for Initial Treatment of HIV-1 Infection. Lancet. 2017;387(10231):2117-2127.
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