Cobicistat
A pharmacokinetic enhancer used in antiretroviral therapy
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Cobicistat is a pharmacokinetic enhancer used in combination with other antiretroviral drugs for the treatment of HIV/AIDS. It is not active against HIV itself but enhances the effectiveness of other drugs by inhibiting the cytochrome P450 3A (CYP3A) enzymes, which are responsible for the metabolism of many antiretroviral drugs.
Mechanism of Action
Cobicistat works by inhibiting the CYP3A enzymes in the liver and intestines. This inhibition leads to increased plasma concentrations of drugs that are metabolized by these enzymes, such as atazanavir and darunavir. By boosting the levels of these drugs, cobicistat allows for lower doses to be used, reducing the potential for side effects and improving patient adherence to therapy.
Clinical Use
Cobicistat is used as a component of fixed-dose combination therapies for the treatment of HIV-1 infection. It is commonly found in combination with other antiretrovirals such as elvitegravir, emtricitabine, and tenofovir. These combinations are used in once-daily regimens that simplify treatment and improve adherence.
Pharmacokinetics
Cobicistat is absorbed in the gastrointestinal tract and reaches peak plasma concentrations approximately 3 to 4 hours after oral administration. It is extensively metabolized in the liver, primarily by CYP3A and CYP2D6 enzymes, and is excreted in the feces and urine.
Side Effects
Common side effects of cobicistat include nausea, diarrhea, and fatigue. It can also cause increases in serum creatinine due to inhibition of renal tubular secretion, which may lead to reduced kidney function in some patients. Monitoring of renal function is recommended during treatment.
Drug Interactions
Due to its mechanism of action, cobicistat can interact with a wide range of drugs that are metabolized by CYP3A enzymes. It is important to review a patient's medication list for potential interactions and adjust dosages accordingly.
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Cobicistat
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