Doravirine

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Doravirine

Chemical structure of Doravirine

Doravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used in the treatment of HIV/AIDS. It is marketed under the brand name Pifeltro and is used in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults. Doravirine is known for its efficacy in suppressing the viral load and its favorable side effect profile compared to other NNRTIs.

Mechanism of Action

Doravirine works by inhibiting the activity of the reverse transcriptase enzyme, which is crucial for the replication of HIV. By binding to the reverse transcriptase enzyme, doravirine prevents the conversion of viral RNA into DNA, thereby blocking the replication of the virus within the host cell.

Pharmacokinetics

Doravirine is administered orally and is well absorbed in the gastrointestinal tract. It has a half-life of approximately 15 hours, allowing for once-daily dosing. The drug is metabolized primarily by the cytochrome P450 enzyme CYP3A4, and it is excreted in both urine and feces.

Clinical Use

Doravirine is indicated for use in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults who have no prior antiretroviral treatment history. It is also used in patients who are virologically suppressed on a stable antiretroviral regimen for at least six months.

Side Effects

Common side effects of doravirine include nausea, dizziness, headache, fatigue, and diarrhea. It is generally well-tolerated, and serious side effects are rare. Patients should be monitored for potential drug interactions, especially with other medications that are metabolized by CYP3A4.

Drug Interactions

Doravirine can interact with other drugs that induce or inhibit CYP3A4. Caution should be exercised when co-administering doravirine with drugs such as rifampin, carbamazepine, and St. John's Wort, as these can decrease the effectiveness of doravirine by increasing its metabolism.

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