INSTGRA (DOLUTEGRAVIR) – inhibits HIV integrase by binding to the active site of integrase and blocking the strand transfer step during the integration of retroviral deoxyribonucleic acid (DNA), which is necessary for the HIV replication cycle. Dolutegravir is slowly separated from the active site of the wild-type DNA integrase complex.
Dolutegravir is rapidly absorbed after oral administration, with a median TCmax achieved 2-3 hours after taking a dose in the form of film-coated tablets. The linearity of the pharmacokinetics of dolutegravir depends on the dose and dosage form.
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