Antiretroviral Agent: Dolutegravir 50 mg is an oral tablet containing an integrase strand transfer inhibitor (INSTI), a key drug class for treating HIV-1 infection.
Adult and Adolescent Dosing: The 50 mg strength is the standard once-daily dose for most adults and adolescents weighing at least 40 kg who are new to HIV treatment. A higher twice-daily dose may be used for patients with integrase inhibitor resistance.
Combination Therapy: It is not used as a monotherapy. It is always prescribed as part of a combination regimen with other antiretroviral agents to provide a complete and effective treatment plan.
Film-Coated Tablet: The tablet is film-coated and should be swallowed whole. It can be taken with or without food.
Advantages
High Barrier to Resistance: Dolutegravir has a high genetic barrier to resistance, meaning it is very difficult for the virus to develop mutations that render the drug ineffective. This makes it a highly durable and reliable treatment option.
Once-Daily Dosing: For most treatment-naïve patients, the 50 mg dose is taken once daily, which simplifies the treatment regimen and significantly improves patient adherence.
Good Safety Profile: It is generally well-tolerated, with a low incidence of serious side effects. This makes it a preferred option for a broad range of patients.
Minimal Drug Interactions: Dolutegravir has a low potential for drug interactions, making it easier to co-prescribe with other medications compared to some older antiretroviral drugs.
Uses
HIV-1 Infection: Indicated for the treatment of HIV-1 infection in adults and adolescents, in combination with other antiretroviral agents.
First-Line Therapy: It is a cornerstone of current first-line antiretroviral therapy (ART) regimens for treatment-naïve patients due to its high efficacy and favorable safety profile.
Treatment-Experienced Patients: It is also used in treatment-experienced patients, including those with integrase inhibitor resistance, often with a twice-daily dosing regimen.
Pregnancy: Dolutegravir is a recommended agent for HIV treatment during pregnancy, particularly after the first trimester, due to its effectiveness and safety profile.
Nature
Integrase Inhibitor: Dolutegravir belongs to the integrase inhibitor class of antiretrovirals.
Mechanism of Action: It works by binding to the active site of the viral enzyme integrase, which is essential for integrating the HIV DNA into the host cell’s DNA. By inhibiting this process, it prevents the virus from replicating.
Post-Entry Inhibition: Dolutegravir acts on a later stage of the viral replication cycle compared to NRTIs and NNRTIs, which target the reverse transcription stage.
Metabolism & Elimination: It is primarily metabolized by the liver enzyme UGT1A1 and, to a lesser extent, by CYP3A. It has a long half-life, allowing for once-daily dosing, and is eliminated mainly via the fecal route.
Storage
Temperature: Store Dolutegravir tablets at a controlled room temperature, typically between 20∘C to 25∘C (68∘F to 77∘F).
Protection: Keep the tablets in their original, tightly closed container, protected from light and moisture.
Administration: The tablet can be taken with or without food. However, for treatment-experienced patients with integrase inhibitor resistance, taking the dose with food may improve absorption.
Patient Compliance: Patients must be educated on the importance of taking every dose as prescribed to maintain a consistent therapeutic drug level and prevent the development of viral resistance.
