Dolutegravir

Definition

Dolutegravir is an antiretroviral medication used in the treatment of human immunodeficiency virus (HIV) infection. It belongs to a class of drugs called integrase strand transfer inhibitors (INSTIs) that work by preventing the HIV virus from integrating its genetic material into the host cell's DNA, thereby interrupting the viral replication process.

5 Must Know Facts For Your Next Test

1. Dolutegravir is approved for the treatment of both treatment-naïve and treatment-experienced HIV-1 infected adults and children.
2. It has a high genetic barrier to resistance, meaning it is less likely for the virus to develop resistance when used as part of a combination antiretroviral regimen.
3. Dolutegravir can be used in both first-line and second-line antiretroviral therapy, and has been shown to be effective in suppressing HIV viral load.
4. The drug is generally well-tolerated, with common side effects including headache, insomnia, and gastrointestinal issues.
5. Dolutegravir is often co-formulated with other antiretroviral medications to create a single-tablet regimen, improving adherence and convenience for patients.

Review Questions

• Explain how dolutegravir, as an integrase inhibitor, interrupts the HIV replication cycle.
  • Dolutegravir is an integrase strand transfer inhibitor that targets the HIV integrase enzyme, a crucial component of the viral replication cycle. The integrase enzyme is responsible for inserting the viral genetic material into the host cell's DNA, allowing the virus to replicate and produce new infectious particles. By inhibiting the integrase enzyme, dolutegravir prevents the integration of the viral DNA, effectively halting the replication process and limiting the spread of the virus within the infected individual.
• Describe the advantages of dolutegravir in the treatment of HIV compared to other antiretroviral drugs.
  • Dolutegravir offers several advantages in the treatment of HIV. Firstly, it has a high genetic barrier to resistance, meaning that the virus is less likely to develop resistance mutations when dolutegravir is used as part of a combination antiretroviral regimen. This improves the long-term effectiveness of the drug. Additionally, dolutegravir has been shown to be effective in both treatment-naïve and treatment-experienced patients, making it a versatile option for various stages of HIV infection. The drug is also often co-formulated with other antiretrovirals, enhancing adherence and convenience for patients by reducing the pill burden.
• Analyze the role of dolutegravir in the overall management of HIV/AIDS, considering its place in the current antiretroviral therapy landscape.
  • Dolutegravir plays a crucial role in the management of HIV/AIDS within the current antiretroviral therapy landscape. As an integrase inhibitor, it provides a unique mechanism of action that complements other classes of antiretroviral drugs, allowing for the construction of highly effective combination regimens. The drug's high genetic barrier to resistance and proven efficacy in both treatment-naïve and treatment-experienced patients make it a valuable option for both first-line and second-line therapy. Furthermore, the availability of co-formulated products containing dolutegravir enhances patient adherence, a critical factor in the long-term success of antiretroviral therapy. By effectively suppressing viral replication and preventing the development of drug resistance, dolutegravir contributes to the overall goal of achieving sustained viral suppression and improving the health outcomes of individuals living with HIV/AIDS.

Related terms

Antiretroviral Therapy (ART): The use of a combination of antiretroviral medications to suppress HIV replication and prevent the progression of the disease.

Integrase Inhibitors: A class of antiretroviral drugs that target the HIV integrase enzyme, preventing the virus from integrating its genetic material into the host cell's DNA.

HIV Replication Cycle: The series of steps the HIV virus takes to replicate and infect new host cells, including entry, reverse transcription, integration, and budding.