dolutegravir

30 August 2024. Related: ARVs, Integrase inhibitors.

Dolutegravir 50 mg is a 9 mm diameter round yellow tablet.

dol-you-TEG-rah-veer

Dolutegravir was approved in Europe in January 2014 and in the US in August 2013.

Dolutegravir (tradename Tivicay) is an integrase inhibitor.
The standard dose is 50 mg once-daily for people who are using HIV treatment for the first time and/or who do not have integrase resistance.
Dolutegravir is best taken after you have woken up (rather than before you sleeo). This is because it can stop you sleeping if you take it before you sleep. For most people this will be in the morning or during the day. If you are on shift work and work at night you would take it before you go to work.
50 mg twice-daily dose is needed in people using dolutegravir in combination with efavirenz, nevirapine, tipranavir/ritonavir, or rifampicin.
50 mg twice-daily is recommended for people who have drug resistance, or suspected drug resistance, to other integrase inhibitors.
For most people, dolutegravir can be taken with or without food. However, taking with a meal is recommended for people with integrase drug resistance as food increases drug levels. This increase is greatest with a high fat meal. (Food study link)
Drug interactions: There is a caution for interactions with some supplements (containing calcium, magnesium or aluminium), antacids and multivitamins. This also includes antacids that include magnesium or aluminium.
This requires separating the dolutegravir dose. These products need to be taken a minimum of two hours after dolutegravir or six hours before. Another important interaction is that dolutegravir doubles levels of metformin, and requires careful monitoring.
This is only for supplements – it is NOT a concern for foods like milk and cheese that contain calcium.
Drug interactions. Please tell your doctor or pharmacist about any other drugs or supplements before taking them with dolutegravir. Drug interactions can also be checked using the online checker at Liverpool University HIV Interaction website:
https://www.hiv-druginteractions.org/checker
A three-in-one formulation of dolutegravir plus abacavir plus 3TC in a single pill called Triumeq was approved in the US and the EU in 2014.
Dolutegravir seems to have fewer side efffects than most other HIV drugs. However, since approval there have been more reports of CNS side effects (similar to efavirenz). These include anxiety, mood changes and difficulty sleeping in less than 1 in 20 (5%) people. If you still get these side effects and you are taking meds in the morning, then it might be better to change to a different drug.
Since approval, several studies have reported that integrase inhibitors, including dolutegravir, are linked with unexplained weight gain. This has been reported more for women compared to men. Also for Africans and African-Americans compared to caucasians. Weight gain was also higher when dolutegravir was used with TAF.
Dolutegravir may work for some people who have already developed low level (early) resistance to other integrase inhibitors like raltegravir or elvitegravir. Dolutegravir is much less likely to work if you have more extensive integrase inhibitor resistance. In one study (VIKING-3), having mutation 148 plus more than two other mutations from the group of G140A/C/S, L74I and E138A/K/T only saw 11% of people getting an undetectable viral load after six months.
As with other ARVs, dolutegravir needs to be used in combination with other drugs that are active in order to avoid developing drug resistance.

Further information

The European patient leaflet and detailed Product Information for dolutegravir is online at this link (as Tivicay) at the European Medicines Agency (EMA) website.

The Patient Information is a simplified summary: what the drug is, why it is used, results from studies and cautions including side effects.

The Product Information is a detailed technical summary that you can access as a PDF file by clicking the ‘Product Information’ tab. It describes more precisely how the drug works and how it is processed by your body. This includes, for example, reported food interaction studies in terms of calories or fat content. It includes more details of the study results and a full list of side effects and drug interactions.