What drugs interact with dolutegravir?
What Other Drugs Interact with Dolutegravir?
- aluminum hydroxide/magnesium carbonate.
- carbamazepine.
- efavirenz.
- etravirine.
- fosamprenavir.
- fosphenytoin.
- magnesium citrate.
- magnesium gluconate.
How is dolutegravir metabolized?
In vitro, dolutegravir is primarily metabolized by UDP-glucuronosyltransferase (UGT) 1A1 and cytochrome P450 (CYP) 3A4 and at clinically relevant concentrations is not an inhibitor of CYP or UGT enzymes (12).
Does dolutegravir interaction with rifampicin?
Dolutegravir is a substrate of UGT1A1 and CYP3A4, both of which are induced by rifampicin. 1 Coadministration with rifampicin results in decreases in dolutegravir plasma exposure, requiring doubling of the daily dose of dolutegravir.
How does dolutegravir interact with metformin?
Conclusions: Dolutegravir significantly increased metformin plasma exposure, which can be partially explained by OCT2 inhibition. It is recommended that dose adjustments of metformin be considered to maintain optimal glycemic control when patients are starting/stopping dolutegravir while taking metformin.
What class of drug is dolutegravir?
Dolutegravir is in a class of medications called HIV integrase inhibitors. It works by decreasing the amount of HIV in your blood and increasing the number of immune cells that help fight infections in your body.
How is Lamivudine metabolized?
Intracellularly it is metabolized to its active triphosphate form by multiple kinases. The triphosphate form competes with deoxycytidine triphosphate for binding to reverse transcriptase, and the incorporation of this 3TC-triphosphate (3TC-TP) form in viral DNA results in chain termination.
What is the mechanism of action of dolutegravir?
The proposed mechanism of action of HIV-1 integrase inhibitors, including dolutegravir, is their ability to chelate enzyme bound cations, thus preventing viral DNA integration into the host genome.
Does Dolutegravir cause hyperglycemia?
In conclusion, hyperglycemia is a potential and noticed side effect of the DTG-based ART regimen. Baseline and periodic monitoring of plasma glucose might be required in ART regimens containing dolutegravir.
Who should not receive dolutegravir?
It is not recommended to take dolutegravir at the time of becoming pregnant or during the first 12 weeks of pregnancy. Dolutegravir is not recommended for women who might become pregnant and should be used with effective contraception.
Does dolutegravir have side effects?
Dolutegravir can cause serious, life-threatening side effects. These include severe skin rash and allergic reactions, liver problems, and drug interactions. Contact your health care provider right away if you develop a rash while taking dolutegravir.
How is dolutegravir metabolized in the body?
Dolutegravir is metabolized by UGT1A1 and, to a lesser extent, by CYP3A4, without being an inducer or inhibitor of the usual metabolic systems. It has a very low potential for drug interactions and can be administered in routine doses with most drugs.
How effective is dolutegravir with two nucleotide reverse-transcriptase inhibitors?
The consistent efficacy coupled with excellent tolerability and infrequent drug–drug interactions makes the co-formulation of dolutegravir with two nucleotide reverse-transcriptase inhibitors an attractive treatment option. This review summarizes the pharmacokinetics, adverse event profile, and efficacy of dolutegravir in the treatment of HIV.
Does dolutegravir interact with other medications?
More than 20 drugs (Table 3) have been assessed for potential drug interactions with dolutegravir. These include ARVs likely to be used in combination therapy, such as NRTIs, non-nucleoside reverse transcriptase inhibitors (NNRTIs), and PIs.
Does demographic diversity affect dolutegravir pharmacokinetic parameters?
Although dolutegravir’s pathways of metabolism and transport may indicate that dolutegravir is relatively unaffected by population diversity, there are currently no studies conducted that have specifically assessed the effects of demographic diversity on dolutegravir pharmacokinetic parameters.