No pharmaceutical opinion available for this interaction.
Rifampin can increase the metabolism (UGT 1A1) and decrease the plasma concentration of Dolutegravir.
UGT1A1 (51%), CYP3A (21%), UGT1A9 (6%) and UGT1A3 (3%); P-gp, BCRP (in vitro)
OCT2 and MATE 1
Possible decrease of clinical efficacy.
Tivicay : In patients who have never received integrase inhibitors, increase dolutegravir dose to 50 mg BID.
Triumeq or Dovato : Administer an additional dose of 50 mg dolutegravir 12 hours after Triumeq or Dovato.
Monitor for clinical efficacy.
Avoid combination in patients with resistance to integrase inhibitors.
Juluca : Concomitant administration contraindicated.
1A2, 2C9, 2E1, P-gp
1A2, 2C9, 2C19, 3A4-7, UGT 1A1, P-gp
Rifabutin (See rifabutine and dolutégravir)
Viral load HIV
|50 mg||50 mg||50 mg||100 mg|
|+ 33% *||- 54% **||- 57%||- 26% †|
|+ 22% *||- 72% **||- 86%||- 76% †|
|- 60% *|
|+ 18% *||- 43% **||- 35%||+ 9% †|
|600 mg||600 mg||600 mg||600 mg|
Dolutegravir 50 mg BID with rifampin compararable to dolutegravir 50 mg QD.
Ref # 2724:
* Comparison is rifampin taken with dolutegravir 50 mg BID compared with dolutegravir QD.
** Comparison is rifampin taken with dolutegravir 50 mg BID compared with dolutegravir 50 mg BID alone.
3 periods tudy with healthy subjects : Dolutegravir 50 mg QD (7 days), Dolutegravir 50 mg BID (7 days) and Dolutegravir 50 mg BID with rifampin (14 days).
One subject had a grade 2 lymphopenia and a rash.
Ref # 2868: The monograph recommends to give dolutegravir 50 mg BID for patients who have no resistance to integrase inhibitors. For patients with resistance to integrase inhibitors, it is suggested to choose an alternative to Rifampin.
Ref #3422 : In this sub-study with 12 HIV-TB co-infected patients, the treatment of dolutegravir 50 mg BID with rifampin 600 mg QD appears to show good efficacy with adequate dolutegravir Cmin. Although only two patients had concentrations of dolutegravir <640 ng/mL, it is suggested that this dose be used only in patients with wild-type HIV. Rifampin had no effect on lamivudine and tenofovir concentrations.
Ref #3424 : † When comparing PK parameters of dolutegravir 100 mg QD in co-administration with rifampin to dolutegravir 50mg QD alone.
Despite the significant decrease in dolutegravir Cmin, concentrations of dolutegravir 100 mg QD with rifampin were above the protein bindingadjusted IC of 64 ng/mL. Further study of this dose are needed.