Darunavir / cobicistat

Ticagrelor

Contraindicated.

No pharmaceutical opinion available for this interaction.

Mechanism

Darunavir / cobicistat can inhibit the CYP 3A4 and P-gp and increase the plasma concentration of Ticagrelor.

Darunavir / cobicistat can inhibit the metabolism (CYP 3A4) and decrease the active metabolite formation of Ticagrelor.

Darunavir / cobicistat

Pharmacodynamic effects

Recommendations

Alternative solution(s)

Ticagrelor

Pharmacodynamic effects

Possible increase of adverse effects.

Possible decrease of clinical efficacy.

Recommendations

Contraindicated. Use alternative.

Alternative solution(s)

Prasugrel (Efficient)

Monitor

Adverse effects of ticagrelor: Bleeding (epistaxis, gastrointestinal/cutaneous hemorrhage), bruising, dyspnea, headache, dizziness, gastrointestinal effects (nausea, vomiting, dyspepsia, diarrhea or constipation), bradycardia.

Tests

Pharmacokinetic parameters

Comment

Ref #3164 : An in vitro study with healthy volunteers showed that ketoconazole, a potent inhibitor of CYP3A4, increased ticagrelor AUC by more than 7.3-fold and Cmax by 2.4-fold and decreased the active metabolite AUC and Cmax by 56% and 89%, respectively.

Reference
  • 2647
    Ticagrelor (Brilinta), AstraZeneca, Ontario, Canada, 14 novembre 2023.
  • 2971
    Egan G, Hughes CA, Ackman ML. Drug interactions between antiplatelet or novel anticoagulant medications and antiretroviral medications. Ann Pharmacother. 2014 Jun; 48 (6): 734-40.
  • 2992
    Zhou D, Anderson TB, Grimm SW. In vitro evaluation of potential drug-drug interactions with ticagrelor: cytochrome P450 reaction phenotyping, inhibition, induction and differential kinetics. Drug Metabolism and Disposition 2011 39: 703-710.
  • 3164
    Teng R, Butler K. Effect of the CYP3A inhibitors, diltiazem and ketoconazole, on ticagrelor pharmacokinetics in healthy volunteers. Journal of Drug Assessment 2013; 2: 30-9.
  • 3071
    Darunavir/cobicistat (Prezcobix), Janssen, Ontario, Canada, 7 avril 2017.
  • 3437
    Darunavir/cobicistat/emtricitabine/tenofovir alafenamide (Symtuza), Janssen Inc, Ontario, Canada, 3 octobre 2018.