Darunavir / cobicistat

Repaglinide

Dosage adjustment may be necessary.

No pharmaceutical opinion available for this interaction.

Mechanism

Darunavir / cobicistat may inhibit CYP 3A4 and OATP1B1 and increase the plasma concentration of Repaglinide.

Darunavir / cobicistat

Pharmacodynamic effects

Recommendations

Alternative solution(s)

Repaglinide

Pharmacodynamic effects

Possible increase of adverse effects.

Recommendations

Monitor for development of adverse effects and adjust dosage if necessary.

Alternative solution(s)

Metformin, DPP-4 Inhibitors, GLP-1 Agonists

Monitor

Signs and symptoms of hypoglycemia : headache, dizziness, tiredness, rapid heartbeat, nervousness, shakiness, nausea and sweating.

Tests

Pharmacokinetic parameters

Comment

Ref #3182 : Co-administration of cyclosporine, an inhibitor of CYP3A4 and strong OATP1B1 inhibitor, caused an increase in repaglinide (0.25 mg) Cmax of 175% and the AUC was 244% of that in the placebo phase. Co-administration of 250 mg clarithromycin, a potent CYP3A4 inhibitor, and a single dose of 0.25 mg repaglinide (after 4 days of twice daily clarithromycin 250 mg resulted in a 40% and 67% increase in repaglinide AUC and Cmax, respectively. Co-administration of itraconazole, a CYP3A4 inhibitor, and a single dose of 0.25 mg repaglinide (on the third day of a regimen of 200 mg initial dose, twice-daily 100 mg itraconazole) resulted in a 40% increase in repaglinide AUC. Co-administration of 200 mg ketoconazole, a potent and competitive inhibitor of CYP3A4, and a single dose of 2 mg repaglinide in healthy subjects (after 4 days of once daily ketoconazole 200 mg) resulted in a 15% and 16% increase in repaglinide.

Comment
Reference
  • 3182
    Repaglinide (GlucoNorm), Novo Nordisk, Ontario, Canada, 9 septembre 2015.