Cobicistat

Repaglinide

Dosage adjustment may be necessary.

No pharmaceutical opinion available for this interaction.

Mechanism

Cobicistat may inhibit CYP 3A4 and OATP1B1 and increase the plasma concentration of Repaglinide.

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.

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