Interação entre Efavirenz e Quinina

QT Prolonging Drugs There is limited information available on the potential for a pharmacodynamic interaction between efavirenz and drugs that prolong the QTc interval.

Antimalarials: Artemether/lumefantrine Atovaquone/ proguanil ↓ artemether * ↓ dihydroartemisinin * ↓ lumefantrine * ↓ atovaquone ↓ proguanil Consider alternatives to artemether/ lumefantrine because of the risk of QT interval prolongation.

Although a causal relationship between a specific drug and the arrhythmia was not established in this case, erythromycin is a CYP3A4 inhibitor and has been shown to increase quinine plasma levels when used concomitantly.

Antiepileptics (AEDs) (Carbamazepine, Phenobarbital, and Phenytoin) Carbamazepine, phenobarbital, and phenytoin are CYP3A4 inducers and may decrease quinine plasma concentrations if used concurrently with quinine sulfate.

Ketoconazole (CYP3A4 Inhibitor) In a crossover study, healthy subjects (N=9) who received a single oral dose of quinine hydrochloride (500 mg) concomitantly with ketoconazole (100 mg twice daily for 3 days) had a mean quinine AUC that was higher by 45% and a mean oral clearance of quinine that was 31% lower than after receiving quinine alone.

Macrolide Antibiotics (Erythromycin, Troleandomycin) (CYP3A4 Inhibitors) In a crossover study (N=10), healthy subjects who received a single oral 600 mg dose of quinine sulfate with the macrolide antibiotic, troleandomycin (500 mg every 8 hours) exhibited a 87% higher mean quinine AUC, a 45% lower mean oral clearance of quinine, and a 81% lower formation clearance…

CYP3A4 inducers or inhibitors Alteration in plasma quinine concentration.