Drug Interaction Report

MONITOR: Coadministration with strong inhibitors of the uridine diphosphate glucuronosyltransferase (UGT) 1A3 and 2B7 enzymes may increase plasma concentrations of selexipag, which are involved in the glucuronidation of its active metabolite. However, data evaluating the interaction are not available.

MANAGEMENT: Caution and clinical monitoring are recommended if selexipag is used with strong UGT 1A3 and UGT 2B7 inhibitors, such as valproic acid.

GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents. Use in combination may result in additive central nervous system depression and/or impairment of judgment, thinking, and psychomotor skills.

MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol. Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Food prolongs the gastrointestinal absorption of selexipag. When taken with food, the time to peak concentration (Tmax) was delayed and peak plasma concentration (Cmax) was approximately 30% lower. Selexipag systemic exposure (AUC) and that of its active metabolite did not significantly change, however. Selexipag may be taken with or without food. Tolerability may be improved when taken with food.