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Kaletra and Selexipag

Determining the interaction of Kaletra and Selexipag and the possibility of their joint administration.

Check result:
Kaletra <> Selexipag
Relevance: 06.08.2022 Reviewer: Shkutko P.M., M.D., in

In the database of official manuals used in the service creation an interaction registered by statistical results of studies was found, which can either lead to negative consequences for the patient health or strengthen a mutual positive effect. A doctor should be consulted to address the issue of joint drug administration.

Consumer:

Consumer information for this minor interaction is not currently available. Some minor drug interactions may not be clinically relevant in all patients. Minor drug interactions do not usually cause harm or require a change in therapy. However, your healthcare provider can determine if adjustments to your medications are needed.

Professional:

Coadministration with lopinavir-ritonavir may increase the plasma concentrations of selexipag and its active metabolite. The mechanism of interaction may involve inhibition by lopinavir-ritonavir of the hepatic uptake transporters OATP 1B1 and 1B3, efflux transporter P-glycoprotein (P-gp), and the hepatic microsomal enzyme CYP450 3A4, all of which contribute to the pharmacokinetic disposition of selexipag. In 20 healthy volunteers, administration of a single 400 mcg dose of selexipag following multiple twice-daily dosing of lopinavir-ritonavir 400 mg-100 mg increased selexipag peak plasma concentration (Cmax) and systemic exposure (AUC) by 2.1- and 2.2-fold, respectively, compared to administration of selexipag alone. With respect to the metabolite, which is the clinically more relevant component of selexipag because it is approximately 37 times more potent, AUC was increased by just 8%. These changes are not considered clinically relevant, and no dosage adjustment of selexipag is recommended when coadministered with lopinavir-ritonavir.

References
  • "Product Information. Uptravi (selexipag)." Actelion Pharmaceuticals US Inc, South San Francisco, CA.
  • Kaufmann P, Niglis S, Bruderer S, et al. "Effect of lopinavir/ritonavir on the pharmacokinetics of selexipag an oral prostacyclin receptor agonist and its active metabolite in healthy subjects." Br J Clin Pharmacol (2015):
Kaletra

Generic Name: lopinavir / ritonavir

Brand name: Kaletra

Synonyms: n.a.

Selexipag

Generic Name: selexipag

Brand name: Uptravi, Uptravi Titration Pack

Synonyms: n.a.

In the course of checking the drug compatibility and interactions, data from the following reference sources was used: Drugs.com, Rxlist.com, Webmd.com, Medscape.com.

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