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Riociguat and Zykadia

Determining the interaction of Riociguat and Zykadia and the possibility of their joint administration.

Check result:
Riociguat <> Zykadia
Relevance: 05.08.2023 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 interaction is not currently available.MONITOR: Coadministration with potent inhibitors of CYP450 3A4 or moderate to potent inhibitors of P-glycoprotein (P-gp) or breast cancer resistant protein (BCRP) may increase the plasma concentrations of riociguat, which is partially metabolized by CYP450 3A and also a substrate of the P-gp and BCRP efflux transporters. Increased levels of riociguat may increase the risk for hypotension. When riociguat was administered with ketoconazole, a potent CYP450 3A4 inhibitor that also inhibits P-gp and BCRP, riociguat peak plasma concentration (Cmax) and systemic exposure (AUC) increased by approximately 1.5- and 2.5-fold, respectively. The Cmax and AUC of the active metabolite, M1, which has 1/3 to 1/10 the pharmacologic activity of riociguat, were reduced by approximately 50% and 25%, respectively. Administration with the potent CYP450 3A4 inhibitor clarithromycin increased the AUC of riociguat by about 30%. The Cmax and AUC of M1 were not significantly altered (i.e.,

Professional:

MONITOR: Coadministration with potent inhibitors of CYP450 3A4 or moderate to potent inhibitors of P-glycoprotein (P-gp) or breast cancer resistant protein (BCRP) may increase the plasma concentrations of riociguat, which is partially metabolized by CYP450 3A and also a substrate of the P-gp and BCRP efflux transporters. Increased levels of riociguat may increase the risk for hypotension. When riociguat was administered with ketoconazole, a potent CYP450 3A4 inhibitor that also inhibits P-gp and BCRP, riociguat peak plasma concentration (Cmax) and systemic exposure (AUC) increased by approximately 1.5- and 2.5-fold, respectively. The Cmax and AUC of the active metabolite, M1, which has 1/3 to 1/10 the pharmacologic activity of riociguat, were reduced by approximately 50% and 25%, respectively. Administration with the potent CYP450 3A4 inhibitor clarithromycin increased the AUC of riociguat by about 30%. The Cmax and AUC of M1 were not significantly altered (i.e.,

References
  • "Product Information. Adempas (riociguat)." Bayer Pharmaceutical Inc, West Haven, CT.
  • Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0
  • Cerner Multum, Inc. "Australian Product Information." O 0
Riociguat

Generic Name: riociguat

Brand name: Adempas

Synonyms: n.a.

Zykadia

Generic Name: ceritinib

Brand name: Zykadia

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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