Fluconazole Injection Solution and Mayzent Starter Pack
Determining the interaction of Fluconazole Injection Solution and Mayzent Starter Pack and the possibility of their joint administration.
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.GENERALLY AVOID: Coadministration with drugs that cause moderate inhibition of CYP450 2C9 and moderate or strong inhibition of CYP450 3A4 may increase the plasma concentrations of siponimod, which is primarily metabolized by these isoenzymes. This interaction includes concomitant use of siponimod with a moderate CYP450 2C9/3A4 dual inhibitor or a moderate CYP450 2C9 inhibitor in combination with a separate moderate or strong CYP450 3A4 inhibitor. In healthy CYP450 2C9*1/*1 genotype volunteers, coadministration of a moderate CYP450 2C9/3A4 dual inhibitor (fluconazole 200 mg daily at steady-state) and siponimod (a single 4 mg dose) resulted in 2-fold and 50% increases in siponimod AUC and terminal half-life, respectively. According to in silico (computer-based) evaluation, use of fluconazole resulted in a 2- to 4-fold increase in the steady-state AUC of siponimod across different CYP450 2C9 genotypes. The CYP450 2C9 genotype influences the fractional contributions of CYP450 2C9 and 3A4 to overall elimination. If the metabolic activity of CYP450 2C9 is decreased, a larger contribution of CYP450 3A4 can be anticipated. MANAGEMENT: Concomitant use of siponimod and drugs that cause moderate inhibition of CYP450 2C9 and moderate or strong inhibition of CYP450 3A4 is not recommended. Caution is advised if siponimod is used in combination with moderate CYP450 2C9 inhibitors. References "Product Information. Mayzent (siponimod)." Novartis Pharmaceuticals, East Hanover, NJ.
Professional:GENERALLY AVOID: Coadministration with drugs that cause moderate inhibition of CYP450 2C9 and moderate or strong inhibition of CYP450 3A4 may increase the plasma concentrations of siponimod, which is primarily metabolized by these isoenzymes. This interaction includes concomitant use of siponimod with a moderate CYP450 2C9/3A4 dual inhibitor or a moderate CYP450 2C9 inhibitor in combination with a separate moderate or strong CYP450 3A4 inhibitor. In healthy CYP450 2C9*1/*1 genotype volunteers, coadministration of a moderate CYP450 2C9/3A4 dual inhibitor (fluconazole 200 mg daily at steady-state) and siponimod (a single 4 mg dose) resulted in 2-fold and 50% increases in siponimod AUC and terminal half-life, respectively. According to in silico (computer-based) evaluation, use of fluconazole resulted in a 2- to 4-fold increase in the steady-state AUC of siponimod across different CYP450 2C9 genotypes. The CYP450 2C9 genotype influences the fractional contributions of CYP450 2C9 and 3A4 to overall elimination. If the metabolic activity of CYP450 2C9 is decreased, a larger contribution of CYP450 3A4 can be anticipated.
MANAGEMENT: Concomitant use of siponimod and drugs that cause moderate inhibition of CYP450 2C9 and moderate or strong inhibition of CYP450 3A4 is not recommended. Caution is advised if siponimod is used in combination with moderate CYP450 2C9 inhibitors.
- "Product Information. Mayzent (siponimod)." Novartis Pharmaceuticals, East Hanover, NJ.
Generic Name: fluconazole
Brand name: Diflucan
Synonyms: Fluconazole
Generic Name: siponimod
Brand name: Mayzent, Mayzent Starter Pack
Synonyms: Mayzent
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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