Naldemedine and Sustiva

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 information for this interaction is not currently available.MONITOR: Coadministration with moderate inducers of CYP450 3A4 may decrease the plasma concentrations of naldemedine, which is primarily metabolized by CYP450 3A4 to nor-naldemedine and to a minor extent by UGT1A3 to naldemedine 3-G. Both metabolites have demonstrated antagonistic activity for opioid receptors, but with less potency than the parent drug. According to the product labeling, administration of naldemedine with 600 mg once daily rifampin, a potent CYP450 3A4 inducer, decreased naldemedine peak plasma concentration (Cmax) by 38% and systemic exposure (AUC) by 83% compared to naldemedine administered alone. Induction of P-glycoprotein efflux transporter by rifampin may have also contributed to the interaction. Physiologically-based pharmacokinetic modeling suggested that concomitant use of efavirenz decreased exposure to naldemedine by 43%; however, the clinical significance is unknown. MANAGEMENT: Caution and monitoring for potential loss of efficacy is recommended with the concomitant use of naldemedine with moderate CYP450 3A4 inducers. References Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0 "Product Information. Symproic (naldemedine)." Shionogi USA Inc, Florham Park, NJ.

MONITOR: Coadministration with moderate inducers of CYP450 3A4 may decrease the plasma concentrations of naldemedine, which is primarily metabolized by CYP450 3A4 to nor-naldemedine and to a minor extent by UGT1A3 to naldemedine 3-G. Both metabolites have demonstrated antagonistic activity for opioid receptors, but with less potency than the parent drug. According to the product labeling, administration of naldemedine with 600 mg once daily rifampin, a potent CYP450 3A4 inducer, decreased naldemedine peak plasma concentration (Cmax) by 38% and systemic exposure (AUC) by 83% compared to naldemedine administered alone. Induction of P-glycoprotein efflux transporter by rifampin may have also contributed to the interaction. Physiologically-based pharmacokinetic modeling suggested that concomitant use of efavirenz decreased exposure to naldemedine by 43%; however, the clinical significance is unknown.

MANAGEMENT: Caution and monitoring for potential loss of efficacy is recommended with the concomitant use of naldemedine with moderate CYP450 3A4 inducers.

Naldemedine

Generic Name: naldemedine

Brand name: Symproic

Synonyms: n.a.

What is Naldemedine?

Sustiva

Generic Name: efavirenz

Brand name: Sustiva

Synonyms: n.a.

What is Sustiva?