Darunavir Tablets and Macitentan

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.

Darunavir may increase the blood levels of macitentan. In some cases, this may increase the risk and/or severity of side effects such as headache, anemia and liver problems, especially during prolonged treatment. You may need a dose adjustment or more frequent monitoring by your doctor to safely use both medications. Call your doctor immediately if you have fever, chills, joint pain or swelling, unusual bleeding or bruising, skin rash, itching, loss of appetite, fatigue, nausea, vomiting, abdominal pain, dark colored urine, light colored stools, and/or yellowing of the skin or eyes, as these may be signs and symptoms of liver damage. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

MONITOR: Coadministration with inhibitors of CYP450 3A4 may increase the plasma concentrations of macitentan, which is primarily metabolized by the isoenzyme. In ten healthy subjects, administration of a single 10 mg oral dose of macitentan on day 5 of treatment with the potent CYP450 3A4 inhibitor ketoconazole (400 mg daily for 24 days) resulted in an approximately 2-fold increase in macitentan systemic exposure (AUC) compared to administration alone. Additionally, there was a 26% reduction in the AUC of the active metabolite, which has been reported to be approximately 5-fold less potent than macitentan in vitro, but whose systemic exposure in human is 2.5-fold higher than that of macitentan. The clinical significance of these changes has not been established. Macitentan was well tolerated with or without ketoconazole in the study, and there were no relevant differences in safety parameters between the treatments.

MANAGEMENT: Caution is advisable if macitentan is used with inhibitors of CYP450 3A4. The product labeling recommends avoiding concomitant use with potent inhibitors (e.g., protease inhibitors, clarithromycin, cobicistat, conivaptan, delavirdine, itraconazole, ketoconazole, nefazodone, posaconazole, voriconazole), but no suggestions are given regarding use with less potent inhibitors. It may be reasonable to monitor therapeutic response to macitentan more closely.

Darunavir Tablets

Generic Name: darunavir

Brand name: Prezista

Synonyms: Darunavir

What is Darunavir Tablets?

Macitentan

Generic Name: macitentan

Brand name: Opsumit

Synonyms: n.a.

What is Macitentan?