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Bosentan Tablets for Oral Suspension and Sildenafil Citrate

Determining the interaction of Bosentan Tablets for Oral Suspension and Sildenafil Citrate and the possibility of their joint administration.

Check result:
Bosentan Tablets for Oral Suspension <> Sildenafil Citrate
Relevance: 05.12.2022 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:

Using sildenafil together with bosentan can alter the blood levels and effects of both medications. Specifically, sildenafil levels may decrease, which may make the medication less effective in treating your condition. At the same time, bosentan levels may become elevated, and you may have an increased risk of side effects such as fluid retention, anemia, low blood pressure, and liver problems. Talk to your doctor or pharmacist if you have any questions or concerns. Your doctor may be able to prescribe alternatives that do not interact, or you may need a dose adjustment or more frequent monitoring by your doctor to safely use both medications. You should seek immediate medical attention if you develop fever, chills, joint pain or swelling, unusual bleeding or bruising, skin rash, itching, loss of appetite, fatigue, nausea, vomiting, dark colored urine, light colored stools, and/or yellowing of the skin or eyes, as these may be signs and symptoms of liver damage related to the use of bosentan. 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.

Professional:

MONITOR: Coadministration of bosentan and sildenafil may result in increased bosentan plasma concentrations and decreased sildenafil plasma concentrations. The mechanism is sildenafil inhibition of bosentan metabolism via CYP450 3A4 and 2C9, and bosentan induction of sildenafil metabolism via these same isoenzymes. In healthy subjects, coadministration of multiple doses of bosentan (125 mg twice a day) and sildenafil (80 mg three times a day) resulted in a 50% increase in bosentan systemic exposure (AUC) and a 63% reduction of sildenafil systemic exposure. Bosentan peak plasma concentration (Cmax) increased by 42% and sildenafil Cmax decreased by 55%. The combination did not lead to clinically significant changes in blood pressure, supine or standing.

MANAGEMENT: No dosage adjustment of either drug is necessary, whether sildenafil is used for the treatment of pulmonary arterial hypertension (PAH) or erectile dysfunction. However, adding sildenafil to bosentan therapy does not provide any beneficial effect on exercise capacity in the treatment of PAH. If prescribed together, the possibility of prolonged and/or increased pharmacologic effects of bosentan, including serious adverse effects such as hepatotoxicity, should be considered. Patients should be advised to seek medical attention if they experience signs and symptoms of hepatotoxicity such as fever, rash, anorexia, nausea, vomiting, fatigue, right upper quadrant pain, dark urine, and jaundice.

References
  • "Product Information. Revatio (sildenafil)." Pfizer U.S. Pharmaceuticals Group, New York, NY.
  • "Product Information. Tracleer (bosentan)." Acetelion Pharmaceuticals US, Inc, South San Francisco, CA.
Bosentan Tablets for Oral Suspension

Generic Name: bosentan

Brand name: Tracleer

Synonyms: Bosentan

Sildenafil Citrate

Generic Name: sildenafil

Brand name: Revatio, Viagra

Synonyms: Sildenafil

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.