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Sildenafil Tablets and Tacrolimus Oral, Intravenous

Determining the interaction of Sildenafil Tablets and Tacrolimus Oral, Intravenous and the possibility of their joint administration.

Check result:
Sildenafil Tablets <> Tacrolimus Oral, Intravenous
Relevance: 06.11.2022 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:

Tacrolimus may increase the blood levels and effects of sildenafil. You may need a dose adjustment or more frequent monitoring by your doctor to safely use both medications. Contact your doctor if your condition changes or you experience nausea, shortness of breath, dizziness, lightheadedness, fainting, visual disturbances, ringing in the ears, vision or hearing loss, chest pain or tightness, irregular heartbeat, and/or priapism (prolonged and painful erection unrelated to sexual activity), as these may be signs and symptoms of excessive sildenafil levels. 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:

ADJUST DOSE: Coadministration with tacrolimus may increase the plasma concentrations of sildenafil and its active metabolite due to competitive inhibition of CYP450 3A4 metabolism by tacrolimus. In a study of ten male kidney transplant patients receiving immunosuppressive therapy containing tacrolimus, administration of a 50 mg dose of sildenafil produced peak plasma drug concentrations (Cmax) and area under the concentration-time curve (AUC) that were 44% and 90% greater, respectively, compared to historical data for healthy volunteers provided by the manufacturer. The elimination half-life was also prolonged (4.7 hours vs. 3 hours). The AUC of the active metabolite was 2.8-fold greater than in historical controls, and elimination half-life was 8.6 hours (vs. 3.5 hours). Pronounced decreases in blood pressure were also observed, which were much more intense and longer lasting than those reported in historical controls following ingestion of a 100 mg sildenafil dose. Sildenafil appears to have no significant effect on the pharmacokinetics of tacrolimus.

MANAGEMENT: A starting dose of 25 mg sildenafil may be appropriate during concomitant therapy with tacrolimus. Patients should be advised to promptly notify their physician if they experience severe adverse effects of sildenafil such as pain or tightness in the chest or jaw, irregular heartbeat, nausea, shortness of breath, visual disturbances, syncope, or prolonged erection (greater than 4 hours).

References
  • Christ B, Brockmeier D, Hauck EW, Friemann S "Interactions of sildenafil and tacrolimus in men with erectile dysfunction after kidney transplantation." Urology 58 (2001): 589-93
Sildenafil Tablets

Generic Name: sildenafil

Brand name: Revatio, Viagra

Synonyms: Sildenafil

Tacrolimus Oral, Intravenous

Generic Name: tacrolimus

Brand name: Astagraf XL, Envarsus XR, Prograf, Hecoria

Synonyms: Tacrolimus (oral and injection), Tacrolimus (Systemic)

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.