Drug intelligence / Profile preview

sildenafil + fluvoxamine

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Sildenafil + fluvoxamine is a combination of two small molecule drugs, each with distinct mechanisms of action. Sildenafil is a phosphodiesterase-5 (PDE5) inhibitor primarily used for the treatment of erectile dysfunction and pulmonary arterial hypertension. It works by inhibiting the enzyme PDE5, leading to increased levels of cyclic guanosine monophosphate (cGMP), resulting in smooth muscle relaxation and vasodilation in the corpus cavernosum or pulmonary vasculature. Fluvoxamine is a selective serotonin reuptake inhibitor (SSRI) used mainly for treating obsessive-compulsive disorder and depression; it increases synaptic serotonin by inhibiting its reuptake in the central nervous system. When combined, fluvoxamine can inhibit cytochrome P450 3A4 (CYP3A4), which metabolizes sildenafil, leading to increased plasma concentrations and enhanced vascular effects of sildenafil[1][2][3]. This combination does not have an established therapeutic indication as a fixed-dose product but may be encountered when both drugs are prescribed concurrently.

02

Targets

CYP3A4 (Cytochrome P450 3A4)SERT (Sodium-dependent serotonin transporter)PDE5 (Phosphodiesterase 5A)

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