Oral Phosphodiesterase Type 5 Inhibitors: Nonerectogenic Beneficial Uses

Abstract

Introduction Phosphodiesterase type 5 (PDE5) hydrolyses cyclic guanylate monophosphate (cGMP) specifically to 5′ GMP. PDE5 inhibitors were a breakthrough medication that addressed a previously unfulfilled medical need. They promoted vascular relaxation in the corpora cavernosa and penile erection during sexual stimulation. Sildenafil, vardenafil, and tadalafil were approved then introduced as effective treatments for male erectile dysfunction. This impact has stimulated academic, clinical, and industrial research. Aim To highlight the nonerectogenic beneficial uses of oral PDE5 inhibitors. Method A systematic review of published studies in this affair based on a Pubmed and medical subject heading databases search of all concerned articles. Main Outcome Measures Demonstrated beneficial as well as applicable uses of oral PDE5 inhibitors. Results As chemical molecules, these drugs were shown to exert potential nonerectogenic beneficial effects. They showed efficacy as a useful adjunct in the management of pulmonary hypertension. Additional uses were extended to different utilities: essential hypertension, benign prostatic hyperplasia, gastrointestinal disorders, endothelial dysfunction, female sexual dysfunction, genital blood flow, exercise capacity, Raynaud's phenomenon, sperm motility, etc. Conclusion Exploring PDE5 inhibitors for their possible medical applications in diverse specialties seems to be beneficial in making use of these molecules for the welfare of humanity.

Substrates, Inducers, Inhibitors and Structure-Activity Relationships of Human Cytochrome P450 2C9 and Implications in Drug Development

“…(109)) are cGMP-specific PDE5 (EC3.1.4.17) inhibitors currently used for the treatment of male erectile dysfunction [900][901][902][903][904]. PDE5 is responsible for degradation of cGMP in the corpus cavernosum in the penis.…”

Long‐lasting neuroprotective effect of sildenafil against 3,4‐methylenedioxymethamphetamine‐ induced 5‐hydroxytryptamine deficits in the rat brain

“…Apart from the efficacy of PDE5 inhibitors in the treatment of erectile dysfunction or pulmonary arterial hypertension (Mostafa, 2008), experimental data show that sildenafil enhances angiogenesis and neurogenesis and improves functional outcome during stroke recovery (Ding et al, 2008), improves learning and memory in the Tg2576 model of Alzheimer's disease and in a senescence accelerated mouse model (Cuadrado-Tejedor et al, 2011;Orejana et al, 2011), and prevents the neurotoxic effects of 3-nitropropionic acid (Puerta et al, 2010a). Moreover, we have recently shown that sildenafil given shortly before MDMA affords complete protection against MDMA-induced 5-HT depletions by opening mitochondrial ATP-sensitive K 1 channels, a key mechanism involved acute preconditioning paradigms (Puerta et al, 2009b).…”

Female sexual dysfunction among menopausal women

“…(2) Psychological counseling, education, and lending a patient ear are the cornerstones of FSD evaluation [52]. (3) Counseling the male partner and treating him if there are any complain of erectile dysfunction [53,54].…”