The pleiotropic effects of phosphodiesterase 5 inhibitors on function and safety in patients with cardiovascular disease and hypertension
The Journal of Clinical Hypertension, 06/20/2012
Chrysant SG et al. – These beneficial pleiotropic and safe cardiovascular effects of phosphodiesterase 5 (PDE–5) inhibitors will be discussed in this concise review.
- Phosphodiesterase 5 (PDE–5) inhibitors are selective blockers of PDE–5, which catalyzes the hydrolysis of cyclic guanosine monophosphate (cGMP) to its corresponding monophosphates. cGMP is a potent vasodilator and nitric oxide donor.
- Since PDE–5 is widely distributed in the body, it was hypothesized that inhibition of its actions could lead to significant vasodilation, which could benefit patients with coronary artery disease.
- This hypothesis led to the development of PDE–5 inhibitors, the first being sildenafil citrate.
- Studies of sildenafil in patients with coronary artery disease demonstrated a modest cardiovascular effect but a potent action on penile erection in men, resulting in sildenafil becoming first–line treatment of erectile dysfunction.
- Two more PDE–5 inhibitors are now US Food and Drug Administration–approved (vardenafil and tadalafil) for the treatment of erectile dysfunction.
- Recent studies have demonstrated several beneficial pleiotropic cardiovascular effects of PDE–5 inhibitors in patients with erectile dysfunction and multiple comorbidities, including coronary artery disease, heart failure, hypertension, and diabetes mellitus.
- Treatment of these conditions with PDE–5 inhibitors has been very effective, safe, and well tolerated.
- Drug interactions have been minimal with the exception of nitrates, where coadministration may result in severe vasodilation and hypotension.