“Our findings further support the concept that the novel class of phosphodiesterase-5 inhibitors, or PDE-5 inhibitors, including vardenafil and sildenafil, may have a new utility in cardiac protection, in addition to their well-known use for the management of erectile dysfunction in men,” said Rakesh C. Kukreja, Ph.D., professor of medicine, physiology, biochemistry and emergency medicine at VCU.
In the study, Kukreja and his team demonstrated that pretreatment with a clinically relevant dose of vardenafil induces a protective effect against heart attack injury by opening the mitochondrial KATP channel in an animal model.
According to Kukreja, PDE-5 is an enzyme responsible for the destruction of cGMP, an intracellular messenger molecule, in heart cells. He said that the mitochondrial KATP channel and cGMP play an important role in preconditioning of the heart following a heart attack. The cGMP also has a hand in the dilation of arteries in the body. PDE-5 inhibitor drugs, such as vardenafil, sildenafil and tadalafil are able to preserve cGMP, and therefore dilation of the arteries by inhibiting PDE-5.
Vardenafil, like sildenafil, stabilizes the mitochondria and protects against damage of the heart by opening the mitochondrial KATP channels in cardiac cells.
“This study provides important information about the mechanism by which the PDE-5 inhibitors work. Furthermore, it is proof that the positive findings of prior studies on sildenafil extend to another PDE-5 inhibitor,” said George Vetrovec, M.D., chair of cardiology at VCU’s School of Medicine.
MEDICA.de; Source: Virginia Commonwealth University