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Chemical structure of sildenafil (Viagra), the prototypical PDE5 inhibitor. A phosphodiesterase type 5 inhibitor (PDE5 inhibitor) is a vasodilating drug that works by blocking the degradative action of cGMP-specific phosphodiesterase type 5 (PDE5) on cyclic GMP in the smooth muscle cells lining the blood vessels supplying various tissues.
Phosphodiesterase-5. A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase (PDE), thereby preventing the inactivation of the intracellular second messengers, cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) by the respective PDE subtype(s).
The US FDA approved sildenafil, a selective inhibitor of cGMP specific phosphodiesterase type 5 (PDE5), for the treatment of PAH in 2005. It is marketed for PAH as Revatio. In 2009, they also approved tadalafil, another PDE5 inhibitor, marketed under the name Adcirca. [83]
In clinical trials, one to three percent of men who used Cialis reported leg pain and, on occasion, pain in their other limbs. This side effect was most common in guys who took 10 to 20 milligrams ...
Inhibitors of PDE can prolong or enhance the effects of physiological processes mediated by cAMP or cGMP by inhibition of their degradation by PDE. [13] Sildenafil (Viagra) is an inhibitor of cGMP-specific phosphodiesterase type 5, which enhances the vasodilatory effects of cGMP in the corpus cavernosum and is used to treat erectile dysfunction.
In general, it is recommended that a combination of psychological and physiological treatments should be used to treat the disorder. [12] Other drugs which may be helpful in the treatment of this condition include dopamine agonists, oxytocin, phosphodiesterase type 5 inhibitors, and alpha-2 receptor blockers like yohimbine. [13]
These drugs came out of research programs focusing on finding PDE5 inhibitors for the treatment of cardiovascular diseases and erectile dysfunction. The two PDE5 inhibitors soon became treatments for these conditions. [22] [23] Tadalafil is the most versatile inhibitor and has the longest half-life, 17.5 hours.
5-ARIs are clinically used in the treatment of conditions that are exacerbated by DHT: [3] Mild-to-moderate benign prostatic hyperplasia and lower urinary tract symptoms; Pattern hair loss in both men and women; 5-ARIs can be used in the treatment of hirsutism in women. [1] The usefulness of 5-ARIs for the potential treatment of acne is uncertain.