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Cialas and PDE Inhibition and Smooth Muscle Relaxation

Phosphodiesterase (PDE) is an enzyme that causes breakdown of cyclic GMP, which is the direct intracellular mediator in the nitric oxide (nonadrenergic, noncholinergic) pathway. Discovery of this pathway led to a Nobel Prize in 1998 for the scientists responsible. The nitric oxide system causes relaxation of smooth muscle in blood vessel walls, ie, vasodilation, in various organ systems. Cealis is outcome of this discovery to treat erectile dysfunction.

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Thus, Cealis joins Viagra and Levitra as alternative oral medications, all 3 now approved by the U.S. FDA, for ED.

In brief, efficacy is approximately 70% with all 3 drugs(Cialis, levitra and viagra). The side effect profile is similar among the 3 drugs, except that blue discoloration of vision (overlap with PDE-6 in the retina) is seen only with Viagra (<0.5%) and muscle aches only with Cialis. Otherwise, vasodilatory side effects (headaches, nasal congestion, flushing) are common with all, but are mild, and only rarely cause men to drop out of clinical trials. All 3 will carry a contra-indication in men using organic nitrates. Otherwise, the long half-life of Cialis (17.5 hours) is noteworthy, earning this drug the nickname ‘weekender,’ as a single dose taken on Friday would still be exerting an effect Sunday (or even Monday).

More than 1 million men around the world have taken Cialis, Beebe said.

Alternative PDE-5 inhibitors Cialis and Levitra will soon be in competition with Viagra, and the launch of these new drugs is certain to bring many men with ED into doctors’ offices. Aside from the long half-life of Cialis, and the excellent track record of Viagra, the differences between the 3 drugs are not great. All appear to be effective and safe, provided concomitant nitrates are avoided,. A potential for serious hypotension exists should an organic nitrate be used along with any of these three PDE-5 inhibitors.