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Although
Viagra, Levitra, and Cialis all work by inhibition of PDE5, tadalafil's
distinguishing pharmacologic feature is its longer half-life (17.5
hours) compared with
Viagra and Levitra (4-5 hours). This longer half-life results in a
longer duration of action and is, in part, responsible for the Cialis
nickname of
the "weekend pill." This longer half-life also is the basis of
current investigation for tadalafil's use in pulmonary arterial hypertension
as a once-daily therapy. At present, sildenafil (trade name Revatio)
is approved in various regions worldwide as a 3-times daily therapy
for pulmonary arterial
hypertension.
Penile erection during sexual stimulation is caused by increased penile blood flow resulting from the relaxation of penile arteries and corpus cavernosal smooth muscle. This response is mediated by the release of nitric oxide (NO) from nerve terminals and endothelial cells, which stimulates the synthesis of cGMP in smooth muscle cells. Cyclic GMP causes smooth muscle relaxation and increased blood flow into the corpus cavernosum. The inhibition of phosphodiesterase type 5 (PDE5) enhances erectile function by increasing the amount of cGMP. Tadalafil (as well as sildenafil and vardenafil) inhibits PDE5. Because sexual stimulation is required to initiate the local release of nitric oxide, the inhibition of PDE5 by tadalafil has no effect in the absence of sexual stimulation. A 20 mg dose of tadalafil is comparable to a 100 mg dose of sildenafil (Viagra). However, the recommended starting dose of Cialis in most patients is 10 mg, taken prior to anticipated sexual activity. The dose may be increased to 20 mg or decreased to 5 mg, based on individual efficacy and tolerability. |
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Vardenafil |
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