Tadalafil
PDE5 Inhibitor | Erectile Function & Blood Flow
Tadalafil is a long-acting PDE5 inhibitor FDA-approved for erectile dysfunction (ED), benign prostatic hyperplasia (BPH), and pulmonary arterial hypertension (PAH). Its extended half-life of approximately 17.5 hours provides a therapeutic window of up to 36 hours, earning it the nickname 'the weekend pill.' Unlike shorter-acting PDE5 inhibitors, tadalafil is uniquely suited for daily low-dose use (2.5-5mg), which maintains steady-state plasma levels and allows for spontaneous sexual activity without timing constraints. Originally developed by ICOS Corporation and marketed by Eli Lilly as Cialis, tadalafil received FDA approval in 2003 for ED and has since become one of the most widely prescribed medications in its class. Beyond sexual health, tadalafil has gained attention for its cardiovascular and hemodynamic benefits, including improved endothelial function, reduced blood pressure, and enhanced exercise capacity.
Moleküler Gösterim
M.W.: 389.40 Da
PubChem 2D yapı diyagramı
Referans Flakon
Referans illüstrasyonu — ürün listesi değildir
Etki Mekanizması
Tadalafil selectively inhibits phosphodiesterase type 5 (PDE5), the enzyme responsible for degrading cyclic guanosine monophosphate (cGMP) in smooth muscle tissue. During sexual stimulation, nitric oxide (NO) is released in the corpus cavernosum, activating guanylate cyclase and increasing cGMP levels. Elevated cGMP causes smooth muscle relaxation in penile arteries and the corpus cavernosum, facilitating increased blood flow and erection. By blocking PDE5, tadalafil prolongs and amplifies this cGMP-mediated vasodilatory signaling cascade. PDE5 is also expressed in pulmonary vasculature, prostatic smooth muscle, and the bladder neck, which accounts for tadalafil's therapeutic effects in PAH and BPH/LUTS. Tadalafil has high selectivity for PDE5 over PDE6 (the retinal isoform), which contributes to its lower incidence of visual disturbances compared to sildenafil.
Tadalafil is a long-acting PDE5 inhibitor FDA-approved for erectile dysfunction (ED), benign prostatic hyperplasia (BPH), and pulmonary arterial hypertension (PAH). Its extended half-life of approximately 17.5 hours provides a therapeutic window of up to 36 hours, earning it the nickname ‘the weekend pill.’ Unlike shorter-acting PDE5 inhibitors, tadalafil is uniquely suited for daily low-dose use (2.5-5mg), which maintains steady-state plasma levels and allows for spontaneous sexual activity without timing constraints. Originally developed by ICOS Corporation and marketed by Eli Lilly as Cialis, tadalafil received FDA approval in 2003 for ED and has since become one of the most widely prescribed medications in its class. Beyond sexual health, tadalafil has gained attention for its cardiovascular and hemodynamic benefits, including improved endothelial function, reduced blood pressure, and enhanced exercise capacity.
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|---|---|---|---|
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Kaynaklar
- Tadalafil for the treatment of benign prostatic hyperplasia — Giuliano F, Uckert S, Maggi M, Birder L, Kiber A, Brock GB
- Tadalafil administered once daily for lower urinary tract symptoms secondary to benign prostatic hyperplasia: a dose finding study — Roehrborn CG, McVary KT, Elion-Mboussa A, Viktrup L
- Hemodynamic effects of tadalafil in patients with heart failure: a randomized, placebo-controlled trial — Giagulli VA, Moghetti P, Kaufman JM, Guastamacchia E, Iacoviello M, Triggiani V
- Phosphodiesterase type 5 (PDE5) inhibitors in the management of erectile dysfunction: an update — Hatzimouratidis K, Hatzichristou DG
- Tadalafil once daily in the treatment of erectile dysfunction: a meta-analysis of randomized controlled trials — Porst H, Rajfer J, Engel JD, Hellstrom WJ