Tadalafil

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Substrate of
  • Inhibits
  • Induces
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Cialis, Tadalafil; Belgium: Cialis; Bulgaria: Cialis; Cyprus: Cialis; Czech Republic: Cialis, Tadalafil; Denmark: Cialis; Estonia: Cialis, Tadalafil; Finland: Cialis; France: Cialis; Germany: Cialis, Tadalafil; Greece: Cialis; Hungary: Cialis; Ireland: Cialis, Tadalafil; Italy: Cialis; Latvia: Cialis, Tadalafil; Lithuania: Adcirca, Cialis; Luxembourg: Cialis; Malta: Cialis; Netherlands: Cialis, Tadalafil; Poland: Cialis, Tadalafil; Portugal: Adcirca, Cialis; Romania: Adcirca, Cialis; Slovakia: Cialis, Tadalafil; Slovenia: Cialis; Spain: Cialis; Sweden: Adcirca, Cialis; UK: Cialis.

North America

Canada: Cialis; USA: Adcirca, Cialis.

Latin America

Argentina: Cialis; Brazil: Cialis; Mexico: Cialis.

Asia

Japan: Cialis.

Drug combinations

Chemistry

Tadalafil: C~22~H~19~N~3~O~4~. Mw: 389.40. (1) Pyrazino[1′,2′:1,6]pyrido[3,4-b]indole-1,4-dione, 6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methyl-, (6R-12aR)-; (2)(6R,12aR)-2,3,6,7,12,12a-Hexahydro-2-methyl-6-[3,4-(methylenedioxy)phenyl] pyrazino[1′,2′:1,6]pyrido[3,4-b]indole-1,4-dione; (3)(6R-trans)-6-(1,3-Benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methyl-pyrazino[1′,2′:1,6]pyrido[3,4-b]indole-1,4-dione. CAS-171596-29-5 (2001).

Pharmacologic Category

Vasodilating Agents; Phosphodiesterase Inhibitors; Phosphodiesterase-5 Enzyme Inhibitor. (ATC-Code: G04BE08).

Mechanism of action

Does not directly cause penile erections, but affects response to sexual stimulation. Physiologic mechanism of erection of penis involves release of nitric oxide (NO) in corpus cavernosum during sexual stimulation. When sexual stimulation causes local release of NO, inhibition of PDE-5 by tadalafil causes increased levels of cGMP in corpus cavernosum, resulting in smooth muscle relaxation and inflow of blood to corpus cavernosum.

Therapeutic use

Treatment of erectile dysfunction.

Pregnancy and lactiation implications

Not indicated for use in women. Teratogenic events not reported in animal reproduction studies. Excretion in breast milk unknown.

Unlabeled use

Contraindications

Concurrent use of organic nitrates in any form (e.g. nitroglycerin, isosorbide dinitrate).

Warnings and precautions

May cause dose-related impairment of color discrimination. Use caution in retinitis pigmentosa. Sudden decrease or loss of hearing reported rarely. Hearing changes may be accompanied by tinnitus and dizziness. Decreases in blood pressure may occur due to vasodilator effects. Use with caution in left ventricular outflow obstruction (aortic stenosis or hypertrophic obstructive cardiomyopathy). May be more sensitive to hypotensive actions. Concurrent use with α-adrenergic antagonist therapy or substantial alcohol consumption may cause symptomatic hypotension. Painful erection >6 hours in duration, rare. Vision loss may occur rarely and be a sign of nonarteritic anterior ischemic optic neuropathy. Use not recommended in degenerative retinal disorders (e.g. retinitis pigmentosa). Use with caution in anatomical deformation of the penis (angulation, cavernosal fibrosis, or Peyronie’s disease), in bleeding disorders, and in hypotension (<90/50 mm Hg), uncontrolled hypertension (>170/100 mm Hg), heart failure within last 6 months, uncontrolled arrhythmias, stroke within last 6 months, MI within last 3 months. Use caution in left ventricular outflow obstruction (e.g. aortic stenosis). There is a degree of cardiac risk associated with sexual activity. Use with caution in patients who have conditions which may predispose them to priapism (sickle cell anemia, multiple myeloma, leukemia). Use with caution in hepatic and renal impairment, in active peptic ulcer disease, and in patients taking α-blockers (may cause hypotension), or strong CYP3A4 inhibitors. Concomitant use (regularly/intermittently) with all forms of nitrates contraindicated. Other treatments for erectile dysfunction use not recommended.

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