Emerging oral drugs for erectile dysfunction.
Erectile dysfunction (ED) is a common medical condition that affects the sexual life of millions of men worldwide. Many drugs are now available for the treatment of ED, with oral pharmacotherapy representing the first-line option for most patients. Sildenafil citrate, an inhibitor of the enzyme phosphodiesterase type 5 (PDE5), is the most widely prescribed oral agent and has a very satisfactory efficacy-safety profile in all patient categories. Tadalafil (Cialis; Eli Lilly & Co., ICOS) and vardenafil (Levitra; Bayer Pharmaceuticals, GlaxoSmithKline) are new PDE5 inhibitors that have recently been approved worldwide. Both have been associated with significant positive efficacy-safety profiles. Apomorphine sublingual is a dopamine D1 and D2 receptor agonist, which has been approved for marketing in Europe. It is best selected for treating patients with mild-to-moderate ED, but it is seldom used in clinical practice due to its limited efficacy and side effects, particularly nausea. Patients who do not respond to oral pharmacotherapy or who are unable to use it are appropriate candidates for intracavernosal and intraurethral therapy. The efficacy of second-line treatment is high, but the attrition rate remains significant. For the purpose of this review, clinical and pharmacological analysis focuses on the recent advances in the field of oral therapy, including PDE5 inhibitors and sublingual apomorphine.
Briganti
Alberto
A
Cattedra di Urologia, University Vita e Salute-San Raffaele, Milan, Italy.
Salonia
Andrea
A
Gallina
Andrea
A
Suardi
Nazareno
N
Rigatti
Patrizio
P
Montorsi
Francesco
F
D000284:Administration, Oral; D000286:Administration, Sublingual; D000328:Adult; D000368:Aged; D001058:Apomorphine / Q000008:administration & dosage / Q000627:therapeutic use; D002243:Carbolines / Q000627:therapeutic use; D015897:Comorbidity; D018592:Cross-Over Studies; D051544:Cytochrome P-450 CYP3A; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism; D018491:Dopamine Agonists / Q000008:administration & dosage / Q000627:therapeutic use; D004311:Double-Blind Method; D004347:Drug Interactions; D007172:Erectile Dysfunction / Q000188:drug therapy* / Q000503:physiopathology; D006801:Humans; D007093:Imidazoles / Q000627:therapeutic use; D008297:Male; D008875:Middle Aged; D015337:Multicenter Studies as Topic; D009569:Nitric Oxide / Q000502:physiology; D010726:Phosphodiesterase Inhibitors / Q000008:administration & dosage / Q000627:therapeutic use; D010879:Piperazines / Q000008:administration & dosage / Q000627:therapeutic use; D011687:Purines; D016032:Randomized Controlled Trials as Topic; D015290:Second Messenger Systems / Q000502:physiology; D000068677:Sildenafil Citrate; D013450:Sulfones / Q000627:therapeutic use; D000068581:Tadalafil; D014227:Triazines / Q000627:therapeutic use; D000069058:Vardenafil Dihydrochloride; D014665:Vasodilator Agents / Q000008:administration & dosage / Q000627:therapeutic use*
D002243:Carbolines; D018491:Dopamine Agonists; D007093:Imidazoles; D010726:Phosphodiesterase Inhibitors; D010879:Piperazines; D011687:Purines; D013450:Sulfones; D014227:Triazines; D014665:Vasodilator Agents; D009569:Nitric Oxide; D000069058:Vardenafil Dihydrochloride; D000068581:Tadalafil; D003577:Cytochrome P-450 Enzyme System; D000068677:Sildenafil Citrate; C104464:CYP3A protein, human; D051544:Cytochrome P-450 CYP3A; D001058:Apomorphine