title: Terodiline inhibition of human bladder contraction. Effects in vitro and in women with unstable bladder.
abstract: Terodiline, a drug with anticholinergic and calcium antagonistic properties, effectively relaxed carbachol-contracted, isolated human bladder preparations. In the concentrations used, terodiline displaced to the right the concentration-response curve obtained on cumulative addition of carbachol. The maximum response was slightly reduced only at the highest terodiline concentration used (5 microM), suggesting a mainly competitive antimuscarinic effect. Nine patients, aged 12--78 years, suffering from urge urinary incontinence were investigated by simultaneous urethro-cystometry before and after treatment with terodiline 12.5 mg twice or three times daily for 10 days. The patients reported subjective improvement with almost no side effects. Objectively, the number of uninhibited bladder contractions and the amplitude of the contractions decreased. The bladder capacity was almost doubled. There were no marked effects on bladder and urethral pressures at rest, and only two of the investigated patients had slight residual urine after treatment. The results suggest that terodiline is a promising alternative to existing drugs for inhibition of undesired detrusor activity.
mesh_terms: D000293:Adolescent; D000328:Adult; D000368:Aged; D002082:Butylamines / Q000494:pharmacology* / Q000627:therapeutic use; D002217:Carbachol / Q000494:pharmacology; D002648:Child; D002675:Child, Preschool; D004305:Dose-Response Relationship, Drug; D005260:Female; D006801:Humans; D007223:Infant; D008297:Male; D008875:Middle Aged; D009130:Muscle, Smooth / Q000187:drug effects / Q000294:innervation; D010276:Parasympatholytics; D011312:Pressure; D014521:Urethra / Q000187:drug effects / Q000503:physiopathology; D001743:Urinary Bladder / Q000187:drug effects / Q000503:physiopathology; D014549:Urinary Incontinence / Q000188:drug therapy*; D014563:Urodynamics / Q000187:drug effects
chemical_list: D002082:Butylamines; D010276:Parasympatholytics; C010637:terodiline; D002217:Carbachol