Active Ingredient History
Tolterodine is competitive muscarinic receptors M3 and M2 antagonist. It was sold under trade names detrol for the treatment of overactive bladder with symptoms of urge urinary incontinence. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors. After oral administration, tolterodine is metabolized in the liver, resulting in the formation of the 5-hydroxymethyl derivative, a major pharmacologically active metabolite. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both tolterodine and the 5-hydroxymethyl metabolite exhibit a high specificity for muscarinic receptors, since both show negligible activity and affinity for other neurotransmitter receptors and other potential cellular targets, such as calcium channels. Tolterodine has a pronounced effect on bladder function. The main effects of tolterodine at 1 and 5 hours were an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure. These findings are consistent with an antimuscarinic action on the lower urinary tract. NCATS
Drug Pricing (per unit)
Note: This drug pricing data is preliminary, incomplete, and may contain errors.
Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
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Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
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Chronic Pain (Phase 4)
Cognition (Phase 4)
Dental Caries (Phase 1)
Genotype (Phase 1)
Health (Phase 2)
Healthy Volunteers (Phase 4)
Low Back Pain (Phase 3)
Lower Urinary Tract Symptoms (Phase 2/Phase 3)
Memory (Phase 4)
Neuralgia (Phase 1/Phase 2)
Pain (Phase 3)
Pelvic Organ Prolapse (Phase 3)
Pharmacokinetics (Phase 4)
Prostatic Hyperplasia (Phase 4)
Prostatic Neoplasms (Phase 4)
Sjogren's Syndrome (Phase 4)
Sleep Apnea, Obstructive (Phase 4)
Ureteral Diseases (Phase 2)
Ureteral Obstruction (Phase 4)
Urinary Bladder Neck Obstruction (Phase 4)
Urinary Incontinence (Phase 4)
Urinary Incontinence, Stress (Phase 4)
Urinary Incontinence, Urge (Phase 4)
Urination Disorders (Phase 2/Phase 3)
Trial | Phase | Start Date | Organizations | Indications |
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