Last reviewed · How we verify
Detrol (TOLTERODINE)
Detrol works by blocking the action of a chemical called acetylcholine at the muscarinic receptors in the bladder muscle.
At a glance
| Generic name | TOLTERODINE |
|---|---|
| Sponsor | Upjohn |
| Drug class | Cholinergic Muscarinic Antagonist |
| Target | Muscarinic acetylcholine receptor M1 |
| Modality | Small molecule |
| Therapeutic area | Metabolic |
| Phase | FDA-approved |
| First approval | 1998 |
Mechanism of action
Tolterodine acts as competitive antagonist of acetylcholine at postganglionic muscarinic receptors. 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 5-hydroxymethyl tolterodine (5-HMT), the major pharmacologically active metabolite. 5-HMT, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both tolterodine and 5HMT exhibit high specificity for muscarinic receptors, since both show negligible activity or affinity for other neurotransmitter receptors and other potential cellular targets, such as calcium channels.
Approved indications
- Bladder muscle dysfunction - overactive
- Increased Urinary Frequency
- Urge incontinence of urine
- Urgent desire to urinate
Common side effects
- Dry mouth
- Abdominal pain
- Constipation
- Headache
- Vertigo/dizziness
- Accommodation abnormalities
- Xerophthalmia
- Urinary retention
- Dysuria
- Diarrhea
- Dyspepsia
- Dry skin
Drug interactions
- atazanavir
- boceprevir
- ciclosporin
- clarithromycin
- conivaptan
- erythromycin
- indinavir
- itraconazole
- ketoconazole
- mibefradil
- miconazole
- nefazodone
Key clinical trials
- TReating Incontinence for Underlying Mental and Physical Health (PHASE4)
- Oxybutynin for Post-surgical Bladder Pain and Urgency (PHASE3)
- Deprescribing dRrugs for Overactive Bladder in General Practice (DROP) (NA)
- The Effect of Nighttime Mirabegron, Solifenacin, Tolterodine, or Oxybutynin on Nocturia, Sexual Function, Autonomic Function, and Lower Urinary Tract Blood Flow Perfusion in Women With Overactive Bladder Syndrome: Randomized Controlled Trial (PHASE3)
- Treatment of Overactive Bladder With Anticholinergic Agents
- Efficacy of Low-Intensity Shockwave Therapy in Treating Radiation Cystitis (EARLY_PHASE1)
- A Multidisciplinary, Multimodal Bundled Care Approach to Chronic Pelvic Pain (PHASE3)
- Efficacy and Tolerability of DITROPAN XL (Oxybutynin Chloride) Versus DETROL LA (Tolterodine Tartrate) in Treatment of Overactive Bladder (PHASE3)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Detrol CI brief — competitive landscape report
- Detrol updates RSS · CI watch RSS
- Upjohn portfolio CI