Trospium chloride
[CAS# 10405-02-4]

Identification

• Classification: Biochemical >> Inhibitor >> Neuronal signaling >> AChR antagonist
• Name: Trospium chloride
• Synonyms: [(1S,5R)-spiro[8-azoniabicyclo[3.2.1]octane-8,1'-azolidin-1-ium]-3-yl] 2-hydroxy-2,2-diphenylacetate chloride
• Molecular Formula: C₂₅H₃₀NO₃^.Cl
• Molecular Weight: 427.97
• CAS Registry Number: 10405-02-4
• EC Number: 233-875-4
• SMILES: C1CC[N+]2(C1)[C@@H]3CC[C@H]2CC(C3)OC(=O)C(C4=CC=CC=C4)(C5=CC=CC=C5)O.[Cl-]

Properties

• Solubility: 2 mg/mL (DMSO)

Safety Data

• Hazard Symbols: GHS07 Warning
• Hazard Statements: H302-H315-H319-H335
• Precautionary Statements: P261-P305+P351+P338

Hazard Classification

Hazard	Class	Category Code	Hazard Statement
Acute toxicity	Acute Tox.	4	H302
Chronic hazardous to the aquatic environment	Aquatic Chronic	3	H412
Acute toxicity	Acute Tox.	4	H332
Acute toxicity	Acute Tox.	4	H312

Discovory and Applicatios

Trospium chloride is a synthetic quaternary ammonium compound used primarily in the treatment of overactive bladder (OAB) and its associated symptoms, including urinary urgency, frequency, and incontinence. It is classified as an antimuscarinic agent and works by blocking the muscarinic receptors in the bladder, specifically the M3 receptors that are responsible for the contraction of the bladder muscle. This inhibition reduces bladder spasms and improves symptoms associated with overactive bladder.

Trospium chloride was first introduced into clinical practice in the early 1990s. Its development was aimed at providing a more effective treatment for patients suffering from urinary incontinence and other related symptoms, with the aim of reducing adverse side effects commonly associated with other antimuscarinic agents. Due to its quaternary ammonium structure, Trospium chloride is less likely to cross the blood-brain barrier, which contributes to a reduced incidence of central nervous system (CNS) side effects such as cognitive impairment and sedation, which are more commonly seen with other medications in this class.

Trospium chloride is generally administered orally in tablet form or as an extended-release formulation, providing flexibility in dosing regimens. The compound is highly water-soluble, but its quaternary ammonium structure limits its absorption from the gastrointestinal tract, resulting in lower systemic exposure compared to some other antimuscarinics. This characteristic makes it particularly useful for patients who are more susceptible to the side effects of antimuscarinic drugs, such as dry mouth, constipation, and blurred vision.

In terms of clinical application, Trospium chloride has been shown to be effective in improving the quality of life for patients with overactive bladder syndrome. Several clinical trials have confirmed its efficacy in reducing urinary frequency, urgency, and incontinence, with an acceptable safety profile. It is often prescribed to patients who do not respond well to lifestyle changes or other non-pharmacologic treatments for OAB.

Beyond its primary use in urology, Trospium chloride has also been explored for other potential applications, including its use in combination with other medications to enhance treatment efficacy for various bladder disorders. However, its most well-established and widely recognized application remains in the treatment of overactive bladder.

Trospium chloride is generally considered safe for use in most patients, though certain populations, such as those with severe renal impairment or hypersensitivity to the drug, may require caution. The medication is typically not recommended during pregnancy, and it should be used with caution in elderly patients due to the potential for age-related pharmacokinetic changes. Regular monitoring and adjustment of dosing may be necessary to optimize treatment outcomes and minimize the risk of adverse effects.

In summary, Trospium chloride is a well-established antimuscarinic agent used in the treatment of overactive bladder. Its development was aimed at providing an effective treatment option with a reduced risk of CNS side effects, making it an important option for patients suffering from this condition. It has demonstrated efficacy in clinical trials and continues to be an essential medication in managing urinary symptoms associated with overactive bladder.

References

2024. Efficacy of xanomeline and trospium chloride in schizophrenia: pooled results from three 5-week, randomized, double-blind, placebo-controlled, EMERGENT trials. Schizophrenia (Heidelberg, Germany), 10.
DOI: 10.1038/s41537-024-00525-6

2025. Emerging Pharmacological Approaches for Psychosis and Agitation in Alzheimer�s Disease. CNS Drugs, 39(2).
DOI: 10.1007/s40263-024-01133-9

2015. Systematic solvate screening of trospium chloride: discovering hydrates of a long-established pharmaceutical. CrystEngComm, 17(33).
DOI: 10.1039/C5CE00744E