Trospium chloride: A quaternary amine with unique pharmacologic properties

@article{Pak2003TrospiumCA,
  title={Trospium chloride: A quaternary amine with unique pharmacologic properties},
  author={Raymond W. Pak and Steven P. Petrou and David Staskin},
  journal={Current Urology Reports},
  year={2003},
  volume={4},
  pages={436-440}
}
The mainstay of pharmacologic treatment of overactive bladder is anticholinergic therapy. Cholinergic blockade is efficacious in decreasing the symptoms of urgency, frequency, and urge incontinence, but also is associated with undesirable side effects such as dry mouth, blurred vision, constipation, and central nervous system side effects. The property of anticholinergic agents that has been associated with increased efficacy and tolerability is receptor specificity. The safety of… 
Trospium chloride: over 20 years of clinical use
TLDR
The presence of unchanged trospium in the bladder – the primary therapeutic site of action – may contribute to pharmacological activity, providing earlier onset and improved and prolonged efficacy compared with other, more extensively metabolized antimuscarinic agents.
Trospium Chloride in the Management of Overactive Bladder
TLDR
Direct comparative studies in patients with overactive bladder indicate that trospium chloride is at least as effective as oxybutynin and tolterodine, and dosage adjustments based on age or sex appear unwarranted, such adjustments may be needed in Patients with severe renal impairment.
Trospium chloride: an anticholinergic quaternary ammonium compound for the treatment of overactive bladder
  • N. Zinner
  • Medicine
    Expert opinion on pharmacotherapy
  • 2005
TLDR
The fast-acting efficacy of trospium chloride, coupled with its good safety profile and tolerability, make it an important new option for treatment of OAB.
Anticholinergics for Overactive Bladder Therapy: Central Nervous System Effects
TLDR
The physicochemical and pharmacokinetic properties of OAB antimuscarinics that affect their propensity to cause adverse CNS effects are discussed, as observed in phase III clinical trials and in specific investigations on cognitive function and sleep architecture.
Improving the Tolerability of Anticholinergic Agents in the Treatment of Overactive Bladder
TLDR
Clinical trials involving a transdermal formulation of oxybutynin have shown that this delivery method may be associated with a lower incidence of anticholinergic adverse events compared with both the immediate-release and the extended-release oral formulations of traditional agents, as well as the most recently approved agents — trospium chloride, solifenacin and darifenACin.
Clinical Pharmacokinetics of Trospium Chloride
TLDR
The pharmacokinetics of trospium chloride have been investigated in healthy volunteers, in patients with renal and hepatic impairment, and in those with symptoms of overactive bladder, after oral, intravenous and intravesical administration.
Blood-Brain Barrier Permeation and Efflux Exclusion of Anticholinergics Used in the Treatment of Overactive Bladder
TLDR
The properties of anticholinergics that affect blood-brain barrier penetration and active transport out of the CNS are reviewed, issues of increased BBB permeability in patients with OAB are discussed, and the clinical implications of BBB penetration on adverse events associated with anticholergics are examined.
Trospium chloride: a different anticholinergic
TLDR
Trospium chloride is the only quaternary amine antimuscarinic approved in the USA and Europe for the treatment of OAB and its distinct pharmacological properties distinguish it from other agents in this class, all of which are tertiary amines.
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TLDR
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