Trospium chloride: A quaternary amine with unique pharmacologic properties

  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},
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
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
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
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
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
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
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
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
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.


Effects of Tolterodine, Trospium Chloride, and Oxybutynin on the Central Nervous System
The results of this study support the findings that oxybutynin as a tertiary amine crosses the blood‐brain barrier, causing significant qEEG activity changes and more pronounced central adverse effects.
Importance of pharmacological and physicochemical properties for tolerance of antimuscarinic drugs in the treatment of detrusor instability and detrusor hyperreflexia--chances for improvement of therapy.
It becomes obvious that there are significant differences between antimuscarinic drugs, which are of clinical relevance and include possible starting points for the development of new drugs and application forms.
The mechanism of action of topiramate
A combination of pharmacological properties that may explain why topiramate is effective in both partial and generalized seizures, and why it is proving efficacious in numerous intractable syndromic epilepsies.
Trospium chloride – an effective drug in the treatment of overactive bladder and detrusor hyperreflexia
Trospium chloride, a quaternary ammonium derivative of nortropanol, has been evaluated in a number of clinical and pharmacological studies and an overview of the results of 20 clinical trials and post-marketing surveillance studies including more than 10 000 patients is presented.
M3 receptor antagonism by the novel antimuscarinic agent solifenacin in the urinary bladder and salivary gland
M3 receptor antagonism by solifenacin could be bladder-selective and may provide new approaches to the pharmacotherapy of overactive bladder, as well as study the tissue selectivity between bladders and salivary glands.
Muscarinic antagonists in development for disorders of smooth muscle function.
Determination of the bioavailability of the quaternary compound trospium chloride in man from urinary excretion data.
For the quaternary compound trospium chloride (Spasmex) which is used as an anticholinergic agent a new sensitive assay method has been developed that allows the quantitative determination of the drug in human urine and plasma and to determine the bioavailability in man.
Selective muscarinic receptor agonists and antagonists.
Novel, selective agonists and antagonists, both in terms of their use in defining muscarinic receptor subtypes and their potential clinical utility are assessed, to provide an advance over earlier therapeutics with which the clinical efficacy was compromised by the side effect profile.
[Intravesical instillation of trospium chloride, oxybutynin and verapamil for relaxation of the bladder detrusor muscle. A placebo controlled, randomized clinical test].
The immediate onset of effect and the lack of adverse drug reactions suggest that treatment with topical oxybutynin or trospium chloride is an effective alternative in patients with intolerable side effects when orally treated.
Trospium chloride versus oxybutynin: a randomized, double-blind, multicentre trial in the treatment of detrusor hyper-reflexia.
Assessment of tolerance in terms of adverse drug effects showed that TCl had certain advantages, and trospium chloride and oxybutynin are of substantially equal value as parasympathetic antagonists.