Clinical Pharmacokinetics of Trospium Chloride

  title={Clinical Pharmacokinetics of Trospium Chloride},
  author={Oxana Doroshyenko and Alexander Jetter and Karl Peter Odenthal and Uwe Fuhr},
  journal={Clinical Pharmacokinetics},
Trospium chloride, a quaternary amine with anticholinergic properties, is used for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and urinary frequency. 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.After oral administration, absorption of the hydrophilic… 
Trospium Chloride Treatment of Overactive Bladder
Trospium chloride is an antimuscarinic agent indicated for the treatment of OAB with symptoms of urge urinary incontinence, urgency, and urinary frequency and appears to be a feasible alternative for patients who cannot tolerate oxybutynin.
Effect of Concomitant Administration of Trospium Chloride Extended Release on the Steady-State Pharmacokinetics of Metformin in Healthy Adults
No dosage adjustment is necessary for met formin when coadministered with trospium chloride XR and metformin under steady-state conditions in healthy male and female subjects, and no safety/tolerability issues of concern were observed with coadministration.
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.
Pharmacokinetic and bioequivalence studies of trospium chloride after a single-dose administration in healthy Chinese volunteers.
The study aimed to compare and evaluate the bioequivalence of a new generic preparation of trospium chloride capsule and the available import tablet for the requirement of state regulatory criteria in China.
Trospium chloride in patients with neurogenic detrusor overactivity: is dose titration of benefit to the patients?
Generally, in patients with neurogenic detrusor overactivity daily doses of 45 mg trospium chloride can be considered as being the standard dose, and dose adjustment, e.g. due to increased body weight, might usually not be necessary.
Once-Daily Trospium Chloride 60 mg Extended Release in Subjects with Overactive Bladder Syndrome Who Use Multiple Concomitant Medications
The data support the conclusion that trospium chloride XR is safe and effective in patients with OAB taking multiple concomitant medications, and predictors of treatment-emergent adverse events (TEAEs) identified by multivariate logistic regression analysis.
Pharmacokinetics of overactive bladder drugs: Getting ahead of the curve
This review summarizes basic pharmacokinetic concepts and demonstrates these concepts using examples of antimuscarinic drugs that treat overactive bladder and offers insight into how the knowledge of pharmacokinetics can be applied to better analyze and understand the pharmacologic literature.
Study of the Population Pharmacokinetic Characteristics of Once-Daily Trospium Chloride 60 mg Extended-Release Capsules in Patients with Overactive Bladder and in Healthy Subjects
Treatment of most patients with overactive bladder with once-daily trospium chloride 60 mg XR should not require consideration of key intrinsic demographic parameters, as the best population pharmacokinetic model was determined to be a two-compartment model with zero-order release into the depot compartment and first-order absorption.
Pharmacokinetic Drug‐Drug Interactions Between Trospium Chloride and Ranitidine Substrates of Organic Cation Transporters in Healthy Human Subjects
Intravenous trospium significantly lowered mean absorption time and relative bioavailability of ranitidine, which was most likely caused by muscarinic receptor blocking effects on intestinal motility and water turnover.


Absorption pattern of trospium chloride along the human gastrointestinal tract assessed using local enteral administration.
Trospium chloride is absorbed primarily in the upper gastrointestinal tract and development of modified release preparations must balance prolonged apparent absorption rates of the drug against a decrease in bioavailability.
Trospium chloride: A quaternary amine with unique pharmacologic properties
Trospium chloride, available in Europe for more than 20 years and under review by the US Food and Drug Administration for the treatment of overactive bladder, is a quaternary amine that is minimally metabolized, not highly protein-bound, and theoretically should not cross the blood brain barrier.
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.
Trospium chloride improves overactive bladder symptoms: a multicenter phase III trial.
Trospium was found to have sustained effectiveness beginning at the end of week 1 in decreasing the number of voids, urge incontinent episodes, total daily micturitions and urge severity, and in increasing volume per void.
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.
Influences of trospium chloride and oxybutynin on quantitative EEG in healthy volunteers
The results suggest that trospium chloride is less likely to produce central nervous adverse effects than to oxybutynin.
Trospium chloride: an effective option for medical treatment of bladder overactivity.
  • I. Füsgen, D. Hauri
  • Medicine
    International journal of clinical pharmacology and therapeutics
  • 2000
This article provides an overview on pharmacological and clinical trials with trospium chloride (TC1) in the treatment of urinary incontinence and selected pharmacologicaland clinical pharmacokinetic data are discussed as a basis for a better interpretation and understanding of the clinical trial results.
Effect of trospium chloride on somnolence and sleepiness in patients with overactive bladder
Trospium chloride did not increase daytime sleepiness or appear to produce CNS adverse effects, as measured by the Stanford Sleepiness Scale and the incidence of CNS adverse events, and there was no difference in these findings across age groups.
Inhibitory effects of trospium chloride on cytochrome P450 enzymes in human liver microsomes.
Trospium chloride has negligible inhibitory effects on CYP3A4, CYP1A2, CyP2E1, CYB2C19, CYp2C9 and CYP2A6 activity but is a reasonably potent inhibitor of CYP 2D6 in vitro.