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Pharmacology of the Lower Urinary Tract
Published in Karl H. Pang, Nadir I. Osman, James W.F. Catto, Christopher R. Chapple, Basic Urological Sciences, 2021
Pedro Abreu-Mendes, João Silva, Francisco Cruz
Intravesical: oxybutynin and trospium chloride increase bladder capacity and produce clinical improvement with few side effects in neurogenic and non-neurogenic detrusor overactivity patients. However, unless a delivery system is developed to allow a continuous release of the drug, intravesical delivery is limited to patients doing intermittent self-catheterisation.
Continence
Published in Andrew Stevens, James Raftery, Jonathan Mant, Sue Simpson, Health Care Needs Assessment, 2018
Catherine W. McGrother, Madeleine Donaldson
There is limited evidence that trospium chloride is useful in the treatment of detrusor overactivity. Randomised controlled trials have shown improvements in urodynamic parameters and subjective symptomatic improvement.201,202 Trospium (20 mg bd) seems to be better tolerated than oxybutynin (5 mg tds) and as the compound does not cross the blood-brain barrier, very few CNS side effects have been reported.
Urinary Incontinence
Published in David M. Luesley, Mark D. Kilby, Obstetrics & Gynaecology, 2016
Dudley Robinson, Linda Cardozo
Trospium chloride is a quaternary ammonium compound which is non-selective for muscarinic receptor subtypes and shows low biological availability. It crosses the blood-brain barrier to a limited extent and hence would appear to have few cognitive effects.117 A placebo-controlled, randomised, double-blind multicentre trial has shown trospium to increase cystometric capacity and bladder volume at first unstable contraction, leading to significant clinical improvement without an increase in adverse effects over placebo.118 When compared to oxybutynin it was found to have comparable efficacy although was associated with a lower incidence of dry mouth and patient withdrawal.119 At present trospium chloride would appear to be as effective as oxybutynin although it may be associated with fewer adverse effects.
Managing autonomic dysfunction in Parkinson’s disease: a review of emerging drugs
Published in Expert Opinion on Emerging Drugs, 2020
Dinkar Kulshreshtha, Jacky Ganguly, Mandar Jog
Oxybutynin and tolterodine are nonselective muscarinic blockers with maximum risk of central side effects. Darifenacin and solifenacin are M3- selective antagonists. Trospium chloride is a nonselective muscarinic antagonist but it does not cross BBB because of low lipid solubility [54]. However, a review of concomitant medications is necessary to assess a patient’s anticholinergic burden, and just adding an anti-muscarinic medication may increase the risk for falls, cognitive impairment and all-cause mortality [55]. In one study, amantadine, as an N-methyl-D-aspartate (NMDA) antagonist in a dose of 150 mg/day decreased urinary frequency, urgency, and urge incontinence without cognitive side effects [56]. α-adrenoceptor blockers decrease urethral resistance during voiding. There is a significant risk of postural hypotension with this class of medications and in PD patients, they should be used sparingly, if at all.
Formulation strategy towards minimizing viscosity mediated negative food effect on disintegration and dissolution of immediate release tablets
Published in Drug Development and Industrial Pharmacy, 2018
Trospium chloride (purity – 99.9%) was gifted by Dr R. Pfleger GmbH, Germany. Mean particle size was 276.7 ± 229.3 µm. Hydroxypropyl methyl cellulose E4M for preparation of viscous disintegration/dissolution medium was obtained from Synopharm (Germany). Primellose (Croscarmellose Sodium, DFE Pharma, Germany, 59.96 ± 38.68 µm), Primojel (Sodium Starch glycolate, DFE Pharma, Germany, 44.94 ± 19.37 µm), and Kollidone CL-SF (Crospovidone, BASF, Germany, 31.30 ± 36.90 µm) were used as superdisintegrants. Tablettose 80 (Lactose, Meggle, Germany, 142.1 ± 145.8 µm), PVP K-30 (Polyvinylpyrrolidon, Carl Roth GmbH, Germany, 267.2 ± 213.9 µm), and magnesium stearate (Fagron GmbH, Germany, 10.18 ± 10.75 µm) were used as filler, binder, and lubricant, respectively, in the direct compression tablet formulations.
The cognitive safety of antimuscarinics in the treatment of overactive bladder
Published in Expert Opinion on Drug Safety, 2020
George Araklitis, Dudley Robinson
When considering patients over the age of 65 years, our first-line medical treatment is trospium chloride. Being a quaternary amine it is less likely to cross the blood-brain barrier, and since it is a P-gp substrate, it can be actively transported out of the central nervous system. Studies suggest that it does not cause cognitive side effects. Alternatively we may consider using fesoterodine due to its bladder specificity, being a P-gp substrate, and its well-documented safety in the elderly population.