Influences of trospium chloride and oxybutynin on quantitative EEG in healthy volunteers

Pietzko, A.; Dimpfel, Wilfried; Schwantes, Ulrich; Topfmeier, P.

doi:10.1007/bf00191165

Cited by 106 publications

(70 citation statements)

References 7 publications

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“…Thus, the selectivity for the urinary bladder over the brain was relatively low for oxybutynin, suggesting a high feasibility of CNS side effects at pharmacological doses to treat OAB. This finding seems to be in a reasonable agreement with previous observations of oxybutynin shown by pharmacological (Sugiyama et al, 1999) and ex vivo receptor binding (Oki et al, 2001) studies in rats and also by clinical studies (Pietzko et al, 1994;Katz et al, 1998;Todorova et al, 2001;Ancelin et al, 2006). In fact, CNS side effect by oxybutynin occurred in patients with OAB and in older subjects receiving this drug (Scheife and Takeda, 2005;Kay et al, 2006).…”

Section: Discussionsupporting

confidence: 91%

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In Vivo Quantitative Autoradiographic Analysis of Brain Muscarinic Receptor Occupancy by Antimuscarinic Agents for Overactive Bladder Treatment

Maruyama¹,

Tsukada²,

Nishiyama³

et al. 2008

J Pharmacol Exp Ther

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We evaluated the effects of five clinically used antimuscarinic agents for overactive bladder (OAB) treatment on in vivo muscarinic receptor binding in rat brain by quantitative autoradiography. There was a dose-related decrease in in vivo specific (ϩ)N-[11 C]methyl-3-piperidyl benzilate ([ 11 C](ϩ)3-MPB) binding in each brain region of rats 10 min after i.v. injection of oxybutynin, propiverine, solifenacin, and tolterodine. Rank order of the i.v. dose for 50% receptor occupancy (RO 50 ) of antimuscarinic agents in rat brain regions was propiverine Ͼ solifenacin Ͼ tolterodine, oxybutynin. There was a good linear relationship between in vivo (pRO 50 values in the rat hippocampus) and in vitro (pK i values in human M 1 receptors) receptor binding activities of propiverine, solifenacin, and tolterodine. The observed RO 50 value of oxybutynin was approximately five times smaller than the predicted in vitro K i value. The dose ratios of antimuscarinic agents for the brain receptor occupancy (RO 50 ) to the inhibition of carbachol-and volume-induced increases in intravesical pressure (ID 50 ), which reflects in vivo selectivity for the urinary bladder over the brain, were greater for solifenacin, tolterodine, and propiverine than oxybutynin. Darifenacin displayed only a slight decrease in specific [11 C](ϩ)3-MPB binding in the rat brain regions, and it was not dose-related. In conclusion, in vivo quantitative autoradiographic analysis of brain muscarinic receptor occupancy may provide fundamental basis for managing central nervous system (CNS) side effects in antimuscarinic therapy for OAB. It is suggested that in the treatment of OAB, CNS side effects can be avoided by antimuscarinic agents with high selectivity for the urinary bladder over the brain.

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Section: Discussionsupporting

confidence: 91%

“…They found that oxybutynin significantly altered qEEG activity, whereas tolterodine and trospium induce only a slight effect on qEEG activity. Similar electrophysiological results in healthy males with oxybutynin have been shown by Pietzko et al (1994).…”

Section: Discussionsupporting

confidence: 84%

In Vivo Quantitative Autoradiographic Analysis of Brain Muscarinic Receptor Occupancy by Antimuscarinic Agents for Overactive Bladder Treatment

Maruyama¹,

Tsukada²,

Nishiyama³

et al. 2008

J Pharmacol Exp Ther

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Section: Cardiovascular Safetysupporting

confidence: 77%

An Overview on Mixed Action Drugs for the Treatment of Overactive Bladder and Detrusor Overactivity

Asimakopoulos

Cerruto²,

Popolo³

et al. 2012

Urol Int

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Objectives: To provide an overview on the efficacy, tolerability, safety and health-related quality of life (HRQoL) of drugs with a mixed action used in the treatment of overactive bladder (OAB). Evidence Acquisition: MEDLINE database and abstract books of the major conferences were searched for relevant publications from 1966 to 2011 and using the key words ‘overactive bladder’, ‘detrusor overactivity’, ‘oxybutynin’, ‘propiverine’, and ‘flavoxate’. Two independent reviewers considered publications for inclusion and extracted relevant data, without performing a meta-analysis. Evidence Synthesis: Old and conflicting data do not support the use of flavoxate, while both propiverine and oxybutynin were found to be more effective than placebo in the treatment of OAB. Propiverine was at least as effective as oxybutynin but with a better tolerability profile even in the pediatric setting. Overall, no serious adverse event for any product was statistically significant compared to placebo. Improvements were seen in HRQoL with treatment by the oxybutynin transdermal delivery system and propiverine extended release. Conclusions: While there is no evidence to suggest the use of flavoxate in the treatment of OAB, both oxybutynin and propiverine appear efficacious and safe. Propiverine shows a better tolerability profile than oxybutynin. Both drugs improve HRQoL of patients affected by OAB. Profiles of each drug and dosage differ and should be considered in making treatment choices.

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“…In 1994 Pietzko et al [22] used quantitative evaluation of the multichannel electroencephalogram (EEG) obtained from young healthy volunteers to study possible CNS adverse effects of oral oxybutynin, oral and intravenous trospium chloride, and no drugs. The biologic activity of these drugs was ascertained by simultaneous recording of the heart rate.…”

Section: Quantitative Topographic Electroencephalogram Studies For Pomentioning

confidence: 99%

Confusion about measuring central nervous system effects

Madersbacher

2007

Curr Bladder Dysfunct Rep

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Influences of trospium chloride and oxybutynin on quantitative EEG in healthy volunteers

Cited by 106 publications

References 7 publications

In Vivo Quantitative Autoradiographic Analysis of Brain Muscarinic Receptor Occupancy by Antimuscarinic Agents for Overactive Bladder Treatment

In Vivo Quantitative Autoradiographic Analysis of Brain Muscarinic Receptor Occupancy by Antimuscarinic Agents for Overactive Bladder Treatment

An Overview on Mixed Action Drugs for the Treatment of Overactive Bladder and Detrusor Overactivity

Confusion about measuring central nervous system effects

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