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a salt or ester of tartaric acid

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/05/26 15:30:19」(JST)

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Tolterodine (Detrol, Detrusitol) is an antimuscarinic drug that is used for symptomatic treatment urinary incontinence.^[1]

It is marketed by Pfizer in Canada and the United States by its brand name Detrol. In Egypt it is also found under the trade names Tolterodine by Sabaa and Incont L.A. by Adwia.

Use [edit]

Detrusor overactivity (DO, contraction of the muscular bladder wall) is the most common form of UI in older adults. It is characterized by uninhibited bladder contractions causing an uncontrollable urge to void. Urinary frequency, urge incontinence and nocturnal incontinence occur. Abnormal bladder contractions that coincide with the urge to void can be measured by urodynamic studies. Treatment is bladder retraining,^[2] pelvic floor therapy or with drugs that inhibit bladder contractions such as oxybutinin and tolterodine.

Pharmacology [edit]

Tolterodine acts on M₂ and M₃ ^[3]subtypes of muscarinic receptors whereas older antimuscarinic treatments for overactive bladder act more specifically on M₃ receptors. It is marketed and manufactured by Pfizer.

Tolterodine, although it acts on all types of receptors, has fewer side effects than oxybutynin (M₃ and M₁ selective, but more so in the parotid than in the bladder) as tolterodine targets the bladder more than other areas of the body. This means that less drug needs to be given daily (due to efficient targeting of the bladder) and so there are fewer side effects.^{[citation needed]}

Side effects [edit]

Known side effects:

Xerostomia (dry mouth)
Decreased gastric motility (upset stomach)
Headache
Constipation
Dry eyes
Sleepiness

The following reactions have been reported in patients who have taken tolterodine since it has become available:

Allergic reactions including swelling
Rapid heartbeat or abnormal heartbeat
Accumulation of fluid in the arms and legs
Hallucinations

Contraindications:

Not to be used in patients with myasthenia gravis and angle closure glaucoma.

Marketing [edit]

New York Times reporter Melody Petersen, who wrote the book Our Daily Meds: How the Pharmaceutical Companies Transformed Themselves into Slick Marketing Machines and Hooked the Nation on Prescription Drugs (Farrar, Straus and Giroux, 2008), said that "the most outrageous thing" she saw covering the pharmaceutical industry was a PowerPoint presentaton on "Creating a Disease," which created a disease called "overactive bladder" for the purpose of marketing Detrol. Doctors try to manage incontinence in non-pharmaceutical ways, she said. Detrol became a blockbuster, said Petersen, despite the adverse effect of severe memory problems.^[4]

References [edit]

^ Philip Van Kerrebroeck, Karl Kreder, Udo Jonas, Norm Zinner, Alan Wein (2001). "Tolterodine once-daily: superior efficacy and tolerability in the treatment of the overactive bladder1". Urology 57 (3): 414–421.
^ Bladder retraining ichelp.org Interstitial Cystitis Association Acessed July 13, 2012
^ [1]
^ This Is Your Country on Drugs: Melody Petersen talks about how we’re hooked on Big Pharma. By George Kenney, In These Times, January 1, 2010

External links [edit]

Detrol - FDA factsheet
Tolterodine
Tolterodine (patient information)

UpToDate Contents

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1. 夜間頻尿：臨床症状、診断、および治療治療 nocturia clinical presentation diagnosis and treatment
2. 女性における尿失禁の治療および予防 treatment and prevention of urinary incontinence in women
3. 男性における下部尿路症状 lower urinary tract symptoms in men
4. 男性の尿失禁 urinary incontinence in men
5. 小児における膀胱機能障害のマネージメント management of bladder dysfunction in children

English Journal

Phase II Study on the Efficacy and Safety of the EP1 Receptor Antagonist ONO-8539 for Nonneurogenic Overactive Bladder Syndrome.

Chapple CR1, Abrams P2, Andersson KE3, Radziszewski P4, Masuda T5, Small M5, Kuwayama T5, Deacon S5.Author information 1Royal Hallamshire Hospital, Sheffield, United Kingdom. Electronic address: c.r.chapple@sheffield.ac.uk.2Southmead Hospital, Bristol Urological Institute, Bristol, United Kingdom.3Wake Forest University School of Medicine, Winston-Salem, North Carolina.4Department of Urology, Medical University of Warsaw, Warsaw, Poland.5ONO Pharma Ltd., London, United Kingdom.AbstractPURPOSE: We evaluated the efficacy, safety and tolerability of the EP1 receptor antagonist ONO-8539 in patients with overactive bladder syndrome.
The Journal of urology.J Urol.2014 Jan;191(1):253-60. doi: 10.1016/j.juro.2013.08.082. Epub 2013 Sep 7.
PURPOSE: We evaluated the efficacy, safety and tolerability of the EP1 receptor antagonist ONO-8539 in patients with overactive bladder syndrome.MATERIALS AND METHODS: This was a 12-week, randomized, double-blind, placebo controlled, parallel group, multicenter study with a 2-week single blind place
PMID 24018240

Mirabegron in overactive bladder: A review of efficacy, safety, and tolerability.

Chapple CR, Cardozo L, Nitti VW, Siddiqui E, Michel MC.Author information Department of Urology, Royal Hallamshire Hospital, Sheffield Teaching Hospitals, Sheffield, United Kingdom.AbstractAIMS: Mirabegron, the first β3 -adrenoceptor agonist to enter clinical practice, has a different mechanism of action from antimuscarinic agents. This review presents data on the efficacy, safety, and tolerability of mirabegron in studies conducted to date.
Neurourology and urodynamics.Neurourol Urodyn.2014 Jan;33(1):17-30. doi: 10.1002/nau.22505. Epub 2013 Oct 11.
AIMS: Mirabegron, the first β3 -adrenoceptor agonist to enter clinical practice, has a different mechanism of action from antimuscarinic agents. This review presents data on the efficacy, safety, and tolerability of mirabegron in studies conducted to date.METHODS: All clinical data on mirabegron th
PMID 24127366

Profiling of enantiopure drugs towards aryl hydrocarbon (AhR), glucocorticoid (GR) and pregnane X (PXR) receptors in human reporter cell lines.

Novotna A1, Kamenickova A1, Pecova M1, Korhonova M1, Bartonkova I1, Dvorak Z2.Author information 1Department of Cell Biology and Genetics, Regional Centre of Advanced Technologies and Materials, Faculty of Science, Palacký University, Šlechtitelů 11, 783 71 Olomouc, Czech Republic.2Department of Cell Biology and Genetics, Regional Centre of Advanced Technologies and Materials, Faculty of Science, Palacký University, Šlechtitelů 11, 783 71 Olomouc, Czech Republic. Electronic address: moulin@email.cz.AbstractIn the past decade, a large number of enantiopure drugs were introduced to clinical practice, since improved therapeutic effects were demonstrated for one of the enantiomers from originally racemic drug. While the therapeutic effects and safety of enantiopure drugs were tested prior to their approval, various biological enantiospecific activities of these, often "old" drugs, remain to be elucidated. In the current paper, we examined enantiospecific effects of clinically used enantiopure drugs containing one chiral center in the structure (i.e. zopiclone, tamsulosin, tolterodine, modafinil, citalopram) towards aryl hydrocarbon (AhR), glucocorticoid (GR) and pregnane X (PXR) receptors in human reporter cell lines. The cytotoxicity (IC50), agonist (EC50) and antagonist effects (IC50) of R-form, S-form and racemic mixture for each tested drugs were determined and compared in AhR-, GR- and PXR-gene reporter cell lines. Since AhR, GR and PXR are key regulators of drug metabolism, energy metabolism, immunity and play many other physiological functions, the data presented here might be of toxicological significance.
Chemico-biological interactions.Chem Biol Interact.2013 Dec 6;208C:64-76. doi: 10.1016/j.cbi.2013.11.018. [Epub ahead of print]
In the past decade, a large number of enantiopure drugs were introduced to clinical practice, since improved therapeutic effects were demonstrated for one of the enantiomers from originally racemic drug. While the therapeutic effects and safety of enantiopure drugs were tested prior to their approva
PMID 24316275

Japanese Journal

臨床研究・症例報告小児排尿機能未熟型夜尿症に対する徐放性酒石酸トルテロジンの短期効果

加納健一,有阪治
小児科臨床 60(9), 1881-1884, 2007-09
NAID 40015529446

High-performance liquid chromatography-electrospray ionization mass spectrometric determination of tolterodine tartrate in human plasma

ZHANG Beibei,ZHANG Zunjian,TIAN Yuan,XU Fengguo
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 824(1), 92-98, 2005-09-25
NAID 10017123833

Therapeutic efficacy of extended release oxybutynin chloride, and immediate release and long acting tolterodine tartrate in children with diurnal urinary incontinence

REINBERG Y
J. Urol. 169, 317-319, 2003
NAID 30009410110

「トルテロジン」

Tolterodine
Systematic (IUPAC) name
	(R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-methylphenol
Clinical data
Trade names	Detrol
AHFS/Drugs.com	monograph
MedlinePlus	a699026
Pregnancy cat.	?
Legal status	?
Pharmacokinetic data
Bioavailability	77%
Protein binding	Approximately 96.3%.
Half-life	1.9-3.7 hours
Identifiers
CAS number	124937-51-5
ATC code	G04BD07
PubChem	CID 443879
DrugBank	DB01036
ChemSpider	391967
UNII	WHE7A56U7K
KEGG	D00646
ChEBI	CHEBI:9622
ChEMBL	CHEMBL1382
Chemical data
Formula	C22H31NO
Mol. mass	325.488 g/mol
	SMILES Oc1ccc(cc1[C@@H](c2ccccc2)CCN(C(C)C)C(C)C;
	InChI InChI=1S/C22H31NO/c1-16(2)23(17(3)4)14-13-20(19-9-7-6-8-10-19)21-15-18(5)11-12-22(21)24/h6-12,15-17,20,24H,13-14H2,1-5H3/t20-/m1/s1 ; Key:OOGJQPCLVADCPB-HXUWFJFHSA-N ;
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