Tolterodine

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 Y
ATC code	G04BD07
PubChem	CID 443879
DrugBank	DB01036
ChemSpider	391967 Y
UNII	WHE7A56U7K Y
KEGG	D00646 Y
ChEBI	CHEBI:9622 Y
ChEMBL	CHEMBL1382 Y
Chemical data
Formula	C22H31NO
Mol. mass	325.488 g/mol
SMILES	eMolecules & PubChem
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 Y Key:OOGJQPCLVADCPB-HXUWFJFHSA-N Y
Y (what is this?)  (verify)

Tolterodine (Detrol, Detrusitol) is an antimuscarinic drug that is used to treat urinary incontinence.

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

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 or with drugs that inhibit bladder contractions such as oxybutinin and tolterodine.

Pharmacology

Tolterodine acts on M₁, M₂, M₃, M₄ and M₅ subtypes of muscarinic receptors whereas modern antimuscarinic treatments for overactive bladder only act on M₃ receptors making them more selective. 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.

Side effects

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

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.

External links

• Detrol - FDA factsheet
• Tolterodine
• Tolterodine (patient information)