Tolterodine

Tolterodine

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Systematic (IUPAC) name
(R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-methylphenol
Clinical data
Trade names	Detrol
AHFS/Drugs.com	monograph
MedlinePlus	a699026
Pregnancy category	AU: B3 US: C (Risk not ruled out)
Legal status	AU: S4 (Prescription only) CA: ℞-only UK: POM (Prescription only) US: ℞-only
Pharmacokinetic data
Bioavailability	77%
Protein binding	Approximately 96.3%.
Biological half-life	1.9-3.7 hours
Identifiers
CAS Number	124937-51-5 Y
ATC code	G04BD07 (WHO)
PubChem	CID: 443879
IUPHAR/BPS	360
DrugBank	DB01036 Y
ChemSpider	391967 Y
UNII	WHE7A56U7K Y
KEGG	D00646 Y
ChEBI	CHEBI:9622 Y
ChEMBL	CHEMBL1382 Y
Chemical data
Formula	C22H31NO
Molecular mass	325.488 g/mol
SMILES Cc1ccc(c(c1)[C@H](CCN(C(C)C)C(C)C)c2ccccc2)O
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
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Tolterodine (Detrol, Detrusitol) is an antimuscarinic drug that is used for symptomatic treatment of 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, pelvic floor therapy or with drugs that inhibit bladder contractions such as oxybutinin and tolterodine.

Pharmacology

Tolterodine acts on M₂ and M₃ 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.

Side effects of tolterodine

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.

External links

• Detrol - FDA factsheet
• Tolterodine