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Tolterodine

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Title: Tolterodine  
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Collection: Muscarinic Antagonists, Pfizer, Phenols
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Tolterodine

Tolterodine
Systematic (IUPAC) name
(R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-methylphenol
Clinical data
Trade names Detrol
AHFS/Drugs.com
MedlinePlus
Pregnancy
category
  • AU: B3
  • US: C (Risk not ruled out)
Legal status
Pharmacokinetic data
Bioavailability 77%
Protein binding Approximately 96.3%.
Biological half-life 1.9-3.7 hours
Identifiers
CAS Registry Number  Y
ATC code G04
PubChem CID:
IUPHAR/BPS
DrugBank  Y
ChemSpider  Y
UNII  Y
KEGG  Y
ChEBI  Y
ChEMBL  Y
Chemical data
Formula C22H31NO
Molecular mass 325.488 g/mol
 Y   

Tolterodine (Detrol, Detrusitol) is an antimuscarinic drug that is used for symptomatic treatment of 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.

Contents

  • Use 1
  • Pharmacology 2
  • Side effects of tolterodine 3
  • References 4
  • External links 5

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,[2] pelvic floor therapy or with drugs that inhibit bladder contractions such as oxybutinin and tolterodine.

Pharmacology

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.

Side effects of tolterodine

Known side effects:

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

Contraindications:

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

References

  1. ^ 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.  
  2. ^ Bladder retraining ichelp.org Interstitial Cystitis Association Accessed July 13, 2012
  3. ^ [2]

External links

  • Detrol - FDA factsheet
  • Tolterodine
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