Tolterodine

Last updated

Tolterodine
Tolterodine.svg
Clinical data
Trade names Detrol, Detrusitol, others
Other namesPNU-200583E
AHFS/Drugs.com Monograph
MedlinePlus a699026
License data
Pregnancy
category
  • AU:B3
Routes of
administration 		By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability 77%
Protein binding Approximately 96.3%
Elimination half-life 1.9–3.7 hours
Identifiers
  • (S)-2-[3-(Diisopropylamino)-1-phenylpropyl]-4-methylphenol
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.232.068 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C22H31NO
Molar mass 325.496 g·mol−1
3D model (JSmol)
  • Cc1ccc(c(c1)[C@H](CCN(C(C)C)C(C)C)c2ccccc2)O
  • 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 Yes check.svgY
  • Key:OOGJQPCLVADCPB-HXUWFJFHSA-N Yes check.svgY
   (verify)

Tolterodine, sold under the brand name Detrol among others, is a medication used to treat frequent urination, urinary incontinence, or urinary urgency. [5] Effects are seen within an hour. [6] It is taken by mouth. [6] [7]

Contents

Common side effects include headache, dry mouth, constipation, and dizziness. [6] Serious side effects may include angioedema, urinary retention, and QT prolongation. [6] Use in pregnancy and breastfeeding are of unclear safety. [5] [8] It works by blocking muscarinic receptors in the bladder thus decreasing bladder contractions. [6]

Tolterodine was approved for medical use in 1998. [6] It is available as a generic medication. [5] In 2020, it was the 271st most commonly prescribed medication in the United States, with more than 1 million prescriptions. [9] [10]

Medical uses

Detrusor overactivity (DO, contraction of the muscular bladder wall) is the most common form of urinary incontinence (UI) in older adults.[ medical citation needed ] It is characterized by uninhibited bladder contractions causing an uncontrollable urge to void.[ medical citation needed ] Urinary frequency, urge incontinence and nocturnal incontinence occur.[ medical citation needed ] Abnormal bladder contractions that coincide with the urge to void can be measured by urodynamic studies.[ medical citation needed ] Treatment is bladder retraining, [11] [ unreliable medical source? ] pelvic floor therapy or with drugs that inhibit bladder contractions such as oxybutynin and tolterodine.[ medical citation needed ]

Side effects

Known side effects:

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

Tolterodine is not recommended for use in people with myasthenia gravis and angle closure glaucoma.

Pharmacology

Tolterodine acts on M2 and M3 [12] subtypes of muscarinic receptors whereas older antimuscarinic treatments for overactive bladder act more specifically on M3 receptors.[ medical citation needed ]

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.[ medical citation needed ]

Society and culture

Brand names

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

Related Research Articles

<span class="mw-page-title-main">Urinary incontinence</span> Uncontrolled leakage of urine

Urinary incontinence (UI), also known as involuntary urination, is any uncontrolled leakage of urine. It is a common and distressing problem, which may have a large impact on quality of life. It has been identified as an important issue in geriatric health care. The term enuresis is often used to refer to urinary incontinence primarily in children, such as nocturnal enuresis. UI is an example of a stigmatized medical condition, which creates barriers to successful management and makes the problem worse. People may be too embarrassed to seek medical help, and attempt to self-manage the symptom in secrecy from others.

<span class="mw-page-title-main">Benzatropine</span> Medication for movement disorders

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<span class="mw-page-title-main">Dicycloverine</span> Antispasmodic agent

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<span class="mw-page-title-main">Ipratropium bromide</span> Type of anticholinergic

Ipratropium bromide, sold under the trade name Atrovent among others, is a type of anticholinergic medication which opens up the medium and large airways in the lungs. It is used to treat the symptoms of chronic obstructive pulmonary disease and asthma. It is used by inhaler or nebulizer. Onset of action is typically within 15 to 30 minutes and lasts for three to five hours.

Diphenoxylate/atropine, also known as co-phenotrope, is a combination of the medications diphenoxylate and atropine, used to treat diarrhea. It should not be used in those in whom Clostridioides difficile infection is a concern. It is taken by mouth. Onset is typically within an hour.

<span class="mw-page-title-main">Tizanidine</span> Muscle relaxant medication

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<span class="mw-page-title-main">Oxybutynin</span> Bladder medication

Oxybutynin, sold as under the brand names Ditropan among others, is a medication used to treat overactive bladder. It works similar to tolterodine, Darifenacin, and Solifenacin. While used for bed wetting in children, evidence to support this use is poor. It is taken by mouth or applied to the skin.

<span class="mw-page-title-main">Brimonidine</span> Chemical compound

Brimonidine is an α2 agonist medication used to treat open-angle glaucoma, ocular hypertension, and rosacea. In rosacea it improves the redness. It is used as eye drops or applied to the skin.

<span class="mw-page-title-main">Darifenacin</span> Medication for urinary incontinence

Darifenacin is a medication used to treat urinary incontinence due to an overactive bladder. It was discovered by scientists at the Pfizer research site in Sandwich, UK under the identifier UK-88,525 and used to be marketed by Novartis. In 2010, the US rights were sold to Warner Chilcott for US$400 million.

<span class="mw-page-title-main">Propantheline bromide</span> Drug for functional gastrointestinal disorders

Propantheline bromide (INN) is an antimuscarinic agent used for the treatment of excessive sweating (hyperhidrosis), cramps or spasms of the stomach, intestines (gut) or bladder, and involuntary urination (enuresis). It can also be used to control the symptoms of irritable bowel syndrome and similar conditions. This agent can also be used for patients who experience intense GI symptoms while tapering off of TCAs.

<span class="mw-page-title-main">Solifenacin</span> Chemical compound

Solifenacin, sold as the brand name Vesicare among others, is a medicine used to treat overactive bladder and neurogenic detrusor overactivity (NDO). It may help with incontinence, urinary frequency, and urinary urgency.

<span class="mw-page-title-main">Trospium chloride</span> Chemical compound

Trospium chloride is used to treat overactive bladder.

<span class="mw-page-title-main">Overactive bladder</span> Condition where a person has a frequent need to urinate

Overactive bladder (OAB) is a common condition where there is a frequent feeling of needing to urinate to a degree that it negatively affects a person's life. The frequent need to urinate may occur during the day, at night, or both. Loss of bladder control may occur with this condition. Overactive bladder affects approximately 11% of the population and more than 40% of people with overactive bladder have incontinence. Conversely, about 40% to 70% of urinary incontinence is due to overactive bladder. Overactive bladder is not life-threatening, but most people with the condition have problems for years.

<span class="mw-page-title-main">Propiverine</span> Chemical compound

Propiverine is an anticholinergic drug used for the treatment of urinary urgency, frequency and urge incontinence, all symptoms of overactive bladder syndrome. It is a muscarinic antagonist. A modified release preparation is also available, taken once daily.

<span class="mw-page-title-main">Overflow incontinence</span> Medical condition

Overflow incontinence is a concept of urinary incontinence, characterized by the involuntary release of urine from an overfull urinary bladder, often in the absence of any urge to urinate. This condition occurs in people who have a blockage of the bladder outlet, or when the muscle that expels urine from the bladder is too weak to empty the bladder normally. Overflow incontinence may also be a side effect of certain medications.

Mirabegron, sold under the brand name Myrbetriq among others, is a medication used to treat overactive bladder. Its benefits are similar to antimuscarinic medication such as solifenacin or tolterodine. It is taken by mouth.

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Autonomic drugs can either inhibit or enhance the functions of the parasympathetic and sympathetic nervous systems. This type of drug can be used to treat a wide range of diseases, such as glaucoma, asthma, urinary, gastrointestinal and cardiopulmonary disorders.

<span class="mw-page-title-main">Vibegron</span> Medication

Vibegron, sold under the brand name Gemtesa, is a medication for the treatment of overactive bladder. Vibegron is a selective beta-3 adrenergic receptor agonist.

References

  1. ↑ "Detrusitol 1mg film-coated tablets - Summary of Product Characteristics (SmPC)". (emc). 9 March 2021. Retrieved 12 May 2022.
  2. ↑ "Detrol- tolterodine tartrate tablet, film coated". DailyMed. 29 September 2021. Retrieved 12 May 2022.
  3. ↑ "Detrol LA- tolterodine tartrate capsule, extended release". DailyMed. 12 October 2020. Retrieved 12 May 2022.
  4. ↑ "List of nationally authorised medicinal products" (PDF). ema.europa.eu. 5 May 2022. Retrieved 9 November 2023.
  5. 1 2 3 British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 762. ISBN   9780857113382.
  6. 1 2 3 4 5 6 "Tolterodine Tartrate Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 3 March 2019.
  7. ↑ Narain S, Parmar M (January 2021). "Tolterodine". StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing. PMID   32491781.
  8. ↑ "Tolterodine Pregnancy and Breastfeeding Warnings". Drugs.com. Retrieved 3 March 2019.
  9. ↑ "The Top 300 of 2020". ClinCalc. Retrieved 7 October 2022.
  10. ↑ "Tolterodine - Drug Usage Statistics". ClinCalc. Retrieved 7 October 2022.
  11. ↑ "Bladder retraining". Interstitial Cystitis Association. Archived from the original on 28 July 2018. Retrieved 6 June 2018.
  12. ↑ "Tolterodine". DrugBank.
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