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Trade names | Detrol, Detrusitol, others |
Other names | PNU-200583E |
AHFS/Drugs.com | Monograph |
MedlinePlus | a699026 |
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Routes of administration | By mouth |
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Pharmacokinetic data | |
Bioavailability | 77% |
Protein binding | Approximately 96.3% |
Elimination half-life | 1.9–3.7 hours |
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ECHA InfoCard | 100.232.068 |
Chemical and physical data | |
Formula | C22H31NO |
Molar mass | 325.496 g·mol−1 |
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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]
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]
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 ]
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.
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 ]
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.
In the US, Detrol is marketed by Viatris after Upjohn was spun off from Pfizer. [13] [14] [15]
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.
Benzatropine (INN), known as benztropine in the United States and Japan, is a medication used to treat movement disorders like parkinsonism and dystonia, as well as extrapyramidal side effects of antipsychotics, including akathisia. It is not useful for tardive dyskinesia. It is taken by mouth or by injection into a vein or muscle. Benefits are seen within two hours and last for up to ten hours.
Ipratropium bromide, sold under the trade name Atrovent among others, is a type of anticholinergic medication which is applied by different routes: inhaler, nebulizer, or nasal spray, for different reasons.
Doxazosin, sold under the brand names Cardura among others, is a medication used to treat symptoms of benign prostatic hyperplasia, hypertension, and posttraumatic stress disorder (PTSD). For high blood pressure, it is a less preferred option. It is taken by mouth.
Percutaneous tibial nerve stimulation (PTNS), also referred to as posterior tibial nerve stimulation, is the least invasive form of neuromodulation used to treat overactive bladder (OAB) and the associated symptoms of urinary urgency, urinary frequency and urge incontinence. These urinary symptoms may also occur with interstitial cystitis and following a radical prostatectomy. Outside the United States, PTNS is also used to treat fecal incontinence.
Oxybutynin, sold under the brand name Ditropan among others, is an anticholinergic medication primarily used to treat overactive bladder. It is widely considered a first-line therapy for overactive bladder due to its well-studied side effect profile, broad applicability, and continued efficacy over long periods of time. It works similar to tolterodine, darifenacin, and solifenacin, although it is usually preferred over these medications. It is sometimes used off-label for treatment of hyperhidrosis, or excessive sweating. It has also been used off-label to treat bed wetting in children, but this use has declined, as it is most likely ineffective in this role. It is taken by mouth or applied to the skin.
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.
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.
Trospium chloride is a muscarinic antagonist used to treat overactive bladder. It has side effects typical of this class of drugs, namely dry mouth, stomach upset, and constipation; these side effects cause problems with people taking their medicine as directed. However it doesn't cause central nervous system side effects like some other muscarinic antagonists. It is in pregnancy category C and is excreted in breast milk.
Diurnal enuresis is daytime wetting. Nocturnal enuresis is nighttime wetting. Enuresis is defined as the involuntary voiding of urine beyond the age of anticipated control. Both of these conditions can occur at the same time, although many children with nighttime wetting will not have wetting during the day. Children with daytime wetting may have frequent urination, have urgent urination or dribble after urinating.
Neurogenic bladder dysfunction, often called by the shortened term neurogenic bladder, refers to urinary bladder problems due to disease or injury of the central nervous system or peripheral nerves involved in the control of urination. There are multiple types of neurogenic bladder depending on the underlying cause and the symptoms. Symptoms include overactive bladder, urinary urgency, frequency, incontinence or difficulty passing urine. A range of diseases or conditions can cause neurogenic bladder including spinal cord injury, multiple sclerosis, stroke, brain injury, spina bifida, peripheral nerve damage, Parkinson's disease, multiple system atrophy or other neurodegenerative diseases. Neurogenic bladder can be diagnosed through a history and physical as well as imaging and more specialized testing. In addition to symptomatic treatment, treatment depends on the nature of the underlying disease and can be managed with behavioral changes, medications, surgeries, or other procedures. The symptoms of neurogenic bladder, especially incontinence, can severely degrade a person's quality of life.
The detrusor muscle, also detrusor urinae muscle, muscularis propria of the urinary bladder and muscularis propria, is smooth muscle found in the wall of the bladder. The detrusor muscle remains relaxed to allow the bladder to store urine, and contracts during urination to release urine. Related are the urethral sphincter muscles which envelop the urethra to control the flow of urine when they contract.
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. This condition is also sometimes characterized by a sudden and involuntary contraction of the bladder muscles, in response to excitement or anticipation. This in turn leads to a frequent and urgent need to urinate.
Fesoterodine is an antimuscarinic drug developed by Schwarz Pharma AG to treat overactive bladder syndrome (OAB). It was approved by the European Medicines Agency in April 2007, the US Food and Drug Administration on October 31, 2008 and Health Canada on February 9, 2012.
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.
Naltalimide (INN) (code name TRK-130, formerly TAK 363) is a novel, centrally-acting opioid drug which is under development by Takeda and Toray for the treatment of overactive bladder/urinary incontinence. It acts as a potent and selective partial agonist of the μ-opioid receptor (Ki = 0.268 nM, EC50 = 2.39 nM, Emax = 66.1%) over the δ-opioid (Ki = 121 nM, EC50 = 26.1 nM, Emax = 71.0%) and κ-opioid receptors (Ki = 8.97 nM, EC50 = 9.51 nM, Emax = 62.6%). Notably, naltalimide somehow appears to lack certain undesirable side effects such as constipation seen with other μ-opioid receptor agonists such as morphine. It enhances bladder storage via suppression of the afferent limb of the micturition reflex pathway.
Serlopitant (INN, codenamed VPD-737) is a drug which acts as an NK1 receptor antagonist. It was assessed in clinical trials for the treatment of urinary incontinence and overactive bladder, but while it was superior to placebo it provided no advantage over existing approved drugs, and was not approved for further development for this indication. Serlopitant is now undergoing clinical trials for the treatment of chronic pruritus (itch)
Autonomic drugs are substances that 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 an disorders, including glaucoma, asthma, and disorders of the urinary, gastrointestinal and circulatory systems.
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.