Solifenacin
Clinical data | |
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Trade names | Vesicare, Vesicare LS |
Other names | YM905 |
AHFS/Drugs.com | Monograph |
MedlinePlus | a605019 |
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Routes of administration | By mouth |
ATC code | |
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Pharmacokinetic data | |
Bioavailability | 90% |
Protein binding | 98% |
Metabolism | CYP3A4 |
Metabolites | Glucuronide, N-oxide, others |
Elimination half-life | 45 to 68 hours |
Excretion | Kidney (69.2%) and fecal (22.5%) |
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Solifenacin, sold as the brand name Vesicare
Benefits appear similar to other medications in the class.[4] It is taken by mouth.[1]
Common side effects include dry mouth, constipation, and
Solifenacin was approved for medical use in the United States in 2004.[1][2][5] In 2021, it was the 228th most commonly prescribed medication in the United States, with more than 1 million prescriptions.[6][7]
Medical use
It is used to treat
Benefits appear similar to other antimuscarinics such as oxybutynin, tolterodine, and darifenacin.[4]
It is also used to treat neurogenic detrusor overactivity (NDO), a form of bladder dysfunction related to neurological impairment, in children ages two years and older.[2] NDO is a dysfunction of the bladder that results from disease or injury in the nervous system.[2] NDO may be related to congenital conditions (often-inherited conditions beginning at or before birth), such as spina bifida (myelomeningocele), or other conditions such as spinal cord injury.[2] With NDO, there is overactivity of the bladder wall muscle, which normally relaxes to allow storage of urine.[2] The bladder wall muscle overactivity results in sporadic bladder muscle contraction, which increases pressure in the bladder and decreases the volume of urine the bladder can hold.[2] If NDO is not treated, increased pressure in the bladder can put the upper urinary tract at risk of harm, including possible permanent damage to the kidneys.[2] In addition, spontaneous bladder muscle contractions can lead to unexpected and frequent leakage of urine with symptoms of urinary urgency (immediate urge to urinate), frequency (urinating more often than normal) and incontinence (loss of bladder control).[2]
Contraindications
Solifenacin is contraindicated for people with
Long QT syndrome is not a contraindication although solifenacin, like tolterodine and darifenacin, binds to hERG channels of the heart and may prolong the QT interval. This mechanism appears to be seldom clinically relevant.[10]
Solifenacin is not to be used in people with gastric retention (reduced emptying of the stomach), uncontrolled narrow angle glaucoma (fluid buildup in the eye which raises eye pressure) or hypersensitivity (allergic reaction) to solifenacin or any of its components.[2] Solifenacin is also not recommended for use in people with severe liver failure, clinically significant bladder outlet obstruction in the absence of clean intermittent catheterization, decreased gastrointestinal motility (slowed intestinal contractions), or at high risk of QT prolongation (an electrical disturbance where the heart muscle takes longer than normal to recharge between beats), including people with a known history of QT prolongation and people taking medications known to prolong the QT interval.[2]
Side effects
The most common
Interactions
Solifenacin is metabolized in the liver by the
As stated above, solifenacin may also prolong the QT interval. Therefore, administering it concomitantly with drugs which also have this effect, such as
Pharmacology
Mechanism of action
Solifenacin is a
Pharmacokinetics
Peak plasma concentrations are reached three to eight hours after absorption from the gut. In the bloodstream, 98% of the substance are bound to
Chemistry
Like other anticholinergics, solifenacin is an
The free base is a yellow oil, while the salt solifenacin
History
The compound was studied using animal models by the
Solifenacin was approved for medical used in the United States in 2004 with an indication to treat overactive bladder in adults 18 years and older.[2][5]
In May 2020, solifenacin was approved for medical use in the United States with an indication to treat neurogenic detrusor overactivity (NDO), a form of bladder dysfunction related to neurological impairment, in children ages two years and older.[2]
The efficacy of solifenacin to treat neurogenic detrusor overactivity (NDO) was established in two clinical trials with a total of 95 pediatric NDO participants, ages two to 17 years old.[2] The studies were designed to measure (as a primary efficacy endpoint) the maximum amount of urine the bladder could hold after 24 weeks of treatment.[2] In the first study, 17 participants ages two to less than five years old were able to hold an average of 39 mL more urine than when the study began.[2] In the second study, 49 participants ages five to 17 years were able to hold an average of 57 mL more urine than when the study began.[2] Reductions in spontaneous bladder contractions, bladder pressure and number of incontinence episodes were also observed in both studies.[2] The approval of Vesicare LS was granted to Astellas Pharma US, Inc.[2]
Society and culture
The INN is solifenacin.
Cost
A 2006
Footnotes
- ^ The name comes from Latin vesica meaning bladder; and care. Thus literally a drug which "takes care of the bladder"
References
- ^ a b c d e f g h i j "Solifenacin Succinate Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists.
- ^ a b c d e f g h i j k l m n o p q r s t u v w x "FDA Approves First Treatment for a Form of Bladder Dysfunction in Pediatric Patients as Young as 2 Years of Age". U.S. Food and Drug Administration (FDA) (Press release). 26 May 2020. Retrieved 26 May 2020. This article incorporates text from this source, which is in the public domain.
- ^ ISBN 9780857113382.
- ^ a b "[93] Are claims for newer drugs for overactive bladder warranted?". Therapeutics Initiative. 22 April 2015. Retrieved 17 March 2019.
- ^ a b "Drug Approval Package: VesiCare (Solifenacin Succinate) NDA #021518". U.S. Food and Drug Administration (FDA). Retrieved 26 May 2020.
- ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
- ^ "Solifenacin - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
- ^ a b c Lexi-Comp (December 2009). "Solifenacin". The Merck Manual Professional. Retrieved 10 June 2011.
- ^ ISBN 978-3-85200-181-4.
- ^ "Vesicare 5mg & 10mg film-coated tablets". eMC. Retrieved 13 December 2015.
- ISBN 978-0-911910-00-1.
- PMID 11488427.
- ^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 47" (PDF). World Health Organization. p. 106. Retrieved 5 February 2017.
- ^ "Teva Introduces Generic of Vesicare to Treat Overactive Bladder". Bloomberg Law. 22 April 2019.
- S2CID 42046036.