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| {{drugbox <!-- Drugbox data refers to free base -->
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| | IUPAC_name = 1-azabicyclo[2.2.2]oct-8-yl (1''S'')-1-phenyl-3,4-dihydro-1''H''-isoquinoline-2-carboxylate
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| | image = 220px-Solifenacin svg.png
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| | CAS_number = 242478-38-2
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| | ATC_prefix = G04
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| | ATC_suffix = BD08
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| | ATC_supplemental =
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| | PubChem = 443937
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| | DrugBank = APRD00168
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| | C = 23 | H = 26 | N = 2 | O = 2
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| | molecular_weight = 362.465 g/mol
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| | bioavailability = 90%
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| | protein_bound = 98%
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| | metabolism = [[Liver|Hepatic]] ([[CYP3A4]]-mediated)
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| | elimination_half-life = 45 to 68 hours
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| | excretion = [[Kidney|Renal]] (69.2%) and fecal (22.5%)
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| | licence_US = Solifenacin
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| | pregnancy_AU = B3
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| | pregnancy_US = C
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| | legal_AU = <!-- Unscheduled / S2 / S4 / S8 -->
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| | legal_UK = <!-- GSL / P / POM / CD -->
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| | legal_US = Rx-only
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| | routes_of_administration = Oral
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| }}
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| {{SI}}
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| {{CMG}}
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| ==Overview==
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| '''Solifenacin''' ([[International Nonproprietary Name|rINN]]), marketed as '''solifenacin [[succinate]]''' under the trade name '''Vesicare''', is a [[urinary]] [[antispasmodic]] of the [[anticholinergic]] class. It is used in the treatment of [[overactive bladder]] with or without [[urinary incontinence#Urge incontinence|urge incontinence]].
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| ==Pharmacology==
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| ===Mechanism of action===
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| Solifenacin is a [[competitive antagonist|competitive]] [[muscarinic acetylcholine receptor]] [[receptor antagonist|antagonist]]. The binding of [[acetylcholine]] to these receptors, particularly the M<sub>3</sub> receptor subtype, plays a critical role in the contraction of [[smooth muscle]]. By preventing the binding of acetylcholine to these receptors, solifenacin reduces smooth muscle [[muscle tone|tone]] in the [[urinary bladder|bladder]], allowing the bladder to retain larger volumes of urine and reducing the number of micturition, urgency and incontinence episodes. Thanks to a long elimination half life, once-a-day dose can offer 24 hour control of the [[urinary bladder]] [[smooth muscle]] tone.
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| ==Contraindications==
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| Solifenacin should not be taken by people with a history of previous hypersensitivity to it, [[urinary retention]], gastric retention, uncontrolled or poorly controlled closed-angle [[glaucoma]], or severe liver disease ([[Child-Pugh score|Child-Pugh]] class C).
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| It is also contraindicated in [[long QT syndrome]], as solifenacin,like [[tolterodine]] and [[darifenacin]], binds to [[HERG]] [[Ion channel|channels]] and may prolong the [[QT interval]].
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| ==Interactions==
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| Solifenacin is metabolized in the liver by the [[cytochrome P450 oxidase|cytochrome P450]] enzyme [[CYP3A4]]. When administered concomitantly with drugs that [[enzyme inhibition|inhibit]] CYP3A4, such as [[ketoconazole]], the metabolism of solifenacin is impaired, leading to an increase in its concentration in the body and a reduction in its excretion. The manufacturer recommends that the dosage of solifenacin not exceed 5 mg a day if it is taken with a potent CYP3A4 inhibitor.
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| As stated above, solifenacin may also prolong the [[QT interval]]. Therefore, it should not be administered concomitantly with drugs which also have this effect, such as [[moxifloxacin]] or [[pimozide]].
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| ==Side effects==
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| {{main|Anticholinergic}}
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| The most common [[adverse drug reaction|side effect]]s of solifenacin are [[dry mouth]], blurred vision, and constipation. As all anticholinergics, solifenacin may rarely cause [[hyperthermia|heat prostration]] due to decreased [[perspiration]].
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| ==Pharmacoeconomics==
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| In a study of [[cost-effectiveness]] analysis, the average medical cost per [[overactive bladder]] patient with successful treatment is reported to be lowest for 5 mg solifenacin ($6863 per annum) among [[anticholinergic]] drugs to treat [[overactive bladder]] in the united states (Pharmacotherapy 2006, 26 1694-1702).
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| {{Urologicals}}
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| ==References==
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| {{Reflist|2}}
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| [[Category:Muscarinic antagonists]]
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| [[de:Solifenacin]]
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| {{WH}}
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| {{WikiDoc Sources}}
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