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Solifenacin

Systematic (IUPAC) name
1-azabicyclo[2.2.2]oct-8-yl (1S)-1-phenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate
Clinical data
Trade names	Vesicare
AHFS/Drugs.com	monograph
MedlinePlus	a605019
Licence data	US FDA:link
Pregnancy cat.	B3 (AU) C (US)
Legal status	POM (UK) ℞-only (US)
Routes	Oral
Pharmacokinetic data
Bioavailability	90%
Protein binding	98%
Half-life	45 to 68 hours
Excretion	Renal (69.2%) and fecal (22.5%)
Identifiers
CAS number	242478-37-1 N
ATC code	G04BD08
PubChem	CID 443938
DrugBank	DB01591
ChemSpider	391992 Y
UNII	A8910SQJ1U Y
ChEMBL	CHEMBL1734 N
Chemical data
Formula	C23H26N2O2
Mol. mass	362.465 g/mol
SMILES O=C(OC2C1CCN(CC1)C2)N5[C@@H](c3ccccc3)c4ccccc4CC5
InChI InChI=1S/C23H26N2O2/c26-23(27-21-16-24-13-10-18(21)11-14-24)25-15-12-17-6-4-5-9-20(17)22(25)19-7-2-1-3-8-19/h1-9,18,21-22H,10-16H2/t21?,22-/m0/s1 Y Key:FBOUYBDGKBSUES-KEKNWZKVSA-N Y
N (what is this?)  (verify)

Solifenacin (INN, trade name Vesicare) is a urinary antispasmodic of the antimuscarinic class. It is used in the treatment of overactive bladder with or without urge incontinence. It is manufactured and marketed by Astellas.

Pharmacology [edit]

Mechanism of action [edit]

Solifenacin is a competitive cholinergic receptor antagonist. The binding of acetylcholine to these receptors, particularly the M₃ 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 tone in the bladder, allowing the bladder to retain larger volumes of urine and reducing the number of micturition, urgency and incontinence episodes. Because of a long elimination half life, a once-a-day dose can offer 24 hour control of the urinary bladder smooth muscle tone.

Contraindications [edit]

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 class C).^[1] It is also contraindicated in long QT syndrome, as solifenacin, like tolterodine and darifenacin, binds to HERG channels and may prolong the QT interval.

Medical uses [edit]

Solifenacin is metabolized in the liver by the cytochrome P450 enzyme CYP3A4. When administered concomitantly with drugs that 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.^[1]

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.

Side effects [edit]

The most common side effects of solifenacin are dry mouth, blurred vision, and constipation. As all anticholinergics, solifenacin may rarely cause heat prostration due to decreased perspiration.^[1]

Pharmacoeconomics [edit]

A 2006 cost-effectiveness study found that 5 mg solifenacin had the lowest cost and highest effectiveness among anticholinergic drugs used to treat overactive bladder in the United States, with an average medical cost per successfully treated patient of $6863 per year.^[2]

References [edit]