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Solifenacin

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Solifenacin

Solifenacin
Systematic (IUPAC) name
1-azabicyclo[2.2.2]oct-3-yl (1R)-1-phenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate
Clinical data
Trade names Vesicare
AHFS/Drugs.com
MedlinePlus
Licence data US FDA:
Pregnancy
category
  • AU: B3
  • US: C (Risk not ruled out)
Legal status
Routes of
administration
Oral
Pharmacokinetic data
Bioavailability 90%
Protein binding 98%
Biological half-life 45 to 68 hours
Excretion Renal (69.2%) and fecal (22.5%)
Identifiers
CAS Registry Number  N
ATC code G04
PubChem CID:
IUPHAR/BPS
DrugBank  YesY
ChemSpider  N
UNII  YesY
ChEMBL  N
Chemical data
Formula C23H26N2O2
Molecular mass 362.465 g/mol
 N   

Solifenacin (INN, trade name Vesicare) is a medicine of the antimuscarinic class and was developed for treating contraction of overactive bladder with[1] urge incontinence. It is manufactured and marketed by Astellas, Teva Pharmaceutical Industries and GlaxoSmithKline

Pharmacology

Mechanism of action

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

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).[2] 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

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.[2]

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

The most common side effects of solifenacin are dry mouth, blurred vision, and constipation. As all anticholinergics, solifenacin may rarely cause hyperthermia due to decreased perspiration.[2]

Pharmacoeconomics

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.[3]

History

The compound was studied using animal models by the Yamanouchi Pharmaceutical Co., Ltd. of Tokyo, Japan. It was known as YM905 when under study in the early 2000s. [4]

References

  1. ^
  2. ^ a b c Retrieved on June 10, 2011.
  3. ^
  4. ^
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