出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/08/17 16:55:50」(JST)
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| Systematic (IUPAC) name | |
|---|---|
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1-azabicyclo[2.2.2]oct-3-yl (1R)-1-phenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate
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| Clinical data | |
| Trade names | Vesicare |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a605019 |
| Licence data | US FDA:link |
| Pregnancy category |
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| Legal status |
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| 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 | 242478-37-1 N |
| ATC code | G04BD08 |
| PubChem | CID: 154059 |
| IUPHAR/BPS | 7483 |
| DrugBank | DB01591 Y |
| ChemSpider | 135771 N |
| UNII | A8910SQJ1U Y |
| ChEMBL | CHEMBL1734 N |
| Chemical data | |
| Formula | C23H26N2O2 |
| Molecular mass | 362.465 g/mol |
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| N (what is this?) (verify) | |
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
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.
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.
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.
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]
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]
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]
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| リンク元 | 「ソリフェナシン」 |
| 関連記事 | 「succinate」 |