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QuickView for solifenacin (compound)
DrugBank
Identification
| Name: | quinuclidin-3'-yl-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate monosuccinate |
|---|---|
| Name (isomeric): | DB01591 |
| Drug Type: | small molecule |
| Synonyms: |
solifenacin succinate
|
| Brand: | Vesicare, Vesikur |
| Category: | Muscarinic Antagonists, Anti-Incontinence Agents, Antispasmodics |
| CAS number: | 242478-37-1 |
Pharmacology
| Indication: | For the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency. |
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| Pharmacology: | Solifenacin is a competitive muscarinic receptor antagonist. Muscarinic receptors play an important role in several major cholinergically mediated functions, including contractions of urinary bladder smooth muscle and stimulation of salivary secretion. |
| Mechanism of Action: |
Solifenacin is a competitive muscarinic acetylcholine 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 th...
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| Absorption: | The absolute bioavailability of solifenacin is approximately 90%, and plasma concentrations of solifenacin are proportional to the dose administered. |
| Protein binding: | Solifenacin is approximately 98% (in vivo) bound to human plasma proteins, principally to alpha1-acid glycoprotein. |
| Biotransformation: | Solifenacin is extensively metabolized in the liver. The primary pathway for elimination is by way of CYP3A4; however, alternate metabolic pathways exist. The primary metabolic routes of solifenacin are through N-oxidation of the quinuclidin ring and 4R-hydroxylation of tetrahydroisoquinoline ring. One pharmacologically active metabolite (4R-hydroxy solifenacin), occurring at low concentrations and unlikely to contribute significantly to clinical activity, and three pharmacologically inactive metabolites (N-glucuronide and the N-oxide and 4R-hydroxy-N-oxide of solifenacin) have been found in human plasma after oral dosing. |
| Route of elimination: | The primary pathway for elimination is by way of CYP3A4; however, alternate metabolic pathways exist. |
| Half Life: | The elimination half-life of solifenacin following chronic dosing is approximately 45-68 hours. |
| Toxicity: | Overdosage with solifenacin can potentially result in severe anticholinergic effects and should be treated accordingly. The highest solifenacin dose given to human volunteers was a single 100 mg dose. Intolerable anticholinergic side effects (fixed and dilated pupils, blurred vision, failure of heel-to-toe exam, tremors and dry skin) occurred on day 3 in normal volunteers taking 50 mg daily (5 times the maximum recommended therapeutic dose). |
| Affected organisms: | Humans and other mammals |
Interactions
| Drug interaction: |
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Targets
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