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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.
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:
ClarithromycinThis potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolism
KetoconazoleThis potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolism
NefazodoneThis potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolism
NelfinavirThis potent CYP3A4 inhibitor slows darifenacin / solifenacin metabolism
GalantaminePossible antagonism of action
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Enzymes