Vesicare Indication:

For the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency.

Vesicare Mechanism Of Action:

Vesicare 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 the bladder to retain larger volumes of urine and reducing the number of incontinence episodes.

Vesicare Drug Interactions:

Not Available

Vesicare Food Interactions:

Not Available

Vesicare Generic Name:

Synonyms:

  • solifenacin succinate

Drug Type:

Small Molecule; Approved

Absorption:

The absolute bioavailability of solifenacin is approximately 90%, and plasma concentrations of solifenacin are proportional to the dose administered.

Toxicity (Overdose):

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).

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.

Half Life:

The elimination half-life of solifenacin following chronic dosing is approximately 45-68 hours.

Dosage Forms of Vesicare:

Tablet Oral

Chemical IUPAC Name:

[(8R)-1-azabicyclo[2.2.2]octan-8-yl] (1S)-1-phenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate; butanedioic acid

Organisms Affected:

Humans and other mammals

Vesicare to general, pharmacology

General, pharmacology..
urinary-tract