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QuickView for Oxybutynin (compound)


PubChem
Name: oxybutynin
PubChem Compound ID: 11349918
Molecular formula: C22H32ClNO3
Molecular weight: 393.947 g/mol
DrugBank
Identification
Name: oxybutynin
Name (isomeric): DB01062
Drug Type: small molecule
Synonyms:
Oxybutyninum [INN-Latin]; transdermal patch; Oxybutinin; oxybutynin topical gel; Oxybutynine [INN-French]; Oxybutynin Hydrochloride; Oxybutynin Chloride; Oxibutinina [INN-Spanish]; Oxybutynin Base; Oxibutyninum
Brand: Ditropan, Ditropan Xl, Oxytrol
Category: Muscarinic Antagonists, Parasympatholytics, Anticholinergic Agents, Antispasmodics, Genitourinary Smooth Muscle Relaxants
CAS number: 5633-20-5
Pharmacology
Indication: For the treatment of overactive bladder.
Pharmacology:
Oxybutynin is an antispasmodic, anticholinergic agent indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency. Oxybutynin relaxes bladder smooth muscle. Oxybutynin exhibits only one-fifth of the anticholinergic activity of atropine on the rabbit detrusor muscle, but four to ten times the ...
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Mechanism of Action:
Oxybutynin exerts a direct antispasmodic effect on smooth muscle and inhibits the muscarinic action of acetylcholine on smooth muscle. No blocking effects occur at skeletal neuromuscular junctions or autonomic ganglia (antinicotinic effects). By inhibiting particularily the M1 and M2 receptors of the bladder, detrusor activity is markedly decreased...
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Absorption: Rapidly absorbed from gastrointestinal tract.
Protein binding: 91%-93%
Biotransformation: Hepatic, primarily by CYP3A4
Route of elimination: Oxybutynin is metabolized primarily by the cytochrome P450 enzyme systems, particularly CYP3A4, found mostly in the liver and gut wall. Oxybutynin is extensively metabolized by the liver, with less than 0.1% of the administered dose excreted unchanged in the urine. Also, less than 0.1% of the administered dose is excreted as the metabolite N-desethyloxybutynin.
Half Life: 12.4-13.2 hours
Toxicity: LD50=1220 mg/kg (Orally in rats, Goldenthal)
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Avoid alcohol.
Take with food.
Drug interaction:
TriprolidineTriprolidine and Oxybutynin, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
DonepezilPossible antagonism of action
TrimethobenzamideTrimethobenzamide and Oxybutynin, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
TrospiumTrospium and Oxybutynin, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
TacrineThe therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Oxybutynin, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
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