An anticholinergic medication used to relieve urinary and bladder difficulties, including frequent urination and inability to control urination, by decreasing muscle spasms of the bladder.
Competitively antagonizes the M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor.
Has direct spasmolytic effects on bladder smooth muscle as a calcium antagonist and local anesthetic, at concentrations exceeding those used clinically.
It is available orally, as a transdermal patch, and as a topical gel.
Common adverse effects include: dry mouth, difficulty in urination, constipation, blurred vision, drowsiness,
Side effects are dose related and can be severe.
Can induce delirium.
About 50% of patients discontinue the drug due to side effects, with 25% complaining of dry mouth.
N-Desethyloxybutynin is an active metabolite of oxybutynin responsible for many adverse effects.
N-Desethyloxybutynin plasma levels may reach as much as six times that of the parent drug after administration of the immediate-release oral formulation.
Long-acting, once daily forms reduce blood levels of N-desethyloxybutynin and allow for a more steady concentration of oxybutynin to be achieved than is possible.
A transdermal patch form of the drug bypasses the first-pass hepatic effect that the oral formulations are subject to.
May make overflow incontinence worse inmdiabetes or neurological diseases like multiple sclerosis or spinal cord trauma.
Has direct antispasmodic effect on smooth muscle and inhibits the muscarinic action of acetylcholine on smooth muscle.
Has no blocking effects at skeletal neuromuscular junctions or autonomic ganglia.
Absorbed within one hour and has an elimination half-life of 2 to 5 hours.
Suspected to is eliminated through the liver.
Contraindicated in patients with untreated angle closure glaucoma and in patients with untreated narrow anterior chambers, in partial or complete obstruction of the gastrointestinal tract, hiatal hernia, gastroesophageal reflux disease, paralytic ileus, megacolon, toxic megacolon, colitis and myasthenia gravis.
Contraindicated in patients with obstructive uropathy and in patients with unstable cardiovascular status.
Significantly improves hot flashes both in frequency and severity.