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Oxybutynin (brand names Ditropan, Lyrinel XL, Lenditro ( ZA ), Driptane ( RU ), Uripan (Middle East) It is also given to help with symptoms associated with kidney stones.
It competitively antagonizes the M 1, M 2, and M 3 subtypes of the muscarinic acetylcholine receptor. It also has direct spasmolytic effects on bladder smooth muscle as a voltage-gated calcium channel antagonist and local anesthetic, but at concentrations far above those used clinically.
Oxybutynin is also a possible treatment of hyperhidrosis (hyperactive sweating).
Contents
1 Clinical efficacy
2 Adverse effects
3 Clinical pharmacology
4 Contraindications
5 Chemistry
6 Formulations
7 References
8 External links
Clinical efficacy
In two trials of patients with overactive bladder, transdermal oxybutynin 3.9 mg/day decreased the number of incontinence episodes and increased average voided volume to a significantly greater extent than placebo. There was no difference between transdermal oxybutynin and extended-release oral tolterodine.
Adverse effects
Common adverse effects that are associated with oxybutynin and other anticholinergics include: dry mouth, difficulty in urination, constipation, blurred vision, drowsiness, and dizziness.
These are dose-related and sometimes severe. In one population studied—after six months, more than half of the patients had stopped taking the medication because of side effects
Oxybutynin’s tendency to reduce sweating can be dangerous. Reduced sweating increases the risk of heat exhaustion and heat stroke in apparently safe situations where normal sweating keeps others safe and comfortable.
N -Desethyloxybutynin is an active metabolite of oxybutynin that is thought responsible for much of the adverse effects associated with the use of oxybutynin. In those with overflow incontinence because of diabetes or neurological diseases like multiple sclerosis or spinal cord trauma, oxybutynin can worsen overflow incontinence since the fundamental problem is that the bladder is not contracting.
A large study linked the development of Alzheimer’s disease and other forms of dementia in those over 65 to the use of oxybutynin, due to its anticholinergic properties.
Clinical pharmacology
Oxybutynin chloride exerts direct antispasmodic effect on smooth muscle and inhibits the muscarinic action of acetylcholine on smooth muscle. It exhibits one-fifth of the anticholinergic activity of atropine on the rabbit detrusor muscle, but four to ten times the antispasmodic activity. No blocking effects occur at skeletal neuromuscular junctions or autonomic ganglia (antinicotinic effects).
Sources say the drug is absorbed within one hour and has an elimination half-life of 2 to 5 hours.
Contraindications
Oxybutynin chloride is contraindicated in patients with untreated narrow angle glaucoma, and in patients with untreated narrow anterior chamber angles—since anticholinergic drugs may aggravate these conditions. It is also contraindicated in partial or complete obstruction of the gastrointestinal tract, hiatal hernia, gastroesophageal reflux disease, paralytic ileus, intestinal atony of the elderly or debilitated patient, megacolon, toxic megacolon complicating ulcerative colitis, severe colitis, and myasthenia gravis. It is contraindicated in patients with obstructive uropathy and in patients with unstable cardiovascular status in acute hemorrhage. Oxybutynin chloride is contraindicated in patients who have demonstrated hypersensitivity to the product.
Chemistry
Oxybutynin contains one stereocenter. Commercial formulations are sold as the racemate. The ( R )-enantiomer is a more potent anticholinergic than either the racemate or the ( S )-enantiomer, which is essentially without anticholinergic activity at doses used in clinical practice. However, ( R )-oxybutynin administered alone offers little or no clinical benefit above and beyond the racemic mixture. The other actions (calcium antagonism, local anesthesia) of oxybutynin are not stereospecific. ( S )-Oxybutynin has not been clinically tested for its spasmolytic effects, but may be clinically useful for the same indications as the racemate, without the unpleasant anticholinergic side effects.
Enantiomers of oxybutynin
CAS-Number: 119618-21-2
CAS-Number: 119618-22-3
Formulations
Oxybutynin is available orally in generic formulation or as the brand-names Ditropan, Lyrinel XL, or Ditrospam, as a transdermal patch under the brand name Oxytrol, and as a topical gel under the brand name Gelnique.

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