Oxytrol
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Oxytrol
OxybutyninSystematic (IUPAC) name4-Diethylaminobut- 2-ynyl2- cyclohexyl-2- hydroxy-2-phenyl-ethanoateIdentifiersCAS number5633-20-5ATC codeG04BD04PubChem4634DrugBankAPRD00427Chemical dataFormulaC22H31NO3 Mol. mass357.486 g/molSMILESeMolecules & PubChemPharmacokinetic dataBioavailability ?Protein binding91%-93%Metabolism ?Half life12.4-13.2 hoursExcretion ?Therapeutic considerationsPregnancy cat.BLegal statusRoutesoral, transdermalOxybutynin is an anticholinergic medication used to relieve urinary and bladder difficulties, including frequent urination and inability to control urination (urge incontinence), by decreasing muscle spasms of the bladder. It competitively antagonizes the M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor. It also has direct spasmolytic effects on bladder smooth muscle as a calcium antagonist and local anesthetic, but at concentrations far above those used clinically. It is available orally in generic formulation and as the brand-names Ditropan and Lyrinel XL, and as a transdermal patch under the brand-name Oxytrol. Also Ditrospam by Avenzor SyriaOxybutynin is also a possible treatment of hyperhidrosis, or hyper-active sweating.// ChemistryOxybutynin 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 the 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. Adverse effectsCommon adverse effects associated with oxybutynin and other anticholinergics include: dry mouth, difficulty in micturition, constipation, blurred vision, drowsiness and dizziness. Anticholinergics have also been known to induce delirium. 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 due to side effects. Dry mouth may be particularly severe; one estimate is that over a quarter of patients who begin oxybutynin treatment may have to stop because of dry mouth.N-Desethyloxybutynin is an active metabolite of oxybutynin that is thought to be responsible for much of the adverse effects associated with the use of oxybutynin. N-Desethyloxybutynin plasma levels may reach as much as six times that of the parent drug after administration of the immediate-release oral formulation. Alternative dosage forms have been developed in an effort to reduce blood levels of N-desethyloxybutynin and allow for a more steady concentration of oxybutynin to be achieved than is possible with the immediate release form. The long-acting formulations also allow once-daily administration instead of the twice-daily doseage required with the immediate-release form. The transdermal patch, in addition to the benefits of the extended-release oral formulations, bypasses the first-pass hepatic effect that the oral formulations are subject to. Clinical pharmacologyOxybutynin 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). ContraindicationsThis section does not cite any references or sources.Please help improve this section by adding citations to reliable sources. Unverifiable material may be challenged and removed. (December 2007)Oxybutynin chloride is contraindicated in patients with untreated angle closure 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, 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.
, September 3, 2002 — Watson Pharmaceuticals announced that on August 30 it had resubmitted a New Drug Application (NDA) to the FDA for Oxytrol (oxybutynin transdermal system), the company’s transdermal oxybutynin therapy for which Watson is seeking an indication for the treatment of overactive bladder with symptoms of urge incontinence,.CORONA,
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Oxytrol
Questions About Overactive Bladder (OAB) How many people are affected by OAB? How many people use OAB medications? How do OAB medications work? Questions about OXYTROL
OXYTROL: Frequently Asked Questions
What is OXYTROL? OXYTROL is the first and only transdermal system (skin patch) to treat overactive bladder (OAB). OXYTROL's transdermal ...
OXYTROL: About OXYTROL
Oxytrol (oxybutynin) reduces muscle spasms of the bladder and urinary tract. Includes Oxytrol side effects, interactions and indications.
Oxytrol Information from Drugs.com
Oxytrol. DRUG CLASS AND MECHANISM: Oxybutynin is a drug for treating bladder spasms. Oxybutynin has a dual mechanism of action. Contraction of the smooth muscle of the bladder is ...
oxybutynin - Health and Medical Information Produced by Doctors ...
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