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Active ingredient: Oxybutynin - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Anticholinergic Agents
  • Antispasmodics
  • Genitourinary Smooth Muscle Relaxants

Dosage Forms

  • Patch
  • Syrup
  • Tablet
  • Tablet (extended-release)

Brands / Synonyms

Ditropan; Ditropan XL; Oxibutinina [Inn-Spanish]; Oxibutyninum; Oxybutinin; Oxybutynin; Oxybutynin Base; Oxybutynin Chloride; Oxybutynin Hydrochloride; Oxybutynine [Inn-French]; Oxybutyninum [Inn-Latin]; Oxytrol


For the treatment of overactive bladder.


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 antispasmodic activity. Antimuscarinic activity resides predominantly in the R-isomer.

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).


Rapidly absorbed from gastrointestinal tract.


LD50=1220 mg/kg (Orally in rats, Goldenthal)

Biotrnasformation / Drug Metabolism

Hepatic, primarily by CYP3A4


DITROPAN XL® is contraindicated in patients with urinary retention, gastric retention and other severe decreased gastrointestinal motility conditions, uncontrolled narrow-angle glaucoma and in patients who are at risk for these conditions.

DITROPAN XL is also contraindicated in patients who have demonstrated hypersensitivity to the drug substance or other components of the product.

Drug Interactions

The concomitant use of oxybutynin with other anticholinergic drugs or with other agents which produce dry mouth, constipation, somnolence (drowsiness), and/or other anticholinergic-like effects may increase the frequency and/or severity of such effects.

Anticholinergic agents may potentially alter the absorption of some concomitantly administered drugs due to anticholinergic effects on gastrointestinal motility. This may be of concern for drugs with a narrow therapeutic index.

Mean oxybutynin chloride plasma concentrations were approximately 2 fold higher when DITROPAN XL was administered with ketoconazole, a potent CYP3A4 inhibitor. Other inhibitors of the cytochrome P450 3A4 enzyme system, such as antimycotic agents (e.g., itraconazole and miconazole) or macrolide antibiotics (e.g., erythromycin and clarithromycin), may alter oxybutynin mean pharmacokinetic parameters (i.e., Cmax and AUC). The clinical relevance of such potential interactions is not known. Caution should be used when such drugs are co-administered.

Concurrent ingestion of antacid (20 mL of antacid containing aluminum hydroxide, magnesium hydroxide, and simethicone) did not significantly affect the exposure of oxybutynin or desethyloxybutynin.


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