Oxytrol - General Information
Oxytrol is 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. It competitively antagonizes the M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor.
Pharmacology of Oxytrol
Oxytrol is an antispasmodic, anticholinergic agent indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency. Oxytrol relaxes bladder smooth muscle. Oxytrol 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.
Oxytrol for patients
Patient should be informed that oxybutynin may produce drowsiness or blurred vision. Alcohal may enhance the drowsiness caused by anticholinergic agents. Fever and heat stroke can occur while anticholinergics are administered in the presence of high environmental temparature. Medication should be taken with the aid of liquids at approximately the same time each day. Patients should not chew, divide, or crush tablets.
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.
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.
Additional information about Oxytrol
Oxytrol Indication: For the treatment of overactive bladder.
Mechanism Of Action: Oxytrol 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).
Drug Interactions: Carbamazepine Oxytrol may cause carbamazepine toxicity
Donepezil Possible antagonism of action
Galantamine Possible antagonism of action
Rivastigmine Possible antagonism of action
Food Interactions: Avoid alcohol.
Take with food.
Generic Name: Oxybutynin
Synonyms: Oxibutinina [Inn-Spanish]; Oxibutyninum; Oxybutynin Base; Oxybutynin Chloride; Oxybutynin Hydrochloride; Oxybutynine [Inn-French]; Oxybutyninum [Inn-Latin]; Oxybutinin
Drug Category: Anticholinergic Agents; Antispasmodics; Genitourinary Smooth Muscle Relaxants
Drug Type: Small Molecule; Approved
Other Brand Names containing Oxybutynin: Ditropan; Ditropan Xl; Oxytrol;
Absorption: Rapidly absorbed from gastrointestinal tract.
Toxicity (Overdose): LD50=1220 mg/kg (Orally in rats, Goldenthal)
Protein Binding: 91%-93%
Biotransformation: Hepatic, primarily by CYP3A4
Half Life: 12.4-13.2 hours
Dosage Forms of Oxytrol: Tablet, extended release Oral
Chemical IUPAC Name: 4-diethylaminobut-2-ynyl 2-cyclohexyl-2-hydroxy-2-phenylacetate
Chemical Formula: C22H31NO3
Oxybutynin on Wikipedia: https://en.wikipedia.org/wiki/Oxybutynin
Organisms Affected: Humans and other mammals