Oxybutynin (oral)

Oxybutynin (oral)
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Kiran Singh, M.D. [2]

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Overview

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Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Indications

• DITROPAN XL® (oxybutynin chloride) is a muscarinic antagonist indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency.

• DITROPAN XL® is also indicated for the treatment of pediatric patients aged 6 years and older with symptoms of detrusor overactivity associated with a neurological condition (e.g., spina bifida).

Dosage

• The recommended starting dose of DITROPAN XL® is 5 or 10 mg once daily at approximately the same time each day. Dosage may be adjusted in 5-mg increments to achieve a balance of efficacy and tolerability (up to a maximum of 30 mg/day). In general, dosage adjustment may proceed at approximately weekly intervals.

DOSAGE FORMS AND STRENGTHS

• DITROPAN XL® extended-release tablets are available as 5, 10 and 15 mg tablets for oral use:

• 5 mg: Pale yellow, round, tablet with "5 XL" printed on one side with black ink.

• 10 mg: Pink, round, tablet with "10 XL" printed on one side with black ink.

• 15 mg: Gray, round, tablet with "15 XL" printed on one side with black ink.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Oxybutynin (oral) in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Oxybutynin (oral) in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding FDA-Labeled Use of Oxybutynin (oral) in pediatric patients.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Oxybutynin (oral) in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Oxybutynin (oral) in pediatric patients.

Contraindications

• DITROPAN XL® is contraindicated in patients with urinary retention, gastric retention and other severe decreased gastrointestinal motility conditions, uncontrolled narrow-angle glaucoma.

• DITROPAN XL® is also contraindicated in patients who have demonstrated hypersensitivity to the drug substance or other components of the product. There have been reports of hypersensitivity reactions, including anaphylaxis and angiodema.

Warnings

Angioedema

• Angioedema of the face, lips, tongue and/or larynx has been reported with oxybutynin. In some cases, angioedema occurred after the first dose. Angioedema associated with upper airway swelling may be life-threatening. If involvement of the tongue, hypopharynx, or larynx occurs, oxybutynin should be promptly discontinued and appropriate therapy and/or measures necessary to ensure a patent airway should be promptly provided.

Central Nervous System Effects

• Oxybutynin is associated with anticholinergic central nervous system (CNS) effects. A variety of CNS anticholinergic effects have been reported, including hallucinations, agitation, confusion and somnolence. Patients should be monitored for signs of anticholinergic CNS effects, particularly in the first few months after beginning treatment or increasing the dose. Advise patients not to drive or operate heavy machinery until they know how DITROPAN XL® affects them. If a patient experiences anticholinergic CNS effects, dose reduction or drug discontinuation should be considered.

• DITROPAN XL® should be used with caution in patients with preexisting dementia treated with cholinesterase inhibitors due to the risk of aggravation of symptoms.

• DITROPAN XL® should be used with caution in patients with Parkinson's disease due to the risk of aggravation of symptoms.

Worsening of Symptoms of Myasthenia Gravis

• DITROPAN XL® should be used with caution in patients with myasthenia gravis due to the risk of aggravation of symptoms.

Worsening of Symptoms of Decreased Gastrointestinal Motility in Patients with Autonomic Neuropathy

• DITROPAN XL® should be used with caution in patients with autonomic neuropathy due to the risk of aggravation of symptoms of decreased gastrointestinal motility.

Urinary Retention

• DITROPAN XL® should be administered with caution to patients with clinically significant bladder outflow obstruction because of the risk of urinary retention.

Gastrointestinal Adverse Reactions

• DITROPAN XL® should be administered with caution to patients with gastrointestinal obstructive disorders because of the risk of gastric retention.

• DITROPAN XL®, like other anticholinergic drugs, may decrease gastrointestinal motility and should be used with caution in patients with conditions such as ulcerative colitis and intestinal atony.

• DITROPAN XL® should be used with caution in patients who have gastroesophageal reflux and/or who are concurrently taking drugs (such as bisphosphonates) that can cause or exacerbate esophagitis.

• As with any other nondeformable material, caution should be used when administering DITROPAN XL® to patients with preexisting severe gastrointestinal narrowing (pathologic or iatrogenic). There have been rare reports of obstructive symptoms in patients with known strictures in association with the ingestion of other drugs in nondeformable controlled-release formulations.

Adverse Reactions

Clinical Trials Experience

• Because clinical trials are conducted under widely varying conditions, the adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.

• The safety and efficacy of DITROPAN XL® (5 to 30 mg/day) was evaluated in 774 adult subjects who participated in five double-blind, controlled clinical trials. In four of the five studies, Ditropan IR (5 to 20 mg/day in 199 subjects) was an active comparator. Adverse reactions reported by ≥ 1% of subjects are shown in Table 1.

This image is provided by the National Library of Medicine.

• The discontinuation rate due to adverse reactions was 4.4% with DITROPAN XL® compared to 0% with Ditropan IR. The most frequent adverse reaction causing discontinuation of study medication was dry mouth (0.7%).

• The following adverse reactions were reported by <1% of DITROPAN XL®-treated patients and at a higher incidence than placebo in clinical trials:

• Metabolism and Nutrition Disorders: anorexia, fluid retention;

• Vascular disorders: hot flush;

• Respiratory, thoracic and mediastinal disorders: dysphonia;

• Gastrointestinal Disorders: dysphagia, frequent bowel movements;

• General disorders and administration site conditions: chest discomfort, thirst.

Postmarketing Experience

• The following additional adverse reactions have been reported from worldwide postmarketing experience with DITROPAN XL®. Because postmarketing reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

• Psychiatric Disorders: psychotic disorder, agitation, hallucinations, memory impairment;

• Nervous System Disorders: convulsions;

• Eye Disorders: glaucoma;

• Cardiac Disorders: arrhythmia, tachycardia, QT interval prolongation;

• Vascular Disorders: flushing

• Skin and Subcutaneous Tissue Disorders: rash

• Renal and Urinary Disorders: impotence

• General Disorders and Administration Site Conditions: hypersensitivity reactions, including angioedema with airway obstruction, urticaria, and face edema; anaphylactic reactions requiring hospitalization for emergency treatment; Injury, poisoning and procedural complications: fall.

• Additional adverse events reported with some other oxybutynin chloride formulations include: cycloplegia, mydriasis, and suppression of lactation.

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. Anticholinergic agents may also antagonize the effects of prokinetic agents, such as metoclopramide.

• 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.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): There is no FDA guidance on usage of Oxybutynin (oral) in women who are pregnant.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Oxybutynin (oral) in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Oxybutynin (oral) during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Oxybutynin (oral) with respect to nursing mothers.

Pediatric Use

There is no FDA guidance on the use of Oxybutynin (oral) with respect to pediatric patients.

Geriatic Use

There is no FDA guidance on the use of Oxybutynin (oral) with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Oxybutynin (oral) with respect to specific gender populations.

Race

There is no FDA guidance on the use of Oxybutynin (oral) with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Oxybutynin (oral) in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Oxybutynin (oral) in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Oxybutynin (oral) in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Oxybutynin (oral) in patients who are immunocompromised.

Administration and Monitoring

Administration

• Oral

Monitoring

There is limited information regarding Monitoring of Oxybutynin (oral) in the drug label.

IV Compatibility

There is limited information regarding IV Compatibility of Oxybutynin (oral) in the drug label.

Overdosage

• The continuous release of oxybutynin from DITROPAN XL® should be considered in the treatment of overdosage. Patients should be monitored for at least 24 hours. Treatment should be symptomatic and supportive. Activated charcoal as well as a cathartic may be administered.

• Overdosage with oxybutynin chloride has been associated with anticholinergic effects including central nervous system excitation, flushing, fever, dehydration, cardiac arrhythmia, vomiting, and urinary retention.

• Ingestion of 100 mg oxybutynin chloride in association with alcohol has been reported in a 13-year-old boy who experienced memory loss, and a 34-year-old woman who developed stupor, followed by disorientation and agitation on awakening, dilated pupils, dry skin, cardiac arrhythmia, and retention of urine. Both patients fully recovered with symptomatic treatment.

Pharmacology

There is limited information regarding Oxybutynin (oral) Pharmacology in the drug label.

Mechanism of Action

• Oxybutynin relaxes bladder smooth muscle. Oxybutynin chloride 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).

• Antimuscarinic activity resides predominantly in the R-isomer. A metabolite, desethyloxybutynin, has pharmacological activity similar to that of oxybutynin in in vitro studies.

Structure

• DITROPAN XL® (oxybutynin chloride) is an antispasmodic, muscarinic antagonist. Each DITROPAN XL® extended-release tablet contains 5 mg, 10 mg, or 15 mg of oxybutynin chloride USP, formulated as a once-a-day controlled-release tablet for oral administration. Oxybutynin chloride is administered as a racemate of R- and S-enantiomers.

• Chemically, oxybutynin chloride is d,l (racemic) 4-diethylamino-2-butynyl phenylcyclohexylglycolate hydrochloride. The empirical formula of oxybutynin chloride is C22H31NO3•HCl.

• Its structural formula is:

This image is provided by the National Library of Medicine.

• Oxybutynin chloride is a white crystalline solid with a molecular weight of 393.9. It is readily soluble in water and acids, but relatively insoluble in alkalis.

• DITROPAN XL® also contains the following inert ingredients: butylated hydroxytoluene, cellulose acetate, hypromellose, lactose, magnesium stearate, polyethylene glycol, polyethylene oxide, polysorbate 80, propylene glycol, sodium chloride, synthetic iron oxides and titanium dioxide.

System Components and Performance

• DITROPAN XL® uses osmotic pressure to deliver oxybutynin chloride at a controlled rate over approximately 24 hours. The system, which resembles a conventional tablet in appearance, comprises an osmotically active bilayer core surrounded by a semipermeable membrane. The bilayer core is composed of a drug layer containing the drug and excipients, and a push layer containing osmotically active components. There is a precision-laser drilled orifice in the semipermeable membrane on the drug-layer side of the tablet. In an aqueous environment, such as the gastrointestinal tract, water permeates through the membrane into the tablet core, causing the drug to go into suspension and the push layer to expand. This expansion pushes the suspended drug out through the orifice. The semipermeable membrane controls the rate at which water permeates into the tablet core, which in turn controls the rate of drug delivery. The controlled rate of drug delivery into the gastrointestinal lumen is thus independent of pH or gastrointestinal motility. The function of DITROPAN XL® depends on the existence of an osmotic gradient between the contents of the bilayer core and the fluid in the gastrointestinal tract. Since the osmotic gradient remains constant, drug delivery remains essentially constant. The biologically inert components of the tablet remain intact during gastrointestinal transit and are eliminated in the feces as an insoluble shell.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Oxybutynin (oral) in the drug label.

Pharmacokinetics

There is limited information regarding Pharmacokinetics of Oxybutynin (oral) in the drug label.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of Oxybutynin (oral) in the drug label.

Clinical Studies

There is limited information regarding Clinical Studies of Oxybutynin (oral) in the drug label.

How Supplied

Storage

There is limited information regarding Oxybutynin (oral) Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Patient Counseling Information of Oxybutynin (oral) in the drug label.

Precautions with Alcohol

• Alcohol-Oxybutynin (oral) interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

• DITROPAN XL®

Look-Alike Drug Names

• A® — B®

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

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