A-Z Drug Facts > Oxybutynin Chloride

Oxybutynin Chloride

Pronouncation: (OX-ee-BYOO-tih-nin KLOR-ide)
Class: Anticholinergic

Trade Names:
Ditropan
- Tablets 5 mg
- Syrup 5 mg/5 mL

Trade Names:
Ditropan XL
- Tablets, extended-release 5 mg
- Tablets, extended-release 10 mg
- Tablets, extended-release 15 mg

Trade Names:
Oxytrol
- Transdermal system 36 mg of oxybutynin delivering 3.9 mg of oxybutynin/day.

Apo-Oxybutynin (Canada)
Gen-Oxybutynin (Canada)
Novo-Oxybutynin (Canada)
Nu-Oxybutynin (Canada)
PMS-Oxybutynin (Canada)

Pharmacology

Feedback for Oxybutynin Chloride As a treatment for... Avg User Ratings [?] Overactive Bladder 7.5 2 comments  Rate it! Urinary Incontinence 4.8 0 comments  Rate it! Compare with other drugs.

Increases bladder capacity, diminishes frequency of uninhibited contractions of detrusor muscle and delays initial desire to void.

Pharmacokinetics

Absorption

Extended-release

Following oral administration of the oxybutynin extended-release (ER) tablet, plasma levels rise for 4 to 6 h; thereafter, steady levels are maintained for up to 24 h. Steady-state levels are achieved by day 3 of repeated ER dosing.

Transdermal system

Following application of the first 3.9 mg/day system, plasma levels increase for approximately 24 to 48 h; reaching C _max of 3 to 4 ng/mL.

Distribution

Extended-release

Plasma concentrations of oxybutynin decline biexponentially following IV or oral administration. The Vd is 193 L after IV administration of 5 mg oxybutynin chloride.

Transdermal system

Widely distributed to body tissues. The Vd was estimated to be 193 L after IV administration of 5 mg oxybutynin chloride.

Metabolism

Extensively metabolized by the liver. Primarily by the CYP3A4 isozyme in the liver and gut wall. Transdermal administration bypasses the first-pass GI and hepatic metabolism.

Elimination

Less than 0.1% excreted unchanged in the urine.

Indications and Usage

Treatment of symptoms of bladder instability associated with voiding in patients with uninhibited and reflex neurogenic bladder (eg, urinary leakage, dysuria). Treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency (ER tablet).

Contraindications

Untreated angle-closure glaucoma; untreated narrow anterior chamber angles; GI obstruction; paralytic ileus; intestinal atony of elderly or debilitated patients; toxic megacolon complicating ulcerative colitis; severe colitis; obstructive uropathy; myasthenia gravis; unstable CV status in acute hemorrhage.

Dosage and Administration

Adults Immediate-release tablet or syrup

PO 5 mg 2 to 3 times daily (max, 5 mg 4 times daily).

ER tablets

PO 5 mg once daily adjusted in 5 mg increments at weekly intervals (max, 30 mg/day).

Children older than 5 yr of age

PO 5 mg twice daily (max, 5 mg 3 times daily).

Transdermal system
Adults

Transdermal 3.9 mg/day applied twice/wk (every 3 or 4 days) to dry, intact skin on abdomen, hip, or buttock, selecting a new application site with each system and avoiding using the same site within 7 days.

General Advice

• Transdermal system
• Remove patch from foil pouch, remove plastic strips covering adhesive layer, and immediately apply to dry, intact skin on the abdomen, buttock, or hip.
• Rotate application sites to avoid reapplication to same site within 7 days.
• To discard used patch, fold used patch, place in foil pouch from new patch, and discard in trash.

Storage/Stability

Store tablets in tightly closed container at room temperature. Store patches in foil pouch at controlled room temperature (59° to 86°F). Protect from moisture and humidity. Do not store patches outside foil pouch.

Drug Interactions

Anticholinergic drugs (eg, amantadine)

Increased risk of anticholinergic adverse reactions.

Beta-blockers (eg, atenolol)

Atenolol plasma levels may be elevated, increasing the risk of adverse reactions.

Digoxin

Increased plasma levels of slow-dissolution oral tablets may be increased.

Haloperidol

Worsening of schizophrenic symptoms; tardive dyskinesia; decreased serum haloperidol concentrations, reducing therapeutic effect.

Phenothiazines

Decreased therapeutic effects of phenothiazines; increased incidence of anticholinergic adverse reactions.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Immediate-release tablets and syrup

Palpitations; tachycardia; vasodilation.

ER tablets

Tachycardia, palpitations, vasodilatation, hypertension, palpitation, vasodilation (2% to less than 5%).

CNS

Immediate-release tablets and syrup

Dizziness; drowsiness; hallucinations; insomnia; restlessness.

ER tablets

Somnolence (11.9%); headache (9.8%); dizziness (6.3%); drowsiness, hallucinations, restlessness, insomnia, nervousness, confusion (2% to less than 5%).

Transdermal system

Fatigue; somnolence; headache (more than 1%).

Dermatologic

Immediate-release tablets and syrup

Decreased sweating; rash.

ER tablets

Rash, dry skin (2% to less than 5%).

Transdermal system

Application-site pruritus, erythema, vesicles, rash and macules (2% or more).

EENT

Immediate-release tablets and syrup

Amblyopia; cycloplegia; decreased lacrimation; mydriasis.

ER tablets

Blurred vision (7.7%); dry eyes (6.1%); decreased lacrimation; mydriasis; amblyopia; cycloplegia; rhinitis; sinusitis; dry nasal and sinus mucous membranes; pharyngitis.

Transdermal system

Abnormal vision (2% or more).

GI

Immediate-release tablets and syrup

Constipation; decreased GI motility; dry mouth; nausea.

ER tablets

Dry mouth (60.8%); constipation (13.1%); diarrhea (9.1%); nausea (8.9%); dyspepsia (6.8%); vomiting, decreased GI motility, flatulence, gastroesophageal reflux (2% to less than 5%).

Transdermal system

Dry mouth, diarrhea, constipation (2% or more); abdominal pain, nausea, flatulence (more than 1%).

Genitourinary

Immediate-release tablets and syrup

Urinary retention and hesitancy.

ER tablets

Impotence, UTI, increased postvoid residual volume, cystitis (2% to less than 5%).

Transdermal system

Dysuria (2% or more).

Respiratory

ER tablets

Upper respiratory tract infection, cough, bronchitis (2% to less than 5%).

Miscellaneous

Immediate-release tablets and syrup

Asthenia; impotence; suppression of lactation.

ER tablets

Asthenia, pain (6.8%); rhinitis (5.6%); UTI (5.1%); decreased sweating, suppression of lactation, abdominal pain, accidental injury, back pain, flu-like syndrome, arthritis (2% to less than 5%).

Transdermal system

Flushing, back pain, application-site burning (more than 1%).

Precautions

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy in children younger than 5 yr of age not established.

Special Risk Patients

Use with caution in the elderly and in patients with renal or hepatic function impairment or autonomic neuropathy.

Anticholinergic effects

Use cautiously with phenothiazines or other drugs with anticholinergic properties because adverse reactions will be additive.

Cardiac and other effects

May aggravate symptoms of hyperthyroidism, coronary heart disease, CHF, cardiac arrhythmias, tachycardia, hypertension, hiatal hernia, and prostatic hypertrophy.

Diarrhea

Diarrhea may be an early symptom of intestinal obstruction in which oxybutynin is contraindicated.

GI disorders

Administration to patients with ulcerative colitis may suppress GI motility and produce paralytic ileus, precipitating or aggravating toxic megacolon.

Heat prostration

Heat prostration may occur when exposed to high environmental temperature.

Urinary retention

Because risk may be increased, use with caution.

Overdosage

Symptoms

CNS excitation, flushing, fever, tachycardia, nausea, respiratory depression, coma.

Patient Information

• Instruct patient to take sips of water frequently, suck on ice chips or sugarless hard candy, or chew sugarless gum if dry mouth occurs.
• Teach patient to use bladder massage to empty bladder.
• Advise patient to use caution in hot weather to reduce risk of heat stroke.
• Advise patient that drug may cause drowsiness or dizziness, and to use caution while driving or performing other tasks requiring mental alertness.
• Advise patient to take oxybutynin ER tablet whole with liquids and not to chew, divide, or crush.
• Inform patient not to be concerned if noticing a tablet in the stool; the tablet shell is eliminated from the body but the drug is released from the tablet at a controlled rate.

• Transdermal system
• Advise patient to review the patient information leaflet that comes with each prescription before using the first time and with each refill.
• Ensure that patient understands how to store, apply, and discard patches.
• Advise patient that new patch is applied twice/wk (eg, every 3 to 4 days) and to rotate application sites to avoid reapplication to the same site within 7 days.
• Advise patient that if patch comes off before scheduled replacement, to discard and apply new patch to new application site and establish new reapplication schedule.
• Advise patient to notify health care provider if application-site reactions occur and are bothersome or occur with each application.

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