Trade Names:Ditropan- Tablets 5 mg- Syrup 5 mg/5 mL
Trade Names:Ditropan XL- Tablets, ER 5 mg- Tablets, ER 10 mg- Tablets, ER 15 mg
Trade Names:Gelnique- Gel 10%
Trade Names:Oxytrol- Transdermal system, topical 36 mg of oxybutynin delivering 3.9 mg of oxybutynin/day.Apo-Oxybutynin (Canada)Gen-Oxybutynin (Canada)Nu-Oxybutynin (Canada)PMS-Oxybutynin (Canada)Uromax (Canada)
Increases bladder capacity, diminishes frequency of uninhibited contractions of detrusor muscle, and delays initial desire to void.
Following oral administration of the oxybutynin 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.Immediate-release tablet and syrup
Rapidly absorbed following oral administration, reaching the C max within 1 h. Bioavailability is approximately 6%.Topical gel
Transported across intact skin into the systemic circulation by passive diffusion across the stratum corneum. Steady-state concentrations are achieved within 7 days of continuous 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.
Plasma concentrations of oxybutynin decline biexponentially following IV or oral administration.
Widely distributed to body tissues. The Vd was estimated to be 193 L after IV administration of oxybutynin chloride 5 mg.
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.
Less than 0.1% excreted unchanged in the urine.
No experience with use in patients with renal function impairment.Hepatic Function Impairment
No experience with use in patients with hepatic function impairment.Elderly
No differences in pharmacokinetics in elderly patients compared with younger patients.Gender
No differences in pharmacokinetics based on gender.Race
Available data suggest that there are no differences in the pharmacokinetics based on race in healthy volunteers. The effect of race on the pharmacokinetics of the topical gel has not been studied.Showering Topical gel
Showering 1 h after application does not affect the overall systemic exposure to oxybutynin.Sunscreen Topical gel
Concurrent application of sunscreen before or after application does not affect systemic exposure to oxybutynin.
Treatment of symptoms of bladder instability associated with voiding in patients with uninhibited and reflex neurogenic bladder (eg, urinary leakage, dysuria) (immediate-release tablet and syrup). Treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency (ER tablet, topical gel, transdermal system); symptoms of detrusor over activity associated with neurological conditions (eg, spina bifida) in children 6 yr of age and older (ER tablet).
Gastric retention; uncontrolled narrow-angle glaucoma; urinary retention; hypersensitivity to any component of the product.ER tablet, immediate-release tablet, and syrup
Other severe decreased GI motility conditions.
PO 5 mg 2 to 3 times daily (max, 5 mg 4 times daily).Children older than 5 yr of age
PO 5 mg twice daily (max, 5 mg 3 times daily).Topical GelAdults
Topical gel Apply contents of 1 sachet once daily to dry, intact skin on the abdomen, upper arms/shoulder, or thighs.ERAdults
PO 5 to 10 mg once daily adjusted in 5 mg increments at weekly intervals (max, 30 mg/day).Children 6 yr of age and older
PO ER 5 mg once daily at approximately the same time. Adjust dose in 5 mg increments to achieve a balance of efficacy and tolerability (max, 20 mg/day).Transdermal systemAdults
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.
Store at 59° to 86° F. Protect from moisture and humidity. Do not store patches outside foil pouch.
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.Inhibitors of CYP3A4 (eg, azole antifungal agents [eg, itraconazole, ketoconazole], macrolide antibiotics [clarithromycin, erythromycin])
Oxybutynin plasma concentrations may be elevated. Coadminister with caution.Phenothiazines (eg, chlorpromazine)
Decreased therapeutic effects of phenothiazines; increased incidence of anticholinergic adverse reactions.Potassium chloride
Arrest or delay of potassium chloride tablet passage through the GI tract as a result of decreased GI motility.
None well documented.
Hypertension, increased BP, palpitations (1% to less than 5%); arrhythmia, tachycardia (postmarketing).Immediate-release tablets and syrup
Decreased and increased BP, palpitations, sinus arrhythmia (1% to 5%); tachycardia (postmarketing).
Somnolence (12%); headache (10%); asthenia (7%); dizziness (6%); confusional state, depression, dysgeusia, fatigue, insomnia, nervousness (1% to less than 5%); agitation, convulsions, hallucinations, psychotic disorder (postmarketing).Immediate-release tablets and syrup
Dizziness (17%); somnolence (14%); headache (8%); nervousness (7%); insomnia (6%); asthenia, confusional state, dysgeusia, fatigue, sinus headache (1% to less than 5%); agitation, convulsions, hallucination, psychotic disorder (postmarketing).Topical gel
Dizziness (3%); fatigue, headache (2%).Transdermal system
Fatigue, headache, somnolence (more than 1%); dizziness (postmarketing).
Dry skin, pruritus (1% to less than 5%); flushing, rash (postmarketing).Immediate-release tablets and syrup
Dry skin, flushing, pruritus (1% to less than 5%); decreased sweating, rash (postmarketing).Topical gel
Pruritus (1%).Transdermal system
Flushing, rash (greater than 1%).
Blurred vision (8%); dry eyes, rhinitis (6%); dry throat, nasal dryness, nasopharyngitis, pharyngolaryngeal pain (1% to less than 5%).Immediate-release tablets and syrup
Blurred vision (10%); dry throat, eye irritation, keratoconjunctivitis sicca, nasal congestion, nasal dryness, nasopharyngitis, pharyngolaryngeal pain (1% to less than 5%); cycloplegia, mydriasis (postmarketing).Topical gel
Nasopharyngitis (3%).Transdermal system
Abnormal vision (3%).
Dry mouth (61%); constipation (13%); diarrhea, nausea (9%); dyspepsia (7%); abdominal pain, flatulence, gastroesophageal reflux disease, loose stools, vomiting (1% to less than 5%).Immediate-release tablets and syrup
Dry mouth (71%); constipation (15%); nausea (12%); dyspepsia (6%); abdominal pain, decreased saliva secretion, diarrhea, dysphagia, eructation, flatulence, loose stools, tongue coating, upper abdominal pain, vomiting (1% to less than 5%); decrease GI motility (postmarketing).Topical gel
Dry mouth (8%); viral gastroenteritis (2%); constipation (1%).Transdermal system
Dry mouth (10%); constipation, diarrhea (3%); abdominal pain, flatulence, nausea (greater than 1%).
Dysuria, UTI (5%); urinary hesitancy, urinary retention (1% to less than 5%); impotence (postmarketing).Immediate-release tablets and syrup
Urinary hesitancy (9%); UTI (7%); urinary retention (6%); dysuria, pollakiuria (1% to less than 5%); impotence, suppression of lactation (postmarketing).Topical gel
UTI (7%).Transdermal system
Application-site reactions including anesthesia, dermatitis, erythema, irritation, pain, papules, and pruritus (5%).Transdermal system
Application-site pruritus (17%); application-site erythema (8%); application-site vesicles (4%); application-site macules, application-site rash (3%); application-site burning (greater than 1%).
Fluid retention, increased blood glucose, thirst (1% to less than 5%).
Arthralgia, back pain, extremity pain (1% to less than 5%).Immediate-release tablets and syrup
Arthralgia, back pain, extremity pain, flank pain (1% to less than 5%).Transdermal system
Back pain (more than 1%).
Bronchitis, cough, sinusitis, upper respiratory tract infection (1% to less than 5%).Immediate-release tablets and syrup
Asthma, bronchitis, cough, hoarseness, sinus congestion, UTI (1% to less than 5%).Topical gel
Upper respiratory tract infection (5%).
Pain (7%); chest pain, cystitis, fall, peripheral edema (1% to less than 5%).Immediate-release tablets and syrup
Cystitis, edema, fall, fungal infections, pain, peripheral edema (1% to less than 5%).
Monitor patients for signs of anticholinergic CNS effects, especially during the first few months of therapy or after dose increases.
Category B .
Safety and efficacy not established in children younger than 5 yr of age.ER
Safety and efficacy not established in children younger than 6 yr of age.Topical gel, transdermal system
Safety and efficacy not established.
Patients developing skin hypersensitivity to oxybutynin topical gel should discontinue treatment.
Use with caution in elderly patients and in patients with renal or hepatic function impairment or autonomic neuropathy. Use with caution in elderly patients, and in patients with hepatic or renal function impairment, GI obstruction, bladder outflow obstruction, ulcerative colitis, intestinal atony, and myasthenia gravis, and in patients with preexisting dementia who are receiving cholinesterase inhibitors.
Use cautiously with phenothiazines or other drugs with anticholinergic properties because adverse reactions will be additive.
May aggravate symptoms of hyperthyroidism, coronary heart disease, CHF, cardiac arrhythmias, tachycardia, hypertension, hiatal hernia, and prostatic hypertrophy.
CNS anticholinergic effects (eg, agitation, confusion, hallucination, somnolence) can occur.
Diarrhea may be an early symptom of intestinal obstruction in which oxybutynin is contraindicated.
The topical gel is alcohol-based and flammable. Patients should avoid open fire or smoking until gel is dry.
Administration to patients with ulcerative colitis may suppress GI motility and produce paralytic ileus, precipitating or aggravating toxic megacolon. Use with caution.
Heat prostration may occur when exposed to high environmental temperature.
Transfer of oxybutynin topical gel to another person can occur when vigorous skin-to-skin contact is made with the application site.
Because risk may be increased, use with caution.
Agitation, cardiac arrhythmia, CNS excitation, coma, dehydration, dilated pupils, disorientation, dry skin, flushing, fever, memory loss, nausea, tachycardia, respiratory depression, stupor, urinary retention, vomiting.
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