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Oxybutynin

Pronunciation

Pronunciation

(oks i BYOO ti nin)

Index Terms

  • Ditropan
  • Oxybutynin Chloride

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Gel, Transdermal:

Gelnique: 3% (92 g [DSC]) [contains propylene glycol]

Gel, Transdermal, as chloride:

Gelnique: 10% (1 g) [contains alcohol, usp]

Patch Twice Weekly, Transdermal:

Oxytrol: 3.9 mg/24 hr (1 ea, 2 ea, 4 ea, 8 ea)

Oxytrol For Women: 3.9 mg/24 hr (4 ea, 8 ea)

Syrup, Oral, as chloride:

Generic: 5 mg/5 mL (5 mL [DSC], 473 mL)

Tablet, Oral, as chloride:

Generic: 5 mg

Tablet Extended Release 24 Hour, Oral, as chloride:

Ditropan XL: 5 mg, 10 mg, 15 mg [contains polysorbate 80]

Generic: 5 mg, 10 mg, 15 mg

Brand Names: U.S.

  • Ditropan XL
  • Gelnique
  • Oxytrol
  • Oxytrol For Women [OTC]

Pharmacologic Category

  • Antispasmodic Agent, Urinary

Pharmacology

Direct antispasmodic effect on smooth muscle, also inhibits the action of acetylcholine on smooth muscle (exhibits 1/5 the anticholinergic activity of atropine, but has 4-10 times the antispasmodic activity); does not block effects at skeletal muscle or at autonomic ganglia; increases bladder capacity, decreases uninhibited contractions, and delays desire to void, therefore, decreases urgency and frequency

Absorption

Oral: Rapid and well absorbed; Transdermal: High

Distribution

IV: Vd: 193 L

Metabolism

Hepatic via CYP3A4; Oral: High first-pass metabolism; forms active and inactive metabolites

Excretion

Urine, as metabolites and unchanged drug (<0.1%)

Onset of Action

Oral: Immediate release: 30 to 60 minutes; Peak effect: 3 to 6 hours; Extended release: Peak effect: 3 days

Time to Peak

Serum: Oral: Immediate release: ~60 minutes; Extended release: 4 to 6 hours; Transdermal: 24 to 48 hours

Duration of Action

Oral: Immediate release: 6 to 10 hours; Extended release: Up to 24 hours; Transdermal 96 hours

Half-Life Elimination

IV: ~2 hours (parent drug), 7 to 8 hours (metabolites); Oral: Immediate release: ~2 to 3 hours; Extended release: ~13 hours; Transdermal: 30 to 64 hours

Protein Binding

>99% primarily to alpha1-acid glycoprotein

Use: Labeled Indications

Treatment of symptoms associated with overactive uninhibited neurogenic or reflex neurogenic bladder (eg, urgency, frequency, leakage, urge incontinence, dysuria); treatment of symptoms associated with detrusor overactivity due to a neurological condition (eg, spina bifida) (extended release tablet only)

Contraindications

Hypersensitivity to oxybutynin or any component of the formulation; patients with or at risk for uncontrolled narrow-angle glaucoma, urinary retention, gastric retention or conditions with severely decreased GI motility

OTC labeling: When used for self-medication, do not use if you have pain or burning when urinating, blood in urine, unexplained lower back or side pain, cloudy or foul-smelling urine; in males; age <18 years; only experience accidental urine loss when cough, sneeze, or laugh; diagnosis of urinary or gastric retention; glaucoma; hypersensitivity to oxybutynin.

Dosing: Adult

Overactive bladder:

Oral:

Immediate release: 5 mg 2 to 3 times daily; maximum: 5 mg 4 times daily

Extended release: Initial: 5 to 10 mg once daily, adjust dose in 5 mg increments at weekly intervals; maximum: 30 mg once daily

Topical gel:

Gelnique 3%: Apply 3 pumps (84 mg) once daily

Gelnique 10%: Apply contents of 1 sachet (100 mg/g) once daily

Transdermal: Apply one 3.9 mg/day patch twice weekly (every 3 to 4 days)

Dosing: Geriatric

Oral: Immediate release: Initial: 2.5 mg 2 to 3 times daily; increase cautiously

Topical gel, transdermal patch: Refer to adult dosing.

Dosing: Pediatric

Neurogenic/Overactive bladder: Oral:

Immediate release: Children: >5 years and Adolescents: 5 mg twice daily; maximum: 5 mg 3 times daily

Extended release: Children ≥6 years and Adolescents: 5 mg once daily; adjust dose as needed in 5 mg increments at weekly intervals; maximum: 20 mg once daily

Dosing: Renal Impairment

No dosage adjustment provided in the manufacturer’s labeling (not studied); use with caution.

Dosing: Hepatic Impairment

No dosage adjustment provided in the manufacturer’s labeling (not studied); use with caution.

Administration

Oral: Administer without regard to meals. Extended release tablets must be swallowed whole with liquid; do not crush, divide, or chew; take at approximately the same time each day.

Topical gel: For topical use only. Apply to clean, dry, intact skin on abdomen, thighs, or upper arms/shoulders. Wash hands after use. Cover treated area with clothing after gel has dried to prevent transfer of medication to others. Do not bathe, shower, or swim until 1 hour after gel applied. Do not apply to recently shaved skin.

Gelnique 3%: Prior to initial use, press pump 4 times to prime pump; discard any gel dispensed from pump during priming. Rotate application sites to avoid skin irritation.

Gelnique 10%: Rotate site; do not apply to same site on consecutive days.

Transdermal: Apply to clean, dry skin on abdomen, hip, or buttock. Select a new site for each new system (avoid reapplication to same site within 7 days). Wear patch under clothing; do not expose to sunlight.

Dietary Considerations

Food causes a slight delay in the absorption of the oral solution and bioavailability is increased by ~25%. Absorption of the extended release tablet is not affected by food. May be taken without regard to meals.

Storage

Immediate release tablet and syrup: Store at 20°C to 25°C (68°F to 77°F). Protect from light.

Extended release tablet: Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Protect from moisture and humidity.

Topical gel (pump or sachets): Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Protect from moisture and humidity. Keep gel away from open flame. Do not store sachets outside the sealed pouch; apply immediately after removal from the protective pouch. Discard used sachets such that accidental application or ingestion by children, pets, or others is avoided.

Transdermal patch: Store at 20°C to 25°C (68°F to 77°F). Protect from moisture and humidity. Do not store outside the sealed pouch; apply immediately after removal from the protective pouch. Discard used patches such that accidental application or ingestion by children, pets, or others is avoided.

Drug Interactions

AbobotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of AbobotulinumtoxinA. Monitor therapy

Acetylcholinesterase Inhibitors: Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Acetylcholinesterase Inhibitors may diminish the therapeutic effect of Anticholinergic Agents. Monitor therapy

Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Alcohol (Ethyl): May enhance the CNS depressant effect of Oxybutynin. Monitor therapy

Amodiaquine: CYP2C8 Inhibitors may increase the serum concentration of Amodiaquine. Avoid combination

Analgesics (Opioid): Anticholinergic Agents may enhance the adverse/toxic effect of Analgesics (Opioid). Specifically, the risk for constipation and urinary retention may be increased with this combination. Monitor therapy

Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Monitor therapy

Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products. Exceptions: Cannabidiol. Monitor therapy

Chloral Betaine: May enhance the adverse/toxic effect of Anticholinergic Agents. Monitor therapy

Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Avoid combination

CYP3A4 Inhibitors (Strong): May increase the serum concentration of Oxybutynin. Monitor therapy

Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Avoid combination

Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Monitor therapy

Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Avoid combination

Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Avoid combination

Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Monitor therapy

Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Avoid combination

Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Monitor therapy

Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Monitor therapy

Nitroglycerin: Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption. Avoid combination

OnabotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of OnabotulinumtoxinA. Monitor therapy

Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. Avoid combination

Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Consider therapy modification

Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Monitor therapy

RimabotulinumtoxinB: Anticholinergic Agents may enhance the anticholinergic effect of RimabotulinumtoxinB. Monitor therapy

Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid using drugs with substantial anticholinergic effects in patients receiving secretin whenever possible. If such agents must be used in combination, monitor closely for a diminished response to secretin. Consider therapy modification

Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Monitor therapy

Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Avoid combination

Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Monitor therapy

Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Test Interactions

May suppress the wheal and flare reactions to skin test antigens.

Adverse Reactions

Oral:

>10%:

Central nervous system: Dizziness (5% to 17%), drowsiness (6% to 14%)

Gastrointestinal: Xerostomia (35% to 71%; dose related), constipation (9% to 15%), nausea (5% to 12%)

1% to 10%:

Cardiovascular: Cardiac arrhythmia (sinus; 1% to <5%), decreased blood pressure (1% to <5%), edema (1% to <5%), flushing (1% to <5%), hypertension (1% to <5%), palpitations (1% to <5%), peripheral edema (1% to <5%)

Central nervous system: Headache (8%), nervousness (7%), insomnia (3% to 6%), confusion (1% to <5%), falling (1% to 5%), fatigue (1% to <5%), flank pain (1% to <5%), pain (1% to <5%)

Dermatologic: Pruritus (1% to <5%), xeroderma (1% to <5%)

Endocrine & metabolic: Fluid retention (1% to <5%), hyperglycemia (1% to <5%), increased thirst (1% to <5%)

Gastrointestinal: Diarrhea (1% to 8%), dyspepsia (5% to 6%), abdominal pain (1% to <5%), dysphagia (1% to <5%), eructation (1% to <5%), flatulence (1% to <5%), unpleasant taste (1% to <5%), vomiting (1% to <5%), gastroesophageal reflux disease (≤1%)

Genitourinary: Urinary hesitancy (2% to 9%), urinary tract infection (7%), urinary retention (1% to 6%), cystitis (1% to <5%), dysuria (1% to <5%), pollakiuria (1% to <5%)

Infection: Fungal infection (1% to <5%)

Neuromuscular & skeletal: Arthralgia (1% to <5%), back pain (1% to <5%), limb pain (1% to <5%), weakness (1% to <5%)

Ophthalmic: Blurred vision (4% to 10%), eye irritation (1% to <5%), keratoconjunctivitis sicca (1% to <5%), xerophthalmia (3%)

Respiratory: Asthma (1% to <5%), bronchitis (1% to <5%), cough (1% to <5%), dry throat (1% to <5%), hoarseness (1% to <5%), nasal congestion (1% to <5%), dry nose (1% to <5%), nasopharyngitis (1% to <5%), pharyngolaryngeal pain (1% to <5%), sinus congestion (1% to <5%), upper respiratory tract infection (1% to <5%)

Topical gel:

>10%:

Gastrointestinal: Xerostomia (8% to 12%)

Local: Application site reaction (6% to 14%; includes anesthesia, irritation, pain, papules)

1% to 10%:

Central nervous system: Dizziness (3%), fatigue (2%), headache (2%)

Dermatologic: Pruritus (1%)

Gastrointestinal: Constipation (1%)

Genitourinary: Urinary tract infection (7%)

Local: Application site erythema (4%), application site rash (3%), application site pruritus (2% to 3%), application site dermatitis (2%)

Ophthalmic: Blurred vision (<2%), xerophthalmia (<2%)

Respiratory: Nasopharyngitis (3%)

Transdermal:

>10%: Local: Application site pruritus (14% to 17%)

1% to 10%:

Dermatologic: Application site macules (3%)

Gastrointestinal: Xerostomia (4% to 10%), constipation (3%), diarrhea (3%)

Genitourinary: Dysuria (2%)

Local: Application site erythema (6% to 8%), application site vesicles (3%), application site rash (3%)

Ophthalmic: Visual disturbance (3%)

Postmarketing and/or case reports (Limited to important or life-threatening): Anaphylaxis, anorexia, cycloplegia, decreased gastrointestinal motility, glaucoma, hallucination, hypersensitivity reaction, impotence, suppressed lactation, memory impairment, mydriasis, psychotic reaction, prolonged Q-T interval on ECG, seizure, tachycardia

Warnings/Precautions

Concerns related to adverse effects:

• Angioedema/hypersensitivity reactions: May cause hypersensitivity, including anaphylaxis and angioedema. Cases of angioedema involving the face, lips, tongue, and/or larynx have been reported with oral oxybutynin; some cases have occurred after a single dose. Discontinue immediately if tongue, hypopharynx, or larynx is involved; promptly initiate appropriate management.

• CNS effects: Anticholinergics may cause agitation, confusion, drowsiness, dizziness, hallucinations, headache, and/or blurred vision, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). Dose reduction or discontinuation should be considered if CNS effects occur.

• Heat prostration: May increase the risk of heat prostration.

Disease-related concerns:

• Bladder flow obstruction: Use with caution in patients with bladder flow obstruction; may increase the risk of urinary retention.

• Cardiovascular disease: Use with caution in patients with CAD, heart failure, hypertension, and/or cardiac arrhythmias; may exacerbate condition.

• Dementia: Use with caution in patients with dementia treated with cholinesterase inhibitors; may aggravate symptoms of disease.

• Gastrointestinal disorders: Use with caution in patients with decreased GI motility or gastrointestinal obstructive disorders (eg, ulcerative colitis, intestinal atony, pyloric stenosis); may increase the risk of gastric retention. In patients with ulcerative colitis, use may decrease gastric motility to the point of increasing the risk of paralytic ileus or toxic megacolon. Use with caution in patients with gastroesophageal reflux or with medications that may exacerbate esophagitis (eg, bisphosphonates).

• Glaucoma: Use with caution in patients with treated angle-closure glaucoma; may exacerbate condition; use is contraindicated with uncontrolled narrow-angle glaucoma.

• Hepatic impairment: Use with caution in patients with hepatic impairment; due to limited experience.

• Hiatal hernia: Use with caution in patients with hiatal hernia.

• Hyperthyroidism: Use with caution in patients with hyperthyroidism; may exacerbate condition.

• Myasthenia gravis: Use with caution in patients with myasthenia gravis; may exacerbate condition.

• Neuropathy: Use with caution in patients with autonomic neuropathy; may aggravate symptoms of decreased GI motility.

• Parkinson disease: Use with caution in patients with Parkinson disease; may aggravate symptoms of disease.

• Prostatic hyperplasia/urinary stricture: Use with caution in patients with prostatic hyperplasia and/or urinary stricture; may cause urinary retention.

• Renal impairment: Use with caution in patients with renal impairment; due to limited experience.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Dosage form specific issues:

• Extended release formulation: The extended release formulation consists of drug within a nondeformable matrix; following drug release/absorption, the matrix/shell is expelled in the stool. The use of nondeformable products in patients with known stricture/narrowing of the GI tract has been associated with symptoms of obstruction (rare).

• Topical gel: To minimize transferring medication to others, cover treatment area with clothing after gel has dried. Discontinue use if skin irritation occurs. Contains ethanol; do not expose to open flame or smoking until gel has dried.

• Transdermal patch: May contain conducting metal (eg, aluminum); remove patch prior to MRI.

Other warnings/precautions:

• OTC labeling: Other causes of frequent urination (UTI, diabetes, early pregnancy, other serious conditions) may need to be considered prior to use. Patients should contact a health care provider if symptoms do not improve within 2 weeks of initial use or for new or worsening symptoms.

Monitoring Parameters

Incontinence episodes, postvoid residual (PVR)

Pregnancy Risk Factor

B

Pregnancy Considerations

Adverse events were not observed in animal reproduction studies.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience blurred vision, diarrhea, nausea, or dry mouth. Have patient report immediately to prescriber severe dizziness, passing out, confusion, hallucinations, agitation, severe fatigue, mood changes, lack of sweat, severe headache, seizures, painful urination, urinary retention, tachycardia, arrhythmia, fast breathing, severe constipation, severe abdominal pain, severe itching, or severe skin irritation (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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