Dosing and uses of Ditropan XL (oxybutynin)
Adult dosage forms and strengths
tablet
- 5mg
tablet, extended-release
- 5mg
- 10mg
- 15mg
syrup
- 5mg/5mL
Overactive Bladder
Relief of symptoms (eg, urge incontinence, frequency, urgency) in patients with uninhibited neurogenic or reflex neurogenic bladder
Immediate-release: 5 mg PO twice/three times daily; not to exceed 5 mg PO four times daily
Extended-release: 5-10 mg/day PO; may be increased by 5 mg/day at weekly intervals; not to exceed 30 mg/day
Dose Modifications
Renal Impairment
- Not studied; use caution
Hepatic Impairment
- Not studied; use caution
Pediatric dosage forms and strengths
tablet
- 5mg
tablet, extended-release
- 5mg
- 10mg
- 15mg
syrup
- 5mg/5mL
Detrusor Overactivity
Bladder overactivity associated with a neurologic condition (eg, spina bifida)
≥5 years (immediate-release): 5 mg PO q12hr; may be increased to 5 mg PO q8hr
≥6 years (extended-release): 5 mg/day PO initially; may be increased by 5 mg/day at weekly intervals; not to exceed 20 mg/day
Geriatric dosage forms and strengths
Overactive Bladder
Relief of symptoms (eg, urge incontinence, frequency, urgency) in patients with uninhibited neurogenic or reflex neurogenic bladder
Immediate-release: Initiate at lower dosage in frail elderly; 2.5 mg PO q8-12hr initially; may be increased to 5 mg q8-12hr if warranted
Extended-release: 5-10 mg PO qDay; pharmacokinetics similar to adults in elderly up to age 78 yr
Ditropan XL (oxybutynin) adverse (side) effects
>10%
Dry mouth (21-71%)
Constipation (7-15%)
Somnolence (2-14%)
Nausea (2-12%)
1-10%
Asthenia (6-10%)
Dizziness (6-10%)
Headache (6-10%)
Blurred vision (6-10%)
Dry eyes (6-10%)
Diarrhea (6-10%)
Nausea (6-10%)
Pain (6-10%)
Rhinitis (6-10%)
<1%
Anorexia
Fluid retention
Hot flush
Dysphonia
Dysphagia
Frequent bowel movements
Chest discomfort
Thirst
Frequency not defined
Cycloplegia
Impairment of mental alertness
Memory impairment
Mydriasis
Tachycardia
QT prolongation
Postmarketing reports
Hallucinations
Confusion
Urinary tract infection
Palpitations
Nasal congestion
Hypertension
Warnings
Contraindications
Hypersensitivity
Gastric or urinary obstruction or retention, paralytic ileus, severe ulcerative colitis
Uncontrolled narrow-angle glaucoma
Relative contraindications: Myasthenia gravis, tachycardia secondary to cardiac insufficiency or thyrotoxicosis
Cautions
Caution in controlled angle-closure glaucoma; mild-to-moderate ulcerative colitis, hyperthyroidism; partial obstructive uropathy; benign prostatic hyperplasia
Caution in hepatic or renal impairment
May increase risk of heat prostration during hot weather
May cause memory loss
Angioedema necessitating hospitalization and emergency medical treatment has occurred with first or subsequent doses of oral oxybutynin; if angioedema develops, oxybutynin-containing products should be discontinued and appropriate therapy promptly provided
Caution with gastrointestinal obstructive disorders or decreased intestinal motility because of the risk of gastric retention
May aggravate symptoms of decreased gastrointestinal motility in patients with autonomic neuropathy
Caution with GERD and/or those taking drugs that can cause or exacerbate esophagitis (eg, bisphosphonates)
Caution with myasthenia gravis because of decreased cholinergic activity
Caution with other anticholinergics (antimuscarinics); may increase risk for xerostomia, constipation, headache, dizziness, and blurred vision
Somnolence reported with oxybutynin-containing products; use caution with activities requiring mental alertness
May aggravate Parkinson disease symptoms
Hallucinations or confusion may occur; monitor
May exacerbate symptoms of heart failure, hypertension, and/or cardiac arrhythmias; use with caution
May aggravate symptoms of dementia in patients cholinesterase inhibitors; use with caution
Use with caution in patients with hiatal hernia
The use of the extended release formulation has been associated (rare) with symptoms of obstruction in patients with known stricture/narrowing of the GI tract
Before using over the counter product, consider other causes of frequent urination, including early pregnancy, diabetes, and other serious conditions; contact healthcare provider if symptoms do not improve with 2 weeks of initial use
Pregnancy and lactation
Pregnancy category: B
Lactation: Unknown; use with caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Ditropan XL (oxybutynin)
Mechanism of action
Exerts antispasmodic and antimuscarinic effects on smooth muscle; delays desire to void, increases bladder capacity, and decreases uninhibited contraction; decreases frequency and urgency
Absorption
Bioavailability: 6% (~1.5-2 times higher for extended-release)
Onset: 30-60 min
Peak effect: 3-6 hr
Duration: 6-10 hr
Peak plasma time: <1 hr (immediate-release); 12 hr (extended release)
Peak plasma concentration: Immediate-release, 3.6 ng/mL (R-) and 7.8 ng/mL (S-); extended-release, 1 ng/mL (R-) and 1.8 ng/mL (S-)
Distribution
Vd: 193 L
Metabolism
Metabolized in liver and gut by CYP3A4; converted to active metabolite N-desethyloxybutynin (DEO) by GI metabolic pathways, which are bypassed in transdermal delivery, resulting in lower DEO ratio
Metabolites: DEO (active)
Elimination
Half-life: 2-3 hr (immediate-release); 12-13 hr (extended-release)
Excretion: Urine
