Oxybutynin
Oxybutynin
Ditropan, Ditropan XL, Oxytrol (transdermal), Gelnique (gel)
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Summary
Common uses
Overactive bladder (urgency, frequency, urge incontinence)0, Neurogenic detrusor overactivity0, Hyperhidrosis (off-label)0
Pharmacy
Starting dose
IR 5 mg PO BID-TID; ER 5-10 mg PO daily, titrate; transdermal patch 3.9 mg/d twice weekly (OTC)
Preparations
5 mg IR tablets; 5, 10, 15 mg ER tablets; 5 mg/5 mL syrup; 3.9 mg/24 h transdermal patch (Oxytrol); 10% topical gel
US FDA Max
30 mg/d (XL) typical
Pharmacology
Routes
Oral, transdermal, topical gel, intravesical
Onset
30-60 minutes (PO)
Duration
IR: 6-10 hours; ER: 24 hours
Half-life
2-3 hours (parent and active N-desethyl metabolite)[1]
Bioavailability
~6% IR oral (substantial first-pass to active N-desethyl metabolite, which contributes most of the antimuscarinic adverse effects); transdermal bypasses first-pass and is better tolerated[1]
Pregnancy
Limited data.[citation needed]
Legal status
OTC (transdermal patch in women) and Rx-only (other forms) in US
Purported mechanism
Oxybutynin is a non-selective muscarinic receptor antagonist with predominant M3 antagonism in the detrusor, relaxing involuntary contractions and increasing functional bladder capacity.0 Lack of M3 selectivity drives the characteristic anticholinergic burden (dry mouth, constipation, blurred vision, urinary retention, CNS effects in elderly). Cumulative anticholinergic exposure is implicated in dementia risk in older adults, which is a growing reason to prefer β3-agonists (mirabegron) or M3-selective antimuscarinics in that population[1].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Ditropan XL (oxybutynin chloride), Janssen, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020897s039lbl.pdf