Oxybutynin (Ditropan)
Non-selective muscarinic (M1-M5) antagonist with additional local anesthetic and spasmolytic effects on detrusor smooth muscle; used for overactive bladder and urinary incontinence. IR 5 mg BID-TID (max 5 mg QID); XL 5-30 mg QD; transdermal patch and topical gel available. Plasma half-life 2-5h IR with first-pass formation of N-desethyloxybutynin (active, contributes to anticholinergic AEs). Oral bioavailability very low (~6%) due to extensive first-pass CYP3A4 metabolism, rationale for transdermal formulations. Heavy anticholinergic burden (dry mouth, constipation, cognitive impairment, especially in elderly).
Projected serum levels — 5 mg, once daily
Maintenance schedule: 5 mg once daily (oral).
Modeled steady state after ~1 days: peak ≈ 0.22 mg, trough ≈ 0.000 mg body load. Population-based estimate over 15 days for a 5 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.
Key facts
- Category
- Urological
- Route modeled
- Oral
- Model confidence
- inferred
- Half-life
- 2.3 h
- Common dose
- 5 mg
- Suggested maximum
- 30 mg/day
- Reference dose range
- 2.5–30 mg (single dose)
- Suggested cadence
- once daily
- Validated against
- 5 mg oral — Cmax 0.007 mg/L at 1 h
Documented interactions
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contraindicated
Carbamazepine (Tegretol) + Oxybutynin (Ditropan)
Carbamazepine (Tegretol) inducer of CYP3A4 predicted to change Oxybutynin (Ditropan) AUC by ~0.20x
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contraindicated
Clarithromycin (Biaxin) + Oxybutynin (Ditropan)
Clarithromycin (Biaxin) mechanism_based of CYP3A4 predicted to change Oxybutynin (Ditropan) AUC by ~10.00x
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contraindicated
Dasatinib (Sprycel) + Oxybutynin (Ditropan)
Dasatinib (Sprycel) time_dependent_inhibitor of CYP3A4 predicted to change Oxybutynin (Ditropan) AUC by ~5.00x
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contraindicated
Diltiazem + Oxybutynin (Ditropan)
Diltiazem mechanism_based of CYP3A4 predicted to change Oxybutynin (Ditropan) AUC by ~10.00x
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contraindicated
Efavirenz (Sustiva) + Oxybutynin (Ditropan)
Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Oxybutynin (Ditropan) AUC by ~0.12x
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contraindicated
Grapefruit (whole fruit) + Oxybutynin (Ditropan)
Grapefruit (whole fruit) mechanism_based of CYP3A4 predicted to change Oxybutynin (Ditropan) AUC by ~10.00x
Serum checks 208 modeled interaction pairings for oxybutynin (ditropan) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.
Research behind this entry
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A double-blind crossover comparison of the safety and efficacy of oxybutynin and propantheline in elderly patients with detrusor instability
Classical comparator trial characterizing oxybutynin efficacy and anticholinergic tolerability profile in elderly patients.
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Pharmacokinetic and safety comparison of a controlled-release oxybutynin formulation versus immediate-release oxybutynin in older adults with urge urinary incontinence
PK and tolerability comparison showing XL formulation achieves smoother plasma profile with reduced peak-related dry-mouth AEs.
2 published studies referenced in the app, each with a plain-language summary.