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Antimuscarinic medications for treatment of women with urge incontinence or overactive bladder (OAB) with incontinence

Antimuscarinic medications for treatment of women with urge incontinence or overactive bladder (OAB) with incontinence
Medication Starting dose Maximum dose Selected characteristics
Darifenacin extended-release
(7.5 and 15 mg tablets)
7.5 mg orally once daily 15 mg orally once daily
  • Refer to "General antimuscarinic issues" below this table
  • Dry mouth (19 to 35%) and constipation (15 to 21%) are common
  • Metabolized in liver by CYP3A4; maximum 7.5 mg daily with strong CYP3A4 inhibitors*
  • Reduced dose for moderate hepatic impairment
  • Not recommended for severe hepatic impairment
Fesoterodine extended-release
(4 and 8 mg tablets)
4 mg orally once daily 8 mg orally once daily
  • Refer to "General antimuscarinic issues" below this table
  • Dry mouth (19 to 35%) and constipation (4 to 6%) are common
  • Metabolized in liver by CYP3A4; maximum 4 mg daily with strong CYP3A4 inhibitors*
  • Reduced dose for severe renal impairment
  • Not recommended for severe hepatic impairment
Oxybutynin immediate-release
(5 mg tablet)
5 mg orally 2 or 3 times daily 5 mg orally 4 times daily
  • Refer to "General antimuscarinic issues" below this table
  • Dry mouth (71%) and constipation (9%) are common
  • Dizziness (17%) and somnolence (14%) can occur
  • Often not tolerated by older adults and medically ill patients due to anticholinergic (including CNS) side effects
  • Reduced dose in older adults
  • Short effect may be useful when continence is desired at specific times
  • Compliance is difficult with frequent dosing
Oxybutynin extended-release
(5, 10, and 15 mg tablets)
5 to 10 mg orally once daily 30 mg orally once daily
  • Refer to "General antimuscarinic issues" below this table
  • Dry mouth (35%) and constipation (9%) are common
  • Somnolence (6%) can occur
  • Compliance is improved with daily dosing
Oxybutynin transdermal
(10% gel sachet [packet] or pump)
Apply 1 sachet (packet) or 1 pump once daily; each packet or pump delivers 1 g of gel equivalent to 100 mg oxybutynin Same as starting dose
  • Refer to "General antimuscarinic issues" below this table
  • Associated with low rates of dry mouth (2 to 12%) and constipation (1%)
  • Apply to clean, dry, intact skin on abdomen, thighs, or upper arms/shoulders
  • Keep area dry for at least 1 hour after application
  • Do not use same application site more than once in 7 days
  • Application site reaction including irritation and dermatitis (up to 14%)
Oxybutynin transdermal
(3.9 mg patch)
Apply 1 patch twice per week (ie, once every 3 to 4 days) Do not exceed starting dose
  • Refer to "General antimuscarinic issues" below this table
  • Available without a prescription (OTC) in the United States and some other countries
  • Associated with low rates of dry mouth (10%) and constipation (3%)
  • Apply under clothing to abdomen, hip, or buttock
  • Do not use same application site more than once in 7 days
  • Application site pruritus (14 to 17%); local erythema (8%), rash (3%)
Solifenacin
(5 and 10 mg tablets
5 mg orally once daily 10 mg orally once daily
  • Refer to "General antimuscarinic issues" below this table
  • Dry mouth (11 to 28%) and constipation (5 to 13%) are common
  • Reduce dose for severe renal impairment or moderate hepatic impairment
  • Not recommended for severe hepatic impairment
  • Metabolized in liver by CYP3A4; maximum 5 mg daily with CYP3A4 inhibitors*
  • Modestly prolongs QTc interval; caution with other QTc prolonging drugs* and in patients with congenital prolonged QT
Tolterodine extended-release
(2 and 4 mg tablets)
2 mg orally once daily 4 mg orally once daily
  • Refer to "General antimuscarinic issues" below this table
  • Dry mouth (23 to 35%) and constipation (6 to 7%) are common
  • Reduced dose for renal and/or hepatic impairment, not recommended for severe renal or hepatic impairment
  • Metabolized in liver by CYPs 3A4 and 2D6; maximum 2 mg daily with strong CYP3A4 inhibitors*
  • Modestly prolongs QTc interval; caution with other QTc prolonging drugs* and in patients with congenital prolonged QT
Tolterodine immediate-release
(1 and 2 mg tablets)
1 mg orally twice daily 2 mg orally twice daily
Trospium extended-release
(60 mg tablet)
60 mg orally once daily Same as starting dose
  • Refer to "General antimuscarinic issues" below this table
  • Need to take on empty stomach or 1 hour before meal
  • Dry mouth (9 to 22%) and constipation (9 to 10%) are common
  • Reduce dose for renal impairment, not recommended for severe renal impairment
  • Not metabolized by CYP and therefore has a low risk of drug-drug interactions
  • Avoid alcohol consumption within 2 hours of using extended-release preparation
Trospium immediate-release
(20 mg tablet)
20 mg orally once daily 20 mg twice daily
General antimuscarinic issues:
  • All antimuscarinics are contraindicated in gastric retention, untreated narrow angle closure glaucoma, and supraventricular tachycardia.
  • Evidence suggests that cumulative exposure to potent antimuscarinics is associated with increased rates of dementia and Alzheimer disease.[1]
  • All antimuscarinics exert peripheral anticholinergic effects (eg, dry mouth, constipation, tachycardia, palpitations).
  • All antimuscarinics may have additive side effects with other medications that have strong anticholinergic effects (eg, first-generation H1 antihistamines, muscle relaxants, tricyclic antidepressants, antipsychotics, inhaled anticholinergic bronchodilators).*
  • Approach to agent selection and dose titration is reviewed in the topic section on pharmacologic therapy of urge incontinence.
CYP: cytochrome P-450 metabolism; CNS: central nervous system; OTC: over-the-counter.
* To check for specific interactions, use the Lexi-Interact program included with UpToDate.
Reference:
  1. Gray SL, Anderson ML, Dublin S, et al. Cumulative use of strong anticholinergics and incident dementia: S prospective cohort study. JAMA 2015; 175:401.
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