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tolterodine (Detrol, Detrol LA)

Tradename: Detrol. Indications: - treatment of urinary frequency & urinary urgency due to urge incontinence & overactive bladder Contraindications: 1) urinary retention 2) gastric retention 3) narrow angle glaucoma Dosage: 1) 1-2 mg PO BID 2) 2-4 mg PO QD (Detrol LA) Tabs: 1,2 mg; 2,4 mg (Detrol LA) Pharmacokinetics: 1) oral absorption increased by food 2) bioavailability 77% 3) peak concentration 1-2 hours after oral dose 4) metabolized in liver by cyt P450 2D6 & cyt P450 3A4 to active 5-hydroxymethyl derivative 5) highly bound to plasma proteins (alpha-1 acid glycoprotein) Adverse effects: 1) anticholinergic effects: a) GI: dry mouth, dyspepsia b) respiratory: bronchitis, cough c) psychiatric: somnolence d) cardiovascular: hypertension, chest pain e) infection (especially fungal) f) increase in urine residual volume 2) central nervous system - headache, vertigo, nervousness Overdose: 1) give activated charcoal 2) electrocardiogram (ECG) monitor Drug interactions: 1) fluoxetine inhibits tolterodine metabolism 2) cyt P450 2D6 & cyt P450 3A4 inhibitors (no data, use caution) a) macrolides, antifungal agents b) maximum dose of tolterodine: 1 mg BID if administered concurrently [5] Mechanism of action: 1) muscarinic receptor antagonist 2) presumptive muscle relaxant 3) newer agent allegedly better tolerated than oxybutynin (Ditropan) 4) allegedly some bladder selectivity [3] a) primarily antagonizes muscarinic M2 receptors & muscarininc M3 receptors [6] b) bladder selectivity vs salivary gland in animal model [5]

Interactions

drug interactions drug adverse effects of parasympatholytics

Related

cytochrome P450 2D6 (cytochrome P450 2D, cytochrome P450 DB1, debrisoquine-4-hydroxylase, CYP2D6) cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)

General

urinary antispasmodic

Properties

MISC-INFO: elimination route LIVER protein-binding 96% pregnancy-category C

Database Correlations

PUBCHEM correlations

References

  1. Physician's Desk Reference (PDR), volume 102, 1999, Medical Economics, 1999
  2. Pharmacia & Upjohn
  3. Eslami M. In: Intensive Course in Geriatric Medicine & Board Review, Marina Del Ray, CA, Sept 12-15, 2001
  4. Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: 220233 (subscription needed) http://www.prescribersletter.com
  5. Geriatric Dosage Handbook, 6th edition, Selma et al eds, Lexi-Comp, Cleveland, 2001
  6. Prescriber's Letter 12(2): 2005 Antimuscarinic Medications for Overactive Bladder Detail-Document#: 210209 (subscription needed) http://www.prescribersletter.com