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Tolterodine

Class
  • Diphenylmethane antimuscarinic
Indications
Administration/Absorption
  • Oral
Dosage

Distribution
  • 96% protein bound
  • VOD 113 L
Mechanism
  • Both tolterodine and its metabolite, 5-hydroxymethyltolterodine, are active
    • Act as competitive antagonists at muscarinic receptors
    • Act on M1, M2, M3, M4 and M5 subtypes
  • High specificity for muscarinic receptors
    • Negligible activity or affinity for other neurotransmitter receptors and other potential cellular targets
      • Such as calcium channels
  • This antagonism results in:
    • inhibition of bladder contraction
    • decrease in detrusor pressure
    • incomplete emptying of the bladder
Excretion
  • Hepatic metabolism
  • 77% urine, 17% feces
  • Half-life 1.9 - 3.6 hr
Side effects
Interactions

Contraindications
Comments