Tolterodine

Class

• • Diphenylmethane antimuscarinic

Indications

• Urinary incontinence

  • • urinary frequency, urgency, or urge incontinence

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

• • fewer side effects than oxybutynin

    • more specific for bladder

  • Xerostomia

  • Decreased gastric motility

• Headache

• Constipation

• Dry eyes

• Sleepiness

Interactions

Contraindications

• • myasthenia gravis

• angle closure glaucoma