Drug information of Tolterodine


Tolterodine

Drug group:

Tolterodine reduces spasms of the bladder muscles. Tolterodine is used to treat overactive bladder with symptoms of urinary frequency, urgency, and incontinence.

Mechanism of effect

Tolterodine acts as a competitive antagonist of acetylcholine at postganglionic muscarinic receptors. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors.

Pharmacodynamic

Tolterodine has a pronounced effect on bladder function.

Pharmacokinetics

Tolterodine is highly bound to plasma proteins, primarily α1-acid glycoproteinolterodine is extensively metabolized by the liver following oral dosing.
Following administration of a 5-mg oral dose of 14C-tolterodine solution to healthy volunteers, 77% of radioactivity was recovered in urine and 17% was recovered in feces in 7 days.
Half life: 1.9-3.7 hours.

Drug indications

overactive bladder

Dosage

Usual Adult Dose for Urinary Incontinence
Immediate release tablets:
-Initial dose: 2 mg orally 2 times a day
-Maintenance dose: 1 to 2 mg orally 2 times a day, depending on patient response and tolerability
Extended release capsules:
-Initial dose: 4 mg orally once a day
-Maintenance dose: 2 to 4 mg orally once a day, depending on patient response and tolerability
Usual Adult Dose for Urinary Frequency
Immediate release tablets:
-Initial dose: 2 mg orally 2 times a day
-Maintenance dose: 1 to 2 mg orally 2 times a day, depending on patient response and tolerability
Extended release capsules:
-Initial dose: 4 mg orally once a day
-Maintenance dose: 2 to 4 mg orally once a day, depending on patient response and tolerability

Alerts

Administer tolterodine tartrate extended-release capsules with caution to patients with clinically significant bladder outflow obstruction, gastrointestinal obstructive disorders , patients with conditions associated with decreased gastrointestinal motility (e.g., intestinal atony), hepatic impairment , Renal impairment, myasthenia gravis, Patients with Congenital or Acquired QT Prolongation.

Points of recommendation

1- In the event of difficulty in breathing, upper airway obstruction, or fall in blood pressure, tolterodine tartrate extended-release capsules should be discontinued and appropriate therapy promptly provided.
2- Patients should be monitored for signs of anticholinergic CNS effects, particularly after beginning treatment or increasing the dose. Advise patients not to drive or operate heavy machinery until the drug's effects have been determined.
3- Take with food.

Pregnancy level

C


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