Brand name: Detrusitol
Active ingredient (generic name): Tolterodine
Manufacturer: Pfizer
Importer: Behestan Darou
Pharmacotherapeutic group: Urinary antispasmodics
Pharmaceutical form: 1mg & 2mg Tablets
Tolterodine is a competitive, specific muscarinic receptor antagonist with selectivity for the urinary bladder over salivary glands in vivo. One of the tolterodine metabolites (5-hydroxymethyl derivative) exhibits a pharmacological profile similar to that of the parent compound. In extensive metabolisers this metabolite contributes significantly to the therapeutic effect.
Pharmacokinetic:
Tolterodine is rapidly absorbed. Both tolterodine and the 5-hydroxymethyl metabolite reach maximal serum concentrations 1-3 hours after dose. The half-life for tolterodine given as the tablet is 2-3 hours in extensive and about 10 hours in poor metabolisers (devoid of CYP2D6). Steady state concentrations are reached within 2 days after administration of the tablets.
After oral administration tolterodine is subject to CYP2D6 catalysed first-pass metabolism in the liver, resulting in the formation of the 5-hydroxymethyl derivative, a major pharmacologically equipotent metabolite.
The absolute bioavailability of tolterodine is 17 % in extensive metabolisers, the majority of the patients, and 65% in poor metabolisers (devoid of CYP2D6).
Therapeutic indication:
It is prescribe for symptomatic treatment of urge incontinence and/or increased urinary frequency and urgency as may occur in patients with overactive bladder syndrome.
Dosage and administration:
The recommended dose is 2 mg twice daily except in patients with impaired liver function or severely impaired renal function for whom the recommended dose is 1 mg twice daily.
Adverse reaction:
Due to the pharmacological effect of Tolterodine it may cause mild to moderate antimuscarinic effects, like dryness of the mouth, dyspepsia, headache, diarrhea, constipation, abdominal pain and dry eyes.
Tolterodine is contraindicated in patients with urinary retention, uncontrolled narrow angle glaucoma, myasthenia gravis, and known hypersensitivity to tolterodine or excipients, severe ulcerative colitis, toxic mega colon.
Pharmacokinetic interactions:
Concomitant systemic medication with potent CYP3A4 inhibitors such as macrolide antibiotics, antifungal agents and antiproteases is not recommended due to increased serum concentrations of tolterodine in poor CYP2D6 metabolizers with risk of overdosage.
Concomitant medication with other drugs that possess antimuscarinic properties may result in more pronounced therapeutic effect and side-effects. Conversely, the therapeutic effect of tolterodine may be reduced by concomitant administration of muscarinic cholinergic receptor agonists.
Special warnings:
Tolterodine shall be used with caution in patients with risk factors for QT-prolongation including concomitant administration of drugs known to prolong QT-interval including Class IA and Class III anti-arrhythmics and it should be administered with caution in patients with hepatic disease.
Pregnancy and lactation:
Detrusitol is not recommended during pregnancy and Studies in animals have shown reproductive toxicity.
Storage temperature:
Room temperature (15-25 C)
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