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Detrusitol Tabs 2mg

DETRUSITOL is indicated for the treatment of overactive bladder with symptoms of urinary urgency, frequency and/or urge incontinence.

Tolterodine L-tartrate 1mg & 2mg tablets

DETRUSITOL tablets are white, round, biconvex, film-coated tablets. The 1mg tablet is engraved with arcs above and below the letters TO and the 2mg tablet is engraved with arcs above and below the letters DT.

Tolterodine is a competitive, specific muscarinic receptor antagonist which exhibits a selectivity for the urinary bladder over salivary glands, which have been demonstrated in non-clinical pharmacological in vivo studies. Tolterodine has a high specificity for muscarinic receptors. A major active metabolite (5-hydroxymethyl derivative or DD 01) of tolterodine exhibits a pharmacological profile which is similar to that of the parent compound. In extensive metabolisers this metabolite contributes significantly to the therapeutic effect of tolterodine (see pharmacokinetics).

The effect of treatment can be expected within 4 weeks.

Tolterodine is rapidly absorbed. Both tolterodine and the 5-hydroxymethyl metabolite reach maximal serum concentrations 1-3 hours after dose. The average peak serum concentrations of tolterodine and the metabolite increase proportionally in the dose interval 1 to 4mg. Tolterodine is mainly metabolised by the polymorphic enzyme CYP2D6 leading to the formation of a pharmacologically active 5-hydroxymethly metabolite. The systemic serum clearance of tolterodine in extensive metabolisers is about 30 L/h and the terminal half-life is 2 to 3 hours. The half-life of the 5-hydroxymethyl metabolite is 3-4 hours. In poor metabolisers (deficient of CYP2D6) tolterodine is dealkylated via CYP3A isoenzymes whereby N-dealkylated tolterodine is formed. This metabolite does not contribute to the clinical effect. The reduced clearance and prolonged half-life (about 10 hours) of the parent compound in poor metabolisers lead to increased concentrations of tolterodine (about 7 fold) associated with undetectable concentrations of the 5-hydroxymethyl metabolite. As a result, the exposure (AUC) of unbound tolterodine in poor metabolisers is similar to the combined exposure of unbound tolterodine and the 5-hydroxymethyl metabolite in patients with CYP2D6 activity given the same dosage regimen. The safety, tolerability and clinical response are similar irrespective of phenotype. Steady state concentrations are reached within 2 days.

The absolute bioavailability of tolterodine is 65% in poor metabolisers (devoid of CYP2D6) and 17% in extensive metabolisers (the majority of patients).

Food does not influence the exposure of the unbound tolterodine and the active 5-hydroxymethyl metabolite in extensive metabolisers, although the tolterodine levels increase when taken with food. Clinically relevant changes are likewise not expected in poor metabolisers.

Tolterodine and the 5-hydroxymethyl metabolite bind primarily to orosomucoid. The unbound fractions are 3.7% and 36% respectively. The volume of distribution of tolterodine is 113 L. The excretion of radioactivity after administration of [14C]-tolterodine is approximately 77% in urine and 17% in faeces. Less than 1% of the dose is excreted unchanged and about 4% as the 5-hydroxymethyl metabolite. The carboxylated metabolite and the corresponding dealkylated metabolite account for about 51% and 29% of the urinary recovery, respectively.

About 2-fold higher exposure of unbound tolterodine and the 5-hydroxymethyl metabolite is found in liver cirrhosis subjects.

DETRUSITOL is indicated for the treatment of overactive bladder with symptoms of urinary urgency, frequency and/or urge incontinence.

Dosage and Administration
The recommended dose is 2mg twice a day. In the case of troublesome side-effects the dose may be reduced from 2mg to 1mg twice a day.

The recommended dose is 1mg twice a day for patients with impaired renal function, impaired liver function, or receiving concomitant ketoconazole or other potent CYP3A inhibitors.

After six months the need for further treatment should be considered.

Safety and effectiveness in children have not been established.

Tolterodine is contraindicated in patients with:

  • Urinary retention
  • Uncontrolled narrow angle glaucoma
  • Known hypersensitivity to tolterodine or excipients
  • Myasthenia Gravis
  • Severe ulcerative colitis
  • Toxic megacolon

Warnings and Precautions
Tolterodine should be used with caution in the following patients:

  • at risk for urinary retention
  • at risk for decreased gastrointestinal motility with impaired renal function. The recommended total daily dose is 2mg (see DOSAGE AND ADMINISTRATION)
  • With impaired hepatic function. The recommended total daily dose is 2mg (see DOSAGE AND ADMINISTRATION)
  • Autonomic neuropathy
  • Hiatus hernia
  • The recommended total daily dose of tolterodine is 2mg for patients on concomitant medication with potent CYP3A inhibitors, such as macrolide antibiotics (e.g. erythromycin and clarithromycin) or azole antifungal agents (e.g. ketoconazole, itraconazole and miconazole)[see DOSAGE AND ADMINISTRATION].

Organic reasons for urge and frequency should be considered before treatment.

Pregnancy and lactation: Clinical experience from pregnant women is lacking. Studies in mice have shown that high doses caused reduced foetal weight, embryolethality and increased incidence of foetal abnormalities. Until more information is available pregnant women should not be treated with tolterodine.

Women of child-bearing potential should be considered for treatment only if using adequate contraception.

Use of tolterodine during lactation should be avoided since no data on excretion into breast milk in humans are available.

Effect on ability to drive and use machines: Since tolterodine may cause accommodation disturbances and influence reaction time, the ability to drive and use machines may be negatively affected.

Adverse Effects
Tolterodine may cause mild-to-moderate antimuscarinic effects, like dryness of the mouth, dyspepsia and reduced lacrimation.

Clinical Trials:
Adverse events considered potentially drug-related from studies of tolterodine are provided below.

10% or more: Dry mouth 
1% to 10%:   Headache, constipation, dizziness/vertigo, abdominal pain, dyspepsia, fatigue, dry eyes, somnolence, abnormal vision (including abnormal accommodation), flatulence, dysuria.

In patients receiving tolterodine tartrate tablets the following events were also considered to be potentially drug related: chest pain, dry skin, bronchitis, increased weight.
1% Urinary retention, confusion, gastrooesophageal reflux, flushed skin, allergic reactions.

Post-marketing Surveillance:
The following events have been reported in association with tolterodine use in clinical practice: anaphylactoid reactions, tachycardia, peripheral oedema.

In toxicity, genotoxicity, carcinogenicity and safety pharmacology studies no clinically relevant effects have been observed, except those related to the pharmacological effect of the medicine.

Reduced foetal weight, embryolethality and increased incidence of foetal malformations have been observed in pregnant mice treated with high doses. No effects were observed at a systemic exposure (measured as Cmax or AUC for unbound tolterodine and its active metabolite) 9-50 times higher than in humans after the highest recommended dose.

In dogs a slight prolongation of the QT interval has been observed at high concentrations of tolterodine or its main metabolite (50-100 times therapeutic levels). In clinical trials, no QT internal prolongation has been found in a large and representative patient material, on recommended doses of DETRUSITOL.

The antimuscarinic effect of tolterodine may become more pronounced when administered to patients receiving other drugs with antimuscarinic effects e.g. antidepressants. Conversely the therapeutic effect of tolterodine may be reduced by concomitant administration of muscarinic cholinergic receptor agonists. The effect of prokinetics like metoclopramide and cisapride may be decreased by tolterodine.

Pharmacokinetic interactions are possible with other drugs metabolised by or inhibiting cytochrome P450 2D6 (CYP2D6) or CYP3A4. Concomitant treatment with fluoxetine does not result in a clinically significant interaction.

Ketoconazole, a potent inhibitor or CYP3A, significantly increased plasma concentrations of tolterodine when coadministered to poor metabolisers (i.e. persons devoid of CYP2D6 metabolic pathway). For patients receiving ketoconazole or other potent CYP3A inhibitors, the recommended total daily dose is 2mg (see DOSAGE AND ADMINISTRATION).

Clinical studies have shown no interactions with warfarin or combined oral contraceptives (ethinyl oestradiol/levonorgestrel).

A clinical study with metabolic probe drugs has not given any evidence that the activity of CYP2D6, 2C19, 3A4 or 1A2 will be inhibited by tolterodine.

The highest dose of tolterodine tartrate given to human volunteers was 12.8mg as a single dose. The most severe adverse events observed were accommodation disturbances and micturition difficulties.

Overdosage with tolterodine can potentially result in severe central antimuscarinic effects and should be treated accordingly.

Pharmaceutical Precautions
36 month shelf life when stored at room temperature (< 25¡ã C).

Medicine Classification
Prescription medicine.

Package Quantities
Polyethene bottles containing 60 and 500 tablets.
Blister packs containing 56 tablets (four strips of 14 tablets).

Further Information
List of excipients:
Microcrystalline cellulose
Calcium hydrogen phosphate dihydrate
Sodium starch glycollate (Type B)
Magnesium stearate
Stearic acid
Titanium dioxide

Name and Address of Manufacturer
PO Box 11-282
Auckland 5


  • Threadworms look like tiny pieces of white cotton on the outside of a bowel motion or around the anus.
  • Signs include irritability, tiredness, itchy bottom, teeth-grinding, bed-wetting, disturbed sleep and nose rubbing.
  • Single-dose treatments are available, repeated at 2 weeks.
  • Treat the whole family.
  • Infection is via direct contact between individuals or contact with contaminated objects, as the eggs remain alive for severalweeks
  • Contrary to popular opinion, worms are not caught from pets.

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