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  • Detrusitol SR
    / Pfizer


    Active Ingredient

    Status in Israel
    RX

    Presentation and Status in Health Basket

    Presentation Basket Yarpa Pharmasoft

    Prolonged-Release Capsules

    28 X 2 mg

    partial basket chart 5143 4284

    Prolonged-Release Capsules

    28 X 4 mg

    partial basket chart 5144 4126

    Related information


    Dosage

    The recommended dose is 4 mg daily. This product should be taken once daily with liquids and swallowed whole. The dose may be lowered to 2 mg daily based on individual response and tolerability, however, limited efficacy data is available for 2 mg. For patients with significantly reduced hepatic or renal function or who are currently taking drugs that are potent inhibitors of CYP3A4, the recommended dose is 2 mg daily.
    For full details see prescribing information.


    Indications

    Overactive bladder with symptoms of urinary frequency, urgency or urge incontinence.


    Contra-Indications

    Hypersensitivity, urinary retention, gastric retention, uncontrolled narrow-angle glaucoma.


    Special Precautions

    General
    Risk of Urinary Retention and Gastric Retention: Capsules should be administered with caution to patients with clinically significant bladder outflow obstruction because of the risk of urinary retention and to patients with gastrointestinal obstructive disorders, such as pyloric stenosis, because of the risk of gastric retention.
    Controlled Narrow-Angle Glaucoma: This product should be used with caution in patients being treated for narrow-angle glaucoma.
    Reduced Hepatic and Renal Function: For patients with significantly reduced hepatic function or renal function, the recommended dose is 2 mg daily. this product should be used with caution in patients with myasthenia gravis. , a disease characterized by decreased cholinergic activity at the neuromuscular junction.1
    Patients with Congenital or Acquired QT Prolongation: In a study of the effect of tolterodine immediate release tablets on the QT interval, the effect on the QT interval appeared greater for 8 mg/day (two times the therapeutic dose) compared to 4 mg/day and was more pronounced in CYP2D6 poor metabolizers (PM) than extensive metabolizers (EMs). The effect of tolterodine 8 mg/day was not as large as that observed after four days of therapeutic dosing with the active control moxifloxacin. However, the confidence intervals overlapped. These observations should be considered in clinical decisions to prescribe for patients with a known history of QT prolongation or patients who are taking Class IA (e.g., quinidine, procainamide) or Class III (e.g.,amiodarone, sotalol) antiarrhythmic medications. There has been no association of Torsade de Pointes in the international post-marketing experience with Detrusitol or Detrusitol SR.
    For full details see prescribing information.


    Side Effects

    Blurred vision, dry mouth, dyspepsia, headache, constipation and xerophthalmia, fatigue, abdominal pain, somnolence, sinusitis. Anaphylactoid reactions, including angioedema. Tachycardia, palpitations, peripheral edema, hallucinations. Disorientation, memory impairment, diarrhea.


    Drug interactions

    For patients receiving ketoconazole or other potent CYP3A4 inhibitors such as other azole antifungals (e.g. itraconazole, miconazole) or macrolide antibiotics (e.g. erythromycin, clarithromycin) or cyclosporine or vinblastine, the recommended dose is 2 mg daily.


    Pregnancy and Lactation

    Pregnancy: Pregnancy Category C. At oral doses of 20 mg/kg/day (approximately 14 times the human exposure), no anomalies or malformations were observed in mice. When given at doses of 30 to 40 mg/kg/day, tolterodine has been shown to cause embryolethality, reduce fetal weight, and increase the incidence of fetal abnormalities (cleft palate, digital abnormalities, intra-abdominal hemorrhage, and various skeletal abnormalities, primarily reduced ossification) in mice. At these doses, the AUC values were about 20- to 25-fold higher than in humans. Rabbits treated subcutaneously at a dose of 0.8 mg/kg/day achieved an AUC of 100 µg·h/L, which is about three-fold higher than that resulting from the human dose. This dose did not result in any embryotoxicity or teratogenicity. There are no studies of tolterodine in pregnant women. Therefore, this product should be used during pregnancy only if the potential benefit for the mother justifies the potential risk to the fetus.
    Nursing Mothers: Tolterodine immediate release is excreted into the milk in mice. Offspring of female mice treated with tolterodine 20 mg/kg/day during the lactation period had slightly reduced body-weight gain. The offspring regained the weight during the maturation phase. It is not known whether tolterodine is excreted in human milk; therefore, this product should not be administered during nursing. A decision should be made whether to discontinue nursing or to discontinue this drug in nursing mothers.
    For full details see prescribing information.


    Overdose

    The highest dose of tolterodine tartrate given to human volunteers was 12.8 mg as single dose. The most severe adverse events observed were accommodation disturbances and micturition difficulties. A 27-month-old child who ingested 5 to 7 tolterodine immediate release tablets 2 mg was treated with a suspension of activated charcoal and was hospitalized overnight with symptoms of dry mouth. The child fully recovered.
    Management of Overdose: Overdose with tolterodine can potentially result in severe central antimuscarinic effects and should be treated accordingly. In the event of tolterodine overdose, standard supportive measures for managing QT prolongation should be adopted. ECG monitoring is recommended in the event of overdose. In dogs, changes in the QT interval (slight prolongation of 10% to 20%) were observed at a suprapharmacologic dose of 4.5 mg/kg, which is about 68 times higher than the recommended human dose. In clinical trials of normal volunteers and patients, QT interval prolongation was observed with tolterodine immediate release at doses up to 8 mg (4 mg bid) and higher doses were not evaluated.
    For full details see prescribing information.


    Manufacturer
    Pfizer Italy
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