Tolterodine Tartrate

Indications

Tolterodine Tartrate is used for: Overactive bladder

Adult Dose

Oral Overactive Bladder, Urge Incontinence Immediate release: 2 mg PO q12hr. Reduce to 1 mg bid if needed to reduce side effects. Extended release: 2-4 mg PO once daily Hepatic impairment Mild to moderate (Child-Pugh class A or B): Not to exceed 1 mg PO q12hr (immediate release) or 2 mg PO once daily (extended release) Severe (Child-Pugh class C): Not recommended

Child Dose

Child < 18 years: Not recommended

Renal Dose

Renal impairment CrCl 10-30 mL/min: Not to exceed 1 mg PO q12hr (immediate release) or 2 mg PO once daily (extended release) CrCl <10 mL/min: Not recommended

Administration

Contra Indications

Severe ulcerative colitis, toxic megacolon, urinary retention, gastric retention, myasthenia gravis, uncontrolled narrow-angle glaucoma, pregnancy.

Precautions

Bladder flow obstruction, GI obstructive disorders, renal or hepatic impairment, autonomic neuropathy, hiatus hernia, risk of decreased GI motility, patients at risk of QT interval prolongation (e.g. electrolyte disturbances, bradycardia, pre-exisiting cardiac disorder). Lactation: Unknown whether drug is distributed in breast milk; do not nurse

Pregnancy-Lactation

Pregnancy There are no available data with use in pregnant women to inform drug-associated risks; in animal reproduction studies, oral administration of tolterodine and its 5-HMT metabolite to pregnant mice during organogenesis did not produce adverse developmental outcomes at doses approximately 9 to 12 times the clinical exposure at a dose of 20 mg/kg/day; however, higher doses produced adverse developmental outcomes Lactation There is no information on presence in human milk, effects on breastfed infant, or on milk production; based on limited data, tolterodine is excreted into milk in mice in low amounts; the development and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant from drug or from underlying maternal condition

Interactions

Increased risk of overdosage with potent CYP3A4 inhibitors e.g. macrolide antibiotics (erythromycin and clarithromycin), azole antifungals (e.g. ketoconazole and itraconazole), protease inhibitors, ciclosporin or vinblastine. Increased risk of torsade de pointes with drugs that prolong the QT interval (e.g. class Ia and class III antiarrhythmics). Increased risk of 'cholinergic neurogenic hypersensitivity' with centrally acting anticholinesterases (e.g. donepezil, rivastigmine). Increased risk of antimuscarinic side effects with antimuscarinic drugs.

Adverse Effects

Side effects of Tolterodine Tartrate : >10% Dry mouth (40%) 1-10% Blurred vision, Constipation, Dizziness, Drowsiness, Dyspepsia, Headache, Xerophthalmia

Mechanism of Action

Tolterodine is a competitive muscarinic receptor antagonist with actions similar to atropine. It is used in the management of urge urinary incontinence, urgency and frequency.