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  • Detrol LA
    (tolterodine tartrate)

    OTHER BRAND NAMES

    Detrol

    THERAPEUTIC CLASS

    Muscarinic antagonist

    DEA CLASS

    RX

    INDICATIONS

    Treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency.

    ADULT DOSAGE

    Adults: (Cap, ER) Usual: 4mg qd. May be lowered to 2mg qd based on response and tolerability. Mild to Moderate Hepatic Impairment (Child-Pugh Class A or B)/Severe Renal Impairment (CrCl 10-30mL/min)/With Potent CYP3A4 Inhibitors (eg, ketoconazole, clarithromycin, ritonavir): Usual: 2mg qd. (Tab) Usual: 2mg bid. May be lowered to 1mg bid based on response and tolerability. Significantly Reduced Hepatic or Renal Function/With Potent CYP3A4 Inhibitors: Usual: 1mg bid.

    ADMINISTRATION

    Oral route. (Cap, ER) Take with water and swallow whole.

    HOW SUPPLIED

    Cap, Extended-Release (ER): (Detrol LA) 2mg, 4mg; Tab: (Detrol) 1mg, 2mg

    CONTRAINDICATIONS

    Urinary/gastric retention, uncontrolled narrow-angle glaucoma, hypersensitivity to fesoterodine fumarate ER tab.

    WARNINGS/PRECAUTIONS

    Anaphylaxis/angioedema requiring hospitalization and emergency treatment occurred with 1st or subsequent doses; d/c and provide appropriate therapy if difficulty in breathing, upper airway obstruction, or fall in BP occurs. Risk of urinary retention; caution in patients with clinically significant bladder outflow obstruction. Risk of gastric retention; caution in patients with GI obstructive disorders (eg, pyloric stenosis). Caution with decreased GI motility (eg, intestinal atony), myasthenia gravis, known history of QT prolongation, hepatic/renal impairment, and in patients being treated for narrow-angle glaucoma. CNS anticholinergic effects (eg, dizziness, somnolence) reported; may impair physical/mental abilities. Monitor for signs of anticholinergic CNS effects (particularly after beginning treatment and increasing the dose); consider dose reduction or d/c if such effects occur. (Cap, ER) Not recommended with severe hepatic impairment (Child-Pugh Class C) or with CrCl <10mL/min.

    ADVERSE REACTIONS

    Dry mouth, dizziness, headache, abdominal pain, constipation.

    DRUG INTERACTIONS

    Caution with Class IA (eg, quinidine, procainamide) or Class III (eg, amiodarone, sotalol) antiarrhythmics. May aggravate dementia symptoms when initiating therapy in patients taking cholinesterase inhibitors. Increased concentrations with ketoconazole or other potent CYP3A4 inhibitors (eg, itraconazole, miconazole, clarithromycin). Increased levels with fluoxetine reported with immediate release tolterodine. May increase the frequency and/or severity of anticholinergic effects with other anticholinergic (antimuscarinic) agents.

    PREGNANCY AND LACTATION

    Category C, not for use in nursing.

    MECHANISM OF ACTION

    Muscarinic receptor antagonist; competitive antagonist of acetylcholine at postganglionic muscarinic receptors mediating urinary bladder contraction and salivation via cholinergic muscarinic receptors.

    PHARMACOKINETICS

    Absorption: Administration of variable doses resulted in different parameters in extensive metabolizers (EM) and poor metabolizers (PM) of CYP2D6. (Tab) Rapid. Distribution: Plasma protein binding (96.3%); (IV) Vd=113L. Metabolism: Liver (extensive); oxidation to 5-hydroxymethyl tolterodine (active metabolite) via CYP2D6; dealkylation via CYP3A4 (PM). Elimination: Urine (77%), feces (17%). (Tab) Single Dose: EM: T1/2=2 hrs; PM: T1/2=6.5 hrs. (Cap, ER) Single Dose: EM: T1/2=8.4 hrs.

    ASSESSMENT

    Assess for hypersensitivity to the drug or fesoterodine fumarate, urinary/gastric retention, bladder outflow obstruction, GI obstructive disorders, decreased GI motility, narrow-angle glaucoma, myasthenia gravis, history of QT prolongation, hepatic/renal impairment, pregnancy/nursing status, and possible drug interactions.

    MONITORING

    Monitor for anaphylaxis, angioedema, difficulty breathing, upper airway obstruction, fall in BP, urinary retention, gastric retention, CNS anticholinergic effects, QT prolongation, hypersensitivity reactions, and other adverse reactions.

    PATIENT COUNSELING

    Inform patients that drug may produce blurred vision, dizziness, or drowsiness. Advise to exercise caution against potentially dangerous activities until drug's effects have been determined.

    STORAGE

    (Tab): 25°C (77°F); excursions permitted to 15-30°C (59-86°F). (Cap, ER): 20-25°C (68-77°F); excursions permitted to 15-30°C (59-86°F). Protect from light.