tolterodine (Rx)

Brand and Other Names:Detrol, Detrol LA
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet, immediate release

  • 1mg
  • 2mg

capsule, extended release

  • 2mg
  • 4mg
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Overactive Bladder, Urge Incontinence

Immediate release: 2 mg PO q12hr; may lower dose to 1 mg twice daily based on response and tolerability

Extended release: 2-4 mg PO once daily; may lower dose to 1 mg twice daily based on response and tolerability

Dosing Modifications

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

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

Strong CYP3A4 inhibitors

  • Not to exceed 1 mg PO q12hr (immediate release) or 2 mg PO once daily (extended release)

Not recommended

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Interactions

Interaction Checker

and tolterodine

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Dry mouth (40%)

            1-10%

            Blurred vision

            Constipation

            Dizziness

            Drowsiness

            Dyspepsia

            Headache

            Xerophthalmia

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            Warnings

            Contraindications

            Urinary or gastric retention

            Uncontrolled narrow-angle glaucoma

            Hypersensitivity to drug or ingredients or to fesoterodine fumarate, which is metabolized to 5-hydroxymethyl tolterodine

            Cautions

            Controlled narrow-angle glaucoma, hepatic, or renal impairment

            Anaphylaxis and angioedema necessitating hospitalization and emergency treatment reported with first or subsequent doses; discontinue immediately if angioedema and hypotension, difficulty breathing, or airway obstruction develop

            Anticholinergic central nervous system effects (eg, dizziness, somnolence) reported; patients should not drive or operate heavy machinery until they adjust to therapy

            Use with caution in patients with myasthenia gravis, which is characterized by decreased cholinergic activity at neuromuscular junction

            When coadministered with strong CYP3A4 inhibitors, tolterodine should be given at reduced dosage

            QTc prolongation reported with high doses; use caution in patients with congenital prolonged QT or in patients receiving concurrent therapy with QTc-prolonging drugs (class Ia or III antiarrhythmics)

            Anticholinergics may potentially adversely affect the clinical course of alzheimer disease in patients receiving cholinesterase inhibitors; monitor for decreases in congnition, functional abilities and increased problematic behaviors in patients with dementia receiving dual therapy with an anticholinesterase inhibitor and a bladder anticholinercgic agent like tolterodine

            May increase risk of urinary retention in patients with bladder flow obstruction (eg, benign prostatic hypertrophy)

            May increase risk of gastric retention in patients with decreased GI motility or gastrointestinal obstructive disorders

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            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

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Competitive muscarinic receptor antagonist; decreases bladder contractions; is more specific for bladder than oxybutynin

            Absorption

            Bioavailability: 77%

            Onset: Overactive bladder, 1 wk; urge incontinence, 1 hr

            Time to peak effect: 2-4 wk

            Peak plasma time: Immediate release, 1-2 hr; extended release, 2-6 hr

            Distribution

            Vd: 113 L

            Metabolism

            Metabolized in liver by CYP2D6 and (to minor extent) CYP3A4

            Metabolites: 5-Hydroxymethyl, dealkylated tolterodine

            Elimination

            Half-life: Parent drug, 1.9-3.7 hr; active metabolite (5-hydroxymethyl), 3 hr (8.7 hr in cirrhosis)

            Total body clearance: 5.7 L/kg/hr

            Excretion: Urine (77%), feces (17%)

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            Images

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.