mirabegron (Rx)

Brand and Other Names:Myrbetriq
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet, extended-release

  • 25mg
  • 50mg
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Overactive Bladder

Monotherapy

  • Indicated for overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary frequency
  • 25 mg PO qDay
  • 25 mg dose is typically effective within 8 weeks
  • May increase to 50 mg PO qDay based on individual efficacy and tolerability

Combination with muscarinic antagonist

  • Indicated in combination with the muscarinic antagonist solifenacin succinate for treatment of OAB with symptoms of urge urinary incontinence, urgency, and urinary frequency
  • Combination regimen: 25 mg PO qDay plus solifenacin succinate 5 mg PO qDay
  • May increase mirabegron to 50 mg PO qDay after 4-8 weeks based on individual efficacy and tolerability

Dosage Modifications

Renal impairment

  • Severe (CrCl 15-29 mL/min): Not to exceed 25 mg/day
  • End-stage renal disease (ESRD): Not recommended

Hepatic impairment

  • Moderate (Child-Pugh B): Not to exceed 25 mg/day
  • Severe (Child Pugh C): Not recommended

Safety and efficacy not established

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Interactions

Interaction Checker

and mirabegron

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Elevated BP occurring predominantly in patients with preexisting hypertension (7.5-11.5%)

            1-10%

            Monotherapy

            • Dry mouth (3-9%)
            • Urinary tract infection (UTI) (2.9-4.2%)
            • Nasopharyngitis (3.5-3.9%)
            • Headache (2.1-3.2%)
            • Back pain (2.8%)
            • Sinusitis (2.7%)
            • Arthralgia (1.3-2.1%)
            • Cystitis (2.1%)
            • Dizziness (2%)
            • Constipation (1.6%)
            • Tachycardia (1.2-1.6%)
            • Diarrhea (1.2-1.5%)
            • Fatigue (1.2-1.4%)
            • Reports of neoplasms (0-1%)

            Combination with solifenacin

            • Dry mouth (7.2-9.3%)
            • UTI (4-8.4%)
            • Constipation (3.9-4.2%)
            • Tachycardia (0.9-2.2%)
            • Dyspepsia (1.1-1.3%)
            • Dizziness (0.4-1.3%)
            • Blurred vision (0.7-1.1%)
            • Arthralgia (0.5-1.1%)

            <1%

            Cardiac disorders (eg, palpitations, elevated BP)

            Eye Disorders (eg, glaucoma, blurry vision)

            GI disorders (eg, dyspepsia, gastritis, abdominal distension)

            Rhinitis

            Elevations in GGT, AST, ALT, LDH

            Renal and urinary disorders (eg, nephrolithiasis, bladder pain)

            Reproductive system disorders (eg, vulvovaginal pruritis, vaginal infection)

            Skin and subcutaneous tissue disorders (eg, urticaria, leukocytoclastic vasculitis, rash, pruritus, purpura, lip edema)

            Stevens-Johnson syndrome associated with increased serum ALT, AST and bilirubin

            Postmarketing Reports

            Urinary retention

            Angioedema of the face, lips, tongue, and larynx, with or without respiratory symptoms

            Nausea, constipation, diarrhea

            Pruritus

            Atrial fibrillation

            Dizziness, headache

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            Warnings

            Contraindications

            Hypersensitivity

            Cautions

            May increase blood pressure; monitor blood pressure periodically, especially in hypertensive patients; not recommended for use in severe uncontrolled hypertensive patients (defined as systolic blood pressure ≥180 mm Hg and/or diastolic blood pressure ≥110 mm Hg)

            Urinary retention may occur with bladder outlet obstruction or with concomitant antimuscarinic therapy; administer with caution in these patients

            Angioedema of the face, lips, tongue, and/or larynx reported; may occur after the first dose or following multiple doses; promptly discontinue and initiate appropriate therapy to ensure a patent airway

            Drug interactions overview

            • Appropriate monitoring is recommended and dose adjustment may be necessary for narrow therapeutic index CYP2D6 substrates
            • Coadministration of digoxin 0.25 mg with a combination of solifenacin 5 mg and mirabegron 50 mg increased digoxin AUC and peak plasma concentration by ~10% and 14%, respectively; for patients who are initiating a combination of mirabegron and digoxin, consider initiating lowest dose for digoxin; monitor serum digoxin concentrations and titrate digoxin dose to obtain the desired clinical effect
            • In studies, ketoconazole increased mirabegron peak plasma concentration by 45% and mirabegron AUC by 80% after multiple dose administration of 400 mg of ketoconazole for 9 days prior to the administration of a single dose of 100 mg mirabegron in 23 male and female healthy subjects
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            Pregnancy & Lactation

            Pregnancy

            There are no studies with the use in pregnant women to inform drug-associated risk for birth defects or miscarriage

            Animal data

            • Administration to pregnant animals during organogenesis resulted in reversible skeletal variations (in rats) at 22-fold (via AUC) the maximum recommended human dose (MRHD) of 50 mg/day and decreased fetal body weights (in rabbits) at 14-fold the MRHD
            • At maternally toxic exposures in rats (96-fold), decreased fetal weight and increased fetal mortality were observed and, in rabbits (36-fold), cardiac findings (fetal cardiomegaly and fetal dilated aortae) were observed

            Lactation

            There is no information on the presence of mirabegron in human milk, the effects on the breastfed child, or the effects on milk production

            Mirabegron-related material was present in rat milk and in the stomach of nursing pups following administrations of a single 10 mg/kg oral dose of 14C-labeled mirabegron to lactating rats

            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

            Beta-3 adrenergic receptor agonist which causes relaxation of the detrusor smooth muscle of the urinary bladder and increases bladder capacity

            Absorption

            Bioavailability: 29% (25-mg), 35% (50-mg)

            Peak Plasma Time: 3.5 hr

            Peak Plasma Concentration: ~3-fold increase from 50 mg dose to 100 mg dose

            AUC: ~2.5-fold increase from 50 mg dose to 100 mg dose

            Steady state: 7 days

            Distribution

            Protein Bound: 71%

            Vd, steady state: 1670 L

            Metabolism

            Via multiple pathways including dealkylation, (direct) glucuronidation, amide hydrolysis, and minimal oxidative metabolism in vivo by CYP2D6 and CYP3A4

            Possible involvement of butylcholinesterase, uridine diphospho-glucuronosyltransferases (UGT) and alcohol dehydrogenase

            Moderate CYP2D6 inhibitor

            Elimination

            Half-Life: 50 hr

            Total body clearance: 57 L/hr (following IV administration)

            Excretion: Urine (55%); feces (34%)

            Excretion, unchanged: Urine (~25%); feces (0%)

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            Administration

            Oral Administration

            May take with or without food

            Swallow whole with water, do not chew, divide, or crush tablet

            Storage

            Extended-release tablets: Store at 25°C (77°F) with excursions permitted from 15-30°C (59-86°F)

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            Formulary

            FormularyPatient Discounts

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            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.
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            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
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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.