mirabegron (Rx)

Brand and Other Names:Myrbetriq
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet, extended-release

  • 25mg
  • 50mg

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

  • Mild-to-moderate (eGFR ≥30 mL/min/1.73 m2): No dosage adjustment required
  • Severe (eGFR 15-29 mL/min/1.73 m2): Not to exceed 25 mg/day
  • eGFR <15mL/min/1.73 m2 or on dialysis: Not recommended

Hepatic impairment

  • Mild (Child-Pugh A): No dosage adjustment required
  • Moderate (Child-Pugh B): Not to exceed 25 mg/day for either starting or maximum dose
  • Severe (Child Pugh C): Not recommended

Dosing Considerations

Granules and tablets are 2 different products and are not substitutable on a milligram-per-milligram basis

Recommended dosage for granules in adults has not been determined

Dosage Forms & Strengths

tablet, extended-release

  • 25mg
  • 50mg

granules for extended-release oral suspension

  • 8mg/mL after reconstitution

Neurogenic Detrusor Overactivity

Indicated for neurogenic detrusor overactivity (NDO) in children aged 3 years and older

<3 years: Safety and efficacy not established

Aged ≥3 years, weight <35 kg

  • Granules for oral suspension
    • 11 kg to <22 kg: 24 mg (3 mL) PO qDay initially; may increase to maximum of 48 mg/day (6 mL)
    • 22 kg to <35 kg: 32 mg (4 mL) PO qDay initially; may increase to maximum of 64 mg/day (8 mL)

Aged ≥3 years, weight ≥35 kg

  • Tablets: 25 mg PO qDay initially; may increase to maximum of 50 mg/day after 4-8 weeks
  • Granules for oral suspension: 48 mg (6 mL) PO qDay initially; may increase to maximum of 80 mg/day (10 mL) after 4-8 weeks

Dosage Modifications

Renal impairment <35 kg

  • Granules for oral suspension
  • eGFR >30 mL/min/1.73 m2: No dosage adjustment required
  • eGFR 15-29 mL/min/1.73 m2
    • 11 kg to <22 kg: Not to exceed 24 mg (3 mL) for either starting or maximum dose
    • 22 kg to <35 kg: Not to exceed 32 mg (4 mL) for either starting or maximum dose
  • eGFR <15 mL/min/1.73 m2 or on dialysis: Not recommended

Renal impairment ≥35 kg

  • Granules for oral suspension
    • eGFR ≥30 mL/min/1.73 m2: No dosage adjustment required
    • eGFR 15-29 mL/min/1.73 m2: 48 mg (6 mL) for either starting or maximum dose
    • eGFR <15 mL/min/1.73 m2 or on dialysis: Not recommended
  • Tablets
    • eGFR ≥30 mL/min/1.73 m2: No dosage adjustment required
    • eGFR 15-29 mL/min/1.73 m2: 25 mg for either starting or maximum dose
    • eGFR <15 mL/min/1.73 m2 or on dialysis: Not recommended

Hepatic impairment <35 kg

  • Granules for oral suspension
  • Mild (Child-Pugh A): No dosage adjustment required
  • Moderate (Child-Pugh B)
    • 11 kg to <22 kg: Not to exceed 24 mg (3 mL) for either starting or maximum dose
    • 22 kg to <35 kg: Not to exceed 32 mg (4 mL) for either starting or maximum dose
  • Severe (Child-Pugh C): Not recommended

Hepatic impairment ≥35 kg

  • Granules for oral suspension
    • Mild (Child-Pugh A): No dosage adjustment required
    • Moderate (Child-Pugh B): Not to exceed 48 mg (6 mL) for either starting or maximum dose
    • Severe (Child Pugh C): Not recommended
  • Tablets
    • Mild (Child-Pugh A): No dosage adjustment required
    • Moderate (Child-Pugh B): Not to exceed 25 mg/day for either starting or maximum dose
    • Severe (Child Pugh C): Not recommended

Dosing Considerations

Granules and tablets are 2 different products and are not substitutable on a milligram-per-milligram basis

Select recommended product based on the indication and child’s weight

Do not combine tablets and granules to achieve a total dose

Recommended dosage for granules in adults has not been determined

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Interactions

Interaction Checker

and mirabegron

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    Contraindicated

      Serious - Use Alternative

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            Adverse Effects

            >10%

            Adults

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

            Children aged 3-17 years

            • Urinary tract infection (24.4%)

            1-10%

            Adults

            • 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%)

            Children aged 3-17 years

            • Nasopharyngitis (5.8%)
            • Constipation (4.7%)
            • Headache (3.5%)
            • Nausea (2.3%)
            • Gastroenteritis (2.3%)
            • Rhinitis (2.3%)
            • Cough (2.3%)

            <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

            Cardiac disorders: Atrial fibrillation

            Gastrointestinal disorders: Nausea, constipation, diarrhea

            Nervous system disorders: Dizziness, headache

            Skin and subcutaneous tissue disorders: Angioedema of the face, lips, tongue, and larynx, with or without respiratory symptoms; pruritus

            Renal and urinary disorders: Urinary retention

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            Warnings

            Contraindications

            Hypersensitivity

            Cautions

            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

            Increased blood pressure

            • May increase blood pressure (BP); monitor BP periodically, especially in hypertensive patients
            • Not recommended for use in severe uncontrolled hypertensive patients (ie, systolic BP ≥180 mm Hg and/or diastolic BP ≥110 mm Hg for adults; systolic and/or diastolic BP >99th percentile plus 5 mm Hg for age, sex, and stature for children)
            • BP increases may be larger in children aged 3 to <12 years compared with adolescents

            Drug interactions overview

            Moderate CYP2D6 inhibitor

            • Sensitive CYP2D6 substrates
              • Appropriate monitoring is recommended and dose adjustment may be necessary for narrow therapeutic index CYP2D6 substrates
            • Digoxin
              • Modify dose
              • 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
              • Consider initiating lowest dose for digoxin; monitor serum digoxin concentrations and titrate digoxin dose to obtain desired clinical effect
            • Concomitant antimuscarinic drugs
              • Use with caution
              • Urinary retention may occur with bladder outlet obstruction or with concomitant antimuscarinic therapy
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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

            Adults (tablets)

            • 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
            • Effect of food: No clinically significant differences in adults

            Pediatrics (tablets or oral suspension)

            • Peak plasma time: 4-5 hr (single dose); 3-4 hr (steady-state)
            • Effect of food
              • Tablets: AUC increased by 120% in fasted stated compared to the fed state
              • Oral suspension: Peak plasma concentration and AUC increased by 170% and 80%, respectively, in fasted stated compared to the fed state

            Distribution

            Adults (tablets)

            • Protein Bound: 71%
            • Vd, steady state: 1670 L

            Pediatrics (tablets or oral suspension)

            • Vd: 4895-13,726 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

            Adults (tablets)

            • Half-Life: 50 hr
            • Total body clearance: 57 L/hr (following IV administration)
            • Excretion: Urine (55%); feces (34%)
            • Excretion, unchanged: Urine (~25%); feces (0%)

            Pediatrics (tablets or oral suspension)

            • Half-life: ~26-31 hr
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            Administration

            Oral Suspension Preparation

            Prepare oral suspension at time of dispensing

            Keep bottle in pouch until time of reconstitution

            Reconstitution

            • Discard pouch and desiccant before reconstitution; do not dispense
            • Tap closed bottle several times to loosen granules
            • Add 100 mL of water to bottle, and immediately shake vigorously for 1 minute, then let it stand for 10-30 minutes; shake vigorously again for 1 minute
            • If granules have not dispersed, shake vigorously for another 1 minute
            • Record 28-day expiration date on container and carton based on reconstitution date
            • Dispense with an appropriate dosing measuring device
            • Reconstituted suspension contains 8 mg/mL

            Oral Administration

            Tablets

            • Adults: May take with or without food
            • Children: Take with food to reduce potential exposure-related risks (eg, increased heart rate)
            • Swallow tablet whole with water, do not chew, divide, or crush

            Oral suspension

            • For pediatric use only; dosage for adults not determined
            • Take with food to reduce potential exposure-related risks (eg, increased heart rate)

            Missed dose

            • <12 hours since missed dose: Take as soon as remembered
            • >12 hours since missed dose: Skip dose and take next dose at usual time

            Storage

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

            Reconstituted oral granules for suspension

            • Store at 20-25ºC (68-77ºF) for up to 28 days
            • Discard unused portion after 28 days
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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.
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            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the 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.