Dosing & Uses
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
- 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
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
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
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
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.
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%)
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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Patient Handout
Formulary
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