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Mirabegron

Medically reviewed by Drugs.com. Last updated on Jul 28, 2020.

Pronunciation

(mir a BEG ron)

Index Terms

  • YM-178

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet Extended Release 24 Hour, Oral:

Myrbetriq: 25 mg, 50 mg

Brand Names: U.S.

  • Myrbetriq

Pharmacologic Category

  • Beta3 Agonist

Pharmacology

Mirabegron, a beta-3 adrenergic receptor agonist, activates beta-3 adrenergic receptors in the bladder resulting in relaxation of the detrusor smooth muscle during the urine storage phase, thus increasing bladder capacity. At usual doses, mirabegron is believed to display selectivity for the beta-3 adrenergic receptor subtype compared to its affinity for the beta-1 and -2 adrenoceptor subtypes. Data have shown that beta-adrenoceptors, predominately the beta-3 subtype, mediate detrusor smooth muscle tone and promote the storage function of the human bladder.

Distribution

Vss: ~1670 L (following IV administration)

Metabolism

Extensive metabolism via multiple pathways (eg, dealkylation, oxidation, glucuronidation, amide hydrolysis) via multiple enzymes (eg, UGT, esterase, CYP3A4, CYP2D6); two major pharmacologically inactive metabolites produced

Excretion

Urine (radiolabeled drug: 55%; unchanged drug: ~25%); feces (radiolabeled drug: 34%; unchanged drug: 0%)

Onset of Action

Efficacy is seen within 8 weeks; steady state achieved within 7 days

Time to Peak

~3.5 hours

Half-Life Elimination

~50 hours

Protein Binding

~71%; binds mainly to albumin and alpha1-acid glycoprotein

Special Populations: Renal Function Impairment

Following single dose administration of mirabegron 100 mg in volunteers with mild renal impairment (estimated glomerular filtration rate [eGFR] 60 to 89 mL/minute/1.73 m2 as estimated by modification of diet in renal disease), mean mirabegron Cmax and AUC were increased by 6% and 31% relative to volunteers with normal renal function. In volunteers with moderate renal impairment (eGFR 30 to 59 mL/minute/1.73 m2), Cmax and AUC were increased by 23% and 66%, respectively. In patients with severe renal impairment (eGFR 15 to 29 mL/minute/1.73 m2), mean Cmax and AUC values were 92% and 118% higher compared with healthy subjects with normal renal function.

Special Populations: Hepatic Function Impairment

Following single-dose administration of mirabegron 100 mg in volunteers with mild hepatic impairment (Child-Pugh class A), mean mirabegron Cmax and AUC were increased by 9% and 19% relative to volunteers with normal hepatic function. In volunteers with moderate hepatic impairment (Child-Pugh class B), mean Cmax and AUC values were 175% and 65% higher.

Special Populations: Gender

The Cmax and AUC of mirabegron were approximately 40% to 50% higher in females than in males. When corrected for differences in body weight, the mirabegron systemic exposure is 20% to 30% higher in females compared with males.

Use: Labeled Indications

Overactive bladder: Treatment of overactive bladder (OAB) with symptoms of urinary frequency, urgency, or urge urinary incontinence as monotherapy or in combination with solifenacin

Contraindications

Hypersensitivity to mirabegron or any component of the formulation

Canadian labeling: Additional contraindications (not in US labeling): Severe uncontrolled hypertension (systolic blood pressure ≥180 mm Hg and/or diastolic blood pressure ≥110 mm Hg); pregnancy

Dosing: Adult

Overactive bladder (OAB): Oral: Initial: 25 mg once daily; efficacy is observed within 8 weeks for 25 mg dose. May increase to 50 mg once daily based on individual patient efficacy and tolerability.

Concomitant use with solifenacin: Initial: 25 mg once daily with solifenacin 5 mg once daily. May increase mirabegron dose to 50 mg once daily after 4 to 8 weeks.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Geriatric

Refer to adult dosing.

Administration

Administer without regard to food. Swallow the tablet whole with water; do not chew, divide, or crush.

Bariatric surgery: Tablet, extended release: Some institutions may have specific protocols that conflict with these recommendations; refer to institutional protocols as appropriate. No IR formulation is available. If safety and efficacy can be effectively monitored, no change in formulation or administration is required after bariatric surgery.

Storage

Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).

Drug Interactions

Ajmaline: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Ajmaline. Monitor therapy

Amitriptyline: CYP2D6 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of Amitriptyline. CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Amitriptyline. Monitor therapy

Amoxapine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Amoxapine. Monitor therapy

Amphetamines: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Amphetamines. Management: Monitor for amphetamine toxicities (including serotonin syndrome) if used with a moderate CYP2D6 inhibitor. Initiate amphetamine therapy at lower doses, monitor frequently, and adjust doses as needed. Discontinue amphetamines if serotoinin syndrome occurs Monitor therapy

Anticholinergic Agents: May enhance the adverse/toxic effect of Mirabegron. Monitor therapy

ARIPiprazole: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of ARIPiprazole. Management: Monitor for increased aripiprazole pharmacologic effects. Aripiprazole dose adjustments may or may not be required based on concomitant therapy, indication, or dosage form. Consult full interaction monograph for specific recommendations. Monitor therapy

ARIPiprazole Lauroxil: CYP2D6 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of ARIPiprazole Lauroxil. Monitor therapy

AtoMOXetine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of AtoMOXetine. Monitor therapy

Brexpiprazole: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Brexpiprazole. Management: If brexpiprazole is to be used together with both a moderate CYP2D6 inhibitor and a strong or moderate CYP3A4 inhibitor, the brexpiprazole dose should be reduced to 25% of the usual dose when treating indications other than major depressive disorder. Monitor therapy

Carvedilol: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Carvedilol. Monitor therapy

ClomiPRAMINE: CYP2D6 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of ClomiPRAMINE. CYP2D6 Inhibitors (Moderate) may increase the serum concentration of ClomiPRAMINE. Monitor therapy

CloZAPine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of CloZAPine. Monitor therapy

Codeine: CYP2D6 Inhibitors (Moderate) may diminish the therapeutic effect of Codeine. These CYP2D6 inhibitors may prevent the metabolic conversion of codeine to its active metabolite morphine. Monitor therapy

Desipramine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Desipramine. Monitor therapy

Deutetrabenazine: CYP2D6 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of Deutetrabenazine. Monitor therapy

Dextromethorphan: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Dextromethorphan. Monitor therapy

Digoxin: Mirabegron may increase the serum concentration of Digoxin. Management: Consider using the lowest dose of digoxin when initiating concurrent mirabegron. Monitor serum digoxin concentrations closely to help guide digoxin dosing. Consider therapy modification

Doxepin (Systemic): CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Doxepin (Systemic). Monitor therapy

Doxepin (Topical): CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Doxepin (Topical). Monitor therapy

DOXOrubicin (Conventional): CYP2D6 Inhibitors (Moderate) may increase the serum concentration of DOXOrubicin (Conventional). Avoid combination

Eliglustat: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Eliglustat. Management: Eliglustat dose is 84 mg daily with CYP2D6 inhibitors. Use is contraindicated (COI) when also combined with strong CYP3A4 inhibitors. When also combined with a moderate CYP3A4 inhibitor, use is COI in CYP2D6 EMs or IMs and should be avoided in CYP2D6 PMs. Consider therapy modification

Flecainide: Mirabegron may increase the serum concentration of Flecainide. Management: Monitor clinical response to flecainide closely. Dose adjustment may be necessary. Canadian mirabegron labeling recommends restricting the maximum adult mirabegron dose to 25 mg/day in patients receiving flecainide. Monitor therapy

Haloperidol: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Haloperidol. Monitor therapy

Iloperidone: CYP2D6 Inhibitors (Moderate) may decrease serum concentrations of the active metabolite(s) of Iloperidone. Specifically, concentrations of the metabolite P95 may be decreased. CYP2D6 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of Iloperidone. Specifically, concentrations of the metabolite P88 may be increased. CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Iloperidone. Monitor therapy

Imipramine: CYP2D6 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of Imipramine. Concentrations of desipramine may be increased. CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Imipramine. Monitor therapy

Indoramin: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Indoramin. Monitor therapy

Ketoconazole (Systemic): May increase the serum concentration of Mirabegron. Monitor therapy

Lofepramine: CYP2D6 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of Lofepramine. The active metabolite of lofepramine is desipramine. Monitor therapy

Mequitazine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Mequitazine. Avoid combination

Metoclopramide: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Metoclopramide. Monitor therapy

Metoprolol: Mirabegron may diminish the antihypertensive effect of Metoprolol. Mirabegron may increase the serum concentration of Metoprolol. Monitor therapy

Nebivolol: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Nebivolol. Monitor therapy

Nortriptyline: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Nortriptyline. Monitor therapy

Oliceridine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Oliceridine. Monitor therapy

Olmutinib: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Olmutinib. Monitor therapy

PARoxetine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of PARoxetine. Monitor therapy

Perhexiline: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Perhexiline. Monitor therapy

Perphenazine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Perphenazine. Monitor therapy

Pimozide: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Pimozide. Monitor therapy

Pitolisant: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Pitolisant. Monitor therapy

Propafenone: Mirabegron may increase the serum concentration of Propafenone. Management: Monitor clinical response to propafenone closely. Dose adjustment may be necessary. Canadian mirabegron labeling recommends restricting the maximum adult mirabegron dose to 25 mg/day in patients receiving propafenone. Monitor therapy

Propranolol: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Propranolol. Monitor therapy

Protriptyline: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Protriptyline. Monitor therapy

RifAMPin: May decrease the serum concentration of Mirabegron. Monitor therapy

RisperiDONE: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of RisperiDONE. Monitor therapy

Solifenacin: Mirabegron may enhance the adverse/toxic effect of Solifenacin. Specifically, the risk of acute urinary retention may be enhanced. Monitor therapy

Tamoxifen: CYP2D6 Inhibitors (Moderate) may decrease serum concentrations of the active metabolite(s) of Tamoxifen. Specifically, CYP2D6 inhibitors may decrease the metabolic formation of highly potent active metabolites. Management: Consider alternatives to the use of moderate CYP2D6 inhibitors with tamoxifen when possible, as the combination may be associated with reduced clinical effectiveness of tamoxifen. Consider therapy modification

Tamsulosin: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Tamsulosin. Monitor therapy

Tetrabenazine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Tetrabenazine. Specifically, concentrations of the active alpha- and beta-dihydrotetrabenazine metabolites may be increased. Monitor therapy

Thioridazine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Thioridazine. Avoid combination

Timolol (Systemic): CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Timolol (Systemic). Monitor therapy

TraMADol: CYP2D6 Inhibitors (Moderate) may decrease serum concentrations of the active metabolite(s) of TraMADol. CYP2D6 Inhibitors (Moderate) may increase the serum concentration of TraMADol. Monitor therapy

Trimipramine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Trimipramine. Monitor therapy

Valbenazine: CYP2D6 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of Valbenazine. Monitor therapy

Vortioxetine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Vortioxetine. Monitor therapy

Zuclopenthixol: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Zuclopenthixol. Monitor therapy

Adverse Reactions

>10%: Cardiovascular: Hypertension (9% to 11%)

1% to 10%:

Cardiovascular: Tachycardia (2%)

Central nervous system: Headache (2% to 4%), dizziness (1% to 3%)

Gastrointestinal: Constipation (1% to 3%), xerostomia (4%), diarrhea (2%), abdominal pain (1%)

Genitourinary: Urinary tract infection (3% to 6%), cystitis (2%)

Infection: Influenza (3%)

Neuromuscular & skeletal: Back pain (3%), arthralgia (2%)

Respiratory: Nasopharyngitis (4%), sinusitis (3%)

<1%, postmarketing, and/or case reports: Abdominal distension, angioedema, anxiety, atrial fibrillation, bladder pain, blurred vision, breast cancer, cerebrovascular accident, confusion, dry eye syndrome, dyspepsia, gastritis, elevated gamma-glutamyl transferase, genital pruritus, glaucoma, hallucination, hypersensitivity angiitis, increased lactate dehydrogenase, increased serum alanine aminotransferase, increased serum aspartate aminotransferase, insomnia, lip edema, malignant neoplasm of lung, malignant neoplasm of prostate, nausea, nephrolithiasis, nonthrombocytopenic purpura, osteoarthritis, palpitations, pruritus, rhinitis, skin rash, urinary retention, urticaria, vaginal infection

Warnings/Precautions

Concerns related to adverse effects:

• Angioedema: Angioedema of the face, lips, tongue, and/or larynx has been reported; some cases have occurred after the first dose. May be life-threatening. Immediately discontinue and institute supportive care if the tongue, hypopharynx, or larynx is involved.

• Blood pressure effects: Dose-related increases in blood pressure have been reported; monitor blood pressure periodically during therapy. Not recommended in patients with severe uncontrolled hypertension (SBP ≥180 and/or DBP ≥110 mm Hg); if used in patients with controlled and less severe hypertension, use with caution and monitor blood pressure closely; exacerbation of preexisting hypertension has been infrequently reported.

Disease-related concerns:

• Bladder flow obstruction: Use with caution in patients with bladder outlet obstruction (BOO) and in patients using concomitant muscarinic antagonists; the risk of urinary retention may be increased.

• Hepatic impairment: Use with caution in patients with mild to moderate hepatic impairment; dosage adjustment is required in patients with moderate hepatic impairment. Use is not recommended in severe hepatic impairment.

• QT prolongation: Use with caution in patients with a history of QT interval prolongation or those receiving medications known to prolong the QT interval. In one thorough QT study, supratherapeutic doses prolonged the QTc interval based on the individual subject-specific correction method (QTcI) in females but not in males (Malik 2012). In general, mirabegron at the recommended dose has a low risk of QT interval prolongation (Sanford 2013).

• Renal impairment: Use with caution in patients with renal impairment; dosage adjustment is required in patients with severe renal impairment. Use is not recommended in ESRD.

Monitoring Parameters

Monitor blood pressure at baseline and then periodically during therapy; signs and symptoms of urinary retention

Pregnancy Considerations

Adverse effects have been observed in some animal reproduction studies.

Patient Education

What is this drug used for?

• It is used to treat an overactive bladder.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Dry mouth

• Flu-like signs

• Back pain

• Joint pain

• Constipation

• Stuffy nose

• Sore throat

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Urinary tract infection like blood in the urine, burning or painful urination, passing a lot of urine, fever, lower abdominal pain, or pelvic pain.

• Fast heartbeat

• Abnormal heartbeat

• Bladder irritation

• Swelling in your throat

• Vision changes

• Severe dizziness

• Passing out

• Severe headache

• Difficult urination

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.