Medication for overactive bladder
Mirabegron
Trade names Myrbetriq, Betanis, Betmiga, others Other names YM-178
AHFS /
Drugs.com
Monograph
MedlinePlus
a612038
License data
Pregnancy category
Routes of administration
By mouth
ATC code
Legal status
AU :
S4 (Prescription only)
UK :
POM (Prescription only)
[1]
US :
℞-only
[2]
EU : Rx-only
[3]
In general: ℞ (Prescription only)
Bioavailability 29–35%
[4]
Protein binding 71%
[4]
Metabolism
Liver via (direct) glucuronidation, amide hydrolysis, and minimal oxidative metabolism in vivo by
CYP2D6 and
CYP3A4 . Some involvement of butylcholinesterase
[4]
Elimination half-life 50 hours
[4]
Excretion Urine (55%), faeces (34%)
[4]
2-(2-Amino-1,3-thiazol-4-yl)-N -[4-(2-{[(2R )-2-hydroxy-2-phenylethyl]amino}ethyl)phenyl]acetamide
CAS Number
PubChem
CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard
100.226.392
Formula C 21 H 24 N 4 O 2 S
Molar mass 396.51 g·mol−1 3D model (
JSmol )
O=C(Nc1ccc(cc1)CCNC[C@H](O)c2ccccc2)Cc3nc(sc3)N
InChI=1S/C21H24N4O2S/c22-21-25-18(14-28-21)12-20(27)24-17-8-6-15(7-9-17)10-11-23-13-19(26)16-4-2-1-3-5-16/h1-9,14,19,23,26H,10-13H2,(H2,22,25)(H,24,27)/t19-/m0/s1
Key:PBAPPPCECJKMCM-IBGZPJMESA-N
Mirabegron , sold under the brand name Myrbetriq among others, is a
medication used to treat
overactive bladder .
[5] Its benefits are similar to
antimuscarinic medication such as
solifenacin or
tolterodine .
[6] It is taken by mouth.
[5]
Common side effects include
high blood pressure , headaches, and
urinary tract infections .
[5] Other significant side effects include
urinary retention ,
irregular heart rate , and
angioedema .
[5]
[7] It works by activating the
β3 adrenergic receptor in the
bladder , resulting in its relaxation.
[5]
[7]
Mirabegron is the first clinically available
beta-3 agonist with approval for use in adults with
overactive bladder . Mirabegron was approved for medical use in the United States and in the European Union in 2012.
[8]
[9]
[3] In 2021, it was the 200th most commonly prescribed medication in the United States, with more than 2 million prescriptions.
[10]
[11] It is available as a
generic medication .
[12]
In the United Kingdom it is less preferred to antimuscarinic medication such as
oxybutynin .
[7]
Medical uses
Mirabegron is used is in the treatment of
overactive bladder .
[13]
[4]
[2]
[1] It works equally well to
antimuscarinic medication such as
solifenacin or
tolterodine .
[6]
[3] In the United Kingdom it is less preferred to these agents.
[7]
Mirabegron is also indicated to treat neurogenic detrusor overactivity (NDO), a bladder dysfunction related to neurological impairment, in children ages three years and older.
[13]
Adverse effects
Adverse effects by incidence:
[4]
[2]
[1]
Very common (>10% incidence) adverse effects include:
Common (1–10% incidence) adverse effects include:
Rare (<1% incidence) adverse effects include:
Palpitations
Blurred vision
Glaucoma
Indigestion
Gastritis
Abdominal distension
Rhinitis
Elevations in liver enzymes (
GGTP ,
AST ,
ALT and
LDH )
Renal and urinary disorders (e.g.,
nephrolithiasis , bladder pain)
Reproductive system disorders (e.g., vulvovaginal pruritus, vaginal infection)
Skin and subcutaneous tissue disorders (e.g., urticaria, leukocytoclastic vasculitis, rash, pruritus, purpura, lip edema)
Stevens–Johnson syndrome associated with increased serum ALT, AST and bilirubin
Urinary retention
Research
As a selective beta-3
adrenergic agonist , mirabegron does not cause the cardiovascular adverse effects of other adrenergic agonists that are active at the
beta-1 and
beta-2 adrenergic receptors . Beta-3 adrenergic agonists activate
brown adipose tissue (BAT) and increase
energy expenditure , leading to research interest in their development as
weight loss drugs .
[14] A combination of mirabegron and
metformin was studied in mice and caused greater weight loss than either drug alone.
[15] A human study in obese individuals found an increase in
insulin sensitivity but no significant weight change, which was hypothesized to be due to low levels of BAT in obese humans and/or the low dose of mirabegron used in the study.
[16]
References
^
a
b
c
"Betmiga 25mg & 50mg prolonged-release tablets" . electronic Medicines Compendium . Astellas Pharma Ltd. 22 February 2013. Archived from
the original on 2 April 2015. Retrieved 17 November 2013 .
^
a
b
c
"Myrbetriq- mirabegron tablet, film coated, extended release" . DailyMed . Retrieved 27 March 2021 .
^
a
b
c
"Betmiga EPAR" .
European Medicines Agency . 17 September 2018. Retrieved 28 April 2020 . Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
^
a
b
c
d
e
f
g
"mirabegron (Rx) - Myrbetriq" . Medscape Reference . WebMD. Retrieved 17 November 2013 .
^
a
b
c
d
e
"Mirabegron Monograph for Professionals" . Drugs.com . American Society of Health-System Pharmacists. Retrieved 18 March 2019 .
^
a
b
"[93] Are claims for newer drugs for overactive bladder warranted?" . Therapeutics Initiative . 22 April 2015. Retrieved 17 March 2019 .
^
a
b
c
d British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 763.
ISBN
9780857113382 .
^
"Drug Approval Package: Myrbetriq (mirabegron) Extended Release Tablets NDA #202611" . U.S.
Food and Drug Administration (FDA) . 10 August 2012. Retrieved 28 April 2020 .
^ Sacco E, Bientinesi R, Tienforti D, Racioppi M, Gulino G, D'Agostino D, et al. (April 2014). "Discovery history and clinical development of mirabegron for the treatment of overactive bladder and urinary incontinence". Expert Opinion on Drug Discovery . 9 (4): 433–448.
doi :
10.1517/17460441.2014.892923 .
PMID
24559030 .
S2CID
26424400 .
^
"The Top 300 of 2021" . ClinCalc .
Archived from the original on 15 January 2024. Retrieved 14 January 2024 .
^
"Mirabegron - Drug Usage Statistics" . ClinCalc . Retrieved 14 January 2024 .
^
"2022 First Generic Drug Approvals" . U.S.
Food and Drug Administration (FDA) . 3 March 2023.
Archived from the original on 30 June 2023. Retrieved 30 June 2023 .
^
a
b
"FDA Approves New indication for Drug to Treat Neurogenic Detrusor Overactivity in Pediatric Patients" . U.S.
Food and Drug Administration (FDA) (Press release). 25 March 2021. Retrieved 26 March 2021 . This article incorporates text from this source, which is in the
public domain .
^ Hainer V (November 2016). "Beta3-adrenoreceptor agonist mirabegron - a potential antiobesity drug?". Expert Opinion on Pharmacotherapy . 17 (16): 2125–2127.
doi :
10.1080/14656566.2016.1233177 .
PMID
27600952 .
S2CID
1308773 .
^ Zhao XY, Liu Y, Zhang X, Zhao BC, Burley G, Yang ZC, et al. (April 2023).
"The combined effect of metformin and mirabegron on diet-induced obesity" . MedComm . 4 (2): e207.
doi :
10.1002/mco2.207 .
PMC
9928947 .
PMID
36818016 .
^ Dehvari N, Sato M, Bokhari MH, Kalinovich A, Ham S, Gao J, et al. (October 2020).
"The metabolic effects of mirabegron are mediated primarily by β3 -adrenoceptors" . Pharmacology Research & Perspectives . 8 (5): e00643.
doi :
10.1002/prp2.643 .
PMC
7437350 .
PMID
32813332 .
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