Mirabegron
{{Short description|Medication for overactive bladder}}
{{Use dmy dates|date=April 2020}}
{{Drugbox
| image = Mirabegron.svg
| width = 300
| alt =
| tradename = Myrbetriq, Betanis, Betmiga, others
| Drugs.com = {{drugs.com|monograph|mirabegron}}
| MedlinePlus = a612038
| DailyMedID = Mirabegron
| pregnancy_AU = B3
| pregnancy_category =
| routes_of_administration = By mouth
| ATC_prefix = G04
| ATC_suffix = BD12
| legal_AU = S4
| legal_CA =
| legal_UK = POM
| legal_US = Rx-only
| legal_EU = Rx-only
| legal_status = Rx-only
| metabolism = Liver via (direct) glucuronidation, amide hydrolysis, and minimal oxidative metabolism in vivo by CYP2D6 and CYP3A4. Some involvement of butylcholinesterase
| elimination_half-life = 50 hours
| excretion = Urine (55%), faeces (34%)
| CAS_number = 223673-61-8
| PubChem = 9865528
| ChemSpiderID = 8041219
| DrugBank = DB08893
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = MVR3JL3B2V
| KEGG = D09535
| ChEBI = 65349
| ChEMBL = 2095212
| synonyms = YM-178
| IUPAC_name = 2-(2-Amino-1,3-thiazol-4-yl)-N-[4-(2-
| C=21 | H=24 | N=4 | O=2 | S=1
| smiles = O=C(Nc1ccc(cc1)CCNC[C@H](O)c2ccccc2)Cc3nc(sc3)N
| StdInChI = 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
| StdInChIKey = PBAPPPCECJKMCM-IBGZPJMESA-N
}}
Mirabegron, sold under the brand name Myrbetriq among others, is a medication used to treat overactive bladder. Its benefits are similar to antimuscarinic medication such as solifenacin or tolterodine.{{cite web |title=[93] Are claims for newer drugs for overactive bladder warranted? |url=https://www.ti.ubc.ca/2015/04/22/are-claims-for-newer-drugs-for-overactive-bladder-warranted/ |website=Therapeutics Initiative |access-date=17 March 2019 |date=22 April 2015}} It is taken by mouth.{{cite web |title=Mirabegron Monograph for Professionals |url=https://www.drugs.com/monograph/mirabegron.html |website=Drugs.com |publisher=American Society of Health-System Pharmacists |access-date=18 March 2019}}
Common side effects include high blood pressure, headaches, and urinary tract infections. Other significant side effects include urinary retention, irregular heart rate, and angioedema. It works by activating the β3 adrenergic receptor in the bladder, resulting in its relaxation.{{cite book|title=British national formulary : BNF 76|date=2018|publisher=Pharmaceutical Press|isbn=9780857113382|pages=763|edition=76}}
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.{{cite web | title=Drug Approval Package: Myrbetriq (mirabegron) Extended Release Tablets NDA #202611 | website=U.S. Food and Drug Administration (FDA) | date=10 August 2012 | url=https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202611Orig1s000TOC.cfm | access-date=28 April 2020}}{{cite journal | vauthors = Sacco E, Bientinesi R, Tienforti D, Racioppi M, Gulino G, D'Agostino D, Vittori M, Bassi P | display-authors = 6 | title = Discovery history and clinical development of mirabegron for the treatment of overactive bladder and urinary incontinence | journal = Expert Opinion on Drug Discovery | volume = 9 | issue = 4 | pages = 433–448 | date = April 2014 | pmid = 24559030 | doi = 10.1517/17460441.2014.892923 | s2cid = 26424400 }}{{cite web | title=Betmiga EPAR | website=European Medicines Agency | date=17 September 2018 | url=https://www.ema.europa.eu/en/medicines/human/EPAR/betmiga | access-date=28 April 2020}} Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged. In 2022, it was the 222nd most commonly prescribed medication in the United States, with more than 1{{nbsp}}million prescriptions.{{cite web | title=The Top 300 of 2022 | url=https://clincalc.com/DrugStats/Top300Drugs.aspx | website=ClinCalc | access-date=30 August 2024 | archive-date=30 August 2024 | archive-url=https://web.archive.org/web/20240830202410/https://clincalc.com/DrugStats/Top300Drugs.aspx | url-status=live }}{{cite web | title = Mirabegron Drug Usage Statistics, United States, 2013 - 2022 | website = ClinCalc | url = https://clincalc.com/DrugStats/Drugs/Mirabegron | access-date = 30 August 2024 }} It is available as a generic medication.{{cite web | title=2022 First Generic Drug Approvals | website=U.S. Food and Drug Administration (FDA) | date=3 March 2023 | url=https://www.fda.gov/drugs/drug-and-biologic-approval-and-ind-activity-reports/2022-first-generic-drug-approvals | archive-url=https://web.archive.org/web/20230630003602/https://www.fda.gov/drugs/drug-and-biologic-approval-and-ind-activity-reports/2022-first-generic-drug-approvals | archive-date=30 June 2023 | url-status=dead | access-date=30 June 2023}}
In the United Kingdom it is less preferred to antimuscarinic medication such as oxybutynin.
Medical uses
Mirabegron is used is in the treatment of overactive bladder.{{cite web|title=mirabegron (Rx) - Myrbetriq|work=Medscape Reference|publisher=WebMD|access-date=17 November 2013|url=http://reference.medscape.com/drug/myrbetriq-mirabegron-999757}}{{cite web | title=Myrbetriq- mirabegron tablet, film coated, extended release | website=DailyMed | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ba9e9e15-e666-4c56-9271-2e24739cfa2d | access-date=27 March 2021}}{{cite web|title=Betmiga 25mg & 50mg prolonged-release tablets|work=electronic Medicines Compendium|publisher=Astellas Pharma Ltd|date=22 February 2013|access-date=17 November 2013|url=http://www.medicines.org.uk/emc/medicine/27429/SPC/Betmiga+25mg+%26+50mg+prolonged-release+tablets/|archive-url=https://web.archive.org/web/20150402091107/http://www.medicines.org.uk/emc/medicine/27429/SPC/Betmiga+25mg+%26+50mg+prolonged-release+tablets/|archive-date=2 April 2015|url-status=dead}} It works equally well to antimuscarinic medication such as solifenacin or tolterodine. In the United Kingdom it is less preferred to these agents.
Mirabegron is also indicated to treat neurogenic detrusor overactivity (NDO), a bladder dysfunction related to neurological impairment, in children ages three years and older.{{cite press release | title=FDA Approves New indication for Drug to Treat Neurogenic Detrusor Overactivity in Pediatric Patients | website=U.S. Food and Drug Administration (FDA) | date=25 March 2021 | url=https://www.fda.gov/news-events/press-announcements/fda-approves-new-indication-drug-treat-neurogenic-detrusor-overactivity-pediatric-patients | archive-url=https://web.archive.org/web/20210325211456/https://www.fda.gov/news-events/press-announcements/fda-approves-new-indication-drug-treat-neurogenic-detrusor-overactivity-pediatric-patients | url-status=dead | archive-date=25 March 2021 | access-date=26 March 2021}} {{PD-notice}}
Adverse effects
Very common (>10% incidence) adverse effects include:
Common (1–10% incidence) adverse effects include:
- Dry mouth
- Nasopharyngitis
- Urinary tract infection (UTI)
- Headache
- Influenza
- Constipation
- Dizziness
- Joint pain
- Cystitis
- Back pain
- Upper respiratory tract infection (URTI)
- Sinusitis
- Diarrhea
- High heart rate
- Fatigue
- Abdominal pain
- Neoplasms (cancers)
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.{{cite journal | vauthors = Hainer V | title = Beta3-adrenoreceptor agonist mirabegron - a potential antiobesity drug? | journal = Expert Opinion on Pharmacotherapy | volume = 17 | issue = 16 | pages = 2125–2127 | date = November 2016 | pmid = 27600952 | doi = 10.1080/14656566.2016.1233177 | s2cid = 1308773 }} A combination of mirabegron and metformin was studied in mice and caused greater weight loss than either drug alone.{{cite journal | vauthors = Zhao XY, Liu Y, Zhang X, Zhao BC, Burley G, Yang ZC, Luo Y, Li AQ, Zhang RX, Liu ZY, Shi YC, Wang QP | display-authors = 6 | title = The combined effect of metformin and mirabegron on diet-induced obesity | journal = MedComm | volume = 4 | issue = 2 | pages = e207 | date = April 2023 | pmid = 36818016 | doi = 10.1002/mco2.207 | pmc = 9928947 }} 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.{{cite journal | vauthors = Dehvari N, Sato M, Bokhari MH, Kalinovich A, Ham S, Gao J, Nguyen HT, Whiting L, Mukaida S, Merlin J, Chia LY, Wootten D, Summers RJ, Evans BA, Bengtsson T, Hutchinson DS | display-authors = 6 | title = The metabolic effects of mirabegron are mediated primarily by β3 -adrenoceptors | journal = Pharmacology Research & Perspectives | volume = 8 | issue = 5 | pages = e00643 | date = October 2020 | pmid = 32813332 | doi = 10.1002/prp2.643 | pmc = 7437350 }}
References
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Further reading
{{refbegin}}
- {{cite journal | vauthors = Sacco E, Bientinesi R | title = Mirabegron: a review of recent data and its prospects in the management of overactive bladder | journal = Therapeutic Advances in Urology | volume = 4 | issue = 6 | pages = 315–324 | date = December 2012 | pmid = 23205058 | pmc = 3491758 | doi = 10.1177/1756287212457114 }}
- {{cite journal | vauthors = Tyagi P, Tyagi V, Chancellor M | title = Mirabegron: a safety review | journal = Expert Opinion on Drug Safety | volume = 10 | issue = 2 | pages = 287–294 | date = March 2011 | pmid = 21142693 | doi = 10.1517/14740338.2011.542146 | s2cid = 207487296 }}
{{refend}}
{{Urologicals}}
{{Adrenergics}}
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