Mirabegron

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Mirabegron
Mirabegron.svg
Clinical data
Trade namesMyrbetriq, Betanis, Betmiga, others
Other namesYM-178
AHFS/Drugs.comMonograph
MedlinePlusa612038
License data
Pregnancy
category
  • AU: B3
Routes of
administration		By mouth (tablets)
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only) [1]
  • US: ℞-only [2]
  • EU: Rx-only [3]
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability29–35%[4]
Protein binding71%[4]
MetabolismLiver via (direct) glucuronidation, amide hydrolysis, and minimal oxidative metabolism in vivo by CYP2D6 and CYP3A4. Some involvement of butylcholinesterase[4]
Elimination half-life50 hours[4]
ExcretionUrine (55%), faeces (34%)[4]
Identifiers
  • 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 InfoCard100.226.392 Edit this at Wikidata
Chemical and physical data
FormulaC21H24N4O2S
Molar mass396.51 g·mol−1
3D model (JSmol)
  • O=C(Nc1ccc(cc1)CCNC[C@H](O)c2ccccc2)Cc3nc(sc3)N
InChI
  • 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 2019, it was the 189th most commonly prescribed medication in the United States, with more than 3 million prescriptions.[10][11] In the United Kingdom it is less preferred to antimuscarinic medication such as oxybutynin.[7]

Medical uses[]

Myrbetriq 50 mg both sides

Its used is in the treatment of overactive bladder.[12][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.[12]

Adverse effects[]

Adverse effects by incidence:[4][2][1]

Very common (>10% incidence) adverse effects include:

  • Elevated blood pressure

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

Pronunciation[]

The brand name Myrbetriq is pronounced /mɪərˈbɛtrɪk/ meer-BET-rik.

References[]

  1. ^ 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.
  2. ^ a b c "Myrbetriq- mirabegron tablet, film coated, extended release". DailyMed. Retrieved 27 March 2021.
  3. ^ a b c "Betmiga EPAR". European Medicines Agency. Retrieved 28 April 2020. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  4. ^ a b c d e f g "mirabegron (Rx) - Myrbetriq". Medscape Reference. WebMD. Retrieved 17 November 2013.
  5. ^ a b c d e "Mirabegron Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 18 March 2019.
  6. ^ a b "[93] Are claims for newer drugs for overactive bladder warranted?". Therapeutics Initiative. 22 April 2015. Retrieved 17 March 2019.
  7. ^ a b c d British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 763. ISBN 9780857113382.
  8. ^ "Drug Approval Package: Myrbetriq (mirabegron) Extended Release Tablets NDA #202611". U.S. Food and Drug Administration (FDA). 10 August 2012. Retrieved 28 April 2020.
  9. ^ 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): 433–48. doi:10.1517/17460441.2014.892923. PMID 24559030. S2CID 26424400.
  10. ^ "The Top 300 of 2019". ClinCalc. Retrieved 16 October 2021.
  11. ^ "Mirabegron - Drug Usage Statistics". ClinCalc. Retrieved 16 October 2021.
  12. ^ 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. Public Domain This article incorporates text from this source, which is in the public domain.

Further reading[]

External links[]

  • "Mirabegron". Drug Information Portal. U.S. National Library of Medicine.
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