Mirabegron

Mirabegron
Names
Trade namesMyrbetriq, Betanis, Betmiga, others
Other namesYM-178
IUPAC name
  • 2-(2-Amino-1,3-thiazol-4-yl)-N-[4-(2-{[(2R)-2-hydroxy-2-phenylethyl]amino}ethyl)phenyl]acetamide
Clinical data
Drug classβ3 adrenergic receptor agonist[1][2]
Main usesOveractive bladder[1]
Side effectsHigh blood pressure, headaches, urinary tract infections[1]
WHO AWaReUnlinkedWikibase error: ⧼unlinkedwikibase-error-statements-entity-not-set⧽
Pregnancy
category
  • AU: B3
  • US: C (Risk not ruled out)
    Routes of
    use    		By mouth (tablets)
    Defined daily dose50 mg[3]
    External links
    AHFS/Drugs.comMonograph
    MedlinePlusa612038
    Legal
    License data
    Legal status
    • AU: S4 (Prescription only)
    • UK: POM (Prescription only)
    • US: ℞-only
    • In general: ℞ (Prescription only)
    Pharmacokinetics
    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]
    Chemical and physical data
    FormulaC21H24N4O2S
    Molar mass396.51 g·mol−1
    3D model (JSmol)
    SMILES
    • 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.[1] Its benefits are similar to antimuscarinic medication such as solifenacin or tolterodine.[5] In the United Kingdom it is less preferred to antimuscarinic medication such as oxybutynin.[2] It is taken by mouth.[1]

    Common side effects include high blood pressure, headaches, and urinary tract infections.[1] Other significant side effects include urinary retention, irregular heart rate, and angioedema.[1][2] It works by activating the β3 adrenergic receptor in the bladder, resulting in its relaxation.[1][2]

    Mirabegron was approved for medical use in the United States and in the European Union in 2012.[6][7][8] A month supply in the United Kingdom costs the NHS about £29 as of 2019.[2] In the United States the wholesale cost of this amount is about 369 USD.[9] In 2017, it was the 191st most commonly prescribed medication in the United States, with more than three million prescriptions.[10][11]

    Medical uses

    Myrbetriq 50 mg both sides

    Its used is in the treatment of overactive bladder.[4][12][13] It works equally well to antimuscarinic medication such as solifenacin or tolterodine.[5][8] In the United Kingdom it is less preferred to these agents.[2]

    Dosage

    The defined daily dose is 50 mg by mouth.[3]

    Side effects

    Side effects by frequency:[4][12][13]

    Very common (>10% incidence):

    Common (1–10% incidence):

    Rare (<1% incidence):

    Pronunciation

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

    Society and culture

    Cost

    A month supply in the United Kingdom costs the NHS about £29 as of 2019.[2] In the United States the wholesale cost of this amount is about 369 USD.[9] In 2017, it was the 191st most commonly prescribed medication in the United States, with more than three million prescriptions.[10][11]

    • Mirabegron costs (US)
      Mirabegron costs (US)
    • Mirabegron prescriptions (US)
      Mirabegron prescriptions (US)

    References

    1. 1 2 3 4 5 6 7 8 "Mirabegron Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Archived from the original on 4 March 2021. Retrieved 18 March 2019.
    2. 1 2 3 4 5 6 7 British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 763. ISBN 9780857113382.
    3. 1 2 "WHOCC - ATC/DDD Index". www.whocc.no. Archived from the original on 16 April 2021. Retrieved 7 September 2020.
    4. 1 2 3 4 5 6 7 "mirabegron (Rx) - Myrbetriq". Medscape Reference. WebMD. Archived from the original on 11 February 2015. Retrieved 17 November 2013.
    5. 1 2 "[93] Are claims for newer drugs for overactive bladder warranted?". Therapeutics Initiative. 22 April 2015. Archived from the original on 2 April 2019. Retrieved 17 March 2019.
    6. ↑ "Drug Approval Package: Myrbetriq (mirabegron) Extended Release Tablets NDA #202611". U.S. Food and Drug Administration (FDA). 10 August 2012. Archived from the original on 8 April 2021. Retrieved 28 April 2020.
    7. ↑ 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.
    8. 1 2 "Betmiga EPAR". European Medicines Agency. Archived from the original on 22 May 2020. Retrieved 28 April 2020. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
    9. 1 2 "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Archived from the original on 6 March 2019. Retrieved 3 March 2019.
    10. 1 2 "The Top 300 of 2020". ClinCalc. Archived from the original on 12 February 2021. Retrieved 11 April 2020.
    11. 1 2 "Mirabegron - Drug Usage Statistics". ClinCalc. Archived from the original on 8 July 2020. Retrieved 11 April 2020.
    12. 1 2 "Myrbetriq (mirabegron) tablet, film coated, extended release [Astellas Pharma US, Inc.]". DailyMed. Astellas Pharma US, Inc. September 2012. Archived from the original on 28 November 2019. Retrieved 17 November 2013.
    13. 1 2 "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.
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