Mirabegron
Mirabegron, sold under the brand name Myrbetriq among others, is a medication used to treat overactive bladder.[2] Its benefits are similar to other antimuscarinic medication such as solifenacin or tolterodine.[3] In the United Kingdom it is less preferred to antimuscarinic medication such as oxybutynin.[4] It is taken by mouth.[2]
Clinical data | |
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Trade names | Myrbetriq, Betanis, Betmiga, others |
Other names | YM-178 |
AHFS/Drugs.com | Monograph |
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Routes of administration | By mouth (tablets) |
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Pharmacokinetic data | |
Bioavailability | 29–35%[1] |
Protein binding | 71%[1] |
Metabolism | Hepatic via (direct) glucuronidation, amide hydrolysis, and minimal oxidative metabolism in vivo by CYP2D6 and CYP3A4. Some involvement of butylcholinesterase[1] |
Elimination half-life | 50 hours[1] |
Excretion | Urine (55%), faeces (34%)[1] |
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ECHA InfoCard | 100.226.392 |
Chemical and physical data | |
Formula | C21H24N4O2S |
Molar mass | 396.506 g/mol g·mol−1 |
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Common side effects include high blood pressure, headaches, and urinary tract infections.[2] Other significant side effects include urinary retention, irregular heart rate, and angioedema.[2][4] It works by activating the β3 adrenergic receptor in the bladder, resulting in its relaxation.[4][2]
Mirabegron was approved for medical use in the United States in 2012.[5][2] A month supply in the United Kingdom costs the NHS about £29 as of 2019.[4] In the United States the wholesale cost of this amount is about 369 USD.[6] In 2016 it was the 263rd most prescribed medication in the United States with more than a million prescriptions.[7]
Medical uses
Its used is in the treatment of overactive bladder.[1][8][9] It works equally well to antimuscarinic medication such as solifenacin or tolterodine.[3] In the United Kingdom it is less preferred to these agents.[4]
Adverse effects
Adverse effects by incidence:[1][8][9]
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
Pronunciation
Myrbetriq is pronounced /mɪərˈbɛtrɪk/ meer-BET-rik.
References
- "mirabegron (Rx) - Myrbetriq". Medscape Reference. WebMD. Retrieved 17 November 2013.
- "Mirabegron Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 18 March 2019.
- "[93] Are claims for newer drugs for overactive bladder warranted?". Therapeutics Initiative. 22 April 2015. Retrieved 17 March 2019.
- British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 763. ISBN 9780857113382.
- Sacco, E; Bientinesi, R; et al. (Apr 2014). "Discovery history and clinical development of mirabegron for the treatment of overactive bladder and urinary incontinence". Expert Opin Drug Discov. 9 (4): 433–48. doi:10.1517/17460441.2014.892923. PMID 24559030.
- "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Retrieved 3 March 2019.
- "The Top 300 of 2019". clincalc.com. Retrieved 22 December 2018.
- "MYRBETRIQ (mirabegron) tablet, film coated, extended release [Astellas Pharma US, Inc.]". DailyMed. Astellas Pharma US, Inc. September 2012. Retrieved 17 November 2013.
- "Betmiga 25mg & 50mg prolonged-release tablets". electronic Medicines Compendium. Astellas Pharma Ltd. 22 February 2013. Retrieved 17 November 2013.
External links
- Sacco, E.; Bientinesi, R. (2012). "Mirabegron: A review of recent data and its prospects in the management of overactive bladder". Therapeutic Advances in Urology. 4 (6): 315–24. doi:10.1177/1756287212457114. PMC 3491758. PMID 23205058.