Peringatan Keamanan

At doses of up to 400mg in healthy volunteers (~8x the recommended maximum), reported symptoms of overdose included palpitations and increased heart rate. Symptoms of chronic overdosage are similar in presentation and may also include a rise in systolic blood pressure. In cases of overdosage, employ standard symptomatic and supportive measures in addition to ECG monitoring.L32853

Mirabegron

DB08893

small molecule approved

Deskripsi

Mirabegron is a sympathomimetic beta-3 adrenergic receptor agonist used to relax the smooth muscle of the bladder in the treatment of urinary frequency and incontinence. It is unique amongst overactive bladder treatment options in that, unlike other treatments such as solifenacin and darifenacin, it lacks significant antimuscarinic activity,A232553 which is responsible both for the therapeutic effects of these medications and their broad range of adverse effects. Mirabegron has a comparatively favorable adverse effect profile as compared to other available treatment options, and its complementary mechanism to the antimuscarinics that came before it allows for its use alongside solifenacin in refractory cases.L32853

Mirabegron first received FDA approval in 2012, under the brand name Myrbetriq, for the treatment of adults with overactive bladder.L32853 An extended-release granule formulation was subsequently granted approval in March 2021 for the treatment of pediatric patients with neurogenic detrusor overactivity.L32853 Mirabegron is also used in other jurisdictions across the globe, including Canada,L32925 the EU,L32945 and Japan.A7469

Struktur Molekul 2D

Berat 396.506
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean terminal elimination half-life of mirabegron in adults being treated for overactive bladder is approximately 50 hours.[L32853] In pediatric patients receiving the granule formulation for the treatment of neurogenic detrusor overactivity, the mean terminal elimination half-life is approximately 26-31 hours.[L32853]
Volume Distribusi Following intravenous administration, mirabegron has an apparent steady-state volume of distribution (Vd) of 1670 L indicating extensive distribution.[L32853]
Klirens (Clearance) Total plasma clearance following intravenous administration is approximately 57 L/h, with renal clearance accounting for roughly 25% at approximately 13 L/h.[L32853]

Absorpsi

The absolute bioavailability of orally administered mirabegron ranges from 29% at a dose of 25 mg to 35% at a dose of 50 mg.L32853 The Tmax for the extended-release tablet and suspension formulations are approximately 3.5 hours, while the Tmax for the granule formulation is 4-5 hours.L32853 Both Cmax and AUC increase more than dose proportionally - an increase in dose from 50mg to 100mg results in a 2.9- and 2.6-fold increase in Cmax and AUC, respectively, whereas an increase from 50mg to 200mg results in a 8.4- and 6.5-fold increase in Cmax and AUC, respectively.L32853 Steady-state concentrations of mirabegron are achieved after approximately 7 days of once-daily administration.L32853

Metabolisme

Mirabegron is extensively metabolized via a number of mechanisms, although unchanged parent drug is still the major circulating component following oral administration.L32853 Presumed metabolic pathways and their resultant metabolites include amide hydrolysis (M5, M16, M17), glucuronidation (mirabegron O-glucuronide, N-glucuronide, N-carbamoylglucuronide, M12), and secondary amine oxidation or dealkylation (M8, M9, M15), amongst others.A232568 The enzymes responsible for the oxidative metabolism of mirabegron are thought to be CYP3A4 and CYP2D6,L32853 while the UDP-glucuronosyltransferases responsible for conjugation reactions have been identified as UGT2B7, UGT1A3, and UGT1A8.A232768 Other enzymes that may be involved in the metabolism of mirabegron include butylcholinesterase and possibly alcohol dehydrogenase.L32853

Rute Eliminasi

Of a 160mg radiolabeled dose administered to healthy volunteers, approximately 55% of the radioactivity was recovered in the urine and 34% in the feces. Approximately 25% of unchanged mirabegron was recovered in the urine while 0% was recovered in the feces.L32853 Renal elimination is achieved primarily via active tubular secretion with some contribution by glomerular filtration.L32853

Interaksi Makanan

1 Data
  • 1. Take with food. While adults may take mirabegron with or without food, prescribing information recommends that children always co-administer mirabegron with food.

Interaksi Obat

1734 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Mirabegron.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Mirabegron.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Mirabegron.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Mirabegron.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Mirabegron.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Mirabegron.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Mirabegron.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Mirabegron.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Mirabegron.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Mirabegron.
Silodosin The excretion of Silodosin can be decreased when combined with Mirabegron.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Mirabegron.
Valsartan Mirabegron may decrease the antihypertensive activities of Valsartan.
Remikiren Mirabegron may decrease the antihypertensive activities of Remikiren.
Olmesartan Mirabegron may decrease the antihypertensive activities of Olmesartan.
Minoxidil Mirabegron may decrease the antihypertensive activities of Minoxidil.
Trandolapril Mirabegron may decrease the antihypertensive activities of Trandolapril.
Benazepril Mirabegron may decrease the antihypertensive activities of Benazepril.
Candoxatril Mirabegron may decrease the antihypertensive activities of Candoxatril.
Nitroglycerin Mirabegron may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Mirabegron may decrease the antihypertensive activities of Metyrosine.
Cryptenamine Mirabegron may decrease the antihypertensive activities of Cryptenamine.
Eprosartan Mirabegron may decrease the antihypertensive activities of Eprosartan.
Quinapril Mirabegron may decrease the antihypertensive activities of Quinapril.
Deserpidine Mirabegron may decrease the antihypertensive activities of Deserpidine.
Pentolinium Mirabegron may decrease the antihypertensive activities of Pentolinium.
Saprisartan Mirabegron may decrease the antihypertensive activities of Saprisartan.
Spirapril Mirabegron may decrease the antihypertensive activities of Spirapril.
Diethylnorspermine Mirabegron may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Mirabegron may decrease the antihypertensive activities of Temocapril.
Hexamethonium Mirabegron may decrease the antihypertensive activities of Hexamethonium.
Rauwolfia serpentina root Mirabegron may decrease the antihypertensive activities of Rauwolfia serpentina root.
Angiotensin 1-7 Mirabegron may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Mirabegron may decrease the antihypertensive activities of Imidapril.
BQ-123 Mirabegron may decrease the antihypertensive activities of BQ-123.
Dihydralazine Mirabegron may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Mirabegron may decrease the antihypertensive activities of Zofenopril.
Guanoxan Mirabegron may decrease the antihypertensive activities of Guanoxan.
Delapril Mirabegron may decrease the antihypertensive activities of Delapril.
Vincamine Mirabegron may decrease the antihypertensive activities of Vincamine.
Linsidomine Mirabegron may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Mirabegron may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Mirabegron may decrease the antihypertensive activities of Tolonidine.
Endralazine Mirabegron may decrease the antihypertensive activities of Endralazine.
Cadralazine Mirabegron may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Mirabegron may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Mirabegron may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Mirabegron may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Mirabegron may decrease the antihypertensive activities of Guanoclor.
Tocopherylquinone Mirabegron may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Mirabegron may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Mirabegron may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Mirabegron may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Mirabegron may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Mirabegron may decrease the antihypertensive activities of Quinaprilat.
Bosentan Mirabegron may decrease the antihypertensive activities of Bosentan.
Irbesartan Mirabegron may decrease the antihypertensive activities of Irbesartan.
Sitaxentan Mirabegron may decrease the antihypertensive activities of Sitaxentan.
Pinacidil Mirabegron may decrease the antihypertensive activities of Pinacidil.
Riociguat The serum concentration of Riociguat can be increased when it is combined with Mirabegron.
Aliskiren Mirabegron may decrease the antihypertensive activities of Aliskiren.
Naftopidil Mirabegron may decrease the antihypertensive activities of Naftopidil.
Enalapril Mirabegron may decrease the antihypertensive activities of Enalapril.
Candesartan cilexetil Mirabegron may decrease the antihypertensive activities of Candesartan cilexetil.
Telmisartan Mirabegron may decrease the antihypertensive activities of Telmisartan.
Captopril Mirabegron may decrease the antihypertensive activities of Captopril.
Cilazapril Mirabegron may decrease the antihypertensive activities of Cilazapril.
Candesartan Mirabegron may decrease the antihypertensive activities of Candesartan.
Ramipril Mirabegron may decrease the antihypertensive activities of Ramipril.
Amlodipine Mirabegron may decrease the antihypertensive activities of Amlodipine.
Perindopril Mirabegron may decrease the antihypertensive activities of Perindopril.
Levamlodipine Mirabegron may decrease the antihypertensive activities of Levamlodipine.
Lercanidipine Mirabegron may decrease the antihypertensive activities of Lercanidipine.
Azilsartan medoxomil Mirabegron may decrease the antihypertensive activities of Azilsartan medoxomil.
Diazoxide Mirabegron may decrease the antihypertensive activities of Diazoxide.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Mirabegron.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Mirabegron.
Tramadol The risk or severity of urinary retention can be increased when Tramadol is combined with Mirabegron.
Trospium The risk or severity of urinary retention can be increased when Trospium is combined with Mirabegron.
Oxyphenonium The risk or severity of urinary retention can be increased when Oxyphenonium is combined with Mirabegron.
Benzatropine The risk or severity of urinary retention can be increased when Benzatropine is combined with Mirabegron.
Disopyramide The risk or severity of urinary retention can be increased when Disopyramide is combined with Mirabegron.
Amitriptyline The risk or severity of urinary retention can be increased when Amitriptyline is combined with Mirabegron.
Ipratropium The risk or severity of urinary retention can be increased when Ipratropium is combined with Mirabegron.
Olanzapine The risk or severity of urinary retention can be increased when Olanzapine is combined with Mirabegron.
Metixene The risk or severity of urinary retention can be increased when Metixene is combined with Mirabegron.
Terfenadine The risk or severity of urinary retention can be increased when Terfenadine is combined with Mirabegron.
Buclizine The risk or severity of urinary retention can be increased when Buclizine is combined with Mirabegron.
Clozapine The risk or severity of urinary retention can be increased when Clozapine is combined with Mirabegron.
Doxylamine The risk or severity of urinary retention can be increased when Doxylamine is combined with Mirabegron.
Trihexyphenidyl The risk or severity of urinary retention can be increased when Trihexyphenidyl is combined with Mirabegron.
Oxyphencyclimine The risk or severity of urinary retention can be increased when Oxyphencyclimine is combined with Mirabegron.
Procyclidine The risk or severity of urinary retention can be increased when Procyclidine is combined with Mirabegron.
Profenamine The risk or severity of urinary retention can be increased when Profenamine is combined with Mirabegron.
Promazine The risk or severity of urinary retention can be increased when Promazine is combined with Mirabegron.
Hyoscyamine The risk or severity of urinary retention can be increased when Hyoscyamine is combined with Mirabegron.
Cyproheptadine The risk or severity of urinary retention can be increased when Cyproheptadine is combined with Mirabegron.
Imipramine The risk or severity of urinary retention can be increased when Imipramine is combined with Mirabegron.
Methscopolamine bromide The risk or severity of urinary retention can be increased when Methscopolamine bromide is combined with Mirabegron.
Chlorpromazine The risk or severity of urinary retention can be increased when Chlorpromazine is combined with Mirabegron.

Target Protein

Beta-3 adrenergic receptor ADRB3
Beta-1 adrenergic receptor ADRB1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17293563
    Takasu T, Ukai M, Sato S, Matsui T, Nagase I, Maruyama T, Sasamata M, Miyata K, Uchida H, Yamaguchi O: Effect of (R)-2-(2-aminothiazol-4-yl)-4'-{2-(2-hydroxy-2-phenylethyl)aminoethyl} acetanilide (YM178), a novel selective beta3-adrenoceptor agonist, on bladder function. J Pharmacol Exp Ther. 2007 May;321(2):642-7. Epub 2007 Feb 9.
  • PMID: 23550899
    Kashyap M, Tyagi P: The pharmacokinetic evaluation of mirabegron as an overactive bladder therapy option. Expert Opin Drug Metab Toxicol. 2013 May;9(5):617-27. doi: 10.1517/17425255.2013.786700. Epub 2013 Apr 4.
  • PMID: 30860748
    Dawood O, El-Zawahry A: Mirabegron .
  • PMID: 22269146
    Takusagawa S, van Lier JJ, Suzuki K, Nagata M, Meijer J, Krauwinkel W, Schaddelee M, Sekiguchi M, Miyashita A, Iwatsubo T, van Gelderen M, Usui T: Absorption, metabolism and excretion of (14)Cmirabegron (YM178), a potent and selective beta(3)-adrenoceptor agonist, after oral administration to healthy male volunteers. Drug Metab Dispos. 2012 Apr;40(4):815-24. doi: 10.1124/dmd.111.043588. Epub 2012 Jan 23.
  • PMID: 29164523
    Konishi K, Tenmizu D, Takusagawa S: Identification of Uridine 5'-Diphosphate-Glucuronosyltransferases Responsible for the Glucuronidation of Mirabegron, a Potent and Selective beta3-Adrenoceptor Agonist, in Human Liver Microsomes. Eur J Drug Metab Pharmacokinet. 2018 Jun;43(3):301-309. doi: 10.1007/s13318-017-0450-x.

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