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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/06/28 15:56:39」(JST)
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Mirabegron
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| Systematic (IUPAC) name |
| 2-(2-Amino-1,3-thiazol-4-yl)-N-[4-(2-{[(2R)-2-hydroxy-2-phenylethyl]amino}ethyl)phenyl]acetamide |
| Clinical data |
| Trade names |
Myrbetriq (US), Betanis (Japan), Betmiga (EU) |
| Licence data |
US FDA:link |
| Pregnancy cat. |
C (US) |
| Legal status |
℞-only (US) |
| Routes |
Oral |
| Identifiers |
| CAS number |
223673-61-8 |
| ATC code |
G04BD12 |
| PubChem |
CID 9865528 |
| ChemSpider |
8041219 |
| Synonyms |
YM-178 |
| Chemical data |
| Formula |
C21H24N4O2S |
| Mol. mass |
396.506 g/mol |
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
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Mirabegron (formerly YM-178, trade name Myrbetriq) is a drug for the treatment of overactive bladder.[1] It was developed by Astellas Pharma and was approved in the United States in July 2012.
Mirabegron activates the β3 adrenergic receptor in the detrusor muscle in the bladder, which leads to muscle relaxation and an increase in bladder capacity.[2]
References[edit]
- ^ Gras, J (2012). "Mirabegron for the treatment of overactive bladder". Drugs of today (Barcelona, Spain : 1998) 48 (1): 25–32. doi:10.1358/dot.2012.48.1.1738056. PMID 22384458.
- ^ "New Drug Approvals 2012 - Pt. XIV - Mirabegron (MyrbetriqTM)". ChEMBL. 5 July 2012. Retrieved 28 September 2012.
External links[edit]
- 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.
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Urologicals, including antispasmodics (G04B)
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| Acidifiers |
- Ammonium chloride
- Calcium chloride
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Urinary antispasmodics
(primarily antimuscarinics) |
- Darifenacin
- Emepronium
- Fesoterodine
- Flavoxate
- Imidafenacin
- Meladrazine
- Mirabegron
- Oxybutynin
- Propiverine
- Solifenacin
- Terodiline
- Tolterodine
- Trospium chloride
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| Other urologicals |
- Urea analogues: Acetohydroxamic acid
- Salicylhydroxamic acid
- Other: Collagen
- Dimethyl sulfoxide
- Magnesium hydroxide
- Pentosan polysulfate
- Phenazopyridine
- Phenyl salicylate
- Succinimide
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noco/acba/cong/tumr, sysi/epon, urte
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proc/itvp, drug (G4B), blte, urte
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Adrenergics
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Receptor ligands
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α1
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- Agonists: 5-FNE
- 6-FNE
- Amidephrine
- Anisodamine
- Anisodine
- Cirazoline
- Dipivefrine
- Dopamine
- Ephedrine
- Epinephrine
- Etilefrine
- Ethylnorepinephrine
- Indanidine
- Levonordefrin
- Metaraminol
- Methoxamine
- Methyldopa
- Midodrine
- Naphazoline
- Norepinephrine
- Octopamine
- Oxymetazoline
- Phenylephrine
- Phenylpropanolamine
- Pseudoephedrine
- Synephrine
- Tetrahydrozoline
Antagonists: Abanoquil
- Adimolol
- Ajmalicine
- Alfuzosin
- Amosulalol
- Arotinolol
- Atiprosin
- Benoxathian
- Buflomedil
- Bunazosin
- Carvedilol
- CI-926
- Corynanthine
- Dapiprazole
- DL-017
- Domesticine
- Doxazosin
- Eugenodilol
- Fenspiride
- GYKI-12,743
- GYKI-16,084
- Hydroxyzine
- Indoramin
- Ketanserin
- L-765,314
- Labetalol
- Mephendioxan
- Metazosin
- Monatepil
- Moxisylyte
- Naftopidil
- Nantenine
- Neldazosin
- Nicergoline
- Niguldipine
- Pelanserin
- Phendioxan
- Phenoxybenzamine
- Phentolamine
- Piperoxan
- Prazosin
- Quinazosin
- Ritanserin
- RS-97,078
- SGB-1,534
- Silodosin
- SL-89.0591
- Spiperone
- Talipexole
- Tamsulosin
- Terazosin
- Tibalosin
- Tiodazosin
- Tipentosin
- Tolazoline
- Trimazosin
- Upidosin
- Urapidil
- Zolertine
- Note that many TCAs, TeCAs, antipsychotics, ergolines, and some piperazines like buspirone and trazodone all antagonize α1-adrenergic receptors as well, which contributes to their side effects such as orthostatic hypotension.
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α2
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- Agonists: (R)-3-Nitrobiphenyline
- 4-NEMD
- 6-FNE
- Amitraz
- Apraclonidine
- Brimonidine
- Cannabivarin
- Clonidine
- Detomidine
- Dexmedetomidine
- Dihydroergotamine
- Dipivefrine
- Dopamine
- Ephedrine
- Ergotamine
- Epinephrine
- Esproquin
- Etilefrine
- Ethylnorepinephrine
- Guanabenz
- Guanfacine
- Guanoxabenz
- Levonordefrin
- Lofexidine
- Medetomidine
- Methyldopa
- Mivazerol
- Naphazoline
- Norepinephrine
- Oxymetazoline
- Phenylpropanolamine
- Piperoxan
- Pseudoephedrine
- Rilmenidine
- Romifidine
- Talipexole
- Tetrahydrozoline
- Tizanidine
- Tolonidine
- Urapidil
- Xylazine
- Xylometazoline
Antagonists: 1-PP
- Adimolol
- Aptazapine
- Atipamezole
- BRL-44408
- Buflomedil
- Cirazoline
- Efaroxan
- Esmirtazapine
- Fenmetozole
- Fluparoxan
- GYKI-12,743
- GYKI-16,084
- Idazoxan
- Mianserin
- Mirtazapine
- MK-912
- NAN-190
- Olanzapine
- Phentolamine
- Phenoxybenzamine
- Piperoxan
- Piribedil
- Rauwolscine
- Rotigotine
- SB-269,970
- Setiptiline
- Spiroxatrine
- Sunepitron
- Tolazoline
- Yohimbine
* Note that many atypical antipsychotics and azapirones like buspirone (via metabolite 1-PP) antagonize α2-adrenergic receptors as well.
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β
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Reuptake inhibitors
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NET
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- Selective norepinephrine reuptake inhibitors: Amedalin
- Atomoxetine (Tomoxetine)
- Ciclazindol
- Daledalin
- Edivoxetine
- Esreboxetine
- Lortalamine
- Mazindol
- Nisoxetine
- Reboxetine
- Talopram
- Talsupram
- Tandamine
- Viloxazine; Norepinephrine-dopamine reuptake inhibitors: Amineptine
- Bupropion (Amfebutamone)
- Fencamine
- Fencamfamine
- Lefetamine
- Levophacetoperane
- LR-5182
- Manifaxine
- Methylphenidate
- Nomifensine
- O-2172
- Radafaxine; Serotonin-norepinephrine reuptake inhibitors: Bicifadine
- Desvenlafaxine
- Duloxetine
- Eclanamine
- Levomilnacipran
- Milnacipran
- Sibutramine
- Venlafaxine; Serotonin-norepinephrine-dopamine reuptake inhibitors: Brasofensine
- Diclofensine
- DOV-102,677
- DOV-21,947
- DOV-216,303
- JNJ-7925476
- JZ-IV-10
- Methylnaphthidate
- Naphyrone
- NS-2359
- PRC200-SS
- SEP-225,289
- SEP-227,162
- Tesofensine; Tricyclic antidepressants: Amitriptyline
- Butriptyline
- Cianopramine
- Clomipramine
- Desipramine
- Dosulepin
- Doxepin
- Imipramine
- Lofepramine
- melitracen
- Nortriptyline
- Protriptyline
- Trimipramine; Tetracyclic antidepressants: Amoxapine
- Maprotiline
- Mianserin
- Oxaprotiline
- Setiptiline; Others: Cocaine
- CP-39,332
- Ethanol
- EXP-561
- Fezolamine
- Ginkgo biloba
- Indeloxazine
- Nefazodone
- Nefopam
- Pridefrine
- Tapentadol
- Tedatioxetine
- Teniloxazine
- Tofenacin
- Tramadol
- Ziprasidone
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VMAT
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- Ibogaine
- Reserpine
- Tetrabenazine
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Enzyme inhibitors
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Anabolism
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PAH
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TH
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- 3-Iodotyrosine
- Aquayamycin
- Bulbocapnine
- Metirosine
- Oudenone
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AAAD
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- Benserazide
- Carbidopa
- DFMD
- Genistein
- Methyldopa
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DBH
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- Bupicomide
- Disulfiram
- Dopastin
- Fusaric acid
- Nepicastat
- Phenopicolinic acid
- Tropolone
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PNMT
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- CGS-19281A
- SKF-64139
- SKF-7698
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Catabolism
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MAO
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- Nonselective: Benmoxin
- Caroxazone
- Echinopsidine
- Furazolidone
- Hydralazine
- Indantadol
- Iproclozide
- Iproniazid
- Isocarboxazid
- Isoniazid
- Linezolid
- Mebanazine
- Metfendrazine
- Nialamide
- Octamoxin
- Paraxazone
- Phenelzine
- Pheniprazine
- Phenoxypropazine
- Pivalylbenzhydrazine
- Procarbazine
- Safrazine
- Tranylcypromine; MAO-A selective: Amiflamine
- Bazinaprine
- Befloxatone
- Befol
- Brofaromine
- Cimoxatone
- Clorgiline
- Esuprone
- Harmala alkaloids (Harmine,
- Harmaline
- Tetrahydroharmine
- Harman
- Norharman, etc)
- Methylene blue
- Metralindole
- Minaprine
- Moclobemide
- Pirlindole
- Sercloremine
- Tetrindole
- Toloxatone
- Tyrima; MAO-B selective:
- Ladostigil
- Lazabemide
- Milacemide
- Mofegiline
- Pargyline
- Rasagiline
- Safinamide
- Selegiline (also D-Deprenyl)
* Note that MAO-B inhibitors also influence norepinephrine/epinephrine levels since they inhibit the breakdown of their precursor dopamine.
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COMT
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- Entacapone
- Nitecapone
- Tolcapone
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Others
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Precursors
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- L-Phenylalanine → L-Tyrosine → L-DOPA (Levodopa) → Dopamine
- L-DOPS (Droxidopa)
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Cofactors
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- Ferrous Iron (Fe2+)
- S-Adenosyl-L-Methionine
- Vitamin B3 (Niacin
- Nicotinamide → NADPH)
- Vitamin B6 (Pyridoxine
- Pyridoxamine
- Pyridoxal → Pyridoxal Phosphate)
- Vitamin B9 (Folic acid → Tetrahydrofolic acid)
- Vitamin C (Ascorbic acid)
- Zinc (Zn2+)
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Others
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- Activity enhancers: BPAP
- PPAP; Release blockers: Bethanidine
- Bretylium
- Guanadrel
- Guanazodine
- Guanclofine
- Guanethidine
- Guanoxan; Toxins: 6-OHDA
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List of adrenergic drugs
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UpToDate Contents
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English Journal
- The use of pharmacotherapy for male patients with urgency and stress incontinence.
- Andersson KE.
- Current opinion in urology.Curr Opin Urol.2014 Nov;24(6):571-7. doi: 10.1097/MOU.0000000000000106.
- PURPOSE OF REVIEW: To summarize recent data on the medical treatment of men with incontinence due to overactive bladder or to stress urinary incontinence published in peer-reviewed journals.RECENT FINDINGS: Previous randomized controlled trials have shown that both antimuscarinic drugs and α1-adren
- PMID 25144147
- Phase II drugs that target cholinergic receptors for the treatment of overactive bladder.
- Zacche MM1, Giarenis I, Cardozo L.
- Expert opinion on investigational drugs.Expert Opin Investig Drugs.2014 Oct;23(10):1365-74. doi: 10.1517/13543784.2014.925877. Epub 2014 Jun 5.
- INTRODUCTION: Overactive bladder (OAB) is a term used to describe the symptom syndrome of urgency, with or without urgency incontinence, usually associated with frequency and nocturia. Antimuscarinics are the most widely prescribed class of drugs for OAB, although their systemic adverse effects limi
- PMID 24899225
- Mirabegron 50 mg once-daily for the treatment of symptoms of overactive bladder: An overview of efficacy and tolerability over 12 weeks and 1 year.
- Chapple CR1, Kaplan SA, Mitcheson D, Blauwet MB, Huang M, Siddiqui E, Khullar V.
- International journal of urology : official journal of the Japanese Urological Association.Int J Urol.2014 Oct;21(10):960-7. doi: 10.1111/iju.12568. Epub 2014 Aug 4.
- The aim of the present review article was to summarize the efficacy and tolerability for mirabegron 50 mg over 12 weeks and 1 year versus placebo (SCORPIO) or tolterodine ER 4 mg (SCORPIO and TAURUS). After a 2-week placebo run-in, adults with overactive bladder symptoms for ≥3 months were ran
- PMID 25092441
Japanese Journal
- 抗コリン薬抵抗性の神経因性膀胱に対するミラベグロンの併用効果 : ビデオウロダイナミクスを用いた検討
- トシル酸スプラタスト(IPD)内服が有効であった好酸球性膀胱炎の1例
- Effect of mirabegron on plasma gonadotropic and steroidal hormone levels in rats after two weeks of oral administration
Related Links
- Mirabegronとは？goo Wikipedia (ウィキペディア) 。出典：Wikipedia（ウィキペディア）フリー百科事典。 Mirabegronとは - goo Wikipedia (ウィキペディア) gooトップ サイトマップ スタートページに設定 RSS ヘルプ メニューへスキップ 本文へ ...
- ミラベグロン(Mirabegron)の検索ならお薬検索QLife（キューライフ）。お医者さんが処方する処方薬と、薬局で買える市販薬(OTC)、の効果と副作用、写真、添付文書、保管方法等を掲載。商品名だけでなく一般名や剤形、色などからも検索 ...
Related Pictures
★リンクテーブル★
[★]
- 英
- mirabegron
- 商
- ベタニス
- 関
- その他の泌尿生殖器官及び肛門用薬。β3アドレナリン受容体、アドレナリン受容体
- 選択的β3アドレナリン受容体作動薬。膀胱平滑筋に新剤するβ3アドレナリン受容体を選択的に刺激することで、膀胱を弛緩させる。これにより過活動膀胱における尿意切迫感、頻尿及び切迫性尿失禁を改善する。
- 50mgを1日1回食後に内服する。中等度の肝機能障害患者(Child-Pughスコア7～9)への投与は1日1回25mgから開始。重度の腎機能障害患者(eGFR15～29mL/min/1.73m2)への投与は1日1回25mgから開始