関: betaxolol hydrochloride

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/10/09 07:49:21」(JST)

wiki en

Betaxolol (trade names Betoptic, Betoptic S, Lokren, Kerlone) is a selective beta₁ receptor blocker used in the treatment of hypertension and glaucoma. Being selective for beta₁ receptors, it typically has fewer systemic side effects than non-selective beta-blockers, for example, not causing bronchospasm (mediated by beta₂ receptors) as timolol may. Betaxolol also shows greater affininty for beta₁ receptors than metoprolol. In addition to its effect on the heart, betaxolol reduces the pressure within the eye (intraocular pressure). This effect is thought to be caused by reducing the production of the liquid (which is called the aqueous humor) within the eye. The precise mechanism of this effect is not known. The reduction in intraocular pressure reduces the risk of damage to the optic nerve and loss of vision in patients with elevated intraocular pressure due to glaucoma.

Betaxolol was approved by the U.S. Food and Drug Administration (FDA) for ocular use as a 0.5% solution (Betoptic) in 1985 and as a 0.25% solution (Betoptic S) in 1989.

Clinical uses

Oral: for the management of hypertension
Ophthalmic: for the management of glaucoma
the drug seems to have an effect of neuroprotection in glaucoma treatment

Dosage

Oral: The initial dose in hypertension is ordinarily 10 mg once daily either alone or added to diuretic therapy.
Ophthalmic: The recommended dose one to two drops in the affected eye(s) twice daily.

Contraindications

Hypersensitivity to the drug
Patients with sinus bradycardia, heart block greater than first degree, cardiogenic shock, and overt cardiac failure

External links

Kerlone prescribing information

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. β遮断剤中毒 beta blocker poisoning
2. Open-angle glaucoma: Treatment
3. 原発性乳児緑内障 primary infantile glaucoma
4. 患者情報：成人における高血圧治療（詳細） high blood pressure treatment in adults beyond the basics

English Journal

Fast and sensitive analysis of beta blockers by ultra-high-performance liquid chromatography coupled with ultra-high-resolution TOF mass spectrometry.

Tomková J1,2, Ondra P1,2, Kocianová E2,3, Václavík J2,3.
Biomedical chromatography : BMC.Biomed Chromatogr.2017 Jul;31(7). doi: 10.1002/bmc.3911. Epub 2017 Jan 4.
PMID 27925253

Influence of cell confluence on the cAMP signalling pathway in vascular smooth muscle cells.

Belacel-Ouari M1, Zhang L1, Hubert F1, Assaly R1, Gerbier R2, Jockers R2, Dauphin F3, Lechêne P1, Fischmeister R1, Manoury B1, Leblais V4.
Cellular signalling.Cell Signal.2017 Jul;35:118-128. doi: 10.1016/j.cellsig.2017.03.025. Epub 2017 Apr 4.
PMID 28389413

Modulation of neuroinflammation and pathology in the 5XFAD mouse model of Alzheimer's disease using a biased and selective beta-1 adrenergic receptor partial agonist.

Ardestani PM1, Evans AK1, Yi B1, Nguyen T1, Coutellier L1, Shamloo M2.
Neuropharmacology.Neuropharmacology.2017 Apr;116:371-386. doi: 10.1016/j.neuropharm.2017.01.010. Epub 2017 Jan 13.
PMID 28089846

Japanese Journal

Effectiveness of Carvedilol on Premature Ventricular Complexes Originating from the Bilateral Papillary Muscles in the Left Ventricle

Nakagawa Eiichiro,Tanaka Chiharu,Matsumi Hiroaki,Mizutani Kazuki,Ito Kazato,Yunoki Kei,Abe Yukio,Komatu Ryu,Haze Kazsuo,Naruko Takahiko,Itoh Akira
Journal of Arrhythmia 27(Supplement), PJ3_061-PJ3_061, 2011
… Ventricular arrhythmia was refractory to betaxolol (10 mg), mexiletine (300 mg) and Atenolol (25 mg). …
NAID 130002130343

Comparative Effects of Amlodipine Monotherapy and Combination Therapy With Betaxolol on Cardiac Autonomic Nervous Activity and Health-Related Quality of Life in Patients With Poorly Controlled Hypertension

Takase Bonpei,Takeishi Yasuchika,Hirai Tadakazu,Lee Jong-Dae,Uzui Hiroyasu,Senda Shoichi,Miwa Kunihisa,Hiraoka Yuji,Kinugawa Toru,Hosokawa Ryohei,Fujita Masatoshi
Circulation journal : official journal of the Japanese Circulation Society 72(5), 764-769, 2008-04-20
… Background The aim of the study was to evaluate whether the combined treatment of calcium channel blocker, amlodipine and /3-blocker, betaxolol, favorably affects cardiac autonomic nervous activity (CANA) and health-related quality of life (HRQL). … Methods and Results A total of 65 patients with a poor blood pressure (BP) control with a low dose amlodipine therapy were randomly assigned to the amlodipine dose-up group (n=21) and betaxolol adding group (n=44). …
NAID 110006680556

Direct Inhibition of N-Methyl-D-Aspartate (NMDA)-Receptor Function by Antiglaucomatous β-Antagonists

NAGATA Tatsuo,UENO Susumu,MORITA Hirofumi,KUBOTA Toshiaki,TOYOHIRA Yumiko,TSUTSUI Masato,TAWARA Akihiko,YANAGIHARA Nobuyuki
Journal of pharmacological sciences 106(3), 423-434, 2008-03-20
… In the present study, we investigated the direct effects of antiglaucoma drugs (timolol, betaxolol, pilocarpine, and latanoprost) on N-methyl-<sc><font size = "-2">D</font></sc>-aspartate (NMDA)-receptor function using a Xenopus oocytes expression system and electrophysiological techniques. …
NAID 10024319147

「ベタキソロール」

Betaxolol
Systematic (IUPAC) name
	(RS)-1-{4-[2-(cyclopropylmethoxy)ethyl]-; phenoxy}-3-(isopropylamino)propan-2-ol
Clinical data
Trade names	Kerlone
AHFS/Drugs.com	monograph
MedlinePlus	a609023
Pregnancy cat.	AU: C; US: C;
Legal status	℞ Prescription only;
Routes	oral, ocular
Pharmacokinetic data
Bioavailability	89%
Metabolism	Hepatic
Half-life	14–22 hours
Excretion	Renal (20%)
Identifiers
CAS number	63659-18-7
ATC code	C07AB05 S01ED02
PubChem	CID 2369
IUPHAR ligand	549
DrugBank	DB00195
ChemSpider	2279
UNII	O0ZR1R6RZ2
KEGG	D07526
ChEBI	CHEBI:3082
ChEMBL	CHEMBL423
Chemical data
Formula	C18H29NO3
Mol. mass	307.428 g/mol
	SMILES O(CCc1ccc(OCC(O)CNC(C)C)cc1)CC2CC2;
	InChI InChI=1S/C18H29NO3/c1-14(2)19-11-17(20)13-22-18-7-5-15(6-8-18)9-10-21-12-16-3-4-16/h5-8,14,16-17,19-20H,3-4,9-13H2,1-2H3 ; Key:NWIUTZDMDHAVTP-UHFFFAOYSA-N ;
(what is this?) (verify)