WordNet

a complex consisting of an organic base in association with hydrogen chloride

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/05/08 07:02:04」(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. 原発性乳児緑内障 primary infantile glaucoma
3. 開放隅角緑内障：治療 open angle glaucoma treatment
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
5. 過敏性腸症候群に対するアロセトロン塩酸塩（Lotronex） alosetron hydrochloride lotronex for irritable bowel syndrome

English Journal

Electrically enhanced microextraction for highly selective transport of three β-blocker drugs.

Seidi S, Yamini Y, Rezazadeh M.SourceDepartment of Chemistry, Tarbiat Modares University, P.O. Box 14115-175, Tehran, Iran.
Journal of pharmaceutical and biomedical analysis.J Pharm Biomed Anal.2011 Dec 15;56(5):859-66. Epub 2011 Jul 29.
Facilitated transport of three β-blocker drugs including atenolol (ATE), betaxolol (BET) and propranolol (PRO) was investigated under electrical field across a supported liquid membrane (SLM) using phosphoric acid derivatives as selective ion carriers, dissolved in 2-nitro phenyl octyl ether (NPOE)
PMID 21856103

Intraocular pressure reduction with a fixed treatment protocol in the Early Manifest Glaucoma Trial.

Heijl A, Leske MC, Hyman L, Yang Z, Bengtsson B; EMGT Group.SourceDepartment of Ophthalmology, Lund University, Malmö University Hospital, Malmö, Sweden. anders.heijl@med.lu.se
Acta ophthalmologica.Acta Ophthalmol.2011 Dec;89(8):749-54. doi: 10.1111/j.1755-3768.2009.01852.x. Epub 2010 Mar 17.
PURPOSE: To evaluate: (i) the relationship between intraocular pressure (IOP) reduction attained with a fixed treatment protocol and the untreated IOP level; (ii) the consistency of IOP reduction over time; and (iii) whether there is a threshold pretreatment IOP level below which IOP reduction might
PMID 20236252

Fatal rhabdomyolysis in a patient with liver cirrhosis after switching from simvastatin to fluvastatin.

Baek SD, Jang SJ, Park SE, Ok TJ, Leem J, Lee HS, Park SJ, Kim TH.SourceDepartment of Internal Medicine, Asan Medical Center, University of Ulsan College of Medicine, Seoul, Korea.
Journal of Korean medical science.J Korean Med Sci.2011 Dec;26(12):1634-7. Epub 2011 Nov 29.
HMG-CoA reductase inhibitors (statins) are widely used to treat hypercholesterolemia. Among the adverse effects associated with these drugs are statin-associated myopathies, ranging from asymptomatic elevation of serum creatine kinase to fatal rhabdomyolysis. Fluvastatin-induced fatal rhabdomyolysis
PMID 22148003

Japanese Journal

Effect of Betaxolol Hydrochloride on Heart Rate Variability Indices during Exercise Stress Testing in Hypertensive Patients(Exercise Test/Cardiac Rehabilitation 3 (IHD), The 69th Annual Scientific Meeting of the Japanese Circulation Society)

Takase Bonpei,Hamane Akira,Akima Takashi,Matsui Takemi,Arakawa Koh,Kusuhara Masatoshi,Ohsuzu Fumitaka,Ishihara Masayuki,Kuirta Akira
Circulation journal : official journal of the Japanese Circulation Society 69(Supplemnt_I), 425, 2005-03-01
NAID 110004053194

Beta1-adrenergic receptor polymorphisms and clinical efficacy of betaxolol hydrochloride in normal volunteers

SCHWARTZ SG
Ophthalmology 112, 2131-2136, 2005
NAID 30009691957

正常眼圧緑内障患者におけるβ-ブロッカー点眼薬ノンレスポンダーの検討

池田陽子,森和彦,石橋健,成瀬繁太,小林ルミ,南條由佳子,水野秀信,中島伸子,木下茂
あたらしい眼科 = Journal of the eye 20(10), 1435-1437, 2003-10-30
NAID 10017018173

Related Pictures

★リンクテーブル★

リンク元	「ベタキソロール」
関連記事	「betaxolol」「hydrochloride」

「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.	C (AU) C (US)
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)