同: Tenormin

WordNet

an oral beta blocker (trade name Tenormin) used in treating hypertension and angina; has adverse side effects (depression and exacerbation of congestive heart failure etc.) (同)Tenormin

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/04/27 09:43:48」(JST)

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Atenolol is a selective β₁ receptor antagonist, a drug belonging to the group of beta blockers (sometimes written β-blockers), a class of drugs used primarily in cardiovascular diseases. Introduced in 1976, atenolol was developed as a replacement for propranolol in the treatment of hypertension. It works by slowing down the heart and reducing its workload. Unlike propranolol, atenolol does not pass through the blood–brain barrier thus avoiding various central nervous system side effects.^[1]

Atenolol is one of the most widely used β-blockers in the United Kingdom and was once the first-line treatment for hypertension.^{[citation needed]} The role for β-blockers in hypertension was downgraded in June 2006 in the United Kingdom to fourth-line, as they perform less appropriately or effectively than newer drugs, particularly in the elderly.^{[citation needed]}

Medical uses

Atenolol is used for a number of conditions including: hypertension, angina, long QT syndrome, acute myocardial infarction, supraventricular tachycardia, ventricular tachycardia, and the symptoms of alcohol withdrawal.^[2]

Due to its hydrophilic (water-attracting) properties, the drug is less suitable in migraine prophylaxis compared to propranolol, because, for this indication, atenolol would have to reach the brain in high concentrations, which is not the case, because atenolol does not pass through the blood–brain barrier.^[1]

Side effects

Atenolol was the main β-blocker identified as carrying a higher risk of provoking type 2 diabetes, leading to its downgrading in the United Kingdom in June 2006 to fourth-line agent in the management of hypertension.^[3]

Provisional data suggests that antihypertensive therapy with atenolol provides weaker protective action against cardiovascular complications (e.g. myocardial infarction and stroke) compared to other antihypertensive drugs. In some cases, diuretics are superior. However, controlled studies are lacking.^[4]

Overdose

Symptoms of overdose are due to excessive pharmacodynamic actions on β₁ and also β₂-receptors. These include bradycardia (slow heartbeat), severe hypotension with shock, acute heart failure, hypoglycemia and bronchospastic reactions. Treatment is largely symptomatic. Hospitalization and intensive monitoring is indicated. In early cases emesis can be induced. Activated charcoal is useful to absorb the drug. Atropine will counteract bradycardia, glucagon helps with hypoglycemia, dobutamine can be given against hypotension and the inhalation of a β₂-mimetic as hexoprenalin or salbutamol will terminate bronchospasms. Blood or plasma atenolol concentrations may be measured to confirm a diagnosis of poisoning in hospitalized patients or to assist in a medicolegal death investigation. Plasma levels are usually less than 3 mg/L during therapeutic administration, but can range from 3–30 mg/L in overdose victims.^[5]^[6]

References

^ ^a ^b Agon P, Goethals P, Van Haver D, Kaufman JM (August 1991). "Permeability of the blood–brain barrier for atenolol studied by positron emission tomography". J. Pharm. Pharmacol. 43 (8): 597–600. doi:10.1111/j.2042-7158.1991.tb03545.x. PMID 1681079.
^ "Atenolol". The American Society of Health-System Pharmacists. Retrieved 3 April 2011.
^ Sheetal Ladva (2006-06-28). "NICE and BHS launch updated hypertension guideline". National Institute for Health and Clinical Excellence.
^ Carlberg B, Samuelsson O, Lindholm LH (2004). "Atenolol in hypertension: is it a wise choice?". Lancet 364 (9446): 1684–9. doi:10.1016/S0140-6736(04)17355-8. PMID 15530629.
^ DeLima LG, Kharasch ED, Butler S (1995). "Successful pharmacologic treatment of massive atenolol overdose: sequential hemodynamics and plasma atenolol concentrations". Anesthesiology 83 (1): 204–207. doi:10.1097/00000542-199507000-00025. PMID 7605000.
^ R. Baselt (2008). Disposition of Toxic Drugs and Chemicals in Man (8th ed.). Foster City, CA: Biomedical Publications. pp. 116–117.

External links

Hope, Jenny (6 September 2006). "Beta-blockers 'increase diabetes risk by 50 per cent'". London: Daily Mail.

UpToDate Contents

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1. β遮断剤の主な副作用 major side effects of beta blockers
2. β遮断剤による甲状腺機能亢進症の治療 beta blockers in the treatment of hyperthyroidism
3. 原発性（本態性）高血圧における治療選択：臨床試験 choice of therapy in primary essential hypertension clinical trials
4. 安定狭心症のマネージメントにおけるβ遮断剤 beta blockers in the management of stable angina pectoris
5. 成人におけるグレーブス甲状腺機能亢進症の治療 treatment of graves hyperthyroidism in adults

English Journal

Simultaneous determination of binary mixture of amlodipine besylate and atenolol based on dual wavelengths.

Lamie NT1.
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy.Spectrochim Acta A Mol Biomol Spectrosc.2015 Oct 5;149:201-7. doi: 10.1016/j.saa.2015.04.077. Epub 2015 Apr 30.
Four, accurate, precise, and sensitive spectrophotometric methods are developed for simultaneous determination of a binary mixture of amlodipine besylate (AM) and atenolol (AT). AM is determined at its λmax 360nm ((0)D), while atenolol can be determined by four different methods. Method (A) is abso
PMID 25958126

Charge-transfer complexes of 2,3-dichloro-5,6-dicyano-1,4-benzoquinone with amino molecules in polar solvents.

Berto S1, Chiavazza E2, Ribotta V1, Daniele PG1, Barolo C3, Giacomino A4, Vione D1, Malandrino M1.
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy.Spectrochim Acta A Mol Biomol Spectrosc.2015 Oct 5;149:75-82. doi: 10.1016/j.saa.2015.04.044. Epub 2015 Apr 25.
The charge-transfer complexes have scientific relevance because this type of molecular interaction is at the basis of the activity of pharmacological compounds and because the absorption bands of the complexes can be used for the quantification of electron donor molecules. This work aims to assess t
PMID 25942088

Combination of UV absorbance and electron donating capacity to assess degradation of micropollutants and formation of bromate during ozonation of wastewater effluents.

Chon K1, Salhi E2, von Gunten U3.
Water research.Water Res.2015 Sep 15;81:388-97. doi: 10.1016/j.watres.2015.05.039. Epub 2015 May 21.
In this study, the changes in UV absorbance at 254 nm (UVA254) and electron donating capacity (EDC) were investigated as surrogate indicators for assessing removal of micropollutants and bromate formation during ozonation of wastewater effluents. To measure the EDC, a novel method based on size exc
PMID 26140990

Japanese Journal

β1-adrenergic receptor gene polymorphisms and the acute response to atenolol in healthy young Japanese subjects

Sasaguri Toshiyuki,Shiraishi Fumie,Yoshihara Tatsuya [他]
Journal of pharmacological sciences 115(4), 490-499, 2011-04
NAID 40018766384

Possible Involvement of β1 Receptors in Various Emetogen-Induced Increases in Salivary Amylase Activity in Rats

Fukui Hideo,Suyama Yoshimi,Iwachido Takako [他],Miwa Eri
Journal of Pharmacological Sciences advpub(0), 1012130486, 2010
… Isoprenaline (0.01 mg/kg, s.c.) produced an increase in salivary amylase and the increase was inhibited by the β1/2-AR antagonist propranolol (5 mg/kg, s.c.) and β1-AR antagonist atenolol (2 mg/kg, s.c.) but not by the β2-AR antagonist butoxamine (8 mg/kg, s.c.). … The increased amylase activity induced by cisplatin (15 mg/kg, i.v.), apomorphine (3 mg/kg, s.c.), or LiCl (120 mg/kg, i.p.) was inhibited significantly by atenolol (2 mg/kg, s.c.) but not by butoxamine (8 mg/kg, s.c.). …
NAID 130000439925

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★リンクテーブル★

リンク元

「アテノロール」

Atenolol
Systematic (IUPAC) name
	(RS)-2-{4-[2-Hydroxy-3-(propan-2-ylamino)propoxy]phenyl}acetamide
Clinical data
Trade names	Tenormin
AHFS/Drugs.com	monograph
MedlinePlus	a684031
Licence data	US FDA:link
Pregnancy; category	AU: C; US: D (Evidence of risk);
Legal status	℞ (Prescription only);
Routes of; administration	Oral or IV
Pharmacokinetic data
Bioavailability	40-50%
Protein binding	6-16%
Metabolism	Hepatic <10%
Half-life	6-7 hours
Excretion	Renal; Lactic (In lactiferous females)
Identifiers
CAS Registry Number	29122-68-7
ATC code	C07AB03
PubChem	CID 2249
IUPHAR ligand	548
DrugBank	DB00335
ChemSpider	2162
UNII	50VV3VW0TI
KEGG	D00235
ChEBI	CHEBI:2904
ChEMBL	CHEMBL24
Chemical data
Formula	C14H22N2O3
Molecular mass	266.336 g/mol
	SMILES O=C(N)Cc1ccc(OCC(O)CNC(C)C)cc1;
	InChI InChI=1S/C14H22N2O3/c1-10(2)16-8-12(17)9-19-13-5-3-11(4-6-13)7-14(15)18/h3-6,10,12,16-17H,7-9H2,1-2H3,(H2,15,18) ; Key:METKIMKYRPQLGS-UHFFFAOYSA-N ;
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　　[★]

英: atenolol
商: アテネミール、アテノリズム、アルセノール、アルマイラー、カテノミン、クシセミン、セーブテンス、セーラジール、テネミール、テノーミン Tenormin、テノミロール、トーワミン、ミロベクト、メゾルミン、メチニン、リスモリース
関: アドレナリン受容体、ビソプロロールメインテート。不整脈用剤

β1選択性β遮断薬。

作用機序

心臓のβ1受容体を選択的に阻害。

適応

本態性高血圧症、狭心症、頻脈性不整脈(洞性頻脈、期外収縮)

[BBB-1] Agon P, Goethals P, Van Haver D, Kaufman JM (August 1991). "Permeability of the blood–brain barrier for atenolol studied by positron emission tomography". J. Pharm. Pharmacol. 43 (8): 597–600. doi:10.1111/j.2042-7158.1991.tb03545.x. PMID 1681079.

[AHFS-2] "Atenolol". The American Society of Health-System Pharmacists. Retrieved 3 April 2011.

[NHSnews-3] Sheetal Ladva (2006-06-28). "NICE and BHS launch updated hypertension guideline". National Institute for Health and Clinical Excellence.

[pmid15530629-4] Carlberg B, Samuelsson O, Lindholm LH (2004). "Atenolol in hypertension: is it a wise choice?". Lancet 364 (9446): 1684–9. doi:10.1016/S0140-6736(04)17355-8. PMID 15530629.

[5] DeLima LG, Kharasch ED, Butler S (1995). "Successful pharmacologic treatment of massive atenolol overdose: sequential hemodynamics and plasma atenolol concentrations". Anesthesiology 83 (1): 204–207. doi:10.1097/00000542-199507000-00025. PMID 7605000.

[6] R. Baselt (2008). Disposition of Toxic Drugs and Chemicals in Man (8th ed.). Foster City, CA: Biomedical Publications. pp. 116–117.

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atenolol