Tenormin

アテノロール

WordNet

1. 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）』「2014/04/10 20:13:19」(JST)

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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 cat.	C (AU) D (US)
Legal status	℞ Prescription only
Routes	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 number	29122-68-7 Y
ATC code	C07AB03
PubChem	CID 2249
IUPHAR ligand	548
DrugBank	DB00335
ChemSpider	2162 Y
UNII	50VV3VW0TI Y
KEGG	D00235 Y
ChEBI	CHEBI:2904 Y
ChEMBL	CHEMBL24 Y
Chemical data
Formula	C14H22N2O3
Mol. 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) Y Key:METKIMKYRPQLGS-UHFFFAOYSA-N Y
Y (what is this?)  (verify)

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. The chemical 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.

Atenolol is one of the most widely used β-blockers in the United Kingdom and was once the first-line treatment for hypertension. 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.

Medical uses

Atenolol is used for a number of conditions including: hypertension, angina, Long cough, acute myocardial infarction, supraventricular tachycardia, ventricular tachycardia, and the symptoms of alcohol withdrawal.

It is also used to treat the symptoms of Graves' disease until antithyroid medication can take effect.

Due to its hydrophilic 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.^{[citation needed]}

Hypertension

Atenolol is currently recommended only in special circumstances as complementary medication in hypertension. More frequently one or more of ACE Inhibitors, calcium antagonists and or diuretics are used as first line therapy.

Contraindications

• bradycardia (pulse less than 60 bpm)
• cardiogenic shock
• asthma (may cause broncho-constriction).
• symptomatic hypotension (blood pressure of less than 90/60 mm Hg with dizziness, vertigo etc.)
• angina of the Prinzmetal type (vasospastic angina)
• metabolic acidosis (a severe condition with a more acidic blood than normal)
• severe disorders in peripheral arterial circulation
• Atrioventricular blockage of second and third degree (a particular form of arrhythmia)
• acutely decompensated congestive heart failure (symptoms may be fluid retention with peripheral edema and/or abdominal fluid retention (ascites), and/or lung edema)
• sick sinus syndrome (a particular form of arrhythmia)
• hypersensitivity and/or allergy to atenolol
• pheochromocytoma (a rare type of tumor of the adrenal glands)
• Atenolol should not be taken by patients with preexisting bronchial asthma.^{[citation needed]}
• Atenolol may retard fetal growth and possibly cause other abnormalities, and is classified by FDA in pregnancy category D. It should be used during pregnancy only if absolutely necessary.

Side effects

See also: Beta blocker

Atenolol causes significantly fewer central nervous system side effects (depression, nightmares).

It 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.

In addition, β-blockers blunt the usual sympathetic nervous system response to hypoglycemia (i.e. sweating, agitation, tachycardia). These drugs therefore have an ability to mask a dangerously low blood sugar, which further decreases their safety and utility in diabetic patients.

Side effects have been known to include the following:^{[citation needed]}

• indigestion, constipation
• dry mouth
• dizziness or faintness (especially cases of orthostatic hypotension)
• cold extremities
• impotence
• rhinitis
• depression
• confusion
• insomnia, nightmares
• fatigue, weakness or lack of energy
• edema

The following more-serious side effects have also been observed and/or reported:^{[citation needed]}

• hallucinations
• low blood pressure (hypotension)
• skin reactions, e.g. rash, hives, flaking of skin, worsening of psoriasis
• sensation of 'pins and needles' hands or feet
• irritated eyes, visual disturbances
• difficulty hearing
• difficulty speaking
• unsteadiness when walking

Atenolol is classified as a β₁-selective (or 'cardioselective') drug, one that exerts greater blocking activity on myocardial β₁-receptors than on β₂ receptors in the lung. The β₂ receptors are responsible for keeping the bronchial system open. If these receptors are blocked, bronchospasm with serious lack of oxygen in the body can result. However, due to its cardioselective properties, the risk of bronchospastic reactions if using atenolol is reduced compared to nonselective drugs as propranolol. Nonetheless, this reaction may also be encountered with atenolol at high doses. Although traditionally β-blockers have been contraindicated when a person carries a diagnosis of asthma, recent studies have revealed that at moderate doses selective β-blockers such as Atenolol are well tolerated.

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.

Unlike most other commonly used β-blockers, atenolol is excreted almost exclusively by the kidneys. This makes it attractive for use in individuals with end-stage liver disease.

Overdose

Symptoms of overdose are due to excessive pharmacodynamic actions on β₁ and also β₂-receptors. These include bradycardia, 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.

Pharmacokinetic data

• t_cmax = 2 to 4 hours after oral dosing (time elapsed before maximal concentration in the blood plasma is reached)
• The mean elimination halflife is 6 hours. However, the action of the usual oral dose of 25 to 100 mg lasts over a period of 24 hours.
• Atenolol is a hydrophilic drug. The concentration found in brain tissue is approximately 15% of the plasma concentration only. The drug crosses the placenta barrier freely. In the milk of breastfeeding mothers, approximately 3 times the plasma concentrations are measured.
• Atenolol is almost exclusively eliminated renally and is well removable by dialysis. A compromised liver function does not lead to higher peak-activity and/or a longer halflife with possible accumulation.

References

7. .K.Viveksarathi et al.,Formulation Development and In-Vitro Evaluation of Gastroretentive Floating tablets of Atenolol. Journal of Pharmaceutical Sciences & Research;2011, Vol.3(12),p1632. http://www.jpsr.pharmainfo.in/Documents/Volumes/vol3Issue12/jpsr%2003111207.pdf

External links

• "Beta-blockers 'increase diabetes risk by 50 per cent'". Daily Mail. 

UpToDate Contents

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• 1. Testing for drugs of abuse (DOA)
• 2. β遮断剤の主な副作用 major side effects of beta blockers
• 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. 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
• 5. 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

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

• β1-noradrenergic system of the central amygdala is involved in state-dependent memory induced by a cannabinoid agonist, WIN55,212-2, in rat.

• Ghiasvand M, Rezayof A, Ahmadi S, Zarrindast MR.SourceInstitute for Cognitive Science Studies, Tehran, Iran.
• Behavioural brain research.Behav Brain Res.2011 Nov 20;225(1):1-6. Epub 2011 Jun 17.
• In the present study, we investigated effects of intra-central amygdala (intra-CeA) administrations of a β1-receptor agonist and antagonist, isoprenaline (isoproterenol) and atenolol respectively, on state-dependent memory induced by a cannabioid agonist, WIN55,212-2. This study used a step-through
• PMID 21704654

Japanese Journal

• 鈍的胸部大動脈損傷に右鎖骨下動脈損傷を合併した１例

• 松浦 正徒,西本 昌義,阿部 紘一郎,秋元 寛
• 日本救急医学会雑誌 19(9), 943-949, 2008
• 症例は58歳の男性。バイク運転中に停車中の自動車に衝突し，救急隊により初期評価で意識障害（JCS 100）を認められたためload and goと判断され当センターに救急搬送された。来院時，患者に意識障害（JCS 10）を認めたが，focused assessment with sonography for trauma（FAST）陰性，血圧は安定しており外出血は認めなかった。胸腹部造影CTで胸部 …
• NAID 130004542214

• 新しいβ遮断薬Atenolol(Tenormin)の狭心症に対する臨床効果--多施設によるopen trial

• 小林 太刀夫 [他]
• 臨牀と研究 58(6), p2021-2034, 1981-06
• NAID 40003786985

Related Links

• Tenormin: Uses, Dosage & Side Effects - Drugs.com

Tenormin side effects Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Call your doctor at once if you have any of these serious ...

• アテノロール:テノーミン - プロバイダー｜interQ MEMBERS

テノーミンとは?アテノロールの効能,副作用等を説明,ジェネリックや薬価も調べられる(おくすり110番:薬事典版) ... 概説 血圧を下げるお薬です。また、狭心症や不整脈の治療にも使用します。 作用 心拍をおさえ心臓を休ませる作用が ...

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★リンクテーブル★

リンク元	「アテノロール」「atenolol」

「アテノロール」

　　[★]

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)

「atenolol」

　　[★] アテノロール

同

Tenormin