Atenolol

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Achtung

• Gefahrenhinweise

  H225：Flüssigkeit und Dampf leicht entzündbar.

  H319：Verursacht schwere Augenreizung.

• Sicherheit

  P210：Von Hitze, heißen Oberflächen, Funken, offenen Flammen und anderen Zündquellenarten fernhalten. Nicht rauchen.

  P261：Einatmen von Staub vermeiden.

  P337+P313：Bei anhaltender Augenreizung: Ärztlichen Rat einholen/ärztliche Hilfe hinzuziehen.

  P403+P235：An einem gut belüfteten Ort aufbewahren. Kühl halten.

Atenolol Chemische Eigenschaften,Einsatz,Produktion Methoden

• R-Sätze Betriebsanweisung:

  R22:Gesundheitsschädlich beim Verschlucken.
  R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
  R20/21/22:Gesundheitsschädlich beim Einatmen,Verschlucken und Berührung mit der Haut.

• S-Sätze Betriebsanweisung:

  S22:Staub nicht einatmen.
  S24/25:Berührung mit den Augen und der Haut vermeiden.
  S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
  S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.

• Chemische Eigenschaften

  White or almost white powder.

• Originator

  Tenormin,Stuart,UK,1976

• Verwenden

  It is used for preventing angina pectoris.

• Verwenden

  Selective b1 adrenergic receptor agonist, anti-hypertensive, anti-anginal, anti-arrhythmic

• Verwenden

  Atenolol is 2-[4′[2-hydroxy-3-(iso-propylamino)propoxy]phenyl]acetamide (12.1.7) [11–13].Atenolol is a selective β1-adrenoblocker, or in other words, a cardioblocker. Like acebutol, atenolol possesses antianginal, antihypotensive, and antiarrhythmic action. It is used for arterial hypotension, preventing attacks of angina, sinus tachycardia, and preventing supraventricular tachyarrhythmia.

• Definition

  ChEBI: An ethanolamine compound having a (4-carbamoylmethylphenoxy)methyl group at the 1-position and an N-isopropyl substituent.

• Manufacturing Process

  1 gram of 1-p-carbamoylmethylphenoxy-2,3-epoxypropane and 10 ml of isopropylamine in 25 ml of methanol is heated in a sealed tube at 110°C for 12 hours. The mixture is evaporated to dryness and the residue is partitioned between 50 ml of chloroform and 50 ml of aqueous 2 N hydrochloric acid. The aqueous acidic layer is separated, made alkaline with sodium carbonate and extracted twice with 50 ml of chloroform each time. The combined extracts are dried and evaporated to dryness and the residue is crystallized from ethyl acetate. There is thus obtained 1-p-carbamoylmethyiphenoxy-3- isopropylamino-2-propanol, MP 146-148°C.
  The 1-p-carbamoylmethylphenoxy-2,3-epoxypropane used as starting material may be obtained as follows: a mixture of 3.2 grams of phydroxyphenylacetamide, 25 ml of epichlorohydrin and 6 drops of piperidine is heated at 95-100°C for 6 hours. The mixture is cooled and filtered and the solid product is crystallized from methanol. There is thus obtained 1-pcarbamoylmethylphencxy- 2,3-epoxypropane, MP 158-160°C.

• Trademarks

  Tenormin (AstraZeneca).

• Therapeutic Function

  Beta-adrenergic blocker

• Allgemeine Beschreibung

  Pharmaceutical secondary standards for application in quality control provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards

• Biologische Aktivität

  Cardioselective β -adrenergic blocker. Antihypertensive, antianginal, antiarrhythmic.

• Biochem/physiol Actions

  Selective β1-adrenoceptor antagonist; antihypertensive; antianginal; antiarrhythmic.

• Clinical Use

  Beta-adrenoceptor blocker:
  
  Hypertension
  
  Angina
  
  Arrhythmias

• Veterinary Drugs and Treatments

  Atenolol may be useful in the treatment of supraventricular tachyarrhythmias, premature ventricular contractions (PVC’s, VPC’s), systemic hypertension and in treating cats with hypertrophic cardiomyopathy. Atenolol is relatively safe to use in animals with bronchospastic disease.

• in vitro

  (r,s)-atenolol was found to differ slightly regarding potency and to be practically equal regarding relative selectivity, while ici 141,292 had slightly higher relative selectivity and much higher potency. (r,s)-atenolol exhibited highest affinity for the beta 1-receptor population. in contrast, ici 118,551 exhibited a very high relative selectivity with highest affinity for the beta 2-receptor subtype [1].

• in vivo

  the renal effects of (r,s)-atenolol in rats were studied. results showed that the iv infusion of (r,s)-atenolol increased urinary sodium excretion, urine volume (uv), urinary potassium excretion and urinary chloride excretion. (r,s)-atenolo intraaortally injected produced an increase in uv and sodium concentration in the urine, inducing a more marked increase in total sodium amount excreted from both kidneys [2].

• Arzneimittelwechselwirkung

  Potentially hazardous interactions with other drugs Anaesthetics: enhanced hypotensive effect. Analgesics: NSAIDs antagonise hypotensive effect. Anti-arrhythmics: increased risk of myocardial depression and bradycardia; increased risk of bradycardia, myocardial depression and AV block with amiodarone; increased risk of myocardial depression and bradycardia with flecainide. Antidepressants: enhanced hypotensive effect with MAOIs.
  Antihypertensives: enhanced hypotensive effect; increased risk of withdrawal hypertension with clonidine; increased risk of first dose hypotensive effect with post-synaptic alpha-blockers such as prazosin.
  Antimalarials: increased risk of bradycardia with mefloquine.
  Antipsychotics enhanced hypotensive effect with phenothiazines.
  Calcium-channel blockers: increased risk of bradycardia and AV block with diltiazem; hypotension and heart failure possible with nifedipine and nisoldipine; asystole, severe hypotension and heart failure with verapamil.
  Cytotoxics: possible increased risk of bradycardia with crizotinib.
  Diuretics: enhanced hypotensive effect.
  Fingolimod: possibly increased risk of bradycardia.
  Moxisylyte: possible severe postural hypotension.
  Sympathomimetics: severe hypertension with
  adrenaline and noradrenaline and possibly with dobutamine.

• Stoffwechsel

  Roughly half of an orally administered dose of atenolol (Tenormin) is absorbed.The drug is eliminated primarily by the kidney and unlike propranolol, undergoes little hepatic metabolism. Its plasma half-life is approximately 6 hours, although if it is administered to a patient with impaired renal function, its half-life can be considerably prolonged.

• Einzelnachweise

  [1] golf, s. ,bjornerheim, r.,erichsen, a., et al. relative selectivity of different β-adrenoceptor antagonists for human heart β1- and β2-receptor subtypes assayed by a radioligand binding technique. scandinavian journal of clinical and laboratory investigation 47(7), 719-723 (1987).
  [2] yamazaki n, monma y, tanabe t. effects of propranolol and atenolol on the rat kidney. nihon yakurigaku zasshi. 1983 may;81(5):333-42.
  [3] stoschitzky k, egginger g, zernig g, klein w, lindner w. stereoselective features of (r)- and (s)-atenolol: clinical pharmacological, pharmacokinetic, and radioligand binding studies. chirality. 1993;5(1):15-9.

Atenolol Upstream-Materialien And Downstream Produkte

Atenolol Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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