Labetalol

Labetalol Struktur
36894-69-6
CAS-Nr.
36894-69-6
Bezeichnung:
Labetalol
Englisch Name:
Labetalol
Synonyma:
Laβlol;ah5158;albetol;LABEIM-B;LABETOLOL;LABETALOL;ibidomide;SeH-15719W;Labeint-A8;Labetalol (AH-5158
CBNumber:
CB7735086
Summenformel:
C19H24N2O3
Molgewicht:
328.41
MOL-Datei:
36894-69-6.mol

Labetalol Eigenschaften

Schmelzpunkt:
188 °C
Siedepunkt:
552.7±50.0 °C(Predicted)
Dichte
1.200±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
Löslichkeit
DMSO : 125 mg/mL (380.62 mM; Need ultrasonic)
pka
pKa 7.41 ± 0.01;9.36± 0.01(H2O,t =25,I=0.15(KCl),Ar)(Approximate)
Aggregatzustand
Solid
Farbe
White to Pale Orange
Stabilität:
Hygroscopic
CAS Datenbank
36894-69-6(CAS DataBase Reference)
NIST chemische Informationen
Benzamide, 2-hydroxy-5-[1-hydroxy-2-[(1-methyl-3-phenylpropyl)amino]ethyl]-(36894-69-6)
Sicherheit
  • Risiko- und Sicherheitserklärung
  • Gefahreninformationscode (GHS)
Bildanzeige (GHS) GHS hazard pictogramsGHS hazard pictogramsGHS hazard pictograms
Alarmwort Warnung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H315 Verursacht Hautreizungen. Hautreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P302+P352, P321,P332+P313, P362
H319 Verursacht schwere Augenreizung. Schwere Augenreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P305+P351+P338,P337+P313P
H335 Kann die Atemwege reizen. Spezifische Zielorgan-Toxizität (einmalige Exposition) Kategorie 3 (Atemwegsreizung) Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" />
H361 Kann vermutlich die Fruchtbarkeit beeinträchtigen oder das Kind im Mutterleib schädigen. Reproduktionstoxizität Kategorie 2 Warnung P201, P202, P281, P308+P313, P405,P501
H411 Giftig für Wasserorganismen, mit langfristiger Wirkung. Langfristig (chronisch) gewässergefährdend Kategorie 2
Sicherheit
P201 Vor Gebrauch besondere Anweisungen einholen.
P202 Vor Gebrauch alle Sicherheitshinweise lesen und verstehen.
P264 Nach Gebrauch gründlich waschen.
P264 Nach Gebrauch gründlich waschen.
P280 Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.
P281 Vorgeschriebene persönliche Schutzausrüstung verwenden.
P302+P352 BEI BERÜHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckmäßig, ein Reinigungsmittel angeben oder, wenn Wasser eindeutig ungeeignet ist, ein alternatives Mittel empfehlen) waschen.
P305+P351+P338 BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen.
P308+P313 BEI Exposition oder falls betroffen: Ärztlichen Rat einholen/ärztliche Hilfe hinzuziehen.
P321 Besondere Behandlung
P332+P313 Bei Hautreizung: Ärztlichen Rat einholen/ärztliche Hilfe hinzuziehen.
P362 Kontaminierte Kleidung ausziehen und vor erneutem Tragen waschen.
P405 Unter Verschluss aufbewahren.
P501 Inhalt/Behälter ... (Entsorgungsvorschriften vom Hersteller anzugeben) zuführen.

Labetalol Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Labetalol is an α-adrenergic and α-1 blocking agent which caused contact dermatitis and a contact anaphylactoid reaction during patch testing in a nurse.

Verwenden

Labetalol is used to treat essential hypertension.

Definition

ChEBI: A secondary amino compound formally derived from ammonia by replacing two of the hydrogens by 2-(3-carbamoyl-4-hydroxyphenyl)-2-hydroxyethyl and 4-phenylbutan-2-yl groups. It is an adrenergic antagonist used to treat high blood pressure.

Biologische Funktion

Labetalol (Normodyne, Trandate) possesses both - blocking and β-blocking activity and is approximately one-third as potent as propranolol as a -blocker and one-tenth as potent as phentolamine as an -blocker. The ratio of β- to α-activity is about 3:1 when labetalol is administered orally and about 7: 1 when it is administered intravenously. Thus the drug can be most conveniently thought of as a β -blocker with some -blocking properties.

Allgemeine Beschreibung

Labetalol is a phenylethanolamine derivative, is representative of a classof drugs that act as competitive blockers at α1-, β1-, andβ2-receptors. It is a more potent β-blocker than α-blocker.Because it has two asymmetric carbon atoms (1 and 1' ), it existsas a mixture of four isomers. It is this mixture that is usedclinically in treating hypertension. The different isomers,however, possess different α- and β-blocking activities. The -blocking activity resides solely in the (1R,1 'R) isomer,whereas the 1-blocking activity is seen in the (1S,1 R) and(1S,1'S) isomers, with the (1S,1'R) isomer possessing thegreater therapeutic activity.

Kontakt-Allergie

This beta-adrenergic and alpha-1 blocking agent caused contact dermatitis and a contact anaphylactoid reaction during patch testing in a nurse.

Mechanism of action

Labetalol produces equilibrium-competitive antagonism at β-receptors but does not exhibit selectivity for β1- or β2-receptors. Like certain other β-blockers (e.g., pindolol and timolol), labetalol possesses some degree of intrinsic activity. This intrinsic activity, or partial agonism, especially at β2-receptors in the vasculature, has been suggested to contribute to the vasodilator effect of the drug. The membrane-stabilizing effect, or local anesthetic action, of propranolol and several other β-blockers, is also possessed by labetalol, and in fact the drug is a reasonably potent local anesthetic.
Labetalol appears to produce relaxation of vascular smooth muscle not only by α-blockade but also by a partial agonist effect at β2-receptors. In addition, labetalol may produce vascular relaxation by a direct non–receptor-mediated effect. Labetalol can block the neuronal uptake of norepinephrine and other catecholamines. This action, plus its slight intrinsic activity at α-receptors, may account for the seemingly paradoxical, although infrequent, increase in blood pressure seen on its initial administration.

Pharmakokinetik

Labetalol is almost completely absorbed from the gastrointestinal tract. However, it is subject to considerable first-pass metabolism, which occurs in both the gastrointestinal tract and the liver, so that only about 25% of an administered dose reaches the systemic circulation. While traces of unchanged labetalol are recovered in the urine, most of the drug is metabolized to inactive glucuronide conjugates.The plasma half-life of labetalol is 6 to 8 hours, and the elimination kinetics are essentially unchanged in patients with impaired renal failure.

Clinical Use

Labetalol is a clinically usefulantihypertensive agent. The rationale for its use in themanagement of hypertension is that its α-receptor–blockingeffects produce vasodilation and its β-receptor–blockingeffects prevent the reflex tachycardia usually associated withvasodilation. Although labetalol is very well absorbed, it undergoesextensive first-pass metabolism.

Nebenwirkungen

There have been reports of excessive hypotension and paradoxical pressor effects following intravenous administration of labetalol. These latter effects may be due to a labetalol-induced blockade of neuronal amine uptake, which increases the concentrations of norepinephrine in the vicinity of its receptors.
Approximately 5% of the patients who receive labetalol complain of side effects typical of noradrenergic nervous system suppression. These include postural hypotension, gastrointestinal distress, tiredness, sexual dysfunction, and tingling of the scalp. Most of these effects are related to α-blockade, although the tingling of the scalp may be due to the drug’s intrinsic activity at α-receptors. Side effects associated with β-blockade, such as induction of bronchospasm and congestive heart failure, may also occur, but generally at a lower frequency than -receptor–associated effects.
Skin rashes have been reported, as has an increase in the titer of antinuclear antibodies. Despite the latter observation, the appearance of a systemic lupus syndrome is rare. Labetalol also has been reported to interfere with chemical measurements of catecholamines and metabolites.

Labetalol Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Labetalol Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global( 100)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Hubei Jusheng Technology Co.,Ltd.
18871490254
linda@hubeijusheng.com CHINA 28180 58
Career Henan Chemica Co
+86-0371-86658258 15093356674;
laboratory@coreychem.com China 30255 58
Hefei TNJ Chemical Industry Co.,Ltd.
0551-65418671
sales@tnjchem.com China 34572 58
Baoji Guokang Bio-Technology Co., Ltd.
0917-3909592 13892490616
gksales1@gk-bio.com China 9333 58
Sinoway Industrial co., ltd.
0592-5800732; +8613806035118
xie@china-sinoway.com China 992 58
sgtlifesciences pvt ltd
+8617013299288
dj@sgtlifesciences.com China 12382 58
InvivoChem
+1-708-310-1919 +1-13798911105
sales@invivochem.cn United States 6393 58
LUYUNJIA CHEMISTRY XIAMEN LIMITED
+86-592-5360779 +86-13055435203
China 5996 58
Shanghai Acmec Biochemical Technology Co., Ltd.
+undefined18621343501
product@acmec-e.com China 33350 58
Aladdin Scientific
+1-833-552-7181
sales@aladdinsci.com United States 57511 58

36894-69-6(Labetalol)Verwandte Suche:


  • 5-[1-HYDROXY-2-[(1-METHYL-3-PHENYLPROPYLAMINO)ETHYL]]SALICYLAMIDE
  • LABETALOL
  • LABETOLOL
  • 5-[1-hydroxy-2-[(1-methyl-3-phenylpropylamino)ethyl]saicylamide
  • Labetalol (base and/or unspecified salts)
  • SeH-15719W
  • 2-hydroxy-5-[(1S)-1-hydroxy-2-{[(2R)-4-phenylbutan-2-yl]aMino}ethyl]benzaMide
  • Laβlol
  • BenzaMide,2-hydroxy-5-[1-hydroxy-2-[(1-Methyl-3-phenylpropyl)aMino]ethyl]-
  • 2-Hydroxy-5-(1-hydroxy-2-((4-phenylbutan-2-yl)amino)ethyl)benzamide
  • 2-Hydroxy-5-(1-hydroxy-2-((4-phenylbutan-2-yl)
  • 2-hydroxy-5-(1-hydroxy-2-((1-methyl-3-phenylpropyl)amino)ethyl)-benzamid
  • 2-hydroxy-5-(1-hydroxy-2-((1-methyl-3-phenylpropyl)amino)ethyl)benzamide
  • 3-carboxamido-4-hydroxy-alpha-((1-methyl-3-phenylpropylamino)methyl)benzyla
  • ah5158
  • albetol
  • ibidomide
  • LABEIM-B
  • Labeint-A8
  • Labetalol USP/EP/BP
  • Labetalol (AH-5158
  • 1H-Benzimidazole-1-carboxylicacid,2,3-dihydro-4-oxo-,ethylester
  • Sch-15719W free base
  • 36894-69-6
  • C19H24N2O3
  • API's
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