Лабеталол
- английское имяLabetalol
- CAS №36894-69-6
- CBNumberCB7735086
- ФормулаC19H24N2O3
- мольный вес328.41
- EINECS253-258-3
- номер MDLMFCD00242941
- файл Mol36894-69-6.mol
химическое свойство
| Температура плавления | 188 °C |
| Температура кипения | 552.7±50.0 °C(Predicted) |
| плотность | 1.200±0.06 g/cm3(Predicted) |
| температура хранения | Store at -20°C |
| растворимость | DMSO : 125 mg/mL (380.62 mM; Need ultrasonic) |
| пка | pKa 7.41 ± 0.01；9.36± 0.01(H2O,t =25,I=0.15(KCl)，Ar)(Approximate) |
| форма | Solid |
| цвет | White to Pale Orange |
| Стабильность | Hygroscopic |
| Справочник по базе данных CAS | 36894-69-6(CAS DataBase Reference) |
| FDA UNII | R5H8897N95 |
| Код УВД | C07AG01 |
| Справочник по химии NIST | Benzamide, 2-hydroxy-5-[1-hydroxy-2-[(1-methyl-3-phenylpropyl)amino]ethyl]-(36894-69-6) |
| Банк данных об опасных веществах | 36894-69-6(Hazardous Substances Data) |
рисовальное письмо(GHS)
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рисовальное письмо(GHS)
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сигнальный язык
предупреждение
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вредная бумага
H315：При попадании на кожу вызывает раздражение.
H319：При попадании в глаза вызывает выраженное раздражение.
H335：Может вызывать раздражение верхних дыхательных путей.
H411：Токсично для водных организмов с долгосрочными последствиями.
H361：Предполагается, что данное вещество может отрицательно повлиять на способность к деторождению или на неродившегося ребенка.
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оператор предупредительных мер
P201：Беречь от тепла, горячих поверхностей, искр, открытого огня и других источников воспламенения. Не курить.
P202：Перед использованием ознакомиться с инструкциями по технике безопасности.
P264：После работы тщательно вымыть кожу.
P280：Использовать перчатки/ средства защиты глаз/ лица.
P281：Пользоваться надлежащим индивидуальным защитным снаряжением.
P302+P352：ПРИ ПОПАДАНИИ НА КОЖУ: Промыть большим количеством воды.
P305+P351+P338：ПРИ ПОПАДАНИИ В ГЛАЗА: Осторожно промыть глаза водой в течение нескольких минут. Снять контактные линзы, если Вы ими пользуетесь и если это легко сделать. Продолжить промывание глаз.
P308+P313：ПРИ подозрении на возможность воздействия обратиться за медицинской помощью.
P332+P313：При возникновении раздражения кожи: обратиться за медицинской помощью.
P405：Хранить в недоступном для посторонних месте.
P501：Удалить содержимое/ контейнер на утвержденных станциях утилизации отходов.
Лабеталол химические свойства, назначение, производство
Описание
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.Использование
Labetalol is used to treat essential hypertension.Определение
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.Биологические функции
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.Общее описание
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.Контактные аллергены
This beta-adrenergic and alpha-1 blocking agent caused contact dermatitis and a contact anaphylactoid reaction during patch testing in a nurse.Механизм действия
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.
Фармакокине?тика
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.Клиническое использование
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.Побочные эффекты
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.
Лабеталол запасные части и сырье
Лабеталол поставщик
| поставщик | телефон | страна | номенклатура продукции | благоприятные условия |
|---|---|---|---|---|
| 18871490254 | CHINA | 28172 | 58 | |
| +86-0371-86658258 +8613203830695 |
China | 30241 | 58 | |
| +86-0551-65418671 +8618949823763 |
China | 34553 | 58 | |
| 0917-3909592 13892490616 |
China | 9315 | 58 | |
| 0592-5800732; +8613806035118 |
China | 988 | 58 | |
| +8617013299288 | China | 12373 | 58 | |
| +1-708-310-1919 +1-13798911105 |
United States | 6391 | 58 | |
| +86-592-5360779 +86-13055435203 |
China | 5988 | 58 | |
| +86-0576225566889 +86-13454675544 |
China | 12272 | 58 | |
| +undefined18621343501 | China | 33338 | 58 |