Labetalol
(Synonyms: 拉贝洛尔,AH5158; Sch-15719W free base) 目录号 : GC64143
An antagonist of α- and β-adrenoreceptors
Cas No.:36894-69-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Labetalol is a competitive antagonist of both α- and β-adrenoreceptors that is effective at nanomolar concentrations.1,2 It is reported to control hypertension.3,4
1.Brittain, R.T., and Levy, G.P.A review of the animal pharmacology of labetalol, a combined α- and β-adrenoceptor-blocking drugBr. J. Clin. Pharmacol.3(4 suppl 3)681-684(1976) 2.Richards, D.A.Pharmacological effects of labetalol in manBr. J. Clin. Pharmacol.3(4 suppl 3)721-723(1976) 3.Owens, W.B.Blood pressure control in acute cerebrovascular diseaseJ. Clin. Hypertens. (Greenwich)13(3)205-211(2011) 4.Kernaghan, D., Duncan, A.C., and McKay, G.A.Hypertension in pregnancy: A review of therapeutic optionsObstet. Med.5(2)44-49(2012)
| Cas No. | 36894-69-6 | SDF | Download SDF |
| 别名 | 拉贝洛尔,AH5158; Sch-15719W free base | ||
| 分子式 | C19H24N2O3 | 分子量 | 328.41 |
| 溶解度 | DMSO : 125 mg/mL (380.62 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.045 mL | 15.2249 mL | 30.4497 mL |
| 5 mM | 0.609 mL | 3.045 mL | 6.0899 mL |
| 10 mM | 0.3045 mL | 1.5225 mL | 3.045 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Labetalol: a review of its pharmacology, pharmacokinetics, clinical uses and adverse effects
Pharmacotherapy 1983 Jul-Aug;3(4):193-219.PMID:6310529DOI:10.1002/j.1875-9114.1983.tb03252.x.
Labetalol is a combined alpha- and beta-adrenoceptor blocking agent for oral and intravenous use in the treatment of hypertension. It is a nonselective antagonist at beta-adrenoceptors and a competitive antagonist of postsynaptic alpha 1-adrenoceptors. Labetalol is more potent at beta that at alpha 1 adrenoceptors in man; the ratio of beta-alpha antagonism is 3:1 after oral and 6.9:1 after intravenous administration. Labetalol is readily absorbed in man after oral administration, but the drug, which is lipid soluble, undergoes considerable hepatic first-pass metabolism and has an absolute bioavailability of approximately 25%. There are no active metabolites, and the elimination half-life of the drug is approximately 6 hours. Unlike conventional beta-adrenoceptor blocking drugs without intrinsic sympathomimetic activity, Labetalol, when given acutely, produces a decrease in peripheral vascular resistance and blood pressure with little alteration in heart rate or cardiac output. However, like conventional beta-blockers, Labetalol may influence the renin-angiotensin-aldosterone system and respiratory function. Clinical studies have shown that the antihypertensive efficacy of Labetalol is superior to placebo and to diuretic therapy and is at least comparable to that of conventional beta-blockers, methyldopa, clonidine and various adrenergic neuronal blockers. Labetalol administered alone or with a diuretic is often effective when other antihypertensive regimens have failed. Studies have shown that Labetalol is effective in the treatment of essential hypertension, renal hypertension, pheochromocytoma, pregnancy hypertension and hypertensive emergencies. In addition, preliminary studies indicate that Labetalol may be of value in the management of ischemic heart disease. The most troublesome side effect of Labetalol therapy is posture-related dizziness. Other reported side effects of the drug include gastrointestinal disturbances, tiredness, headache, scalp tingling, skin rashes, urinary retention and impotence. Side effects related to the beta-adrenoceptor blocking effect of Labetalol, including asthma, heart failure and Raynaud's phenomenon, have been reported in rare instances.
Labetalol
Drug Intell Clin Pharm 1983 Oct;17(10):704-12.PMID:6354658doi
Labetalol is a competitive antagonist of alpha 1-, beta 1-, and beta 2-adrenergic receptors. The hemodynamic effects of the drug include reduced blood pressure, heart rate, and peripheral resistance, with little change in resting cardiac output or stroke volume. In open trials and controlled studies, Labetalol was an effective antihypertensive. Labetalol compared favorably with beta-blockers alone or in combination with vasodilators, for the treatment of hypertension. Reductions in heart rate are less pronounced with Labetalol as compared with propranolol. Labetalol produces rapid reductions in blood pressure when administered intravenously for severe hypertension. The most frequent adverse reactions to the drug include fatigue, postural symptoms, headache, and gastrointestinal complaints. Labetalol may prove advantageous when vasodilation in addition to beta-blockade is desired, or for selected patients experiencing adverse effects attributable to beta-blockade. Until the clinical profile of Labetalol is better defined, the use of the drug should be limited.
Methyldopa versus Labetalol or no medication for treatment of mild and moderate chronic hypertension during pregnancy: a randomized clinical trial
Hypertens Pregnancy 2020 Nov;39(4):393-398.PMID:32697618DOI:10.1080/10641955.2020.1791902.
Objective: to assess the maternal and fetal outcome in women with mild to moderate chronic hypertension on antihypertensive drug (methyldopa or Labetalol) therapy compared to no medication. Methods: This multicenter randomized clinical study was conducted at Menoufia University hospital, Shibin El-kom Teaching hospital at Menoufia governorate, Egypt.486 pregnant women with mild to moderate chronic hypertension were randomized into three groups; methyldopa group (n = 164), Labetalol group (n = 160), and control or no medication group (n = 162) who were followed from the beginning of pregnancy till the end of puerperium to record maternal and fetal outcome. Results: There was a highly significant difference between treatment groups (methyldopa and Labetalol) and control group regarding the development of maternal severe hypertension, development of preeclampsia, renal impairment, presence of ECG changes, placental abruption, and repeated admission to hospital for blood pressure control (p < 0.001) with higher occurrence in the control (no treatment) group. Neonates in the Labetalol group were more prone for the development of small for gestational age (SGA), neonatal hypotension, neonatal hyperbilirubinemia, and admission to NICU than their counterparts in the methyldopa and control groups (p < 0.001). The rate of prematurity was significantly higher in the control group than the treatment groups (p < 0.05). Conclusion: Treatment of mild to moderate chronic hypertension during pregnancy is beneficial in decreasing both maternal and fetal morbidity. The use of Labetalol was associated with higher rates of SGA, neonatal hypotension, and neonatal hyperbilirubinemia compared to methyldopa or no medication.
Distinct outcomes of Labetalol exposed infants: case reports and systematic review
J Matern Fetal Neonatal Med 2021 Jun;34(12):2012-2018.PMID:31510808DOI:10.1080/14767058.2019.1651270.
Background: The adverse effects of long-term maternal exposure of Labetalol on neonates have been recognized clinically. But there are few systematic studies on their clinical demonstrations and potential mechanisms. Methods: A death case of an infant with long-term maternal Labetalol exposure was reported and compared with two case reports from the literature. A systematic literature review was carried out followed by a retrospective analysis on neonatal Labetalol withdrawal effects. Results: It was discovered that Labetalol withdrawal effects initially cause various degrees of hypotension, hypoglycemia, and bradycardia among exposed neonates. Some life-threatening cases can also occur within 1 week after birth. Long-term maternal exposure of Labetalol, preterm infants with birth asphyxia, acidosis, hypoalbuminemia, and cardiac defects are their primary features. Possible mechanisms were concluded as labetalol-induced effects on the vascular and sympathetic nervous system as well as tissue oxygen extraction. Conclusions: Neonatal Labetalol withdrawal effects include early-onset and late-onset demonstrations, the latter can be life-threatening. A possible mechanism is multiple factors induced imbalance of sympathetic homeostasis increases neonatal vulnerability to common stresses. Long-term exposed preterm infants complicated with asphyxia, acidosis, hypoalbuminemia and cardiac defects, should be provided with intense care during the first week after birth. Further work is necessary to enrich this hypothesis.
Labetalol: a review of its pharmacology and therapeutic use in hypertension
Drugs 1978 Apr;15(4):251-70.PMID:25757DOI:10.2165/00003495-197815040-00002.
Labetalol is an orally active adrenoceptor blocking drug which is a competitive antagonist at both alpha- and beta-adrenoceptor sites. Its beta-blocking effects resemble those of propranolol, but its overall haemodynamic effects are akin to those of a comination of propranolol and an alpha-adrenoceptor blocking drugs such as phenoxybenzamine. Unlike with conventional beta-adrenoceptor blocking drugs, acute administration of Labetalol reduces peripheral vascular resistance and blood pressure and has little effect on cardiac output. Theoretically, Labetalol has advantages over beta-adrenoceptor blocking drugs alone in the treatment of hypertension, but any real advantage, particulary in mild or moderate hypertension, has yet to be conclusively demonstrated in therapeutic trials. Labetalol may be particularly useful in some patients whose blood pressure is not adequately controlled by beta-adrenoceptor blocking drugs alone or combined with a diuretic, but possibly at the expense of a postural hypotensive effect. Postural hypotension is the most troublesome side-effect, occasionally necessitating withdrawal of therapy, but severe side-effects such as are seen with effective antihypertensive dosages of phenoxybenzamine do not occur with Labetalol.