Metoprolol
(Synonyms: 美托洛尔) 目录号 : GC36603
Metoprolol is a cardioselective β1-adrenergic blocking agent with log Kd values of ?7.26±0.07, ?6.89±0.09, ?5.16±0.12 for β1, β2, and β3 adrenoceptors, respectively. It is used for acute myocardial infarction, heart failure, angina pectoris and mild to moderate hypertension.
Cas No.:51384-51-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Metoprolol is a cardioselective β1-adrenergic blocking agent with log Kd values of ?7.26±0.07, ?6.89±0.09, ?5.16±0.12 for β1, β2, and β3 adrenoceptors, respectively. It is used for acute myocardial infarction, heart failure, angina pectoris and mild to moderate hypertension.
[1] Jillian G Baker. Br J Pharmacol. 2005, 144(3): 317–322.
| Cas No. | 51384-51-1 | SDF | |
| 别名 | 美托洛尔 | ||
| Canonical SMILES | OC(CNC(C)C)COC1=CC=C(CCOC)C=C1 | ||
| 分子式 | C15H25NO3 | 分子量 | 267.36 |
| 溶解度 | DMSO : 53mg/mL | 储存条件 | Store at -20°C, protect from light |
| 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 | 3.7403 mL | 18.7014 mL | 37.4028 mL |
| 5 mM | 0.7481 mL | 3.7403 mL | 7.4806 mL |
| 10 mM | 0.374 mL | 1.8701 mL | 3.7403 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。
Metoprolol succinate combination in the treatment of hypertension
Angiology 2009 Oct-Nov;60(5):608-13.PMID:19033265DOI:10.1177/0003319708326450.
Metoprolol is a selective beta(1)-adrenergic antagonist extensively used since 1975. Metoprolol has proven its efficacy in reducing cardiovascular events and mortality in patients with hypertension and coronary heart disease. A recently developed controlled release/ extended-release formulation of Metoprolol succinate was designed to provide relatively constant Metoprolol plasma concentrations and beta(1)-blockade while retaining the convenience of once daily administration. A 100-mg Metoprolol controlled/extended-release tablet contains 95 mg of Metoprolol succinate and is considered to have equivalent activity of 100 mg Metoprolol tartrate. After ingestion, the tablet disintegrates into individual pellets and each pellet acts as a diffusion cell releasing the drug at a relatively constant rate over a period of approximately 20 hours. The aim of this review was to determine the pharmacokinetic and pharmacodynamic properties of Metoprolol succinate and to apply those properties in combination with other drugs mainly diuretics in the treatment of hypertension.
Effects of extended-release Metoprolol succinate in patients undergoing non-cardiac surgery (POISE trial): a randomised controlled trial
Lancet 2008 May 31;371(9627):1839-47.PMID:18479744DOI:10.1016/S0140-6736(08)60601-7.
Background: Trials of beta blockers in patients undergoing non-cardiac surgery have reported conflicting results. This randomised controlled trial, done in 190 hospitals in 23 countries, was designed to investigate the effects of perioperative beta blockers. Methods: We randomly assigned 8351 patients with, or at risk of, atherosclerotic disease who were undergoing non-cardiac surgery to receive extended-release Metoprolol succinate (n=4174) or placebo (n=4177), by a computerised randomisation phone service. Study treatment was started 2-4 h before surgery and continued for 30 days. Patients, health-care providers, data collectors, and outcome adjudicators were masked to treatment allocation. The primary endpoint was a composite of cardiovascular death, non-fatal myocardial infarction, and non-fatal cardiac arrest. Analyses were by intention to treat. This trial is registered with ClinicalTrials.gov, number NCT00182039. Findings: All 8351 patients were included in analyses; 8331 (99.8%) patients completed the 30-day follow-up. Fewer patients in the Metoprolol group than in the placebo group reached the primary endpoint (244 [5.8%] patients in the Metoprolol group vs 290 [6.9%] in the placebo group; hazard ratio 0.84, 95% CI 0.70-0.99; p=0.0399). Fewer patients in the Metoprolol group than in the placebo group had a myocardial infarction (176 [4.2%] vs 239 [5.7%] patients; 0.73, 0.60-0.89; p=0.0017). However, there were more deaths in the Metoprolol group than in the placebo group (129 [3.1%] vs 97 [2.3%] patients; 1.33, 1.03-1.74; p=0.0317). More patients in the Metoprolol group than in the placebo group had a stroke (41 [1.0%] vs 19 [0.5%] patients; 2.17, 1.26-3.74; p=0.0053). Interpretation: Our results highlight the risk in assuming a perioperative beta-blocker regimen has benefit without substantial harm, and the importance and need for large randomised trials in the perioperative setting. Patients are unlikely to accept the risks associated with perioperative extended-release Metoprolol.
Effects of Metoprolol on Exercise Hemodynamics in Patients With Obstructive Hypertrophic Cardiomyopathy
J Am Coll Cardiol 2022 Apr 26;79(16):1565-1575.PMID:35450573DOI:10.1016/j.jacc.2022.02.024.
Background: The relationship between exercise hemodynamics, loading conditions, and medical treatment in patients with obstructive hypertrophic cardiomyopathy (HCM) is incompletely understood. Objectives: This study aimed to investigate the effect of Metoprolol on invasive hemodynamic parameters at rest and during exercise in patients with obstructive HCM. Methods: This randomized, double-blind, placebo-controlled crossover trial enrolled 28 patients with obstructive HCM and New York Heart Association functional class ≥II. Patients were randomized to initiate either Metoprolol 150 mg or placebo for 2 consecutive 2-week periods. Right-heart catheterization and echocardiography were performed at rest and during exercise at the end of each treatment period. The primary outcome was the difference in pulmonary capillary wedge pressure (ΔPCWP) between peak exercise and rest. Results: No treatment effect on ΔPCWP was observed between Metoprolol and placebo treatment (21 ± 9 mm Hg vs 23 ± 9 mm Hg; P = 0.12). At rest, Metoprolol lowered heart rate (P < 0.0001), left ventricular outflow tract (LVOT) gradient (P = 0.01), and increased left ventricular end-diastolic volume (P = 0.02) and stroke volume (SV) (+6.4; 95% CI: 0.02-17.7; P = 0.049). During peak exercise, Metoprolol was associated with a lower heart rate (P < 0.0001), a lower LVOT gradient (P = 0.0005), lesser degree of mitral regurgitation (P = 0.004), and increased SV (+9 mL; 95% CI: 2-15 mL; P = 0.008). Conclusions: In patients with obstructive HCM, exercise was associated with an abnormal rise in PCWP, which was unaffected by Metoprolol. However, Metoprolol increased SV at rest and peak exercise following changes in end-diastolic volume, LVOT gradient, and degree of mitral regurgitation. (The Effect of Metoprolol in Patients With Hypertrophic Obstructive Cardiomyopathy [TEMPO]; NCT03532802).
Metoprolol: a review of its use in chronic heart failure
Drugs 2000 Sep;60(3):647-78.PMID:11030472DOI:10.2165/00003495-200060030-00011.
Metoprolol, a relatively selective beta1-blocker, is devoid of intrinsic sympathomimetic activity and possesses weak membrane stabilising activity. The drug has an established role in the management of essential hypertension and angina pectoris, and more recently, in patients with chronic heart failure. The effects of Metoprolol controlled-release/extended-release (CR/XL) in patients with stable, predominantly mild to moderate (NYHA functional class II to III) chronic heart failure have been evaluated in the large Metoprolol CR/XL Randomised Intervention Trial in Congestive Heart Failure (MERIT-HF) trial and the much smaller Randomized Evaluation of Strategies for Left Ventricular Dysfunction (RESOLVD) pilot study. Treatment with Metoprolol CR/XL was initiated at a low dosage of 12.5 to 25 mg once daily and gradually increased at 2-weekly intervals until the target dosage (200 mg once daily) or maximal tolerated dosage had been attained in patients receiving standard therapy for heart failure. At 12 months, Metoprolol CR/XL was associated with a 34% reduction in relative risk of all-cause mortality in patients with chronic heart failure due to ischaemic or dilated cardiomyopathy in the MERIT-HF trial. The incidence of sudden death and death due to progressive heart failure were both significantly decreased with Metoprolol CR/XL. Similarly, a trend towards decreased mortality in the Metoprolol CR/XL group compared with placebo was observed in the RESOLVD trial. Data from small numbers of patients with severe (NYHA functional class IV) heart failure indicate that Metoprolol CR/XL is effective in this subset of patients. However, no firm conclusions can yet be drawn. Improvement from baseline values in NYHA functional class, exercise capacity and some measures of quality of life with Metoprolol CR/XL or immediate-release Metoprolol were significantly greater than those with placebo. The drug is well tolerated when treatment is initiated in low dosages and gradually increased at intervals of 1 to 2 weeks. Conclusions: Metoprolol CR/XL effectively decreases mortality and improves clinical status in patients with stable mild to moderate (NYHA functional class II or III) chronic heart failure due to left ventricular systolic dysfunction, and the drug is effective in patients with ischaemic or dilated cardiomyopathy. Although limited data indicate that Metoprolol CR/XL is effective in patients with severe (NYHA functional class IV) chronic heart failure, more data are needed to confirm these findings. Treatment with Metoprolol CR/XL significantly reduced the incidence of sudden death and death due to progressive heart failure.
Felodipine/Metoprolol: a review of the fixed dose controlled release formulation in the management of essential hypertension
Drugs 2000 Jan;59(1):141-57.PMID:10718104DOI:10.2165/00003495-200059010-00011.
The main objective of fixed dose combination therapy for hypertension is to improve blood pressure (BP) control with lower, better tolerated dosages of 2 antihypertensives rather than higher dosages of a single agent. Felodipine and Metoprolol lower BP via different, but complementary, mechanisms and controlled release formulations of these 2 drugs are available as a fixed dose combination, felodipine/Metoprolol. In clinical trials in patients with hypertension, felodipine/Metoprolol was significantly more effective than placebo and the respective monotherapies administered at the same dosages. Mean BP was reduced to < 155/90 mm Hg in patients treated with combination therapy and controlled in approximately 70% of patients. In one study that titrated dosages to effect, fewer felodipine/Metoprolol than felodipine or Metoprolol monotherapy recipients required dosage increases to achieve BP control (45 vs 60 and 67%, respectively). Data from double blind comparative studies show that the antihypertensive efficacy of felodipine/Metoprolol 5 to 10/50 to 100 mg/day is significantly greater than that of enalapril monotherapy or captopril plus hydrochlorothiazide and equivalent to nifedipine/atenolol and amlodipine. In comparisons with enalapril, fewer felodipine/Metoprolol than enalapril recipients required dosage titration to achieve BP control. Compared with amlodipine, felodipine/Metoprolol significantly reduced mean 24-hour average BP (8.9/5.5 vs 14.4/9.5 mm Hg after 6 weeks; p < 0.001). Both treatments preserved diurnal rhythm. Long term follow-up studies show that the antihypertensive effect of felodipine/Metoprolol occurs mostly during the first month of treatment with small additional decreases in BP being observed in the second and third months, and a relatively constant effect thereafter. According to a validated questionnaire, quality of life was relatively similar during 12 weeks treatment with felodipine/Metoprolol, enalapril or placebo. In a retrospective pharmacoeconomic analysis conducted in Sweden, felodipine/Metoprolol was more cost effective than enalapril as initial treatment for hypertension. Peripheral oedema, headache and flushing were the most commonly reported adverse events with felodipine/Metoprolol and felodipine monotherapy, whereas dizziness, fatigue, headache and respiratory infection were more frequent with Metoprolol monotherapy. Dose-dependent adverse events such as oedema may occur less often in patients taking lower dosages in combination than in those taking higher dosages of felodipine monotherapy. Thus, patients with hypertension treated with felodipine/Metoprolol experience greater control of BP, with less need for dosage titration, than those treated with felodipine, Metoprolol or enalapril monotherapy. Importantly this greater efficacy does not appear to be associated with a higher incidence of adverse events relative to monotherapy. Additionally, in short term studies felodipine/Metoprolol had a similar (minimal) effect on QOL to enalapril monotherapy but was more cost effective.