Metaraminol (tartrate)
(Synonyms: 重酒石酸间羟胺,Metaradrine tartrate) 目录号 : GC44170
A vasoconstrictor
Cas No.:33402-03-8
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
Metaraminol is a vasoconstrictor. In vivo, metaraminol (0.05 mg/kg) increases cardiac output, mean arterial pressure, and coronary blood flow and decreases pulse rate in a canine model of cardiogenic shock. It increases survival in a canine model of hemorrhagic hypotension. Metaraminol also reverses acetoxycycloheximide-induced transient amnesia in a shock avoidance test in rats.
| Cas No. | 33402-03-8 | SDF | |
| 别名 | 重酒石酸间羟胺,Metaradrine tartrate | ||
| Canonical SMILES | OC1=CC=CC([C@@H](O)[C@@H](N)C)=C1.OC([C@H](O)[C@@H](O)C(O)=O)=O | ||
| 分子式 | C9H13NO2•C4H6O6 | 分子量 | 317.3 |
| 溶解度 | DMF: 10 mg/ml,DMSO: 20 mg/ml,PBS (pH 7.2): 10 mg/ml | 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 | 3.1516 mL | 15.758 mL | 31.5159 mL |
| 5 mM | 0.6303 mL | 3.1516 mL | 6.3032 mL |
| 10 mM | 0.3152 mL | 1.5758 mL | 3.1516 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。
Dose equivalence between Metaraminol and norepinephrine in critical care
Br J Clin Pharmacol 2022 Jan;88(1):303-310.PMID:34197654DOI:10.1111/bcp.14969.
Aims: The aim of this study was to determine the conversion dose ratio between continuous infusion Metaraminol and norepinephrine in critically ill patients with shock. Methods: A retrospective cohort study was conducted in adult patients with shock admitted to an intensive care unit from 29 October 2018 to 30 October 2019 and who transitioned from Metaraminol monotherapy to norepinephrine monotherapy. Mean arterial pressure (MAP) and infusion doses for both drugs were collected at hourly intervals; 2 hours before to 5 hours after switching from Metaraminol monotherapy to norepinephrine monotherapy. The conversion dose ratio was defined as the ratio of Metaraminol (μg.kg-1 .min-1) : norepinephrine (μg.kg-1 .min-1 ) required to achieve a similar MAP. Results: A total of 43 out of 144 eligible patients were included. The median age was 68 years (IQR 56-76) and 22 (51%) were male. There was no significant difference between the baseline MAP during Metaraminol monotherapy (median 71 mm Hg, IQR 66-76) and the post-transition MAP during norepinephrine monotherapy (median 70 mm Hg, IQR 66-73) (P = .09). The median conversion dose ratio between Metaraminol and norepinephrine was 13 (IQR 7-24). In the sensitivity analyses, the median conversion dose ratio using the maximum and the mean norepinephrine infusion dose was 8 (IQR 5-16) and 12 (IQR 8-23), respectively. Conclusion: A conversion dose ratio of 10:1 (Metaraminol μg.kg-1 .min-1 :norepinephrine μg.kg-1 .min-1 ) may be used in critically ill patients with shock to account for ease of calculations and variability of the conversion ratio in the primary and sensitivity analyses.
Pharmacoepidemiology of Metaraminol in critically ill patients with shock in a tertiary care hospital
Aust Crit Care 2021 Nov;34(6):573-579.PMID:33663948DOI:10.1016/j.aucc.2021.01.002.
Background: Metaraminol is increasingly used as a vasopressor in critically ill patients. Nevertheless, there remains limited evidence to support its use in international guidelines for management of shock. Objectives: The aim of the study was to describe the pharmacoepidemiology of Metaraminol in critically ill patients with shock. Methods: A retrospective observational study was conducted in an intensive care unit (ICU) in Sydney, Australia. Patients admitted during a 1-year time frame who received Metaraminol intravenous infusions for management of shock were included. Results: A total of 152 patients were included. When Metaraminol was used, it was the most common first-line vasopressor started for management of shock (97%, n = 147) and was used as monotherapy in 53% (n = 81) of patients. The median duration of Metaraminol infusion in the ICU was 7 h (interquartile range [IQR] = 3 to 19), and the median maximum Metaraminol infusion rate in the ICU was 4.0 mg/h (IQR = 2.5 to 6.0). Peripheral vasopressor infusions were used in 96% (n = 146/152) of patients for a median duration of 7 h (IQR = 2 to 18). In all these cases, the peripheral vasopressor used was Metaraminol (100%, n = 146/146). Patients were commonly switched from Metaraminol to noradrenaline infusions after insertion of a central venous catheter (R2 = 0.89). Patients treated with Metaraminol monotherapy had a lower Acute Physiology and Chronic Health Evaluation III score (58 vs 68; median difference = -9, 95% confidence interval = -16 to -3; p < 0.01) and a shorter duration of overall vasopressor use in the ICU (12 vs 39 h, median difference = -24 h, 95% confidence interval = -31 to -18; p < 0.01) than those treated with combination vasopressors. No extravasation injury was reported in the study cohort. Conclusions: Metaraminol is often administered as a first-line peripheral vasopressor in the ICU and is used as a single agent in patients with lower severity of shock.
Development of analytical methods for the detection of Metaraminol in the horse
J Anal Toxicol 2000 May-Jun;24(4):281-8.PMID:10872576DOI:10.1093/jat/24.4.281.
Aramine (Metaraminol bitartrate) has been found in the possession of horse trainers and veterinarians who have been investigated for possible inappropriate drug administration to racing horses. Metaraminol (3-hydroxyphenylisopropanolamine) is a sympathomimetic amine that directly and indirectly affects adrenergic receptors, with alpha effects being predominant. Because it has the potential to affect the performance of a racing horse, its use is prohibited. In the present study, methods for the detection of Metaraminol were developed. Metaraminol was found to be extracted with poor recovery (< 50%) from aqueous solutions by routine basic extraction or cation exchange/reversed-phase solid-phase extraction techniques. However, an extractive acetylation method gave good (> 90%) recovery of Metaraminol from aqueous samples. Sequential urine samples collected from horses administered Metaraminol intramuscularly at 0.02, 0.10, and 0.23 mg/kg were extracted by the developed extractive acetylation procedure and analyzed by gas chromatography-mass spectrometry (GC-MS) in full-scan and selected ion monitoring modes. Norphenylephrine was used as an internal standard for quantitative analysis. The maximum concentration of Metaraminol occurred between 1 and 2 h postadministration. Metaraminol was detected in the 0.23 mg/kg administration urine for 24 h postadministration. Metaraminol was detected for the 0.10 and 0.02 mg/kg doses for approximately 8 h postadministration. No apparent biotransformation products were observed in a reaction mixture of Metaraminol and horse liver microsomal reaction mixture. Comparison of gas chromatograms of the extracts of the postadministration urine samples with those of the pre-administration samples failed to reveal any exogenous compound other than Metaraminol.
Comparison of Metaraminol, Phenylephrine, and Norepinephrine Infusion for Prevention of Hypotension During Combined Spinal-Epidural Anaesthesia for Elective Caesarean Section: A Three-Arm, Randomized, Double-Blind, Non-Inferiority Trial
Drug Des Devel Ther 2022 Jan 7;16:117-127.PMID:35027821DOI:10.2147/DDDT.S331177.
Background: A direct comparison of phenylephrine, Metaraminol, and norepinephrine in preventing hypotension during spinal anaesthesia for elective caesarean section has never been made. Patients and methods: Seventy-five parturients scheduled for elective caesarean section were randomly assigned into the three groups. After spinal anaesthesia induction, patients received a bonus dose of vasopressor (norepinephrine 4ug, phenylephrine 50ug, or Metaraminol 250ug) combined with continuous infusion (norepinephrine 8ug/mL, phenylephrine 100ug/mL, or Metaraminol 500ug/mL) at a rate of 30 mL/h to prevent hypotension. The primary outcome was umbilical arterial (UA) pH and other intraoperative data were also recorded. Results: The UA pH was 7.32±0.03 for Metaraminol, 7.31±0.03 for phenylephrine, and 7.31±0.03 for norepinephrine. The 95% CI of MD was -0.011 to 0.026 comparing Metaraminol with norepinephrine and 0.0181 to 0.0182 comparing phenylephrine with norepinephrine. Both lower bounds of the 95% CI of MD were above the predetermined lower boundary of clinical non-inferiority of -0.03, indicating both Metaraminol and phenylephrine were non-inferior to norepinephrine. Moreover, the incidence of hypotension was lower in Metaraminol compared with norepinephrine (P = 0.01). However, the incidence of hypertension was significantly lower in both phenylephrine and Metaraminol compared with norepinephrine. Conclusion: Both Metaraminol and phenylephrine were non-inferior to norepinephrine with respect to neonatal UA pH when used as a bolus and continuous infusion to prevent hypotension during combined spinal-epidural anaesthesia for elective caesarean section.
Metaraminol use during spinal anaesthesia for caesarean section: a meta-analysis of randomised controlled trials
Int J Obstet Anesth 2019 Aug;39:42-50.PMID:30772119DOI:10.1016/j.ijoa.2019.01.009.
Introduction: During caesarean section, the use of a vasopressor is often required to achieve haemodynamic stability of the parturient. Metaraminol is a vasopressor used in this context in some countries. However, the differences between Metaraminol and other vasopressors remain unclear. Methods: A search of the PubMed, Cochrane Library, and Embase databases was performed to identify randomised controlled trials comparing the use of Metaraminol with other vasopressors during spinal anaesthesia at caesarean section. The selected studies were subjected to meta-analysis and risk-of-bias assessment. Results: Four randomised, controlled trials met the selection criteria and 409 parturients who underwent an elective caesarean section were included in this meta-analysis. The quality of these trials was good. Metaraminol was associated with higher umbilical arterial pH (standardised mean difference [SMD] 0.82, 95% CI 0.01 to 1.62, P=0.05); a lower incidence of fetal acidosis (RR 0.08, 95% CI 0.01 to 0.63, P=0.02); and a lower incidence of nausea or vomiting (RR 0.16, 95% CI 0.04 to 0.57, P=0.0005) than was ephedrine. Metaraminol resulted in higher umbilical arterial pH (SMD 0.42, 95% CI 0.15 to 0.68, P=0.002) but a higher incidence of reactive hypertension (RR 1.80, 95% CI 1.32 to 2.46, P=0.0002) than did phenylephrine. Conclusion: The results of this study showed that for spinal anaesthesia at elective caesarean section, Metaraminol may be a more suitable vasopressor than ephedrine and its effects are at least not inferior to those of phenylephrine.