Levomepromazine
(Synonyms: 左美吗嗪,(±)-Methotrimeprazine; dl-Methotrimeprazine) 目录号 : GC36444
Methotrimeprazine (Levomepromazine) 是一种口服有效的抗精神病药物，通常用于在保守治疗中缓解恶心和呕吐。Methotrimeprazine (Levomepromazine) 对多种神经递质受体具有拮抗作用，包括多巴胺能、胆碱能、血清素和组胺受体。
Cas No.:60-99-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Methotrimeprazine (Levomepromazine) is an orally available neuroleptic agent, which is commonly used to relieve nausea and vomiting in palliative care settings. Levomepromazine has antagonist actions at multiple neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin and histamine receptors[1].
[1]. Cox L, et al. Levomepromazine for nausea and vomiting in palliative care. Cochrane Database Syst Rev. 2015 Nov 2;(11):CD009420. [2]. Sivaraman P, et al. Levomepromazine for schizophrenia. Cochrane Database Syst Rev. 2010 Oct 6;(10):CD007779.
| Cas No. | 60-99-1 | SDF | |
| 别名 | 左美吗嗪,(±)-Methotrimeprazine; dl-Methotrimeprazine | ||
| Canonical SMILES | COC1=CC=C2SC3=C(N(C2=C1)C[C@@H](CN(C)C)C)C=CC=C3 | ||
| 分子式 | C19H24N2OS | 分子量 | 328.47 |
| 溶解度 | DMSO: 14.29 mg/mL (43.50 mM) | 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 | 3.0444 mL | 15.2221 mL | 30.4442 mL |
| 5 mM | 0.6089 mL | 3.0444 mL | 6.0888 mL |
| 10 mM | 0.3044 mL | 1.5222 mL | 3.0444 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。
Levomepromazine for schizophrenia
Cochrane Database Syst Rev 2010 Oct 6;2010(10):CD007779.PMID:20927765DOI:10.1002/14651858.CD007779.pub2.
Background: Levomepromazine is an 'older' typical antipsychotic medication licensed for use in schizophrenia but sparingly prescribed in the United Kingdom. Objectives: To determine the clinical effects and safety of Levomepromazine compared with placebo or antipsychotic medications for schizophrenia and schizophreniform psychoses. Search strategy: We searched the Cochrane Schizophrenia Group's Register (December 2008) which is based on regular searches of, amongst others, BIOSIS, CENTRAL CINAHL, EMBASE, MEDLINE and PsycINFO. References of all identified studies were inspected for further trials. We also contacted relevant pharmaceutical companies for additional information. Selection criteria: All randomised trials comparing Levomepromazine with placebo or other antipsychotics for schizophrenia and schizophreniform psychoses were included. Data collection and analysis: Data were extracted independently. For dichotomous outcomes, we calculated relative risk (RR) (random-effects model), 95% confidence intervals (CI) and, where appropriate, number needed to treat (NNT) was calculated. We avoided the use of number needed to harm (NNH), as an alternative we used number needed to treat for an additional beneficial outcome (NNTB) and number needed to treat for an additional harmful outcome (NNTH) to indicate the direction of effect. For continuous outcomes, we calculated weighted mean differences (WMD). Main results: The review currently includes 4 RCTs with 192 participants. For our primary outcome of leaving the study early, Levomepromazine was not significantly different compared with other antipsychotics. The Levomepromazine arm was significantly better on CGI severity compared with chlorpromazine (n=38, 1 RCT, WMD -0.80 CI -1.51 to -0.09). Risperidone was better for CGI endpoint scores (n=42, 1 RCT, RR 2.33 CI 1.11 to 4.89, NNT 3 CI 2 to 10) compared with Levomepromazine. Recipients given Levomepromazine had a better BPRS endpoint score (n=38, 1 RCT, WMD -9.00, CI -17.46 to -0.54) and PANSS total score (n=38, 1 RCT, WMD -15.90, CI -30.30 to -1.50) than chlorpromazine. Risperidone recipients noticed a significant difference for the outcome 'at least 20% reduction' on BPRS endpoint score (n=42, 1 RCT, RR 3.33 CI 1.07 to 10.42, NNT 3 CI 2 to 14) compared with Levomepromazine. Levomepromazine caused less tremor (n=41, 1 RCT RR 0.12 CI 0.02 to 0.87 NNTB 3 CI 2 to 8), less antiparkinsonian medication administration (n=79, 2 RCTs, RR 0.39 CI 0.17 to 0.90, NNTB 5, CI 2 to 21) compared with haloperidol. Levomepromazine caused less akathisia compared with chlorpromazine, but more hypotension compared with risperidone (n=42, 1 RCT, RR 2.50 CI 1.21 to 5.18, NNTH 3, CI 2 to 7). Dizziness was common with Levomepromazine compared with other antipsychotic medications. Authors' conclusions: Available data does not enable us to confidently comment on the effectiveness of Levomepromazine for schizophrenia. Larger, more robust, studies comparing Levomepromazine with other antipsychotics including clozapine are much needed.
Levomepromazine for nausea and vomiting in palliative care
Cochrane Database Syst Rev 2015 Nov 2;2015(11):CD009420.PMID:26524693DOI:10.1002/14651858.CD009420.pub3.
Background: This is an updated version of the original Cochrane Review published in Issue 4, 2013, on Levomepromazine for nausea and vomiting in palliative care.Nausea and vomiting are common, distressing symptoms for patients receiving palliative care. There are several drugs which can be used to treat these symptoms, known as antiemetics. Levomepromazine is an antipsychotic drug is commonly used as an antiemetic to alleviate nausea and vomiting in palliative care settings. Objectives: To evaluate the efficacy of, and adverse events associated with, Levomepromazine for the treatment of nausea and vomiting in palliative care patients. Search methods: For this update we searched electronic databases, including those of Cochrane Central Register of Controlled Trials (CENTRAL), MEDLINE and EMBASE, up to February 2015. We searched clinical trial registers on 7 October 2015 for ongoing trials. Selection criteria: Randomised controlled trials of Levomepromazine for the treatment of nausea or vomiting, or both, in adults receiving palliative care. We excluded studies in which symptoms were thought to be due to pregnancy or surgery. Data collection and analysis: We assessed the potential relevance of studies based on titles and abstracts. We obtained copies of any study reports that appeared to meet the inclusion criteria for further assessment. At least two review authors read each paper to determine suitability for inclusion and discussed discrepancies in order to achieve a consensus. Main results: In the original review, we identified 421 abstracts using the search strategy. We considered eight studies for inclusion but ultimately excluded them all from the review. We updated the search in February 2015 and identified 35 abstracts, but again none met the inclusion criteria. We identified two trials from clinical trial registers, one of which is ongoing and one of which was closed due to poor recruitment. Authors' conclusions: As in the initial review, we identified no published randomised controlled trials examining the use of Levomepromazine for the management of nausea and vomiting in adults receiving palliative care, and our conclusion (that further studies of Levomepromazine and other antiemetic agents are needed to provide better evidence for their use in this setting) remains unchanged. We did, however, identify one ongoing study that we hope will contribute to the evidence base for this intervention in future updates of this review.
Focus on Levomepromazine
Curr Med Res Opin 2004 Dec;20(12):1877-81.PMID:15701205DOI:10.1185/030079904X12708.
This is a review of the uses of Levomepromazine in psychiatry, based upon MEDLINE, PSYCLIT and EMBASE literature searches. The main indications for this drug in psychiatry are schizophrenia and schizoaffective disorder. Levomepromazine's sedative properties particularly fit it to use in psychiatric intensive care. There is also some evidence to suggest it has efficacy in drug-resistant psychosis, although this property of the drug does require further research. In other areas of medicine Levomepromazine has been used in: alleviating bronchoconstriction; as a preoperative sedative; in terminal pain control and postoperative analgesia; and in the control of nausea. Some antimycobacterial properties have been recorded. The drug should not be prescribed to patients at high risk of accidental or suicidal overdose.
Levomepromazine for nausea and vomiting in palliative care
Cochrane Database Syst Rev 2013 Apr 30;(4):CD009420.PMID:23633372DOI:10.1002/14651858.CD009420.pub2.
Background: Nausea and vomiting are common, distressing symptoms for patients receiving palliative care. There are several agents which can be used to treat these symptoms. Levomepromazine is an antipsychotic drug which is commonly used to alleviate nausea and vomiting in palliative care settings. Objectives: To evaluate the efficacy of and adverse events (both minor and serious) associated with the use of Levomepromazine for the treatment of nausea and vomiting in palliative care patients. Search methods: We searched the electronic databases including CENTRAL, MEDLINE, and EMBASE using relevant search terms and synonyms in March 2013. Selection criteria: Randomised controlled trials of Levomepromazine for the treatment of nausea or vomiting, or both, for adults receiving palliative care. Studies where symptoms were thought to be due to pregnancy or surgery were excluded. Data collection and analysis: The potential relevance of studies was assessed based on titles and abstracts. Any study reports which appeared to meet the inclusion criteria were obtained for further assessment. All three authors read these papers to determine their suitability for inclusion and discussed discrepancies to achieve a consensus. Main results: The search strategy identified 421 abstracts from which eight studies were considered but all were excluded from the review. Authors' conclusions: No randomised controlled trials were identified examining the use of Levomepromazine for nausea and vomiting in palliative care. Further studies of Levomepromazine and other antiemetic agents are needed to provide better evidence for their use in this setting.
Levomepromazine (methotrimeprazine) and the last 48 hours
Hosp Med 1999 Aug;60(8):564-7.PMID:10621810DOI:10.12968/hosp.1999.60.8.1175.
Levomepromazine (previously known as methotrimeprazine) has a broad range of beneficial effects in the terminal phase of many illnesses, resulting from its combined antipsychotic, anxiolytic and sedative actions. Levomepromazine can safely be administered in a continuous subcutaneous infusion with most other commonly used drugs in palliative care.