Metoclopramide (hydrochloride)
(Synonyms: 盐酸甲氧氯普胺) 目录号 : GC44186
An orally bioavailable 5-HT3 and D2 receptor antagonist
Cas No.:7232-21-5
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Metoclopramide is an orally bioavailable serotonin (5-HT) receptor 5-HT3 antagonist with Ki and IC50 values of 995 and 308 nM, respectively, in rat cortical membranes. It is also a dopamine receptor 2 (D2) antagonist (IC50 = 483 nM in rat brain synaptic membranes). Oral administration of metoclopramide inhibits emesis induced by cisplatin and apomorphine in ferrets and dogs with ED50 values of 6.17 and 0.45 mg/kg, respectively. Metoclopramide reversibly inhibits human acetylcholinesterase (AChE) isolated from the caudate nucleus (Kis = 9.3 and 82 μM for competitive and non-competitive inhibition, respectively). Formulations containing metoclopramide have been used as anti-emetic and antipsychotic agents.
| Cas No. | 7232-21-5 | SDF | |
| 别名 | 盐酸甲氧氯普胺 | ||
| Canonical SMILES | ClC1=CC(C(NCCN(CC)CC)=O)=C(OC)C=C1N.Cl | ||
| 分子式 | C14H22ClN3O2•HCl | 分子量 | 336.3 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.9735 mL | 14.8677 mL | 29.7354 mL |
| 5 mM | 0.5947 mL | 2.9735 mL | 5.9471 mL |
| 10 mM | 0.2974 mL | 1.4868 mL | 2.9735 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。
Metoclopramide for the treatment of diabetic gastroparesis
Expert Rev Gastroenterol Hepatol 2019 Aug;13(8):711-721.PMID:31314613DOI:10.1080/17474124.2019.1645594.
Introduction: Gastroparesis is a chronic disorder of the stomach characterized by delayed gastric emptying without mechanical obstruction. Diabetes is the most commonly known cause of gastroparesis. Management of diabetic gastroparesis involves lifestyle modifications, glycemic control, pharmacological drugs, and for refractory cases surgical treatments. Metoclopramide remains the only drug approved by the Food and Drug Administration for diabetic gastroparesis. The aim of this article is to provide a concise review of the pharmacology, clinical efficacy and tolerability of Metoclopramide. Areas covered: We searched PubMed using the key words 'Metoclopramide', 'diabetic gastroparesis', and 'gastric emptying'. The relevant articles and their bibliography were reviewed. Metoclopramide acts on several different receptors; primarily as a dopamine receptor antagonist, both peripherally improving gastric emptying, and centrally resulting in an anti-emetic effect. Metoclopramide side effects, mostly related to its ability to cross the blood-brain barrier, include drowsiness, restlessness, hyperprolactinemia, and tardive dyskinesia (TD), a movement disorder that may be irreversible. Expert opinion: Metoclopramide carries a black box warning for use >12 weeks due to the risk of TD. However, gastroparesis patients experience chronic symptoms often requiring prolonged treatments. Physicians and patients look forward to FDA approval of new agents for gastroparesis with better efficacy and safety profile.
Gastroparesis, Metoclopramide, and tardive dyskinesia: Risk revisited
Neurogastroenterol Motil 2019 Nov;31(11):e13617.PMID:31050085DOI:10.1111/nmo.13617.
Background: Metoclopramide is primarily a dopamine receptor antagonist, with 5HT3 receptor antagonist and 5HT4 receptor agonist activity, and used as an antiemetic and gastroprokinetic since almost 50 years. Regulatory authorities issued restrictions and recommendations regarding long-term use of the drug at oral doses exceeding 10 mg 3-4 times daily because of the risk for development of tardive dyskinesia. The aim of our study was to review mechanism(s) of action and pharmacokinetic-pharmacodynamic properties of Metoclopramide, as well as the risk of metoclopramide-induced tardive dyskinesia, factors that may change drug exposure in humans, and to summarize the clinical context for appropriate use of the drug. Methods: A PubMed, Google Scholar, and Cross Reference search was done using the key words and combined searches: drug-drug interaction, gastroparesis, Metoclopramide, natural history, pharmacokinetics, pharmacodynamics, drug-drug interaction, outcome, risk factors, tardive dyskinesia. Key results: Data show that the risk of tardive dyskinesia from Metoclopramide is low, in the range of 0.1% per 1000 patient years. This is far below a previously estimated 1%-10% risk suggested in treatment guidelines by regulatory authorities. High-risk groups are elderly females, diabetics, patients with liver or kidney failure, and patients with concomitant antipsychotic drug therapy, which reduces the threshold for neurological complications. Conclusions & inferences: The risk of tardive dyskinesia due to Metoclopramide is far below approximated numbers in treatment guidelines. This risk and the influence of known risk factors should be considered when starting a course of Metoclopramide for treatment of gastroparesis.
Ondansetron and Metoclopramide as second-line antiemetics in women with nausea and vomiting in pregnancy: the EMPOWER pilot factorial RCT
Health Technol Assess 2021 Nov;25(63):1-116.PMID:34782054DOI:10.3310/hta25630.
Background: Around one-third of pregnant women suffer from moderate to severe nausea and vomiting, causing physical and emotional distress and reducing their quality of life. There is no cure for nausea and vomiting in pregnancy. Management focuses on relieving symptoms and preventing morbidity, and often requires antiemetic therapy. National guidelines make recommendations about first-, second- and third-line antiemetic therapies, although care varies in different hospitals and women report feeling unsupported, dissatisfied and depressed. Objectives: To determine whether or not, in addition to intravenous rehydration, ondansetron compared with no ondansetron and Metoclopramide compared with no Metoclopramide reduced the rate of treatment failure up to 10 days after drug initiation; improved symptom severity at 2, 5 and 10 days after drug initiation; improved quality of life at 10 days after drug initiation; and had an acceptable side effect and safety profile. To estimate the incremental cost per treatment failure avoided and the net monetary benefits from the perspectives of the NHS and women. Design: This was a multicentre, double-dummy, randomised, double-blinded, dummy-controlled 2 × 2 factorial trial (with an internal pilot phase), with qualitative and health economic evaluations. Participants: Thirty-three patients (who were < 17 weeks pregnant and who attended hospital with nausea and vomiting after little or no improvement with first-line antiemetic medication) who attended 12 secondary care NHS trusts in England, 22 health-care professionals and 21 women participated in the qualitative evaluation. Interventions: Participants were randomly allocated to one of four treatment groups (1 : 1 : 1: 1 ratio): (1) Metoclopramide and dummy ondansetron; (2) ondansetron and dummy Metoclopramide; (3) Metoclopramide and ondansetron; or (4) double dummy. Trial medication was initially given intravenously and then continued orally once women were able to tolerate oral fluids for a maximum of 10 days of treatment. Main outcome measures: The primary end point was the number of participants who experienced treatment failure, which was defined as the need for further treatment because symptoms had worsened between 12 hours and 10 days post treatment. The main economic outcomes were incremental cost per additional successful treatment and incremental net benefit. Results: Of the 592 patients screened, 122 were considered eligible and 33 were recruited into the internal pilot (Metoclopramide and dummy ondansetron, n = 8; ondansetron and dummy Metoclopramide, n = 8; Metoclopramide and ondansetron, n = 8; double dummy, n = 9). Owing to slow recruitment, the trial did not progress beyond the pilot. Fifteen out of 30 evaluable participants experienced treatment failure. No statistical analyses were performed. The main reason for ineligibility was prior treatment with trial drugs, reflecting an unpredicted change in prescribing practice at several points along the care pathway. The qualitative evaluation identified the requirements of the study protocol, in relation to guidelines on anti-sickness drugs, and the diversity of pathways to care as key hurdles to recruitment while the role of research staff was a key enabler. No important adverse events or side effects were reported. Limitations: The pilot trial failed to achieve the recruitment target owing to unforeseen changes in the provision of care. Conclusions: The trial was unable to provide evidence to support clinician decisions about the best choice of second-line antiemetic for nausea and vomiting in pregnancy. Trial registration: Current Controlled Trials ISRCTN16924692 and EudraCT 2017-001651-31. Funding: This project was funded by the National Institute for Health Research (NIHR) Health Technology Assessment programme and will be published in full in Health Technology Assessment; Vol. 25, No. 63. See the NIHR Journals Library website for further project information.
Intranasal Metoclopramide
Drugs 1999 Aug;58(2):315-22; discussion 323-4.PMID:10473023DOI:10.2165/00003495-199958020-00012.
Intranasal Metoclopramide is a new formulation of an established and effective antiemetic drug. Absorption after intranasal administration was lower than after oral or intravenous administration; otherwise the pharmacodynamic and pharmacokinetic profiles of the intranasal and parenteral formulations were similar. Intranasal and intramuscular Metoclopramide showed similar efficacy in the control of acute emesis induced by moderately emetogenic chemotherapy in 12 patients. Intranasal Metoclopramide 80mg significantly reduced the frequency of acute vomiting in 43 patients receiving highly emetogenic chemotherapy. A pilot study suggested that intranasal Metoclopramide, with or without dexamethasone, may reduce cisplatin-induced delayed emesis. In a randomised crossover trial in 40 patients, intranasal Metoclopramide or oral Metoclopramide, both with dexamethasone, were equally effective in the control of delayed emesis induced by moderately-emetogenic chemotherapy. One 30 patient study suggests that intranasal Metoclopramide has similar efficacy to oral Metoclopramide in the treatment of functional dyspepsia. A non-significant trend to reducing postoperative nausea and vomiting has been seen in two trials of intranasal Metoclopramide. Intranasal Metoclopramide caused minor irritation of the nasal membrane and unpleasant taste in some patients, but was otherwise well tolerated. None of the more serious extrapyramidal effects sometimes associated with Metoclopramide were reported.
Metoclopramide--a review
Med J Aust 1986 Mar 31;144(7):366-9.PMID:3515136DOI:10.5694/j.1326-5377.1986.tb115923.x.
Metoclopramide has wide applications in both clinical and experimental medicine. It is useful in the management of gastro-oesophageal reflux and gastric stasis. It is being used increasingly in the management of nausea and vomiting, and at high doses will significantly relieve the emesis that is induced by cytotoxic agents. Metoclopramide also has an important place in the investigation of the role of dopamine in physiological and pathological processes.