Prochlorperazine (maleate)
(Synonyms: 丙氯拉嗪) 目录号 : GC44687
A dopamine D2 receptor antagonist
Cas No.:84-02-6
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
Prochlorperazine is a dopamine D2 receptor antagonist with Ki values of 4.7 and 2.9 nM for rat recombinant D2 receptors in CHO cells and rat striatal membranes, respectively. It also binds to rat recombinant D3 receptors expressed in CHO cells (Ki = 35 nM) and to the serotonin (5-HT) receptor subtype 5-HT3 in N1E-115 mouse neuroblastoma cell membranes (Ki = 1,200 nM). Prochlorperazine (2 mg/kg) increases the latency to paw licking in a hot plate test, indicating analgesia, an effect that is blocked by antisense oligonucleotides against the M1 muscarinic receptor. It also inhibits emesis induced by apomorphine in dogs (ED50 = 0.34 mg/kg). Formulations containing prochlorperazine have been used in the treatment of psychotic disorders and as antiemetics.
| Cas No. | 84-02-6 | SDF | |
| 别名 | 丙氯拉嗪 | ||
| Canonical SMILES | CN1CCN(CCCN2C(C=CC=C3)=C3SC4=C2C=C(Cl)C=C4)CC1.O=C(O)/C=C\C(O)=O.O=C(O)/C=C\C(O)=O | ||
| 分子式 | C20H24ClN3S•2C4H4O4 | 分子量 | 606.1 |
| 溶解度 | DMSO: 10 mg/ml,DMSO:PBS (pH 7.2)(1:5): 0.16 mg/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 | 1.6499 mL | 8.2495 mL | 16.4989 mL |
| 5 mM | 0.33 mL | 1.6499 mL | 3.2998 mL |
| 10 mM | 0.165 mL | 0.8249 mL | 1.6499 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。
The Safety of Prochlorperazine in Children: A Systematic Review and Meta-Analysis
Drug Saf 2016 Jun;39(6):509-16.PMID:26884326DOI:10.1007/s40264-016-0398-9.
Introduction: Prochlorperazine is recommended for adults with breakthrough or refractory chemotherapy-induced nausea and vomiting (CINV). The objective of this review was to describe its safety in children when given for any indication to help define its role for CINV control in children. Methods: Electronic searches of MEDLINE, EMBASE, PsycINFO, and the Cochrane Central Register of Controlled Trials were performed as of 9 March 2015. All studies in English reporting adverse effects (AEs) associated with Prochlorperazine in children (≤18 years) were included. AEs were synthesized for prospective studies. Results: Forty-nine (15 prospective) studies evaluating the use of Prochlorperazine in 758 children were included. The most commonly reported AEs in prospective studies of Prochlorperazine in children were sedation (multiple-dose studies: 10 %, 95 % CI 5-21) and extrapyramidal symptoms (EPS) (single-dose studies: 9 %, 95 % CI 3-29; multiple-dose studies: 4 %, 95 % CI 1-11). Serious AEs (seizure, neuroleptic malignant syndrome, autonomic collapse, tardive dyskinesia) were rarely associated with Prochlorperazine use in children. Five fatalities were reported in children receiving Prochlorperazine. Limitations: The limitations of this systematic review and meta-analysis were that the AEs reported in the included studies were heterogeneous, the prospective use of systematic clinical tools to identify AEs was rare, and the risk of bias in most prospective studies was moderate. Conclusions: The most common AEs reported with the pediatric use of Prochlorperazine are EPS and sedation. Fatalities, life-threatening, and persistent AEs have also been reported.
MAGraine: Magnesium compared to conventional therapy for treatment of migraines
Am J Emerg Med 2021 Jan;39:28-33.PMID:33041146DOI:10.1016/j.ajem.2020.09.033.
Due to the healthcare burden associated with migraines, prompt and effective treatment is vital to improve patient outcomes and ED workflow. This was a prospective, randomized, double-blind trial. Adults who presented to the ED with a diagnosis of migraine from August of 2019 to March of 2020 were included. Pregnant patients, or with renal impairment were excluded. Patients were randomized to receive intravenous magnesium, Prochlorperazine, or metoclopramide. The primary outcome was change in pain from baseline on a numeric rating scale (NRS) evaluated at 30 min after initiation of infusion of study drug. Secondary outcomes included NRS at 60 and 120 min, ED length of stay, necessity for rescue analgesia, and adverse effects. A total of 157 patients were analyzed in this study. Sixty-one patients received magnesium, 52 received Prochlorperazine, and 44 received metoclopramide. Most patients were white females, and the median age was 36 years. Hypertension and migraines were the most common comorbidities, with a third of the patients reporting an aura. There was a median decrease in NRS at 30 min of three points across all three treatment arms. The median decrease in NRS (IQR) at 60 min was -4 (2-6) in the magnesium group, -3 (2-5) in the metoclopramide group, and -4.5 (2-7) in the Prochlorperazine group (p = 0.27). There were no statistically significant differences in ED length of stay, rescue analgesia, or adverse effects. Reported adverse effects were dizziness, anxiety, and akathisia. No significant difference was observed in NRS at 30 min between magnesium, metoclopramide and Prochlorperazine.
Simultaneous quantification of sumatriptan succinate and Prochlorperazine maleate in orodispersible films using two validated UV-spectroscopic methods
Pak J Pharm Sci 2022 Jan;35(1(Supplementary)):183-194.PMID:35228176doi
The study aimed at simultaneous quantification of sumatriptan succinate (SUM) and Prochlorperazine maleate (PCP) in an orodispersible film using two validated spectroscopic methods viz. simultaneous equation (Method I) and the Q-absorption ratio (Method II). The Method I involved measurement of absorbances at λmax of both drugs while in Method II, absorbances were measured at isosbestic wavelength and λmax of one of the two components. Method validation were accomplished as per the ICH guidelines. A 1:1 mixture of the drugs and an orodispersible film (ODF) containing these drugs were assayed by both methods. The absorbance data of SUM and PCP in both methods were linear at respective wavelengths with correlation coefficient values >0.995. Both methods were precise as % RSD in repeatability, interday and intraday precision was less than 2. The estimation of SUM and PCP from the film dosage form by method I was104.74% and 98.34% and by method II was 103.45% and 98.85%, respectively, with a standard deviation <2. The study concluded that both the methods were simple, reliable and robust and can be applied successfully for the simultaneous quantification of SUM and PCP in mixture and orodispersible film dosage form.
Indomethacin/Prochlorperazine/caffeine: a review of its use in the acute treatment of migraine and in the treatment of episodic tension-type headache
CNS Drugs 2011 Apr;25(4):343-58.PMID:21425885DOI:10.2165/11206740-000000000-00000.
The indomethacin/Prochlorperazine/caffeine fixed combination (Difmetré®) combines the NSAID indomethacin with the phenothiazine antiemetic Prochlorperazine and caffeine. It is currently available as two oral (effervescent tablet and coated tablet) and two rectal (suppository and low-dose suppository) formulations. Oral and rectal formulations of indomethacin/Prochlorperazine/caffeine were effective and generally well tolerated in the treatment of migraine and episodic tension-type headache (TTH) in adult patients participating in randomized, multicentre, active-comparator controlled studies. For the most part, the efficacy of oral indomethacin/Prochlorperazine/caffeine did not significantly differ from that of oral sumatriptan in patients with migraine and oral nimesulide in patients with episodic TTH. With rectal administration, indomethacin/Prochlorperazine/caffeine was, in general, significantly more effective than sumatriptan in patients with migraine. Thus, oral and rectal formulations of indomethacin/Prochlorperazine/caffeine provide a further option in the acute treatment of migraine and in the treatment of episodic TTH in adult patients.
Quantification of Prochlorperazine maleate in human plasma by liquid chromatography-mass spectrometry: Application to a bioequivalence study
J Chromatogr B Analyt Technol Biomed Life Sci 2009 Oct 1;877(27):3243-7.PMID:19682959DOI:10.1016/j.jchromb.2009.07.038.
A sensitive and specific method using a one-step liquid-liquid extraction with dichloromethane followed by liquid chromatographic-electrospray ionization-mass spectrometric was developed and validated to determine Prochlorperazine maleate in human plasma using amitriptyline hydrochloride as an internal standard. The samples were separated using a Thermo Hypersil-Hypurity C18 reversed-phase column (150mmx2.1mm i.d., 5mum). A mobile phase containing 10mM ammonium acetate (pH 3.6)-methanol-acetonitrile (27:68:5, v/v/v) was used isocratically eluting at a flow rate of 0.22ml/min. The average extraction recovery of Prochlorperazine and internal standard were 81.8+/-2.2% and 79.5+/-3.7%, respectively. Prochlorperazine maleate and internal standard were measured by electrospray ion source in positive selective ion monitoring mode. The method demonstrated that good linearity ranged from 0.20 to 6.40ng/ml with r(2)=0.9989. The limit of quantification for Prochlorperazine maleate in the plasma was 0.20ng/ml. The established method has been successfully applied to a bioequivalence study of two Prochlorperazine maleate formulations in 18 healthy male Chinese volunteers.