Cyclizine (hydrochloride)
(Synonyms: 盐酸苯甲嗪) 目录号 : GC47138
A histamine H1 receptor antagonist
Cas No.:303-25-3
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
Cyclizine is a histamine H1 receptor antagonist.1,2,3 It binds selectively to histamine H1 receptors (Kd = 5 nM) over H2 and H3 receptors (Kds = 1,600 and >580 nM, respectively).3 Cyclizine inhibits anti-IgE-induced histamine release from isolated human lung fragments with an IC50 value of 5.42 µM but induces histamine release with a 50% release concentration (RC50) of 10.81 µM.4 It reduces LPS-induced nitrite accumulation and protein levels of induced nitric oxide synthase (iNOS) in RAW 264.7 cells when used at a concentration of 100 nM.2 Cyclizine (10 and 20 mg/kg) reduces immobility in the forced swim test in rats.5
1.Hamlin, K.E., Weston, A.W., Fischer, F.E., et al.Histamine antagonists. II.1 Unsymmetrical 1,4-disubstituted piperazinesJ. Am. Chem. Soc.71(8)2731-2734(2019) 2.KrÁlovÁ, J., Ra?kovÁ, L., PekarovÁ, M., et al.The effects of H1-antihistamines on the nitric oxide production by RAW 264.7 cells with respect to their lipophilicityInt. Immunopharmacol.9(7-8)990-995(2009) 3.Hill, S.J.Distribution, properties, and functional characteristics of three classes of histamine receptorPharmacol. Rev.42(1)45-83(1990) 4.Church, M.K., and Gradidge, C.F.Inhibition of histamine release from human lung in vitro by antihistamines and related drugsBr. J. Pharmacol.69(4)663-667(2019) 5.Khanwelkar, C.C., Gokhale, D.V., Santakke, A.V., et al.Effects of H1-receptor antagonists in antidepressant tests in ratsAl Ameen J. Med. Sci.1(2)84-92(2008)
| Cas No. | 303-25-3 | SDF | |
| 别名 | 盐酸苯甲嗪 | ||
| Canonical SMILES | CN1CCN(C(C2=CC=CC=C2)C3=CC=CC=C3)CC1.Cl | ||
| 分子式 | C18H22N2.HCl | 分子量 | 302.8 |
| 溶解度 | Methanol: 1 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 | 3.3025 mL | 16.5125 mL | 33.0251 mL |
| 5 mM | 0.6605 mL | 3.3025 mL | 6.605 mL |
| 10 mM | 0.3303 mL | 1.6513 mL | 3.3025 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。
[Cyclizine is sold in Denmark as an over-the-counter drug and has serious side effects when overdosed]
Ugeskr Laeger 2018 Jan 15;180(3):V07170519.PMID:29336302doi
Cyclizine is sold in Denmark as an over-the-counter drug and affects not only histaminergic but also muscarinergic, serotonergic and α-adrenergic receptors, with side effects such as respiratory depression and cardiac arrhythmias, leading to fatalities. Due to the numerous side effects, it raises questions concerning the status of Cyclizine as an over-the-counter drug. Data of healthcare contacts because of Cyclizine intoxication in the 2014-2016 period should be analyzed to further illuminate the health risk of Cyclizine poisoning.
Cyclizine pharmacovigilance in hospice/palliative care: net effects for nausea or vomiting
BMJ Support Palliat Care 2022 Nov 10;bmjspcare-2022-003795.PMID:36357164DOI:10.1136/spcare-2022-003795.
Objectives: To describe the contemporary real-world use of Cyclizine for nausea or vomiting, and the associated benefits and harms. Methods: This was a prospective, consecutive case series of routine clinical use of Cyclizine for nausea or vomiting in palliative care conducted across 19 sites in Australia, Aotearoa/New Zealand and the UK. Clinical outcomes were graded using the National Cancer Institute Common Terminology Criteria for Adverse Events at baseline and 72 hours after initiation of Cyclizine. Ad hoc safety reporting continued for 2 weeks. Results: Data were collected from 101 patients between May 2018 and December 2020. Cyclizine was mostly used in combination with another antiemetic. Overall, 79 patients benefited and 32 experienced harm (56 had benefit without harm; 9 had harm without benefit). The most common harms were constipation (13%), somnolence (9%) and confusion (7%), adding to the already high rates of these symptoms at baseline. For the four patients with serious harms (grade ≥3), these were exacerbations of existing symptoms. Nine patients stopped Cyclizine at 72 hours and a further 20 patients within 2 weeks. The most common reasons for stopping were lack of benefit and symptom resolution; none stopped because of harms. Conclusions: When used as described in a palliative care setting, Cyclizine benefits about three-quarters of patients, with about one-third experiencing tolerable harms.
Bioequivalence study of Cyclizine hydrochloride 50 mg tablets in healthy volunteers: a randomized, open-label, single-dose study
Ther Deliv 2016 Aug;7(8):545-51.PMID:27444494DOI:10.4155/tde-2016-0023.
Background: Cyclizine is used in the treatment and prevention of nausea and vomiting. We aimed to demonstrate bioequivalence between two formulations of Cyclizine 50 mg tablets. Methods/results: This single-dose, two-treatment, two-period, two-sequence, open-label, randomized crossover study was conducted on 32 healthy male volunteers. The average values for Cmax, Tmax, AUC0-t and AUC0-inf were 21.50 ng/ml, 3.85 h, 423.71 ng.h/ml and 489.26 ng.h/ml, for Cyclizine 50 mg (test) versus 20.39 ng/ml, 4.34 h, 410.56 ng.h/ml and 473.86 ng.h/ml for Valoid 50 mg (reference). The 90% CI of the mean ratios of Cmax (geometric mean ratio: 101.81 ng/ml), and AUC0-t (101.81 ng.h/ml) were within the bioequivalence range of 80 to 125%. Both drugs were well tolerated. Conclusion: Cyclizine 50 mg is bioequivalent to the reference.
Stimulation of the wrist acupuncture point PC6 for preventing postoperative nausea and vomiting
Cochrane Database Syst Rev 2015 Nov 2;2015(11):CD003281.PMID:26522652DOI:10.1002/14651858.CD003281.pub4.
Background: Postoperative nausea and vomiting (PONV) are common complications following surgery and anaesthesia. Antiemetic drugs are only partially effective in preventing PONV. An alternative approach is to stimulate the PC6 acupoint on the wrist. This is an update of a Cochrane review first published in 2004, updated in 2009 and now in 2015. Objectives: To determine the effectiveness and safety of PC6 acupoint stimulation with or without antiemetic drug versus sham or antiemetic drug for the prevention of PONV in people undergoing surgery. Search methods: We searched the Cochrane Central Register of Controlled Trials (CENTRAL) (Cochrane Library, Issue 12, 2014), MEDLINE (January 2008 to December 2014), EMBASE (January 2008 to December 2014), ISI Web of Science (January 2008 to December 2014), World Health Organization Clinical Trials Registry, ClinicalTrials.gov, and reference lists of articles to identify additional studies. We applied no language restrictions. Selection criteria: All randomized trials of techniques that stimulated the PC6 acupoint compared with sham treatment or drug therapy, or combined PC6 acupoint and drug therapy compared to drug therapy, for the prevention of PONV. Interventions used in these trials included acupuncture, electro-acupuncture, transcutaneous electrical acupoint stimulation, transcutaneous nerve stimulation, laser stimulation, capsicum plaster, acu-stimulation device, and acupressure in people undergoing surgery. Primary outcomes were the incidences of nausea and vomiting after surgery. Secondary outcomes were the need for rescue antiemetic therapy and adverse effects. Data collection and analysis: Two review authors independently extracted the data and assessed the risk of bias domains for each trial. We used a random-effects model and reported risk ratio (RR) with associated 95% confidence interval (95% CI). We used trial sequential analyses to help provide information on when we had reached firm evidence in cumulative meta-analyses of the primary outcomes, based on a 30% risk ratio reduction in PONV. Main results: We included 59 trials involving 7667 participants. We rated two trials at low risk of bias in all domains (selection, attrition, reporting, blinding and other). We rated 25 trials at high risk in one or more risk-of-bias domains. Compared with sham treatment, PC6 acupoint stimulation significantly reduced the incidence of nausea (RR 0.68, 95% CI 0.60 to 0.77; 40 trials, 4742 participants), vomiting (RR 0.60, 95% CI 0.51 to 0.71; 45 trials, 5147 participants) and the need for rescue antiemetics (RR 0.64, 95% CI 0.55 to 0.73; 39 trials, 4622 participants). As heterogeneity among trials was substantial and there were study limitations, we rated the quality of evidence as low. Using trial sequential analysis, the required information size and boundary for benefit were reached for both primary outcomes.PC6 acupoint stimulation was compared with six different types of antiemetic drugs (metoclopramide, Cyclizine, prochlorperazine, droperidol. ondansetron and dexamethasone). There was no difference between PC6 acupoint stimulation and antiemetic drugs in the incidence of nausea (RR 0.91, 95% CI 0.75 to 1.10; 14 trials, 1332 participants), vomiting (RR 0.93, 95% CI 0.74 to 1.17; 19 trials, 1708 participants), or the need for rescue antiemetics (RR 0.87, 95% CI 0.65 to 1.16; 9 trials, 895 participants). We rated the quality of evidence as moderate, due to the study limitations. Using trial sequential analyses, the futility boundary was crossed before the required information size was surpassed for both primary outcomes.Compared to antiemetic drugs, the combination of PC6 acupoint stimulation and antiemetic therapy reduced the incidence of vomiting (RR 0.56, 95% CI 0.35 to 0.91; 9 trials, 687 participants) but not nausea (RR 0.79, 95% CI 0.55 to 1.13; 8 trials, 642 participants). We rated the quality of evidence as very low, due to substantial heterogeneity among trials, study limitations and imprecision. Using trial sequential analysis, none of the boundaries for benefit, harm or futility were crossed for PONV. The need for rescue antiemetic was lower in the combination PC6 acupoint stimulation and antiemetic group than the antiemetic group (RR 0.61, 95% CI 0.44 to 0.86; 5 trials, 419 participants).The side effects associated with PC6 acupoint stimulation were minor, transient and self-limiting (e.g. skin irritation, blistering, redness and pain) in 14 trials. Publication bias was not apparent in the contour-enhanced funnel plots. Authors' conclusions: There is low-quality evidence supporting the use of PC6 acupoint stimulation over sham. Compared to the last update in 2009, no further sham comparison trials are needed. We found that there is moderate-quality evidence showing no difference between PC6 acupoint stimulation and antiemetic drugs to prevent PONV. Further PC6 acupoint stimulation versus antiemetic trials are futile in showing a significant difference, which is a new finding in this update. There is inconclusive evidence supporting the use of a combined strategy of PC6 acupoint stimulation and antiemetic drug over drug prophylaxis, and further high-quality trials are needed.
Post-operative Cyclizine misuse
Scott Med J 2013 Nov;58(4):e1-2.PMID:24215049DOI:10.1177/0036933013508039.
Cyclizine is commonly prescribed as an anti-emetic post-operatively. We report a case of a 51-year-old woman who developed addiction to intravenous Cyclizine following regular administration at recommended doses. This is the first report of Cyclizine misuse post-operatively. We compare this case to Cyclizine abuse reported amongst other populations. Prescribers should be aware of the potential of Cyclizine as a drug of abuse.