Fluphenazine decanoate
(Synonyms: 癸氟奋乃静) 目录号 : GC39192
Fluphenazine decanoate 是一种长效的吩噻嗪抗精神病药，用于治疗精神分裂症。Fluphenazine decanoate 也是一种高度且连续的多巴胺 D2 受体阻滞剂。
Cas No.:5002-47-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Fluphenazine decanoate is a long-acting phenothiazine neuroleptic that used to treat schizophrenia. Fluphenazine decanoate is also a high and continuous dopamine D2 receptor blocker[1][2][3].
[1]. Wagman JD, et al. The effect of fluphenazine decanoate on glucocorticoid production, reproductive cyclicity, and the behavioral stress response in the Persian onager (Equus hemionus onager). Zoo Biol. 2015 Nov;34(6):525-34. [2]. Uchida H, et al. Dose and dosing frequency of long-acting injectable antipsychotics: a systematic review of PET and SPECT data and clinical implications. J Clin Psychopharmacol. 2014 Dec;34(6):728-35. [3]. Weiss RB, et al. Long-acting neuroleptic use for reproductive management of non-domestic ungulates using the domestic goat (Capra hircus) as a model. Zoo Biol. 2014 May-Jun;33(3):204-11.
| Cas No. | 5002-47-1 | SDF | |
| 别名 | 癸氟奋乃静 | ||
| Canonical SMILES | CCCCCCCCCC(OCCN1CCN(CCCN2C3=C(C=CC=C3)SC4=CC=C(C(F)(F)F)C=C24)CC1)=O | ||
| 分子式 | C32H44F3N3O2S | 分子量 | 591.77 |
| 溶解度 | DMSO: 125 mg/mL (211.23 mM); Ethanol: 50 mg/mL (84.49 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 | 1.6898 mL | 8.4492 mL | 16.8985 mL |
| 5 mM | 0.338 mL | 1.6898 mL | 3.3797 mL |
| 10 mM | 0.169 mL | 0.8449 mL | 1.6898 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。
Fluphenazine decanoate-induced bradycardia: A case report
Neuropsychopharmacol Rep 2022 Sep;42(3):368-373.PMID:35373519DOI:10.1002/npr2.12251.
Sinus tachycardia and orthostatic hypotension have been so far reported among the negative cardiovascular complications of antipsychotic agents. This study aimed to report a case with bradycardia induced by Fluphenazine decanoate administration. The patient was a 29-year-old man, admitted to the general teaching hospital in Sari, Iran, with a complaint of abdominal and gastric pain as well as weight loss following 7 months of fasting based on religious delusions. The patient developed bradycardia, 36 hours after Fluphenazine decanoate administration. His pulse rate was also 46 beats per min (bpm). The antipsychotic medication was thus held and the patient did not take any drugs. On the 21st day after discontinuing this agent, the pulse rate reached 70 bpm. This case report notifies that much more attention should be paid to all patients before starting Fluphenazine decanoate administration, and close cardiac monitoring must be done.
Fluphenazine decanoate (depot) and enanthate for schizophrenia
Cochrane Database Syst Rev 2015 Feb 5;(2):CD000307.PMID:25654768DOI:10.1002/14651858.CD000307.pub2.
Background: Intramuscular injections (depot preparations) offer an advantage over oral medication for treating schizophrenia by reducing poor compliance. The benefits gained by long-acting preparations, however, may be offset by a higher incidence of adverse effects. Objectives: To assess the effects of Fluphenazine decanoate and enanthate versus oral anti-psychotics and other depot neuroleptic preparations for individuals with schizophrenia in terms of clinical, social and economic outcomes. Search methods: We searched the Cochrane Schizophrenia Group's Trials Register (February 2011 and October 16, 2013), which is based on regular searches of CINAHL, BIOSIS, AMED, EMBASE, PubMed, MEDLINE, PsycINFO, and registries of clinical trials. Selection criteria: We considered all relevant randomised controlled trials (RCTs) focusing on people with schizophrenia comparing Fluphenazine decanoate or enanthate with placebo or oral anti-psychotics or other depot preparations. Data collection and analysis: We reliably selected, assessed the quality, and extracted data of the included studies. For dichotomous data, we estimated risk ratio (RR) with 95% confidence intervals (CI). Analysis was by intention-to-treat. We used the mean difference (MD) for normal continuous data. We excluded continuous data if loss to follow-up was greater than 50%. Tests of heterogeneity and for publication bias were undertaken. We used a fixed-effect model for all analyses unless there was high heterogeneity. For this update. we assessed risk of bias of included studies and used the GRADE (Grading of Recommendations Assessment, Development and Evaluation) approach to create a 'Summary of findings' table. Main results: This review now includes 73 randomised studies, with 4870 participants. Overall, the quality of the evidence is low to very low.Compared with placebo, use of Fluphenazine decanoate does not result in any significant differences in death, nor does it reduce relapse over six months to one year, but one longer-term study found that relapse was significantly reduced in the fluphenazine arm (n = 54, 1 RCT, RR 0.35, CI 0.19 to 0.64, very low quality evidence). A very similar number of people left the medium-term studies (six months to one year) early in the Fluphenazine decanoate (24%) and placebo (19%) groups, however, a two-year study significantly favoured Fluphenazine decanoate (n = 54, 1 RCT, RR 0.47, CI 0.23 to 0.96, very low quality evidence). No significant differences were found in mental state measured on the Brief Psychiatric Rating Scale (BPRS) or in extrapyramidal adverse effects, although these outcomes were only reported in one small study each. No study comparing Fluphenazine decanoate with placebo reported clinically significant changes in global state or hospital admissions.Fluphenazine decanoate does not reduce relapse more than oral neuroleptics in the medium term (n = 419, 6 RCTs, RR 1.46 CI 0.75 to 2.83, very low quality evidence). A small study found no difference in clinically significant changes in global state. No difference in the number of participants leaving the study early was found between Fluphenazine decanoate (17%) and oral neuroleptics (18%), and no significant differences were found in mental state measured on the BPRS. Extrapyramidal adverse effects were significantly less for people receiving Fluphenazine decanoate compared with oral neuroleptics (n = 259, 3 RCTs, RR 0.47 CI 0.24 to 0.91, very low quality evidence). No study comparing Fluphenazine decanoate with oral neuroleptics reported death or hospital admissions.No significant difference in relapse rates in the medium term between Fluphenazine decanoate and fluphenazine enanthate was found (n = 49, 1 RCT, RR 2.43, CI 0.71 to 8.32, very low quality evidence), immediate- and short-term studies were also equivocal. One small study reported the number of participants leaving the study early (29% versus 12%) and mental state measured on the BPRS and found no significant difference for either outcome. No significant difference was found in extrapyramidal adverse effects between Fluphenazine decanoate and fluphenazine enanthate. No study comparing Fluphenazine decanoate with fluphenazine enanthate reported death, clinically significant changes in global state or hospital admissions. Authors' conclusions: There are more data for Fluphenazine decanoate than for the enanthate ester. Both are effective antipsychotic preparations. Fluphenazine decanoate produced fewer movement disorder effects than other oral antipsychotics but data were of low quality, and overall, adverse effect data were equivocal. In the context of trials, there is little advantage of these depots over oral medications in terms of compliance but this is unlikely to be applicable to everyday clinical practice.
Depot Fluphenazine decanoate and enanthate for schizophrenia
Cochrane Database Syst Rev 2005 Jan 25;(1):CD000307.PMID:15674872DOI:10.1002/14651858.CD000307.
Background: Intramuscular injections (depot preparations) offer an advantage over oral medication for treating schizophrenia by reducing poor compliance. The benefits gained by long acting preparations, however, may be offset by a higher incidence of adverse effects. Objectives: To investigate the clinical effects of Fluphenazine decanoate and enanthate. Search strategy: For this update we searched the Cochrane Schizophrenia Group's Register (May 2002). Selection criteria: We considered all relevant randomised clinical controlled trials focusing on people with schizophrenia comparing Fluphenazine decanoate or enanthate with placebo or oral anti-psychotics or other depot preparations. Data collection and analysis: We reliably selected, quality rated and data extracted studies. For dichotomous data we estimated relative risk (RR) with 95% confidence intervals (CI), and, where possible, the number needed to treat/harm (NNT/H). Analysis was by intention-to-treat. We used the weighted mean difference (WMD) for normal continuous data. Tests of heterogeneity and for publication bias were undertaken. Main results: This review now includes 70 randomised studies. Compared with placebo, Fluphenazine decanoate did not reduce relapse over 6 months to 1 year, but one longer term study found that relapse was significantly reduced in the fluphenazine arm (n=54, RR 0.35, CI 0.2 to 0.6, NNT 2 CI 2 to 4). Fluphenazine decanoate does not reduce relapse more than oral neuroleptics (n=419, 6 RCTs, RR relapse 26-52 weeks 1.46 CI 0.8 to 2.8) or other depot antipsychotics (n=581, 11 RCTs, RR relapse 26-52 weeks 0.82 CI 0.6 to 1.2). Relapse rates over 6 months to 1 year were not significantly different between standard dosage of Fluphenazine decanoate over a low dose group (n=523, 4 RCTs, RR 2.09 CI 0.6 to 7.1). Movement disorders were significantly less for people receiving Fluphenazine decanoate compared with oral neuroleptics (n=259, 3 RCTs, RR 0.47 CI 0.2 to 0.9, NNT 14 CI 10 to 82). For fluphenazine enanthate there were limited data but no clear difference in global change (0 to 5 weeks) when compared with oral neuroleptics (n=31, 1 RCTs, RR 0.67 CI 0.3 to 1.7), and in relapse rates over 6-26 weeks between fluphenazine enanthate and other depots. Compared with placebo, giving the enanthate caused no more people to need need anticholinergic drugs (n=25, 1 RCT, RR 9.69 CI 0.6 to 163.0) and movement disorders, tardive dyskinesia, tremor, blurred vision and dry mouth were equally prevalent when enanthate was compared with other depot neuroleptics. Authors' conclusions: There are more data for Fluphenazine decanoate than for the enanthate ester. Both are effective antipsychotic preparations. In the context of trials, there is little advantage of these depots over oral medications in terms of compliance but this is unlikely to be applicable to everyday clinical practice.
Depot fluphenazine for schizophrenia
Cochrane Database Syst Rev 2000;(2):CD000307.PMID:10796340DOI:10.1002/14651858.CD000307.
Background: In the years after the discovery of oral antipsychotic medications, it became clear that there was a link between stopping medication and relapse of psychotic symptoms. A series of long-acting preparations was developed. These depot preparations, are frequently used for those who find taking oral medication on a regular basis difficult or unacceptable. However, it has been a consistent concern that any reduction in relapse rate afforded by the depot preparations may be offset by an increase in undesirable side effects. There is one oral preparation and two depot forms (enanthate (Moditen) and decanoate (Modecate)). The decanoate form is more frequently used but both versions were reviewed in this work. Objectives: To compare depot fluphenazine medication to oral fluphenazine for treatment of schizophrenia. Search strategy: Electronic searches of Biological Abstracts, CSG's Register, EMBASE, LILACS, MEDLINE, PsycLIT, SCISEARCH, hand searching the references of all identified studies and contacting the manufacturers of the compounds. Selection criteria: All randomised clinical trials that compared fluphenazine enanthate or Fluphenazine decanoate to oral fluphenazine for people with schizophrenia or other psychoses were included. Data collection and analysis: One reviewer (CEA) inspected study citations and then the second reviewer (ME) independently inspected 20% of citations to ensure reliability. Full reports of the studies of agreed relevance were obtained and data extracted in the same manner by the authors. Trials were allocated to three quality categories, as described in the Cochrane Collaboration Handbook. Data were analysed on an intention-to-treat basis, and, where possible, parametric continuous data were presented. Tests for heterogeneity were undertaken. Main results: Data were very limited. There was no difference between fluphenazine hydrochloride and its depot form for outcomes such as global impression of functioning, relapse/re-hospitalisation, poor initial response to treatment, leaving the study early, depressed mood / suicide and side effects such as movement disorders, uncomfortable dry mouth, sleep problems and weight gain were equally common in both groups. Direct measures of mental state, social functioning and satisfaction with care were either not measured or presented in such as way as to make any analysis impossible. Reviewer's conclusions: All six included studies relate to people with schizophrenia who are already stable on oral fluphenazine or seem contented to stay in the studies. How the data from this review relate to everyday psychiatric practices, where compliance with medication is more problematic, is debatable. The use of depot fluphenazine continues to be based on clinical judgement rather than evidence from methodical evaluation within trials. A large pragmatic randomized controlled trial is long overdue.
Bromperidol decanoate (depot) for schizophrenia
Cochrane Database Syst Rev 2011 Sep 7;(9):CD001719.PMID:21901678DOI:10.1002/14651858.CD001719.pub3.
Background: Antipsychotic drugs are the mainstay treatment for schizophrenia. Long-acting depot injections of drugs such as bromperidol decanoate are extensively used as a means of long-term maintenance treatment. Objectives: To assess the effects of depot bromperidol versus placebo, oral antipsychotics and other depot antipsychotic preparations for people with schizophrenia in terms of clinical, social and economic outcomes. Search strategy: For this 2011 update we searched the Cochrane Schizophrenia Group's Register (February 2011). Selection criteria: We sought all randomised trials focusing on people with schizophrenia where depot bromperidol, oral antipsychotics or other depot preparations. Primary outcomes were clinically significant change in global function, service utilisation outcomes (hospital admission, days in hospital), relapse. Data collection and analysis: For this 2011 update MP independently extracted data, CEA carried out the reliability check. We calculated fixed-effect risk ratios (RR) and 95% confidence intervals (CI) for dichotomous data, and calculated weighted or standardised means for continuous data. Where possible, we calculated the number needed to treat statistic (NNT). Analysis was by intention-to-treat. Main results: We have included no new trials in this 2011 update (4 RCTs, total n = 117). A single, small study of six months' duration compared bromperidol decanoate with placebo injection. Similar numbers left the study before completion (n = 20, 1 RCT, RR 0.4 CI 0.1 to 1.6) and there were no clear differences between bromperidol decanoate and placebo for a list of adverse effects (n = 20, 1 RCT, RR akathisia 2.0 CI 0.21 to 18.69, RR increased weight 3.0 CI 0.14 to 65.9, RR tremor 0.33 CI 0.04 to 2.69). When bromperidol decanoate was compared with fluphenazine depot, we found no important change on global outcome (n = 30, RR no clinical important improvement 1.50 CI 0.29 to 7.73). People allocated to Fluphenazine decanoate and haloperidol decanoate had fewer relapses than those given bromperidol decanoate (n = 77, RR 3.92 Cl 1.05 to 14.60, NNH 6 CI 2 to 341). People allocated bromperidol decanoate required additional antipsychotic medication somewhat more frequently than those taking Fluphenazine decanoate and haloperidol decanoate, but the results did not reach conventional levels of statistical significance (n = 77, 2 RCTs, RR 1.72 CI 0.7 to 4.2). The use of benzodiazepine drugs was very similar in both groups (n = 77, 2 RCTs, RR 1.08 CI 0.68 to 1.70). People left the bromperidol decanoate group more frequent than those taking other depot preparation due to any cause (n = 97, 3 RCTs, RR 2.17 CI 1.00 to 4.73). Anticholinergic adverse effects were equally common between bromperidol and other depots (n = 47, RR 3.13 CI 0.7 to 14.0) and additional anticholinergic medication was needed with equal frequency in both depot groups, although results did tend to favour the bromperidol decanoate group (n = 97, 3 RCTs, RR 0.80 CI 0.64 to 1.01). The incidence of movement disorders was similar in both depot groups (n = 77, 2 RCTs, RR 0.74 CI 0.47 to 1.17). Authors' conclusions: Minimal poorly reported trial data suggests that bromperidol decanoate may be better than placebo injection but less valuable than fluphenazine or haloperidol decanoate. If bromperidol decanoate is available it may be a viable choice, especially when there are reasons not to use fluphenazine or haloperidol decanoate. Well-conducted and reported randomised trials are needed to inform practice.