Paliperidone palmitate
(Synonyms: 棕榈酸帕利哌酮,9-Hydroxyrisperidone palmitate) 目录号 : GC61167
Paliperidone Palmitate (9-hydroxyrisperidone palmitate) is a palmitate ester of paliperidone, which is a dopamine antagonist and 5-HT2A antagonist of the atypical antipsychotic class.
Cas No.:199739-10-1
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
Paliperidone Palmitate (9-hydroxyrisperidone palmitate) is a palmitate ester of paliperidone, which is a dopamine antagonist and 5-HT2A antagonist of the atypical antipsychotic class.
| Cas No. | 199739-10-1 | SDF | |
| 别名 | 棕榈酸帕利哌酮,9-Hydroxyrisperidone palmitate | ||
| Canonical SMILES | O=C(OC1CCCN(C1=NC(C)=C2CCN3CCC(C4=NOC5=C4C=CC(F)=C5)CC3)C2=O)CCCCCCCCCCCCCCC | ||
| 分子式 | C39H57FN4O4 | 分子量 | 664.89 |
| 溶解度 | 储存条件 | 4°C, away from moisture and 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 | 1.504 mL | 7.52 mL | 15.0401 mL |
| 5 mM | 0.3008 mL | 1.504 mL | 3.008 mL |
| 10 mM | 0.1504 mL | 0.752 mL | 1.504 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。
Paliperidone palmitate: effectiveness, safety, and the use for treatment of schizophrenia
Psychiatr Pol 2017 Feb 26;51(1):7-21.PMID:28455891DOI:10.12740/PP/64581.
The aim of the study was to summarize the efficacy and tolerability of Paliperidone palmitate, an atypical long-acting antipsychotic drug. Paliperidone is a 9-hydroxy metabolite of risperidone with a slightly different receptor profile and significantly different pharmacokinetic profile. After the short review of its pharmacological properties, the efficacy of the drug in comparison to placebo or to an active comparator was described. The studies revealed the effectiveness of Paliperidone palmitate in the treatment of psychotic symptoms, mainly schizophrenia. The drug proved to be efficacious in both acute psychotic symptoms treatment and long-term treatment. Its efficacy in patients with schizophrenia was similar and sometimes even better than the efficacy of other long-acting drugs, such as risperidone or olanzapine. In the pharmacoeconomic studies, paliperidone proved to be cost-effective in comparison to risperidone or olanzapine. The review of the literature also underlined that Paliperidone palmitate is well tolerated, compared with placebo. Frequency and severity of side-effects such as extrapyramidal symptoms, hyperprolactinemia and weight gain, was similar or less than those found in treatment with other atypical antipsychotics, including long-acting ones.
A Randomized, Double-Blind, Multicenter, Noninferiority Study Comparing Paliperidone palmitate 6-Month Versus the 3-Month Long-Acting Injectable in Patients With Schizophrenia
Int J Neuropsychopharmacol 2022 Mar 17;25(3):238-251.PMID:34791283DOI:10.1093/ijnp/pyab071.
Background: This double-blind (DB), randomized, parallel-group study was designed to evaluate efficacy and safety of Paliperidone palmitate 6-month (PP6M) formulation relative to Paliperidone palmitate 3-month (PP3M) formulation in patients with schizophrenia. Methods: Following screening, patients entered an open-label (OL) maintenance phase and received 1 injection cycle of Paliperidone palmitate 1-month (PP1M; 100 or 150 mg eq.) or PP3M (350 or 525 mg eq.). Clinically stable patients were randomized (2:1) to receive PP6M (700 or 1000 mg eq., gluteal injections) or PP3M (350 or 525 mg eq.) in a 12-month DB phase; 2 doses of PP6M (corresponding to doses of PP1M and PP3M) were chosen. Results: Overall, 1036 patients were screened, 838 entered the OL phase, and 702 (mean age: 40.8 years) were randomized (PP6M: 478; PP3M: 224); 618 (88.0%) patients completed the DB phase (PP6M: 416 [87.0%]; PP3M: 202 [90.2%]). Relapse rates were PP6M, 7.5% (n = 36) and PP3M, 4.9% (n = 11). The Kaplan-Meier estimate of the difference (95% CI) between treatment groups (PP6M - PP3M) in the percentages of patients who remained relapse free was -2.9% (-6.8%, 1.1%), thus meeting noninferiority criteria (95% CI lower bound is larger than the pre-specified noninferiority margin of -10%). Secondary efficacy endpoints corroborated the primary analysis. Incidences of treatment-emergent adverse events were similar between PP6M (62.1%) and PP3M (58.5%). No new safety concerns emerged. Conclusions: The efficacy of a twice-yearly dosing regimen of PP6M was noninferior to that of PP3M in preventing relapse in patients with schizophrenia adequately treated with PP1M or PP3M. Trial registration: Clinical Trials.gov identifier: NCT03345342.
Long-Acting Injectable Paliperidone palmitate: A Review of Efficacy and Safety
Psychopharmacol Bull 2017 May 15;47(2):42-52.PMID:28626271doi
Objective: Summarize and synthesize the current literature regarding long-acting injectable Paliperidone palmitate for the treatment of schizophrenia. Methods: A literature search of PubMed, Embase, and Web of Science was conducted in February 2016, using the following search terms in varying permutations: schizophrenia; antipsychotic medication; long-acting injectable; Paliperidone palmitate; 3-monthly injectable. Results: Once-monthly injectable Paliperidone palmitate (PDP) has demonstrated comparable efficacy as 1st-generation long-acting injectable antipsychotics (LAIAs) in reducing disease severity and re-hospitalizations in schizophrenic patients. However, PDP leads to significantly less extrapyramidal symptoms than these older medications indicating a superior safety profile. Compared to oral 2nd-generation antipsychotics, PDP has shown less incidence of disease relapse related to medication non-compliance, particularly in real world populations. It also showed a similar safety profile as oral 2nd-generation antipsychotics, but with greater incidence of mild injection-site pain. A novel 3-monthly formulation of PDP has shown similar safety and efficacy as once-monthly PDP compared to placebo. Conclusions: Overall, both 1-month and 3-month formulations of PDP are safe and effective in the treatment of schizophrenia and schizoaffective disorder. They may be most effective in patients with prior failed treatment of oral antipsychotics or other LAIAs, in patients with a history of medication noncompliance, or in patients with an individual preference for less frequent dosing.
Paliperidone palmitate three-month depot formulation: a helpful innovation with practical pitfalls
Australas Psychiatry 2018 Apr;26(2):206-209.PMID:29359582DOI:10.1177/1039856217751986.
Objective: Paliperidone palmitate is now available as a three-month depot injection. This paper will review the pharmacokinetics, pharmacodynamics, efficacy and tolerability, as well as practical issues and pitfalls for clinicians with this innovative treatment for schizophrenia. Conclusion: The three-month depot formulation of paliperidone for the treatment of schizophrenia is not a new compound. The nanocrystalline structure of the three-month formulation is larger and takes longer to disperse than the one-month formulation, hence its extended depot action. As expected, it is non-inferior to one-month depot paliperidone, and superior to placebo, for the treatment of schizophrenia. The side effect profile of three-month paliperidone is identical to the one-month formulation. The relapse rate on treatment is low, and the median time to relapse after ceasing the drug is 395 days. An understanding of half-life and kinetics is crucial for clinicians using this compound, and the loading strategy is important to ensure effectiveness. There are significant challenges: ensuring timely administration and switching a three-month depot treatment to another antipsychotic may be problematic. Paliperidone palmitate three-month depot injection represents an advance for both convenience and effectiveness in the long term psychopharmacological treatment of schizophrenia.
Effect of 3-monthly Paliperidone palmitate on hospitalisation in a naturalistic schizophrenia cohort - A five-year mirror image study
J Psychiatr Res 2022 Apr;148:131-136.PMID:35123325DOI:10.1016/j.jpsychires.2022.01.044.
Purpose/background: Currently the longest-acting antipsychotic formulation widespread clinical use is paliperidone 3-monthly injection (PP3M). While its efficacy has been shown in rigorous trials, there are few data relating to its effect on hospitalisation in normal clinical practice. Methods/procedures: This was a mirror-image study (3 years before; 2 years after) of hospitalisations before and after beginning paliperidone 1-monthly (PP1M) and switching to 3-monthly within 18 months. All consecutive patients prescribed paliperidone long-acting injections with its licence (F20 schizophrenia diagnosis; 18-65 years) were included. The setting was an urban, specialist mental health organisation In London, UK. Findings/results: In total 378 patients were initiated on PP3M during the study period. After applying inclusion criteria, 76 patients were retained and followed-up for 2 years. Mean duration of PP1M use before starting 3-monthly injections was 6 months (range 3-18 months). Of the 76 patients initiated, 13 patients discontinued PP3M within 2 years of starting PP1M or were lost to follow-up. Mean hospitalisations per patient per year fell from 0.55 (SD 0.46) before paliperidone to 0.05 (SD 0.19) after initiation (p < 0.001). Only 5 of 76 PP1M/PP3M participants were hospitalised during the 2-year follow up. The mean number of bed days per year before paliperidone initiation was 32.2 (SD 44.3) and after paliperidone initiation it was 23.0 (SD 53.2) (p = 0.004). Almost all of the bed days after initiation were associated with the index admission during which PP1M was started. Implications/conclusions: In patients stabilised on PP1M and switched to PP3M in normal clinical practice, rehospitalisation is very uncommon and much reduced compared with previous treatments.