生物活性

• 描述Prochlorperazine (Dimaleate) is a D(2) antagonist. Prochlorperazine (1-2 mg/kg s.c./i.p.) produced an increase of the pain threshold in the mouse hot-plate test. Prochlorperazine also elicited a dose-dependent increase in ACh release from rat cerebral cortex. In the antinociceptive dose-range, prochlorperazine did not impair mouse performance evaluated by the rota-rod and hole-board tests. Thus, prochlorperazine exerted an antinociceptive effect mediated by a central cholinergic mechanism^[3]. Prochlorperazine is a phenothiazine-class antipsychotic drug and induces concentration-dependent loss in cell viability with EC50 value of 18.49 μM. Prochlorperazine in a concentration of 0.001 μM stimulated melanogenesis, while in concentrations 1.0 and 10.0 μM melanization process was inhibited. Furthermore, the drug in concentrations of 0.1, 1.0 and 10.0 μM caused changes in cellular antioxidant defense system, what indicated the induction of oxidative stress^[4]. Prochlorperazine is recommended for adults with breakthrough or refractory chemotherapy-induced nausea and vomiting (CINV). The most common AEs (adverse effects) reported with the pediatric use of prochlorperazine are EPS (extrapyramidal symptoms) and sedation. Fatalities, life-threatening, and persistent AEs have also been reported^[5]. IV hydromorphone is substantially less effective than IV prochlorperazine for the treatment of acute migraine in the ED (emergency department) and should not be used as first-line therapy^[6]. Buccally absorbed prochlorperazine (BAP) is an effective, non-invasive treatment for migraine headaches when compared to intravenous prochlorperazine (IVP)^[7].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT00475085	Nausea	Phase 3	Completed	-	United States, Alabama ... more >> MBCCOP - Gulf Coast Mobile, Alabama, United States, 36695 United States, Illinois CCOP - Central Illinois Decatur, Illinois, United States, 62526 United States, Kansas CCOP - Wichita Wichita, Kansas, United States, 67214-3882 United States, Michigan CCOP - Grand Rapids Grand Rapids, Michigan, United States, 49503 CCOP - Kalamazoo Kalamazoo, Michigan, United States, 49007-3731 United States, Minnesota CCOP - Metro-Minnesota St. Louis Park, Minnesota, United States, 55416 United States, Missouri CCOP - Kansas City Kansas City, Missouri, United States, 64131 United States, Nevada CCOP - Nevada Cancer Research Foundation Las Vegas, Nevada, United States, 89106 United States, New York CCOP - Hematology-Oncology Associates of Central New York East Syracuse, New York, United States, 13057 CCOP - North Shore University Hospital Manhassett, New York, United States, 11030 United States, North Carolina CCOP - Southeast Cancer Control Consortium Goldsboro, North Carolina, United States, 27534-9479 United States, Ohio CCOP - Columbus Columbus, Ohio, United States, 43215 CCOP - Dayton Dayton, Ohio, United States, 45429 United States, South Carolina CCOP - Greenville Greenville, South Carolina, United States, 29615 United States, Washington CCOP - Northwest Tacoma, Washington, United States, 98405-0986 United States, Wisconsin CCOP - Marshfield Clinic Research Foundation Marshfield, Wisconsin, United States, 54449 Collapse <<
  NCT00475085	-	-	Completed	-	-
  NCT03684005	Cancer	Not Applicable	Recruiting	December 2019	United States, Michigan ... more >> Barbara Ann Karmanos Cancer Institute Recruiting Detroit, Michigan, United States, 48201 Principal Investigator: Felicity Harper, Ph.D.          Sub-Investigator: Elisabeth I. Heath, M.D.          Sub-Investigator: Louis Penner, Ph.D. Collapse <<

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• 参考文献

• [1] Huang L, Zhao S, et al. An integrated bioinformatics approach identifies elevated cyclin E2 expression and E2F activity as distinct features of tamoxifen resistant breast tumors. PLoS One. 2011;6(7):e22274.

  [2] Ghelardini C, Galeotti N, et al. Prochlorperazine induces central antinociception mediated by the muscarinic system. Pharmacol Res. 2004 Sep;50(3):351-8.

  [3] Ghelardini C, Galeotti N, Uslenghi C, Grazioli I, Bartolini A. Prochlorperazine induces central antinociception mediated by the muscarinic system. Pharmacol Res. 2004;50(3):351‐358

  [4] Otręba M, Wrześniok D, Rok J, Beberok A, Buszman E. Prochlorperazine interaction with melanin and melanocytes. Pharmazie. 2017;72(3):171‐176

  [5] Lau Moon Lin M, Robinson PD, Flank J, Sung L, Dupuis LL. The Safety of Prochlorperazine in Children: A Systematic Review and Meta-Analysis. Drug Saf. 2016;39(6):509‐516

  [6] Friedman BW, Irizarry E, Solorzano C, et al. Randomized study of IV prochlorperazine plus diphenhydramine vs IV hydromorphone for migraine. Neurology. 2017;89(20):2075‐2082

  [7] Fernando T, Lumanauw DD, Youn S, et al. Buccally absorbed vs intravenous prochlorperazine for treatment of migraines headaches. Acta Neurol Scand. 2019;140(1):72‐77

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