Droperidol

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Chemical Structure| 548-73-2 同义名 : 氟哌利多 ;Dehydrobenzperidol; DHBP; Taylor Brand of Droperidol; Kern Brand of Droperidol; Janssen Brand of Droperidol; Properidol; Dridol; Inapsine; Droleptan; NSC 169874
CAS号 : 548-73-2
货号 : A541340
分子式 : C22H22FN3O2
纯度 : 99%+
分子量 : 379.43
MDL号 : MFCD00083290
存储条件:

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 35 mg/mL(92.24 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

生物活性
描述 Droperidol, a dopamine-2 receptor antagonist, is a butyrophenone, with anti-emetic, sedative and anti-anxiety properties. Parenteral droperidol is an effective option for the treatment of acute migraine. The minimum effective dose is 2.5 mg given IM or IV (intramuscularly or intravenously ). The most commonly reported adverse effects were extrapyramidal symptoms and sedation[3]. QT prolongation is noted with multiple medication classes, and droperidol increases QT interval in a dose-dependent fashion among susceptible individuals[4]. Midazolam-droperidol combination therapy is superior, in the doses studied, to either droperidol or olanzapine monotherapy for intravenous sedation of the acutely agitated ED (emergency department) patient[5]. Droperidol significantly reduced opioid-induced PONV (postoperative nausea and vomiting) in adults during PCA (patient-controlled analgesia) and had a morphine-sparing effect. Droperidol is generally well tolerated and the incidence of adverse effects is similar to that observed with placebo and the serotonin 5-HT3 receptor antagonists (setrons)[6].
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
NCT03506789 Postoperative Pain Phase 4 Recruiting June 30, 2020 Denmark ... 展开 >> Gildhøj Privathospital Not yet recruiting Brøndbyvester, Denmark, 2605 Contact: Niels A Pedersen, MD          Bispebjerg Hospital Recruiting Copenhagen, Denmark, 2400 Contact: Troels H Lunn, DMSc          Sjællands Universitetshospital, Køge Not yet recruiting Køge, Denmark, 4600 Contact: Ole Mathiesen, MD, PhD, Assoc Prof.          Næstsved Sygehus Recruiting Næstved, Denmark, 4700 Contact: Kasper S Gasbjerg, MD          Odense Universitetshospital Not yet recruiting Odense, Denmark, 5000 Contact: Søren Overgaard, DMSc 收起 <<
NCT03618082 Immediate Severe Postoperative... 展开 >> Pain Perioperative Hemodynamic 收起 << Phase 3 Not yet recruiting March 31, 2021 France ... 展开 >> CHU Clermont-Ferrand Not yet recruiting Clermont-Ferrand, Auvergne, France, 63003 Contact: Lise LACLAUTRE    04 73 75 49 63    drci@chu-clermontferrand.fr    Principal Investigator: Jean-Etienne BAZIN          Sub-Investigator: Bernard ALLAOUICHE          Sub-Investigator: Emmanuel FUTIER          Sub-Investigator: Lionel BOUVET          Sub-Investigator: Régis FUZIER          Sub-Investigator: Elizabeth GAERTNER          Sub-Investigator: Mathieu JEANNE          Sub-Investigator: Hervé MUSELLEC 收起 <<
NCT03036514 Pain, Postoperative Not Applicable Active, not recruiting February 2019 Belgium ... 展开 >> University hospital Antwerp Edegem, Antwerp, Belgium, 2650 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.64mL

0.53mL

0.26mL

13.18mL

2.64mL

1.32mL

26.36mL

5.27mL

2.64mL

参考文献

[1]Kao LW, Kirk MA, et al. Droperidol, QT prolongation, and sudden death: what is the evidence? Ann Emerg Med. 2003 Apr;41(4):546-58.

[2]Adamantidis MM, Kerram P, et al. Droperidol exerts dual effects on repolarization and induces early afterdepolarizations and triggered activity in rabbit Purkinje fibers. J Pharmacol Exp Ther. 1993 Aug;266(2):884-93.

[3]Thomas MC, Musselman ME, Shewmaker J. Droperidol for the treatment of acute migraine headaches. Ann Pharmacother. 2015;49(2):233‐240

[4]Perkins J, Ho JD, Vilke GM, DeMers G. American Academy of Emergency Medicine Position Statement: Safety of Droperidol Use in the Emergency Department. J Emerg Med. 2015;49(1):91‐97

[5]Taylor DM, Yap CYL, Knott JC, et al. Midazolam-Droperidol, Droperidol, or Olanzapine for Acute Agitation: A Randomized Clinical Trial. Ann Emerg Med. 2017;69(3):318‐326.e1

[6]McKeage K, Simpson D, Wagstaff AJ. Intravenous droperidol: a review of its use in the management of postoperative nausea and vomiting. Drugs. 2006;66(16):2123‐2147