Chemistry:Droperidol

From HandWiki
Short description: Antidopaminergic drug
Droperidol
Skeletal formula of droperidol
Ball-and-stick model of droperidol
Clinical data
Pregnancy
category
  • AU: C
  • US: C (Risk not ruled out)
Routes of
administration		Intravenous, Intramuscular
Drug classTypical antipsychotic
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • BR: Class C1 (Other controlled substances)
  • UK: POM (Prescription only)
  • US: ℞-only
Pharmacokinetic data
MetabolismHepatic
Elimination half-life2.3 hours
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC22H22FN3O2
Molar mass379.435 g·mol−1
3D model (JSmol)

Droperidol /droʊˈpɛrIdɔːl/ (Inapsine, Droleptan, Dridol, Xomolix, Innovar [combination with fentanyl]) is an antidopaminergic drug used as an antiemetic (that is, to prevent or treat nausea) and as an antipsychotic. Droperidol is also often used as a rapid sedative in intensive-care treatment, and where "agitation aggression or violent behavior"[1] are present.[2][3]

History

Discovered at Janssen Pharmaceutica in 1961, droperidol is a butyrophenone which acts as a potent D2 (dopamine receptor) antagonist with some histamine and serotonin antagonist activity.[4]

Medical use

It has a central antiemetic action and effectively prevents postoperative nausea and vomiting in adults using doses as low as 0.625 mg.

For treatment of nausea and vomiting, droperidol and ondansetron are equally effective; droperidol is more effective than metoclopramide.[5] It has also been used as an antipsychotic in doses ranging from 5 to 10 mg given as an intramuscular injection, generally in cases of severe agitation in a psychotic patient who is refusing oral medication. Its use in intramuscular sedation has been replaced by intramuscular preparations of haloperidol and olanzapine. Some practitioners recommend the use of 0.5 mg to 1 mg intravenously for the treatment of vertigo in an otherwise healthy elderly patients who have not responded to Epley maneuvers.

Black box warning

In 2001, the FDA changed the labeling requirements for droperidol injection to include a Black Box Warning, citing concerns of QT prolongation and torsades de pointes. The evidence for this is disputed, with 9 reported cases of torsades in 30 years and all of those having received doses in excess of 5 mg.[6] QT prolongation is a dose-related effect,[7] and it appears that droperidol is not a significant risk in low doses. A study in 2015 showed that droperidol is relatively safe and effective for the management of violent and aggressive adult[8] patients in hospital emergency departments in doses of 10mg and above and that there was no increased risk of QT prolongation and torsades de pointes.

Side effects

Dysphoria, sedation, hypotension resulting from peripheral alpha adrenoceptor blockade, prolongation of QT interval which can lead to torsades de pointes, and extrapyramidal side effects such as dystonic reactions/neuroleptic malignant syndrome.[9]

References

  1. ↑ Edge R, Argáez C. Droperidol for Agitation in Acute Care [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2021 Jan. Available from: https://www.ncbi.nlm.nih.gov/books/NBK571530/
  2. ↑ "American Academy of Emergency Medicine Position Statement: Safety of Droperidol Use in the Emergency Department". The Journal of Emergency Medicine 49 (1): 91–97. July 2015. doi:10.1016/j.jemermed.2014.12.024. PMID 25837231. 
  3. ↑ "Rescue Sedation When Treating Acute Agitation in the Emergency Department With Intramuscular Antipsychotics". The Journal of Emergency Medicine 56 (5): 484–490. May 2019. doi:10.1016/j.jemermed.2018.12.036. PMID 30745194. 
  4. ↑ "Relationship of neuroleptic drug effects at brain dopamine, serotonin, alpha-adrenergic, and histamine receptors to clinical potency". The American Journal of Psychiatry 137 (12): 1518–1522. December 1980. doi:10.1176/ajp.137.12.1518. PMID 6108081. 
  5. ↑ "Comparative efficacy and safety of ondansetron, droperidol, and metoclopramide for preventing postoperative nausea and vomiting: a meta-analysis". Anesthesia and Analgesia 88 (6): 1370–1379. June 1999. doi:10.1213/00000539-199906000-00032. PMID 10357347. 
  6. ↑ "Droperidol, QT prolongation, and sudden death: what is the evidence?". Annals of Emergency Medicine 41 (4): 546–558. April 2003. doi:10.1067/mem.2003.110. PMID 12658255. 
  7. ↑ "Droperidol causes a dose-dependent prolongation of the QT interval". Anesthesia and Analgesia 79 (5): 983–986. November 1994. doi:10.1213/00000539-199411000-00028. PMID 7978420. 
  8. ↑ "The Safety and Effectiveness of Droperidol for Sedation of Acute Behavioral Disturbance in the Emergency Department". Annals of Emergency Medicine 66 (3): 230–238.e1. September 2015. doi:10.1016/j.annemergmed.2015.03.016. PMID 25890395. 
  9. ↑ "Acute dystonia by droperidol during intravenous patient-controlled analgesia in young patients". Journal of Korean Medical Science 17 (5): 715–717. October 2002. doi:10.3346/jkms.2002.17.5.715. PMID 12378031. 

Further reading



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