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Droperidol



Droperidol
Systematic (IUPAC) name
1-[1-[4-(4-fluorophenyl)-4-oxo-butyl]- 3,6-dihydro-2H-pyridin-4-yl]- 3H-benzoimidazol- 2-one
Identifiers
CAS number 548-73-2
ATC code N01AX01 N05AD08
PubChem 3168
DrugBank APRD00939
Chemical data
Formula C22H22FN3O2 
Mol. mass 379.428 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism Hepatic
Half life 2.3 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.

C (US)

Legal status
Routes Intraveneous, Intramuscular

Droperidol (Dropletan®, Dridol® or Inapsine®) is an antidopaminergic drug used as an antiemetic and antipsychotic. It was discovered at Janssen Pharmaceutica in 1961.

Additional recommended knowledge

Droperidol is a butyrophenone, and is a potent D2 (dopamine receptor) antagonist with some histamine and serotonin antagonist activity. It has a central antiemetic action and is frequently used in the treatment of postoperative nausea and vomiting in adult doses as low as 0.625 or 1.25 mg.

It has also been used as an anti-psychotic in doses as high as 10mg i.m.

In 2001, the FDA changed the labeling requirements for droperidol injection, to include a so-called "Black Box Warning", citing concerns of QT prolongation and torsades de pointes. The evidence for this is disputed, with less than 20 reported cases of torsades in 30 years and most of those having received doses in excess of 50mg in a 24-hour period. It appears that the QT-prolongation is a dose-related effect and that in low doses, droperidol is not a significant risk.

Some practitioners recommend the use of 0.5 mg to 1 mg I.V. for the treatment of vertigo in an otherwise healthy elderly patient who hasn’t responded to Epley maneuvers.

Side effects

If you experience any of the rare side-effects such as spasms of the face, one should have diphenhydramine (Benadryl®) injected into their IV to block the effects of the drug. If one is at home, fast acting Benadryl® dissolving mouth strips should be taken followed by a pill.

References

  • Scuderi PE: Droperidol: Many questions, few answers. Anesthesiology 2003; 98: 289-90
  • Lischke V, Behne M, Doelken P, Schledt U, Probst S, Vettermann J. Droperidol causes a dose-dependent prolongation of the QT interval. Department of Anesthesiology and Resuscitation, Johann Wolfgang Goethe-University Clinics, Frankfurt am Main, Germany.
  • Emergency Medicine Magazine : http://www.emedmag.com/html/pre/tri/1005.asp
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Droperidol". A list of authors is available in Wikipedia.
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