Droperidol

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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. Discovered at Janssen Pharmaceutica in 1961, it 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 antipsychotic in doses ranging from 5 to 10mg given as an intramuscular injection, generally in cases of severe agitation in a psychotic patient who is refusing oral medication. However 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. Droperidol can also cause hypotension. Its use in intramuscular sedation has been replaced by intramuscular preparations of haloperidol, midazolam, clonazepam and olanzapine.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 patient who hasn’t responded to Epley maneuvers.

[edit] Side effects

Dysphoria, Sedation, Hypotension resulting from peripheral alpha adrenoceptor blockade, Prolongation of QT interval which can lead to Torsades de Pointes, Extrapyramidal side effects such as dystonic reactions/ neuroleptic malignant syndrome - If you experience any of the rare side-effects such as spasms of the face, one should have diphenhydramine (Benadryl) or Benztropine (Cogentin) 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.

[edit] 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

[edit] External links

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