Droperidol

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Image:Droperidol.png
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	N01 AX01 N05 AD08
PubChem	3168
DrugBank	APRD00939
Chemical data
Formula	C₂₂H₂₂FN₃O₂
Mol. weight	379.428 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	?

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

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.

[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.

[edit] External links

Link page to external chemical sources.

General anesthetics (N01A) edit
Ethers:	Diethyl ether, Vinyl ether, Desflurane, Enflurane, Isoflurane, Methoxyflurane, Sevoflurane
Haloalkanes:	Chloroform, Halothane, Trichloroethylene
Barbiturates:	Hexobarbital, Methohexital, Narcobarbital, Thiopental
Opioids:	Alfentanil, Anileridine, Fentanyl, Phenoperidine, Remifentanil, Sufentanil
Others:	Alfaxalone, Minaxolone, Droperidol, Esketamine, Etomidate, Hydroxybutyric acid, Ketamine, Nitrous oxide, Propanidid, Propofol

Antipsychotics (N05A) edit
Phenothiazine typical antipsychotics:	Chlorpromazine, Fluphenazine, Mesoridazine, Perphenazine, Prochlorperazine, Promazine, Thioridazine, Trifluoperazine
Other typical antipsychotics:	Chlorprothixene, Droperidol, Flupentixol, Haloperidol, Loxapine, Molindone, Pimozide, Sulforidazine, Thiothixene
Atypical antipsychotics:	Amisulpride, Aripiprazole, Clozapine, Olanzapine, Quetiapine, Risperidone/Paliperidone, Sertindole, Sulpiride, Ziprasidone, Zotepine