Droperidol

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Droperidol chemical structure Droperidol
1-[1-[4-(4-fluorophenyl)-4-oxo-butyl]- 3,6-dihydro-2H-pyridin-4-yl]- 3H-benzoimidazol- 2-one IUPAC name
CAS number 548-73-2	ATC code N01AX01 .
PubChem 3168	DrugBank APRD00939
Chemical formula	{{{chemical_formula}}}
Molecular weight	379.428 g/mol
Bioavailability
Metabolism	Hepatic
Elimination half-life	2.3 hours
Excretion	{{{excretion}}}
Pregnancy category	C (US)
Legal status
Routes of administration	Intraveneous, Intramuscular

Droperidol (Dropletan® or Inapsine®) 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.

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.

External links

• Link page to external chemical sources.

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