Droperidol

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Cat Number

API548732

CAS Number

548-73-2

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Product Detail Description Scientific Support Customer Q&A

CAS Number

548-73-2

EINECS

208-957-8

Storage

Store at room temperature

Synonyms

Droleptan; Dehydrobenzperidol; Inapsine; Dridol; Properidol; Sintodril; Sintosian

Molecular Formula

C22H22FN3O2

Molecular Weight

379.4

Smiles

C1CN(CC=C1N2C3=CC=CC=C3NC2=O)CCCC(=O)C4=CC=C(C=C4)F

Appearance

White to light yellow crystalline powder

Melting Point

148-149℃

Boiling Point

616.4±65.0℃ at 760 mmHg

Relative Density

1.3±0.1

General Description

Droperidol is a butyrophenone first-generation antipsychotic with a primary mechanism of action as a central dopamine D2-receptor antagonist. It was approved by the FDA in 1971 for the treatment of nausea, vomiting, anxiety, and sedation.

Mechanism of Action

Droperidol exerts its sedative, antipsychotic, and antiemetic effects by antagonizing the dopamine-2 receptor (D2-R). It also exhibits mild alpha-1 adrenergic blockade and sedative effects. The drug has a rapid onset of action with effects seen in 3-10 minutes and a duration of action that lasts approximately 2 to 4 hours.

Application

In the emergency department, droperidol is used to manage acute agitation, headaches, nausea, vomiting, and vertigo. For chemical sedation of the agitated patient, it has a rapid onset and is more effective and faster than haloperidol. It is also an effective antiemetic in postoperative and emergent settings, and is a potent treatment for acute headaches and vertigo.

This updated Cochrane review (four trials) found that droperidol was more effective than placebo at achieving tranquillisation or sleep by 30 minutes (RR 1.18) and reduced the need for additional medication. Compared with haloperidol, droperidol showed similar efficacy but required less additional medication. Against midazolam, droperidol was less rapidly tranquillising, whereas compared with olanzapine, it showed similar efficacy but again reduced the need for rescue medication. Adverse cardiovascular or respiratory events did not differ significantly from comparators, though evidence for some outcomes was of moderate to low quality. Droperidol appears effective for acute agitation, but further high‑quality trials are needed.

Fig. 1 Risk of bias graph: review authors' judgements about each risk of bias item presented as percentages across all included studies. (Khokhar MA, et al., 2016)

References

Khokhar MA, Rathbone J. Droperidol for psychosis-induced aggression or agitation. Cochrane Database Syst Rev. 2016;12(12):CD002830.

Does Droperidol require protection from light during storage?

Yes, it is photosensitive. Prolonged UV exposure can cause photodegradation and discoloration. Store in light-resistant, tightly sealed containers, preferably amber glass.

What is the recommended storage temperature for Droperidol?

Store at controlled room temperature (15-25°C). Avoid excessive heat above 30°C, which can accelerate oxidative degradation and impurity formation.

Is Droperidol hygroscopic, and how does this affect its stability?

It exhibits low hygroscopicity. However, under high humidity (>70% RH), it may absorb moisture and clump. Storage with desiccant is recommended.

How is the impurity 4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one monitored?

This process-related impurity is quantified using a stability-indicating HPLC method, ensuring it remains below ICH qualification thresholds.