Droperidol

Dopamine-2 Receptor Antagonist — NERVOUS SYSTEM

Key facts

Droperidol is an ofp drug in the Dopamine-2 Receptor Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 1970. Its mechanism of action is classified as Dopamine D2 Antagonists. DrugCentral lists 22 molecular targets, including DRD2, ADRA1D and HTR2A. Recorded indications include Intra-Operative Nausea and Vomiting and Post-Operative Nausea and Vomiting.

• Approval status: ofp (first approved 1970 by the FDA).
• Drug class: Dopamine-2 Receptor Antagonist.
• Mechanism of action: Dopamine D2 Antagonists.
• Molecular targets: DRD2, ADRA1D, HTR2A and DRD4 (22 listed in DrugCentral).
• Indications: Intra-Operative Nausea and Vomiting and Post-Operative Nausea and Vomiting.
• ATC code: N05AD08 (Butyrophenone derivatives).
• Molecular formula: C22H22FN3O2; molecular weight 379.44 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• Intra-Operative Nausea and Vomiting
• Post-Operative Nausea and Vomiting

Contraindications (37)

• Acute exacerbation of asthma
• Alcoholism
• Benign intracranial hypertension
• Benign prostatic hyperplasia
• Bradycardia
• Cardiomegaly
• Central nervous system depression
• Chronic disease of respiratory system
• Chronic heart failure
• Chronic obstructive lung disease
• Congenital long QT syndrome
• Cor pulmonale
• Decreased cardiac function
• Decreased respiratory function
• Dehydration
• Depressive disorder
• Disease of liver
• Disorder of biliary tract
• Drug AND/OR toxin-induced diarrhea
• Extrapyramidal disease
• Hypertensive disorder
• Hypokalemia
• Hypomagnesemia
• Hypovolemia
• Inflammatory bowel disease
• Injury of head
• Kidney disease
• Lesion of brain
• Neuroleptic malignant syndrome
• Orthostatic hypotension
• + 7 more

Mechanism & targets

• Mechanism of action (MoA): Dopamine D2 Antagonists
• Established pharmacologic class: Dopamine-2 Receptor Antagonist

Molecular targets (22)

Target	Gene	Action	Activity
D(2) dopamine receptor	DRD2	antagonist	Ki 9.60
Alpha-1D adrenergic receptor	ADRA1D	unknown	Ki 9.18
5-hydroxytryptamine receptor 2A	HTR2A	antagonist	Ki 9.13
D(4) dopamine receptor	DRD4	unknown	Ki 9.08
D(3) dopamine receptor	DRD3	unknown	Ki 9.03
Alpha-1A adrenergic receptor	Adra1a	unknown	IC50 8.78
Alpha-1B adrenergic receptor	Adra1b	unknown	Ki 8.01
Potassium voltage-gated channel subfamily H member 2	KCNH2	unknown	IC50 7.49
Alpha-2B adrenergic receptor	ADRA2B	unknown	Ki 7.00
5-hydroxytryptamine receptor 1A	HTR1A	unknown	Ki 6.86
5-hydroxytryptamine receptor 2C	HTR2C	unknown	Ki 6.62
5-hydroxytryptamine receptor 1A	Htr1a	unknown	IC50 6.62
Alpha-2C adrenergic receptor	ADRA2C	unknown	Ki 6.59
Histamine H1 receptor	HRH1	unknown	Ki 6.28
Muscarinic acetylcholine receptor M4	CHRM4	unknown	Ki 6.27
D(1A) dopamine receptor	DRD1	unknown	Ki 6.26
5-hydroxytryptamine receptor 4	HTR4	unknown	Ki 6.20
Sodium channel alpha subunits; brain (Types I, II, III)	SCN1A|SCN2A|SCN3A	unknown	IC50 6.13
5-hydroxytryptamine receptor 2B	HTR2B	unknown	Ki 6.07
Alpha-2A adrenergic receptor	ADRA2A	unknown	Ki 5.95

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1970-06-11	FDA	—	AKORN INC

ATC classification

ATC code	Therapeutic hierarchy
N05AD08	NERVOUS SYSTEM › PSYCHOLEPTICS › ANTIPSYCHOTICS › Butyrophenone derivatives

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Anaphylactic shock	388.8
Streptococcal sepsis	126.7
Restlessness	114.4
Nail bed inflammation	109.9
Pseudomonal sepsis	107.8
Nasal mucosal disorder	103.8
Anaphylactic reaction	91.6
Vascular device infection	88.0
Varicose vein	86.0
Metastases to lymph nodes	80.8
Brain oedema	77.2
Oliguria	70.5

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Droperidol is on its molecule page.

• Molecular formula: C₂₂H₂₂FN₃O₂
• Molecular weight: 379.44 g/mol
• CAS number: 548-73-2
• InChIKey: RMEDXOLNCUSCGS-UHFFFAOYSA-N
• PubChem CID: 3168

FC1=CC=C(C=C1)C(=O)CCCN1CCC(=CC1)N1C(=O)NC2=C1C=CC=C2

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Droperidol used for?

DrugCentral lists the following indications for Droperidol: Intra-Operative Nausea and Vomiting and Post-Operative Nausea and Vomiting.

How does Droperidol work?

Droperidol is classified as Dopamine D2 Antagonists; its molecular targets in DrugCentral include DRD2 (antagonist), ADRA1D, HTR2A (antagonist) and DRD4.

When was Droperidol first approved?

Droperidol was first approved by the FDA in 1970.

What drug class does Droperidol belong to?

Droperidol is in the Dopamine-2 Receptor Antagonist class.

What is the chemical formula of Droperidol?

Droperidol has the molecular formula C22H22FN3O2 and a molecular weight of 379.44 g/mol.

Sources

• DrugCentral drug card 966 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1108 — compound record and bioactivity
• PubChem CID 3168 — chemical identifiers
• DrugBank DB00450 — drug record
• FDA UNII O9U0F09D5X — substance identity
• DailyMed: FDA labels for Droperidol — current prescribing information (label search)
• UniProt P14416 (DRD2) — target protein
• UniProt P25100 (ADRA1D) — target protein
• UniProt P28223 (HTR2A) — target protein
• UniProt P21917 (DRD4) — target protein
• UniProt P35462 (DRD3) — target protein
• UniProt Q12809 (KCNH2) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.