droperidol indications/contra

Stem definitionDrug idCAS RN
antipsychotics, haloperidol derivatives 966 548-73-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • droperidol
  • dehydrobenzperidol
  • droleptan
  • inapsin
  • inapsine
  • neurolidol
A butyrophenone with general properties similar to those of HALOPERIDOL. It is used in conjunction with an opioid analgesic such as FENTANYL to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon. It is also used as a premedicant, as an antiemetic, and for the control of agitation in acute psychoses. (From Martindale, The Extra Pharmacopoeia, 29th ed, p593)
  • Molecular weight: 379.44
  • Formula: C22H22FN3O2
  • CLOGP: 3.06
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 52.65
  • ALOGS: -3.59
  • ROTB: 6

Drug dosage:

DoseUnitRoute
2.50 mg P

Approvals:

DateAgencyCompanyOrphan
June 11, 1970 FDA AKORN INC

FDA Adverse Event Reporting System

scroll-->
MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Acute kidney injury 192.08 55.80 56 281 49627 3335895
Oliguria 122.57 55.80 22 315 2128 3383394
Haematuria 88.97 55.80 22 315 9930 3375592
Drug hypersensitivity 84.81 55.80 28 309 35652 3349870
Dystonia 69.29 55.80 15 322 3752 3381770
Electrocardiogram QT prolonged 58.21 55.80 16 321 10779 3374743

Pharmacologic Action:

scroll-->
SourceCodeDescription
ATC N05AD08 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Butyrophenone derivatives
FDA MoA N0000175799 Dopamine D2 Antagonists
FDA EPC N0000175800 Dopamine-2 Receptor Antagonist
MeSH PA D000759 Adjuvants, Anesthesia
MeSH PA D000932 Antiemetics
MeSH PA D014150 Antipsychotic Agents
MeSH PA D001337 Autonomic Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D015259 Dopamine Agents
MeSH PA D018492 Dopamine Antagonists
MeSH PA D065127 Dopamine D2 Receptor Antagonists
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents
CHEBI has role CHEBI:50919 antiemetic
CHEBI has role CHEBI:48561 dopaminergic antagonist
CHEBI has role CHEBI:60807 anaesthesia adjuvant
CHEBI has role CHEBI:65190 first generation antipsychotic

Drug Use (View source of the data)

scroll-->
DiseaseRelationSNOMED_IDDOID
Intra-Operative Nausea and Vomiting indication
Post-Operative Nausea and Vomiting indication
Alcoholism contraindication 7200002
Cardiomegaly contraindication 8186001
Chronic obstructive lung disease contraindication 13645005 DOID:3083
Neuroleptic malignant syndrome contraindication 15244003 DOID:14464
Chronic disease of respiratory system contraindication 17097001
Inflammatory bowel disease contraindication 24526004 DOID:0050589
Hypovolemia contraindication 28560003
Orthostatic hypotension contraindication 28651003
Torsades de pointes contraindication 31722008
Dehydration contraindication 34095006
Depressive disorder contraindication 35489007 DOID:2848
Hypertensive disorder contraindication 38341003 DOID:10763
Hypokalemia contraindication 43339004
Decreased cardiac function contraindication 43650005
Chronic heart failure contraindication 48447003
Bradycardia contraindication 48867003
Paralytic ileus contraindication 55525008 DOID:8442
Drug AND/OR toxin-induced diarrhea contraindication 65979008
Substance abuse contraindication 66214007
Benign intracranial hypertension contraindication 68267002 DOID:11459
Extrapyramidal disease contraindication 76349003
Urethral stricture contraindication 76618002
Decreased respiratory function contraindication 80954004
Injury of head contraindication 82271004
Cor pulmonale contraindication 83291003 DOID:8515
Kidney disease contraindication 90708001 DOID:2527
Disorder of biliary tract contraindication 105997008 DOID:9741
Prolonged QT interval contraindication 111975006
Procedure on urinary system contraindication 118677009
Hypomagnesemia contraindication 190855004
Disease of liver contraindication 235856003 DOID:409
Benign prostatic hyperplasia contraindication 266569009 DOID:2883
Lesion of brain contraindication 301766008
Pheochromocytoma contraindication 302835009
Central nervous system depression contraindication 418072004
Congenital long QT syndrome contraindication 442917000
Acute exacerbation of asthma contraindication 708038006

Acid dissociation constants calculated using MoKa v3.0.0

scroll-->
Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.6 acidic
pKa2 7.59 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

scroll-->
TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
D(2) dopamine receptor GPCR ANTAGONIST Ki 9.60 PDSP CHEMBL
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 9.13 DRUG MATRIX CHEMBL
Alpha-2A adrenergic receptor GPCR Ki 5.95 DRUG MATRIX
5-hydroxytryptamine receptor 1A GPCR Ki 6.86 DRUG MATRIX
5-hydroxytryptamine receptor 2B GPCR Ki 6.07 DRUG MATRIX
5-hydroxytryptamine receptor 2C GPCR Ki 6.62 DRUG MATRIX
Alpha-2B adrenergic receptor GPCR Ki 7.00 DRUG MATRIX
D(3) dopamine receptor GPCR Ki 9.03 DRUG MATRIX
Histamine H1 receptor GPCR Ki 6.28 DRUG MATRIX
Muscarinic acetylcholine receptor M4 GPCR Ki 6.27 DRUG MATRIX
Muscarinic acetylcholine receptor M5 GPCR Ki 5.78 DRUG MATRIX
Alpha-2C adrenergic receptor GPCR Ki 6.59 DRUG MATRIX
Alpha-1D adrenergic receptor GPCR Ki 9.17 DRUG MATRIX
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel IC50 6.13 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 7.49 CHEMBL
D(4) dopamine receptor GPCR Ki 9.08 PDSP
D(1A) dopamine receptor GPCR Ki 6.26 DRUG MATRIX
5-hydroxytryptamine receptor 4 GPCR Ki 6.20 DRUG MATRIX
Alpha-1B adrenergic receptor GPCR Ki 8.01 DRUG MATRIX
Membrane-associated progesterone receptor component 1 Membrane receptor Ki 5.69 DRUG MATRIX
5-hydroxytryptamine receptor 1A GPCR IC50 6.62 CHEMBL
Alpha-1A adrenergic receptor GPCR IC50 8.78 CHEMBL

External reference:

scroll-->
IDSource
DB00450 DRUGBANK_ID
4019047 VUID
N0000147316 NUI
C0013136 UMLSCUI
7172 IUPHAR_LIGAND_ID
D00308 KEGG_DRUG
3392 MMSL
3648 RXNORM
26574002 SNOMEDCT_US
387146001 SNOMEDCT_US
4646 MMSL
d00219 MMSL
4019047 VANDF
N0000006827 NDFRT
N0000147316 NDFRT
001517 NDDF
CHEMBL1108 ChEMBL_ID
3168 PUBCHEM_CID
D004329 MESH_DESCRIPTOR_UI
O9U0F09D5X UNII
1609 INN_ID
CHEBI:4717 CHEBI

Pharmaceutical products:

scroll-->
ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Droperidol HUMAN PRESCRIPTION DRUG LABEL 1 0409-1187 INJECTION, SOLUTION 2.50 mg INTRAMUSCULAR ANDA 14 sections
Droperidol HUMAN PRESCRIPTION DRUG LABEL 1 0517-9702 INJECTION, SOLUTION 2.50 mg INTRAMUSCULAR ANDA 14 sections