droperidol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

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: 3.26
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 52.65
  • ALOGS: -3.59
  • ROTB: 6
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
2.50 mg P

ADMET properties:

PropertyValueReference
BA (Bioavailability) 75 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1.41 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 8.92 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.90 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 0.10 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
June 11, 1970 FDA AKORN INC

FDA Adverse Event Reporting System (Female)

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
Anaphylactic shock 164.34 34.17 49 1690 23584 63463699
Oliguria 95.27 34.17 26 1713 9075 63478208
Acute kidney injury 66.66 34.17 56 1683 263359 63223924
Cardiac arrest 49.39 34.17 31 1708 92514 63394769
Torsade de pointes 44.89 34.17 16 1723 13335 63473948
Apnoea 44.44 34.17 14 1725 8008 63479275
Dystonia 44.36 34.17 16 1723 13803 63473480
Drug reaction with eosinophilia and systemic symptoms 42.47 34.17 20 1719 33816 63453467
Haematuria 42.11 34.17 19 1720 29138 63458145
Skin depigmentation 37.47 34.17 8 1731 991 63486292
Drug hypersensitivity 37.17 34.17 44 1695 310643 63176640
Allergy test negative 35.89 34.17 6 1733 198 63487085
Tachycardia 35.83 34.17 28 1711 118128 63369155
Drug interaction 35.20 34.17 37 1702 229094 63258189

FDA Adverse Event Reporting System (Male)

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
Anaphylactic shock 94.03 39.58 28 782 15913 34940208

FDA Adverse Event Reporting System (Geriatric)

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
Anaphylactic shock 244.11 29.35 76 2494 35920 79705898
Oliguria 68.34 29.35 24 2546 16285 79725533
Acute kidney injury 56.42 29.35 76 2494 519328 79222490
Anaphylactic reaction 47.53 29.35 31 2539 83712 79658106
Dystonia 41.46 29.35 18 2552 21381 79720437
Apnoea 40.66 29.35 15 2555 11689 79730129
Torsade de pointes 39.90 29.35 17 2553 19295 79722523
Cardiac arrest 38.96 29.35 37 2533 172059 79569759
Electrocardiogram QT prolonged 38.40 29.35 28 2542 90358 79651460
Drug reaction with eosinophilia and systemic symptoms 36.97 29.35 24 2546 64220 79677598
Neuromuscular block prolonged 35.92 29.35 8 2562 1022 79740796
Skin depigmentation 35.33 29.35 8 2562 1102 79740716
Drug hypersensitivity 32.70 29.35 44 2526 298872 79442946
Tachycardia 32.43 29.35 34 2536 177734 79564084
Allergy test negative 31.96 29.35 6 2564 328 79741490
Neuroleptic malignant syndrome 31.19 29.35 16 2554 27543 79714275
Drug interaction 30.90 29.35 51 2519 415132 79326686
Ventricular tachycardia 30.01 29.35 18 2552 41917 79699901

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AD08 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Butyrophenone derivatives
CHEBI has role CHEBI:48561 dopaminergic antagonists
CHEBI has role CHEBI:50919 antiemetico
CHEBI has role CHEBI:60807 anaesthestic adjuvant
CHEBI has role CHEBI:65190 typical antipsychotic drugs
MeSH PA D000759 Adjuvants, Anesthesia
MeSH PA D000932 Antiemetics
MeSH PA D014150 Antipsychotic 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
FDA MoA N0000175799 Dopamine D2 Antagonists
FDA EPC N0000175800 Dopamine-2 Receptor Antagonist

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Post-Operative Nausea and Vomiting indication 1488000
Intra-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
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:557
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
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




🐶 Veterinary Drug Use

SpeciesUseRelation
Dogs General anesthesia Indication
Dogs Analgesia and tranquilizers Indication

🐶 Veterinary products

ProductApplicantIngredients
Innovar-Vet Injection Intervet Inc. 2

Acid dissociation constants calculated using MoKa v3.0.0

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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 9.13 DRUG MATRIX CHEMBL
D(2) dopamine receptor GPCR ANTAGONIST Ki 9.60 PDSP CHEMBL
Alpha-2A adrenergic receptor GPCR Ki 5.95 DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 7.49 CHEMBL
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
D(4) dopamine receptor GPCR Ki 9.08 PDSP
Alpha-1D adrenergic receptor GPCR Ki 9.18 DRUG MATRIX
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel IC50 6.13 CHEMBL
D(1A) dopamine receptor GPCR Ki 6.26 DRUG MATRIX
Alpha-1B adrenergic receptor GPCR Ki 8.01 DRUG MATRIX
Membrane-associated progesterone receptor component 1 Membrane receptor Ki 5.70 DRUG MATRIX
Alpha-1A adrenergic receptor GPCR IC50 8.78 CHEMBL
5-hydroxytryptamine receptor 1A GPCR IC50 6.62 CHEMBL
5-hydroxytryptamine receptor 4 GPCR Ki 6.20 DRUG MATRIX

External reference:

IDSource
4019047 VUID
N0000147316 NUI
D00308 KEGG_DRUG
4019047 VANDF
C0013136 UMLSCUI
CHEBI:4717 CHEBI
USS PDB_CHEM_ID
CHEMBL1108 ChEMBL_ID
DB00450 DRUGBANK_ID
D004329 MESH_DESCRIPTOR_UI
3168 PUBCHEM_CID
7172 IUPHAR_LIGAND_ID
1609 INN_ID
O9U0F09D5X UNII
3648 RXNORM
2356 MMSL
3392 MMSL
4646 MMSL
d00219 MMSL
001517 NDDF
26574002 SNOMEDCT_US
387146001 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
DROPERIDOL HUMAN PRESCRIPTION DRUG LABEL 1 0143-9514 INJECTION, SOLUTION 2.50 mg INTRAMUSCULAR ANDA 20 sections
DROPERIDOL HUMAN PRESCRIPTION DRUG LABEL 1 0143-9515 INJECTION, SOLUTION 2.50 mg INTRAMUSCULAR ANDA 20 sections
Droperidol HUMAN PRESCRIPTION DRUG LABEL 1 0517-9702 INJECTION, SOLUTION 2.50 mg INTRAMUSCULAR ANDA 21 sections
Droperidol HUMAN PRESCRIPTION DRUG LABEL 1 0517-9702 INJECTION, SOLUTION 2.50 mg INTRAMUSCULAR ANDA 21 sections