droperidol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 3.019 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.811 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 27.040 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 14.689 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 9.320 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 24.280 % High 1
herg hERG pIC50 5.993 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 9.247 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 32.961 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 6.080 % High 1
kinase-safety-class ACVR2B,ALK,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,KIT,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MARK4,MET,NTRK2,PAK4,PDK1,PDK2,PDK4,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TTK 38
kinase-selectivity-class AXL,CAMK2D,EIF2AK3,GRK2,SIK2,STK33,TTK 7
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 3.177 High 1
mh-clint Mouse hepatocyte intrinsic clearance 63.680 High 1
mppb Mouse plasma protein binding (% unbound) 8.920 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 13.740 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 15.280 % High 1
rh-clint Rat hepatocyte intrinsic clearance 89.125 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 41.120 % High 1
rppb Rat plasma protein binding (% unbound) 7.650 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 18.493 uM High 1

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 232.04 36.04 69 2518 31548 90594312
Streptococcal sepsis 107.20 36.04 24 2563 3560 90622300
Pseudomonal sepsis 102.84 36.04 24 2563 4278 90621582
Restlessness 100.78 36.04 38 2549 35682 90590178
Nail bed inflammation 93.46 36.04 19 2568 1782 90624078
Oliguria 90.16 36.04 26 2561 10598 90615262
Nasal mucosal disorder 87.01 36.04 18 2569 1839 90624021
Vascular device infection 74.29 36.04 23 2564 11929 90613931
Varicose vein 71.49 36.04 20 2567 7307 90618553
Metastases to lymph nodes 70.58 36.04 22 2565 11667 90614193
Brain oedema 69.69 36.04 24 2563 17361 90608499
Candida infection 67.21 36.04 28 2559 34029 90591831
Acute kidney injury 66.35 36.04 62 2525 320325 90305535
Metastases to central nervous system 61.81 36.04 22 2565 17520 90608340
Paronychia 60.89 36.04 18 2569 7988 90617872
Anaphylactic reaction 60.09 36.04 35 2552 87489 90538371
Cardiac arrest 46.96 36.04 32 2555 104903 90520957
Anuria 46.27 36.04 17 2570 14801 90611059
Dystonia 44.17 36.04 17 2570 16802 90609058
Skin fissures 44.06 36.04 18 2569 20791 90605069
Altered state of consciousness 42.99 36.04 20 2567 31512 90594348
Torsade de pointes 42.22 36.04 16 2571 15166 90610694
Bronchospasm 40.75 36.04 17 2570 20692 90605168
Haematuria 38.06 36.04 19 2568 34918 90590942
Apnoea 37.73 36.04 13 2574 9401 90616459
Tachycardia 37.40 36.04 33 2554 157640 90468220
Drug reaction with eosinophilia and systemic symptoms 37.22 36.04 20 2567 42738 90583122
Lactic acidosis 36.79 36.04 21 2566 50442 90575418

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 158.94 40.17 47 1055 23470 42596763

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 371.69 32.87 115 3578 51431 110534175
Streptococcal sepsis 100.12 32.87 25 3668 5047 110580559
Nail bed inflammation 93.86 32.87 20 3673 2010 110583596
Nasal mucosal disorder 89.62 32.87 19 3674 1864 110583742
Anaphylactic reaction 87.95 32.87 52 3641 114248 110471358
Restlessness 87.49 32.87 41 3652 56218 110529388
Pseudomonal sepsis 85.78 32.87 25 3668 9021 110576585
Varicose vein 73.93 32.87 21 3672 6919 110578687
Vascular device infection 67.19 32.87 24 3669 16488 110569118
Metastases to lymph nodes 65.54 32.87 23 3670 15009 110570597
Oliguria 64.33 32.87 24 3669 18633 110566973
Acute kidney injury 59.00 32.87 88 3605 635342 109950264
Brain oedema 58.85 32.87 26 3667 31072 110554534
Paronychia 56.25 32.87 19 3674 11062 110574544
Metastases to central nervous system 56.20 32.87 23 3670 22794 110562812
Candida infection 53.78 32.87 28 3665 47981 110537625
Skin fissures 41.65 32.87 19 3674 24439 110561167
Dystonia 40.68 32.87 19 3674 25786 110559820
Electrocardiogram QT prolonged 39.15 32.87 31 3662 108929 110476677
Anuria 38.61 32.87 18 3675 24323 110561283
Local anaesthetic systemic toxicity 38.28 32.87 12 3681 5525 110580081
Apnoea 37.90 32.87 15 3678 13624 110571982
Drug interaction 37.63 32.87 63 3630 500120 110085486
Torsade de pointes 36.74 32.87 17 3676 22583 110563023
Cardio-respiratory arrest 35.41 32.87 30 3663 115806 110469800
Cardiac arrest 35.40 32.87 38 3655 196715 110388891
Bronchospasm 34.90 32.87 18 3675 30221 110555385
Lactic acidosis 34.62 32.87 27 3666 92784 110492822
Hepatic cytolysis 34.50 32.87 22 3671 55031 110530575
Neuromuscular block prolonged 34.12 32.87 8 3685 1239 110584367
Altered state of consciousness 33.58 32.87 22 3671 57604 110528002
Hypotension 32.94 32.87 61 3632 523788 110061818
Neuroleptic malignant syndrome 32.89 32.87 18 3675 34041 110551565

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AD08 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Butyrophenone derivatives
MeSH PA D000759 Adjuvants, Anesthesia
MeSH PA D000932 Antiemetics
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014150 Antipsychotic Agents
MeSH PA D015259 Dopamine Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018492 Dopamine Antagonists
MeSH PA D065127 Dopamine D2 Receptor Antagonists
CHEBI has role CHEBI:35480 analgesic
CHEBI has role CHEBI:48561 dopaminergic antagonist
CHEBI has role CHEBI:50919 antiemetic
CHEBI has role CHEBI:60807 anaesthesia adjuvant
CHEBI has role CHEBI:65190 first generation antipsychotic
FDA MoA N0000175799 Dopamine D2 Antagonists
FDA EPC N0000175800 Dopamine-2 Receptor Antagonist

Related Drugs by ATC class:

N05AD Butyrophenone derivatives 8 drugs
benperidolbromperidolhaloperidollumateperonemelperonemoperonepipamperonetrifluperidol

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
O9U0F09D5X INXIGHT DRUGS

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