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acepromazine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 73 | 61-00-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Acepromazine, a phenothiazine derivatives, was first used in the 1950s in the treatment of PSYCHOSES. Now, it is commonly used as tranquilizer/sedative agent in dogs, cats, horses, and other animals. It is thought to block dopamine receptors in the brain or inhibit the activity of dopamine in other ways.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | g | O |
| 50 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 55 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.256 | Moderate | 0.71 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.662 | Moderate | 0.71 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 30.620 | 10^-6 cm/s | Moderate | 0.71 |
| herg | hERG pIC50 | 5.822 | pIC50 | Moderate | 0.71 |
| dh-clint | Dog hepatocyte intrinsic clearance | 191.867 | uL/min/10^6 cells | Moderate | 0.71 |
| dppb | Dog plasma protein binding (% unbound) | 18.190 | % | Moderate | 0.71 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 19.460 | % | Moderate | 0.71 |
| hh-clint | Human hepatocyte intrinsic clearance | 27.733 | uL/min/10^6 cells | Moderate | 0.71 |
| hlm-clint | Human liver microsomal intrinsic clearance | 36.898 | uL/min/mg protein | Moderate | 0.71 |
| hppb | Human plasma protein binding (% unbound) | 16.470 | % | Moderate | 0.71 |
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,AKT1,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,CSF1R,DDR1,DYRK1B,EIF2AK3,EPHA2,EPHB4,ERBB2,FLT3,GRK2,GSK3B,INSR,ITK,JAK1,JAK2,JAK3,KIT,MAP3K1,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MELK,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1,ULK2,ZAP70 | 67 | |||
| kinase-selectivity-class | EIF2AK3,PDK4,STK33,TEK,TTK | 5 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.714 | Moderate | 0.71 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 254.683 | Moderate | 0.71 | |
| mppb | Mouse plasma protein binding (% unbound) | 16.960 | Moderate | 0.71 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 2.188 | Moderate | 0.71 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | Moderate | 0.70 | |
| pppb | Pig plasma protein binding (% unbound) | 34.730 | % | Moderate | 0.71 |
| rh-clint | Rat hepatocyte intrinsic clearance | 261.216 | uL/min/10^6 cells | Moderate | 0.71 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 57.600 | % | Moderate | 0.71 |
| rppb | Rat plasma protein binding (% unbound) | 16 | % | Moderate | 0.71 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 855.067 | uM | Moderate | 0.71 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| None | FDA |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N05AA04 | NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Phenothiazines with aliphatic side-chain |
| MeSH PA | D002492 | Central Nervous System Depressants |
| 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 |
| CHEBI has role | CHEBI:35476 | antipsychotic agent |
| CHEBI has role | CHEBI:37930 | phenothiazine antipsychotic drug |
Related Drugs by ATC class:
N05AA Phenothiazines with aliphatic side-chain 6 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Cats | Control intractable animals during examination, treatment, grooming, x-ray and minor surgical procedures | Indication |
| Cats | Itching caused by skin irritation | Indication |
| Cats | Control vomiting associated with motion sickness | Indication |
| Dogs | Control intractable animals during examination, treatment, grooming, x-ray and minor surgical procedures | Indication |
| Dogs | Itching caused by skin irritation | Indication |
| Dogs | Control vomiting associated with motion sickness | Indication |
| Horses | Controll fractious animals during examination,treatment, loading and transportation | Indication |
| Horses | Local anesthesia for firing, castration, neurectomy, removal of skin tumors, ocular surgery and applying casts | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| PromAce Injectable | Boehringer lngelheim Animal Health USA Inc. | 1 |
| PromAce Tablets | Boehringer lngelheim Animal Health USA Inc. | 1 |
| Acepromazine Maleate Injection | Boehringer lngelheim Animal Health USA Inc. | 1 |
| PromAce | Boehringer lngelheim Animal Health USA Inc. | 1 |
| Acepromazine Maleate Injection | Elanco US Inc. | 1 |
| Acepromazine Maleate Injection | Boehringer lngelheim Animal Health USA Inc. | 1 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.04 | Basic |
| pKa2 | 1.82 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| D(1A) dopamine receptor | GPCR | ANTAGONIST | DRUGBANK | DRUGBANK | |||||
| D(2) dopamine receptor | GPCR | ANTAGONIST | DRUGBANK | DRUGBANK | |||||
| Major prion protein | Surface antigen | EC50 | 5.30 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| N0000167279 | NUI |
| D07065 | KEGG_DRUG |
| 627-70-3 | SECONDARY_CAS_RN |
| 1114057 | RXNORM |
| C0000959 | UMLSCUI |
| CHEBI:44932 | CHEBI |
| PMZ | PDB_CHEM_ID |
| CHEMBL39560 | ChEMBL_ID |
| D000075 | MESH_DESCRIPTOR_UI |
| DB01614 | DRUGBANK_ID |
| 667 | INN_ID |
| 54EJ303F0R | UNII |
| 6077 | PUBCHEM_CID |
| NOCODE | MMSL |
| CHEMBL1883146 | ChEMBL_ID |
| 3598-37-6 | SECONDARY_CAS_RN |
| 005220 | NDDF |
| 005221 | NDDF |
| 412076009 | SNOMEDCT_US |
| 96218000 | SNOMEDCT_US |
Pharmaceutical products:
None