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perazine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2100 | 84-97-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A phenothiazine antipsychotic with actions and uses similar to those of CHLORPROMAZINE. Extrapyramidal symptoms may be more common than other side effects.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | g | O |
| 0.10 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 3 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.914 | High | 0.80 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.789 | High | 0.80 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 27.040 | 10^-6 cm/s | High | 0.80 |
| dh-clint | Dog hepatocyte intrinsic clearance | 50.466 | uL/min/10^6 cells | High | 0.80 |
| dppb | Dog plasma protein binding (% unbound) | 5.440 | % | High | 0.80 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 8.450 | % | High | 0.80 |
| herg | hERG pIC50 | 5.935 | pIC50 | High | 0.80 |
| hh-clint | Human hepatocyte intrinsic clearance | 12.162 | uL/min/10^6 cells | High | 0.80 |
| hlm-clint | Human liver microsomal intrinsic clearance | 57.943 | uL/min/mg protein | High | 0.80 |
| hppb | Human plasma protein binding (% unbound) | 4.520 | % | High | 0.80 |
| kinase-safety-class | ACVR2B,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPKAPK2,MET,MTOR,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1,TTK | 43 | |||
| kinase-selectivity-class | AXL,PDK4,SIK2 | 3 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.524 | High | 0.80 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 219.280 | High | 0.80 | |
| mppb | Mouse plasma protein binding (% unbound) | 7.760 | High | 0.80 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 5.395 | High | 0.80 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 17.550 | % | High | 0.80 |
| rh-clint | Rat hepatocyte intrinsic clearance | 264.241 | uL/min/10^6 cells | High | 0.80 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 33.390 | % | High | 0.80 |
| rppb | Rat plasma protein binding (% unbound) | 6.390 | % | High | 0.80 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 722.770 | uM | High | 0.80 |
Approvals:
None
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Disturbance in attention | 70.71 | 57.55 | 24 | 898 | 47085 | 90580440 |
| Psychomotor retardation | 65.41 | 57.55 | 14 | 908 | 4775 | 90622750 |
| Flat affect | 60.02 | 57.55 | 11 | 911 | 1700 | 90625825 |
| Vascular stent thrombosis | 57.87 | 57.55 | 10 | 912 | 1106 | 90626419 |
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Drug interaction | 79.56 | 53.20 | 59 | 1353 | 500124 | 110087763 |
| Psychomotor retardation | 60.42 | 53.20 | 15 | 1397 | 7777 | 110580110 |
| Disturbance in attention | 58.87 | 53.20 | 24 | 1388 | 61971 | 110525916 |
| Anhedonia | 54.64 | 53.20 | 16 | 1396 | 15412 | 110572475 |
| Flat affect | 53.32 | 53.20 | 11 | 1401 | 2494 | 110585393 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N05AB10 | NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Phenothiazines with piperazine structure |
| 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:35469 | antidepressant |
| CHEBI has role | CHEBI:35474 | anxiolytic drug |
| CHEBI has role | CHEBI:35476 | antipsychotic agent |
| CHEBI has role | CHEBI:37930 | phenothiazine antipsychotic drug |
| CHEBI has role | CHEBI:48561 | dopaminergic antagonist |
Related Drugs by ATC class:
N05AB Phenothiazines with piperazine structure 9 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Ascariasis | indication | 2435008 | DOID:456 |
| Nausea and vomiting | indication | 16932000 | |
| Anxiety | indication | 48694002 | |
| Schizophrenia | indication | 58214004 | DOID:5419 |
| Chemotherapy-induced nausea and vomiting | indication | 236084000 | |
| Enterobiasis | indication | 266162007 | |
| Vomiting | indication | 422400008 | |
| Nausea | indication | 422587007 | |
| Nonpsychotic Anxiety | indication | ||
| Prolonged-Severe Nausea and Vomiting | indication | ||
| Brain damage | contraindication | 2470005 | |
| Tachyarrhythmia | contraindication | 6285003 | |
| Urinary tract obstruction | contraindication | 7163005 | DOID:5200 |
| Alcoholism | contraindication | 7200002 | |
| Organophosphate poisoning | contraindication | 8260003 | |
| Weight gain finding | contraindication | 8943002 | |
| Severe chronic ulcerative colitis | contraindication | 14311001 | |
| Neuroleptic malignant syndrome | contraindication | 15244003 | DOID:14464 |
| Senile dementia | contraindication | 15662003 | |
| Chronic disease of respiratory system | contraindication | 17097001 | |
| Cirrhosis of liver | contraindication | 19943007 | DOID:5082 |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Glaucoma | contraindication | 23986001 | DOID:1686 |
| Toxic megacolon | contraindication | 28536002 | DOID:1770 |
| Orthostatic hypotension | contraindication | 28651003 | |
| Atony of colon | contraindication | 29479008 | |
| Retinal disorder | contraindication | 29555009 | DOID:5679 |
| Torsades de pointes | contraindication | 31722008 | |
| Parkinsonism | contraindication | 32798002 | |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Complete trisomy 21 syndrome | contraindication | 41040004 | DOID:14250 |
| Alcoholic liver damage | contraindication | 41309000 | |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Low blood pressure | contraindication | 45007003 | |
| Achalasia of esophagus | contraindication | 45564002 | DOID:9164 |
| Chronic heart failure | contraindication | 48447003 | |
| Bradycardia | contraindication | 48867003 | |
| Paralytic ileus | contraindication | 55525008 | DOID:8442 |
| Peptic reflux disease | contraindication | 57643001 | |
| Ulcerative colitis | contraindication | 64766004 | DOID:8577 |
| Drug AND/OR toxin-induced diarrhea | contraindication | 65979008 | |
| Extrapyramidal disease | contraindication | 76349003 | |
| Chronic hepatitis | contraindication | 76783007 | DOID:2237 |
| Spastic paralysis | contraindication | 78403003 | |
| Disturbance of salivary secretion | contraindication | 78948009 | |
| Hyperglycemia | contraindication | 80394007 | DOID:4195 |
| Hiatal hernia | contraindication | 84089009 | DOID:12642 |
| Epilepsy | contraindication | 84757009 | DOID:1826 |
| Leukopenia | contraindication | 84828003 | DOID:615 |
| Stupor | contraindication | 89458003 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Myasthenia gravis | contraindication | 91637004 | DOID:437 |
| Tardive dyskinesia | contraindication | 102449007 | |
| Prolonged QT interval | contraindication | 111975006 | |
| Diminished sweating | contraindication | 111980002 | |
| Gastrointestinal obstruction | contraindication | 126765001 | |
| Acute disease of cardiovascular system | contraindication | 128487001 | |
| Autonomic dysreflexia | contraindication | 129618003 | |
| Bleeding | contraindication | 131148009 | |
| Angina pectoris | contraindication | 194828000 | |
| Myocardial dysfunction | contraindication | 233928007 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Bladder outflow obstruction | contraindication | 236645006 | |
| Metabolic syndrome X | contraindication | 237602007 | DOID:14221 |
| Hyperprolactinemia | contraindication | 237662005 | DOID:12700 |
| Pyloric obstruction | contraindication | 244815007 | |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Retention of urine | contraindication | 267064002 | |
| Anemia | contraindication | 271737000 | DOID:2355 |
| Drowsy | contraindication | 271782001 | |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
| Coma | contraindication | 371632003 | |
| At risk for aspiration | contraindication | 371736008 | |
| Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
| Visual impairment | contraindication | 397540003 | |
| Gastric ulcer | contraindication | 397825006 | DOID:10808 |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Chronic lung disease | contraindication | 413839001 | |
| Disorder of coronary artery | contraindication | 414024009 | |
| Myocardial ischemia | contraindication | 414795007 | DOID:3393 |
| Obesity | contraindication | 414916001 | DOID:9970 |
| Congenital long QT syndrome | contraindication | 442917000 | |
| Carcinoma of female breast | contraindication | 447782002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.74 | Basic |
| pKa2 | 4.74 | Basic |
| pKa3 | 3.55 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Lysine-specific histone demethylase 1A | Enzyme | IC50 | 6.04 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| N0000167278 | NUI |
| C0030969 | UMLSCUI |
| CHEMBL1697766 | ChEMBL_ID |
| DB12710 | DRUGBANK_ID |
| D010464 | MESH_DESCRIPTOR_UI |
| 4744 | PUBCHEM_CID |
| 8915147A2B | UNII |
| 8042 | RXNORM |
| 006779 | NDDF |
| 25002001 | SNOMEDCT_US |
| CHEBI:59118 | CHEBI |
| 8915147A2B | INXIGHT DRUGS |
Pharmaceutical products:
None