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methdilazine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1742 | 1982-37-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 16 | mg | O |
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.231 | High | 0.84 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.855 | High | 0.84 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 25.410 | 10^-6 cm/s | High | 0.84 |
| dh-clint | Dog hepatocyte intrinsic clearance | 154.170 | uL/min/10^6 cells | High | 0.84 |
| dppb | Dog plasma protein binding (% unbound) | 4.680 | % | High | 0.84 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 9.920 | % | High | 0.84 |
| herg | hERG pIC50 | 5.734 | pIC50 | High | 0.84 |
| hh-clint | Human hepatocyte intrinsic clearance | 18.239 | uL/min/10^6 cells | High | 0.84 |
| hlm-clint | Human liver microsomal intrinsic clearance | 24.774 | uL/min/mg protein | High | 0.84 |
| hppb | Human plasma protein binding (% unbound) | 6.700 | % | High | 0.84 |
| kinase-safety-class | ACVR2B,AKT2,AXL,BRAF,CAMK2B,CAMK2D,CDK5,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAP3K7,MAPK10,MAPK12,MET,NTRK2,PDK2,PDK4,PIM2,PRKDC | 21 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 0.587 | High | 0.84 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.028 | High | 0.84 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 246.604 | High | 0.84 | |
| mppb | Mouse plasma protein binding (% unbound) | 9.420 | High | 0.84 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 5.117 | High | 0.84 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 21.590 | % | High | 0.84 |
| rat-kpuu-brain | Rat brain Kpuu | 0.334 | % | High | 0.84 |
| rh-clint | Rat hepatocyte intrinsic clearance | 433.511 | uL/min/10^6 cells | High | 0.84 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 40.840 | % | High | 0.84 |
| rppb | Rat plasma protein binding (% unbound) | 11.110 | % | High | 0.84 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 944.061 | uM | High | 0.84 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| None | FDA | WESTWOOD SQUIBB |
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 | R06AD04 | RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Phenothiazine derivatives |
| CHEBI has role | CHEBI:37956 | histamine antagonist |
| CHEBI has role | CHEBI:48873 | cholinergic antagonist |
| CHEBI has role | CHEBI:59683 | antipruritic drug |
Related Drugs by ATC class:
R06AD Phenothiazine derivatives 8 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Dermatographic urticaria | indication | 7632005 | DOID:743 |
| Angioedema | indication | 41291007 | DOID:1558 |
| General anesthesia | indication | 50697003 | |
| Allergic rhinitis | indication | 61582004 | |
| Nasal discharge | indication | 64531003 | |
| Nasal congestion | indication | 68235000 | |
| Sneezing | indication | 76067001 | |
| Urticaria | indication | 126485001 | |
| Itching of skin | indication | 418363000 | |
| Allergic conjunctivitis | indication | 473460002 | DOID:11204 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.18 | Basic |
| pKa2 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Histamine H1 receptor | GPCR | ANTAGONIST | CHEMBL | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019825 | VUID |
| N0000147914 | NUI |
| D04979 | KEGG_DRUG |
| 4018666 | VANDF |
| 4019825 | VANDF |
| C0066101 | UMLSCUI |
| CHEBI:6823 | CHEBI |
| CHEMBL1200959 | ChEMBL_ID |
| DB00902 | DRUGBANK_ID |
| CHEMBL1200532 | ChEMBL_ID |
| C044642 | MESH_SUPPLEMENTAL_RECORD_UI |
| 14677 | PUBCHEM_CID |
| 7231 | IUPHAR_LIGAND_ID |
| 879 | INN_ID |
| 1229-35-2 | SECONDARY_CAS_RN |
| 4Q13LY9Z8X | UNII |
| 29648 | RXNORM |
| 5068 | MMSL |
| d00789 | MMSL |
| 001538 | NDDF |
| 004618 | NDDF |
| 18462008 | SNOMEDCT_US |
| 400745007 | SNOMEDCT_US |
| 47176005 | SNOMEDCT_US |
| 4Q13LY9Z8X | INXIGHT DRUGS |
Pharmaceutical products:
None