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pralidoxime 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2231 | 51-15-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Hosey CM, Chan R, Benet LZ |
| Vd (Volume of distribution) | 0.80 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 9 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 1 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.40 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 655 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BA (Bioavailability) | 25 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -1.535 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.661 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.557 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.262 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 88.230 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 92.610 | % | High | 1 |
| herg | hERG pIC50 | 4.339 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 2 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.076 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 72.180 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,IGF1R,ITK,JAK1,JAK2,JAK3,KIT,MAP2K6,MAP3K1,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAPK1,MAPK10,MAPK12,MAPK7,MAPK8,MAPK9,MAPKAPK2,MAPKAPK5,MARK4,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ZAP70 | 71 | |||
| kinase-selectivity-class | ACVR2A,ACVR2B,AURKB,AXL,BRAF,CDK4,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,JAK2,MAP2K3,MAP2K4,MAP2K6,MAP3K14,MAPK12,MAPK7,MAPK8,SIK2,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 | 28 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 0.433 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.649 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 3.532 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 96.610 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.587 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 93.880 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.042 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 2.624 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 95.880 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 84.390 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 931.108 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 11, 1964 | FDA | BAXTER HLTHCARE CORP |
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)
| 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 |
|---|---|---|---|---|---|---|
| Bronchial secretion retention | 25.40 | 24.17 | 3 | 3 | 3 | 113944 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | V03AB04 | VARIOUS ALL OTHER THERAPEUTIC PRODUCTS ALL OTHER THERAPEUTIC PRODUCTS Antidotes |
| ATC | V03AB54 | VARIOUS ALL OTHER THERAPEUTIC PRODUCTS ALL OTHER THERAPEUTIC PRODUCTS Antidotes |
| FDA MoA | N0000000080 | Cholinesterase Reactivators |
| MeSH PA | D000931 | Antidotes |
| MeSH PA | D002801 | Cholinesterase Reactivators |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018678 | Cholinergic Agents |
| MeSH PA | D020011 | Protective Agents |
| FDA EPC | N0000175742 | Cholinesterase Reactivator |
| CHEBI has role | CHEBI:38323 | cholinergic drug |
| CHEBI has role | CHEBI:50241 | cholinesterase reactivator |
| CHEBI has role | CHEBI:90753 | antidote to organophosphate poisoning |
| CHEBI has role | CHEBI:136860 | antidote to sarin poisoning |
| CHEBI has role | CHEBI:50247 | antidote |
Related Drugs by ATC class:
V03AB Antidotes 28 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Organophosphate poisoning | indication | 8260003 | |
| Poisoning due to Nerve Agent | indication | ||
| Cholinesterase Inhibitors Toxicity | indication | ||
| Organophosphorous Overdose | indication | ||
| Atrial flutter | contraindication | 5370000 | |
| Chronic obstructive lung disease | contraindication | 13645005 | DOID:3083 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Heart disease | contraindication | 56265001 | DOID:114 |
| Acute nephropathy | contraindication | 58574008 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Pyloric obstruction | contraindication | 244815007 | |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
| Myocardial infarction in recovery phase | contraindication | 418044006 |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Cats | Poisoning caused by pesticides and chemicals of the organophosphate class which have anticholinesterase activity | Indication |
| Dogs | Poisoning caused by pesticides and chemicals of the organophosphate class which have anticholinesterase activity | Indication |
| Horses | Poisoning caused by pesticides and chemicals of the organophosphate class which have anticholinesterase activity | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| Protopam | Zoetis Inc. | 1 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.87 | acidic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Acetylcholinesterase | Enzyme | ACTIVATOR | Kd | 4.59 | CHEMBL | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D00469 | KEGG_DRUG |
| 94-63-3 | SECONDARY_CAS_RN |
| 14018-50-9 | SECONDARY_CAS_RN |
| 4018484 | VANDF |
| 4019900 | VANDF |
| C0071808 | UMLSCUI |
| CHEBI:8354 | CHEBI |
| CHEMBL1420 | ChEMBL_ID |
| DB00733 | DRUGBANK_ID |
| CHEMBL14577 | ChEMBL_ID |
| CHEMBL748 | ChEMBL_ID |
| 135398747 | PUBCHEM_CID |
| C028797 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7597 | IUPHAR_LIGAND_ID |
| P7MU9UTP52 | UNII |
| 34345 | RXNORM |
| 5339 | MMSL |
| d01409 | MMSL |
| 001095 | NDDF |
| 004542 | NDDF |
| 007941 | NDDF |
| 1186942004 | SNOMEDCT_US |
| 17356001 | SNOMEDCT_US |
| 387527005 | SNOMEDCT_US |
| 922004 | SNOMEDCT_US |
| 851 | INN_ID |
| 25615-00-3 | SECONDARY_CAS_RN |
| P7MU9UTP52 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Protopam Chloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60977-141 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 1 g | INTRAVENOUS | NDA | 26 sections |