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sulfamethizole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| anti-infectives, sulfonamides | 2512 | 144-82-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A sulfathiazole antibacterial agent.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 4 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 4 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.61 mg/mL | Bocci G, Oprea TI, Benet LZ |
| EoM (Fraction excreted unchanged in urine) | 86 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 211.38 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -1.051 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 7.145 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 6.353 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.811 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 18.460 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 23.770 | % | High | 1 |
| herg | hERG pIC50 | 4 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.466 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.105 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 8.060 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,ALK,AURKA,AURKB,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,ITK,JAK1,JAK2,KIT,MAP2K6,MAP3K1,MAP3K21,MAP3K7,MAP4K1,MAPK7,MAPK9,MARK4,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 | 54 | |||
| kinase-selectivity-class | ACVR2A,AURKA,AXL,CDK9,DDR1,DYRK1B,ERBB2,GRK2,MAP2K3,MAP2K6,MAP3K7,MAPK7,MARK4,PDK4,PRKDC,SGK1,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 | 23 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.388 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 2.838 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 33.950 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.611 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 14.180 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 1.832 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 92.370 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 5.730 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 1002.305 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 28, 1953 | FDA |
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 |
|---|---|---|---|---|---|---|
| Humidity intolerance | 48.54 | 44.77 | 8 | 1468 | 412 | 90626559 |
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 |
|---|---|---|---|---|---|---|
| Microsporidia infection | 66.54 | 49.79 | 12 | 1321 | 1427 | 110586539 |
| Polymyositis | 55.21 | 49.79 | 12 | 1321 | 3696 | 110584270 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | B05CA04 | BLOOD AND BLOOD FORMING ORGANS BLOOD SUBSTITUTES AND PERFUSION SOLUTIONS IRRIGATING SOLUTIONS Antiinfectives |
| ATC | D06BA04 | DERMATOLOGICALS ANTIBIOTICS AND CHEMOTHERAPEUTICS FOR DERMATOLOGICAL USE CHEMOTHERAPEUTICS FOR TOPICAL USE Sulfonamides |
| ATC | J01EB02 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE SULFONAMIDES AND TRIMETHOPRIM Short-acting sulfonamides |
| ATC | S01AB01 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIINFECTIVES Sulfonamides |
| MeSH PA | D000890 | Anti-Infective Agents |
| CHEBI has role | CHEBI:33281 | antimicrobial agent |
| CHEBI has role | CHEBI:33282 | antibacterial agent |
| CHEBI has role | CHEBI:35441 | antiinfective agent |
| CHEBI has role | CHEBI:50502 | EC 2.5.1.15 (dihydropteroate synthase) inhibitor |
| CHEBI has role | CHEBI:66981 | ophthalmology drug |
| CHEBI has role | CHEBI:88188 | drug allergen |
Related Drugs by ATC class:
B05CA Antiinfectives 8 drugs
D06BA Sulfonamides 5 drugs
J01EB Short-acting sulfonamides 7 drugs
S01AB Sulfonamides 4 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Acute otitis media | indication | 3110003 | |
| Haemophilus Influenzae Acute Otitis Media | indication | 19021002 | |
| Shigellosis | indication | 36188001 | |
| Klebsiella cystitis | indication | 60867007 | |
| Escherichia coli urinary tract infection | indication | 301011002 | |
| Proteus urinary tract infection | indication | 301012009 | |
| Bacterial urinary infection | indication | 312124009 | |
| Infective otitis media | indication | 312218008 | |
| Pneumocystosis jiroveci pneumonia | indication | 415125002 | DOID:11339 |
| Pneumocystis Carinii Pneumonia Prevention | indication | ||
| Morganella Morganii Urinary Tract Infection | indication | ||
| Streptococcus Pneumoniae Chronic Bronchitis | indication | ||
| Haemophilus Influenzae Chronic Bronchitis | indication | ||
| Renal tubular acidosis | contraindication | 1776003 | DOID:14219 |
| Respiratory acidosis | contraindication | 12326000 | |
| Hyperkalemia | contraindication | 14140009 | |
| Metabolic acidosis, normal anion gap, acidifying salts | contraindication | 18104000 | |
| Glomerulonephritis | contraindication | 36171008 | DOID:2921 |
| Acute hepatitis | contraindication | 37871000 | |
| Diabetes mellitus type 2 | contraindication | 44054006 | DOID:9352 |
| Uremia | contraindication | 44730006 | DOID:4676 |
| Diabetes mellitus type 1 | contraindication | 46635009 | DOID:9744 |
| Acute nephropathy | contraindication | 58574008 | |
| Hepatic failure | contraindication | 59927004 | |
| Decreased respiratory function | contraindication | 80954004 | |
| Hyponatremia | contraindication | 89627008 | |
| Gout | contraindication | 90560007 | DOID:13189 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Anemia due to enzyme deficiency | contraindication | 111577008 | |
| Deficiency of glucose-6-phosphate dehydrogenase | contraindication | 124134002 | DOID:2862 |
| Disease of blood AND/OR blood-forming organ | contraindication | 191124002 | DOID:74 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Disorder of electrolytes | contraindication | 237840007 | |
| Pregnancy, function | contraindication | 289908002 | |
| Primary adrenocortical insufficiency | contraindication | 373662000 | |
| Pseudomembranous enterocolitis | contraindication | 397683000 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Recurrent Calcium Renal Calculi | contraindication |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Cats | Urinary tract infections | Indication |
| Cats | Management of complications resulting from surgical manipulations of the urinary tract | Indication |
| Dogs | Urinary tract infections | Indication |
| Dogs | Management of complications resulting from surgical manipulations of the urinary tract | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| Mesulfin Tablets | Zoetis Inc. | 2 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 5.34 | acidic |
| pKa2 | 2.81 | Basic |
| pKa3 | 2.17 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Dihydropteroate synthase | Enzyme | INHIBITOR | WOMBAT-PK | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4018493 | VUID |
| N0000146815 | NUI |
| D00870 | KEGG_DRUG |
| 4018493 | VANDF |
| C0038687 | UMLSCUI |
| CHEBI:9331 | CHEBI |
| CHEMBL1191 | ChEMBL_ID |
| DB00576 | DRUGBANK_ID |
| D013419 | MESH_DESCRIPTOR_UI |
| 5328 | PUBCHEM_CID |
| 12683 | IUPHAR_LIGAND_ID |
| 529 | INN_ID |
| 25W8454H16 | UNII |
| 10179 | RXNORM |
| 5525 | MMSL |
| d01090 | MMSL |
| 002822 | NDDF |
| 387389006 | SNOMEDCT_US |
| 70254000 | SNOMEDCT_US |
Pharmaceutical products:
None