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sulfafurazole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| anti-infectives, sulfonamides | 2529 | 127-69-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A short-acting sulfonamide antibacterial with activity against a wide range of gram- negative and gram-positive organisms.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 4 | g | O |
| 4 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 4 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.13 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 49 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 249.52 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 96 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.17 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 0.30 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.08 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 7.40 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -0.876 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 2.153 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 9.954 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 2.153 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 13.200 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 18.780 | % | High | 1 |
| herg | hERG pIC50 | 4.158 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.253 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.221 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 8.360 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,IKBKB,ITK,JAK1,JAK2,KIT,MAP2K6,MAP3K1,MAP3K21,MAP3K7,MAPK1,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MAPKAPK5,MARK4,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1,ZAP70 | 59 | |||
| kinase-selectivity-class | ACVR2A,AURKA,AURKB,AXL,CAMK2D,CDK9,DDR1,DYRK1B,EPHB4,ERBB2,FGFR1,FLT3,GRK2,IKBKB,JAK1,JAK2,MAP2K3,MAP2K6,MAP3K1,MAP3K21,MAP3K7,MAP4K1,MAPK12,MAPK7,MARK4,MTOR,NTRK3,PDK2,PDK4,PIK3CB,PRKDC,SGK1,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1,ULK2 | 40 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 2.655 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.607 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 7.178 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 26.640 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.798 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 11.200 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.052 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 2.183 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 90.980 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 4.860 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 968.278 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 7, 1971 | FDA | ALRA |
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 | J01EB05 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE SULFONAMIDES AND TRIMETHOPRIM Short-acting sulfonamides |
| ATC | S01AB02 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIINFECTIVES Sulfonamides |
| FDA CS | M0020790 | Sulfonamides |
| FDA EPC | N0000175504 | Sulfonamide Antimicrobial |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| MeSH PA | D000977 | Antiparasitic Agents |
| MeSH PA | D000981 | Antiprotozoal Agents |
| MeSH PA | D003049 | Coccidiostats |
| CHEBI has role | CHEBI:36047 | antibacterial drug |
| CHEBI has role | CHEBI:33282 | antibacterial agent |
| CHEBI has role | CHEBI:66981 | ophthalmology drug |
| CHEBI has role | CHEBI:88188 | drug allergen |
Related Drugs by ATC class:
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 |
|---|---|---|---|
| Trachoma | indication | 2576002 | DOID:11265 |
| Acute otitis media | indication | 3110003 | |
| Haemophilus Influenzae Acute Otitis Media | indication | 19021002 | |
| Nocardiosis | indication | 29227009 | DOID:2312 |
| Falciparum malaria | indication | 62676009 | DOID:14067 |
| Urinary tract infectious disease | indication | 68566005 | |
| Urethritis due to Chlamydia trachomatis | indication | 179101003 | |
| Meningococcal meningitis | indication | 192644005 | |
| Chlamydial conjunctivitis | indication | 231861005 | DOID:13800 |
| Chancroid | indication | 266143009 | DOID:13778 |
| Infective otitis media | indication | 312218008 | |
| Pneumococcal Acute Otitis Media | indication | ||
| Chlamydia Cervicitis | indication | ||
| Lymphogranuloma venereum | off-label use | 186946009 | DOID:13819 |
| Urinary tract obstruction | contraindication | 7163005 | DOID:5200 |
| Torsades de pointes | contraindication | 31722008 | |
| Glomerulonephritis | contraindication | 36171008 | DOID:2921 |
| Acute hepatitis | contraindication | 37871000 | |
| Third trimester pregnancy | contraindication | 41587001 | |
| Uremia | contraindication | 44730006 | DOID:4676 |
| Megaloblastic anemia due to folate deficiency | contraindication | 85649008 | DOID:14026 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Myasthenia gravis | contraindication | 91637004 | DOID:437 |
| Cholestatic hepatitis | contraindication | 95556007 | |
| Anemia due to enzyme deficiency | contraindication | 111577008 | |
| Prolonged QT interval | contraindication | 111975006 | |
| Deficiency of glucose-6-phosphate dehydrogenase | contraindication | 124134002 | DOID:2862 |
| Gastrointestinal obstruction | contraindication | 126765001 | |
| Hearing disorder | contraindication | 128540005 | |
| Liver function tests abnormal | contraindication | 166603001 | |
| Disease of blood AND/OR blood-forming organ | contraindication | 191124002 | DOID:74 |
| Asthma | contraindication | 195967001 | DOID:2841 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
| Aplastic anemia | contraindication | 306058006 | DOID:12449 |
| Pseudomembranous enterocolitis | contraindication | 397683000 | |
| Porphyria | contraindication | 418470004 | |
| Slow acetylator due to N-acetyltransferase enzyme variant | contraindication | 425079005 | |
| Congenital long QT syndrome | contraindication | 442917000 |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Cats | Bacterial pneumonia | Indication |
| Cats | Bacterial enteritis | Indication |
| Dogs | Bacterial pneumonia | Indication |
| Dogs | Bacterial enteritis | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| Soxisol Tablets | Zoetis Inc. | 1 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 5.0 | acidic |
| pKa2 | 2.08 | 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 H4 receptor | GPCR | IC50 | 5.55 | WOMBAT-PK | |||||
| Endothelin-1 receptor | GPCR | IC50 | 6.11 | CHEMBL | |||||
| Endothelin B receptor | GPCR | IC50 | 4.62 | CHEMBL | |||||
| Dihydropteroate synthase | Enzyme | INHIBITOR | DRUGBANK | CHEMBL | |||||
| Dihydroorotate dehydrogenase (quinone), mitochondrial | Enzyme | WOMBAT-PK | |||||||
| Endothelin-1 receptor | GPCR | IC50 | 6.11 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4017767 | VUID |
| N0000178993 | NUI |
| D00450 | KEGG_DRUG |
| 4017765 | VANDF |
| 4017767 | VANDF |
| C0038745 | UMLSCUI |
| CHEBI:102484 | CHEBI |
| CHEMBL453 | ChEMBL_ID |
| CHEMBL1200321 | ChEMBL_ID |
| DB00263 | DRUGBANK_ID |
| 4299-60-9 | SECONDARY_CAS_RN |
| 5344 | PUBCHEM_CID |
| 10207 | RXNORM |
| 5531 | MMSL |
| 5533 | MMSL |
| 7990 | MMSL |
| d00120 | MMSL |
| 002818 | NDDF |
| 002820 | NDDF |
| 108866009 | SNOMEDCT_US |
| 372858002 | SNOMEDCT_US |
| 80732005 | SNOMEDCT_US |
| D013444 | MESH_DESCRIPTOR_UI |
| D013411 | MESH_DESCRIPTOR_UI |
| 4177 | INN_ID |
| 12700 | IUPHAR_LIGAND_ID |
| 740T4C525W | UNII |
Pharmaceutical products:
None