Stem definition | Drug id | CAS RN |
---|---|---|
anti-infectives, sulfonamides | 2500 | 68-35-9 |
Dose | Unit | Route |
---|---|---|
0.60 | g | O |
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) | 57 % | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 684.95 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 90 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Vd (Volume of distribution) | 0.29 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 0.55 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.44 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 7 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Aug. 11, 1941 | FDA | LEDERLE |
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 hypersensitivity | 165.66 | 34.81 | 96 | 1309 | 250914 | 50352805 |
Lipase increased | 155.67 | 34.81 | 38 | 1367 | 8503 | 50595216 |
Pancreatitis | 99.02 | 34.81 | 39 | 1366 | 42575 | 50561144 |
Drug reaction with eosinophilia and systemic symptoms | 95.13 | 34.81 | 34 | 1371 | 28390 | 50575329 |
Pancytopenia | 44.15 | 34.81 | 28 | 1377 | 84002 | 50519717 |
Astigmatism | 43.26 | 34.81 | 9 | 1396 | 972 | 50602747 |
Pneumonia aspiration | 37.69 | 34.81 | 18 | 1387 | 30986 | 50572733 |
Hepatocellular injury | 37.56 | 34.81 | 17 | 1388 | 25930 | 50577789 |
Coma | 35.05 | 34.81 | 21 | 1384 | 56858 | 50546861 |
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 |
---|---|---|---|---|---|---|
Toxic epidermal necrolysis | 81.03 | 30.52 | 30 | 1223 | 18123 | 29555151 |
Stevens-Johnson syndrome | 44.58 | 30.52 | 19 | 1234 | 16478 | 29556796 |
Cerebral toxoplasmosis | 36.19 | 30.52 | 9 | 1244 | 1407 | 29571867 |
Central pain syndrome | 32.02 | 30.52 | 5 | 1248 | 67 | 29573207 |
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 reaction with eosinophilia and systemic symptoms | 98.09 | 27.76 | 45 | 2302 | 54172 | 64442213 |
Toxic epidermal necrolysis | 67.64 | 27.76 | 31 | 2316 | 37135 | 64459250 |
Pancytopenia | 64.15 | 27.76 | 48 | 2299 | 143261 | 64353124 |
Cerebral toxoplasmosis | 45.29 | 27.76 | 11 | 2336 | 1815 | 64494570 |
Drug hypersensitivity | 43.22 | 27.76 | 48 | 2299 | 237767 | 64258618 |
Astigmatism | 39.81 | 27.76 | 9 | 2338 | 1089 | 64495296 |
Hepatocellular injury | 31.67 | 27.76 | 20 | 2327 | 45215 | 64451170 |
Pulmonary venous thrombosis | 30.53 | 27.76 | 5 | 2342 | 108 | 64496277 |
Infection protozoal | 30.26 | 27.76 | 4 | 2343 | 17 | 64496368 |
None
Source | Code | Description |
---|---|---|
ATC | J01EC02 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE SULFONAMIDES AND TRIMETHOPRIM Intermediate-acting sulfonamides |
ATC | J01EE02 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE SULFONAMIDES AND TRIMETHOPRIM Combinations of sulfonamides and trimethoprim, incl. derivatives |
ATC | J01EE06 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE SULFONAMIDES AND TRIMETHOPRIM Combinations of sulfonamides and trimethoprim, incl. derivatives |
FDA CS | M0020790 | Sulfonamides |
FDA EPC | N0000175503 | Sulfonamide Antibacterial |
MeSH PA | D000900 | Anti-Bacterial Agents |
MeSH PA | D000890 | Anti-Infective Agents |
MeSH PA | D000977 | Antiparasitic Agents |
MeSH PA | D000981 | Antiprotozoal Agents |
MeSH PA | D003049 | Coccidiostats |
CHEBI has role | CHEBI:33281 | antibiotics |
CHEBI has role | CHEBI:35441 | antiinfective agents |
CHEBI has role | CHEBI:35703 | Xenobiotic |
CHEBI has role | CHEBI:35818 | coccidiostats |
CHEBI has role | CHEBI:35820 | antiprotozoal drugs |
CHEBI has role | CHEBI:50502 | dihydropteroate synthase inhibitors |
CHEBI has role | CHEBI:74234 | sepiapterin reductase inhibitors |
CHEBI has role | CHEBI:78298 | environmental contaminants |
CHEBI has role | CHEBI:88188 | allergenic drug |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Chorioretinitis | indication | 46627006 | DOID:8886 |
Skin ulcer | indication | 46742003 | |
Ulcerative colitis | indication | 64766004 | DOID:8577 |
Congenital toxoplasmosis | indication | 73893000 | DOID:13336 |
Toxoplasmosis | indication | 187192000 | DOID:9965 |
Toxoplasmosis associated with acquired immunodeficiency syndrome | indication | 421666009 | |
Rheumatic Fever Prevention | indication | ||
Burn Wound Infections | indication | ||
Encephalitis due to Toxoplasmosis | indication | ||
Minor Bacterial Skin Infections | indication | ||
Collagenous colitis | off-label use | 19311003 | DOID:0060183 |
Psoriasis with arthropathy | off-label use | 33339001 | |
Crohn's disease | off-label use | 34000006 | |
Rheumatoid arthritis | off-label use | 69896004 | DOID:7148 |
Systemic sclerosis | off-label use | 89155008 | DOID:418 |
Juvenile rheumatoid arthritis | off-label use | 410795001 | |
Toxoplasmosis Prevention | off-label use | ||
Urinary tract obstruction | contraindication | 7163005 | DOID:5200 |
Third trimester pregnancy | contraindication | 41587001 | |
Leukopenia | contraindication | 84828003 | DOID:615 |
Megaloblastic anemia due to folate deficiency | contraindication | 85649008 | DOID:14026 |
Kidney disease | contraindication | 90708001 | DOID:557 |
Anemia due to enzyme deficiency | contraindication | 111577008 | |
Deficiency of glucose-6-phosphate dehydrogenase | contraindication | 124134002 | DOID:2862 |
Gastrointestinal obstruction | contraindication | 126765001 | |
Disease of blood AND/OR blood-forming organ | contraindication | 191124002 | DOID:74 |
Superimposed infection | contraindication | 193198003 | |
Asthma | contraindication | 195967001 | DOID:2841 |
Disease of liver | contraindication | 235856003 | DOID:409 |
Anemia | contraindication | 271737000 | DOID:2355 |
Pregnancy, function | contraindication | 289908002 | |
Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
Aplastic anemia | contraindication | 306058006 | DOID:12449 |
Breastfeeding (mother) | contraindication | 413712001 | |
Porphyria | contraindication | 418470004 | |
Slow acetylator due to N-acetyltransferase enzyme variant | contraindication | 425079005 |
Species | Use | Relation |
---|---|---|
Dogs | Systemic antibacterial action against sensitive organisms to surgery | Indication |
Dogs | Systemic antibacterial action against sensitive organisms to debridement | Indication |
Dogs | Control of bacterial infection during the treatment of acute urinary tract infections | Indication |
Dogs | Control of bacterial infection during the treatment of acute bacterial complications of distemper | Indication |
Dogs | Control of bacterial infection during the treatment of acute respiratory tract infections | Indication |
Dogs | Control of bacterial infection during the treatment of acute alimentary tract infections | Indication |
Dogs | Control of bacterial infection during the treatment of wound infections | Indication |
Dogs | Control of bacterial infection during the treatment of abscesses | Indication |
Horses | Systemic antibacterial action against sensitive organisms during treatment of acute strangles | Indication |
Horses | Systemic antibacterial action against sensitive organisms during respiratory infections | Indication |
Horses | Systemic antibacterial action against sensitive organisms during acute urogenital infections | Indication |
Horses | Systemic antibacterial action against sensitive organisms during wound infections | Indication |
Horses | Systemic antibacterial action against sensitive organisms during abscesses | Indication |
Product | Applicant | Ingredients |
---|---|---|
Tribrissen 120 Tablets, Tribrissen 30 Tablets, Tribrissen 480 Tablets, Tribrissen 960 Tablets | Intervet Inc. | 2 |
Tribrissen 24% Injection | Intervet Inc. | 2 |
Tribrissen 48% Injection | Intervet Inc. | 2 |
Di-Trim Tablets | Zoetis Inc. | 2 |
Tribrissen 400 Oral Paste | Intervet Inc. | 2 |
Di-Trim 24% | Zoetis Inc. | 2 |
Di-Trim 48% Injection | Zoetis Inc. | 2 |
Di-Trim 400 Paste | Zoetis Inc. | 2 |
Tribrissen 60 Oral Suspension | Intervet Inc. | 2 |
ReBalance | Pegasus Laboratories Inc. | 2 |
EQUISUL-SDT | Aurora Pharmaceutical Inc. | 2 |
Uniprim Powder | Neogen Corp. | 2 |
Tucoprim Powder | Zoetis Inc. | 2 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 6.6 | acidic |
pKa2 | 2.03 | Basic |
pKa3 | 1.41 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
5-hydroxytryptamine receptor 2A | GPCR | IC50 | 6.03 | WOMBAT-PK | |||||
5-hydroxytryptamine receptor 2B | GPCR | IC50 | 4.96 | WOMBAT-PK | |||||
Aurora kinase A | Kinase | IC50 | 4.68 | CHEMBL | |||||
High affinity choline transporter 1 | Transporter | IC50 | 4.24 | WOMBAT-PK | |||||
Dihydropteroate synthase | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
Dihydroorotate dehydrogenase (quinone), mitochondrial | Enzyme | WOMBAT-PK |
ID | Source |
---|---|
D00587 | KEGG_DRUG |
547-32-0 | SECONDARY_CAS_RN |
4017497 | VANDF |
C0038675 | UMLSCUI |
CHEBI:9328 | CHEBI |
CHEMBL439 | ChEMBL_ID |
CHEMBL1200351 | ChEMBL_ID |
DB00359 | DRUGBANK_ID |
D013411 | MESH_DESCRIPTOR_UI |
5215 | PUBCHEM_CID |
421 | INN_ID |
0N7609K889 | UNII |
10171 | RXNORM |
13920 | MMSL |
2022 | MMSL |
5523 | MMSL |
7798 | MMSL |
87818 | MMSL |
d00118 | MMSL |
002814 | NDDF |
014626 | NDDF |
371400009 | SNOMEDCT_US |
74523009 | SNOMEDCT_US |
768490003 | SNOMEDCT_US |
422 | INN_ID |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Sulfadiazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0185-0757 | TABLET | 500 mg | ORAL | ANDA | 18 sections |
SULFADIAZINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42806-757 | TABLET | 500 mg | ORAL | ANDA | 19 sections |