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sulfacetamide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| anti-infectives, sulfonamides | 2497 | 144-80-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An anti-bacterial agent that is used topically to treat skin infections and orally for urinary tract infections.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -2.263 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.380 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 2.642 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.126 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 69.710 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 52.650 | % | High | 1 |
| herg | hERG pIC50 | 3.756 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.820 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.097 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 61.750 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,IKBKB,ITK,JAK1,JAK2,KIT,MAP2K6,MAP3K1,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAPK1,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MTOR,NTRK2,PAK4,PDK1,PDK2,PDPK1,PIK3CB,PIK3CD,PIM2,PLK1,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1,ULK2,ZAP70 | 62 | |||
| kinase-selectivity-class | ACVR2A,AURKA,AXL,CDK9,DDR1,DYRK1B,EPHB4,ERBB2,GRK2,JAK1,MAP2K3,MAP2K6,MAP3K7,MAPK12,MAPK7,MARK4,PRKDC,SGK1,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 | 25 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.873 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 4.613 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 84.390 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.582 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 53.680 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 1.585 | 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) | 36.420 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 922.571 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 12, 1945 | FDA | ORTHO MCNEIL PHARM |
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 |
|---|---|---|---|---|---|---|
| Drug hypersensitivity | 387.60 | 36.72 | 172 | 1264 | 463437 | 90163574 |
| Bronchiectasis | 154.79 | 36.72 | 41 | 1395 | 22289 | 90604722 |
| Hypothyroidism | 123.65 | 36.72 | 42 | 1394 | 53085 | 90573926 |
| Bone erosion | 119.81 | 36.72 | 41 | 1395 | 52980 | 90574031 |
| Loss of personal independence in daily activities | 82.44 | 36.72 | 41 | 1395 | 136064 | 90490947 |
| Neutropenia | 65.69 | 36.72 | 42 | 1394 | 224862 | 90402149 |
| Red blood cell sedimentation rate abnormal | 51.77 | 36.72 | 18 | 1418 | 24186 | 90602825 |
| Hypersensitivity | 50.83 | 36.72 | 48 | 1388 | 454629 | 90172382 |
| Synovitis | 45.02 | 36.72 | 39 | 1397 | 329713 | 90297298 |
| Drug intolerance | 43.88 | 36.72 | 44 | 1392 | 447547 | 90179464 |
FDA Adverse Event Reporting System (Male)
| 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 | 42.57 | 39.61 | 15 | 134 | 99374 | 42521812 |
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 |
|---|---|---|---|---|---|---|
| Drug hypersensitivity | 224.74 | 30.31 | 103 | 1034 | 453987 | 110134175 |
| Bronchiectasis | 84.87 | 30.31 | 26 | 1111 | 36467 | 110551695 |
| Bone erosion | 78.74 | 30.31 | 26 | 1111 | 46345 | 110541817 |
| Hypothyroidism | 67.24 | 30.31 | 26 | 1111 | 72873 | 110515289 |
| Loss of personal independence in daily activities | 49.25 | 30.31 | 26 | 1111 | 149994 | 110438168 |
| Joint stiffness | 44.80 | 30.31 | 19 | 1118 | 67224 | 110520938 |
| Synovitis | 34.83 | 30.31 | 26 | 1111 | 274066 | 110314096 |
| Neutropenia | 33.68 | 30.31 | 29 | 1108 | 374591 | 110213571 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | D10AF06 | DERMATOLOGICALS ANTI-ACNE PREPARATIONS ANTI-ACNE PREPARATIONS FOR TOPICAL USE Antiinfectives for treatment of acne |
| ATC | S01AB04 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIINFECTIVES Sulfonamides |
| FDA CS | M0020790 | Sulfonamides |
| FDA EPC | N0000175503 | Sulfonamide Antibacterial |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000891 | Anti-Infective Agents, Local |
| MeSH PA | D000892 | Anti-Infective Agents, Urinary |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| CHEBI has role | CHEBI:33281 | antimicrobial agent |
| CHEBI has role | CHEBI:35441 | antiinfective agent |
| CHEBI has role | CHEBI:36047 | antibacterial drug |
| CHEBI has role | CHEBI:50502 | EC 2.5.1.15 (dihydropteroate synthase) inhibitor |
| CHEBI has role | CHEBI:66981 | ophthalmology drug |
| CHEBI has role | CHEBI:67079 | anti-inflammatory agent |
Related Drugs by ATC class:
D10AF Antiinfectives for treatment of acne 6 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 |
| Seborrheic dermatitis | indication | 50563003 | DOID:8741 |
| Vulvovaginitis | indication | 53277000 | DOID:2273 |
| Blepharoconjunctivitis | indication | 68659002 | DOID:2456 |
| Iridocyclitis | indication | 77971008 | |
| Acne vulgaris | indication | 88616000 | |
| Amebic infection | indication | 111910009 | DOID:9181 |
| Uveitis | indication | 128473001 | DOID:13141 |
| Pityriasis simplex | indication | 200767005 | |
| Chlamydial conjunctivitis | indication | 231861005 | DOID:13800 |
| Infective blepharitis | indication | 312219000 | |
| Superficial Ocular Infection | indication | ||
| Gardnerella Vaginalis Bacterial Vaginosis | indication | ||
| Bacterial conjunctivitis | off-label use | 128350005 | DOID:9700 |
| Bacterial keratitis | off-label use | 314557000 | |
| Rosacea | off-label use | 398909004 | DOID:8881 |
| Ocular hypertension | contraindication | 4210003 | DOID:9282 |
| Herpes simplex keratitis | contraindication | 9389005 | |
| Herpes simplex dendritic keratitis | contraindication | 29943008 | |
| Fungal infection of eye | contraindication | 31194008 | |
| Severe myopia | contraindication | 34187009 | |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Tuberculosis of eye | contraindication | 49107007 | |
| Heart disease | contraindication | 56265001 | DOID:114 |
| Arteriosclerotic vascular disease | contraindication | 72092001 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Open-angle glaucoma | contraindication | 84494001 | DOID:1067 |
| Krukenberg spindle | contraindication | 85430004 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Anemia due to enzyme deficiency | contraindication | 111577008 | |
| Deficiency of glucose-6-phosphate dehydrogenase | contraindication | 124134002 | DOID:2862 |
| Eye infection | contraindication | 128351009 | |
| Bacterial infection of eye | contraindication | 128984004 | |
| Disease of blood AND/OR blood-forming organ | contraindication | 191124002 | DOID:74 |
| Arterial aneurysm | contraindication | 233981004 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Eruption of skin | contraindication | 271807003 | DOID:0050486 |
| Viral eye infection | contraindication | 312132001 | |
| Skin irritation | contraindication | 367466007 | |
| Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
| Vaccinia keratitis | contraindication | 397552005 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Disorder of coronary artery | contraindication | 414024009 | |
| Denuded skin | contraindication | 418242004 | |
| Porphyria | contraindication | 418470004 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 5.48 | acidic |
| pKa2 | 1.93 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Dihydrofolate reductase | Enzyme | IC50 | 4.74 | CHEMBL | |||||
| Dihydropteroate synthase | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
| Dihydrofolate reductase | Enzyme | IC50 | 4.66 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4018557 | VUID |
| N0000146877 | NUI |
| D00871 | KEGG_DRUG |
| 6209-17-2 | SECONDARY_CAS_RN |
| 4018203 | VANDF |
| 4018557 | VANDF |
| C0038670 | UMLSCUI |
| CHEBI:63845 | CHEBI |
| CHEMBL455 | ChEMBL_ID |
| DB00634 | DRUGBANK_ID |
| CHEMBL1723241 | ChEMBL_ID |
| D013409 | MESH_DESCRIPTOR_UI |
| 5320 | PUBCHEM_CID |
| 12633 | IUPHAR_LIGAND_ID |
| 122 | INN_ID |
| 4965G3J0F5 | UNII |
| 10169 | RXNORM |
| 12509 | MMSL |
| 5495 | MMSL |
| 7988 | MMSL |
| 002821 | NDDF |
| 004890 | NDDF |
| 108867000 | SNOMEDCT_US |
| 23827009 | SNOMEDCT_US |
| 372676007 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Sodium Sulfacetamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0168-0484 | SOLUTION | 100 mg | TOPICAL | Unapproved drug other | 18 sections |
| Avar-e Green | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0178-0460 | CREAM | 100 mg | TOPICAL | unapproved drug other | 13 sections |
| Avar-e LS | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0178-0465 | CREAM | 100 mg | TOPICAL | unapproved drug other | 12 sections |
| Avar-e | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0178-0470 | CREAM | 100 mg | TOPICAL | unapproved drug other | 12 sections |
| AVAR LS | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0178-0475 | EMULSION | 100 mg | TOPICAL | unapproved drug other | 12 sections |
| AVAR | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0178-0480 | EMULSION | 100 mg | TOPICAL | unapproved drug other | 12 sections |
| OVACE Plus | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0178-0485 | SHAMPOO | 100 mg | TOPICAL | unapproved drug other | 12 sections |
| OVACE Plus | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0178-0490 | LIQUID | 100 mg | TOPICAL | unapproved drug other | 12 sections |
| OvacePlusPlus | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0178-0495 | CREAM | 100 mg | TOPICAL | unapproved drug other | 12 sections |
| OVACE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0178-0499 | LIQUID | 100 mg | TOPICAL | unapproved drug other | 12 sections |
| OvacePlus | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0178-0620 | LOTION | 98 mg | TOPICAL | unapproved drug other | 12 sections |
| OVACE PLUS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0178-0630 | LIQUID | 100 mg | TOPICAL | unapproved drug other | 12 sections |
| Klaron | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-5198 | LOTION | 100 mg | TOPICAL | NDA | 16 sections |
| Sodium Sulfacetamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16477-410 | LIQUID | 100 mg | TOPICAL | unapproved drug other | 19 sections |
| Sodium Sulfacetamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16477-411 | SHAMPOO | 100 mg | TOPICAL | unapproved drug other | 19 sections |
| SULFACETAMIDE SODIUM | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-209 | SOLUTION/ DROPS | 100 mg | OPHTHALMIC | ANDA | 10 sections |
| Sulfacetamide Sodium and Prednisolone Sodium Phosphate | HUMAN PRESCRIPTION DRUG LABEL | 2 | 21695-186 | SOLUTION | 100 mg | OPHTHALMIC | ANDA | 18 sections |
| Sulfacetamide Sodium | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-525 | SOLUTION | 100 mg | OPHTHALMIC | ANDA | 18 sections |
| Sulfacetamide Sodium and Prednisolone Sodium Phosphate | HUMAN PRESCRIPTION DRUG LABEL | 2 | 24208-317 | SOLUTION/ DROPS | 100 mg | OPHTHALMIC | ANDA | 20 sections |
| Sulfacetamide Sodium | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24208-670 | SOLUTION/ DROPS | 100 mg | OPHTHALMIC | ANDA | 18 sections |
| SULFACETAMIDE SODIUM, SULFUR | HUMAN PRESCRIPTION DRUG LABEL | 2 | 24470-925 | EMULSION | 100 mg | TOPICAL | unapproved drug other | 12 sections |
| SULFACETAMIDE SODIUM, SULFUR | HUMAN PRESCRIPTION DRUG LABEL | 2 | 24470-932 | LOTION | 100 mg | TOPICAL | unapproved drug other | 12 sections |
| SULFACETAMIDE SODIUM, SULFUR | HUMAN PRESCRIPTION DRUG LABEL | 2 | 24470-933 | SUSPENSION | 100 mg | TOPICAL | unapproved drug other | 12 sections |
| SULFACETAMIDE SODIUM, SULFUR | HUMAN PRESCRIPTION DRUG LABEL | 2 | 24470-934 | LOTION | 100 mg | TOPICAL | unapproved drug other | 13 sections |
| SULFACETAMIDE SODIUM | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24470-935 | GEL | 100 mg | TOPICAL | unapproved drug other | 10 sections |
| SULFACETAMIDE SODIUM | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24470-937 | LIQUID | 100 mg | TOPICAL | unapproved drug other | 10 sections |
| Plexion | HUMAN PRESCRIPTION DRUG LABEL | 2 | 24470-941 | LIQUID | 98 mg | TOPICAL | unapproved drug other | 12 sections |
| Plexion | HUMAN PRESCRIPTION DRUG LABEL | 2 | 24470-942 | CREAM | 98 mg | TOPICAL | unapproved drug other | 12 sections |
| Plexion | HUMAN PRESCRIPTION DRUG LABEL | 2 | 24470-944 | LOTION | 98 mg | TOPICAL | unapproved drug other | 12 sections |
| SODIUM SULFACETAMIDE, SULFUR | HUMAN PRESCRIPTION DRUG LABEL | 2 | 24470-950 | LIQUID | 90 mg | TOPICAL | unapproved drug other | 12 sections |