sulfacetamide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
anti-infectives, sulfonamides 2497 144-80-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • sulfacetamide
  • acetosulfamin
  • acetosulfamine
  • formosulfacetamide
  • N-Acetylsulfanilamide
  • N-Sulfanilylacetamide
  • sulfacet
  • sulfacetimide
  • sulphacetamide
  • sulfacetamide sodium
  • sulfacetamide sodic hydrate
An anti-bacterial agent that is used topically to treat skin infections and orally for urinary tract infections.
  • Molecular weight: 214.24
  • Formula: C8H10N2O3S
  • CLOGP: -0.98
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 2
  • TPSA: 89.26
  • ALOGS: -1.71
  • ROTB: 1
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
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:

DateAgencyCompanyOrphan
Sept. 12, 1945 FDA ORTHO MCNEIL PHARM

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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:

SourceCodeDescription
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
chloramphenicolclindamycinerythromycinmeclocyclineminocyclinenadifloxacin
S01AB Sulfonamides 4 drugs
sulfadicramidesulfafurazolesulfamethizolesulfaphenazole

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Dihydrofolate reductase Enzyme IC50 4.74 CHEMBL
Dihydropteroate synthase Enzyme INHIBITOR CHEMBL CHEMBL
Dihydrofolate reductase Enzyme IC50 4.66 CHEMBL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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