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

Stem definitionDrug idCAS RN
antibiotics, cefalosporanic acid derivatives 525 53994-73-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cefaclor
  • alfacet
  • ceclor
  • cephaclor
  • distaclor
  • losefar
  • cefaclor hydrate
Semisynthetic, broad-spectrum antibiotic derivative of CEPHALEXIN.
  • Molecular weight: 367.80
  • Formula: C15H14ClN3O4S
  • CLOGP: -1.64
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 3
  • TPSA: 112.73
  • ALOGS: -3.24
  • ROTB: 4
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
1 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 8.59 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 52 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 67.97 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 90 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -1.555 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.807 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 0.601 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 1.832 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 72.500 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 46.490 % High 1
herg hERG pIC50 4.661 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.738 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 4.036 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 57.320 % High 1
kinase-safety-class ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,ERBB2,GRK2,GRK3,GSK3B,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,NTRK2,PDK1,PDK2,PIK3CB,PIM2,PRKDC,SIK2,STK33,SYK,TEK,TGFBR1 38
kinase-selectivity-class AXL,BRAF,CDK9,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,JAK2,MAP2K6,MAPK7,PRKDC,STK33,SYK,TEK,TGFBR1,TTK 17
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 0.593 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.820 High 1
mh-clint Mouse hepatocyte intrinsic clearance 2.328 High 1
mppb Mouse plasma protein binding (% unbound) 67.070 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 1.026 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 44.100 % High 1
rat-kpuu-brain Rat brain Kpuu 0.009 % High 1
rh-clint Rat hepatocyte intrinsic clearance 1.828 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 89.490 % High 1
rppb Rat plasma protein binding (% unbound) 46.380 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 972.747 uM High 1

Approvals:

DateAgencyCompanyOrphan
April 4, 1979 FDA

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 616.33 25.63 352 4519 463257 90160319
International normalised ratio fluctuation 515.55 25.63 96 4775 2997 90620579
Cross sensitivity reaction 440.14 25.63 83 4788 2774 90620802
Type IV hypersensitivity reaction 419.82 25.63 84 4787 3842 90619734
Bloody discharge 401.09 25.63 74 4797 2189 90621387
Lyme disease 342.79 25.63 72 4799 4190 90619386
Rash maculo-papular 157.69 25.63 65 4806 40868 90582708
Iron deficiency 143.42 25.63 42 4829 9570 90614006
Therapeutic product effect incomplete 121.68 25.63 93 4778 193803 90429773
Platelet count increased 111.47 25.63 42 4829 20817 90602759
Secretion discharge 103.42 25.63 37 4834 15859 90607717
Infection 92.20 25.63 105 4766 361989 90261587
Staphylococcal infection 77.56 25.63 42 4829 48397 90575179
Drug intolerance 70.03 25.63 102 4769 447489 90176087
Muscle tension dysphonia 67.42 25.63 12 4859 287 90623289
Red blood cell sedimentation rate increased 59.23 25.63 43 4828 82552 90541024
Dysphemia 52.84 25.63 15 4856 3055 90620521
Immunisation reaction 50.05 25.63 11 4860 789 90622787
Toxic epidermal necrolysis 48.72 25.63 27 4844 32501 90591075
Oedema 42.43 25.63 53 4818 200242 90423334
Vomiting 41.74 25.63 114 4757 788179 89835397
Restrictive pulmonary disease 38.22 25.63 11 4860 2351 90621225
Polyglandular disorder 37.27 25.63 7 4864 227 90623349
Vaccination complication 36.64 25.63 9 4862 1050 90622526
Clostridium difficile infection 35.77 25.63 23 4848 36222 90587354
Endocrine disorder 32.41 25.63 8 4863 952 90622624
Oral pruritus 31.61 25.63 10 4861 2941 90620635
Anaemia folate deficiency 31.36 25.63 7 4864 539 90623037
Food intolerance 28.87 25.63 10 4861 3892 90619684
Oropharyngeal discomfort 28.78 25.63 12 4859 7723 90615853
Hypoparathyroidism 27.14 25.63 7 4864 994 90622582
Hypoaesthesia 26.98 25.63 55 4816 314155 90309421
Chronic hepatitis 26.20 25.63 7 4864 1138 90622438
Dizziness 26.04 25.63 80 4791 589204 90034372
Rash erythematous 25.76 25.63 24 4847 65080 90558496

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
Cross sensitivity reaction 91.20 27.26 19 1459 1656 42618201
Type IV hypersensitivity reaction 78.70 27.26 18 1460 2419 42617438
Drug hypersensitivity 61.96 27.26 40 1438 99349 42520508
Complex regional pain syndrome 33.26 27.26 7 1471 638 42619219
Lymphocyte count decreased 29.98 27.26 16 1462 27793 42592064
Medical device implantation 27.81 27.26 6 1472 615 42619242
Hypoproteinaemia 27.38 27.26 8 1470 2804 42617053

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
International normalised ratio fluctuation 497.74 22.38 98 6049 3982 110579170
Drug hypersensitivity 494.39 22.38 308 5839 453782 110129370
Cross sensitivity reaction 490.55 22.38 102 6045 5465 110577687
Type IV hypersensitivity reaction 482.38 22.38 102 6045 5931 110577221
Bloody discharge 396.98 22.38 76 6071 2657 110580495
Lyme disease 350.82 22.38 74 6073 4242 110578910
Rash maculo-papular 149.98 22.38 76 6071 74146 110509006
Iron deficiency 122.51 22.38 44 6103 18432 110564720
Platelet count increased 117.68 22.38 47 6100 26287 110556865
Therapeutic product effect incomplete 113.18 22.38 96 6051 223709 110359443
Secretion discharge 100.52 22.38 39 6108 20205 110562947
Infection 97.59 22.38 110 6037 362090 110221062
Drug intolerance 71.83 22.38 100 6047 406412 110176740
Staphylococcal infection 69.22 22.38 45 6102 69899 110513253
Red blood cell sedimentation rate increased 64.61 22.38 45 6102 78257 110504895
Muscle tension dysphonia 60.73 22.38 11 6136 281 110582871
Oedema 58.53 22.38 65 6082 209911 110373241
Immunisation reaction 49.55 22.38 11 6136 798 110582354
Toxic epidermal necrolysis 47.71 22.38 33 6114 56694 110526458
Vomiting 46.66 22.38 133 6014 910542 109672610
Lymphocyte count decreased 45.12 22.38 32 6115 57211 110525941
Dysphemia 44.11 22.38 14 6133 4023 110579129
Hypoproteinaemia 42.58 22.38 15 6132 5930 110577222
Neutrophil count decreased 38.15 22.38 40 6107 120901 110462251
Polyglandular disorder 36.69 22.38 7 6140 239 110582913
Restrictive pulmonary disease 34.36 22.38 11 6136 3248 110579904
Hyperuricaemia 29.65 22.38 15 6132 14516 110568636
Anaemia folate deficiency 29.38 22.38 7 6140 694 110582458
Vaccination complication 27.84 22.38 7 6140 868 110582284
Hypoaesthesia 26.83 22.38 56 6091 314167 110268985
Urticaria 26.27 22.38 56 6091 318801 110264351
Oral pruritus 26.18 22.38 9 6138 3311 110579841
Endocrine disorder 26.10 22.38 7 6140 1117 110582035
White blood cell count decreased 25.86 22.38 46 6101 229344 110353808
Hypoparathyroidism 23.96 22.38 7 6140 1523 110581629
Presbyopia 23.95 22.38 6 6141 733 110582419
Food intolerance 23.45 22.38 9 6138 4518 110578634
Condition aggravated 23.44 22.38 6 6141 734830 109848322
Chronic hepatitis 22.95 22.38 7 6140 1765 110581387

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J01DC04 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
OTHER BETA-LACTAM ANTIBACTERIALS
Second-generation cephalosporins
CHEBI has role CHEBI:36047 antibacterial drug
CHEBI has role CHEBI:88188 drug allergen
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000900 Anti-Bacterial Agents

Related Drugs by ATC class:

J01DC Second-generation cephalosporins 13 drugs
cefamandolecefbuperazonecefmetazolecefminoxcefonicidceforanidecefotetancefotiamcefoxitincefprozilcefuroximeflomoxef show all 13 →

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

DiseaseRelationSNOMED_IDDOID
Infection of skin AND/OR subcutaneous tissue indication 19824006
Pneumonia due to Streptococcus indication 34020007
Streptococcal tonsillitis indication 41582007
Lower respiratory tract infection indication 50417007
Upper respiratory infection indication 54150009
Urinary tract infectious disease indication 68566005
Haemophilus influenzae pneumonia indication 70036007
Tonsillitis indication 90176007 DOID:10456
Acute Moraxella catarrhalis bronchitis indication 195722003
Acute bacterial bronchitis indication 233598009
Pneumonia indication 233604007 DOID:552
Streptococcus pyogenes infection indication 302809008
Infective otitis media indication 312218008
Pharyngitis indication 405737000 DOID:2275
Infection due to Staphylococcus aureus indication 406602003
Moraxella Catarrhalis Chronic Bronchitis indication
Haemophilus Influenzae Bronchitis indication
Haemophilus Influenzae Chronic Bronchitis indication
Streptococcus Pneumoniae Bronchitis indication
Streptococcus Pneumoniae Chronic Bronchitis indication
Pyrexia of unknown origin off-label use 7520000
Pseudomembranous enterocolitis contraindication 397683000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 2.02 acidic
pKa2 13.93 acidic
pKa3 7.67 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
Bacterial penicillin-binding protein Enzyme INHIBITOR CHEMBL CHEMBL
Penicillin-binding protein 1A Enzyme WOMBAT-PK
Streptokinase A Enzyme EC50 6.33 WOMBAT-PK

External reference:

IDSource
4017534 VUID
N0000145917 NUI
D00256 KEGG_DRUG
70356-03-5 SECONDARY_CAS_RN
203635 RXNORM
C0007537 UMLSCUI
CHEBI:3478 CHEBI
8XI PDB_CHEM_ID
CHEMBL1201018 ChEMBL_ID
DB00833 DRUGBANK_ID
D002433 MESH_DESCRIPTOR_UI
51039 PUBCHEM_CID
10897 IUPHAR_LIGAND_ID
69K7K19H4L UNII
4368 MMSL
862 MMSL
871 MMSL
d00081 MMSL
387270009 SNOMEDCT_US
4937008 SNOMEDCT_US
4017534 VANDF
002726 NDDF
69K7K19H4L INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Cefaclor HUMAN PRESCRIPTION DRUG LABEL 1 0093-1087 TABLET, FILM COATED, EXTENDED RELEASE 500 mg ORAL ANDA 24 sections
CEFACLOR HUMAN PRESCRIPTION DRUG LABEL 1 21695-782 SUSPENSION 250 mg ORAL ANDA 21 sections
Cefaclor HUMAN PRESCRIPTION DRUG LABEL 1 50090-1602 CAPSULE 500 mg ORAL ANDA 23 sections
Cefaclor HUMAN PRESCRIPTION DRUG LABEL 1 54868-3478 CAPSULE 250 mg ORAL ANDA 13 sections
Cefaclor HUMAN PRESCRIPTION DRUG LABEL 1 54868-3511 CAPSULE 500 mg ORAL ANDA 13 sections
Cefaclor HUMAN PRESCRIPTION DRUG LABEL 1 61442-171 CAPSULE 250 mg ORAL ANDA 22 sections
Cefaclor HUMAN PRESCRIPTION DRUG LABEL 1 61442-172 CAPSULE 500 mg ORAL ANDA 22 sections
Cefaclor HUMAN PRESCRIPTION DRUG LABEL 1 81948-6250 SUSPENSION 250 mg ORAL ANDA 22 sections