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cefaclor 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antibiotics, cefalosporanic acid derivatives | 525 | 53994-73-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Semisynthetic, broad-spectrum antibiotic derivative of CEPHALEXIN.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| 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:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 4, 1979 | FDA |
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 | 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 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 |
|---|---|---|---|---|---|---|
| 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 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 |
|---|---|---|---|---|---|---|
| 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:
| Source | Code | Description |
|---|---|---|
| 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
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 level | Dissociation constant | Type (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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 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:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |