cefotaxime Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antibiotics, cefalosporanic acid derivatives | 546 | 63527-52-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Semisynthetic broad-spectrum cephalosporin.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 4 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 30 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 376.38 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 0.19 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 2.70 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.60 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.20 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 11, 1981 | FDA | SANOFI AVENTIS US |
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 reaction with eosinophilia and systemic symptoms | 212.46 | 25.53 | 91 | 5424 | 32709 | 53310842 |
| Hepatocellular injury | 100.79 | 25.53 | 53 | 5462 | 29933 | 53313618 |
| Eosinophilia | 99.17 | 25.53 | 47 | 5468 | 21288 | 53322263 |
| Premature baby | 87.09 | 25.53 | 42 | 5473 | 19759 | 53323792 |
| Toxic epidermal necrolysis | 83.06 | 25.53 | 43 | 5472 | 23507 | 53320044 |
| Patent ductus arteriosus | 81.40 | 25.53 | 26 | 5489 | 4092 | 53339459 |
| Septic shock | 69.67 | 25.53 | 55 | 5460 | 62174 | 53281377 |
| Acute generalised exanthematous pustulosis | 64.73 | 25.53 | 28 | 5487 | 10253 | 53333298 |
| Pyrexia | 63.77 | 25.53 | 133 | 5382 | 403060 | 52940491 |
| Rash maculo-papular | 58.22 | 25.53 | 37 | 5478 | 29712 | 53313839 |
| Fatigue | 54.76 | 25.53 | 6 | 5509 | 730500 | 52613051 |
| Purpura | 53.77 | 25.53 | 25 | 5490 | 10828 | 53332723 |
| Laryngeal stenosis | 52.75 | 25.53 | 13 | 5502 | 793 | 53342758 |
| Foetal exposure during pregnancy | 50.69 | 25.53 | 36 | 5479 | 34679 | 53308872 |
| Hydrocephalus | 45.65 | 25.53 | 18 | 5497 | 5218 | 53338333 |
| Umbilical erythema | 45.31 | 25.53 | 8 | 5507 | 91 | 53343460 |
| Agranulocytosis | 42.67 | 25.53 | 28 | 5487 | 23721 | 53319830 |
| Encephalopathy | 42.17 | 25.53 | 33 | 5482 | 36775 | 53306776 |
| Thrombocytopenia | 41.85 | 25.53 | 61 | 5454 | 138666 | 53204885 |
| Multiple organ dysfunction syndrome | 41.48 | 25.53 | 39 | 5476 | 55638 | 53287913 |
| Haemophagocytic lymphohistiocytosis | 39.00 | 25.53 | 19 | 5496 | 9118 | 53334433 |
| Necrosis | 38.76 | 25.53 | 16 | 5499 | 5215 | 53338336 |
| Subperiosteal abscess | 37.42 | 25.53 | 5 | 5510 | 5 | 53343546 |
| Sepsis | 35.22 | 25.53 | 58 | 5457 | 146371 | 53197180 |
| Necrotising enterocolitis neonatal | 34.12 | 25.53 | 7 | 5508 | 184 | 53343367 |
| Lactic acidosis | 33.46 | 25.53 | 29 | 5486 | 37224 | 53306327 |
| Brain abscess | 33.26 | 25.53 | 11 | 5504 | 1930 | 53341621 |
| Sepsis neonatal | 32.60 | 25.53 | 8 | 5507 | 479 | 53343072 |
| Acute kidney injury | 32.36 | 25.53 | 77 | 5438 | 253791 | 53089760 |
| Ventricular dysfunction | 32.34 | 25.53 | 12 | 5503 | 2951 | 53340600 |
| Death neonatal | 32.02 | 25.53 | 7 | 5508 | 251 | 53343300 |
| Petechiae | 31.90 | 25.53 | 19 | 5496 | 13586 | 53329965 |
| Toxic shock syndrome streptococcal | 31.74 | 25.53 | 6 | 5509 | 102 | 53343449 |
| Neutropenia | 31.68 | 25.53 | 58 | 5457 | 159127 | 53184424 |
| Cholestasis | 31.30 | 25.53 | 25 | 5490 | 28670 | 53314881 |
| Pulmonary necrosis | 30.72 | 25.53 | 6 | 5509 | 122 | 53343429 |
| Hepatic failure | 30.40 | 25.53 | 27 | 5488 | 35779 | 53307772 |
| Stenotrophomonas infection | 30.39 | 25.53 | 10 | 5505 | 1726 | 53341825 |
| Disseminated intravascular coagulation | 30.05 | 25.53 | 21 | 5494 | 19698 | 53323853 |
| Central nervous system necrosis | 29.61 | 25.53 | 6 | 5509 | 148 | 53343403 |
| Arthralgia | 29.58 | 25.53 | 5 | 5510 | 439778 | 52903773 |
| Cross sensitivity reaction | 28.59 | 25.53 | 10 | 5505 | 2077 | 53341474 |
| Intraventricular haemorrhage neonatal | 28.35 | 25.53 | 6 | 5509 | 184 | 53343367 |
| Clostridium bacteraemia | 27.93 | 25.53 | 6 | 5509 | 198 | 53343353 |
| Hyperleukocytosis | 27.20 | 25.53 | 7 | 5508 | 509 | 53343042 |
| Oligohydramnios | 27.03 | 25.53 | 13 | 5502 | 6063 | 53337488 |
| Respiratory acidosis | 26.41 | 25.53 | 13 | 5502 | 6375 | 53337176 |
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 reaction with eosinophilia and systemic symptoms | 283.66 | 23.11 | 137 | 6608 | 32348 | 32474433 |
| Rash maculo-papular | 149.29 | 23.11 | 85 | 6660 | 27937 | 32478844 |
| Hepatocellular injury | 130.03 | 23.11 | 75 | 6670 | 25243 | 32481538 |
| Eosinophilia | 104.90 | 23.11 | 65 | 6680 | 24893 | 32481888 |
| Toxic epidermal necrolysis | 92.57 | 23.11 | 56 | 6689 | 20537 | 32486244 |
| Agranulocytosis | 64.55 | 23.11 | 47 | 6698 | 23430 | 32483351 |
| Haemophagocytic lymphohistiocytosis | 56.59 | 23.11 | 33 | 6712 | 11302 | 32495479 |
| Clostridium difficile colitis | 51.90 | 23.11 | 34 | 6711 | 14297 | 32492484 |
| Pyrexia | 49.61 | 23.11 | 162 | 6583 | 319806 | 32186975 |
| Purpura | 48.24 | 23.11 | 29 | 6716 | 10496 | 32496285 |
| Toxic skin eruption | 48.12 | 23.11 | 30 | 6715 | 11584 | 32495197 |
| Acute kidney injury | 46.74 | 23.11 | 150 | 6595 | 293318 | 32213463 |
| Klebsiella infection | 44.47 | 23.11 | 25 | 6720 | 7987 | 32498794 |
| Cholestasis | 40.40 | 23.11 | 38 | 6707 | 26995 | 32479786 |
| Fatigue | 37.63 | 23.11 | 13 | 6732 | 350688 | 32156093 |
| Face oedema | 35.62 | 23.11 | 25 | 6720 | 11750 | 32495031 |
| Thrombotic microangiopathy | 35.56 | 23.11 | 23 | 6722 | 9459 | 32497322 |
| Neutropenia | 34.69 | 23.11 | 85 | 6660 | 142090 | 32364691 |
| Death | 33.47 | 23.11 | 19 | 6726 | 382498 | 32124283 |
| Septic shock | 32.14 | 23.11 | 54 | 6691 | 68935 | 32437846 |
| Nausea | 30.94 | 23.11 | 14 | 6731 | 320835 | 32185946 |
| Brain abscess | 30.52 | 23.11 | 14 | 6731 | 2920 | 32503861 |
| Learning disorder | 30.49 | 23.11 | 10 | 6735 | 846 | 32505935 |
| Thrombocytopenia | 30.34 | 23.11 | 83 | 6662 | 148216 | 32358565 |
| Haematoma muscle | 28.66 | 23.11 | 10 | 6735 | 1022 | 32505759 |
| CNS ventriculitis | 27.36 | 23.11 | 7 | 6738 | 244 | 32506537 |
| ADAMTS13 activity decreased | 27.19 | 23.11 | 6 | 6739 | 109 | 32506672 |
| Respiratory gas exchange disorder | 27.15 | 23.11 | 8 | 6737 | 475 | 32506306 |
| Systemic candida | 27.06 | 23.11 | 13 | 6732 | 3008 | 32503773 |
| Rash | 26.24 | 23.11 | 99 | 6646 | 209234 | 32297547 |
| Hyperthermia | 26.16 | 23.11 | 20 | 6725 | 10708 | 32496073 |
| Gamma-glutamyltransferase increased | 26.01 | 23.11 | 32 | 6713 | 30750 | 32476031 |
| Red blood cell schistocytes present | 25.81 | 23.11 | 7 | 6738 | 307 | 32506474 |
| Drug ineffective | 25.71 | 23.11 | 151 | 6594 | 383326 | 32123455 |
| Neonatal disorder | 25.49 | 23.11 | 9 | 6736 | 952 | 32505829 |
| Bicytopenia | 25.31 | 23.11 | 11 | 6734 | 2020 | 32504761 |
| Vasculitis necrotising | 24.90 | 23.11 | 8 | 6737 | 634 | 32506147 |
| Pancytopenia | 24.88 | 23.11 | 57 | 6688 | 91178 | 32415603 |
| Acute generalised exanthematous pustulosis | 24.69 | 23.11 | 16 | 6729 | 6597 | 32500184 |
| Hepatic cytolysis | 23.61 | 23.11 | 17 | 6728 | 8316 | 32498465 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J01DD01 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER BETA-LACTAM ANTIBACTERIALS Third-generation cephalosporins |
| ATC | J01DD51 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER BETA-LACTAM ANTIBACTERIALS Third-generation cephalosporins |
| FDA CS | M0003827 | Cephalosporins |
| FDA EPC | N0000175488 | Cephalosporin Antibacterial |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| MeSH PA | D000890 | Anti-Infective Agents |
| CHEBI has role | CHEBI:36047 | antibacterial drugs |
| CHEBI has role | CHEBI:88188 | allergenic drug |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Streptococcal meningitis | indication | 4510004 | DOID:11574 |
| Septicemia due to Escherichia coli | indication | 9323009 | |
| Bacterial septicemia | indication | 10001005 | DOID:0040085 |
| Infection of skin AND/OR subcutaneous tissue | indication | 19824006 | |
| Staphylococcal pneumonia | indication | 22754005 | |
| Streptococcal septicemia | indication | 29577008 | |
| Pneumonia due to Streptococcus | indication | 34020007 | |
| Neonatal conjunctivitis | indication | 34298002 | DOID:9699 |
| Pneumonia due to Pseudomonas | indication | 41381004 | |
| Bacterial arthritis | indication | 48245008 | |
| Peritonitis | indication | 48661000 | |
| Lower respiratory tract infection | indication | 50417007 | |
| Pneumonia due to Escherichia coli | indication | 51530003 | |
| Bacterial pneumonia | indication | 53084003 | DOID:874 |
| Klebsiella cystitis | indication | 60867007 | |
| Haemophilus influenzae pneumonia | indication | 70036007 | |
| Bacterial infection due to Serratia | indication | 71120004 | |
| Septicemia due to Serratia | indication | 82091000 | |
| Bacterial meningitis | indication | 95883001 | DOID:9470 |
| Infection of bone | indication | 111253001 | |
| Female genital tract infection | indication | 125585007 | |
| Infectious disease of abdomen | indication | 128070006 | |
| Bacterial infection due to Klebsiella pneumoniae | indication | 186435004 | |
| Meningococcal meningitis | indication | 192644005 | |
| Escherichia coli meningitis | indication | 192655005 | |
| Proteus pneumonia | indication | 195888009 | |
| Sepsis of the newborn | indication | 206376005 | |
| Neonatal pneumonia | indication | 233619008 | |
| Neonatal meningitis | indication | 276674008 | |
| Escherichia coli urinary tract infection | indication | 301011002 | |
| Proteus urinary tract infection | indication | 301012009 | |
| Bacterial urinary infection | indication | 312124009 | |
| Meningitis due to Klebsiella mobilis | indication | 420585007 | |
| Sepsis due to Staphylococcus aureus | indication | 448417001 | |
| Cesarean Section Infection Prevention | indication | ||
| Streptococcal Peritonitis | indication | ||
| E. Coli Peritonitis | indication | ||
| E. Coli Endometritis | indication | ||
| Haemophilus Influenzae Type B Infections | indication | ||
| Neonatal Group B Streptococcal Septicemia | indication | ||
| Klebsiella Endometritis | indication | ||
| Proteus Endometritis | indication | ||
| Enterococcus Pelvic Cellulitis | indication | ||
| Prevention of Perioperative Infection | indication | ||
| Proteus Mirabilis Osteomyelitis | indication | ||
| Bacteroides Pelvic Cellulitis | indication | ||
| Klebsiella Pelvic Inflammatory Disease | indication | ||
| Staphylococcus Endometritis | indication | ||
| H. Influenzae Meningitis | indication | ||
| Clostridium Pelvic Inflammatory Disease | indication | ||
| Haemophilus Parainfluenzae Pneumonia | indication | ||
| Bacteroides Pelvic Inflammatory Disease | indication | ||
| Staphylococcus Pelvic Inflammatory Disease | indication | ||
| Proteus Peritonitis | indication | ||
| Clostridium Endometritis | indication | ||
| Staphylococcus Epidermidis Urinary Tract Infection | indication | ||
| Enterococcus Pelvic Inflammatory Disease | indication | ||
| Morganella Morganii Urinary Tract Infection | indication | ||
| Fusobacterium Pelvic Inflammatory Disease | indication | ||
| Streptococcus Osteomyelitis | indication | ||
| Enterococcus Urinary Tract Infection | indication | ||
| Clostridium Pelvic Cellulitis | indication | ||
| Serratia Urinary Tract Infection | indication | ||
| Enterobacter Pneumonia | indication | ||
| Enterobacter Pelvic Inflammatory Disease | indication | ||
| Bacteroides Endometritis | indication | ||
| Providencia Urinary Tract Infection | indication | ||
| Citrobacter Urinary Tract Infection | indication | ||
| Fusobacterium Endometritis | indication | ||
| Proteus Pelvic Inflammatory Disease | indication | ||
| Clostridium Peritonitis | indication | ||
| Staphylococcus Aureus Urinary Tract Infection | indication | ||
| E. Coli Pelvic Inflammatory Disease | indication | ||
| E. Coli Pelvic Cellulitis | indication | ||
| Enterobacter Endometritis | indication | ||
| Pseudomonas Aeruginosa Urinary Tract Infection | indication | ||
| Klebsiella Pneumoniae Peritonitis | indication | ||
| Enterococcus Endometritis | indication | ||
| Pyrexia of unknown origin | off-label use | 7520000 | |
| Acute gonococcal cervicitis | off-label use | 20943002 | DOID:10615 |
| Lyme disease | off-label use | 23502006 | DOID:11729 |
| Acute gonococcal urethritis | off-label use | 29864006 | |
| Lyme arthritis | off-label use | 33937009 | |
| Pseudotuberculosis | off-label use | 36753006 | |
| Gonorrhea of rectum | off-label use | 42746002 | |
| Lyme carditis | off-label use | 77863005 | |
| Infection by Yersinia enterocolitica | off-label use | 80960004 | |
| Ventilator-acquired pneumonia | off-label use | 429271009 | |
| Disseminated Gonococcal Infection | off-label use | ||
| Lyme Disease of the Central Nervous System | off-label use | ||
| Acute nephropathy | contraindication | 58574008 | |
| Pseudomembranous enterocolitis | contraindication | 397683000 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 2.39 | acidic |
| pKa2 | 13.31 | acidic |
| pKa3 | 3.1 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Peptidoglycan synthase FtsI | Enzyme | INHIBITOR | IC50 | 6.24 | WOMBAT-PK | CHEMBL | |||
| Penicillin-binding protein 1A | Enzyme | INHIBITOR | IC50 | 6.51 | WOMBAT-PK | CHEMBL | |||
| Penicillin-binding protein 1B | Enzyme | INHIBITOR | IC50 | 5.66 | WOMBAT-PK | CHEMBL | |||
| Penicillin-binding protein 2 | Enzyme | INHIBITOR | IC50 | 4.62 | WOMBAT-PK | CHEMBL | |||
| Beta-lactamase | Enzyme | Ki | 6.30 | CHEMBL | |||||
| Beta-lactamase | Enzyme | Ki | 5.60 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019663 | VUID |
| N0000147755 | NUI |
| D00919 | KEGG_DRUG |
| 64485-93-4 | SECONDARY_CAS_RN |
| C0007554 | UMLSCUI |
| CHEBI:3498 | CHEBI |
| CE3 | PDB_CHEM_ID |
| CHEMBL1010 | ChEMBL_ID |
| CHEMBL1730 | ChEMBL_ID |
| D002439 | MESH_DESCRIPTOR_UI |
| DB00493 | DRUGBANK_ID |
| 10893 | IUPHAR_LIGAND_ID |
| 4504 | INN_ID |
| N2GI8B1GK7 | UNII |
| 10695961 | PUBCHEM_CID |
| 203117 | RXNORM |
| 42787 | MMSL |
| 4378 | MMSL |
| d00008 | MMSL |
| 002727 | NDDF |
| 004845 | NDDF |
| 3334000 | SNOMEDCT_US |
| 372704003 | SNOMEDCT_US |
| 41722006 | SNOMEDCT_US |
| 4018466 | VANDF |
| 4019663 | VANDF |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Cefotaxime | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9930 | INJECTION, POWDER, FOR SOLUTION | 500 mg | INTRAMUSCULAR | ANDA | 24 sections |
| Cefotaxime | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9931 | INJECTION, POWDER, FOR SOLUTION | 1 g | INTRAMUSCULAR | ANDA | 24 sections |
| Cefotaxime | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9933 | INJECTION, POWDER, FOR SOLUTION | 2 g | INTRAMUSCULAR | ANDA | 24 sections |
| Cefotaxime | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9935 | INJECTION | 10 g | INTRAVENOUS | ANDA | 24 sections |
| Cefotaxime | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21586-011 | POWDER, FOR SOLUTION | 1 g | INTRAMUSCULAR | Unapproved drug for use in drug shortage | 2 sections |
| Cefotaxime | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21586-012 | POWDER, FOR SOLUTION | 2 g | INTRAMUSCULAR | Unapproved drug for use in drug shortage | 2 sections |
| CEFOTAXIME | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55648-947 | INJECTION, POWDER, FOR SOLUTION | 500 mg | INTRAMUSCULAR | ANDA | 11 sections |
| CEFOTAXIME | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55648-948 | INJECTION, POWDER, FOR SOLUTION | 2 g | INTRAMUSCULAR | ANDA | 11 sections |
| CEFOTAXIME | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55648-986 | INJECTION, POWDER, FOR SOLUTION | 1 g | INTRAMUSCULAR | ANDA | 11 sections |
| Cefotaxime | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64679-947 | INJECTION, POWDER, FOR SOLUTION | 500 mg | INTRAMUSCULAR | ANDA | 20 sections |
| Cefotaxime | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64679-948 | INJECTION, POWDER, FOR SOLUTION | 2 g | INTRAMUSCULAR | ANDA | 20 sections |
| Cefotaxime | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64679-986 | INJECTION, POWDER, FOR SOLUTION | 1 g | INTRAMUSCULAR | ANDA | 20 sections |