Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C16H16N2O6S2.C2H7NO |
| Molecular Weight | 457.521 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
NCCO.[H][C@]12SCC(COC(C)=O)=C(N1C(=O)[C@H]2NC(=O)CC3=CC=CS3)C(O)=O
InChI
InChIKey=DZGMMKAGEYLTBD-XRZFDKQNSA-N
InChI=1S/C16H16N2O6S2.C2H7NO/c1-8(19)24-6-9-7-26-15-12(14(21)18(15)13(9)16(22)23)17-11(20)5-10-3-2-4-25-10;3-1-2-4/h2-4,12,15H,5-7H2,1H3,(H,17,20)(H,22,23);4H,1-3H2/t12-,15-;/m1./s1
| Molecular Formula | C2H7NO |
| Molecular Weight | 61.0831 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C16H16N2O6S2 |
| Molecular Weight | 396.438 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: description was created based on several sources, including:
http://www.druginfosys.com/drug.aspx?drugcode=150 | http://cdn-1.consultaremedios.com.br/bulas/2/14787.pdf
Curator's Comment: description was created based on several sources, including:
http://www.druginfosys.com/drug.aspx?drugcode=150 | http://cdn-1.consultaremedios.com.br/bulas/2/14787.pdf
Cephalothin is a first generation, semisynthetic analogue of natural cephalosporin antibiotic. The in-vitro bactericidal action of Cephalothin results from inhibition of cell-wall synthesis. In general, Cephalothin has higher activity against Gram positive than Gram negative organisms. Cephalothin is primarily indicated in conditions like bone and joint infection, genitourinary tract infections, respiratory tract infections, soft tissue and skin infections and others. The severe or irreversible adverse effects of Cephalothin, which give rise to further complications, include nephrotoxicity, hemolytic anemia. Cephalothin produces potentially life-threatening effects, which include anaphylaxis, serum sickness syndrome. The symptomatic adverse reactions produced by Cephalothin are: rashes, urticaria, allergic reactions, thrombophlebitis, pain at injection site. Co-administration of diuretics, such as furanthril, ethacrynic acid and nephrotoxic antibiotics may increase the risk of renal damage. Reciprocal inactivation could be observed during in vitro mixing of Cephalothin with aminoglycosides.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2354204 |
|||
Target ID: P15555 Gene ID: NA Gene Symbol: NA Target Organism: Streptomyces sp. (strain R61) |
|||
Target ID: Q9Y694 Gene ID: 10864.0 Gene Symbol: SLC22A7 Target Organism: Homo sapiens (Human) |
1.41 mM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Curative | KEFLIN Approved UseCephalothin is indicated in the treatment of serious infections caused by susceptible strains of the designated microorganisms in the respiratory tract infections, skin and soft-tissue infections, genito-urinary tract infections, septicaemia, including endocarditis, bone and joint infections. Launch Date1974 |
|||
| Curative | KEFLIN Approved UseCephalothin is indicated in the treatment of serious infections caused by susceptible strains of the designated microorganisms in the respiratory tract infections, skin and soft-tissue infections, genito-urinary tract infections, septicaemia, including endocarditis, bone and joint infections. Launch Date1974 |
|||
| Curative | KEFLIN Approved UseCephalothin is indicated in the treatment of serious infections caused by susceptible strains of the designated microorganisms in the respiratory tract infections, skin and soft-tissue infections, genito-urinary tract infections, septicaemia, including endocarditis, bone and joint infections. Launch Date1974 |
|||
| Curative | KEFLIN Approved UseCephalothin is indicated in the treatment of serious infections caused by susceptible strains of the designated microorganisms in the respiratory tract infections, skin and soft-tissue infections, genito-urinary tract infections, septicaemia, including endocarditis, bone and joint infections. Launch Date1974 |
|||
| Curative | KEFLIN Approved UseCephalothin is indicated in the treatment of serious infections caused by susceptible strains of the designated microorganisms in the respiratory tract infections, skin and soft-tissue infections, genito-urinary tract infections, septicaemia, including endocarditis, bone and joint infections. Launch Date1974 |
|||
| Curative | KEFLIN Approved UseCephalothin is indicated in the treatment of serious infections caused by susceptible strains of the designated microorganisms in the respiratory tract infections, skin and soft-tissue infections, genito-urinary tract infections, septicaemia, including endocarditis, bone and joint infections. Launch Date1974 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
20.8 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15830475/ |
3 g single, intravenous dose: 3 g route of administration: Intravenous experiment type: SINGLE co-administered: |
CEPHALOTHIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
25.2 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15830475/ |
3 g single, intravenous dose: 3 g route of administration: Intravenous experiment type: SINGLE co-administered: |
CEPHALOTHIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
28 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15830475/ |
3 g single, intravenous dose: 3 g route of administration: Intravenous experiment type: SINGLE co-administered: |
CEPHALOTHIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
2 g 3 times / day steady, oral Recommended Dose: 2 g, 3 times / day Route: oral Route: steady Dose: 2 g, 3 times / day Sources: |
unhealthy, 18 - 91 years n = 159 Health Status: unhealthy Condition: infections Age Group: 18 - 91 years Sex: M+F Population Size: 159 Sources: |
Disc. AE: Death, Urinary tract yeast infection... AEs leading to discontinuation/dose reduction: Death (grade 5, 13 patients) Sources: Urinary tract yeast infection (1 patient) |
1 g single, intramuscular Recommended |
healthy, 23 - 28 years n = 7 Health Status: healthy Age Group: 23 - 28 years Sex: M+F Population Size: 7 Sources: |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Urinary tract yeast infection | 1 patient Disc. AE |
2 g 3 times / day steady, oral Recommended Dose: 2 g, 3 times / day Route: oral Route: steady Dose: 2 g, 3 times / day Sources: |
unhealthy, 18 - 91 years n = 159 Health Status: unhealthy Condition: infections Age Group: 18 - 91 years Sex: M+F Population Size: 159 Sources: |
| Death | grade 5, 13 patients Disc. AE |
2 g 3 times / day steady, oral Recommended Dose: 2 g, 3 times / day Route: oral Route: steady Dose: 2 g, 3 times / day Sources: |
unhealthy, 18 - 91 years n = 159 Health Status: unhealthy Condition: infections Age Group: 18 - 91 years Sex: M+F Population Size: 159 Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Therapeutic efficacy of tobramycin--a clinical and laboratory evaluation. | 1975 Dec |
|
| Acute renal failure associated with cephalosporin therapy. | 1975 Jun |
|
| Acute interstitial nephritis. | 1976 Jan |
|
| Identification of penicillin allergenic determinants that bind IgE antibodies in the sera of subjects with penicillin allergy. | 1990 Nov |
|
| [Fosfomycin: an underrated antibiotic for urinary tract infections due to Escherichia coli]. | 2001 Dec |
|
| Antimicrobial sensitivity and adherence study in strains of coagulase-negative Staphylococcus spp. | 2001 Jul-Sep |
|
| Antimicrobial susceptibility of udder pathogens isolated from dairy herds in the west littoral region of Uruguay. | 2002 |
|
| Interaction of human organic anion transporters with various cephalosporin antibiotics. | 2002 Mar 8 |
|
| Antibiotics induce apoptosis of human peritoneal mesothelial cells. | 2003 Jun |
|
| Antimicrobial resistance in Gram-negative bacilli isolated from infant formulas. | 2003 Nov 21 |
|
| The vitro efficacy of beta-lactam and beta-lactamase inhibitors against multidrug resistant clinical strains of Mycobacterium tuberculosis. | 2004 Apr |
|
| [Necrotizing lymphadenitis caused by Nocardia asteroides in a healthy girl]. | 2004 Apr-Jun |
|
| "Streptococcus milleri" endocarditis caused by Streptococcus anginosus. | 2004 Feb |
|
| Molecular evaluation of antibiotic susceptibility of Tropheryma whipplei in axenic medium. | 2005 Feb |
|
| Antimicrobial susceptibility of bifidobacteria. | 2005 Jan |
|
| Antimicrobial resistance in Salmonella enteritidis strains isolated from broiler carcasses, food, human and poultry-related samples. | 2005 Jan 1 |
|
| [Community-acquired methicillin-resistant Staphylococcus aureus disseminated disease]. | 2006 |
|
| Occurrence and characterization of Aeromonas spp. in mussels from the Adriatic Sea. | 2006 Aug |
|
| Integron presence in a multiresistant Morganella morganii isolate. | 2006 Jun |
|
| In vivo selection of OmpK35-deficient mutant after cefuroxime therapy for primary liver abscess caused by Klebsiella pneumoniae. | 2006 Oct |
|
| Antimicrobial resistance of Yersinia enterocolitica strains from human patients, pigs and retail pork in Switzerland. | 2007 Apr 1 |
|
| Pulsed-field gel electrophoresis in the identification of the origin of bacterial keratitis caused by Pseudomonas aeruginosa. | 2007 Jul |
|
| Characterization of antimicrobial resistance patterns and class 1 integrons in Escherichia coli O26 isolated from humans and animals. | 2007 Mar |
|
| Characterization of Klebsiella pneumoniae isolates from New Zealand sea lion (Phocarctos hookeri) pups during and after the epidemics on Enderby Island, Auckland Islands. | 2007 May 16 |
|
| Campylobacter canadensis sp. nov., from captive whooping cranes in Canada. | 2007 Nov |
|
| [Review of the actions in prevention of infections in total arthroplasty of hip]. | 2007 Nov-Dec |
|
| [Integrons and their relationship with resistance phenotype in Gram negative bacilli isolated in the Hospital Torres Galdames, Iquique, Chile]. | 2007 Oct |
|
| Structure-function studies of arginine at position 276 in CTX-M beta-lactamases. | 2008 Apr |
|
| Antibiotic resistance of commensal Escherichia coli of food-producing animals from three Vojvodinian farms, Serbia. | 2008 Apr |
|
| Assay for integrons and pattern of antibiotic resistance in clinical Escherichia coli strains by PCR-RFLP in Southern Iran. | 2008 Jan |
|
| Antimicrobial resistance of Salmonella enterica isolates from apparently healthy and clinically ill finishing pigs in Spain. | 2008 May |
|
| [Antimicrobial resistance of uropathogens among outpatients, 2000-2004]. | 2008 May-Jun |
|
| Determination of cephalosporins in solid binary mixtures by polarized IR- and Raman spectroscopy. | 2008 Sep 10 |
|
| The photosynthetic apparatus and its regulation in the aerobic gammaproteobacterium Congregibacter litoralis gen. nov., sp. nov. | 2009 |
|
| Protective effect of topical antibiotics in breast augmentation. | 2009 Aug |
|
| [Are antimicrobials useful in closed thoracostomy due to trauma?]. | 2009 Jan-Feb |
|
| Rapid evolution of virulence and drug resistance in the emerging zoonotic pathogen Streptococcus suis. | 2009 Jul 15 |
|
| Effects of mosapride on motility of the small intestine and caecum in normal horses after jejunocaecostomy. | 2009 Jun |
|
| [Characterization of Listeria monocytogenes isolates obtained from raw cheese samples acquired from different Costa Rican producer zones]. | 2009 Mar |
|
| Antibacterial effects of Iranian fennel essential oil on isolates of Acinetobacter baumannii. | 2009 May 1 |
Sample Use Guides
The usual dosage range is 500 mg to 1 g of cefalotin every four to six hours. In severe infections, this may be increased by giving the injections every four hours or, when the desired response is not obtained, by raising the dose to 1 g. In lifethreatening infections, in patients with normal renal function, doses up to 2 g every four hours may be required.
Route of Administration:
Other
| Substance Class |
Chemical
Created
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Edited
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| Record UNII |
IW6KLJ5ANA
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| Record Status |
Validated (UNII)
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| Record Version |
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