Antimicrobial Activity, Pharmacokinetics, Adverse Reactions, and Therapeutic Indications of Cefoperazone

Funk, Elizabeth; Strausbaugh, Larry J.

doi:10.1002/j.1875-9114.1982.tb03186.x

Cited by 13 publications

(3 citation statements)

References 44 publications

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“…The pharmacokinetics of cefoperazone have been extensively studied after intramuscular and intravenous injection and have been reviewed by Brogden et al (1981), Neu (1981), Funk and Strausbaugh (1982), Lode (1983) and by Lyon (1983). Some reported pharmacokinetic parameters are shown in table IV.…”

Section: Ce!operazonementioning

confidence: 99%

Clinical Pharmacokinetics of the Third Generation Cephalosporins

Balant

Dayer

Auckenthaler

1985

Clinical Pharmacokinetics

106

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At the present time, the third generation cephalosporins that are already on the market or close to this point include cefsulodin, cefotaxime, cefoperazone, latamoxef, ceftriaxone, ceftazidime, ceftizoxime and cefotetan. Other newer compounds are also under development but have not been included in this review. None of the third generation compounds is suitable for oral administration and, accordingly, their pharmacokinetics have been studied only after intravenous and intramuscular administration. Microbiological assays and HPLC methods have been used for the measurement of plasma/serum, urine, bile and cerebrospinal fluid (CSF) concentrations. As found with cefotaxime, microbiological assays should only be used when the full metabolite spectrum of a particular drug is known, as otherwise, the presence of microbiologically active metabolites may lead to erroneous conclusions. Under normal conditions, the major route of elimination is via the kidneys for cefsulodin, latamoxef, ceftazidime, ceftizoxime and cefotetan. In contrast, cefoperazone is mainly eliminated in the bile, whereas cefotaxime and ceftriaxone depend both on the liver and the kidneys for their elimination. With the exception of ceftriaxone, which has a longer elimination half-life (i.e. around 8 hours), all the other third generation cephalosporins have a t1/2 ranging between 1.5 and 2.5 hours. Plasma protein binding is variable from one compound to another. However, the clinical relevance of this parameter is not clearly established since tissue penetration also depends on the relative affinity of the drug for tissue components. Third generation cephalosporins seem to penetrate adequately into the CSF and, thus pharmacokinetically appear to be appropriate agents for the treatment of meningitis. The degree of modification of pharmacokinetic parameters by renal insufficiency or hepatic diseases depends, as for other drugs, on the extent to which the compound is excreted via the kidneys or the liver. The third generation cephalosporins have been extensively studied under these conditions and recommendations for dosage modification in special circumstances are available for most of them. The pharmacokinetics of some third generation cephalosporins may be modified in neonates and elderly patients. Accordingly, their use at the extremes of age must be accompanied by a closer than usual clinical monitoring of the patient. From a clinical point of view, the third generation cephalosporins possess reliable pharmacokinetic properties.(ABSTRACT TRUNCATED AT 400 WORDS)

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Section: Ce!operazonementioning

confidence: 99%

Clinical Pharmacokinetics of the Third Generation Cephalosporins

Balant

Dayer

Auckenthaler

1985

Clinical Pharmacokinetics

106

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“…The ligand was further stabilized through a π−π stacking interaction with His41 and an HB and a salt-bridge with Glu166, which is essential for keeping the S1 pocket in the correct shape and the enzyme in the active conformation. 6 Concerning cefaclor binding mode, the oxygen of its β-lactam ring was bound to histidine at position 41, also involved in a π−π stacking interaction with the phenyl ring of the drug (Figure 1B), while cefadroxil and cefoperazone, two broad-spectrum antiobiotic agents used in the treatment of respiratory tract infections, peritonitis, skin infections, endometritis, and bacterial septicaemia, 42 were found to establish pivotal HBs with Cys145 and Glu166. Moreover, the phenol OH group of both cefadroxil and cefoperazone was involved in 2 HBs with Thr190 and Gln192.…”

Section: ■ Results and Discussionmentioning

confidence: 99%

Targeting SARS-CoV-2 Main Protease: A Successful Story Guided by an In Silico Drug Repurposing Approach

Ambrosio

Costa

Romeo

et al. 2023

J. Chem. Inf. Model.

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The SARS-CoV-2 main protease (M pro ) is a crucial enzyme for viral replication and has been considered an attractive drug target for the treatment of COVID-19. In this study, virtual screening techniques and in vitro assays were combined to identify novel M pro inhibitors starting from around 8000 FDA-approved drugs. The docking analysis highlighted 17 promising best hits, biologically characterized in terms of their M pro inhibitory activity. Among them, 7 cephalosporins and the oral anticoagulant betrixaban were able to block the enzyme activity in the micromolar range with no cytotoxic effect at the highest concentration tested. After the evaluation of the degree of conservation of M pro residues involved in the binding with the studied ligands, the ligands' activity on SARS-CoV-2 replication was assessed. The ability of betrixaban to affect SARS-CoV-2 replication associated to its antithrombotic effect could pave the way for its possible use in the treatment of hospitalized COVID-19 patients.

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“…The mostly prescribed dose is 1g followed by 2g BD (5). Preference of ceftriaxone was maybe due to its widest spectrum of activity, good penetration into CSF andproven less harmful in vast of population.Commonly prescribed dose was 1g according to collected results and preferable route of administration was I.V this was because of the fact I.M route is not considering suitable for administration of large doses and may cause injection site swelling (8). The use of cephalosporin was found to be high for the treatment of CNS infections except meningitis (21.9%) followed by respiratory tract infections (14.4%), abdominal infections (7.5%), Urinary tract infection (5.6%), meningitis (5.6%), ENT (5%), bone and joint disorders (1.9%), sepsis (1.3%).…”

Section: Discussionmentioning

confidence: 99%

RATIONAL USE OF 3rd GENERATION CEPHALOSPORINS IN TERTIARY CARE HOSPITALS: A CONCURRENT DUR

2022

IJPIHS

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Background: Assessment of use of antimicrobials can be performed by evaluating their use. Drug use evaluation is a performance improvement method that concentrates on improvement and evaluation of drug use processes to achieve optimal patient outcomes. Objective: The objective of this study was the evaluation of 3rd generation cephalosporins in tertiary care hospitals of Lahore. Method: A concurrent cross-sectional study was conducted on 160 patient files selected using systematic random sampling method from in-patient prescriptions with 3rd generation cephalosporin during hospitalization in tertiary care hospitals. Descriptive statistics were applied by using IBM SPSS statistics version 28. Results: Out of the 200 patient file, 160 patient files have complete information of the prescribed drug. Among the 160 patients, 67(41%) were female and 93(58.1%) males. Among 160 patients, 141(88.1%) Ceftriaxone was most commonly prescribed drug followed by 14(8.8%) Cefoperazone (in combination with salbactam) the 5(3.1%) were given cefixime and in indications for drug being prescribed 103(64.5%) were found to be appropriate while 57(35.5%) were inappropriate. (Not according to the WHO criteria for prescribing the third-generation cephalosporin). Conclusions: To improve the rational use of 3 rd generation cephalosporins and prevent the development of resistance; prescribers should adhere to the national standard treatment guideline.

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Antimicrobial Activity, Pharmacokinetics, Adverse Reactions, and Therapeutic Indications of Cefoperazone

Cited by 13 publications

References 44 publications

Clinical Pharmacokinetics of the Third Generation Cephalosporins

Clinical Pharmacokinetics of the Third Generation Cephalosporins

Targeting SARS-CoV-2 Main Protease: A Successful Story Guided by an In Silico Drug Repurposing Approach

RATIONAL USE OF 3rd GENERATION CEPHALOSPORINS IN TERTIARY CARE HOSPITALS: A CONCURRENT DUR

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