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Three-ways crossover bioequivalence study of cephalexin in healthy Malay volunteers

Liew KB, Peh KK, Loh GO, Tan YT

Drug Dev Ind Pharm, 2014 Sep;40(9):1156-62.
PMID: 23688276 DOI: 10.3109/03639045.2013.798805

Although the general pharmacokinetics of cephalexin is quite established up-to-date, however, no population-based study on Cephalexin pharmacokinetics profile in Malay population has been reported yet in the literature.

Matched MeSH terms: Cephalexin/pharmacokinetics*
Optimizing of pharmaceutical active compounds biodegradability in secondary effluents by β-lactamase from Bacillus subtilis using central composite design

Al-Gheethi A, Noman E, Radin Mohamed RMS, Ismail N, Bin Abdullah AH, Mohd Kassim AH

J Hazard Mater, 2019 03 05;365:883-894.
PMID: 30497042 DOI: 10.1016/j.jhazmat.2018.11.068

Biodegradation of pharmaceuticals active compounds (PACs) in secondary effluents by using B. subtilis 2012WTNC as a function of β-lactamase was optimized using response surface methodology (RSM) designed by central composite design (CCD). Four factors including initial concentration of bacteria (1-6 log10 CFU mL-1), incubation period (1-14 days), incubation temperature (20-40 °C) and initial concentration of PACs (1-5 mg L-1) were investigated. The optimal operating factors for biodegradation process determined using response surface methodology (RSM) was recorded with 5.57 log10 CFU mL-1 of B. subtilis, for 10.38 days, at 36.62 °C and with 4.14 mg L-1 of (cephalexin/amoxicillin) with R2 coefficient of 0.99. The biodegradation was 83.81 and 93.94% respectively. The relationship among the independent variables was significant (p cephalexin against E. coli and S. aureus after degradation using B. subtilis which reflects the higher potential of bacteria to biodegrade PACs in secondary effluents. B. subtilis has the potential for biodegradation of PACs in the secondary effluents.

Matched MeSH terms: Cephalexin/metabolism*; Cephalexin/pharmacology
Cephalexin removal by a novel Cu-Zn bionanocomposite biosynthesized in secondary metabolic products of Aspergillus arenarioides EAN603 with pumpkin peels medium: Optimization, kinetic and artificial neural network models

Al-Gheethi A, Noman E, Saphira Radin Mohamed RM, Talip B, Vo DN, Algaifi HA

J Hazard Mater, 2021 10 05;419:126500.
PMID: 34214856 DOI: 10.1016/j.jhazmat.2021.126500

The present study aimed to investigate the removal efficiency of cephalexin (CFX) by a novel Cu-Zn bionanocomposite biosynthesized in the secondary metabolic products of Aspergillus arenarioides EAN603 with pumpkin peels medium (CZ-BNC-APP). The optimization study was performed based on CFX concentrations (1, 10.5 and 20 ppm); CZ-BNC-APP dosage (10, 55 and 100 mg/L); time (10, 55 and 100 min), temperature (20, 32.5 and 45 °C). The artificial neural network (ANN) model was used to understand the CFX behavior for the factors affecting removal process. The CZ-BNC-APP showed an irregular shape with porous structure and size between 20 and 80 nm. The FTIR detected CC, C-O and OH groups. ANN model revealed that CZ-BNC-APP dosage exhibited the vital role in the removal process, while the removal process having a thermodynamic nature. The CFX removal was optimized with 12.41 ppm CFX, 60.60 mg/L of CZ-BNC-APP, after 97.55 min and at 35 °C, the real maximum removal was 95.53% with 100.52 mg g-1 of the maximum adsorption capacity and 99.5% of the coefficient. The adsorption of CFX on CZ-BNC-APP was fitted with pseudo-second-order model and both Langmuir and Freundlich isotherms models. These findings revealed that CZ-BNC-APP exhibited high potential to remove CFX.

Matched MeSH terms: Cephalexin
Interethnic differences of PEPT2 (SLC15A2) polymorphism distribution and associations with cephalexin pharmacokinetics in healthy Asian subjects

Liu R, Tang AM, Tan YL, Limenta LM, Lee EJ

Eur J Clin Pharmacol, 2009 Jan;65(1):65-70.
PMID: 18766334 DOI: 10.1007/s00228-008-0488-4

OBJECTIVES: The aims of this study were to characterize the population frequency of PEPT2 (SLC15A2) polymorphic variants in three Asian ethnic populations, namely Chinese, Malay and Asian Indian, and to investigate the associations of ethnicity (Chinese vs. Asian Indian), PEPT2 haplotype and cephalexin pharmacokinetics in healthy Asian subjects.
METHODS: PEPT2 polymorphisms were screened from a cohort of 96 Chinese, 96 Malay and 96 Asian Indian subjects. Cephalexin (1000 mg, orally) pharmacokinetics was characterized in an additional 15 Chinese and 15 Asian Indian healthy subjects. These 30 subjects were subsequently genotyped for their PEPT2 polymorphisms.
RESULTS: In total, ten common single nucleotide polymorphisms (SNPs) were detected in the three populations, forming two PEPT2 haplotypes. There were significant ethnic differences in PEPT2 haplotype distribution: the frequencies of the *1 and *2 alleles were 0.307 and 0.693 in the Chinese population, 0.495 and 0.505 in the Malay population and 0.729 and 0.271 in Asian Indian population, respectively. The C (max) of cephalexin was significantly lower in the Chinese (29.80 +/- 4.09 microg ml(-1)) population than in the Asian Indian one (33.29 +/- 4.97 microg ml(-1); P = 0.045). This difference could be explained by the higher average body weight of the Chinese population. There was no other significant difference in cephalexin pharmacokinetics between either ethnic or PEPT2 genotype groups.
CONCLUSION: PEPT2 polymorphism distributions differ significantly between Chinese, Malay and Asian Indian populations. However, cephalexin pharmacokinetics is not meaningfully different between Chinese and Asian Indians. The association between the PEPT2 haplotype and cephalexin pharmacokinetics could not be confirmed, and future studies under better controlled conditions are needed.

Matched MeSH terms: Cephalexin/administration & dosage; Cephalexin/pharmacokinetics*
Single-step pyrolysis of phosphoric acid-activated chitin for efficient adsorption of cephalexin antibiotic

Khanday WA, Ahmed MJ, Okoye PU, Hummadi EH, Hameed BH

Bioresour Technol, 2019 May;280:255-259.
PMID: 30772638 DOI: 10.1016/j.biortech.2019.02.003

Cephalexin (CFX) antibiotic, a potent pharmaceutical water pollutant, was efficiently removed by activated carbon (AC) derived from a single-step pyrolysis of phosphoric acid-activated chitin. Experimental conditions such as temperature, CFX initial concentration, and solution pH were screened in batch adsorption. Phosphoric acid activation of chitin and subsequent pyrolysis tailored the Brunauer-Emmett-Teller surface area, total pore volume, and average pore diameter to 1199.02 m2/g, 0.641 cm3/g, and 21.37 Å, respectively. The Langmuir isotherm adequately described the equilibrium data for CFX adsorption on chitin-AC, with an R2 of 0.99 and a monolayer capacity of 245.19 mg/g at 50 °C. Chitin-AC showed higher adsorption capacity compared with other ACs derived from industrial and agricultural precursors. When activated by phosphoric acid, chitin-AC featured functional multi-sites for vast antibiotic adsorption treatment. Overall, chitin-AC could be a promising adsorbent for removal of CFX.

Matched MeSH terms: Cephalexin
Fulltext Single-dose oral treatment with cefaclor for men with uncomplicated gonococcal urethritis

Lim HB

Med J Malaysia, 1984 Dec;39(4):272-4.
PMID: 6400040

Sixty patients with uncomplicated gonococcal urethritis were treated with a single dose oral regime comprising 3 g of cefaclor and 1 g of probenecid. Forty-eight patients (80%) returned for follow-up and the overall cure rate among them was 91.6%. Among the isolates, 25 (41.7%) showed penicillinase producing Neisseria gonorrhoeae (PPNG) strains. The cure rate for patients infected with PPNG was 85% while the cure rate for non-PPNG was 96.4%. Further work is required to establish the optimum dosage for this particular regimen.

Matched MeSH terms: Cephalexin/analogs & derivatives*
Fulltext Genotypic to Phenotypic Resistance Discrepancies Identified Involving β-Lactamase Genes, blaKPC, blaIMP, blaNDM-1, and blaVIM in Uropathogenic Klebsiella pneumoniae

Urmi UL, Nahar S, Rana M, Sultana F, Jahan N, Hossain B, et al.

Infect Drug Resist, 2020;13:2863-2875.
PMID: 32903880 DOI: 10.2147/IDR.S262493

Introduction: Klebsiella pneumoniae carbapenemase (KPC) belongs to the Group-A β-lactamases that incorporate serine at their active site and hydrolyze various penicillins, cephalosporins, and carbapenems. Metallo-beta-lactamases (MBLs) are group-B enzymes that contain one or two essential zinc ions in the active sites and hydrolyze almost all clinically available β-lactam antibiotics. Klebsiella pneumoniae remains the pathogen with the most antimicrobial resistance to KPC and MBLs.
Methods: This research investigated the blaKPC, and MBL genes, namely, blaIMP, blaVIM, and blaNDM-1 and their phenotypic resistance to K. pneumoniae isolated from urinary tract infections (UTI) in Bangladesh. Isolated UTI K. pneumoniae were identified by API-20E and 16s rDNA gene analysis. Their phenotypic antimicrobial resistance was examined by the Kirby-Bauer disc diffusion method, followed by minimal inhibitory concentration (MIC) determination. blaKPC, blaIMP, blaNDM-1, and blaVIM genes were evaluated by polymerase chain reactions (PCR) and confirmed by sequencing.
Results: Fifty-eight K. pneumoniae were identified from 142 acute UTI cases. Their phenotypic resistance to amoxycillin-clavulanic acid, cephalexin, cefuroxime, ceftriaxone, and imipenem were 98.3%, 100%, 96.5%, 91.4%, 75.1%, respectively. Over half (31/58) of the isolates contained either blaKPC or one of the MBL genes. Individual prevalence of blaKPC, blaIMP, blaNDM-1, and blaVIM were 15.5% (9), 10.3% (6), 22.4% (13), and 19% (11), respectively. Of these, eight isolates (25.8%, 8/31) were found to have two genes in four different combinations. The co-existence of the ESBL genes generated more resistance than each one individually. Some isolates appeared phenotypically susceptible to imipenem in the presence of blaKPC, blaIMP, blaVIM, and blaNDM-1 genes, singly or in combination.
Conclusion: The discrepancy of genotype and phenotype resistance has significant consequences for clinical bacteriology, precision in diagnosis, the prudent selection of antimicrobials, and rational prescribing. Heterogeneous phenotypes of antimicrobial susceptibility testing should be taken seriously to avoid inappropriate diagnostic and therapeutic decisions.

Matched MeSH terms: Cephalexin