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PubMed2004

Effect of insulin on cephalexin uptake and transepithelial transport in the human intestinal cell line Caco-2.

We investigated whether cephalexin transport in Caco-2 cells is regulated by insulin. After the insulin pretreatment, cephalexin uptake, and transport as well as PEPT1 mRNA and protein expression in the cells were measured. Cephalexin uptake was significantly increased by the insulin pretreatment. Insulin significantly increased cephalexin saturable uptake, but had no significant effect on the non-saturable one. PEPT1 protein expression on the apical membrane, but not PEPT1 mRNA expression, was increased by the insulin pretreatment. The enhancement of cephalexin uptake by the insulin pretreatment was inhibited by genistein, a tyrosine kinase inhibitor, and colchicine, an agent that disrupts protein translocation. Apical-to-basolateral transport of cephalexin has increased by the insulin pretreatment at the apical side and long-term insulin pretreatment at the basolateral side. It is considered that insulin mainly binds to its receptor on the apical and basolateral membranes, thereby promoting PEPT1 translocation from the intracellular pool to the apical membrane surface; consequently, PEPT1 protein expression on the apical membrane is increased.

Biological Transport↗
PubMed1995

Mechanisms of transport of quinapril in Caco-2 cell monolayers: comparison with cephalexin.

PURPOSE: To determine the transport mechanisms of quinapril and cephalexin in Caco-2 cell monolayers, a cell culture model of the human small intestinal epithelium. METHODS: Uptake, transepithelial transport and intracellular accumulations of these two drugs were measured using Caco-2 cell monolayers grown onto Millicells and magnetically stirred diffusion chambers. RESULTS: Transepithelial transport, apical (AP)4 uptake and intracellular accumulation of both drugs depended on the maintenance of a transepithelial proton gradient and temperature of the medium. However, quinapril transport and accumulation, which did not display a maximum at approximately pH 6, was more sensitive to proton gradient change, whereas cephalexin transport was more sensitive to concentration change (range 0.5-5 mM). In addition, quinapril (1 mM) transport was decreased significantly (p < 0.05) by 10 mM cephalexin, loracarbef, Gly-Pro and Phe-Pro, but not by enalapril; whereas cephalexin (0.1 mM) transport was decreased significantly (p < 0.05) by all four compounds. Similarly, AP quinapril (1 mM) uptake was also decreased by 10 mM loracarbef, Gly-Pro, cephalexin, and enalapril, but these inhibitory effects (20-50%) were quantitatively less than their inhibitory effects on cephalexin uptake (50-90%). Finally, the AP uptake of quinapril was also significantly (p < 0.05) inhibited by FCCP (10 micrograms/ml), amiloride (0.5 mM), DEP (0.5 mM), and staurosporine (5 nM). CONCLUSIONS: The transport of quinapril in the Caco-2 cells is via a combination of the carrier-mediated proton gradient-dependent peptide transporter and passive diffusion.

Amino Acid Sequence↗
PubMed1999

Absorption kinetics and bioavailability of cephalexin in the dog after oral and intramuscular administration.

The pharmacokinetics of cephalexin, a first generation cephalosporin, were investigated in dogs using two formulations marketed for humans, but also often employed by practitioners for pet therapy. Cephalexin was administered to five dogs intravenously and intramuscularly as a sodium salt and by the oral route as a monohydrate. The dosage was always 20 mg/kg of active ingredient. A microbiological assay with Sarcina lutea as the test organism was adopted to measure cephalexin concentrations in serum. The mean residence time (MRT) median values after intravenous (i.v.), intramuscular (i.m.) and oral administration (p.o.) were 86 min, 200 min, and 279 min, respectively. After i.m. and oral dosing the peak serum concentrations (24.2 +/- 1.8 micrograms/mL and 20.3 +/- 1.7 micrograms/mL, respectively) were attained at 90 min in all dogs and bioavailabilities were 63 +/- 10% and 57 +/- 5%, respectively. The time course of the cephalexin serum concentrations after oral administration was best described by a model incorporating saturable absorption kinetics of the Michaelis-Menten type: thus in the gastrointestinal tract of dogs a carrier mediated transport for cephalexin similar to that reported in humans, may exist. The predicted average serum concentrations of cephalexin after repeated i.m. and oral administration indicated that, in order to maintain the therapeutic concentrations, the 20 mg/kg b.w. dosage should be administered every 6-8 h.

Absorption↗
PubMed1983

Comparison of pharmacokinetics of sodium and lysine cephalexin in calves.

The pharmacokinetics of sodium and lysine cephalexins were investigated after intravenous and intramuscular administration of a single dose rate of 30 mg.kg-1 body weight in calves. The data for the two salts administered intravenously were pooled, the resulting pharmacokinetic disposition of cephalexin indicating a distribution half-time (t1/2 alpha) and an elimination half-time (t1/2 beta) of 9.78 and 62.0 min, respectively. Following intramuscular administration some pharmacokinetic differences were recorded between the cephalexin preparations: lysine cephalexin was more rapidly eliminated (t1/2kel = 55.2 min) than sodium cephalexin (t1/2kel = 89.8 min), although the peak blood level was higher and attained after a longer time with lysine cephalexin.

Animals↗
PubMed1977

Comparison of pharmacological and antimicrobial properties of cefadroxil and cephalexin.

Pharmacological and antimicrobial properties of cefadroxil, a new cephalosporin antibiotic, were compared with cephalexin. Absorption and excretion were studied in 20 healthy men. Peak concentrations of the drugs in serum were similar after ingestion of single 500-mg tablets. The concentration of cefadroxil in serum was more sustained than that of cephalexin. Levels of cefadroxil in serum after a dose of 1,000 mg were approximately twice those after a 500-mg dose through 6 h. Each drug administered in a dose of 500 mg every 6 h for 24 h resulted in concentrations in serum that were similar to a single dose without accumulation. Ninety-three percent of the cefadroxil and 85% of the cephalexin were excreted in urine after ingestions of single 500-mg tablets. The urine concentration of cefadroxil was more sustained than cephalexin. Minimal inhibitory and minimal bactericidal concentrations for clinical isolates were comparable with each drug. Cefadroxil compares favorably with cephalexin in this study. Sustained levels of cefadroxil in serum and urine suggest that this drug may be given at less frequent intervals than cephalexin.

Adult↗
PubMed1975

Comparative efficacy of cephalexin and ampicillin for shigellosis and other types of acute diarrhea in infants and children.

Most ampicillin-resistant Shigella are susceptible to cephalexin. Randomized treatment with cephalexin or ampicillin was given to 154 infants and children with acute diarrhea. Rectal swab cultures revealed Shigella in 42%, Salmonella in 6%, enteropathogenic Escherichia coli in 2%, and no pathogen in 50%. Cephalexin failed to eradicate Shigella after 5 days of treatment in 76% of patients as contrasted with 28% of ampicillin-treated patients with susceptible organisms. Shigella persisted in 78% of ampicillin-treated patients with resistant organisms. Diarrhea lasted more than 5 days in 43% of cephalexin-treated patients, in 56% of the ampicillin group with resistant organisms, but in only 9% of ampicillin-treated patients with susceptible organisms. The failure of cephalexin was due to the relatively high minimal inhibitory concentrations and minimal bacterial concentrations of 5 or 10 mug/ml and, although serum concentrations were twice the minimal bacterial concentration, they were not sufficient to demonstrate killing by the serum dilution method. In vitro susceptibility or resistance of Shigella to ampicillin correlated with clinical success or failure. Cephalexin is not a suitable drug for treatment of shigellosis in patients with ampicillin-resistant organisms.

Ampicillin↗
PubMed1990

Anti-cephalexin monoclonal antibodies and their cross-reactivities to cephems and penams.

Three cell lines producing monoclonal antibodies (MAbs), Cep1-2, 2-2 and 6, against cephalexin were established and the immunoglobulin class of the MAbs was IgM. The cross-reactions of the MAbs with penams and cephems were examined by enzyme-linked immunosorbent assay (ELISA). The cross-reactivities of Cep1-2 and 2-2 were scarcely influenced by the structures of acyl side chains of cephems and penams. The cross-reactivities of Cep1-2 were affected by the presence or absence of dihydrothiazolidine ring of cephem nucleus in hapten-protein conjugates which were prepared by alkaline method, MBS method and activated ester method but the cross-reactivities of Cep2-2 were not. The findings suggest that Cep1-2 recognize the degradate product(s) of cephem nucleus and Cep2-2 recognize a new antigenic determinant (NAD), which is formed by the conjugation of beta-lactam and carrier protein. On the other hand, the cross-reactivities of Cep6 were influenced by the structure of amino acyl side chain. It seems that Cep6 recognize specifically the acyl side chain at the C-7 of cephem. In ELISA inhibition test, three MAbs showed different inhibition pattern. The reaction of Cep1-2 with cephalexin-HSA was inhibited by cephalexin lysate. Cep2-2 and Cep6 were weakly inhibited by the binding to cephalexin-HSA by cephalexin lysate. Furthermore, the reactions of all MAbs were remarkably inhibited by penicillamine. The above results indicate that the MAbs can recognize at least three epitopes of the degradate product(s) of cephem nucleus, NAD and acyl side chain in cephalexin-protein conjugate.

Animals↗
PubMed1991

Clinical comparison of cefuroxime axetil, cephalexin and cefadroxil in the treatment of patients with primary infections of the skin or skin structures.

This study was designed to compare the clinical and bacteriological efficacy of three oral cephalosporins, cefuroxime axetil, cephalexin and cefadroxil, in the treatment of patients with mild to moderate infections of the skin or skin structures. A total of 330 patients were enrolled at 10 centers and were randomly assigned to receive cefuroxime axetil 250 mg (n = 107), cephalexin 500 mg (n = 111) or cefadroxil 500 mg (n = 112), twice daily for 10 days. Patients were assessed for their clinical and bacteriological responses once during treatment (3-5 days) and twice after treatment (1-3 and 10-14 days). A total of 353 bacterial isolates were obtained: Staphylococcus aureus (41%), Staphylococcus epidermidis (33%) and Streptococcus pyogenes (5%). A satisfactory clinical outcome (cure or improvement) was achieved in 97% (89/92), 89% (80/90) and 94% (82/87) of the clinically evaluable patients treated with cefuroxime axetil, cephalexin or cefadroxil, respectively (p = 0.047, cefuroxime axetil vs. cephalexin). With respect to the eradication of the bacterial pathogens, a satisfactory outcome (cure or presumed cure) was obtained in 96% (69/72), 85% (60/71) and 93% (63/68) of bacteriologically evaluable patients treated with cefuroxime axetil, cephalexin and cefadroxil, respectively (p = 0.026, cefuroxime axetil vs. cephalexin). All three study drugs were well tolerated, with adverse events affecting the gastrointestinal system most commonly reported. There were no significant differences between treatment groups in the incidence of drug-related adverse events.

Adolescent↗
PubMed1987

Transport mechanism of cephalexin in isolated hepatocytes.

By using isolated rat hepatocytes, the mechanism of uptake of a zwitterionic beta-lactam antibiotic, cephalexin, was clarified. The uptake followed the combination of saturable carrier-mediated and nonsaturable first-order rate processes. The kinetic parameters were estimated as follows (mean +/- SD): maximum uptake rate (Vmax), 2.28 +/- 0.24 nmol/min/mg of protein; Michaelis constant (Kt), 6.28 +/- 0.31 mM and first-order rate constant (kd), 0.11 +/- 0.012 nmol/min/mg of protein/mM. There was no inhibitory effect by amino acids, dipeptides or organic cations, whereas an organic anion, probenecid, markedly inhibited the hepatic uptake of cephalexin. Several beta-lactam antibiotics including zwitterionic and anionic derivatives inhibited cephalexin uptake significantly. The inhibition kinetics revealed that benzylpenicillin and the stereo-isomer l-cephalexin competitively inhibited cephalexin uptake. Furthermore, the efflux of cephalexin from the cells was stimulated by adding benzylpenicillin in the extracellular medium. These results demonstrated that all beta-lactam antibiotics have a common transport system with an organic anion such as probenecid, irrespective of their ionic charges, though a cationic charge on the molecule is less advantageous for being recognized by the carrier system.

Amino Acids↗
PubMed2002

Effect of cephalexin on the pharmacokinetics of metformin in healthy human volunteers.

The purpose of this study was to assess the effect of a single dose of cephalexin on the pharmacokinetics of metformin in healthy human volunteers. A 2 x 2 double blind randomized crossover study was conducted in 12 healthy human volunteers. Each subject received orally either 500 mg of metformin with a placebo or a combination of 500 mg of metformin and 500 mg of cephalexin. Serum and urine levels of metformin were estimated by a validated HPLC method. The systemic disposition of metformin was altered by the co-administration of cephalexin. Cephalexin increased Cmax and AUC by an average of 34% and 24%, respectively, and reduced renal clearance to 14%. The renal clearance of metformin was reduced in a time-dependent manner in the presence of cephalexin. Hence, it is concluded that cephalexin inhibits the renal tubular secretion of metformin resulting in higher circulating serum concentrations.

Area Under Curve↗
PubMedDate not supplied

Formulation and release kinetics of cephalexin monohydrate from biodegradable polymeric microspheres.

Sustained release cephalexin microspheres have been formulated with poly(L-lactic acid) for intraperitoneal administration. Microspheres were prepared with spray-dried cephalexin by phase separation in organic solvent containing a fixed concentration of polymer, then sieve-sized. Batch-to-batch reproducibility of microsphere size distribution and encapsulation efficiency ( > 95%) were demonstrated. The quality of the microspheres was dependent on the rate of stirring during preparation and was highest as 400 rpm. Scanning electron micrographs revealed approximately spherical shapes and porous surfaces. The release of cephalexin followed second order dissolution model kinetics for multiparticulate systems. The apparent second order rate constant, k2, was lowest for the highest sieve-size fraction (250-425 microns) and varied with drug loading reaching a minimum at 33% w/w. A lower molecular weight PLA of 50 000 produced a faster release of cephalexin from microspheres. Cephalexin was released from microspheres for at least 4 h compared to only 10 min for complete dissolution of an equivalent weight of cephalexin powder, indicating sustained release which may be appropriate in treating localized infections.

Cephalexin↗
PubMed2000

Moxifloxacin versus cephalexin in the treatment of uncomplicated skin infections.

The efficacy and safety of oral moxifloxacin (400 mg once daily, 7 days) versus cephalexin (500 mg three times daily, 7 days) were compared in a prospective, multicentre, randomised, double-blind trial in 401 adults with uncomplicated skin infections. Clinical outcome was evaluated in 351 patients. Moxifloxacin proved to be as effective as cephalexin both clinically (90% versus 91%, respectively) and bacteriologically in eradicating the most frequently isolated pathogen Staphylococcus aureus (92% and 93%, respectively). Moxifloxacin was more effective than cephalexin in eliminating Streptococcus spp. (90% and 82%, respectively). Drug-related adverse events were comparable in both treatment groups with the most frequently reported being nausea in the moxifloxacin-treated patients and headache in the cephalexin-treated patients. Medication was discontinued due to unwanted reactions in 3% of the moxifloxacin- and 4% of the cephalexin-treated patients. Moxifloxacin, 400 mg once daily for 7 days, is as safe and effective as cephalexin 500 mg three times daily for 7 days in the treatment of uncomplicated skin infections.

Adolescent↗
PubMed2001

Correlation between epithelial cell permeability of cephalexin and expression of intestinal oligopeptide transporter.

The proton-coupled oligopeptide transporter (PEPT1) has been shown to mediate mucosal cell transport of di- and tripeptide, and some peptidomimetic drugs. In this study, we determined the correlation between PEPT1 protein expression and the permeability of cephalexin, a substrate of PEPT1, in human PEPT1 (hPEPT1)-overexpressed Caco-2 cells (Caco-2/hPEPT1 cells) and rat jejunum. Caco-2/hPEPT1 cells with various levels of hPEPT1 expression were established by an adenoviral transfection system. The effective intestinal permeability (P(eff)) in rat jejunum was evaluated using a single pass in situ perfusion method. The level of PEPT1 in Caco-2/hPEPT1 cells and rat intestinal mucosal samples was quantitated by densitometry after immunoblotting and enhanced chemiluminescence detection. In Caco-2/hPEPT1 cells, an excellent correlation was observed between cephalexin uptake and hPEPT1 expression (R2 = 0.96, P < 0.005). This demonstrates that cephalexin uptake is directly proportional to hPEPT1 expression. In the rat perfusion study, the mean P(eff) +/- S.D. (n = 15) of cephalexin was 3.89 +/- 1.63 x 10(-5) cm/s. A very significant correlation between PEPT1 expression and cephalexin permeability with an R2 = 0.63 (P < 0.001) was observed. This indicates that the variation in PEPT1 expression is one of the major factors accounting for variable intestinal cephalexin absorption. To our knowledge, this is the most direct evidence that variation of PEPT1 expression is correlated with absorption permeability variation of peptide-like compounds in vitro and in vivo.

Algorithms↗
PubMed1988

Stability of cephalexin monohydrate suspension in polypropylene oral syringes.

The stability of cephalexin monohydrate suspension in plastic oral syringes was studied. Commercially available cephalexin monohydrate powder for oral administration was reconstituted according to the manufacturer's instructions and stored in the original containers or drawn into 5-mL clear polypropylene oral syringes. The original containers and syringes were divided into groups and stored at -20, 4, 25, 40, 60, or 80 degrees C. Powder from two additional lots was similarly reconstituted and packaged; these original containers and syringes were stored at 80 degrees C only to assess interlot variability. Immediately after reconstitution and at specified times during storage, three syringes and the corresponding three original containers stored at each temperature were removed, and their contents were analyzed for cephalexin concentration using the standard USP iodometric assay for antibiotics. The stability-indicating nature of the assay was documented. Cephalexin monohydrate followed a first-order rate of degradation at temperatures of 40, 60, and 80 degrees C. At temperatures of -20, 4, and 25 degrees C, cephalexin monohydrate exhibited no appreciable degradation during the 90-day study period. Cephalexin monohydrate suspension reconstituted from powder as a suspension and repackaged in clear polypropylene oral syringes was stable for 90 days when stored under ambient, refrigerated, and frozen conditions.

Administration, Oral↗
PubMed1987

[The effect of cephalexin on thrombocyte function in diabetics and normal persons].

Studies on the Effect of Cephalexin on Platelet Functions in Diabetics and Healthy Volunteers. The effect of cephalexin (Ceporexin) on platelet functions of diabetics with proliferative retinopathy and of healthy volunteers was studied. Cephalexin, 3 X 1 g for 7 days, reduced epinephrine- and collagen-induced platelet aggregation of the diabetics in a significant, but clinically not relevant manner. Platelet factor-3 availability and retraction remained unaffected by treatment with cephalexin. Cephalexin in vitro in a concentration of 500 mg/l reduced the rate and peak amplitude of platelet aggregation in diabetics and healthy volunteers to the same extent. The in vitro inhibition of epinephrine- and collagen-induced platelet aggregation was lacking clinical relevance. Platelet factor-3 availability was not changed by addition of cephalexin in vitro; the retraction was significantly increased, however, without clinical relevance.

Adult↗
PubMed1998

Mupirocin cream is as effective as oral cephalexin in the treatment of secondarily infected wounds.

BACKGROUND: Topical antimicrobials have been considered for treatment of secondarily infected wounds because of the potential for reduced risk of adverse effects and greater patient convenience. We compared mupirocin cream with oral cephalexin in the treatment of wounds such as small lacerations, abrasions, or sutured wounds. METHODS: In 2 identical randomized double-blind studies, 706 patients with secondarily infected wounds (small lacerations, abrasions, or sutured wounds) received either mupirocin cream topically 3 times daily or cephalexin orally 4 times daily for 10 days. RESULTS: Clinical success at follow-up was equivalent in the two groups: 95.1% and 95.3% in the mupirocin cream and the cephalexin groups, respectively (95% confidence interval [CI], -4.0% to 3.6%; P = .89). The intention-to-treat success rate was 83% in both groups. Bacteriologic success at follow-up was also comparable: 96.9% in the mupirocin cream and 98.9% in the cephalexin groups (95% CI, -6.0% to 2.0%; P = .22). The occurrence of adverse experiences related to study treatment was similar for the 2 groups, with fewer patients in the mupirocin cream group reporting diarrhea (1.1% vs 2.3% for cephalexin). CONCLUSIONS: Mupirocin cream applied topically 3 times daily is as effective as oral cephalexin given 4 times daily for the treatment of secondarily infected wounds and was well tolerated.

Administration, Cutaneous↗
PubMed2002

A two-step, one-pot enzymatic synthesis of cephalexin from D-phenylglycine nitrile.

A cascade of two enzymatic transformations is employed in a one-pot synthesis of cephalexin. The nitrile hydratase (from R. rhodochrous MAWE)-catalyzed hydration of D-phenylglycine nitrile to the corresponding amide was combined with the penicillin G acylase (penicillin amidohydrolase, E.C. 3.5.1.11)-catalyzed acylation of 7-ADCA with the in situ-formed amide to afford a two-step, one-pot synthesis of cephalexin. D-Phenylglycine nitrile appeared to have a remarkable selective inhibitory effect on the penicillin G acylase, resulting in a threefold increase in the synthesis/hydrolysis (S/H) ratio. 1,5-Dihydroxynaphthalene, when added to the reaction mixture, cocrystallized with cephalexin. The resulting low cephalexin concentration prevented its chemical as well as enzymatic degradation; cephalexin was obtained at 79% yield with an S/H ratio of 7.7.

Acetonitriles↗
PubMed1990

Uptake of the cephalosporin, cephalexin, by a dipeptide transport carrier in the human intestinal cell line, Caco-2.

The transport of the orally absorbed cephalosporin, cephalexin, was examined in the human epithelial cell line, Caco-2 that possesses intestinal enterocyte-like properties when cultured. In sodium-free buffer, the cells accumulated 1 mM D-[9-14C]cephalexin against a concentration gradient and obtained a distribution ratio of 3.5 within 180 min. Drug uptake was maximal when the extracellular pH was 6.0. Uptake was reduced by metabolic inhibitors and by protonophores indicating that uptake was energy- and proton-dependent. Kinetic analysis of the concentration dependence of the rate of cephalexin uptake showed that a non-saturable component (Kd of 0.18 +/- 0.01 nmol/min per mg protein per mM) and a transport system with a Km of 7.5 +/- 2.8 mM and a Vmax of 6.5 +/- 0.9 nmol/min per mg protein were responsible for drug uptake. Uptake was competitively inhibited by dipeptides. The transport carrier exhibited stereospecificity for the L-isomer of cephalexin. Drug uptake was not affected by the presence of amino acids, organic anions, 4-acetamido-4'-isothiocyanostilbene-2,2'-disulfonic acid or 4,4'-diisothiocyano-2,2'-disulfonic stilbene. Therefore, Caco-2 cells take up cephalexin by a proton-dependent dipeptide transport carrier that closely resembles the transporter present in the intestine. Caco-2 cells represent a cellular model for future studies of the dipeptide transporter.

2,4-Dinitrophenol↗