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The concentrations of five cephalosporins and amoxicillin in breast milk were studied in 42 voluntarily participating lactating mothers using standard assay methods. Each mother received one single dose of 1 g of either an orally or intravenously administered antibiotic. Amoxicillin, cephalexin, and cefadroxil were given orally, and peak milk concentrations averaged 0.81 +/- 0.33 microgram/ml at 5 hours, 0.50 +/- 0.23 microgram/ml at 4 hours, and 1.64 +/- 0.73 microgram/ml at 6 hours, respectively. Cephalothin, cephapirin and cefotaxime were given as an i.v. bolus injection, and peak milk concentrations at 2 hours averaged 0.47 +/- 0.14 microgram/ml, 0.43 +/- 0.16 microgram/ml and 0.32 +/- 0.09 microgram/ml, respectively. The high concentrations of cefadroxil can be explained by its low rate of elimination and higher fat solubility. Milk/serum ratios for all antibiotics were increasing as serum concentrations were diminishing, especially with cephalothin and cephapirin whose serum concentrations are rapidly declining. The significance of bactericidal concentrations in breast milk remains to be evaluated.
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Minimum inhibitory concentrations (MICs) of cefadroxil were determined for 749 defined clinically-significant bacteria isolated in a London teaching hospital and for 63 strains from an international collection of Gram-negative bacilli. Assuming a breakpoint of 16 mg/l, for the hospital isolates 81.8% of Gram-negative bacilli and 83.4% of Gram-positive cocci were sensitive. No significant difference between in-patient, out-patient or community-acquired isolates was found. Ninety-five and a half per cent of Escherichia coli, Klebsiella aerogenes (including gentamicin-resistant strains), Proteus mirabilis, and (with the exception of Streptococcus faecalis and methicillin-resistant Staphylococcus aureus) all Gram-positive cocci were sensitive. Of 41 strains of Enterobacter spp., were resistant. Most indole-positive Proteus, and all Serratia and Acinetobacter spp. were resistant, including 36 additional strains taken from an international collection. Of 30 strains of Haemophilus influenzae, only six had MICs of 16 mg/l or less. For disc susceptibility testing, the standard disc containing 30 micrograms of cefadroxil reliably gave zones of greater than 17 mm for organisms with MICs of less than 16 mg/l. A zone of less than 14 mm corresponded to MICs of greater than 64 mg/l. Despite a lack of controlled clinical trials, the results of this study (taken with favourable pharmacokinetics) suggest that cefadroxil has potential as an oral cephalosporin in hospital practice in the U.K.
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A total of 1979 invitations to participate in the survey were sent, and 253 responses were received during the 4-month study period. Of respondents, 81% were in private practice. Respondents averaged 21 ± 9 years in practice, and 34 ± 50 implant-based breast reconstructions were performed per year. A majority of surgeons used chlorhexidine to prepare the surgical site (52%), a triple antibiotic soak for the implant prior to placement (50%) and povidone-iodine for implant pocket irrigation (44%). A no-touch technique utilizing the Keller funnel was adopted by 69% of surgeons. Regarding antibiotic use in the postoperative period, first-generation cephalosporins (eg, cephalexin, cefadroxil) were used by a majority of surgeons (84%), and the most common duration was until drain removal (45%).
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The frequency of symptomatic relapses following various antibiotic treatments for group A beta-hemolytic streptococcal tonsillopharyngitis was evaluated in 1080 pediatric patients. Within 5 days of completing therapy, the rank-order frequency of treatment failures was (1) penicillin, (2) amoxicillin, (3) first-generation cephalosporins, (4) beta-lactamase stable cephalosporins and amoxicillin-clavulanate ( P = .005). Retreatment of symptomatic failures resulted in another symptomatic relapse more often with penicillin than with cephalosporins (P = .02). Clinicians should be aware that the rate of symptomatic failures after antibiotic therapy for group A beta-hemolytic streptococcal tonsillopharyngitis differs by drug and is not an uncommon event.
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A reversed-phase column liquid chromatographic method was developed for the assay of cefadroxil in bulk drugs and pharmaceutical preparations. An equation was derived showing a linear relationship between peak-area ratios of cefadroxil to dimethylphthalate (internal standard) and the cefadroxil concentration over a range of 0.02-0.8 mg/ml (r = 0.9999). Standard addition recoveries were generally greater than 97.7%. The coefficients of variation in the within-day assay were between 0.36 and 0.65, and in the between-day assay was 0.71%. The column liquid chromatographic assay results were compared with those obtained from a microbiological assay, which indicated that the proposed method is a suitable substitute for the microbiological method for potency assays and stability studies of cefadroxil preparations.
To investigate the relative efficacy of orally administered cefadroxil and penicillin V in the treatment of group A streptococcal (GABHS) pharyngitis and the mechanism(s) responsible for failure of antimicrobial therapy to eradicate GABHS from the pharynx.
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The solubility vs. pH profiles of five ionizable drugs of different nature (a monoprotic acid, a monoprotic base, a diprotic base and two amphoteric compounds showing a zwitterionic species each one) have been determined through two different methodologies: the classical shake-flask (S-F) and the potentiometric Cheqsol methods using in both instances the appropriate Henderson-Hasselbalch (H-H) or derived relationships. The results obtained independently from both approaches are consistent. A critical revision about the influence of the electrolyte used as buffering agent in the S-F method on the obtained solubility values is also performed. Thus, some deviations of the experimental points with respect the H-H profiles can be attributed to specific interactions between the buffering electrolyte and the drug due to the hydrotrophic character of citric and lactic acids. In other cases, the observed deviations are independent of the buffers used since they are caused by the formation of new species such as drug aggregates (cefadroxil) or the precipitation of a salt from a cationic species of the analyzed compound (quetiapine).
Cefatrizine, a new orally administered cephalosporin, was tested against 400 clinical isolates. Cefatrizine had excellent activity against gram-positive cocci, inhibiting all except enterococci at minimal inhibitory concentrations below 1 mug/ml. Cefatrizine inhibited the majority of Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, and Salmonella at concentrations below 12.5 mug/ml. Although cefatrizine was not hydrolyzed by many beta-lactamases, it did not inhibit a number of strains of Enterobacter, Serratia, or indole-positive Proteus. Cefatrizine was more active than cephalothin or cephalexin against E. coli, Klebsiella, Enterobacter, Citrobacter, Salmonella, and Shigella. Its overall activity was less than that of cefoxitin against strains resistant to cephalothin, but its activity against cephalothin-susceptible strains was equivalent to that of cefamandole.
The absorption and disposition kinetics of [3H]cefadroxil were determined in wild-type and PepT1 knockout mice after 44.5, 89.1, 178, and 356 nmol/g oral doses of drug. The pharmacokinetics of [3H]cefadroxil were also determined in both genotypes after 44.5 nmol/g intravenous bolus doses.
In this review, the principal drugs used for prevention and treatment of pain--analgesics, and swelling--antibiotics, are examined. The rationale for prevention of pain and swelling is given. Then the specific drugs are considered. The analgesics evaluated include: the non-steroidal anti-inflammatory agents (e.g., aspirin, acetaminophen, ibuprofen, diflunisal); and the narcotics (e.g., codeine, oxycodone, hydrocodone, meperidine). The antibiotics evaluated include: the penicillins (e.g., penicillin V, ampicillin, methicillin); the cephalosporins (e.g., cephalexin, cefadroxil); the erythromycins (e.g., erythromycin stearate, erythromycin base); clindamycin; metronidazole; and some rarely used drugs (e.g., ciprofloxacin).
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Eight Italian clinical centers carried out a controlled double-blind/double-dummy evaluation of the effectiveness of two different administration schedules of cefatrizine, an orally active cephalosporin. The first schedule provided for once-a-day administration of 1.5 gm of the drug, and the second one for twice-a-day administration of 0.75 gm. The trial included 160 patients affected by bacterial diseases of the respiratory apparatus. The two drug administration schedules were found to be equivalent in clinical and bacteriological results and in tolerability.
Neuropeptide inactivation is generally thought to occur via peptidase-mediated degradation. However, a recent study found increased analgesia after L-kyotorphin (L-Tyr-L-Arg; L-KTP) administration in mice lacking an oligopeptide transporter, PEPT2. The current study examines the role of PEPT2 in L-KTP uptake by astrocytes and compares it to astrocytic L-KTP degradation. L-[(3)H]KTP uptake was measured in primary cultures of neonatal astrocytes from rats and from Pept2(+/+) and Pept2(-/-) mice. Uptake was further characterized using potential inhibitors. L-[(3)H]KTP degradation was examined in primary astrocyte cultures from Pept2(-/-) mice by following the formation of L-[(3)H]tyrosine. The uptake of L-[(3)H]KTP in both rat and Pept2(+/+) mouse neonatal astrocytes was inhibited by known PEPT2 inhibitors. L-[(3)H]KTP uptake was also reduced in Pept2(-/-) astrocytes as compared to those from Pept2(+/+) mice. Kinetic analysis indicated the presence of a high affinity (K(m) approximately 50 microM) transporter for L-[(3)H]KTP, identified as Pept2, and a low affinity transporter (K(m) approximately 3-4 mM), inhibited by amastatin, bestatin and tyrosine. Astrocytes also degraded L-KTP through a low affinity peptidase (K(m) approximately 2 mM). Astrocytic clearance of L-KTP occurs via both peptidase activity and transport. These processes occur at similar rates and may be linked. This supports the contention that oligopeptide transport may have an impact on the extracellular clearance (and potentially activity) of certain neuropeptides.
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Oral cephalosporins (cefixime, cefdinir, cefetamet, ceftibuten, cefpodoxime, loracarbef, cefprozil, cefuroxime, cefaclor, cefadroxil and BAY 3522) were compared by their antibacterial profile including stability against new beta-lactamases. Both activity and antibacterial spectrum of compounds structurally related to third generation parenteral cephalosporins (of the oximino class) were superior to established compounds. Activity against staphylococci was found to be highest for cefdinir, cefprozil and BAY 3522. Cefetamet, ceftibuten and cefixime demonstrate no clinically meaningful antistaphylococcal activity while the other compounds investigated demonstrate intermediate activity. The antibacterial spectrum was broadest for cefdinir and cefpodoxime. New oral cephalosporins are equally inactive as established compounds against Enterobacter spp., Morganella, Listeria, Pseudomonas and Acinetobacter spp., methicillin-resistant staphylococci, Enterococcus spp., penicillin-resistant pneumococci and anaerobes. New extended broad-spectrum betalactamases (TEM-3, TEM-5, TEM-6, TEM-7, SHV-2, SHV-3, SHV-4, SHV-5, CMY-1, CMY-2, and CTX-M) are active against the majority of oral cephalosporins. Ceftibuten, cefetamet, cefixime and cefdinir were stable against some of these enzymes even to a higher extent than parenteral cephalosporins. New oral cephalosporins should improve the therapeutic perspectives of oral cephalosporins due to their higher activity against pathogens marginally susceptible to established compounds (higher multiplicity of maximum plasma concentrations over MICs of the pathogens) and furthermore by including in their spectrum organisms resistant to established absorbable cephalosporins (e.g. Proteus spp., Providencia spp., Citrobacter spp., and Serratia spp.).
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Cefadroxil (Duricef, Mead Johnson and Company), resembles cephalexin and cephradine in spectrum of antibacterial activity but differs in human pharmacokinetic properties. Whether the latter are likely to affect activity in vivo was assessed by determining bactericidal activity against clinical isolates under conditions simulating the variation of drug concentration in the blood stream after an oral dose of 500 mg to adults. In this kinetic model, cefadroxil was more active than cephalexin or cephradine against Staphylococcus aureus, Streptococcus pneumoniae, Klebsiella pneumoniae, Proteus mirabilis, Haemophilus influenzae and one of two strains of Escherichia coli. The other strain of E. coli was virtually unaffected by the cephalosporins. S. pyogenes was equally susceptible to all three cephalosporins. Analysis of the results suggest that the pharmocokinetic properties of an antibiotic affect its activity in the blood stream, provided the susceptibility of the infecting organism is concentration-dependent within the range of drug concentration occurring in serum.
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Co-administration of piperine, an alkaloid isolated from Piper nigrum L. enhanced bioavailability of beta lactam antibiotics, amoxycillin trihydrate and cefotaxime sodium significantly in rats. The improved bioavailability is reflected in various pharmacokinetic parameters viz. tmax, Cmax, t(1/2) and AUC, of these antibiotics. The increased bioavailability could be attributed to the effect of piperine on microsomal metabolising enzymes or enzymes system.
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To evaluate the effect of foal age on the pharmacokinetics of cefadroxil, five foals were administered cefadroxil in a single intravenous dose (5 mg/kg) and a single oral dose (10 or 20 mg/kg) at ages of 0.5, 1, 2, 3 and 5 months. Pharmacokinetic parameters of terminal elimination rate constant (beta(po)), oral mean residence time (MRTpo), mean absorption time (MAT), rate constant for oral absorption (Ka), bioavailability F, peak serum concentrations (Cmax) and time of peak concentration (tmax), were evaluated in a repeated measures analysis over dose. Across animal ages, parameters for the intravenous dose did not change significantly over animal age (P > or = 0.05). Mean values +/- SEM were: beta(IV) = 0.633 +/- 0.038 h-1; Cl = 0.316 +/- 0.010 L/kg/h; Vc = 0.196 +/- 0.008 L/kg; Varea = 0.526 +/- 0.024 L/kg; VSS = 0.374 +/- 0.014 L/kg; MRTiv = 1.22 +/- 0.07 h; Kel = 1.67 +/- 0.08 h-1. Following oral administration, drug absorption became faster with age (P < 0.05), as reflected by MRTpo, MAT, Ka and tmax. However, oral bioavailability (+/- SE) declined significantly (P < 0.05) from 99.6 +/- 3.69% at 0.5 months to 14.5 +/- 1.40% at 5 months of age. To evaluate a dose effect on the pharmacokinetic parameters, a series of oral doses (5, 10, 20 and 40 mg/kg) were administered to these foals at 1 month of age. beta(po) (0.548 +/- 0.023 h-1) and F (68.26 +/- 2.43%) were not affected significantly by the size of the dose. Cmax was approximately doubled with each two-fold increase in dose: 3.15 +/- 0.15, 5.84 +/- 0.48, 12.17 +/- 0.93 and 19.71 +/- 2.19 micrograms/mL. Dose-dependent kinetics were observed in MRTpo, MAT, Ka and tmax.
In order to study the interaction of sulfamoyl- and phenoxy diuretics as well as of beta-lactam antibiotics with the contraluminal anion and cation transport systems the inhibitory potency of these substances against the influx of 3H-para-aminohippurate, 14C-succinate, 35S-sulfate and 3H-N1-methylnicotinamide into cortical tubular cells have been determined. 1.) 2-, 3- and 4-sulfamoylbenzoate inhibit contraluminal PAH influx. N-dipropyl substitution to yield probenecid or ring-substitution to yield furosemide and piretanide augment the inhibitory potency. However, hydrochlorothiazide and acetazolamide exert only a moderate inhibitory potency. Succinate transport was inhibited by furosemide only. Sulfate transport was inhibited by furosemide and 3-sulfamoyl-4-phenoxybenzoate as well as by probenecid, piretanide, hydrochlorothiazide and acetazolamide. 2.) Phenoxyacetate, -propionate, and -butyrate exert increasing inhibition against PAH transport. The weed-killers 2,4-dichloro-, and 2,4,5-trichlorophenoxyacetate (2,4 D and 2,4,5 T) had a similar inhibitory potency, while ethacrynic acid showed a lower and the uricosuric tienilic acid a higher inhibitory potency. None of the compounds of this group interact with contraluminal succinate transport, and only the multiring-substituted compounds 2,4 D, 2,4,5 T, ethacrynic and tienilic acid interact slightly with the sulfate transporter. 3.) The monocarboxylic penicillins benzylpenicillin and phenoxymethylpenicillin as well as the dicarboxylic ticarcillin interact with the contraluminal PAH transport. The aminopenicillin ampicillin had a lower, and apalcillin a higher inhibitory potency than monocarboxylic penicillin. Benzylpenicillin showed small inhibition against succinate transport and ticarcillin against sulfate transport. 4.) The monocarboxylic cephalosporine, 6315 S Shionogi, and the aminocephalosporines, cephalexin and cefadroxil, showed an app. Ki.PAH as the comparable penicillins. The zwitterions cephaloridine and cefpirome did not interact with the PAH transporter, but with the organic cation (NMN) transporter. Amongst the amino-thiazol-containing compounds cefotaxime, ceftriaxone, and cefodizime, increasing interaction with the PAH transporter was seen dependent of a second ionizable anionic group. Compounds with two ionizable anionic groups (cefsulodin, ceftriaxone, cefodizime) exert also a small inhibitory potency against sulfate transport. None of the cephalosporins interacted with the dicarboxylate transporter. The interaction pattern of the tested compounds is in accordance with the specificity requirements for the contraluminal transporters depending on electrical charge and hydrophobicity.
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The in vitro activity of ampicillin, amoxicillin/clavulanate, cefadroxil, cefaclor, cefuroxime (axetil), co-trimoxazole, doxycycline, ciprofloxacin, ofloxacin, erythromycin, and roxithromycin was tested against unselected isolates of S. pneumoniae (70), H. influenzae (93), and M. catarrhalis (46), cultured from clinically significant sputum samples of general practice patients. All isolates of S. pneumoniae were highly susceptible to ampicillin; cefadroxil and cefaclor were markedly less active on a weight basis; resistance was only observed with co-trimoxazole (4.3%), doxycycline (5.7%), and erythromycin (2.9%); however, ciprofloxacin and ofloxacin showed median MICs (MIC50), that were only one dilution below breakpoint. Beta-lactamase was detected in 14.0% of H. influenzae isolates; all isolates were susceptible to amoxicillin/clavulanate, cefaclor, and cefuroxime (axetil), although MICs were generally higher for cefaclor; the highest activity was exhibited by ciprofloxacin and ofloxacin; apart from cefadroxil, erythromycin, and roxithromycin, that showed only marginal activity, resistance was observed with co-trimoxazole (4.3%) and doxycycline (1.1%). All (including 71.7% of beta-lactamase producing) isolates of M. catarrhalis were susceptible to amoxicillin/clavulanate, cefaclor and cefuroxime (axetil), although MICs were markedly lower for amoxicillin/clavulanate; ciprofloxacin and ofloxacin showed the lowest MICs; resistance was only observed with cefadroxil (2.2%). In conclusion, the antimicrobial agents showing the most uniformly high in vitro activity against the 3 common community respiratory pathogens tested in the present study, were amoxicillin/clavulanate and, to a lesser extent, cefuroxime (axetil).
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Urine specimens were collected for culture and antimicrobial susceptibility testing against mecillinam, ampicillin, cefadroxil, trimethoprim, nitrofurantoin and quinolones from the residents of 32 and 22 nursing homes, respectively. The residents were capable of providing a voided urine sample in 2003 and 2012. In 2012 urine specimens were also collected from residents with urinary catheters. Any antibiotic treatment during the previous month was registered in 2003 as well as hospitalisation and any antibiotic treatment during the previous six months in 2012.
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The transport characteristics of chemically modified phenylalanylglycine (Phe-Gly) with butyric acid (C4-Phe-Gly) and caproic acid (C6-Phe-Gly) were examined using rabbit intestinal brush-border membrane vesicles (BBMVs). In the presence of an inwardly H+ gradient (pH 7.5 inside, pH 6.0 outside), the uptake of Phe-Gly via BBMVs was significantly enhanced by the covalent attachment of butyric or caproic acid to the N-terminal of Phe-Gly. Moreover, C4-Phe-Gly uptake was stimulated by the trans-stimulation effect of some dipeptides and cefadroxil, and was inhibited by other dipeptides and cefadroxil. These results indicate that N-terminal modified Phe-Gly with fatty acids are transported into BBMVs via an oligopeptide transporter. Therefore, chemical modification of dipeptides with fatty acids can enhance the intestinal absorption of dipeptide by a carrier-mediated transport via an oligopeptide transporter.
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The cephalosporin antibiotics have been employed with increasing frequency since their introduction into clinical practice in the early 1960s. With the exception of cephaloridine, cephalosporin compounds are not associated with the production of significant untoward effects. The availability of newer cephalosporins, both oral and parenteral, with enhanced antibacterial activity, has expanded the clinical indications for administration of these antibiotics.
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Antimicrobial agents have greatly reduced the incidence of intracranial complications of infections of the middle ear and mastoid. Too many prescriptions and overconsumption of antibiotics when otitis media is suspected has caused resistance to many antibiotics, leading to a pronounced and justifiable desire to reduce the widespread excessive use of antibiotics. The possible untoward consequences of a too restricted antibiotic policy, however, is illustrated by the following case of a 14-year-old boy who, after non-treatment of an ear infection, fell ill with one-sided headache and vomiting caused by a lateral sinus thrombosis. After intravenous treatment with antibiotics, anticoagulants and ventilation of the middle ear, the infection was cured without complications. This case calls attention to the symptoms of otitic complications arising outside the temporal bone. The physician must always bear in mind the possibility of an unusual event. The general treatment of endocranial complications is outlined, giving details of the treatment given in this special case. We stress that one should not be too cautious in prescribing antibiotics in otitis media.
The transport of dipeptides and beta-lactam antibiotics across the rat renal basolateral membrane was examined. The initial uptake of glycylsarcosine and cefadroxil by rat renal basolateral membrane vesicles was inhibited by the presence of all the di- and tripeptides and beta-lactam antibiotics that were tested in this study. However, the uptake of both substrates was not inhibited by glycine, an amino acid. The initial uptake of zwitterionic beta-lactam antibiotics, cefadroxil, cephradine, and cephalexin, was stimulated by preloaded glycylsarcosine (countertransport effect). On the other hand, the uptake of dianionic beta-lactam antibiotics, ceftibuten and cefixime, was not affected. A concentration-dependent initial uptake of glycylsarcosine and cefadroxil suggested the existence of a carrier-mediated mechanism, whereas the transport of ceftibuten did not show any saturated uptake. The transporter that participates in the permeation of dipeptides and beta-lactam antibiotics across basolateral membranes showed lower affinity than did PEPT1 and PEPT2. This is the first study that showed an evidence for a peptide transporter, expressed in the rat renal basolateral membrane, that recognizes zwitterionic beta-lactam antibiotics using basolateral membrane vesicles isolated from normal rat kidney.
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Cefetamet pivoxil is an oral third-generation cephalosporin which is hydrolysed to form the active agent, cefetamet. Cefetamet has excellent in vitro activity against the major respiratory pathogens Streptococcus pneumoniae, Haemophilus influenzae, Moraxella (Branhamella) catarrhalis and group A beta-haemolytic streptococci; it is active against beta-lactamase-producing strains of H. influenzae and M. catarrhalis, but has poor activity against penicillin-resistant S. pneumoniae. Cefetamet has marked activity against Neisseria gonorrhoeae and possesses a broad spectrum of activity against Enterobacteriaceae. Both staphylococci and Pseudomonas spp. are resistant to cefetamet. Cefetamet pivoxil has been investigated in the treatment of both upper and lower community-acquired respiratory tract infections and has demonstrated equivalent efficacy to a number of more established agents, namely cefaclor, amoxicillin and cefixime. In patients with group A beta-haemolytic streptococcal pharyngotonsillitis, a 7-day course of cefetamet pivoxil was as effective as a 10-day course of the standard agent, phenoxymethylpenicillin, in this indication. In complicated urinary tract infections, cefetamet pivoxil showed similar efficacy to cefadroxil, cefaclor and cefuroxime axetil. Cefetamet pivoxil was effective in the treatment of otitis media, pneumonia, pharyngotonsillitis and urinary tract infections in children. Preliminary data indicate that single dose cefetamet pivoxil can effectively eradicate N. gonorrhoeae from both men and women. Cefetamet pivoxil has a tolerability profile similar to that of other oral cephalosporins, with gastrointestinal effects being the most commonly reported adverse events. To date, no symptoms of carnitine deficiency have been reported with cefetamet pivoxil. Cefetamet pivoxil offers effective alternative oral therapy for outpatient treatment of community-acquired respiratory tract infections, with the advantage of improved activity against H. influenzae and increased beta-lactamase stability. However, its use in areas with a high incidence of penicillin-resistant S. pneumoniae is likely to be limited. Cefetamet pivoxil is also effective in the treatment of urinary tract infections, although further trials are required to define any comparative advantages over other oral agents.
Uptake of cefadroxil and its two acetyl-derivatives, N-acetyl- and O-acetyl-cefadroxil, into the brush-border membrane vesicles (BBMV) was measured at [pH]o = 5.5, 7.4 and [pH]i = 7.4. Both acetyl-derivatives showed a significantly slower uptake than cefadroxil at [pH]o = 5.5 and 7.4. Cefadroxil and the two derivatives showed a higher uptake rate in the presence of an inward H+ gradient ([pH]o = 5.5, [pH]i = 7.4). At [pH]o = 5.5, uptake of cefadroxil into BBMV was inhibited by N-acetyl-, O-acetyl-, N-BOC-, and N-BOC-O-acetyl-cefadroxil, but not by cephalothin and cefuroxime. At [pH]o = 7.4, no inhibition of cefadroxil uptake was evident for any inhibitors. There were two different transporters responsible for the uptake of cefadroxil at pH 5.5 and 7.4. One is the H(+)-coupled dipeptide transport system, and the other is the neutral pH-preferring system. The alpha-amino group may be essential for the transport of cefadroxil by both transport systems. Although the phenolic group in the side chain is not an essential functional group of beta-lactam antibiotics, an additional derivation on the phenolic group of cefadroxil also inhibited both the H(+)-coupled dipeptide transport system and the neutral pH-preferring transport system.
Baicalin (baicalein-7-glucuronide) is a flavonoid purified from Scutellaria baicalensis Georgi that has traditionally been used for treatment of hypertension, cardiovascular diseases, and viral hepatitis. In this study, the effects of intestinal microbiota on the pharmacokinetics of baicalin were investigated in normal and antibiotic-pretreated rats following p.o. administration of 100 mg/kg baicalin by using liquid chromatography/ion trap mass spectrometry. When rats were pretreated orally with cefadroxil, oxytetracycline and erythromycin for 3 days to control the number of intestinal bacteria, the pharmacokinetic parameters of oral baicalin were significantly affected by antibiotics: Cmax, T1/2(β), Kel and AUC values were significantly changed compared to those in normal rats. These results indicate that intestinal microbiota might play a key role in the oral pharmacokinetics of baicalin.
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The minimal inhibitory concentrations (MIC) of cephalexin, cephradine, cefaclor, cefatrizine and cefadroxil for Salmonella species, Escherichia coli and Pasteurella multocida isolated previously from young calves were determined. The MIC90 values for cephalexin, cephradine and cefadroxil ranged between 3.12 micrograms ml-1 and 12.5 micrograms ml-1, whereas those of cefatrizine and cefaclor were 3.12 micrograms ml-1 and 0.78 microgram ml-1, respectively. Each drug was administered intravenously and orally to groups of pre-ruminating calves and orally to early ruminating calves. Although the pharmacokinetic characteristics of the drugs after intravenous injection were similar to other beta-lactam antibiotics, significant differences between the cephalosporins examined were found in respect of certain kinetic parameters. The drugs showed rapid absorption into the systemic circulation after oral administration to pre-ruminating calves but the elimination half-life values (t1/2 beta) varied between three hours (cefaclor and cefadroxil) and nine hours (cefatrizine). The bioavailability of the drugs was about 35 per cent of the administered dose. Co-administration of probenecid with each antibiotic caused a twofold or greater increase in peak serum drug concentrations (Cmax) but the effect on t1/2 beta was variable. Cephalexin, cephradine and cefaclor given to the ruminating calves resulted in very low serum or plasma concentrations and their use should be restricted to younger calves. Cefadroxil was found to give the highest serum concentrations in this age group but had significantly lower bioavailability when compared with the unweaned calves. Provisional oral dosage regimens were computed for each cephalosporin on the basis of the MIC data and the kinetic parameters derived from intravenous and oral drug administration.
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Transporters (OATs, MRPs, and perhaps OATPs) that can be inhibited by probenecid play an important role in mediating the brain-to-blood efflux of cefadroxil at the BBB. The uptake of cefadroxil in brain cells involves both the influx transporter PEPT2 and efflux transporters (probenecid-inhibitable). These findings demonstrate that drug-drug interactions via relevant transporters may affect the distribution of cephalosporins in both brain ECF and ICF.
The sample is placed in the sample vessel of a RH cell and the moisture content of the air flow is controlled. From the RH cell the air flow is conducted into a subsequent perfusion cell in which a saturated salt solution has been loaded. The RH cell and perfusion cells are positioned in the sample sides of two twin calorimetric units. Depending on the moisture content in the outlet flow leaving the preceding RH cell, the heat flow signal from the subsequent perfusion cell will vary. By means of blank measurement with identical settings, the rate of water sorption can be calculated and, by integration, the amount of sorbed water is obtained.