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PubMed2005

Therapeutic options for pneumococcal pneumonia in Turkey.

BACKGROUND: Community-acquired pneumonia (CAP) is a leading cause of morbidity and mortality worldwide. Streptococcus pneumoniae continues to be the most important causative agent in CAP. OBJECTIVE: This article reviews options for the empiric treatment of pneumococcal pneumonia in Turkey based on local epidemiologic data. METHODS: This was a retrospective review of studies evaluating antimicrobial susceptibility patterns among clinical isolates of S pneumoniae in Turkey from 2000 onward. Relevant studies were identified through literature searches of both Turkish (Ulakbim and Pleksus) and international (MEDLINE) databases using the search terms S pneumoniae and Turkey. Only antibiotics likely to be used in pneumococcal pneumonia were evaluated. The minimum concentration required to inhibit 90% of isolates (MIC(90)) for each antibiotic was obtained by averaging all reported values to arrive at a single value for the entire country. RESULTS: The MIC(90) for penicillin was 1 g/mL; among all isolates of S pneumoniae, 6.4% were penicillin resistant and 30.9% showed intermediate susceptibility. The MIC(90)s and overall rates of resistance (combined intermediate susceptibility and resistance) for the other antibiotics studied were as follows: cefaclor, 4 microg/mL (26.3%); cefuroxime, 2 microg/mL (15.4%); ceftriaxone, 0.25 microg/mL (0.75%); imipenem, 0.06 microg/mL (0%); erythromycin, 2 microg/mL (13.9%); clarithromycin, 2 microg/mL (13.7%); azithromycin, 2 microg/mL (13.8%); telithromycin, 0.06 microg/mL (no published breakpoints); trimethoprim-sulfamethoxazole, 4 microg/mL (63.8%); tetracycline, 16 microg/mL (24.6%); ciprofloxacin, 2 microg/mL (no published breakpoints); ofloxacin, 2 microg/mL (4%); levofloxacin, 1 microg/mL (0%); gemifloxacin, 0.06 microg/mL (no published breakpoints); and moxifloxacin, 0.06 microg/mL (0%). Penicillin G, at standard parenteral doses, has been shown to achieve concentrations above the MIC for >40% to 100% of the dosing interval, depending on the MIC of the isolate. Based on pharmacodynamic studies, the MIC(90) for penicillin in Turkey should easily be exceeded with the use of penicillin G 3 mU QID. In vitro, susceptibility is generally greater to amoxicillin than to penicillin, with average amoxicillin MIC values approximately 1 dilution lower than those for penicillin. Amoxicillin's better pharmacodynamic/pharmacokinetic properties relative to penicillin make it a reasonable option for the treatment of CAP. In pharmacodynamic studies, amoxicillin 1 g TID achieved and maintained serum concentrations of 2 to 4 microg/mL for at least 40% of the dosing interval. A new formulation of amoxicillin/clavulanate given 2000/125 mg BID is expected to eradicate isolates of S pneumoniae at an amoxicillin MIC < or = 4 microg/mL. CONCLUSIONS: Based on data from Turkish surveillance studies performed from 2000 onward, high-dose parenteral penicillin G and parenteral/oral amoxicillin may be initial choices for the empiric treatment of uncomplicated pneumococcal pneumonia in Turkey. If these agents cannot be used for any reason, other options include parenteral cefuroxime, ceftriaxone, cefotaxime, newer quinolones, macrolides, and telithromycin. Due to elevated rates of resistance in Turkey, trimethoprim-sulfamethoxazole and tetracyclines are not recommended for empiric use in these infections.

Anti-Bacterial Agents↗
PubMed2004

Antimicrobial susceptibility patterns, beta-lactamases, and biochemical identification of Yokenella regensburgei strains.

Yokenella regensburgei is an opportunistic human pathogen that phenotypically resembles Hafnia alvei. The susceptibility of 10 Y. regensburgei strains to 75 antimicrobial agents was examined, applying a microdilution procedure in cation-adjusted Mueller-Hinton broth (CAMHB) and IsoSensitest broth (ISB). beta-Lactamases were characterized phenotypically with beta-lactamase activity and induction assays. Genotypically, PCR experiments applying degenerated primer pairs for the detection of AmpC beta-lactamase genes were performed. Examining the phenotypic properties of Yokenella and 76 H. alvei strains with commercial identification systems and conventional tests, a database for an accurate biochemical separation of Y. regensburgei from H. alvei was established. In CAMHB, all tested yokenellae were resistant or at least of intermediate susceptibility to penicillin G, oxacillin, amoxicillin, amoxicillin-clavulanate, cefaclor, cefazoline, loracarbef, cefoxitin, all tested macrolides, lincosamides, streptogramins, ketolides, fusidic acid, glycopeptides, linezolid, and rifampicin. All Yokenella strains were sensitive to several beta-lactams, all tested aminoglycosides, chloramphenicol, folate-pathway inhibitors, fosfomycin, nitrofurantion, quinolones, and tetracyclines. In ISB, the minimum inhibitory concentration (MIC) values of several beta-lactams were one to four MIC doubling dilution steps lower than those found in CAMHB (depending on the beta-lactam). All yokenellae yielded specific amplification products for ampC, and all of these strains expressed beta-lactamases that were strongly inducible. Hydroxyproline amidase, maltosidase, tri-peptidase, proline deaminase, catalase reaction, Voges-Proskauer test, and fermentation of glycerol, melibiose and myo-inositol were suitable parameters to separate Y. regensburgei from H. alvei.

Anti-Bacterial Agents↗
PubMed2005

Interaction of 31 beta-lactam antibiotics with the H+/peptide symporter PEPT2: analysis of affinity constants and comparison with PEPT1.

The activity of the renal peptide transporters PEPT2 and PEPT1 determines-among other factors such as metabolic stability in liver and plasma-the circulatory half-life of penicillins and cephalosporins during therapy. This study was initiated to examine systematically the interaction of beta-lactam antibiotics with PEPT2. Interaction of 31 cephalosporins and penicillins with the carrier protein was characterized by measuring their ability to inhibit the uptake of [(14)C]Gly-Sar into renal SKPT cells. Cefadroxil, cefaclor, cyclacillin, cephradine, cephalexin and moxalactam were recognized by PEPT2 with very high affinity comparable to that of natural dipeptides (K(i)=3-100microM). Ceftibuten, dicloxacillin, amoxicillin, metampicillin, cloxacillin, ampicillin, cefixime, cefamandole, oxacillin and cefmetazole interacted with PEPT2 with medium affinity (K(i)=0.1-5mM). For the other beta-lactam antibiotics studied interaction was very low or not measurable (K(i)>5mM). The affinity constants of beta-lactam antibiotics at rPEPT2 and hPEPT1 are significantly correlated, but the rank orders are not identical. Decisive differences between PEPT1 and PEPT2 recognition of the N-terminal part of the compounds became evident. Moreover, this large data set of affinity constants of beta-lactam antibiotics will be useful for structure-transport (binding) analyses of PEPT2.

Animals↗
PubMed2004

Antimicrobial resistance of Streptococcus pneumoniae and Haemophilus influenzae in Sao Paulo, Brazil from 1996 to 2000.

This study was undertaken to assess the in vitro activity of several antimicrobial agents against Brazilian isolates of Streptococcus pneumoniae and Haemophilus influenzae from 1996 to 2000. The antibiotics used were penicillin, amoxicillin/clavulanic acid (A/C), ampicillin, amoxicillin, cefaclor, cefdinir, cefixime, cefprozil, ceftriaxone, cefuroxime, azithromycin, clarithromycin, erythromycin, ciprofloxacin, levofloxacin, ofloxacin, chloramphenicol, clindamycin, doxycycline and trimethoprim/sulphamethoxazole (T/S). MICs were determined by the National Committee for Clinical Laboratory Standards (NCCLS) method and interpreted using NCCLS and PK/PD breakpoints. For S. pneumoniae 80.0% were penicillin susceptible, 18.3% intermediate, 1.7% resistant; most active agents were amoxicillin, A/C, ceftriaxone and levofloxacin; T/S was the least active agent. Beta-lactamase was produced by 13.7% of H. influenzae. All were susceptible to A/C, cefdinir, cefixime, ceftriaxone and quinolones. The least active agents were T/S and macrolides.

Adolescent↗
PubMed2005

Antibiotic susceptibility and serotype distribution in Streptococcus pneumoniae circulating in Italy: results of the SEMPRE surveillance study (2000-2002).

During 2000-2002, 20 clinical microbiology centres collected 1623 Streptococcus pneumoniae isolates. Susceptibility to penicillin, amoxicillin, amoxicillin/clavulanic acid, cefaclor, cefuroxime, cefotaxime, clarithromycin, ciprofloxacin, levofloxacin, rifampicin and teicoplanin was determined locally by the Etest and/or by the microdilution method by three co-ordinating centres. Total resistance to penicillin increased from 15.2% to 16.1% and macrolide resistance increased from 37.9% to 43.7%. Overall, the most effective drugs (>99% susceptible strains) were amoxicillin, amoxicillin/clavulanic acid, levofloxacin and rifampicin. The most frequent serotypes were: 23F (15.8%), 3 (10.8%) 14 (9.1%), 19F (9.1%), 6B (7.2%), 19A (6.9%) and 6A (4.8%). In conclusion, penicillin and macrolide resistance is increasing in Italy, whilst fluoroquinolone currently remains active. The most common serotypes circulating are included in the heptavalent conjugate vaccine, with the exception of type 3.

Anti-Bacterial Agents↗
PubMed2006

Immediate allergic reactions to cephalosporins: evaluation of cross-reactivity with a panel of penicillins and cephalosporins.

BACKGROUND: Allergy to cephalosporins has mainly been evaluated in the context of patients with confirmed penicillin allergy. The problem of studying cross-reactivity in subjects primarily sensitized to cephalosporins and potentially allergic to penicillins has not been sufficiently addressed. OBJECTIVE: To evaluate the in vitro IgE response and cross-reactivity to betalactams in patients with immediate allergic reactions to cephalosporins. METHODS: The study included 24 patients with immediate allergic reactions to cephalosporins and RAST-positive to at least 1 cephalosporin. Skin testing and RAST were performed with a panel of penicillins and cephalosporins. RAST inhibition assay with different monomeric conjugates of penicillin and cephalosporin was performed to establish cross-reactivity. RESULTS: The culprit cephalosporins were cefaclor (N = 7), cefonicid (N = 1), cefotaxime (N = 2), ceftazidime (N = 2), ceftriaxone (N = 3), and cefuroxime (N = 9). Two patients had a positive skin test result to penicillin determinants, and 22 patients had a negative result to penicillin determinants and tolerated benzylpenicillin administration. Of these 22, 19 had a positive skin test result to cephalosporins and divided into patients reacting only to the culprit cephalosporin (63.2%) and those reacting to more than 1 cephalosporin (36.8%). RAST and RAST inhibition studies confirmed that the side chain at the R1 position is crucial for recognition. CONCLUSION: The R1 side chain rather than the betalactam structure, shared by penicillins and cephalosporins, seems to play a dominant role in determining the specificity of immunologic reactions to cephalosporins. Thus, penicillin can be administered safely to patients allergic to cephalosporins and with a negative skin test result to penicillin determinants.

Adolescent↗
PubMed2004

The use of a monolithic column to improve the simultaneous determination of four cephalosporin antibiotics in pharmaceuticals and body fluids by HPLC after solid phase extraction--a comparison with a conventional reversed-phase silica-based column.

The use of a monolithic column (Chromolith, SpeedROD RP-18e, by Merck) was studied on the determination of cephalosporin antibiotics. Results were compared with those from a previously developed analytical method using conventional silica-based analytical column. A rapid, accurate and sensitive method has been developed and validated for the quantitative simultaneous determination of four cephalosporins: Cephalexine and Cephadroxil (first generation), Cefaclor (second generation) and Cefotaxim (third generation) in pharmaceuticals as well as in human blood serum and urine. Hydroflumethiazide (HFM) (3,4-dihydro-6(trifluoromethyl)-2H-1,2,4-benzothiadiazine-7-sulfonamide-1,1-dioxide) was used as an internal standard at a concentration of 1.5 ng/microL. A rectilinear relationship was observed up to 5 ng/microL for the four compounds. Analysis time was less than 4 min. The statistical evaluation of the method was examined by means of within-day repeatability (n=8) and day-to-day precision (n=8) and was found to be satisfactory with high accuracy and precision results. The method was applied to the determination of the cephalosporins in commercial pharmaceuticals and in biological fluids: human blood serum after solid phase extraction and urine simply after filtration and dilution. Recovery of analytes in spiked serum samples was in the range from 88.7 to 107.8%, while for urine samples recovery was from 98.0 to 105.6%. By comparing the figures of merit for the monolithic column and the silica-based one, regarding the determination of the four cephalosporins investigated in the present study, the outstanding efficiency of the monolithic column can be noticed.

Body Fluids↗
PubMed2006

Selective method for the determination of cefdinir in human plasma using liquid chromatography electrospray ionization tandam mass spectrometry.

A sensitive and selective liquid chromatographic-tandem mass spectrometric (LC-MS/MS) method was developed for the determination of cefdinir in human plasma. After a simple protein precipitation using trichloracetic acid, the post-treatment samples were applied to a prepacked RP18 Waters SymmetryShield column interfaced with a triple quadrupole tandem mass spectrometer. Positive electrospray ionization was employed as the ionization source. The mobile phase consisted of methanol-water-formic acid (25:75:0.075, v/v/v). The analyte and I.S. cefaclor were both detected by the use of selected reaction monitoring mode. The method was linear in the concentration range of 5-2,000 ng/ml. The lower limit of quantification was 5 ng/ml. The intra- and inter-day relative standard deviation across three validation runs over the entire concentration range was less than 4.3%. The accuracy determined at three concentrations (36, 360 and 1,800 ng/ml for cefdinir) ranged from 99.6 to 106.7% in terms of recovery. The chromatographic run time for each plasma sample was less than 3 min. The method herein described was successfully applied for the evaluation of pharmacokinetic profiles of cefdinir capsule in 12 healthy volunteers.

Anti-Infective Agents↗
PubMed2004

[Epidemiology of Haemophilus influenzae strains identified in 2001 in France, and assessment of their susceptibility to beta-lactams].

UNLABELLED: The aim of this study was to describe the epidemiology of H. influenzae strains collected in 2001 at the National Reference Center and to evaluate their susceptibility to beta-lactams. METHODS: The demographic characteristics were recorded for each strain, then were determined their capsular serotyping (slide agglutination with specific antisera), as well as their beta-lactamase production (chromogenic cephalosporin test, Nitrocefin), and their MICs (agar dilution method on Haemophilus Test Medium) for amoxicillin (AMX), co-amoxiclav (AMC), cefpodoxime (CPD), cefaclor (CEC), cefuroxime (CXM), and cefotaxime (CTX). RESULTS: 41.3% of the 752 strains were identified in bronchial secretions, 20.6% in conjunctivitis, 11.3% in otitis media, and 11% in blood cultures. 96.3% of the strains were not capsulated and 3.7% were of type b, d, e or f. 33.8% of the strains were beta-lactamase producers (TEM type), 45.8% of these were identified in otitis pus and 27.7% in bronchial secretions. One hundred and forty-two strains (18.9%) presented reduced susceptibility to beta-lactams (modification of target) associated or not with bla+. MICs 50/90 against bla+ strains were: AMX 1/32, AMC 0.12/1, CTX 0.007/0.03, CPD 0.03/0.12, CEC 1/64, CXM 0.25/1. Against low BLNAR and bla+ strains, MICs 50/90 were: AMX 2/32, AMC 0.25/2, CTX 0.015/0.06, CPD 0.06/0.25, CEC 4/64, CXM 0.25/4. And against low BLNAR strains MICs 50/90 were: AMX 0.25/8, AMC 0.25/8, CTX 0.015/0.12, CPD 0.06/0.50, CEC 4/32, CXM 0.25/4. CONCLUSIONS: Both bla+ and modifications of PBP are widespread among strains isolated in France. CTX, and CPD remain the most active compounds whatever the resistance mechanisms.

Colony Count, Microbial↗
PubMed2004

Sequence of the 68,869 bp IncP-1alpha plasmid pTB11 from a waste-water treatment plant reveals a highly conserved backbone, a Tn402-like integron and other transposable elements.

To analyse the significance of conjugative broad-host-range IncP-1alpha plasmids for the spread of antibiotic resistance determinants in waste-water treatment plants we isolated and characterised five different IncP-1alpha plasmids from bacteria of activated sludge and the final effluents of a municipal waste-water treatment plant. These plasmids mediate resistance to ampicillin, cefaclor, cefuroxime, gentamicin, kanamycin, spectinomycin, streptomycin, tetracycline, tobramycin, and trimethoprim. The complete 68,869 bp DNA-sequence of the IncP-1alpha plasmid pTB11 was determined. The pTB11 backbone modules for replication (Rep), mating pair formation (Trb), multimer resolution (Mrs), post-segregational killing (Psk), conjugative DNA-transfer (Tra), plasmid control (Ctl), and stable maintenance and inheritance (KilA, KilE, and KilC) are highly conserved as compared to the 'Birmingham' IncP-1alpha plasmids. In contrast to the 'Birmingham' plasmids pTB11 carries an insert of a Tn402-derivative integrating a class 1 integron in the intergenic region between the multimer resolution operon parCBA and the post-segregational killing operon parDE. The integron comprises the resistance gene cassettes oxa2 (beta-lactamase), aacA4 (aminoglycoside-6'N-acetyltransferase), and aadA1 (aminoglycoside-3'-adenylyltransferase) and a complete tniABQR transposition module. Integron-specific sequences were also identified on other IncP-1alpha plasmids analysed in this work. In contrast to the 'Birmingham' plasmids the pTB11 tetracycline resistance module carries a pecM- and a pncA-like gene downstream of the tetracycline resistance gene tetA and contains an insertion of the new insertion sequence element ISTB11. The transposable elements IS21 and Tn1 which disrupted, respectively, orf7 and klcB on the 'Birmingham' plasmids are not present on pTB11. Identification of IncP-1alpha plasmids in bacteria of the waste-water treatment plant's final effluents indicates that bacteria carrying these kind of plasmids are released into the environment.

Base Sequence↗
PubMed1997

Structural specificity requirements in the binding of beta lactam antibiotics to human serum albumin.

The binding of some cephalosporins of pharmacological interest, to human serum albumin was studied using ultrafiltration method. The identification of the binding sites in albumin was also performed using probes for the so-called sites I, II, bilirubin and fatty acids binding sites. Cephalosporins were classified into three groups according to their affinity for albumin: low affinity (K = 10-10(2) M-1), medium affinity (K = 10(3) M-1) and high affinity (K = 10(4) M-1). Cephalosporin binding to albumin produced a perturbation of several basic amino acids of the protein such as histidine and lysine. It was found that only cefuroxime, ceftazidime and cefoperazone interact slightly with site I on serum albumin, while site II possesses capacity to bind: cephradine, cephalexin, ceftazidime, ceftriaxone, cefoperazone, cefaclor and cefsulodin. The bilirubin binding site showed capacity to interact with a great number of cephalosporins: ceftriaxone, cefazolin, cephaloglycin, cefamandole, cefotaxime, cefoxitin, cefuroxime, cefoperazone and cefadroxil. Ceftriaxone showed capacity to bind to the fatty acid binding site on HSA. No relation was found between the displacement of the marker and the chemical nature of the substituents at R1 and R2. Cephalosporins interact with HSA at the binding region that involves: tyrosyl 411, histidyl 146 and lysyls 195, 199, 225, 240 and 525 residues. The chemical modification of specific amino acids showed that the interaction of these amino acids with beta lactam antibiotics is not carried out to the same extent for all the cephalosporins tested. The results obtained revealed that the binding sites for cephalosporins on albumin are structurally heterogeneous, having different amino acids in the vicinity of the ligand molecule.

Acid-Base Equilibrium↗
PubMed1987

Investigation of perchlorate, phosphate and ion-pairing eluent modifiers for the separation of cephalosporin epimers.

The retention behavior of several pairs of 7 alpha- and 7 beta-cephalosporin epimers was investigated using perchlorate, phosphate and ion-pairing eluent modifiers. At pH 2.5, sodium perchlorate, sodium phosphate and sodium pentanesulfonate all provided separation of epimers with free 7-amino groups. When the 7-amino group was blocked, as in cephalexin and cefaclor, sodium perchlorate gave the best separation at pH 2.5. A tetrabutylammonium ion-pairing system at pH 7.0 provided separation of all epimer pairs containing a free carboxylic acid at the 3 position. Hydrophobic, residual silanol and ionic interactions were factors in the retention mechanism of the cephalosporins under the conditions investigated. An ionic interaction of perchlorate with the protonated amine of the cephalosporin was postulated as an explanation of the retention and selectivity effects observed with perchlorate as an eluent modifier.

Cephalosporins↗
PubMed2000

Characterization of cephalosporin transfer between aqueous and colloidal phases by micellar electrokinetic chromatography.

A new electrokinetic chromatographic method was applied to the determination of the partition coefficient between water and micelle for a group of cephalosporins (cefmetazol, cephradin, cefaclor, ceftazidim, cefodizim, cephapirin, cephalothin and ceftriaxon) using sodium dodecyl sulphate as an anionic surfactant in microemulsion and in micellar systems. In the new method, the running buffer contains both the micelles and the drug, and the injected solution contains the same concentration of micelles as the running buffer but not the drug. The mobility of the drug can be measured from a negative peak recorded the chromatogram. The required parameters for the determination of the capacity factor (mu(aq) and /mu(me) are the electrophoretic mobilities of the solutes in the aqueous and the micelle phases, mu(eff) is the effective mobility in the micellar system or in the microemulsion) were measured by the new micellar and microemulsion electrokinetic chromatography technique. Linear log-log relationships were found between both the micelle-water partition coefficient and the capacity factor and the n-octanol-water partition coefficient.

Cephalosporins↗
PubMed1993

Histological and bacteriological findings in long-term ileocystoplasty and colocystoplasty in the rat.

The long-term effects of bladder reconstruction using bowel were studied in rats. Bladder surgery consisted of cystotomy and closure, ileo- or colocystoplasty, or placement of a reverse serosal (Thal) patch of ileum. At least one-third of all groups received prophylactic cefaclor, postoperatively. Monthly urine cultures were obtained, and survivors were sacrificed at 1 year. Antimicrobial therapy markedly reduced the incidence of chronic colonization after cystoplasty. However, the majority of rats in the Thal patch group remained colonized because of acquired vesicoileal fistulae. Vesical stones were often present in this group and were also seen in 6 of 43 (14%) and 3 of 33 (9%) in the ileocystoplasty and colocystoplasty groups, respectively. Transitional cell papillomas and/or hyperplasia was seen at 20 of 42 (48%) uroileal and 20 of 31 (64%) urocolonic anastomoses (p = .15). Hyperplastic lesions could not be correlated with bacteriuria. Focal nonpapillary transitional cell carcinoma was seen once in the colocystoplasty group, and low grade papillary transitional cell tumors were noted once in each of the cystostomy and ileocystoplasty groups and twice in Thal patch rats with ileovesical fistulae. These findings suggest that the rat uroenteric anastomosis is susceptible to proliferative change which is rarely malignant in nature and occurs in the presence or absence of bacteriuria.

Animals↗
PubMed1981

Recent advances in the pathogenesis, diagnosis, and management of otitis media.

1. Otitis media is one of the most common diseases of childhood. 2. Pathogenesis is related to eustachian tube dysfunction. 3. Etiology is primarily bacterial (S. pneumoniae, 40 per cent; H. influenzae, 20 per cent). Bacteria are also present in chronic otitis media with effusion ("secretory otitis"). 4. H. Influenzae is present in all age groups, and 15 to 30 per cent are ampicillin-resistant. 5. Diagnosis is by pneumatic otoscopy, or tympanometry, or both. 6. Tympanocentesis and/or myringotomy is important diagnostic-therapeutic procedure in selected patients. 7. Ampicillin (or amoxicillin) is initial therapy of choice. 8. Erythromycin and sulfonamide, trimethoprim-sulfamethoxazole, or cefaclor is recommended for those who have poor clinical response to initial antimicrobial therapy. 9. Efficacy is yet to be shown for antimicrobial prophylaxis, decongestants, antihistamines, myringotomy and tympanostomy tubes, and adenoidectomy with or without tonsillectomy. 10. Attendant conductive hearing loss is probably related to abnormalities in cognition, language, and learning.

Acoustic Impedance Tests↗
PubMed2001

Release profile of antimicrobial agents from alpha-tricalcium phosphate cement.

A new method for treating carious dentine with alpha-tricalcium phosphate (alpha-TCP) dental cement containing antimicrobial agents has been recently introduced. However, the release behavior of antimicrobial agents from this cement has not yet been clarified. The aim of this study is therefore to examine the release profile of the antimicrobial agents from the alpha-TCP cement. Three kinds of antimicrobial agents (metronidazole, cefaclor and ciprofloxacin) were added to two commercially available alpha-TCP cements (new apatite liner type I and type II). The set cements were then immersed in water at 37 degrees C and the released antimicrobial agents and Ca ion were determined at regular intervals for three months. In addition, scanning electron microscopic observations were conducted before and after immersion for three months. The release profile of the cements containing antimicrobial agents varied depending on the types of antimicrobial agents. The incorporation of antimicrobial agents affected the setting reaction of the cements. The release behavior of the drugs also varied depending on the types of the cements. The differences in the release profile between type I and type II cements reflected the structures and compositions of their matrices.

Anti-Infective Agents↗
PubMed1999

Safety profile of sparfloxacin, a new fluoroquinolone antibiotic.

The safety profile of sparfloxacin, a newer fluoroquinolone antibiotic, was examined through an integrated analysis of safety data from 6 multicenter phase III trials. These consisted of 5 double-masked, randomized, comparative trials of sparfloxacin (a 400-mg oral loading dose followed by 200 mg/d for 10 days) versus standard therapies (erythromycin, cefaclor, ofloxacin, clarithromycin, and ciprofloxacin) and I open-label trial (noncomparative) in patients with: community-acquired pneumonia (2 trials); acute bacterial exacerbations of chronic bronchitis (1 trial); acute maxillary sinusitis (2 trials, one of which was the noncomparative trial); and complicated skin and skin-structure infections (1 trial). Overall, 401 (25.3%) of 1585 patients treated with sparfloxacin and 374 (28.1%) of 1331 receiving a comparator regimen experienced at least 1 adverse event considered to be related to the study medication. Photosensitivity reactions, usually of mild-to-moderate severity, were seen more frequently with sparfloxacin (7.4%) than with comparator agents (0.5%), whereas gastrointestinal reactions (diarrhea, nausea, dyspepsia, abdominal pain, vomiting, and flatulence), insomnia, and taste perversion were more common in patients taking comparator drugs (22.3% vs 12.1%, 4.3% vs 1.5%, and 2.9% vs 1.2%, respectively). Analysis of electrocardiographic findings showed that the mean change from baseline in QT interval corrected for heart rate (QTc) was significantly greater in sparfloxacin-treated patients (10 msec) than in patients given comparator drugs (3 msec), but no associated ventricular arrhythmias were detected. Adverse events led to discontinuation of study medication in 104 (6.6%) patients receiving sparfloxacin and 118 (8.9%) given com parator drugs. Sparfloxacin may be considered an appropriate choice for the treatment of certain community-acquired infections for patients who are not at risk for photosensitivity reactions or adverse events associated with prolongation of the QTc interval.

Adolescent↗
PubMed2000

Sparfloxacin: a review.

BACKGROUND: The continuing increase in the rate of penicillin and cephalosporin resistance among respiratory pathogens and of cross-resistance to macrolide antibiotics has led to the recommendation that fluoroquinolone antibiotics be used to treat high-risk patients with community-acquired pneumonia (CAP) and acute bacterial exacerbations of chronic bronchitis (ABECB). OBJECTIVE: This review focuses on sparfloxacin, an oral fluoroquinolone, discussing its mechanism of action, activity, pharmacokinetic characteristics, safety, and efficacy in CAP and ABECB. METHODS: Studies were identified by a MEDLINE search of the literature from 1990 to 1999, supplemented by educational materials from conferences and symposia. RESULTS: Sparfloxacin is active against the major respiratory pathogens and against the atypical pathogens in pneumonia that are being reported with increasing frequency. Its long half-life permits once-daily dosing. In large trials in CAP and ABECB in which all isolates were susceptible to both comparators, sparfloxacin was found to have similar efficacy to erythromycin, cefaclor, amoxicillin, ofloxacin, and clarithromycin. Its safety profile is similar to that of the macrolides and other quinolone antimicrobial agents. Photosensitivity, nausea, and diarrhea are the most common adverse events reported in clinical trials of sparfloxacin. Its use is contraindicated in patients with QTc-interval prolongation. CONCLUSION: The increasing prevalence of beta-lactam- and macrolide-resistant bacteria in respiratory infections emphasizes the need for newer agents such as the fluoroquinolones. The choice between agents should be based on activity against the relevant respiratory pathogens in high-risk patients.

Anti-Infective Agents↗