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PubMed1996

Antimicrobial ear drop medication therapy.

Ear drop medication, which delivers a concentrated drug directly to the lesion, is a useful therapeutic approach in that it provides enhanced efficacy at the affected site while avoiding the side effects accompanying systemic administration of the drug. In the present study we evaluated the effectiveness of three recently developed antibacterial agents with no proven ototoxicity: cefmenoxime (CMX), fosfomycin (FOM), and ofloxacin (OFLX). The bacterial eradication rate, the bacterial persistence rate, and the fungal infection rate were 91.4%, 2.9% and 5.7% for CMX, 71.2%, 20.9% and 7.0% for FOM, and 88.4%, 4.7% and 7.0% for OFLX, respectively. For lomefloxacin (LFLX) (with one week of treatment), the eradication rate and the persistence rate were 80.2% and 19.8%, respectively. It is advisable to limit the duration of treatment with the same otic drug; using the drug for more than 4 weeks at the most should be avoided.

Administration, Topical↗
PubMed1996

[Antibiotic sensitivity of aerobic gram-negative bacilli isolated from severe infections in 1992: results of a French multicenter study. Groupe d'Etude d'Infections à bacilles à Gram Négatif (GEIGN)].

OBJECTIVES: Antibiotic susceptibility of 649 gram-negative bacilli involved in severe infections and isolated in 18 teaching hospitals from January to December 1992 was evaluated. METHODS: Minimal Inhibitory Concentrations were determined by agar dilution method for piperacillin, piperacillin+ tazobactam and imipenem, and by a microdilution method for 11 other antibiotics (amoxicillin, amoxicillin + clavulanic acid, cefotaxime, ceftazidime, aztreonam, ticarcillin, ciprofloxacin, fosfomycin, tobramycin, gentamicin, amikacin). Criteria of Comité Français de l'Antibiogramme de la Société Française de Microbiologie were followed for interpretation. Betalactamases were identified by isoelectric focusing and overproduction of cephalosporinase was defined by the resistance phenotype. The main species isolated were Escherichia coli (45%), Pseudomonas aeruginosa (14%), Klebsiella pneumoniae (7.8%), Salmonella spp. (7.5%), Enterobacter cloacae (4%) and Klebsiella oxytoca (4%). Most of the strains were isolated from blood culture (72.3%), respiratory tract (11.4%) and intraabdominal infections (8.6%). Most of the enterobacteria isolates were susceptible to imipenem, aztreonam, amikacin and ciprofloxacin (percentages of susceptibility were respectively 99.3, 98, 98.3 and 96.3); in most of cases clavulanic acid did not entirely restore sensitivity to amoxicillin of penicillinase-producing strains. Among 89 P. aeruginosa strains, 82% were susceptible to imipenem and ceftazidime, 81% to the association piperacillin + tazobactam and 51% to ticarcillin. Resistance rates are very high for Acinetobacter baumannii except for imipenem. CONCLUSION: Production of TEM-type penicillinase and over-production of the chromosomal cephalosporinase are the most widely observed mechanisms of resistance (respectively 22% and 9% of 649 strains). Prevalence of extended spectrum betalactamases was low (1%) and essentially observed for K. pneumoniae.

Anti-Bacterial Agents↗
PubMed1997

[Serotypes and drug susceptibility of Pseudomonas aeruginosa isolated from clinical specimens].

Between January, 1982 and December, 1994, 236 Pseudomonas aeruginosa strains were isolated from clinical specimens at our division, and were tested for serotypes and drug-susceptibilities to 15 antibiotics. Serotype G strains were isolated at the highest frequency (32.6%), and followed by strains of serotype B (15.7%), A (11.9%), E (9.3%), I (7.2%), F and M (5.5%), non-typable (5.1%), D (3.4%), H (2.1%), C and K (0.8%). We examined the changes of isolation frequencies of different serotypes annually. Isolation frequencies of serotypes E and F showed tendency to decrease, whereas serotype I has been isolated increasingly year by year. MIC90's of the 15 antibiotics were as follows, tosufloxacin: 0.78 microgram/ml, biapenem (BIPM) and ofloxacin (OFLX): 3.13 micrograms/ml, imipenem (IPM), ceftazidime, cefozopran, cefsulodin and gentamicin: 6.25 micrograms/ml, aztreonam and amikacin: 12.5 micrograms/ml, piperacillin, cefoperazone and minocycline (MINO): 25 micrograms/ml, fosfomycin: > 100 micrograms/ml and chloramphenicol: > 200 micrograms/ml. MIC90'S of IPM, BIPM, MINO and OFLX increased 4-fold from stage I (1982-1987) through stage III (1992-1994) and the isolation frequency of drug-resistant strains increased year by year. In other words, antibiotic resistant strains appeared increasing with time. No relationship between serotypes and drug-resistance were observed.

Anti-Bacterial Agents↗
PubMed1997

[Kinds of antimicrobial agents and their mode of actions].

Hardness of development of drug-resistant bacteria has cross relation with mechanisms of antibacterial activities of antimicrobial agents. When the site of action of certain antibiotic is single enzyme and the enzyme can be converted to tolerant against the antibiotic by change of single amino acid retaining the enzymatic activity, drug-resistant bacteria can emerge easily. On the other hand, if the site of action is complex metabolic reactions, the drug-resistant bacteria would emerge hardly, because multiple mutations are required in this case. So that knowledges of mechanisms of antimicrobial agents are important to prevent the development of drug-resistant bacteria. Antimicrobial agents are classified into several categories, i.e. inhibitors for bacterial cell wall such as beta-lactam drugs, fosfomycin, and vancomycin; inhibitors for protein biosynthesis such as tetracyclibnes, macrolides, aminoglycoside antibiotics; inhibitors for DNA synthesis such as 4-quinolones; inhibitors for RNA synthesis such as rifampicin.

Anti-Bacterial Agents↗
PubMed1997

Acinetobacter radioresistens metabolizing aromatic compounds. 2. Biochemical and microbiological characterization of the strain.

The metabolic potentialities of an Acinetobacter radioresistens strain, isolated from the soil adjacent to an activated sludge plant, were investigated. Among 26 aromatic substrates tested, only phenol, benzoate and catechol were metabolized. Since this strain possessed abundant plasmid DNA, the antibiotic and heavy metal resistance was examined, and the bacterial cells proved to be sensitive to all metals (Ni, Tl, Pb, Cd, Ag, Co, Zn) and antibiotics tested except for Fosfomycin and chloramphenicol. The degradation kinetics for phenol and benzoate as the sole carbon/energy source (pH 7, 30 degrees C) displayed different trends, confirmed by the bacterial growth curve. Crude extracts from phenol-grown cultures showed both phenol hydroxylating activity and catechol dioxygenating activity. Phenol hydroxylase possessed a reductase component able to reduce nitroblue tetrazolium (NBT) and cytochrome C, thus exhibiting differences from previously reported monocomponent phenol hydroxylases from the same genus. Catechol dioxygenase is an intradiol-cleaving enzyme recognizing also substituted catechols.

Acinetobacter↗
PubMed1996

[Typing, resistance behavior and occurrence of methicillin-resistant Staphylococcus aureus strains in a surgical intensive care unit].

Over a period of three years, the frequency of the appearance of methicillin-resistant S. aureus strains (MRSA) was observed on a surgical intensive care unit. During this above-mentioned period of investigation it came to a heaped occurrence of nosocomial infections on this ICU with altogether 332 S. aureus-stems being isolated from different patient specimen. 204 (61.5%) of these were resistant against methicillin and could be divided into 48 first- and 156 follow-up-isolates. The thereupon accomplished differentiation of the 48 MRSA-first isolates by means of lysotyping and the pioneered GenePath Strain Typing System for a standardized pulsed-field-gel-electrophoresis (PFGE) gave the proof of 7 different MRSA-types. Around 7 different, in part parallel chains of infection on this ICU were observed, which could be led back to different strains. In reference to all analyzed S. aureus, an especially high rate (90%) of MRSA on this ICU could be isolated in taken wound-swabs, followed by 83.3% MRSA at catheter tips and 71,9% in tracheal and bronchial secretion. A consideration of the antibiotic susceptibility yielded, that also gentamicin and the quinolones showed an in-vitro resistance against MRSA, while fosfomycin, fusidic acid, chloramphenicol and trimethoprim/sulfamethoxazole reached positive responding rates between 80 and 100%. On the other hand, presently still 100% of the explored MRSA-strains are susceptible for glycopeptides such as vancomycin and teicoplanin. Because of intensive hospital hygienic measures the number of newly isolated MRSA could be reduced clearly on this ward.

Anti-Bacterial Agents↗
PubMed1998

Bacterial pathogens (non-Mycobacterium) from sputum culture and antimicrobial susceptibility.

Sputum culture of patients at Siriraj Hospital, Bangkok was 49.84% positive for bacterial pathogens in 1994 and 40.95% in 1995. The average incidence of gram-negative rods was 3.11 fold more than the combination of gram-positive cocci and gram-negative cocci. The most common gram-negative rod was Pseudomonas aeruginosa, followed by either Klebsiella pneumoniae or Acinetobacter anitratus depending on year. The most common coccus was Staphylococcus aureus. From both years, the number of Haemophilus influenzae, Streptococcus pneumoniae, Burkholderia pseudomallei and Nocardia spp isolated were 122, 93, 13 and 11 strains respectively. For antimicrobial susceptibility, P. aeruginosa was sensitive to ceftazidime, imipenem, gentamicin, amikacin, netilmicin, ciprofloxacin (range 56-89%). S. aureus (MSSA) was sensitive to common used drugs. S. aureus (MRSA) was sensitive to co-trimoxazole, fosfomycin, vancomycin (range 57-100%) and resistant to most drugs.

Anti-Bacterial Agents↗
PubMed1998

[Peptostreptococcus magnus osteoarticular infections after orthopedic surgery. 14 cases and pathogenicity factors].

We report a retrospective study of 14 Peptostreptococcus magnus bone and joint infections, following orthopaedic prostheses or implantation of fixation devices, diagnosed in two Paris hospitals between 1992 and 1996. Five patients experienced a knee joint infection after anterior cruciate ligament reconstruction with 4 artificial grafts, and 9 caught joint or wound infections, after limb traumatic injuries or bone neoplastic ruptures involving femur, tibia, calcaneum and humerus, treated by arthroplasty or osteosynthesis with implantation of biomaterials. Septic arthritis was experienced one week to one year after reconstructive surgery, and had evolved for several months to years before etiologic diagnosis in 5 cases. Specimens of pus, tissues or removed implants produced numerous slow growing small colonies of Gram positive cocci arranged in clumps on culture media incubated in anaerobic atmosphere only. In 10 patients, the same organism was disclosed in several separate specimens. The identification of P. magnus was assessed by the enzyme profile (rapid ID 32A API strips), gaz liquid chromatography, catalase and coagulase production, resistance to novobiocin and Na polyanethol sulphonate. Antibiotic sensitivity testing performed by disc method was constant to penicillin G, amoxicillin, cefuroxime, cefoxitin, imipenem and pristinamycin with penicillin G MICs < 0.125 mg/l and metronidazole MICs < 1 mg/l. Erythromycin, clindamycin, rifampicin, tetracycline and fosfomycin were active against more than 70% of P. magnus. All patients were cured after a prolonged course of various antibiotics and surgical removal of the foreign material whenever possible. We studied in vitro binding of P. magnus with extracellular matrix proteins adsorbed onto biomaterials, by particle agglutination assays of latex beads coated with proteins. Eighty one% of strains bound to collagen, 69% to fibrinogen and 46% to fibronectin. Comparison of orthopaedic strains with strains of other infections and from skin showed a correlation between P. magnus from bone and joint infections and their fibrinogen binding ability (69% against 20%, p < 0.05).

Adolescent↗
PubMed2003

New antimalarial drugs.

Approximately 40% of the world population live in areas with the risk of malaria. Each year, 300-500 million people suffer from acute malaria, and 0.5-2.5 million die from the disease. Although malaria has been widely eradicated in many parts of the world, the global number of cases continues to rise. The most important reason for this alarming situation is the rapid spread of malaria parasites that are resistant to antimalarial drugs, especially chloroquine, which is by far the most frequently used. The development of new antimalarial drugs has been neglected since the 1970s owing to the end colonialism, changes in the areas of military engagement, and the restricted market potential. Only in recent years, in part supported by public funding programs, has interest in the development of antimalarial drugs been renewed. New data available from the recently sequenced genome of the malaria parasite Plasmodium falciparum and the application of methods of modern drug design promise to bring significant development in the fight against this disease.

Aminoquinolines↗
PubMed2005

Alkoxycarbonyloxyethyl ester prodrugs of FR900098 with improved in vivo antimalarial activity.

FR900098 represents a derivative of the new antimalarial drug fosmidomycin with enhanced activity. The mechanism of action is the inhibition of the 1-desoxy-D-xylulose 5-phosphate (DOXP) reductoisomerase, an essential enzyme of the mevalonate independent pathway of isoprenoid biosynthesis. Prodrugs with increased oral activity in mice infected with the rodent malaria parasite Plasmodium vinckei were obtained by masking the phosphonate moiety of FR900098 as alkoxycarbonyloxyethyl esters.

Administration, Oral↗
PubMed2005

A fragment-based approach to understanding inhibition of 1-deoxy-D-xylulose-5-phosphate reductoisomerase.

The inhibition of 1-deoxy-D-xylulose-5-phosphate reductoisomerase (DXR) by fosmidomycin was studied by using a kinetic assay based on the consumption of NADPH and synthetic substrate. Fosmidomycin is a slow tight-binding inhibitor of DXR that shows strong negative cooperativity (absolute value(h) = 0.3) in binding. Cooperativity is displayed during the initial (weak, K0.5 = 10 microM) binding event and does not change as the binding tightens to the equilibrium value of 0.9 nM over a period of seconds to minutes. A series of fosmidomycin fragments was examined, but all showed much weaker inhibition, in the mM range. A series of cyclic fosmidomycin analogues was also synthesised and tested, but these showed high-microM binding at best. None of the synthetic compounds showed time-dependent inhibition. We concluded that the slow tight-binding behaviour, and perhaps also cooperativity, are mediated by significant reorganisation of the active site upon fosmidomycin binding. This makes the rational design of new inhibitors of DXR difficult at best.

Aldose-Ketose Isomerases↗
PubMed1975

Rapid methods for bioavailability determination utilizing urinary excretion data.

Two equations were developed which enable urinary excretion data to be utilized for estimating drug bioavailability within 12 hr-starting between one and two half-lives of the drug, depending upon the relative rates of absorption, distribution, and elimination. Both equations were examined using simulated data for both the one- and two-compartment open models. One equation was tested using literature data with excellent results.

Absorption↗
PubMed2005

The plastid of Plasmodium spp.: a target for inhibitors.

Determined efforts are being made to explore the non-photosynthetic plastid organelle of Plasmodium falciparum as a target for drug development. Certain antibiotics that block organellar protein synthesis are already in clinical use as antimalarials. However, all the indications are that these should be used only in combination with conventional antimalarials. The use of antibiotics such as doxycycline and clindamycin may reduce the development of drug resistant parasites and such means to avoid drug resistance should be explored hand-in-hand with drug development. Genomic information predicts that fatty acid type II (FAS II) and isoprenoid biosynthetic pathways are localized to the plastid. However, clinical trials with fosmidomycin (a specific inhibitor of DOXP reductase in the non-mevalonate pathway for isoprenoids) suggest it too should only be used in drug combinations. Prospects for more potent antimalarial compounds have emerged from studies of several of the enzymes involved in the FAS II pathway. Lead antibiotics such as thiolactomycin (an inhibitor of beta-ketoacyl-ACP synthase) and triclosan (a specific inhibitor of enoyl-ACP reductase) have led to structurally similar, active compounds that rapidly kill ring- and trophozoite-stage parasites. The FAS II pathway is of particular interest to the pharma-industry.

Animals↗
PubMed1993

Cefotaxime desensitization.

We report the successful desensitization to cefotaxime in a patient with severe lumbar osteomyelitis of unknown bacteriology and hypersensitivity to the drug. Desensitization was carried out because of the unknown bacteriology, the favorable response to cefotaxime at that time, and hypersensitivity to other antibiotics. On the first day the patient received 1 mg cefotaxime intravenously. The dose was increased for 13 successive days to 4 g cefotaxime intravenously per day. No allergic reaction occurred during desensitization or within 4 weeks of observation under this therapy. Patients with severe infections of unknown bacteriology might benefit from desensitization if therapy with a second-choice antibiotic is impossible.

Cefotaxime↗
PubMed1985

Renal gammagraphy with 99mTc-phosphomycin.

99mTc-Phosphomycin, a new radiopharmaceutical for kidney visualization, was used for animal experiments and tests of 171 patients. The results confirmed the usefulness of this product. The ease and yield of the labelling procedure, the low cost of the product, the excellent quality of the images and the functional information obtained showed that the use of 99mTc-phosphomycin as a radiopharmaceutical for kidney visualization has many advantages.

Adolescent↗
PubMed1983

The influence of uremia on the accessibility of phosphomycin into interstitial tissue fluid.

The entry and persistence of phosphomycin in interstitial tissue fluid (ITF) were studied in 9 patients with normal renal function and 8 patients with varying degrees of renal impairment, all of whom received a single i.v. dose of 30 mg/kg. ITF was obtained from skin blisters produced by suction. The antibiotic followed a two-compartment open kinetic model. In patients with normal renal function, phosphomycin is incorporated rapidly into the ITF reaching a level of 60.4 micrograms/ml 60 min after administration. There was no statistically significant difference between the elimination rates from serum and ITF. The serum half-life of the slow disposition phase was 1.75 h in patients with normal renal function. There was a linear correlation between the elimination half-life of phosphomycin in serum and ITF in subjects with differing degrees of renal impairment.

Adult↗
PubMed1983

[Release delay of various antibiotics from resorbable tricalcium phosphate ceramic granules with soluble coating for local treatment of osteomyelitis. An animal experiment study].

The releasing kinetic of antibiotics from tricalcium phosphate beads was studied in animal experiments. The porous TCP-beads were filled with antibiotics and coated with biodegradable substances for delaying the release of the antibiotics. There were high tissue levels of antibiotics in the surrounding bone for many days. This method gains an increase in therapeutic safety in treatment of osteomyelitis. The coated TCP-antibiotic beads are used simultaneously as bone graft and for treatment of the bone infection. There is no need for further operation.

Animals↗