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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Pharmacy world & science 8 (1986), S. 40-41 
    ISSN: 1573-739X
    Keywords: Drug evaluation, preclinical ; Drug resistance ; Pharmacokinetics ; Quinolones ; Side effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract On the basis of antimicrobial activity, resistance development, pharmacokinetics, side effects and pre-clinical results, the applicability of the quinolones ciprofloxacin, enoxacin, norfloxacin, ofloxacin and pefloxacin is assessed. These quinolones seem especially useful in infections in hospitalized patients, in gonococcal infections and in urinary tract infections. Also salmonellosis and shigellosis might be indications for quinolones.
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Pharmacy world & science 8 (1986), S. 26-28 
    ISSN: 1573-739X
    Keywords: Drug resistance ; In vitro activity ; Quinolones ; Spectrum of activity
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The first quinolone compound, nalidixic acid, showed activity against a limited number of Gram-negative micro-organisms. ‘One step’ resistance developed hiin vitro and during treatment. Resistance was not mediated by transfer of R-plasmids, which is a characteristic of all quinolones. Newer quinolones like oxolinic acid, piromidic acid, cinoxacin and pipemidic acid exhibit an extended spectrum of activity against Gram-negative bacteria at lower MIC values. In recent years fluorinated quinolones were introduced like ciprofloxacin, norfloxacin, pefloxacin, ofloxacin, enoxacin and amifloxacin. These compounds exhibitin vitro a broad spectrum of activity against Gram-negative and Gram-positive bacteria at MIC values seventy to four hundred times less than those for nalidixic acid. Thein vitro activity of these compounds has been investigated in a large study of uncomplicated urinary tract infections in general practice (PINISU). No resistance was found. The fluorinated quinolones are very promising antimicrobial agents for a limited number of indications.
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Pharmacy world & science 11 (1989), S. 3-8 
    ISSN: 1573-739X
    Keywords: Biochemistry ; Clofazimine ; Dapsone ; Ethionamide ; Isoniazide ; Mechanism of action ; Mycobacterium leprae ; Prothionamide ; Quinolones ; Ribonucleotide reductase inhibitors ; Rifampicin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract From a pharmacochemical point of view the existing anti-leprotics as well as possible innovations in the chemotherapy of leprosy are discussed. Of the main anti-leprotics, which are used nowadays — dapsone, rifampicin, clofazimine, isoniazide, ethionamide and prothionamide — the mechanism of action, the main problems in their application and possibilities to develop improved variants are reviewed. Based on the chemistry ofMycobacterium leprae, the target systems for new anti-leprotics are identified. These systems include the cell wall, the catabolism of reactive oxygen species, the metabolisms of carbon sources, the amino acid metabolism and the uptake of iron. Two possible new lead structures from other fields, 4-quinolones and mycobacterial ribonucleotide reductase inhibitors are presented.
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    Pharmacy world & science 11 (1989), S. 33-43 
    ISSN: 1573-739X
    Keywords: Bacteriology ; Ciprofloxacin ; Clinical trials ; Fleroxacin ; Lomefloxacin ; Pharmacokinetics ; Quinolones ; Temafloxacin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The properties of several new, investigational quinolones are reviewed. Desirable characteristics of new quinolones are improved activity against especially Gram-positive bacteria, longer elimination half-life, slower development of resistance, fewer side effectsetc. Fleroxacin and lomefloxacin have entered phase III trials: their main advantage lies in improved pharmacokinetics. AM-1091, AT-4140 and T-3262 are still in early phases of development and show improved activity against Gram-positive bacteria. They also show a reduced penetration of the blood-brain barrier, probably resulting in fewer side effects in the central nervous system. AM-1091 shows incomplete cross-resistance with ciprofloxacin.
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  • 5
    Electronic Resource
    Electronic Resource
    Springer
    Pharmacy world & science 11 (1989), S. 132-133 
    ISSN: 1573-739X
    Keywords: Bronchitis ; Cross infection ; Immunocompromised host ; Pneumonia ; Quinolones
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The new quinolones are rarely indicated for the treatment of community-acquired pneumonia in the normal host. For nosocomial pneumonia they may be used when a Gram-negative aerobic bacillus is the causative organism. Pneumonia in the compromised host may be an indication for a quinolone. In the hypogammaglobulinaemic patient withHaemophilus influenzae pneumonia, the quinolones may be used, especially when the organism is resistant to other drugs. For the neutropenic patient with Gram-negative pneumonia the quinolones may be a good choice. However, more clinical studies are needed. In treatment for exacerbations of chronic bronchitis, failures seem to be associated with pneumococcal infections. For patients with cystic fibrosis, the quinolones offer successful ambulatory treatment for theirPseudomonas andHaemophilus infections. The information regarding dosage schedules is still incomplete.
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    Pharmacy world & science 8 (1986), S. 22-25 
    ISSN: 1573-739X
    Keywords: DNA gyrase ; Drug resistance ; Mechanism of action ; Quinolones ; Structure-activity relationship
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The quinolones are synthetic antibiotics chemically related to nalidixic acid. Since its introduction, several structural analogues have been synthesized. A fundamental breakthrough was the addition of a fluorine atom. The quinolones interfere with bacterial DNA transcription by inhibiting the enzyme DNA gyrase, that so far has only been found in bacteria. The nature of the activity of the quinolones on DNA gyrase makes it highly unlikely that resistance is carried on plasmids.
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    Springer
    Pharmacy world & science 8 (1986), S. 72-78 
    ISSN: 1573-739X
    Keywords: Bacterial infections ; Drug resistance ; Drug treatment ; Intestinal decontamination ; Quinolones ; Side effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract A comparative evaluation is made on activity, resistance problems and side effects of nine quinolones. These data and the information on clinical experiences are used to outline the author's view on the present position of these compounds in treatment policies. The following indications seem appropriate: norfloxacin or pipemidic acid in lower urinary tract infection, secondary to nitrofurantoin and sulfonamides; one of the more active quinolones, like ciprofloxacin, in case of therapy failure or multiple resistance; application for gonorrhoea appears attractive, but data on long-term effects and resistance are needed; in antibacterial combinations for selective bowel decontamination. Comparative clinical trials are essential before other indications for quinolones in clinical policies can be defined.
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  • 8
    Electronic Resource
    Electronic Resource
    Springer
    Pharmacy world & science 8 (1986), S. 1-21 
    ISSN: 1573-739X
    Keywords: Drug evaluation ; Drug interactions ; Drug resistance ; Mechanism of action ; Minimum inhibitory concentration ; Pharmacokinetics ; Quinolones ; Side effects ; Structure-activity relationship
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Quinolones, chemically related to nalidixic acid, have a strong and rapid bactericidal action against Gram-negative bacteria, includingPs. aeruginosa, someMycobacteria, Legionella andStaphylococci. Streptococci and anaerobic bacteria are usually less sensitive. The quinolones exert their bactericidal action through inhibition of the enzyme DNA gyrase. Quinolones are absorbed for 50–100% from the gastro-intestinal tract, their volume of distribution is generally high (2 l/kg) and high concentrations are reached in almost all organs. The elimination half-lives range from 4 to 14 h. The efficacy of quinolones in urinary tract infections has been shown in many studies. They also seem to be effective in many serious infections. In animal studies their efficacy was generally equal or superior to aminoglycosides. Until now only mild and infrequent side effects have been reported.
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  • 9
    ISSN: 1573-739X
    Keywords: Absorption ; Kidney failure ; Metabolism ; Pharmacokinetics ; Quinolones ; Renal excretion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The quinolones are relatively poorly absorbed from the gastrointestinal tract. The elimination proceeds mainly by renal excretion. The half-life of elimination depends on the molecular structure and varies between 2 and 10 h. Impaired kidney function is expected to increase the half-life of elimination. though this effect is not always observed. Since the 4-oxo-metabolites show a higher renal clearance than the parent drug, renal impairment will result in a cumulation of the metabolites in the body.
    Type of Medium: Electronic Resource
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  • 10
    ISSN: 1573-739X
    Keywords: Bronchitis ; Drug evaluation ; Drug interactions ; Minimum inhibitory concentrations ; Pharmacokinetics ; Quinolones ; Side effects ; Theophylline
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Results are presented from 186 hospitalized patients treated for acute purulent exacerbations of chronic bronchitis with orally administered ciprofloxacin (80 patients), enoxacin (26 patients), ofloxacin (30 patients) or pefloxacin (50 patients). In general, good clinical results were observed in 50–70% of the patients treated, most failures being due to relapses or reinfections withStreptococcus pneumoniae orPseudomonas aeruginosa. Studies on blood and sputum concentration suggested that gastro-intestinal absorption was not always satisfactory. Unwanted drug effects were noted with all agents studied, generally presenting as stomach pain, nausea, hallucinations, or dizziness. Most adverse drug reactions were seen with enoxacin, often but not always during concomitant treatment with theophylline.
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