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2.
Drugs Exp Clin Res ; 15(10): 465-76, 1989.
Article in English | MEDLINE | ID: mdl-2632215

ABSTRACT

The antimicrobial activity of ribostamycin, a unique aminoglycoside antibiotic possessing a neutral sugar component, was compared with those of gentamicin, ampicillin and lincomycin in vitro and in vivo. Ribostamycin showed comparable or slightly weaker in vitro activity than the reference antibiotics against Gram-positive bacteria. Against Gram-negative bacteria, ribostamycin was less active than gentamicin, but comparable to or more active than ampicillin. Lincomycin was less active or inactive to Gram-negative bacteria. Ribostamycin was active against some gentamicin-resistant bacteria, especially K. pneumoniae possessing the aminoglycoside-modifying enzymes AAC(3)-l and AAD(2"). The in vivo activity of ribostamycin was weaker than that of gentamicin, but comparable to that of ampicillin and lincomycin against Gram-positive bacteria, and superior to that of ampicillin against Gram-negative bacteria. The in vivo activity of ribostamycin was characterized by (i) and ED50 value not so affected by the challenge inoculum as that of ampicillin; (ii) a lower ED50 value by bolus administration than that by divided administration of the same dosage; and (iii) a lower ED50 value than that expected from the MIC value as compared with that of ampicillin and lincomycin. These characteristics are explained by the rapid and potent bactericidal activity of ribostamycin at high inoculum and high drug concentration, assisted by high serum concentration in mice.


Subject(s)
Anti-Bacterial Agents/pharmacology , Bacteria/drug effects , Bacterial Infections/drug therapy , Ampicillin/pharmacology , Ampicillin/therapeutic use , Animals , Anti-Bacterial Agents/therapeutic use , Bacterial Infections/microbiology , Gentamicins/pharmacology , Gentamicins/therapeutic use , Lincomycin/pharmacology , Lincomycin/therapeutic use , Male , Mice , Mice, Inbred ICR , Microbial Sensitivity Tests , Ribostamycin/pharmacology , Ribostamycin/therapeutic use
3.
J UOEH ; 6(1): 87-90, 1984 Mar 01.
Article in English | MEDLINE | ID: mdl-6433423

ABSTRACT

A 23-year-old unmarried man was infected with gonorrhoea from a prostitute in Fukuoka City and was treated with ampicillin which resulted in failure. By a rapid iodometric test it was found that the isolates before the treatment were penicillinase-negative. After the ampicillin treatment, however, the isolates turned to penicillinase-positive but were, in fact, a mixture of penicillinase-positive and penicillinase-negative gonococcal strains. Treatment by spectinomycin and doxycycline resulted in failure but the gonorrhoea was cured by ribostamycin.


Subject(s)
Gonorrhea/microbiology , Neisseria gonorrhoeae/enzymology , Penicillinase/biosynthesis , Adult , Drug Resistance, Microbial , Gonorrhea/drug therapy , Humans , Male , Neisseria gonorrhoeae/classification , Neisseria gonorrhoeae/isolation & purification , Ribostamycin/therapeutic use
6.
Minerva Med ; 73(34): 2169-78, 1982 Sep 08.
Article in Italian | MEDLINE | ID: mdl-7110598

ABSTRACT

Between April 1977 and April 1981, three schedules of prophylactic antibiotic therapy using four different antibiotics -- Cefaloridine, an association of Tobramycin-Lincomycin, and Ribostamycin -- have been employed in the surgical treatment of a series of patients. clinical experiments were carried out administering the dose of chosen antibiotic one hour before and a few hours after surgery, without prior selection of patients and without considering what type of surgery they were to undertake. The clinical series presented was submitted to statistical analysis for the purpose of monitoring the effectiveness of the therapeutic programmes adopted to prevent postoperative infections of the surgical focus and of the skin wound, comparisons also being made of the different types of drug. The high number and variability of the factors affecting this type of experiment are attributed equally to the patient's physiological and metabolic features and to the types of lesions and surgical intervention carried out. The rationality of these therapeutic solutions are assessed by comparison with traditional programmes of antibiotic administration carried out solely in the postoperative period for a prolonged time. Practicality, cost and incidence of side effects (infrequent) and the absence of serious toxic consequences are also discussed.


Subject(s)
Surgical Wound Infection/prevention & control , Adult , Aged , Cephaloridine/therapeutic use , Diarrhea/etiology , Female , Humans , Lincomycin/therapeutic use , Male , Middle Aged , Postoperative Care , Preoperative Care , Ribostamycin/therapeutic use , Tobramycin/therapeutic use , Urinary Catheterization/adverse effects , Urinary Tract Infections/etiology
8.
Immun Infekt ; 9(2): 66-71, 1981 Apr.
Article in German | MEDLINE | ID: mdl-7228116

ABSTRACT

Nephrotoxicity, pharmacokinetics, and therapeutic efficacy of ribostamycin were evaluated in rats. Measures of nephrotoxicity were urinary excretion of tubular cells and malate dehydrogenase. The i.v. injections of ribostamycin lead to the same tubular cell excretion values as the i.m. injections. Parallel administration of D-glucaro-delta-lactam reduced the nephrotoxic effect of ribostamycin significantly. The lowest dose which leads to a significantly increased loss of tubular cells was 20 mg/kg/d and was distinctly above that of gentamicin, indicating a lower nephrotoxicity. This corresponded to lower renal ribostamycin concentrations after a single dose administration as well as after 9 times repeated dosing. In chemotherapy of the acute pyelonephritis of the rat ribostamycin was inferior to gentamicin at dosages of 2.5 or 5 mg/kg.


Subject(s)
Anti-Bacterial Agents/therapeutic use , Pyelonephritis/drug therapy , Ribostamycin/therapeutic use , Animals , Female , Gentamicins/therapeutic use , Glucaric Acid/analogs & derivatives , Glucaric Acid/therapeutic use , Half-Life , Kidney/drug effects , Lactams/therapeutic use , Rats , Ribostamycin/metabolism , Tissue Distribution
9.
Minerva Med ; 71(4): 279-85, 1980 Feb 11.
Article in Italian | MEDLINE | ID: mdl-7354947

ABSTRACT

Results in the treatment of mostly Gram-negative infections of the respiratory apparatus (30 subjects) and the urinary apparatus (20 subjects) with ribostamycin are reported. These were regarded as good overall, as shown by the bacteriological findings. An extremely high sensitivity to the antibiotic was noted in isolated germs from both types of infection. This good response in vitro was matched by an equally encouraging bacteriological result in vivo.


Subject(s)
Anti-Bacterial Agents/therapeutic use , Bacterial Infections/drug therapy , Respiratory Tract Infections/drug therapy , Ribostamycin/therapeutic use , Urinary Tract Infections/drug therapy , Adult , Aged , Bacteria/drug effects , Female , Humans , Male , Microbial Sensitivity Tests , Middle Aged , Ribostamycin/pharmacology
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