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Biomedical subjects

W Stille

Publications and source records attributed to W Stille.

At least 55 records · Page 3Linked to original sources

4-quinolones inhibit biotransformation of caffeine.

The pharmacokinetics of caffeine, including formation of its major metabolite paraxanthine in plasma, has been investigated in 12 healthy males (age 20-40 years) alone and during co-administration of the 4-quinolones ofloxacin, norfloxacin, pipemidic acid, ciprofloxacin, and enoxacin; ciprofloxacin and enoxacin were given in 3 different dose levels. The naphthyridine derivative enoxacin and the pyrido-pyrimidine derivative pipemidic acid had caused marked inhibition of caffeine and paraxanthine metabolism, whereas the genuine quinolone derivatives norfloxacin and ciprofloxacin had little effect, and the pyrido-benzoxacine derivative ofloxacin had no detectable effect. The different molecular and spatial structures of the compounds appear to be responsible for the differences in inhibitory potency.

Adult↗

Clinical efficacy and safety of teicoplanin.

This was an open efficacy and safety study in 310 hospitalized patients (187 male and 123 female) with infection by Gram-positive bacteria. The age range was 12-88 years (mean 49.8 years), and 80 of the patients were older than 65 years. Teicoplanin was given either by fast iv or by im injection, in most cases at a dose of 200 or 400 mg every 24 h with an initial dose of 400 mg. For both routes of administration the mean total daily dose was 286 +/- 5 mg/day. The mean duration of treatment was 8.2 days (range 1-37 days). The infections comprised 133 skin or soft tissue, 53 joint or bone, 40 urinary tract, 39 upper respiratory tract, 21 lower respiratory tract, nine septicaemia, four gastro-intestinal tract and 11 miscellaneous. All Gram-positive bacteria isolated were sensitive to teicoplanin. Teicoplanin was the sole antimicrobial agent given in 269 of the 310 patients. Clinical cure occurred in 79.7%, and improvement in 13.6%. Adverse events related to teicoplanin occurred in 7.7% of the patients. Most were minor and in only six patients was treatment discontinued because of adverse events (three allergy, two bronchospasm, one tremor). The laboratory values and audiometry indices in 67 patients showed no significant changes. Teicoplanin was considered an effective and well-tolerated treatment for Gram-positive infections in this study.

Adolescent↗

[Ciprofloxacin in combination with other antimicrobial substances].

The antibacterial activity of ciprofloxacin, either alone or in combination with azlocillin, imipenem, mezlocillin or tobramycin, was tested against enterococcus and pseudomonas species. No synergy or antagonism was found by means of the checkerboard titration method used. Subsequently, the bactericidal activity of ciprofloxacin (2 x minimal inhibitory concentration, MIC), azlocillin, imipenem, mezlocillin or tobramycin (2 x MIC) either alone or in combination (1 x MIC each of each substance) was tested against individual strains. No reduction of bactericidal activity in comparison with the effect of the single substances at higher concentration was found, even though the concentrations of each substance were halved. An antagonism is unlikely when ciprofloxacin is combined with one of the beta-lactams studied or with tobramycin. More likely is a slight synergistic effect.

Anti-Bacterial Agents↗

Autopsy findings in AIDS--a histopathological analysis of fifty cases.

Fifty consecutive AIDS autopsy cases were evaluated. All subjects showed one or more opportunistic infections and malignancies included in the AIDS case definition with cytomegalovirus and Kaposi's sarcoma being most prevalent. Mycobacterial and cryptococcal infections occurred only infrequently. Most patients of our series after successful treatment of Pneumocystis carinii pneumonia or cerebral toxoplasmosis later succumbed to less treatable conditions like disseminated cytomegalovirus or fungal infections or malignant lymphoma. In the absence of specific treatment for the HIV infection leading to these lethal complications special emphasis must be put on the prevention of HIV transmission and spread.

Acquired Immunodeficiency Syndrome↗

[Cryptosporidium infections in AIDS].

Investigations for cryptosporidia were carried out on 250 fecal samples from 131 HIV-positive patients between December 1985 and July 1986 with kinyoun carbolfuchsin staining. Cryptosporidial oocysts could be detected in six homosexual men. All of the cryptosporidia excretors had symptoms of enteritis. The clinical course and the prognosis depended on the immunological resistance of the host. Five patients with pronounced immune defect had therapy-resistant chronic diarrhea. In one patient with a slight immune defect, the cryptosporidial infection cured spontaneously. A spacial separation of cryptosporidia excretors and patients with weakened resistance is to be considered in view of the possible severe progress form with low tendency to cure and the still lacking specific chemotherapy.

Acquired Immunodeficiency Syndrome↗

Decrease of caffeine elimination in man during co-administration of 4-quinolones.

The single dose pharmacokinetics of caffeine (220-230 mg per dose) were investigated in 12 healthy male volunteers before and during treatment with ofloxacin (200 mg bd), ciprofloxacin (250 mg bd) and enoxacin (400 mg bd) with a cross-over study design. None of the parameters: mean elimination half-life (T1/2el), Cmax, total body clearance (Cltot) and the volume of distribution (aVd) of caffeine were noticeably altered by administration of ofloxacin. Striking changes were observed, however, after administration of enoxacin: the T1/2el was prolonged by as much as 260%, the Cmax increased by 41%; the aVd was reduced by 20% and Cltot by 78% (mean values). Treatment with ciprofloxacin led to a prolongation of T1/2el by 15%, to a decrease of aVd by 25% and to a 33% decrease of Cltot. The results of this intra-individual comparison of caffeine pharmacokinetic data demonstrate that treatment with ciprofloxacin and enoxacin may have a significant inhibitory effect on caffeine elimination.

Adult↗

Bactericidal activity of ofloxacin versus roxithromycin in the treatment of Streptococcus pneumoniae.

Ofloxacin is highly active against Gram-negative aerobic bacilli, but moderately active against Gram-positive cocci. The minimal inhibitory concentrations (MICs) against Streptococcus pneumoniae range between 1 and 2 mg/L. MICs of roxithromycin (RU 28965) against S. pneumoniae range between 0.004 and 0.03 mg/L, but Gram-negative bacilli are resistant. The bactericidal activities of ofloxacin and roxithromycin were evaluated against 15 strains of S. pneumoniae, which were isolated recently from clinical specimens. Killing activity was evaluated under conditions simulating serum pharmacokinetic parameters. Initial concentrations were 10 mg/L for roxithromycin and 2 mg/L for ofloxacin, and the half-life was 6 hours for both compounds. Under these conditions, roxithromycin was rapidly bactericidal. The speed at which pneumococci were killed was faster with roxithromycin than with ofloxacin. No regrowth was seen with roxithromycin, but regrowth occurred in 8 of 15 strains with ofloxacin.

Anti-Bacterial Agents↗