Disease relevance of ROSAMICIN

• In vitro susceptibility of Ureaplasma urealyticum to rosaramicin [1].
• In vitro activity of rosaramicin against Chlamydia trachomatis [2].
• Evaluation of rosaramicin phosphate in treatment of experimental syphilis in rabbits [3].
• Rosaramicin treatment of gonococcal urethritis in men [4].
• Gastrointestinal side effects, including nausea, vomiting, and abdominal pain, occurred in ten of 19 patients given erythromycin and in 13 of 18 given rosaramicin [5].

High impact information on ROSAMICIN

• The absorption of oral solution was 58%, and the absolute bioavailability of rosaramicin was 35% [6].
• The pharmacokinetics of rosaramicin was studied in subjects receiving 500 mg of the drug (i) by 1-h intravenous infusion, (ii) in solution orally, or (iii) as tablets orally [7].
• Only a small amount of unchanged rosaramicin was present in the urine (7 to 9% of urinary radioactivity), but none was present in the feces [7].
• Roxithromycin and two other investigational macrolides (A-56268 and rosaramicin) demonstrated better in-vitro activity than erythromycin [8].
• Minimally elevated levels of alanine aminotransferase in serum occurred in four (22.2%) of 18 rosaramicin recipients [5].

Chemical compound and disease context of ROSAMICIN

• Inhibitory and lethal activities of rosaramicin, erythromycin, and clindamycin against Campylobacter fetus subsp jejuni and intestinalis [9].
• Ureaplasma urealyticum was eliminated from 12 of the 14 men treated with rosaramicin and from 15 of the 19 receiving tetracycline [10].
• A comparison of the in vitro activity of rosaramicin and minocin against 52 bovine Ureaplasma sp. strains, 20 of which were isolated from semen, 23 from vaginal swabs, and nine from preputial washings, has shown that both antibiotics have good inhibitory action against the strains tested [11].

Biological context of ROSAMICIN

• Pharmacokinetics and metabolism of rosaramicin in humans [7].
• The static effect of rosaramicin on Ureaplasma urealyticum and the development of antibiotic resistance [12].
• These results allow us to speculate that L18 and L19 belong to the high-affinity binding site of rosaramicin antibiotic [13].
• The enzyme (molecular mass 87 kDa) showed a high degree of substrate specificity, not acting on other glycosylated macrolides such as methymycin, lankamycin and rosaramicin which are substrates for the glycosyltransferase [14].
• In a test involving 41 cows inseminated once at estrus with rosaramicin-treated semen (162 mcg/mL) the nonreturn rate was 24% compared to a calculated average for this semen of 63% (n = 3310) [15].

Anatomical context of ROSAMICIN

• The excretion of rosaramicin in breast milk [16].
• The affinities of E. coli ribosomes for rosaramicin and dihydrorosaramicin are in good agreement with the minimal inhibitory concentration of these drugs for microorganisms [17].
• Two studies were conducted to assess the toxicity of rosaramicin (a macrolide antibiotic) when given intravenously for 30 consecutive days to beagle dogs with and without a tapetum lucidum (a light reflecting structure within the choroid of the eye) [18].
• Courses of treatment with tetracyclines, spectinomycin, erythromycin, rosaramicin, and clindamycin on each occasion reduced the numbers of ureaplasma isolated from the urethra and the severity of disease [19].

Analytical, diagnostic and therapeutic context of ROSAMICIN

• The plasma area under the curve of unchanged rosaramicin was only 5% that of total radioactivity after oral administration and 8% after i.v. administration, indicating extensive metabolism of the drug [6].
• A urinary metabolite of rosaramicin in man was isolated and purified by a preparative HPLC method [20].

References