Biological Studies With Rosamicin, a New Micromonospora-Provuced Macrolide Antibiotic

Waitz, J. A.; Drube, C. G.; Moss, Eugene L.; Weinstein, Marvin

doi:10.7164/antibiotics.25.647

Cited by 44 publications

(24 citation statements)

References 5 publications

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“…The activity of rosamicin against M. hominis was greatly diminished compared to its activity against ureaplasmas and was consistent with the findings of WALTZ et al 9) Although rosamicin has shown very good action against ureaplasmas, it remains to be seen whether this drug is as effective in vivo as it is in vitro.…”

Section: Discussionsupporting

confidence: 79%

Rosamicin, a macrolide with in vitro activity against Ureaplasma urealyticum.

Hill

Sutton²

1979

J. Antibiot.

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A new macrolide antibiotic, rosamicin, was shown to have much greater activity in vitro against ureaplasmas isolated from humans than erythromycin or the tetracyclines tested. A marked ureaplasmacidal effect was also shown.Ureaplasma urealyticum has been implicated in both genital disease and infertility in man, but it has not always proved very responsive to available antibiotics and an effective antibiotic treatment is urgently required.BRUNNER et al.1) showed that 57 % of patients with acute or chronic prostatitis were infected with U. urealvticum, compared with only 14%. of healthy controls (ureaplasmas never exceeded 102 colonyforming units per ml in the controls), and they considered it to be the causative organism in 29%of acute and 23 % of chronic cases. GUPTA et al.2) and FRIBERG et al.3) found higher concentrations of ureaplasmas in the genitaltracts of sterile couples than in those of fertile controls.There is evidence that ureaplasmas can be the causative organisms of `non-specific' urethritis.TAYLOR-ROBINSON et al.4) experimentally induced non-specific urethritis in two male volunteers by inoculating a culture of U. urealyticum into their urethras.EVANS et al.5) showed that 10% of ureaplasma isolates were resistant to tetracycline and that all of them were sensitive to erythromycin. Repeated passage increased the resistance to minocycline of three out of four strains. As the concentration required to inhibit growth increased with exposure time, it appears that tetracycline(s) have a static rather than a ureaplasmacidal effect. FORD et al.6) have also reported a case of non-specific urethritis associated with a ureaplasma strain which was resistant to tetracycline but which, however, responded to erythromycin.The findings of SPAEPEN et al.7) were also consistent with those of EVANS et al.5), in so far as they found that increasing concentrations of the four tetracyclines tested were required to inhibit the ureaplasmas examined. Ureaplasmas could, however, be recovered seven days after treatment from 42 % of 50 patients. In contrast to EVANS et al.5) they showed that only 11.4 % of the ureaplasma strains examined were inhibited by 4.0 1sg/ml of erythromycin.A new micromonospora-produced macrolide antibiotic, rosamicin, has shown good results against various mycoplasmas. WAGMAN et al.8), who described it, also tested it against M. gallisepticum, and WALTZ et al.9) examined its activity against four more mycoplasma species. These included four strains of M. pneumoniae, five strains of M. orale, five strains of M. salivarium and one strain of M. hominis.M. hominis was inhibited by 0.4,ug/ml of rosamicin and all other species were inhibited by a concent-

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Section: Discussionsupporting

confidence: 79%

Rosamicin, a macrolide with in vitro activity against Ureaplasma urealyticum.

Hill

Sutton²

1979

J. Antibiot.

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“…A similar effect on rosamicin has been reported by Waitz et al. in an earlier study (9). Rosamicin also showed an enhanced activity with alkalinization in this study.…”

Section: Discussionsupporting

confidence: 76%

“…It shares certain chemical and biological characteristics with erythromycin (8,9). The purposes of this study were as follows: (i) to determine the in vitro activity of rosamicin against gram-positive cocci and compare its activity to that of erythromycin and lincomycin; (ii) to determine the extent of cross-resistance of gram-positive cocci to rosamicin, erythromycin, and lincomycin; and (iii) to compare the effects of alkalinization on the in vitro activities of rosamicin and erythromycin against gram-negative bacilli.…”

mentioning

confidence: 99%

Rosamicin: Evaluation In Vitro and Comparison with Erythromycin and Lincomycin

1974

Antimicrob Agents Chemother

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Rosamicin is a new. macrolide antibiotic produced by Micromonospora rosaria. It shares certain chemical and biological characteristics with erythromycin. Activity against gram-positive strains was assayed by broth dilution and compared to that of erythromycin and lincomycin. Rosamicin was bacteriostatic and inhibited most strains of Staphylococcus aureus, Staphylococcus epidermidis, enterococci, viridans streptococci, and group A streptococci in concentrations of 0.02 to 4.0 ,g/ml. Results were similar for erythromycin and for lincomycin (excluding enterococci). Cross-resistance of gram-positive organismsto these three antimicrobial agents was incomplete. Rosamicin was more active than erythromycin against Enterobacteriaceae and Pseudomonas at pH 7.2. Alkalinization of the medium enhanced the activity of both rosamicin and erythromycin; however, rosamicin was still more active than erythromycin against all gram-negative strains at pH 7.6 and 8.0. In view of the high degree of in vitro activity of rosamicin against gram-positive organisms, lack of complete cross-resistance with erythromycin and lincomycin, and the greater activity of rosamicin than erythromycin against gram-negative organisms, further investigation of this macrolide is warranted.

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“…For the pharmacokinetic study, a rosaramicin solution (100 mg/ml) for oral administration was obtained by adding 3 ml of sterile water to the sterile vial containing rosaramicin sodium dihydrogen phosphate, lyophilized powder (equivalent to 300 mg of rosaramicin base). The rosaramicin solution (2.5 mg/ml) for intravenous infusion was obtained by adding 12 ml of the oral solution to 468 ml of saline. The 250-mg rosaramicin tablets were manufactured by Schering Corp.…”

Section: Methodsmentioning

confidence: 99%

“…Rosaramicin has been shown to have good in vitro activity against gram-positive aerobes and anaerobes. In addition, rosaramicin has been shown to have greater in vitro activity than erythromycin against a variety of gram-negative organisms and anaerobes, including Bacteroides and Mvcoplasma species (12). This paper describes the pharmacokinetics of rosaramicin in subjects receiving 500-mg doses by (i) 1-h intravenous infusion, (ii) solution orally, or (iii) tablets orally.…”

mentioning

confidence: 99%

Pharmacokinetics and metabolism of rosaramicin in humans

Lin¹,

Chung²,

Gural³

et al. 1984

Antimicrob Agents Chemother

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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. After intravenous administration, the rosaramicin levels in serum declined rapidly with t112S of 0.27 h for the distribution phase and 3.28 h for the elimination phase. The apparent volume of distribution was 3.78 liter/kg, and the total body clearance was 13.41 ml/min per kg, indicating extensive tissue distribution or metabolism or both. Similar pharmacokinetic data were obtained after oral administration of the drug in solution or tablets and after intravenous dosing. The absolute bioavailability of the drug administered orally, in either tablets or solution, was 32 to 39%. The metabolism and excretion of [14C]rosaramicin administered orally were also evaluated in volunteers. The serum area under the curve (oo) of unchanged rosaramicin was 19% of that of total radioactivity, indicating extensive metabolism of the drug. About 7.0% of the radioactivity was recovered in the urine, and 86.7% was recovered in the feces. 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. The major metabolite, 20-bis-ureidorosaramicin, represented 17 to 38% of the radioactivity in the urine and 26 to 29% of the radioactivity in the feces.Rosaramicin is a broad-spectrum macrolide antibiotic, similar to erythromycin (1, 10). The antibiotic is isolated from fermentation broth of Micromonospora rosaria (11). Rosaramicin has been shown to have good in vitro activity against gram-positive aerobes and anaerobes. In addition, rosaramicin has been shown to have greater in vitro activity than erythromycin against a variety of gram-negative organisms and anaerobes, including Bacteroides and Mvcoplasma species (12). This paper describes the pharmacokinetics of rosaramicin in subjects receiving 500-mg doses by (i) 1-h intravenous infusion, (ii) solution orally, or (iii) tablets orally. The metabolism and excretion of ['4C]rosaramicin after oral administration of a 500-mg dose of [14C]rosaramicin were also evaluated. MATERIALS AND METHODSCompound. For the pharmacokinetic study, a rosaramicin solution (100 mg/ml) for oral administration was obtained by adding 3 ml of sterile water to the sterile vial containing rosaramicin sodium dihydrogen phosphate, lyophilized powder (equivalent to 300 mg of rosaramicin base). The rosaramicin solution (2.5 mg/ml) for intravenous infusion was obtained by adding 12 ml of the oral solution to 468 ml of saline. The 250-mg rosaramicin tablets were manufactured by Schering Corp.For the metabolic study, 5-[14C]rosaramicin (Fig. 1) inverse isotope dilution technique and high-pressure liquid chromatography (HPLC), was greater than 95%.Administration of rosaramicin. Twelve healthy male volunteers participated in the pharmacokinetic study of single blind three-way crossover design. After an 8-h fast, each subject received 500 mg of rosaramicin as (i) two 250-mg...

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Biological Studies With Rosamicin, a New Micromonospora-Provuced Macrolide Antibiotic

Cited by 44 publications

References 5 publications

Rosamicin, a macrolide with in vitro activity against Ureaplasma urealyticum.

Rosamicin, a macrolide with in vitro activity against Ureaplasma urealyticum.

Rosamicin: Evaluation In Vitro and Comparison with Erythromycin and Lincomycin

Pharmacokinetics and metabolism of rosaramicin in humans

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