Abstract
RP 59500 is a new semisynthetic injectable streptogramin with excellent activity against most gram-positive bacteria. In order to assess its potential for the treatment of tissue infections, the pharmacokinetics and penetration into suction blister fluid were studied in a pilot phase I study in six male volunteers following a single infusion of 12 mg/kg over 1 h. Plasma and suction blister fluid concentrations were determined by microbiological assay. The mean peak concentration in plasma was 8.65 mg/l at the end of infusion. The mean plasma elimination half-life was 1.48 h. The mean peak concentration in interstitial fluid was 2.41 mg/l and was reached after 1 h in two volunteers and after 2 h in the other four. The mean percentage penetration for the interval 0–6 h was 82.5 %. RP 59500 was still detectable in interstitial fluid at 6 h at a mean concentration of 0.92 ± 0.25 mg/l. The data of this pilot study demonstrate good penetration of RP 59500 into non-inflammatory interstitial fluid.
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Barrière JC, Bouanchaud DH, Paris JM, Rolin O, Harris NV, Smith C: Antimicrobial activity againstStaphylococcus aureus of semisynthetic injectable streptogramins/RP 59500 and related compounds. Journal of Antimicrobial Chemotherapy 1992, 30, Supplment A: 1–8.
Bouanchaud DH: In vitro and in vivo synergic activity and fractional inhibitory concentration of the components of a semisynthetic streptogramin, RP 59500. Journal of Antimicrobial Chemotherapy 1992, 30, Supplement A: 95–99.
Fass RJ: In vitro activity of RP 59500, a semisynthetic injectable pristinamycin, against staphylococci, streptococci, and enterococci. Antimicrobial Agents and Chemotherapy 1991, 35: 553–559.
Goto S, Miyazaki S, Kaneko Y: The in-vitro activity of RP 59500 against gram-positive cocci. Journal of Antimicrobial Chemotherapy 1992, 30: 25–28.
Pechère JC: In vitro activity of RP 59500, a semisynthetic streptogramin, against staphylococci and streptococci. Journal of Antimicrobial Chemotherapy 1992, 30, Supplement A: 15–18.
Etienne SD, Montay G, Le Liboux A, Frydman A, Garaud JJ: A phase I, double-blind, placebo-controlled study of the tolerance and pharmacokinetic of RP 59500. Journal of Antimicrobial Chemotherapy 1992, 30, Supplement A: 123–131.
Kiistala U, Mustakallio KK: Dermo-epidermal separation with suction. Journal of Investigation and Dermatology 1967, 48: 466–477.
Wise R: The clinical relevance of protein binding and tissue concentrations in antimicrobial therapy. Clinical Pharmacokinetics 1986, 11: 470–482.
Carbon C: Significance of tissue levels for prediction of antibiotic efficacy and determination of dosage. European Journal of Clinical Microbiology & Infectious Diseases 1990, 9: 594–598.
Bergan R: Pharmacokinetics of tissue penetration of antibiotics. Reviews of Infectious Diseases 1981, 3: 45–66.
Desnottes JF, Diallo N: Cellular uptake and intracellular bactericidal activity of RP 59500 in murine macrophages. Journal of Antimicrobial Chemotherapy 1992, 30, Supplement A: 107–115.
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Bernard, E., Bensoussan, M., Bensoussan, F. et al. Pharmacokinetics and suction blister fluid penetration of a semisynthetic injectable streptogramin RP 59500 (RP 57669/ RP 54476). Eur. J. Clin. Microbiol. Infect. Dis. 13, 768–771 (1994). https://doi.org/10.1007/BF02276064
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DOI: https://doi.org/10.1007/BF02276064