Pharmacokinetics and suction blister fluid penetration of a semisynthetic injectable streptogramin RP 59500 (RP 57669/ RP 54476).
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.
Bernard
E
E
Maladies Infectieuses et Tropicales, Hôpital de l'Archet, Nice, France.
Bensoussan
M
M
Bensoussan
F
F
Etienne
S
S
Cazenave
I
I
Carsenti-Etesse
E
E
Le Roux
Y
Y
Montay
G
G
Dellamonica
P
P
D000328:Adult; D001768:Blister / Q000378:metabolism; D005110:Extracellular Space / Q000378:metabolism*; D006207:Half-Life; D006801:Humans; D007262:Infusions, Intravenous; D008297:Male; D014018:Tissue Distribution; D014769:Virginiamycin / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
D014769:Virginiamycin; C062940:quinupristin-dalfopristin