[Pharmacokinetics of moxalactam in adults]. 1983

G Humbert, and A Leroy, and J P Fillastre

Specific characteristics of Moxalactam, a new beta-lactam antibiotic, are high serum concentrations, prolonged half-life and good tissular diffusion. After IM injection of a single dose of 0.25, 0.5 and 1 g, the maximum serum concentration, achieved at one hour, averages 13, 16-21 and 30-50 micrograms/ml. After rapid IV injection of 0.5 and 1 g, the average maximum serum concentrations are 90 and 150 micrograms/ml; after an IV infusion of 2 g over 20 minutes, maximum concentrations are 150 to 180 micrograms/ml. Moxalactam elimination kinetics are linear, independent from the dose and route of administration, with a distribution half-life (T 1/2 alpha) between 0.20 and 0.60 hours and an elimination half-life (T 1/2 beta) between 2 and 2.5 hours (range: 1.9 and 3.1 hours). The apparent distribution volume is between 15 and 18 liters, i.e. 20 to 25% of the body weight. Serum or total clearances and renal clearances are respectively 80 to 100 and 50 to 90 ml/mn, with wide variations from one author to another. Approximately 70 to 90% of the administered dose are eliminated in the urine over 24 hours, without any tubular secretion. Renal failure results in a progressive increase of the elimination half-life, which can reach 20 hours in patients with anuria; approximately 50% of the injected dose are recovered by hemodialysis. Many pharmacokinetic studies have demonstrated the excellent diffusion of the agent in the various tissues and body fluids, particularly in the CSF. From the collation of bacteriologic and pharmacokinetic data, dosage regimens adjusted to the renal function can be proposed.

UI MeSH Term Description Entries
D007668 Kidney Body organ that filters blood for the secretion of URINE and that regulates ion concentrations. Kidneys
D007676 Kidney Failure, Chronic The end-stage of CHRONIC RENAL INSUFFICIENCY. It is characterized by the severe irreversible kidney damage (as measured by the level of PROTEINURIA) and the reduction in GLOMERULAR FILTRATION RATE to less than 15 ml per min (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002). These patients generally require HEMODIALYSIS or KIDNEY TRANSPLANTATION. ESRD,End-Stage Renal Disease,Renal Disease, End-Stage,Renal Failure, Chronic,Renal Failure, End-Stage,Chronic Kidney Failure,End-Stage Kidney Disease,Chronic Renal Failure,Disease, End-Stage Kidney,Disease, End-Stage Renal,End Stage Kidney Disease,End Stage Renal Disease,End-Stage Renal Failure,Kidney Disease, End-Stage,Renal Disease, End Stage,Renal Failure, End Stage
D007700 Kinetics The rate dynamics in chemical or physical systems.
D009070 Moxalactam Broad- spectrum beta-lactam antibiotic similar in structure to the CEPHALOSPORINS except for the substitution of an oxaazabicyclo moiety for the thiaazabicyclo moiety of certain CEPHALOSPORINS. It has been proposed especially for the meningitides because it passes the blood-brain barrier and for anaerobic infections. 1-Oxacephalosporin,6059-S,Disodium Latamoxef,Disodium Moxalactam,Festamoxin,Lamoxactam,Latamoxef,Lilly 127935,Ly-127935,Ly127935,Moxalactam Disodium,S-6059,Shiomarin,1 Oxacephalosporin,6059 S,6059S,Disodium, Moxalactam,Latamoxef, Disodium,Ly 127935,Moxalactam, Disodium,S 6059,S6059
D002511 Cephalosporins A group of broad-spectrum antibiotics first isolated from the Mediterranean fungus ACREMONIUM. They contain the beta-lactam moiety thia-azabicyclo-octenecarboxylic acid also called 7-aminocephalosporanic acid. Antibiotics, Cephalosporin,Cephalosporanic Acid,Cephalosporin,Cephalosporin Antibiotic,Cephalosporanic Acids,Acid, Cephalosporanic,Acids, Cephalosporanic,Antibiotic, Cephalosporin,Cephalosporin Antibiotics
D002513 Cephamycins Naturally occurring family of beta-lactam cephalosporin-type antibiotics having a 7-methoxy group and possessing marked resistance to the action of beta-lactamases from gram-positive and gram-negative organisms. Antibiotics, Cephamycin,Cephamycin,Cephamycin Antibiotics
D004058 Diffusion The tendency of a gas or solute to pass from a point of higher pressure or concentration to a point of lower pressure or concentration and to distribute itself throughout the available space. Diffusion, especially FACILITATED DIFFUSION, is a major mechanism of BIOLOGICAL TRANSPORT. Diffusions
D006207 Half-Life The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity. Halflife,Half Life,Half-Lifes,Halflifes
D006435 Renal Dialysis Therapy for the insufficient cleansing of the BLOOD by the kidneys based on dialysis and including hemodialysis, PERITONEAL DIALYSIS, and HEMODIAFILTRATION. Dialysis, Extracorporeal,Dialysis, Renal,Extracorporeal Dialysis,Hemodialysis,Dialyses, Extracorporeal,Dialyses, Renal,Extracorporeal Dialyses,Hemodialyses,Renal Dialyses
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man

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