Pharmacokinetics of intravitreal carbenicillin, cefazolin, and gentamicin in rhesus monkeys. 1983

M Barza, and A Kane, and J Baum

Although intravitreal injection of antibiotics is being used more widely in treatment of bacterial endophthalmitis, the pharmacokinetic principles that underlie such therapy have been derived exclusively from experiments in the rabbit. Therefore, we studied several representative antibiotics in normal eyes of rhesus monkeys. Carbenicillin (1,000 micrograms), cefazolin (1,000 micrograms), or gentamicin (100 micrograms) was injected intravitreally. Vitreous and aqueous humors were aspirated at intervals up to 96 hours after injection. The half-life values in the vitreous humor were: carbenicillin 10 hours, cefazolin 7 hours, and gentamicin 33 hours. Concomitant intraperitoneal administration of probenecid prolonged the vitreal half-life of carbenicillin to 20 hours and of cefazolin to 30 hours. The estimated vitreous volumes in these monkeys were approximately 3.0-4.0 ml. These results are consistent with the hypothesis that, in primates as in rabbits, beta-lactam antibiotics are eliminated via the retinal route and the aminoglycoside via the anterior route. This supports the applicability of the rabbit model to the treatment of endophthalmitis in humans.

UI MeSH Term Description Entries
D007267 Injections Introduction of substances into the body using a needle and syringe. Injectables,Injectable,Injection
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008253 Macaca mulatta A species of the genus MACACA inhabiting India, China, and other parts of Asia. The species is used extensively in biomedical research and adapts very well to living with humans. Chinese Rhesus Macaques,Macaca mulatta lasiota,Monkey, Rhesus,Rhesus Monkey,Rhesus Macaque,Chinese Rhesus Macaque,Macaca mulatta lasiotas,Macaque, Rhesus,Rhesus Macaque, Chinese,Rhesus Macaques,Rhesus Macaques, Chinese,Rhesus Monkeys
D002228 Carbenicillin Broad-spectrum semisynthetic penicillin derivative used parenterally. It is susceptible to gastric juice and penicillinase and may damage platelet function. Carboxybenzyl Penicillin,Anabactyl,Carbapen,Carbecin,Carbenicillin Disodium,Geopen,Microcillin,Pyopen,Disodium, Carbenicillin,Penicillin, Carboxybenzyl
D002437 Cefazolin A semisynthetic cephalosporin analog with broad-spectrum antibiotic action due to inhibition of bacterial cell wall synthesis. It attains high serum levels and is excreted quickly via the urine. Cephazolin,Ancef,Cefamedin,Cefamezine,Cefazolin Sodium,Cephamezine,Cephazolin Sodium,Gramaxin,Kefzol,Sodium Cephazolin,Totacef,Cephazolin, Sodium,Sodium, Cefazolin,Sodium, Cephazolin
D005260 Female Females
D005839 Gentamicins A complex of closely related aminoglycosides obtained from MICROMONOSPORA purpurea and related species. They are broad-spectrum antibiotics, but may cause ear and kidney damage. They act to inhibit PROTEIN BIOSYNTHESIS. Gentamicin Sulfate (USP),Gentamycin,G-Myticin,Garamycin,Gentacycol,Gentamicin,Gentamicin Sulfate,Gentamycins,Gentavet,Genticin,G Myticin,GMyticin,Sulfate, Gentamicin
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
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001082 Aqueous Humor The clear, watery fluid which fills the anterior and posterior chambers of the eye. It has a refractive index lower than the crystalline lens, which it surrounds, and is involved in the metabolism of the cornea and the crystalline lens. (Cline et al., Dictionary of Visual Science, 4th ed, p319) Aqueous Flare,Intraocular Fluid,Aqueous Flares,Aqueous Humors,Flare, Aqueous,Fluid, Intraocular,Fluids, Intraocular,Humor, Aqueous,Humors, Aqueous,Intraocular Fluids

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