Antibiotic tissue penetration and its relevance: models of tissue penetration and their meaning

Nix, David E.; Goodwin, Shirley; Peloquin, Charles A.; Rotella, Denise L.; Schentag, J J

doi:10.1128/aac.35.10.1947

Cited by 132 publications

(97 citation statements)

References 59 publications

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“…All studies have so far reported a lack of accumulation (ie, an apparent intracellular concentration lower than the extracellular one at equilibrium) for all b-lactams whether in phagocytic [9][10][11][12][13][14][15] or nonphagocytic cells and tissues in general [16]. It has often been concluded that b-lactams are unable to penetrate cells, which is probably incorrect because most of the representatives of this class of drug do diffuse reasonably well through biologic membranes.…”

Section: B-lactamsmentioning

confidence: 99%

Intracellular pharmacodynamics of antibiotics

Carryn

Chanteux

Seral

et al. 2003

Infectious Disease Clinics of North America

172

151

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Section: B-lactamsmentioning

confidence: 99%

Intracellular pharmacodynamics of antibiotics

Carryn

Chanteux

Seral

et al. 2003

Infectious Disease Clinics of North America

172

151

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“…For each type of tissue assay, an antibiotic calibration range was determined with the organ involved (6,45). The elimination half-life (t1/2/) was calculated according to a single-compartment model by exponential regression of the concentrations in serum from 0.25 to 2 h. Areas under the curve (AUCs) from 0 to 6 h were calculated by the trapezoidal rule method.…”

mentioning

confidence: 99%

Pharmacokinetics, toxicity, and efficacy of liposomal capreomycin in disseminated Mycobacterium avium beige mouse model

Conte¹,

Gallou²,

Potel³

et al. 1994

Antimicrob Agents Chemother

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Capreomycin was incorporated into multilamellar vesicles of pure dipalmitoylphosphatidylcholine. The pharmacokinetics and nephrotoxicity of capreomycin in the free and liposomal forms were studied in normal mice. The efficacies of the two forms were evaluated by using the Mycobacterium avium complex beige mouse model. Approximately 107 viable M. avium cells were injected intravenously. Seven days later, treatment with either liposomal or free capreomycin at 60 or 120 mg/kg of body weight was administered daily for 5 days. Mice were sacrificed 5 days after the end of treatment, and the viable bacteria in liver, spleen, lungs, and blood were counted. After 5 days of treatment with dosages of 60 or 120 mg/kg/day, the level of blood urea nitrogen increased in the group treated with free capreomycin but not in the group treated with liposomal capreomycin. After intravenous injection of 120 mg/kg, liposomes enhanced the diffusion of capreomycin in the spleen, lungs, and kidneys and increased the half-life in serum. The 120-mg/kg dose of liposomal capreomycin significantly reduced the number of viable mycobacteria in the liver, spleen, and blood compared with those in the controls. Although these results are promising, further studies are needed to assess the efficacy of liposomal capreomycin for the treatment of M. avium complex infections.Since the appearance of the human immunodeficiency virus (HIV), the incidence of Mycobacterium avium complex (MAC) infections has increased considerably and has involved between 18 and 50% of HIV-infected patients (17,24,33). Treatment is difficult because of the weakened immune defense system of the host and the resistance of MAC strains to many classic antituberculous agents. Moreover, the phenotypes of resistance of these strains are very heterogeneous (25,26,49).Experimental infection models involving animal or human macrophage cultures and acute or chronic infections in the mouse have been developed to assess the activities of antiinfectious agents against MAC (32). Numerous studies have been performed either in vitro (25,28,36,49) or on macrophages (46) and in animal models (6,21,34,38,39) with classic or more recent antituberculous agents (ciprofloxacin, sparfloxacin, azithromycin, and clarithromycin) alone or in combi-

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“…Those compounds are also easily transported across the blood-brain barrier [1][2][3][4]. Fourth-generation cephalosporins are used to treat infections of the urinary tract, lungs, skin and soft tissues as well as in postoperative prophylaxis [3].…”

Section: Introductionmentioning

confidence: 99%

Critical parameters for the stability of cefquinome sulfate in aqueous solutions and solid phase

Dołhań

Urbaniak

Manuszewska

et al. 2017

Reac Kinet Mech Cat

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Cefquinome sulfate is a veterinary, parenteral, fourth-generation cephalosporin with a methoxyimino-aminothiazolyl moiety into the acyl side chain and the quaternary quinoline group at position 3 of the cefem ring. Cefquinome sulfate is known to undergo degradation, which could be additionally increased by the presence of some critical factors such as temperature, relative air humidity, buffer components as well as hydrogen and hydroxide ions. The aim of this study was to evaluate the factors underlying the stability of cefquinome sulfate (CFQ) in aqueous solution and in the solid state taking into account general and specific acid-base hydrolysis in the pH range 0.45-10.48 at 343 K; the effect of temperature on the stability at 0% RH and an increased relative air humidity (RH = 76.4%); the influence of relative air humidity at 343 K (66.5-90%). To determine the observed rate constants, an isocratic HPLC-UV method was used. The three pK a values of cefquinome sulfate, kinetic (k obs. , k pH ), and activation parameters (E a , DH = , and DS = ) were determined.

show abstract

Antibiotic tissue penetration and its relevance: models of tissue penetration and their meaning

Cited by 132 publications

References 59 publications

Intracellular pharmacodynamics of antibiotics

Intracellular pharmacodynamics of antibiotics

Pharmacokinetics, toxicity, and efficacy of liposomal capreomycin in disseminated Mycobacterium avium beige mouse model

Critical parameters for the stability of cefquinome sulfate in aqueous solutions and solid phase

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