Clinical Pharmacokinetics

Greenblatt, David J.; Koch‐Weser, Jan

doi:10.1056/nejm197511062931905

Cited by 187 publications

(101 citation statements)

References 27 publications

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“…The mean residence time (MRT) was calculated as the time after application required for eliminating 63.2% of the substance, solving the equation: The calculations were performed by standard methods (10). If applicable, the results are normalized for a 70-kg body weight or a 1.73-m2 body surface area.…”

Section: Methodsmentioning

confidence: 99%

Effects of standard breakfast on pharmacokinetics of oral zidovudine in patients with AIDS

Ruhnke

Bauer

Seifert

et al. 1993

Antimicrob Agents Chemother

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The influence of a standard breakfast on the single-dose pharmacokinetics of zidovudine (AZT) after oral administration of 100 and 250 mg of AZT was studied in 27 subjects with advanced human immunodeficiency virus infection (Centers for Disease Control stage IV). Concentrations of AZT and the 5'-glucuronide metabolite (GAZT) [B]). Recoveries (AZT and GAZT) in urine varied with both dosages, reflecting more a problem of accounting for the metabolite GAZT in urine than a relevant difference (100 mg, 115% [F] and 76.5% [B]; 250 mg, 71% [F] and 99.4% [B]). Our data suggest that absorption of AZT in human immunodeficiency virus-infected subjects is extremely variable, with a high degree of interindividual differences. Furthermore, breakfast had a marked influence on the absorption of AZT, suggesting that the drug should be taken in a fasting state.

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Section: Methodsmentioning

confidence: 99%

Effects of standard breakfast on pharmacokinetics of oral zidovudine in patients with AIDS

Ruhnke

Bauer

Seifert

et al. 1993

Antimicrob Agents Chemother

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“…; 2, 100 and 200 mg i.v. ; 3,200 and 400 mg orally) with 10 (2,12,16), C(t) = Ae-'(t -t') + Be-P(' -to) -C(t)oeka(t -, where C(t) represents the concentration in serum at time t in milligrams per liter, A and B (in milligrams per liter) are the zero intercepts of the tangents (x and 3 with the ordinate, and ox and ,B (per minute) represent the slopes of the rapid initial and slow terminal distribution and elimination phases, respectively; ka is the absorption rate, and to is the lag time. After i.v.…”

Section: Methodsmentioning

confidence: 99%

“…The mathematical calculation of the constants and pharmacokinetic parameters was performed by standard methods as previously described (12,13,16,20). The Wilcoxon test for paired differences was used to distinguish the differences within the pharmacokinetic parameters.…”

Section: Methodsmentioning

confidence: 99%

Pharmacokinetics of ofloxacin after parenteral and oral administration

Lode

Höffken

Olschewski

et al. 1987

Antimicrob Agents Chemother

144

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In 10 volunteers, the pharmacokinetics of ofloxacin {HOE 280, DL 8280; (+)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido-[1,2,3-deI [1,4] 1.4 liters/kg of body weight) suggested effective diffusion into the extravascular space. High total and renal clearances indicated primarily renal excretion with additional elimination pathways, such as tubular secretion and extrarenal elimination. After oral administration, absorption was excellent, and the absolute bioavailability following 200 mg of ofloxacin could be calculated at >0.95. Maximal concentrations in serum were attained 1.2 to 1.9 h after dosing; areas under the curve increased in proportion to dose between 200 and 400 mg of oral ofloxacin. The amount of known metabolites (demethyl and N-oxide compounds) excreted in urine reached only 4.3% (intravenously) and 4.0% (orally). Transient headaches in some volunteers were the only side effects registered.6-Fluoro-7-piperazino-4-quinolones are noteworthy both for the wide range and intensity of activities against gramnegative bacilli and cocci in vitro and the capacity to control experimentally induced systemic infections with selected bacteria when administered orally in well-tolerated doses (9,15,27).Ofloxacin {HOE 280, DL 8280; (±)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl) -7-oxo-7H-pyrido[1,2,3-de] [1,4]benzoxacine-6-carboxylic acid} is a new quinolone carboxylic acid derivative showing a broad antimicrobial spectrum against gram-positive and gram-negative bacteria (1,11,17,22,27). This substance was found to be more active than norfloxacin and pipemidic acid (22), its in vitro antibacterial activity being almost comparable to those of gentamicin, tobramycin, and newer cephalosporins (9,11,27). When first introduced, ofloxacin could only be administered orally, but recently a parenteral form was developed.The purpose of this study was to investigate the pharmacokinetic properties of this quinolone after oral and intravenous (i.v.) administration of various doses to determine the bioavailability and metabolism of this drug.(Part of this study was presented at the 24th Interscience

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“…The first review in the English language of the state of knowledge in pharmacokinetics was published by Nelson in 1961. 3 Since that time, the study of pharmaco-kinetic:s has expanded greatly and has been the subject of several review articles and books [4][5][6][7] Pha;macokinetics involves the application of mathematical models to drug concentration-time data to obtain rate and volume estimates for movement between and size of abstract body comp;mments. Recognizing the limitations and dealing only in abstraction, in recent years the area of physiological pharmacokineties has been developed.…”

Section: (B) Histor 3' Of Pharmacokineticsmentioning

confidence: 99%