Abstract
Using a randomized crossover design involving 12 normal subjects, we studied comparatively the pharmacokinetics and tolerance of three aminoglycoside antibiotics, gentamicin, sisomicin, and tobramycin. Serum concentrations were determined during 8 h and the urine recovery rate was determined within 24 h after a 1-h intravenous infusion of the respective antibiotic in a dose of 1 mg/kg of body weight. Microbiological assay was performed with the agar diffusion test (Bacillus subtilis); pharmacokinetic calculations were performed by means of a digital computer on the basis of a mathematical model of an open, two-compartment system. Of the three antibiotics studied, gentamicin showed the lowest concentration in serum after termination of the 1-h infusion (3.85 +/- 0.67 mug/ml), and the serum-regression curve steadily lay below those of the two other antibiotics. Sisomicin had the highest serum concentrations (4,66 +/- 1.24 mug/ml) and the serum-level curve exceeded that of the two other antibiotics. Tobramycin occupied a position between sisomicin and gentamicin in form of its serum level characteristics. Corresponding to the serum kinetics we also found slight differences in the pharmacokinetic parameters, especially in serum half-lives, elimination constants, and areas under the serum level curves. The test of liver and kidney functions and the hematological systems, as well as the function of the stato-acusticus nerve, showed no pathological changes by any of the three antibiotics tested.
MeSH Terms
Adult
Anti-Bacterial Agents/metabolism
Clinical Trials as Topic
Female
Gentamicins/administration & dosage,metabolism
Half-Life
Humans
Infusions, Parenteral
Kinetics
Male
Middle Aged
Sisomicin/administration & dosage,metabolism
Tobramycin/administration & dosage,metabolism
Chemicals
Anti-Bacterial Agents
Gentamicins
Tobramycin
Sisomicin
Authors & Affiliations
3 authors, click to expand affiliations / ORCID
Lode H
Kemmerich B
Koeppe P
References (21)
21 references, click to expand
-
GENTAMICIN SULFATE, NEW ANTIBIOTIC AGAINST GRAM-NEGATIVE BACILLI. LABORATORY, PHARMACOLOGICAL, AND CLINICAL EVALUATION.
JAMA. 1964 Sep 14;189:817-22
PMID: 14172278
-
Pharmacology of gentamicin in man.
J Infect Dis. 1971 Dec;124 Suppl:S98-105
PMID: 5126254
-
Serum levels of gentamicin and tobramycin after slow intravenous bolus injection.
Lancet. 1974 Mar 9;1(7854):378-9
PMID: 4131032
-
Pharmacokinetics of the aminoglycoside antibiotic tobramycin in humans.
Antimicrob Agents Chemother. 1973 Apr;3(4):469-73
PMID: 4208290
-
Pharmacokinetic studies of tobramycin and gentamicin.
Antimicrob Agents Chemother. 1973 Apr;3(4):445-50
PMID: 4208289
-
The unpredictability of serum concentrations of gentamicin: pharmacokinetics of gentamicin in patients with normal and abnormal renal function.
J Infect Dis. 1974 Aug;130(2):150-4
PMID: 4842335
-
In vitro bactericidal effectiveness of four aminoglycoside antibiotics.
Antimicrob Agents Chemother. 1973 Jan;3(1):87-94
PMID: 4790579
-
Sisomicin: evaluation in vitro and comparison with gentamicin and tobramycin.
Antimicrob Agents Chemother. 1973 Jan;3(1):24-8
PMID: 4790572
-
Tobramycin and gentamicin concentrations in the serum of normal and anephric patients.
Antimicrob Agents Chemother. 1973 Jan;3(1):125-9
PMID: 4790568
-
Serum protein binding of the aminoglycoside antibiotics.
Antimicrob Agents Chemother. 1972 Sep;2(3):214-6
PMID: 4790560
-
In vitro studies of tobramycin.
Antimicrob Agents Chemother. 1972 Sep;2(3):109-13
PMID: 4790551
-
Activity of five aminoglycoside antibiotics in vitro against gram-negative bacilli and Staphylococcus aureus.
Antimicrob Agents Chemother. 1973 Dec;4(6):617-25
PMID: 4793881
-
Comparative pharmacokinetics of tobramycin and gentamicin.
Clin Pharmacol Ther. 1973 May-Jun;14(3):396-403
PMID: 4698568
-
Comparative activity of sisomicin, gentamicin, kanamycin, and tobramycin.
Antimicrob Agents Chemother. 1972 Dec;2(6):431-7
PMID: 4670437
-
In vitro studies of tobramycin, an aminoglycoside antibiotic.
Antimicrob Agents Chemother. 1972 Jan;1(1):41-5
PMID: 4670427
-
[The use of a digital computer in the development of dosage recommendations for antibiotic therapy].
Arzneimittelforschung. 1972 Feb;22(2):311-9
PMID: 5067482
-
Antibiotic 6640. 3. Biological studies with antibiotic 6640, a new broad-spectrum aminoglycoside antibiotic.
J Antibiot (Tokyo). 1970 Nov;23(11):559-65
PMID: 4992170
-
[Pharmacological and therapeutic properties of gentamicin. Experimental studies on the effect level, excretion, stability and therapeutic indications].
Arzneimittelforschung. 1968 Sep;18(9):1119-23
PMID: 4974678
-
Antibiotic 6640. II. Fermentation, isolation, and properties.
J Antibiot (Tokyo). 1970 Nov;23(11):555-8
PMID: 5487130
-
Antibiotic 6640, a new Micromonospora-produced aminoglycoside antibiotic.
J Antibiot (Tokyo). 1970 Nov;23(11):551-4
PMID: 5487129
-
Assessment of pharmacokinetic constants from postinfusion blood curves obtained after I.V. infusion.
J Pharm Sci. 1970 Jan;59(1):53-5
PMID: 5411325