• 대한약리학회지
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• 제19권1호
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• pp.71-76
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• 1983

Aminoglycoside antibiotics are reported to enhance the amylase release from isolated slices of pancreas in vitro and the mode of action of aminoglycosides on amylase release is considered different from those of acetylcholine or cholecystokinin(CCK), i.e., electronmicroscopically intact zymogen granules are appeared in the lumen of pancreatic acini by treatment of aminoglycosides. It is known that atropine blocks the secretagogue effect of acetylcholine, and phenoxybenzamine is reported to block the effects of CCK or its analogue caerulein. Present study was undertaken to investigate the mode of action of aminoglycosides on the amylase release using atropine, phenoxybenzamine and propranolol as a membrane stabilizing agent in slices of chicken pancreas. The results are summarized as follows : 1) Streptomycin and kanamycin increased the amylase release significantly from slices of chicken pancreas. 2) The effect of streptomycin was inhibited by atropine but not by phenoxybenzamine or propranolol. 3) The amylase release by acetylcholine was blocked by atropine tut the effect of cholecystokinin octapeptide(CCK-8) was not influenced by atropine, phenoxybenzamine or propranolol. 4) Pretreatment of streptomycin enhanced the secretagogue effect of acetylcholine or CCK-8. From these results it is suggested that amylase releasing effects of aminoglycosides are mediated in part by cholinergic stimulation and in part by membrane alteration and these effects are enhanced by acetylcholine or cholecystokinin.

• Clinical and Experimental Pediatrics
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• 제51권10호
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• pp.1038-1041
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• 2008

Aminoglycosides are frequently used antibiotics in children. The multiple daily dosing (MDD) in infants and children is twice or three times daily depending on age. Recent studies in adults have shown that once daily dosing (ODD) maximizes the bactericidal activity and might minimize the toxicity of antibiotics. So, I reviewed many studies about efficacy, toxicity and cost effectiveness of ODD of aminoglycosides in children. Most studies suggest that ODD compared with MDD of aminoglycosides is theoretically more efficacious and has no higher toxicity in infants and children. But, the total number of patients included in the studies is not large. Multi-center, controlled prospective studies are required in larger numbers of infants and children to determine the efficacy and safety of the ODD regimen in children before ODD of aminoglycosides can be recommended for routine use.

• 한국임상약학회지
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• 제12권1호
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• pp.7-12
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• 2002

Pharmacokinetic parameters and dosage of aminoglycosides (AGs) were studied retrospectively in 36 patients with neutropenic fever after stem cell transplantation in Seoul National University Hospital from July 1996 to June 2001. AGs pharmacokinetic parameters were calculated with steady-state peak and trough serum drug concentrations by the method of Sawchuk and Zaske et at. The calculated aminoglycosides volume of distribution and clearance were greater than population value $(0.36\pm0.06\;L/kg,\;116\pm32\;ml/min/1.73\;m^2,\;respectively)$. The average dosage of aminoglycosides required to maintain optimal serum AGs concentration was also greater than recommended dose in insert paper. The average dosage of amikacin was $11\pm2.1$ mg/kg every 12 hours (In case of tobramycin, $2.09\pm0.37$ mg/kg every 8 hours or $2.59\pm0.20$ mg/kg every 12 hours). The relationship between AGs volume of distribution and sex, serum albumin (g/dl), body mass index $(kg/m^2)$, body weight change $(\%)$, the amount of fluid inpu (ml/kg/day), the degree of hematocrit decrease $(\%)$ were studied respectively. Univariate anlysis revealed that body mass index $(kg/m^2)$, the amount of fluid input (ml/kg/day) and the degree of hematocrit decrease $(\%)$ had significant correlation with aminoglycosides volume of distribution. But sex, serum albumin, body weight change $(\%)$ had no significant correlation with aminoglycosides volume of distribution.

• 한국임상약학회지
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• 제8권2호
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• pp.83-88
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• 1998

Improved knowledge of the time course of antimicrobial activity should provide useful information for designing optimal dosage regimen. In contrast to $\beta$-lactam, aminoglycosides tend to induce a prolonged postantibiotic effect against aerobic or facultative gram negative rods and clinical outcome was significantly correlated with achieving peak serum concentrations. The objective of this study was to compare the efficacy, safety of e same total daily dose of amikacin and gentamicin given either twice or thrice daily in the treatment of patients. Consecutive patients over 20 years old with a suspected or confirmed infection for which an aminoglycosides was indicated were eligible. Exclusion criteria were known allergy to aminoglycosides, renal impairment, granulocytopenia and pregnancy. Patients were treated with intravenous amikacin 15 mg/kg/day or gentamicin 4.5 mg/kg/day either in two devided or in three devided. Seventy-four patients with infection were enrolled in this study of amikacin twice daily (A2, n=29), gentamicin twice daily (G2, n=8) vs amikacin thrice daily (A3, n=30), gentamicin thrice daily (G3, n=7). Baseline characteristics were comparable in G2 and G3. The clinical cure rate (including partial improve) were $89.0\%\;and\;86.0\%$ in A2 group and A3 group respectively. The bacteriologic cure rate were $99.0\%\;and\;85.7\%$ in A2 group and in A3 group respectively. The clinical and bacteriologic effects were difficult to compare G2 with G3, because of the small numbers of patients. The serum creatinin rose in $3.44\%$ (1 in 29) of patients in the A2 group compared to $13.3\%$ (4 in 30) in e A3 group. Although audiometry was not performed, there was no clinical evidence of ototoxicity in any of the patients. In our opinion, twice-daily regimen of aminoglycosides is more effective and less nephrotoxic than thrice-daily regimen.

• 한국동물위생학회지
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• 제23권1호
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• pp.19-28
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• 2000

There are several main antibacterial susceptibility tests, such as agar dilution method, broth dilution method and disk diffusion technique. Especially, for minimal inhibitory concentration (MIC) test, agar dilution method has been widely used. But that method is so complicated and bothering that it's difficult to treat a large amount of strains. On the other hand, modified broth dilution method(add 1% glucose and 0.018% phenol red as a pH indicator to broth) is fast and easy to perform. Most of all, it can visualize the result by color. The MICs of 22 antibiotics Including penicillins, aminoglycosides, cephalothin, chloramphenicol, lincomycin, ceftiofur, vancomycin and quinolones, erythromycin, colistin. sul-fadimethoxine, trimethoprim for arcanobacterium pyogenes 14 strains, actinobacillus pleuropneu-moniae 41 strains and pasteurella multocida 37 strains, which were collected from porcine during 1996 ∼ 1999, were determined by modified broth dilution method. Actinobacillus pleuropneumoniae was highly susceptible to all kinds of quinolones such as ciprofloxacin, enrofloxacin and norfloxacin and to all aminoglycosides, like gentamicin, apramycin, kanamycin and ampicillin, cephalothin and ceftiofur. But It was quite resistant to solfadimethoxin, colistin and vancomycin. Pasteurella multocida was found to have high susceptibility to ampicillin, cephalothin, chlorampenicol and gentamicin but had mid-degree susceptibility to other aminoglycosides. In addition, it was susceptible to norfloxacin and nalidixic acid, but not to newer fluoroquinolone like ciprofloxacin and enrofloxacin and it was resistant to colistin and kanamycin. Arcanobacterium pyogenes was highly susceptible to most of quinolones such as cipoofloxacin, enrofloxacin and norfloxacin and gentamicin and penicillin G. But it also obtained high resistance against the early quinolone, nalidixic acid and aminoglycosides such as amikacin, apramycin and kanamycin and erythromycin, chlorampenicol, tetracyclin and vancomycin.

• 한국임상약학회지
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• 제9권1호
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• pp.15-18
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• 1999

Ascertainment of accurate pharmacokinetic parameters for aminoglycoside dosing remains critical, as the serum drug concentration relates directly to both the therapeutic response and toxic effect. In the initial dosing of aminoglycosides, the volume of distribution is especially important because the dosage is calculated by multiplying the volume of distribution by the desired serum concentration. Aminoglycosides distribute into mainly the extracellular fluid and it has been reported that the volume of distribution is 0.25 L/kg. Penetration of polar aminoglycosides into adipose tissue occurs to some extent, but varies according to the degree of obesity. Therefore, dosages may be overestimated or underestimated according to the type of the dosing weight in overweight or underweight patients. Prior investigations have suggested various dosing weights which are multiplied by the popular volume of distribution to calculate the total volume of distribution. Based on other investigations, we calculated a new dosing weight which was applicable to all patients regardless of obesity in order to use the popular volume of distribution. We estimated IBW+$0.414^{\ast}$(TBW-IBW) as a new dosing weight with the SAS program. A new dosing weight is similar to those of other studies which examined in morbidly obese patients. Consequently we suggests that the dosing weight reported in morbidly obese patients can be extended to a broader patients population. But we found that the volume of distribution per kilogram from our patients was significantly larger than that for foreign patients(0.343L/kg vs 0.25 L/kg)(Kor. J. Clin. Pharm. 1999; 9(1): 15-18)

• 한국동물위생학회지
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• 제40권1호
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• pp.27-33
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• 2017

Salmonella enterica subsp. enterica is a common microbial flora in pet turtles, which could opportunistically become pathogenic to human. Their possession of aminoglycoside resistance genes has important significance both in humans and animal medicine. In this study, twenty-one Salmonella enterica subsp. enterica were isolated from thirty-five individual turtles purchased from pet shops and online markets in Korea. In order to characterize the aminoglycoside susceptibility patterns, antimicrobial susceptibility tests were performed against gentamicin, amikacin and kanamycin of aminoglycoside antimicrobial group. Each of the isolates showed susceptibility to all tested aminoglycosides in disk diffusion and minimum inhibitory concentration (MIC) tests. PCR assay was carried out to determine aminoglycoside resistance genes, integron and integron mediated aminoglycoside genes. None of the isolates showed aac(3)-IIa, aac-(6')-Ib, armA, aphAI-IAB aminoglycoside resistance genes. Only, five isolates (24%) harbored class 1 integron related IntI1 integrase gene. The results suggest that Salmonella enterica subsp. enterica strains isolated from pet turtles are less resistance to aminoglycosides and don't harbor any aminoglycosides resistance genes.

• Journal of Microbiology and Biotechnology
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• 제13권5호
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• pp.828-831
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• 2003

Although most of the DOS containing aminoglycosides are produced by Streptomyces, very little information is available about their biosynthesis. In the present paper, we report a method to isolate DOI synthase, a key enzyme in the biosynthesis of DOS, from aminoglycoside producer Streptomyces. PCR primers based on conserved region of DOI synthases were specific and reliable for the isolation of the biosynthetic genes of DOS containing aminoglycosides or the screening of the aminoglycoside producers. The use of DOI synthase as a probe could save both time and cost of cloning aminoglycoside biosynthetic genes.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-1
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• pp.81-84
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• 2003

Aminoglycoside antibiotics are among the chlinically important antibiotics and a major structural feature is the existence of characteristic aminocyclitol aglycones [1]. Considering the structural features, aminoglycosides are classified in to two classes. The first are those containing fully substituted aminocyclitol such as streptomycin, hygromycin, fortimycin, etc. (omitted)

• 한국임상약학회지
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• 제13권2호
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• pp.55-58
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• 2003

Astromicin is an aminoglycoside antiviotic that is structually different from conventional aminoglycosides. Astromicin has been shown to be active against aerobic Gram-negative bacilli. The pharmacokinetics of astromicin were determined in 12 healthy volunteers ($65.5\pm5.23\;kg$ of body weight) following a 30-min continuous intravenous infusion at a dose of 200 mg. The plasma and urine samples were collected up to 24 h and drug concentrations were measured by a bioassay using Bacillus subtilis. Pharmacokinetic parameters were calculated by fitting individual concentration-time curve to a one-exponential decay model. The plasma levels were $16.9\pm1.68\;and\;1.05\pm0.346\l{\mu}g/ml$ at 0 h and 8 h after the infusion, respectively. The elimination half-life of astromicin was $1.86\pm0.360\;h$ The volume of distribution was $0.182\pm0.0164\;L/kg$, and the total body clearance was $5.25\pm1.74\;L/h$. These pharmacokinetic parameters were similar to these of gentamicin, tobramycin, and amikacin. Therefore, it is recommended that therapeutic drug monitoring of astromicin could be conducted in a similar fashion as the other aminoglycosides.