Changes in serum levels of quinolones in rats under the influence of experimental trauma

Trichilis, A.; Tesserommatis, C.; Varonos, D.

doi:10.1007/bf03190070

Cited by 12 publications

(6 citation statements)

References 29 publications

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“…In addition, the more pronounced ampicillin displacement from salicylate may be caused by the difference in the pk, values, since the value of salicylate is closer to that of ampicillin (Table II) [22]. It is of note that this in vitro study could well support the hypothesis that an increase in the free concentrations of antimicrobial agents may be due to their displacement from their binding sites in the simultaneous presence of NSAIDs [11][12][13][14][15]. Such an increase observed in clinical or experimental studies in vivo could be attributed to this competitive protein binding.…”

Section: Discussionsupporting

confidence: 69%

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Adjuvant arthritis-induced changes on ampicillin binding in serum and tissues under the influence of non-steroidal anti-inflammatory drugs in rats

Tigka

Daskala

Rallis

et al. 2005

European Journal of Drug Metabolism and Pharmacokinetics

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Adjuvant arthritis, as a model for investigating rheumatoid arthritis (RA), is characterized by reduced plasma albumin levels and interferes with drug binding in the plasma and tissues (liver and bone). Ampicillin interacts with non-steroidal anti-inflammatory drugs (NSAIDs) due to the acidic pk(a). The aim of this study was to investigate in vitro the concentrations of ampicillin in the serum, femur, mandible and liver proteins following the co-administration of ketoprofen, flurbiprofen, ibuprofen, oxyphenbutazone and ASA in adjuvant arthritis versus healthy control rats. Ampicillin binding was found to be reduced in the serum of arthritic rats, and ampicillin binding to serum proteins was also reduced under the influence of NSAIDs in the control animals. Differences in ampicillin binding were observed in the various tissues due to the effect of adjuvant arthritis as well as that due to the co-administration of NSAIDs. In conclusion, this in vitro study may provide a plausible explanation for the ampicillin-NSAIDs interaction and such a finding may be of therapeutic significance in the treatment of painful arthritic disease such as RA.

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Section: Discussionsupporting

confidence: 69%

“…Their free concentrations reflect the biologically active drugin the tissues andserum, andwhendrug displacement isinvolved, this may leadto increasedantimicrobialactivity [14,15].…”

Section: Introductionmentioning

confidence: 99%

Adjuvant arthritis-induced changes on ampicillin binding in serum and tissues under the influence of non-steroidal anti-inflammatory drugs in rats

Tigka

Daskala

Rallis

et al. 2005

European Journal of Drug Metabolism and Pharmacokinetics

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“…In a model of surgical trauma in rats treated with quinolones we have reported increased quinolone concentration in tissues. Moreover in the same model, when ibuprofen was co-administered with quinolones the latter were increased in both serum and tissues (36,37). Comparable results were observed in a hyperlipidaemic experimental model, where Wistar rats were treated with cephalosporins simultaneously with ibuprofen.…”

Section: Diseases Influence Drug-pro-tein Bindingsupporting

confidence: 53%

The role of the protein-binding on the mode of drug action as well the interactions with other drugs

Tesseromatis

Alevizou

2008

Eur. J. Drug Metabol. Pharmacokinet.

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Drug transport and disposition are influenced by a non-specific and reversible drug binding to plasma and tissues proteins. Albumin and al acid glycoprotein are the most important transport proteins of the blood. Albumin possesses specific sites for acidic and basic drug binding and can interact with them in the plasma since a third site is trapped only by digoxin. Diseases and stress conditions induce conformational changes either in plasma or in tissue proteins by the synthesis of endogenous substances which can strong interfere with the amount of the free pharmacological effective drug ratio. This may affect the binding of drugs in target molecules inducing significant pharmacokinetic alterations. Stress conditions are associated with FFA increase in serum playing an antagonistic role with other acidic molecules (e.g. ampicillin) to the same binding site. The bounded drug is displaced and freer ratio is available to interact with various organ receptors leading to pharmacological effect enhancement and therefore to side effects manifestation such as seizures. Furthermore conjunctive tissues diseases, ageing, prolonged bleeding, starvation or diseases affecting protein profile, characterized by reduced total plasma proteins, followed by albumin decrease and lessen binding sites lead to more free drug availability enhancing its pharmacological effect. Increased a1-acid glycoprotein the acute phase protein as by heart infraction or liver morbidities (e.g CCl4 intoxication) mainly occupied from basic substances, in the case of cationic drug treatment resulted to the enhancement of them and consequently to pronounced effectiveness. In addition, renal failure reduced free fractions of many acidic drugs. It may be concluded that by narrowed therapeutic index of a medicine, and when drug/drug or drug/disease interactions are anticipated, drug monitoring seems to be necessary for its dosage adjustment.

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“…Lidocaine was measured by using 14C_ lidocaine in serum, and the incubation medium of the above tissues. According to the literature the drug levels in tissue of small animals such as rats has the same values in homogenated tissues as in the incubation solution of tissues slices or in the incubation medium of a total organ (15).…”

Section: Methodsmentioning

confidence: 99%

Changes of lidocaine levels in rat serum and tissue under stress and hyperlipidaemic diets

Karakitsos¹,

Karabinis²,

Kotsiou

2009

Eur. J. Drug Metabol. Pharmacokinet.

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Hyperlipidaemic diets induce increase in serum lipid profile (total cholesterol, triglycerides, LDL etc). It has also been proven that stress interferes in lipid metabolism. Many drugs modify their pharmacokinetic properties in presence of lipoproteins, as a result of alterations in their plasma protein and tissue binding. Lidocaine, a synthetic amide, used as a local anesthetic and secondary as antiarrhythmic agent is also protein bound and therefore conditions, which favor lidocaine dissociation from plasma proteins, modify its pharmacokinetic profile. The purpose of this study was: To investigate and compare the effects of stress( cold water 4 degrees C swimming of 20 days duration) and various high lipid diets (olive oil, butter, sunflower oil) on the serum and tissue (liver and tongue) levels of 14C lidocaine.

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Changes in serum levels of quinolones in rats under the influence of experimental trauma

Cited by 12 publications

References 29 publications

Adjuvant arthritis-induced changes on ampicillin binding in serum and tissues under the influence of non-steroidal anti-inflammatory drugs in rats

Adjuvant arthritis-induced changes on ampicillin binding in serum and tissues under the influence of non-steroidal anti-inflammatory drugs in rats

The role of the protein-binding on the mode of drug action as well the interactions with other drugs

Changes of lidocaine levels in rat serum and tissue under stress and hyperlipidaemic diets

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