Effects of propranolol or paracetamol on lidocaine concentrations in serum and tissues

Saranteas, Theodosios; Mourouzis, Constantinos; Koumoura, F; Tesseromatis, C.

doi:10.1053/joms.2003.50090

Cited by 12 publications

(9 citation statements)

References 16 publications

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“…Both drugs are known to possess a higher affinity of binding to alpha-acid glycoprotein than to albumin, but in clinical practice only the amount of the free active fraction is important, since this is responsible for the pharmacological effect. These results are in agreement with previous studies in which co-administration of other cationic drugs was shown to increase the concentration of free lidocaine in serum and tissues (2,9).…”

Section: Discussionsupporting

confidence: 93%

“…Combined administration of propranolol and lidocaine leads to a decrease in the total concentration and the percentage protein binding of lidocaine in tissues, and thus may increase the quantitative importance of this displacement. Additionally, co-administration with paracetamol or propranolol interferes with the metabolic profile of lidocaine, resulting in pharmacokinetic interactions that may be significant when determining the appropriate dose of lidocaine in clinical practice (9).…”

Section: Introductionmentioning

confidence: 99%

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The influence of clonidine co-administration on the extent of lidocaine protein binding to rat serum and tissues

et al. 2011

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Lidocaine is an amide local anesthetic and clonidine is an antihypertensive (α2-adrenergic agonist).The use of these two drugs in combination is recommended to enhance the analgesic effect of lidocaine. The aim of this study was to investigate the influence of clonidine co-administration on the extent of lidocaine binding to rat serum, heart and maxillofacial tissues in vivo and in vitro. Thirty-two Wistar rats received either lidocaine alone, or lidocaine and clonidine, in the masseter muscle, and were then sacrificed 15 or 30 min after treatment. Serum, masseter, mandible and heart samples were then isolated and incubated in 0.9% NaCl solution for 12 h at 8°C. The extent of binding in the incubation medium and the serum was estimated by ultrafiltration, and the free lidocaine fraction was determined by the radioscopic method in a β-counter. An in vitro procedure was also performed. Serum, heart, masseter and mandible samples were incubated at 37°C for 15 or 30 min in Ringer's solution containing either lidocaine or lidocaine and clonidine, and the samples were similarly subjected to ultrafiltration. The percentage binding of lidocaine was again estimated by the radioscopic method. Lidocaine levels were found to be increased by clonidine co-administration in vivo and the free lidocaine fraction was enhanced in vitro as well in the examined tissues, obviously through mechanisms related to protein binding alterations. (J Oral Sci 53, 61-66, 2011)

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Section: Discussionsupporting

confidence: 93%

Section: Introductionmentioning

confidence: 99%

The influence of clonidine co-administration on the extent of lidocaine protein binding to rat serum and tissues

et al. 2011

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“…Propranolol levels were enhanced under the influence of lidocaine as has been shown above and reported by many other investigators probably which may be due to an antagonism connected with both drugs' common (24)(25)(26).It is suggested that the displacement of propranolol from its binding sites to serum and tissue proteins may occur. This is important for the cardiac tissue because of the propranolol's affinity to it, which may affect the heart function, since even a negligible enhancement modifies the clinical outcome.…”

Section: Discussionsupporting

confidence: 63%

“…25 The concentration of propranolol was measured in the animals' serum, heart and liver incubation medium in the beta-counter as referred to in previous reports (16).…”

Section: Methodsmentioning

confidence: 99%

H3 Propranolol serum levels following lidocaine administration in rats with CCL4 — induced liver damage

Kotsiou

Tsamouri²,

Anagnostopoulou³

et al. 2006

European Journal of Drug Metabolism and Pharmacokinetics

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“…antimicrobials displaced by NSAIDs or lidocaine by propranolol) from albumin show similarities in many tissues, in normal or disease states. Possibly the occurring in vivo complexities may be due to interactions between drugs and endogenous ligands for HSA or tissue proteins (40,54,56).…”

Section: Tissue Binding Of Drugsmentioning

confidence: 99%

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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Effects of propranolol or paracetamol on lidocaine concentrations in serum and tissues

Cited by 12 publications

References 16 publications

The influence of clonidine co-administration on the extent of lidocaine protein binding to rat serum and tissues

The influence of clonidine co-administration on the extent of lidocaine protein binding to rat serum and tissues

H3 Propranolol serum levels following lidocaine administration in rats with CCL4 — induced liver damage

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

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