Anti-inflammatory activity of H1-receptor antagonists: review of recent experimental research.

Anti-inflammatory activity of H1-receptor antagonists: review of recent experimental research. OBJECTIVE: To compare the anti-inflammatory effects of fexofenadine with other H(1)-receptor antagonists in vitro. DATA SOURCES: Published literature. STUDY SELECTION: Recent experimental studies on anti-inflammatory effects of H(1)-receptor antagonists. Databases searched: Medline, Medscape. Period covered: 1990-2003. Search terms: second-, third-generation antihistamines; sedating, nonsedating antihistamines; in vitro anti-inflammatory activity; cetirizine; ebastine; loratadine; fexofenadine; desloratadine. RESULTS: Second- and third-generation H(1)-receptor antagonists may demonstrate significant in vitro anti-inflammatory activity at concentrations considered to be clinically relevant. In some instances, higher (supraclinical) concentrations are required to achieve comparable effects. CONCLUSIONS: Experimental research suggests that second- and third-generation H(1)-receptor antagonists may achieve anti-inflammatory effects in a clinical context. Further studies are required to support this conclusion. Journal ISSN: 0300-7995 Issue: 20-1 (2004) Pages: 73-81

Amitriptyline plasma protein binding: effect of plasma pH and relevance to clinical overdose.
Amitriptyline plasma protein binding: effect of plasma pH and relevance to clinical overdose. Reversing ventricular ectopy with plasma alkalinization following acute tricyclic antidepressant overdose is a recognized mode of therapy. The mechanism responsible for this effect is unclear. Changes in plasma protein binding of free drug, effects of the sodium ion on the myocardium, and alterations of plasma concentrations of alpha-1-acid glycoprotein may all interact to alter toxicity of tricyclics in overdose. An in vitro investigation using equilibrium dialysis was designed to examine the effect of altering plasma pH on percentage of free amitriptyline at clinical overdose plasma concentrations. A 1973 report on this effect lacked adequate controls and was faulty in experimental protocol. The current investigation used plasma concentrations typically present in amitriptyline overdose, a sensitive gas liquid chromatographic assay to detect total and free drug, and adequate control of plasma pH. The results of two separate experiments demonstrated a significant decrease in percentage of free amitriptyline of 20% over a pH range of 7.0-7.4 (P less than 0.05) and 42% over a pH range of 7.4-7.8 (P less than 0.05). The rate of change in slope in both experiments was not significantly different (P less than 0.01) indicating similar effects of pH change on plasma protein binding of amitriptyline within the two groups. Journal ISSN: 0735-6757 Issue: 4-2 (1986) Pages: 121-5

Effects of combined administration of L-tryptophan and tricyclic antidepressants on alpha 2- and beta-adrenoceptors and monoamine levels in rat brain.
Effects of combined administration of L-tryptophan and tricyclic antidepressants on alpha 2- and beta-adrenoceptors and monoamine levels in rat brain. In order to test whether co-administration of a serotonin precursor with antidepressant drugs could potentiate the effects of the antidepressants on monoamines or adrenoceptors in rat brain, L-tryptophan (20 mg/kg) was administered to rats daily for 7 or 15 days, either alone or in combination with desipramine (10 mg/kg) or amitriptyline (10 mg/kg). After treatment with L-tryptophan for 7 days, increases were observed in rat hypothalamic and frontal cortex 5-hydroxy-3-indoleacetic acid levels as well as in hypothalamic dopamine and nucleus accumbens 3,4-dihydroxyphenylacetic acid levels. After 15 days, hippocampal beta-adrenoceptor density was found to be decreased. There was no evidence of potentiation of desipramine or amitriptyline action when L-tryptophan was administered in combination with the antidepressants. On the contrary, the antidepressants appeared to interact with L-tryptophan to reduce its effects. Journal ISSN: 0364-3190 Issue: 10-12 (1985) Pages: 1661-71

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[zinc]

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[hoodia]

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