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Pharmacokinetics and Pharmacodynamics

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No 1 (2014)
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FROM THE EDITOR

CURRENT REVIEWS

4-13 5972
Abstract
The role of cytochrome P450 isoforms CYP1A2 and in the metabolism of caffeine is described. Caffeine pharmacokinetics data in humans and laboratory animals are presented. Examples of drug-drug interactions of cubstrate marker caffeine with different drugs are given.
14-20 2150
Abstract
In an overview and critical article discusses plant lectins in terms of their importance as biologically active substances in pharmaceutical preparations. Focuses on the critical analysis of the possible values of lectins medicinal plants in pharmaceuticals and analysis of the most common errors scientific papers on the subject. The analysis of some pharmaceuticals, in which the main active ingredients are declared lectins.

THEORETICAL BASIS

BIOEQUIVALENCE STUDIES

37-43 893
Abstract
In the review of the main problems holding bioanalytical part of bioequivalence studies of medicines in Russia. The analysis of the major causes of failure when performing studies of bioequivalence and pharmacokinetics.

PHARMACOKINETICS STUDIES

44-49 1014
Abstract
Work is devoted to a comparative analysis of the pharmacological action and integral indicators pharmacokinetics of 1,4- benzodiazepine - phenazepam and levan, as well as their total active 3-oximetabolite formed by different mechanisms. It is shown that in the tests levan antagonism corazolum and thiosemicarbazide inferior phenazepam anticonvulsant activity, but surpasses phenazepam on activity in the maximal electroshock test and has a lower severity miorelaxation action. Comparison effects of phenazepam and levad with effects of 3-oximetabolite indicate greater similarity effects than metabolite with phenazepam. With the use of radiolabeled compounds were established change in the ratio of the areas under the concentration curve 3-oximetabolite in the brain and blood when administered phenazepam (AUCbrain / AUCblood = 0,96 ± 0,27) or levan (AUCbrain / AUCblood = 1,4 ± 0,1). This fact is associated with different ways of biotransformation: oxidative hydroxylation of phenazepam CYP450 and nonspecific carboxylesterase hydrolysis of levan, which explains the difference in the pharmacological effect of the test compounds.
50-51 490
Abstract
In the study of excretion of the drug was found that glutaron determined in urine for at least 72 hours of the study. Renal clearance is 123 ml/hour, extrarenal - 34.84 ml/hour by intravenous route of administration. Superiority over extrarenal and renal clearance correlates with earlier data on the distribution of glutaron in organs and tissues. The drug was determined in the organs responsible for elimination (liver, kidneys and lungs) at high concentrations.
52-56 664
Abstract
The pharmacological properties of new coordination compound - the biologically active substance - cobalt bis(citrate) stannate was studied. The result of researching are: the compound has antiviral activity against human influenza virus strains A/ Honghong/1/68 (H3N2), A/PR/8/34 (H1N1), and influenza virus H5N3 in tissue culture chorio-allantoic membranes (CAM) of chick embryos 11-12 daily and monolayer culture of MDCK cells used. Compound has a low toxicity (by intraperitoneal injection LD50 = 206,63 mg/kg; orally - LD50 = 1836,76), that gives perspective to further his preclinical studies as an antiviral agent.
57-62 1017
Abstract
In the past 25 years, there has been an exponential introduction of new antiepileptic drugs (AEDs) in clinical practice. As is often the treatment of epilepsy carried throughout of life, as part of the patient assigned to polytherapy with other AEDs, their drug-drug interactions are an important factor in the treatment of epilepsy, which can be a major therapeutic challenge. For new AEDs interaction particularly important because they often can only be assigned to an add-on polytherapy, at least the first prescribing. Main pharmacokinetics interaction associated with the induction or inhibition of hepatic enzymes, while mainly pharmacodynamics interaction may result in synergy against adverse effects, although there are also examples of anticonvulsant synergism. This article describes in detail the pharmacokinetics and pharmacodynamics interaction of new AEDs (zonisamide and perampanel) with other AEDs.

HISTORY

63-73 8028
Abstract
Article is devoted to historical review of pharmacology and pharmacy herbal medicines since ancient times.

ANNIVERSARIES



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ISSN 2587-7836 (Print)
ISSN 2686-8830 (Online)