Therapeutic drug monitoring is an important part of antiepileptic therapy, and the search for alternative non-invasive methods of such monitoring represents an actual task for clinical neurology. For this purpose, we determined by gas chromatography and mass spectroscopy the levels of the anticonvulsant carbamazepine in the plasma and saliva of healthy volunteers aged 1825 years after one oral dose of 200 mg. Maximal drug concentration was 2.62.7 g/ml in the plasma and 0.75 g/ml inthe saliva; mean saliva/plasma drug level ratio was 0.3. Time necessary to reach maximal concentration was 67 hrs for both plasma and saliva. T1/2 was also equal for both sources: 1516 hrs. Significant correlation between the plasma and saliva carbamazepine concentrations was revealed (R2=0,893). Thus, while treating epilepsy patients with carbamazepine, it is possible to use the saliva as an adequate biological sample for conducting non-invasive drug monitoring.
Nanotechnologies is a new and rapidly developing field of science and engineering related to targeted manipulation of objects sized within the nano-diapason (1091012 m); this means principally new characteristics and qualities of the respective systems to be constructed. In the paper, problems of nanotechnology applications in clinical neurology are considered, namely, possibilities and prospects of the use, in diagnostic and medicinal purposes, of biochips, nanosensors, bioreactors, immunonanoparticles, biodegradable polymers, convectionenhanced drug delivery, etc. in various diseases of the nervous system. Special attention is paid to the development of pharmacotherapeutic applications, including drug transport systems and targeted nanotherapy, which outlines modern nanomedicine. Different medicinal nanoformulations are discussed, including polymeric nanoparticles, fullerenes, dendrimers, liposomes, nanotubes, etc. The authors experience in the study of stable glycosphyngolipid nanotubes and nanoliposomes as the drug delivery system is presented. For this purpose, the model of skin vasomotor reaction stimulation by cutaneous nitroglycerin application was used: the effect of nitroglycerin was shown to rise 1.5 times with nanotubes as carriers, and 2.5 times with nanoliposomes.
Anticonvulsant activity and pharmacokinetics of nanoemulsion and unmodified substance of carbamazepine were compared in experiments on mice. Carbamazepine nanoemulsion demonstrated significant anticonvulsant activity and was superior to unmodified substance of carbamazepine against seizures induced by maximum electric shock and picrotoxin. Relative bioavailability of carbamazepine after administration of nanoemulsion was 160% compared to unmodified substance. Carbamazepine nanoemulsion more effectively penetrated through BBB by 1.5 times in comparison with unmodified substance.
This paper presents the results of therapeutic drug monitoring of lamotrigine, an anticonvulsant epilepsy medication, in patients with cryptogenic focal epilepsy using plasma and saliva as a biological material for drug testing. Comparative analysis of the steady-state plasma and saliva lamotrigine concentrations (Сss MIN and Сss MAX) allows the conclusion that saliva can be used as a suitable biological substrate for therapeutic drug monitoring.
The effect of treatment course of bioflavonoids quercetin and diquertin on phospholipids and fatty acid composition of erythrocytes membranes and amilorid-dependent activity Na+/H+ transmembrane exchanger of erythrocytes have been studied in condition of chronic physical tension in mice in consequence of extraordinary running strain. The studied drugs actively prevented from the changes of chemical composition and as a result structural and functional changes of erythrocytes membranes. It is established that the studied bioflavonoids prevented from the development of extraordinary physical strain syndrome.
Due to the emergence of new technologies in a pharmakokinetics, a pharmacogenetics and analytical chemistry, the medicine comes to qualitatively new stage of development. Therapeutic drug monitoring as the mean of the real time pharmacotherapy efficiency control becomes the basis of rational therapy in modern medicine. In the article various aspects of the therapeutic drug monitoring (TDM) as subsection of clinical pharmacology are discussed. The main indications to carrying out TDM and the main TDM procedures are submitted. Value of TDM for an epileptology is discussed. The special attention is paid to the bioanalytical methods and new methodical approaches (such as non-invasive drug monitoring and equilibrium dialysis) applied in TDM. TDM role as an independent discipline of a medical sciences, with concentration on modern pharmacokinetics computer programs is separately analyzed.
Effect of a course of treatment by bioflavonoids quercetin and diquertin on the physical work capacity, oxidant and antioxidant status of organism, and hemorheological parameters and deformability of erythrocytes have been studied under conditions of chronic physical overstrain in mice caused by sequential extraordinary running load. The drugs effectively prevent the development of oxidative stress, loss of elasticity of erythrocyte membranes and growth in dynamic blood viscosity in microcirculatory link of hemodynamics. It is established that both bioflavonoids significantly increase the physical work capacity of animals and prevent from the development of physical overstrain syndrome.
У мышей изучено влияние курсового применения биофлавоноидов кверцетина и диквертина на физическую работоспособность, окислительный и антиокислительный статус организма, а также гемореологические параметры крови и деформируемость эритроцитов в условиях хронического физического перенапряжения, вызванного чрезмерными беговыми нагрузками. Изученные препараты предотвращали развитие окислительного стресса, уменьшение эластичности мембран эритроцитов и повышение динамической вязкости крови в микроциркуляторном звене гемодинамики. Установлено, что биофлавоноиды существенно повышали физическую работоспособность животных и предотвращали развитие синдрома перенапряжения.
The applications of nanotechnology to pharmacology are reviewed. The potential applications of biochips, nanosensors, bioreactors, neural stem cells, immune nanoparticles, biodegradable polymers, and convection-enhanced drug delivery in the diagnostics and treatment of diseases are discussed. Specific attention is given to developments in chemotherapeutic means, including advanced drug delivery systems and targeted nanotherapy, which will form the basis of the future nanomedicine. Numerous novel medicinal forms are discussed, including polymeric nanoparticles, nanotubes, micelles, liposomes, dendrimers, fullerenes, and hydrogels. In particular, highly stable glycosphyngolipid nanotubes and nanoliposomes are proposed as drug delivery systems. For this purpose, the model of stimulation of skin vasomotor reactions by nitroglycerin application is developed. The effect of nitroglycerin is shown to increase 1.5 times when used in the form of a dispersion with nanotubes as carriers and almost 2.5 times in the case of a dispersion with nanoliposomes as carriers. Nanotechnologically manufactured biologically active substances Apiton-25 (containing apis products) and Microhydrin (containing SiO2 nanoparticles, silicon hydrogen bonds Si-H, and free negative charges for free radical neutralization) have been studied. The results indicate that both Apiton-25 and Microhydrin upon peroral administration enhance the cyclic trial performance during prolonged submaximal exercise in endurance-trained cyclists.
The purpose of the research was to consider moral-ethical, legal and medical aspects of stand tests and practical implementation of dietary supplements in sport of maxirnumachievements. In the author's opinion there are two necessary conditions in applying dietary supplements and medications which are the following: 1.. Both dietary supplements and medications approved by W.ADA must be tested on athletes-volunteers in a stand experiment in a laboratory of clinical pharmacology and anti-dope control certified by the Ministry of Public Health of the Russian Federation according to all the rules. 2.. It's prohibited to apply dietary supplements and medications in any kind of sport without any theoretically substantiated facts testifying to their efficiency. The most crucial questions for The Federal agency on physical culture, sport and tourism are the following: 1. If the tested medication can increase adaptation to physical loading (increase exercise efficiency and accelerate rehabilitation processes). 2. If it has dopes or their metabolites prohibited by WADA in its formula. The author suggests creating a medical card of pharmacological support as a patient history where all measures connected with pharmacological support should be registered taking into account loadings, diet and other rehabilitation procedures (massage, sauna, psycho-therapeutic, psycho-analytical influences etc). Conclusion The application of dietary supplements in sport medicine has two aspects: • ·the treatment of ill athletes, veterans of sport like other citizens according to the constitution of the Russian Federation: the increase of the athletes' adaptation to physical loading in conditions of educational-training process and competitions. The latter has a number of peculiarities and approvals that should be present for each medication (code certificates, anti-dope certificates, final report on practical efficiency and some other documents).
The applications of nanotechnology to pharmacology are reviewed. The potential applications of biochips, nanosensors, bioreactors, neural stem cells, immune nanoparticles, biodegradable polymers, and convection-enhanced drug delivery in the diagnostics and treatment of diseases are discussed. Specific attention is given to developments in chemotherapeutic means, including advanced drug delivery systems and targeted nanotherapy, which will form the basis of the future nanomedicine. Numerous novel medicinal forms are discussed, including polymeric nanoparticles, nanotubes, micelles, liposomes, dendrimers, fullerenes, and hydrogels. In particular, highly stable glycosphyngolipid nanotubes and nanoliposomes are proposed as drug delivery systems. For this purpose, the model of stimulation of skin vasomotor reactions by nitroglycerin application is developed. The effect of nitroglycerin is shown to increase 1.5 times when used in the form of a dispersion with nanotubes as carriers and almost 2.5 times in the case of a dispersion with nanoliposomes as carriers. Nanotechnologically manufactured biologically active substances Apiton-25 (containing apis products) and Microhydrin (containing SiO 2 nanoparticles, silicon hydrogen bonds Si-H, and free negative charges for free radical neutralization) have been studied. The results indicate that both Apiton-25 and Microhydrin upon peroral administration enhance the cyclic trial performance during prolonged submaximal exercise in endurance-trained cyclists.
Drugs used by athletes for the improvement of results are described and classified with respect to chemical structure and pharmacological action. The main groups of drugs treated as doping are considered and the WADA requirements to prohibited preparations are formulated. The main effects produced by drugs on the athletes and animals (race horses, fight dogs, etc.) are described and the measures of therapy against side effects are outlined.
Drugs used by athletes for the improvement of results are described and classified with respect to chemical structure and pharmacological action. The main groups of drugs treated as doping are considered and the WADA requirements to prohibited preparations are formulated. The main effects produced by drugs on the athletes and animals (race horses, fight dogs, etc ) are described and the measures of therapy against side effects are outlined.
The influence of vitamax, synergin, and alpha-tocopherol on the exercise performance (ultimate run on a tretbahn with increasing load) of high-rank athletes has been studied. Peculiarities of the drug action upon lipid peroxidation (LPO) in unsaturated fatty acids were studied by a chemiluminescence technique and by monitoring the malonic dialdehyde in the course of a 21-day treatment-training session and within a 5-day period after termination of the drug administration. Vitamax and synergin increase the working capacity of high-rank athletes on the 10th and 11st day of administration, respectively, while alpha-tocopherol produces such effect only on the 21st day. All the drugs studied possess antioxidant properties, which are also more pronounced for vitamax and synergin.