ABSTRACT
OBJECTIVE: To study the penetration of mexidol through the blood-brain barrier into different brain compartments and cell mitochondria. MATERIAL AND METHODS: The study was carried out on adult male Wistar rats using the drug mexidol ("Farmasoft" Russia). The penetration of mexidol into different compartments of the brain (the cortex, cerebellum, thalamus and medulla) and distribution between mitochondrial and cytoplasmic fractions of the cerebral cortex was studied. The concentration of mexidol in blood plasma and brain tissues was measured using HPLC. RESULTS AND CONCLUSION: Mexidol penetrated through the blood-brain barrier into brain compartments of rats with the maximal accumulation in the cortex. In the brain cortex cells, mexidol was identified in the cytoplasmic and mitochondrial fractions.
Subject(s)
Antioxidants/pharmacokinetics , Blood-Brain Barrier/metabolism , Picolines/pharmacokinetics , Animals , Cerebellum/metabolism , Cerebral Cortex/metabolism , Cytosol/metabolism , Male , Medulla Oblongata/metabolism , Mitochondria/metabolism , Rats , Rats, Wistar , Thalamus/metabolism , Tissue DistributionABSTRACT
The research consists in the investigation of the sex differences of P-glycoprotein functional activity and expression in Chinchilla rabbits. P-glycoprotein functional activity was assessed by the pharmacokinetics of its probe substrate--fexofenadine after its single oral administration. P-glycoprotein expression was investigated by immunohistochemistry method. It is shown that male's maximal concentration of fexofenadine, its areas under concentration-time curves, half-life and retention time were higher and its clearance was lower than female's. The efficient differences in pharmacokinetic parameters of fexofenadine confirm more intensive excretion and less intensive absorption in gastro-intestinal tract of fexofenadine. This data indicate that P-glycoprotein activity is more active in female than in male. Immunohistochemistry analysis shows that total liver and intestine P-glycoprotein expression is more intensive in females, than in males that correlates with its more active functioning.
Subject(s)
ATP Binding Cassette Transporter, Subfamily B, Member 1/metabolism , Histamine H1 Antagonists, Non-Sedating/pharmacokinetics , Intestinal Mucosa/metabolism , Liver/metabolism , Terfenadine/analogs & derivatives , ATP Binding Cassette Transporter, Subfamily B, Member 1/genetics , Administration, Oral , Animals , Area Under Curve , Female , Gene Expression , Half-Life , Histamine H1 Antagonists, Non-Sedating/metabolism , Intestines/drug effects , Liver/drug effects , Male , Rabbits , Sex Factors , Terfenadine/metabolism , Terfenadine/pharmacokineticsABSTRACT
In the review of literature the structure, localization and a physiological role of efflux biobiotics and xenobiotics transporter - P-glycoprotein - is characterized, molecular mechanisms of induction and inhibition of its functional activity are systematized.
Subject(s)
ATP Binding Cassette Transporter, Subfamily B, Member 1/genetics , Gene Expression Regulation/genetics , Polymorphism, Genetic , RNA, Messenger/genetics , ATP Binding Cassette Transporter, Subfamily B, Member 1/chemistry , ATP Binding Cassette Transporter, Subfamily B, Member 1/metabolism , Animals , Gene Dosage , Humans , Promoter Regions, Genetic , Protein Transport , RNA Stability , RNA, Messenger/metabolism , Signal Transduction , Xenobiotics/metabolismABSTRACT
Objective. To compare pharmacokinetic parameters of mexidol (coated tablets, "Farmasoft") and mexiprim (tablets film-coated, "STADA CIS"). Material and methods. The study included 14 adult male Chinchilla rabbits. Concentration of 2-ethyl-6-methyl-3-hydroxypyridine succinate in the blood plasma of animals was analyzed using HPLC with UV detection. Results and conclusion. Mexidol as compared to mexiprim was more completely and rapidly absorbed from the gastrointestinal tract, it was confirmed by the higher value of maximal concentration of 2-ethyl-6-methyl-3-hydroxypyridine succinate and less maximal concentration time after mexidol administration. The drugs had similar excretion that was confirmed by the lack of significant differences in the values of total clearance, half-life, and the average retention time.
ABSTRACT
Hippophae, Rosa and plantain oils have been shown to produce and essential therapeutic action on chemical burns of rabbit eye. The effect was attained in the phases of trophic disturbances and epithelialization.
Subject(s)
Burns, Chemical/drug therapy , Eye Burns/drug therapy , Plant Oils/therapeutic use , Plantago , Plants, Medicinal , Animals , Corneal Injuries , Drug Evaluation, Preclinical , Female , Male , Ophthalmic Solutions , Rabbits , Time FactorsSubject(s)
Blood Vessels/metabolism , Carbon Tetrachloride Poisoning/metabolism , Catecholamines/metabolism , Chemical and Drug Induced Liver Injury/metabolism , Electrolytes/metabolism , Water-Electrolyte Balance/drug effects , Acute Disease , Animals , Blood Vessels/drug effects , Carbon Tetrachloride Poisoning/drug therapy , Cats , Chemical and Drug Induced Liver Injury/drug therapy , Drug Evaluation, Preclinical , Silymarin/therapeutic use , Time FactorsABSTRACT
Experiments on cats with dichloroethane affection of the liver showed that changes in the electrolyte balance in the wall of blood vessels differing in structure and function occurred in phases in different periods of the examination. The course of hepatitis was characterized by gradual exhaustion of epinephrine and norepinephrine stores in the vascular wall. Aevit causes increase of the calcium content, riboflavin--a decrease of the calcium level and increase of the sodium concentration, and legalon causes an increase of the potassium, calcium, and magnesium content.
Subject(s)
Blood Vessels/metabolism , Catecholamines/metabolism , Chemical and Drug Induced Liver Injury/drug therapy , Electrolytes/metabolism , Animals , Cats , Chemical and Drug Induced Liver Injury/metabolism , Female , MaleABSTRACT
The effect of testosterone propionate (1 mg/kg) on the specific activity of lactate dehydrogenase, malate dehydrogenase, contents of pyruvic and lactic acids, levels of catecholamines in target tissues and non-target tissues of rats was studied. Deficit of androgens and their single compensation by administering testosterone propionate lead to an inhibition of energy formation, a decrease of enzyme activity and contents of metabolites in tissues of the seminal vesicles. The course administration of testosterone propionate increases the activity of malate dehydrogenase in the aorta and myocardium. Acetylsalicylic acid (40 mg/kg) induces an increase of noradrenaline levels in the heart and aorta along with an increase of androgen level in the organism.
Subject(s)
Blood Vessels/drug effects , Catecholamines/metabolism , Energy Metabolism/drug effects , Testosterone/pharmacology , Animals , Aorta/drug effects , Aorta/metabolism , Aspirin/pharmacology , Blood Vessels/metabolism , Heart/drug effects , L-Lactate Dehydrogenase/metabolism , Lactates/metabolism , Lactic Acid , Malate Dehydrogenase/metabolism , Male , Myocardium/metabolism , Orchiectomy , Pyruvates/metabolism , Pyruvic Acid , Rats , Seminal Vesicles/drug effects , Seminal Vesicles/metabolismABSTRACT
The spasmolysant fenicaberane was found to induce diverse changes in electrolyte levels, a significant increase of lactate content in all vascular zones, various changes in pyruvate levels depending on the vascular tissue type.
Subject(s)
Benzofurans/pharmacology , Blood Vessels/drug effects , Carbohydrate Metabolism , Parasympatholytics/pharmacology , Animals , Blood Vessels/metabolism , Cats , Electrolytes/metabolism , Female , Lactates/metabolism , Lactic Acid , Male , NAD/metabolism , Oxidation-Reduction , Pyruvates/metabolism , Pyruvic AcidABSTRACT
The effects of aevite and riboflavin on electrolyte balance in the vessel wall were studied in toxic hepatitis in the cat. Significant changes in the contents of Na+, K+, Ca2+ and Mg2+ ions in the hepatic blood vessels were found in all periods of observation. The treatment of toxic hepatitis with aevite and riboflavin results in normalization of electrolyte balance of the vessel wall.
