ABSTRACT
The pharmacokinetics of 4-methyl-2,6-diisobornylphenol (MDIBP) in rat blood plasma has been studied after intravenous injection. The drug concentration in the plasma was determined using a reverse-phase HPLC procedure. It is shown that MDIBP rapidly penetrates into intensively perfused organs, but is slowly eliminated from the organism (MRT value amounting to 9 h).
Subject(s)
Antioxidants/pharmacokinetics , Camphanes/pharmacokinetics , Cresols/pharmacokinetics , Models, Biological , Animals , Antioxidants/administration & dosage , Antioxidants/chemistry , Camphanes/administration & dosage , Camphanes/blood , Camphanes/chemistry , Cresols/administration & dosage , Cresols/blood , Cresols/chemistry , Injections, Intravenous , Male , Organ Specificity , Rats , Rats, Wistar , Tissue DistributionABSTRACT
Distribution of p-tyrosol in organism was studied in rats after a single intravenous administration in a dose of 200 mg/kg. It was shown that p-tyrosol rapidly penetrates into well perfused organs (brain, heart, kidneys). The maximum concentration ofp-tyrosol in these organs was determined in 1 minute after administration, and the mean distribution constant was within 0.8-1.11. The albumin bound fraction ofp-tyrozol amounted to 0.26-0.30.
Subject(s)
Anti-Arrhythmia Agents/pharmacokinetics , Brain Chemistry , Kidney/chemistry , Myocardium/chemistry , Phenylethyl Alcohol/analogs & derivatives , Animals , Anti-Arrhythmia Agents/administration & dosage , Anti-Arrhythmia Agents/blood , Arrhythmias, Cardiac/drug therapy , Biological Availability , Biotransformation , Half-Life , Injections, Intravenous , Kidney/blood supply , Phenylethyl Alcohol/administration & dosage , Phenylethyl Alcohol/blood , Phenylethyl Alcohol/pharmacokinetics , Protein Binding , Rats , Serum Albumin/metabolism , Spectrometry, Fluorescence , Tissue DistributionABSTRACT
We demonstrated in experiments on rats with left coronary artery occlusion that intravenous administration of 20 mg/kg n-tyrosol during ischemia limited manifestations of oxidative stress in myocardial tissue during early post reperfusion period: content of diene and triene conjugates lowered 16 and 20%, respectively. This was associated with higher preservation of cardiomyocytes and reduction of the infarction zone.
Subject(s)
Disease Models, Animal , Myocardial Infarction , Myocardial Reperfusion Injury , Oxidative Stress/drug effects , Phenylethyl Alcohol/analogs & derivatives , Rats, Wistar , Animals , Antioxidants/administration & dosage , Antioxidants/metabolism , Cardiotonic Agents/administration & dosage , Cardiotonic Agents/metabolism , Coronary Vessels/pathology , Coronary Vessels/physiopathology , Electrocardiography , Injections, Intravenous , Male , Myocardial Infarction/diagnosis , Myocardial Infarction/drug therapy , Myocardial Infarction/metabolism , Myocardial Infarction/pathology , Myocardial Infarction/physiopathology , Myocardial Reperfusion/adverse effects , Myocardial Reperfusion Injury/drug therapy , Myocardial Reperfusion Injury/etiology , Myocardial Reperfusion Injury/metabolism , Myocardial Reperfusion Injury/pathology , Myocardial Reperfusion Injury/physiopathology , Myocardium/metabolism , Myocardium/pathology , Phenylethyl Alcohol/administration & dosage , Phenylethyl Alcohol/metabolism , RatsABSTRACT
We studied the antithrombotic and thrombolytic effects of Trombovazim, a highly-purified proteolytic enzyme preparation obtained by immobilization of bacterial proteinases (Bacillus) on polyethylene oxide with a molecular weight of 1.5 kDa. Blood absorption of the preparation was evaluated after intragastric administration. In vitro experiments showed that Trombovazim produces anticoagulant and thrombolytic effects, which manifested in inhibition of fibrin clot formation and acceleration of its lysis. Drug concentration in the blood was elevated from the 4th to the 7th hour after intragastric administration of Trombovazim in a dose of 2250 U/kg, being maximum by the 5th hour (0.044+/-0.011 U/ml). Course treatment with Trombovazim (1000 U intragastrically, twice daily for 3 days) had a thrombolytic effect on rats with experimental intravascular thrombosis. This effect was manifested in a decrease in thrombus weight and increase in the percent of rats with recanalization of the occluded carotid artery.
Subject(s)
Anticoagulants/pharmacology , Bacterial Proteins/pharmacology , Carotid Artery Thrombosis/drug therapy , Peptide Hydrolases/pharmacology , Animals , Anticoagulants/blood , Anticoagulants/pharmacokinetics , Bacterial Proteins/blood , Bacterial Proteins/pharmacokinetics , Blood Coagulation/drug effects , Blood Coagulation/physiology , Carotid Arteries/drug effects , Carotid Arteries/physiopathology , Carotid Artery Thrombosis/chemically induced , Cerebrovascular Circulation/drug effects , Ferrous Compounds , Fibrin/metabolism , Male , Peptide Hydrolases/blood , Peptide Hydrolases/pharmacokinetics , Rats , Rats, Wistar , Time FactorsABSTRACT
Antiarrhythmic activity of n-tyrosol was demonstrated on the model of early occlusion and reperfusion arrhythmia. The preparation reduces the incidence of ventricular tachycardia and fibrillation, increases the percent of animals without ventricular arrhythmia, and moderates the severity of developing ventricular arrhythmias.
Subject(s)
Anti-Arrhythmia Agents/therapeutic use , Myocardial Reperfusion Injury/drug therapy , Phenylethyl Alcohol/analogs & derivatives , Animals , Phenylethyl Alcohol/therapeutic use , Rats , Rats, Wistar , Tachycardia, Ventricular/prevention & control , Ventricular Fibrillation/prevention & controlABSTRACT
The effect of Neutrostim (preparation of granulocytic colony-stimulating factor) on recovery of myocardial tissue after acute myocardial infarction was studied in rats. A course of Neutrostim after ligation of the left coronary artery led to normalization of electrocardiographic and morphological parameters of the myocardium after one month.
Subject(s)
Granulocyte Colony-Stimulating Factor/therapeutic use , Myocardial Infarction/therapy , Myocardium/pathology , Animals , Coronary Vessels , Electrocardiography , Granulocyte Colony-Stimulating Factor/pharmacology , Ligation , Male , Myocardial Infarction/pathology , Myocardial Infarction/physiopathology , Rats , Rats, Wistar , Time FactorsABSTRACT
Polyetox, a medicinal form of high-molecular-weight poly(ethylene oxide) (HMWPEO) improved peripheral blood supply, normalized the overall oxygen consumption, decreased erythrocyte aggregation, and reduced blood viscosity at low shear rate, and restored the antiturbulent properties (hydrodynamic index) of blood in the experiments on rats with crush syndrome. In rats with low resistance, polyetox increased the cardiac output.
