piperidines and etozolin

The influence of Etozolin (Elkapin) on the carbohydrate metabolism was studied in 10 healthy volunteers, 6 patients with chemical diabetes and 10 with overt diabetes by blood glucose measurements and oral glucose tolerance tests with determinations of serum insulin levels. The healthy volunteers received 800 mg Etozolin per day during the treatment period of 3 days, the two groups of patients 400 mg Etozolin for 8 days. The laboratory parameters of the treatment period were compared with the corresponding values of the pre- and posttreatment periods and evaluated statistically. There was no statistically significant difference in the carbohydrate metabolism between the 3 test periods in all groups studied. As a result of the induced diuresis body weight, serum electrolytes and urine volume changed significantly during the Etozolin treatment as compared with the pre- and posttreatment values. Other changes of laboratory parameters could not be seen. In diabetic hypertensive patients a significant reduction of blood pressure was observed.

Topics: Adult; Aged; Blood Glucose; Carbohydrate Metabolism; Clinical Trials as Topic; Diabetes Mellitus; Drug Tolerance; Glucose Tolerance Test; Humans; Insulin; Middle Aged; Piperidines; Thiazoles; Time Factors

In a double-blind study under strict, standardized hospital conditions, the antihypertensive effect of etozolin was evalulated in 100 patients with hypertension. 50 patients received the drug, 50 placebo. The study was carried out over 22 days (5 days without medication, 12 days therapy, 5 days follow-up). A significantly better reduction of systolic and diastolic blood pressure in the supine and upright positions was observed with etozolin as compared to the pre-period and the placebo group. There were only minor side-effects; in 4 patients, therapy had to be interrupted because of orthostatic complaints.

Topics: Diuretics; Double-Blind Method; Drug Evaluation; Humans; Hypertension; Piperidines; Placebos; Thiazoles

Topics: Blood Coagulation; Blood Coagulation Tests; Diuretics; Fibrinolysis; Humans; Piperidines; Thiazoles

Topics: Chromatography, High Pressure Liquid; Female; Fetus; Humans; Maternal-Fetal Exchange; Piperidines; Placenta; Pregnancy; Pregnancy Trimester, First; Pregnancy Trimester, Second; Reference Values; Thiazoles

A sensitive and specific method for the determination of the diuretic Ethyl (Z)-(3-methyl-4-oxo-5-piperidino-thiazolidin-2-ylidene) acetate (etozolin, Elkapin) and its pharmacologically active main metabolite, (Z)-(3-methyl-4-oxo-5-piperidino-thiazolidin-2-ylidene) acetic acid (ozolinone), at therapeutic concentrations in plasma is described. The method is based on high performance liquid chromatography and the use of two structurally similar internal standards. Etozolin and its metabolite are extracted from the plasma into dichloromethane at pH 9 and pH 5, respectively, and the resulting residues are analyzed on a silica gel column. The elution peaks are detected by UV absorption at 281 nm. The sensitivity for both compounds is 20 ng/ml plasma. The precision of the method is about +/- 5%. The applicability to pharmacokinetic studies of etozolin is shown.

Topics: Benzothiadiazines; Chromatography, High Pressure Liquid; Diuretics; Humans; Piperidines; Sodium Chloride Symporter Inhibitors; Thiazoles; Time Factors

Topics: Antihypertensive Agents; Diuretics; Edema; Female; Humans; Hypertension; Male; Piperidines; Thiazoles

Topics: Diuretics; Dogs; Kidney; Pharmacology; Physiological Phenomena; Piperidines; Research; Thiazoles