Biomedical subjects
Publications and source records attributed to G Kaik.
N-Amidino-2-(2,6-dichlorophenyl)-acetamide hydrochloride (guanfacine) reduces blood pressure dose-dependently for more than 38 h. The blood pressure lowering effect is not seen immediately after medication. Side effects are: decrease in heart rate, orthostatic effect, dizziness and weariness.
UNLABELLED: The effect of mepindolol-sulfate (2 x 2.5 mg) was tested in 20 patients with coronary heart disease in a controlled study against placebo resp. propranolol (3 x 40 mg). RESULTS: 1. The frequency and intensity of anginal attacks were reduced significantly under mepindolol-sulfate therapy.-- 2. There was a significant improvement of ergometric exercise tolerance under mepindolol-sulfate therapy.--3. Additionally a reduction of ST-depression in ECG was found under mepindolol-sulfate.--4. In patients with coronary heart disease the clinical effect of mepindolol-sulfate in a daily dose of 2 x 2.5 mg was equal to propranolol in a daily dose of 3 x 40 mg.
In a prospective study 73 patients on maintenance digitalis treatment at the Paracelsus Institute, Bad Hall, were clinically examined and the dosage of the drug was adjusted according to cardiac symptoms. The clinical effects were correlated to digoxin concentrations measured on the day following admission to hospital and on the 21st day of treatment. The following practical conclusions were reached: 1. More than 50% of the patients were underdigitalized. 2. There is often no indication for digitalis therapy in patients with a low daily maintenance digoxin dosage and normal renal funciton. 3. The usual recommended maintenance dosage of digoxin provides serum digoxin levels in the lower region of the therapeutic range. 4. Patients with symptoms of decompensation taking an average dosage of digoxin need more digitalis. There is generally no danger of toxicity when the dosage is increased. 5. The serum digoxin concentration in patients with slightly reduced renal function lies in the upper region of the therapeutic range with usual doses of digoxin.
The effect of calculation stress on hemodynamic parameters and plasma adrenalin and noradrenalin was studied in two groups of 6 male subjects, before and during beta-Blockade. One group received propranolol 15 mg i.v. and the other received mepindolol sulphate 0,5 mg i.v. There was an increase in heart rate, cardiac output and blood pressure during mental stress. A significant increase in plasma adrenalin but not in noradrenalin occurred at the same time. The stress-induced rise in HR but not that in blood pressure could be prevented by beta-receptor blockage with propranolol and mepindolol sulfate. The peripheral resistance (PR) and diastolic blood pressure in stress were even higher after propranolol than in the control study. Propranolol had no effect on the increased adrenalin concentration during stress, but it was prevented by mepindolol sulfate. There was no correlation between the increase in HR and that in adrenalin during stress, but the HR in stress and the HR reaction to infused isoproterenol were highly correlated.
The acute bronchodilator effect of the beta 2-adrenoceptor agonist terbutaline was tested single-blind cross-over in out-patients with chronic obstructive airways disease (intrinsic asthma). In 7 series comparisons were made with other marketed bronchodilators. Airways resistance was measured by whole body plethysmography. In another 3 series the effect on heart rate of terbutaline and other adrenocepter agonists was tested in healthy volunteers. Terbutaline and the adrenoceptor agonists clenbuterol, epinephrine, fenoterol, hexoprenaline, isoprenaline, metaproterenol, reproterol and salbutamol, the vagolytics atropine, ipratropium bromide and AA 22-263, the xanthinederivative theophylline ethylenediamine and one combined substance drug were used.
In patients with hyperkinetic heart syndrome we found at rest a higher heart rate, a higher stroke volume and a higher cardiac output than in normal volunteers. Therefore blood pressure is high although peripheral resistance is lower than in normals. Similar circulatory differences were found under conditions of mental stress. After beta-adrenergic blockade with 15 mg Propranolol heart rate and cardiac output decrease, whereas peripheral resistance increases. Mean blood pressure thus remains unchanged. Even after beta-adrenergic blockade circulatory differences between normals and patients with hyperkinetic heart syndrome are seen. The possible causes of these differences are discussed.
The hemodynamic effects of 20 mg Bufuralol-HCl and of 15 mg Propranolol given to hypertensives i.v. at rest and under physical exercise conditions were examined. It could be shown that Bufuralol-HCl lowered the diastolic BP and PR at rest already in the acute experiment, contrary to Propranolol. Under physical exercise conditions the diastolic BP is lowered, the PR remains unchanged in spite of reduced CO. After exclusion of other possible explanations, Bufuralol-HCl may lower the diastolic BP acutely at least partly by inhibition of cerebral beta-receptors. A faster and better liquor diffusion could be the reason for these results. It can be assumed that the acute BP lowering effect is mediated by the same mechanism as the chronic effect of the other beta-receptor blocking drugs.
In this hemodynamic study a new beta-receptor blocker, Bufuralol-hydrochloride was compared with Pindolol under an Isoproterenol infusion with increasing doses in healthy male volunteers. We found the following results: 1. Before Isoproterenol peripheral resistance increased after acute i.v. application of Pindolol but decreased after Bufuralol-hydrochloride i.v. application. 2. After beta-receptor blockade with either Bufuralol-hydrochloride or with Pindolol a shift to the right of the dose effect relationship concerning heart rate and cardiac output under Isoproterenol infusion was observed, indicating beta 1-blockade. 3. The reduction of peripheral resistance which is usually observed as a sign of beta 2-blockade was also shifted to the right under the influence of both drugs. 4. This proves Bufuralol-hydrochloride to be a non-specific beta-blocking agent with an affinity to the beta 1- and beta 2-receptors. 5. Although Bufuralol-hydrochloride has a beta 2-blocking property which is even more pronounced than that of Pindolol, it reduces acutely, intravenously given, peripheral resistance.
The acute bronchodilator effect of the beta 2-adrenoceptor agonist terbutaline was tested single-blind cross-over in out-patients with chronic obstructive airways disease (intrinsic asthma). In 7 series comparisons were made with other marketed bronchodilators. Airways resistance was measured by whole body plethysmography. In another 3 series the effect on heart rate of terbutaline and other adrenoceptor agonists was tested in healthy volunteers. Terbutaline and the adrenoceptor agonists clenbuterol, epinephrine, fenoterol, hexoprenaline, isoprenaline, metaproterenol, reproterol and salbutamol, the vagolytics atropine, ipratropium bromide and AA 28-263, the xanthine-derivative theophylline ethylenediamine and one combined substance drug were used.
A new beta-receptor blocker (Celiprolol) was characterized in man by haemodynamic studies carried out on a random cross-over basis in 6 volunteers before and after intravenous administration of the drug or propranolol. The studies were performed at rest and in response to ergometer exercise. The studies showed that: 1. Celiprolol is a cardio-selective beta-receptor blocker with pronounced intrinsic sympathomimetic activity. Hence, Celiprolol increases the heart rate and cardiac output at rest. 2. The heart rate was reduced by Celiprolol during pronounced physical exercise. 3. Celiprolol probably has only a very slight blocking effect on those, beta1-receptors which mediate a positive inotropic effect. 4. The increase in blood pressure during exercise was less pronounced during Celiprolol medication than with propranolol.
The hemodynamic effects of a new beta-receptor blocking agent, bufuraolo HCl, were compared with those of pindolol. Contrary to pindolol, bufuralol HCl induces a decrease of the peripheral resistance immediately. Under exercise conditions, the peripheral resistance increases under pindolol whereas it remains constant under bufuralol HCl in spite of reduced cardiac output. As an explanation, an effect of bufuralol HCl on peripheral resistance is discussed which might be independent of the beta-receptor blocking effects in the periphery.
UNLABELLED: The effect of exercise upon hemodynamic variables was investigated in seven patients with coronary artery disease during an eight-week double blind cross-over study with placebo and with mepindolol-sulfate, a new beta-receptor blocking agent. RESULTS: 1. The first hemodynamic sign of myocardial ischemia during exercise was an increase of pulmonary capillary pressure in parallel with ST-segment depression in the Ecg. 2. Angina was accompanied by a fall of the stroke volume and an increase of the peripheral resistance. 3. During beta-receptor blockade with mepindolol-sulfate angina was compensated, the unfavourable hemodynamic effects seen during placebo did not occur. 4. No signs of congestive heart failure were found during mepindolol-sulfate-therapy. 5. Mepindolol-sulfate showed a pronounced blood-pressure lowering effect.
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UNLABELLED: The hemodynamic effect of mepindolol-sulfate, a new non-cardioselective beta-receptor blocking agent, was compared with the hemodynamic effect of propranolol at rest and during exercise in five patients with coronary artery disease during an eight week double blind cross-over study. RESULTS: 1. The beta-receptor blocking effect of mepindolol-sulfate is 25 times higher than that of propranolol. 2. No hemodynamic difference between mepindolol-sulfate and propranolol was seen at rest. 3. The increase of blood pressure during exercise was less pronounced during mepindolol-sulfate-medication compared to propranolol. 4. Propranolol seems to achieve a more pronounced negative inotropic effect than mepindolol-sulfate.
The pharmakokinetic data (elimination half-life, apparent distribution volume, total and renal clearance and cumulative urine excretion) were determined after intravenous administration of 1 mg digoxin in 9 female patients with an average age of 52 +/- 15 years with manifest hyperthyroidism. The study protocol was repeated after normalization of thyroid function by means of conventional thyrostatic therapy. Digoxin was determined by radioimmunoassay.
The acute bronchodilator effect of aerosolized fenoterol, salbutamol, ipratropium bromide, and terbutaline was tested in single-blind cross-over trials by whole body plethysmography. In 4 different series, patients with chronic obstructive airway disease were investigated using combined alternating medication. Only commercially available metered dose inhalers were included in this study. Special attention was paid to comparison of the efficacy of administration by the investigator and by the patients themselves. The doses recommended by the manufacturers sometimes resulted in widely different bronchodilation when the metered dose inhalers were administered by the patients. Some possible reasons for these results and some implications with regard to different types of inhalers, single doses, instruction of the patients and evaluation of clinical trials are discussed.
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