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Biomedical subjects

G Kaik

Publications and source records attributed to G Kaik.

At least 55 records · Page 3Linked to original sources

A model for distinguishing between beta1-receptors which mediate a specific effect on the heart rate and those which mediate a positively inotropic effect.

The study was conducted in six healthy male volunteers aged between 20 and 30 years. Cardiac output was determined by means of the Swan-Ganz-thermodilution-method. A control-study was carried out, during which an isoproterenolinfusion with increasing doses was given. Fifty minutes after i.v. injection of a beta-receptor-blocker the hemodynamic parameters were measured again under increasing doses of isoproterenol until the block was overcome. This study procedure was performed twice in each subject at an interval of at least 14 days. For the one study 15 mg propranolol i.v. and for the other 0,5 mg mepindolol i.v., a new beta-receptor-blocker, were injected. After i.v. injection of propranolol the dose-response-relationship-curve for the heart-rate (HR) and stroke volume (SV) describes a definite shift to the right. After mepindolol the dose-effect curve for the heart rate describes a definite shift to the right, as seen with propranolol. In contrast, only a very slight shift can be seen in respect of the SV increase, i.e. the SV and HR curves dissociate under mepindolol. The results of our study indicate, that a distinction can be made with respect to the so-called beta 1-receptors between those mediating a specific effect on the heart-rate and those mediating a mainly positive inotropic effect.

Adrenergic beta-Antagonists↗

The bio-availability of beta-acetyldigoxine (Novodigal) alone and combined with oxyfedrine (Ildamen-Novodigal).

The bio-availability of various galenic preparations of beta-acetyldigoxine was tested in six healthy probands after a single oral dose (1 mg). The availability parameters were calculated from the areas under the plasma concentration curves and from the cumulative urinal excretion. There was no significant difference between the bio-availabilities of Novodigal (beta-acetyledigoxine tablets), Ildamen-Novodigal (beta-acetyldigoxine and oxyfedrine) and an alcoholic solution of beta-acetyldigoxine. Correlation calculations showed that the determination of the plasma concentration courses up to six hours after substance application are most favourite in regard to judging the absorption processes of digoxine preparations. For the assessment of the bio-availability, the methods of comparing the areas under the blood level curves of 0 to 6 hrs and of comparing the cumulative urinal excretion over a period of 24 hrs were of equal validity.

Adult↗

The bio-availability of beta-acetyldigoxine alone and combined with aluminum hydroxide and magnesium hydroxide (Alucol).

The bio-availability of Novodigal (beta-acetyldigoxine) alone and applied together with Alucol (aluminum hydroxide, magnesium hydroxide) was studied in six healthy probands. Bio-availability parameters were calculated from the areas under the plasma concentration curves and from the comparison of the blood levels after absorption during steady state. There was no significant difference between the bio-availability of beta-acetyldigoxine alone and that of the combination with Alucol. Thus, beta-acetyldigoxine combined with antacids of the aluminum hydroxide and magnesium hydroxide type can be applied in the same dosage as usual since no decrease of effect has to be apprehended.

Adult↗

[Onset of action and maximum effect of bronchodilators administered by a metered dose inhaler. Clinical investigations with fenoterol, hexoprenaline, ipratropium bromide, isoprenaline, orciprenaline, salbutamol and terbutaline (author's transl)].

The acute effect of bronchodilatory metered dose inhalers was tested by whole-body plethysmography in patients with chronic obstructive airway disease. All patients had already used metered dose inhalers. The 18 patients of group A were successfully using the parasympatholytic drug ipratropium bromide. The onset of action of hexoprenaline, salbutamol and terbutaline was slightly quicker than that of ipratropium bromide but the maximum bronchodilation was similar. The 18 patients of group B considered adrenergics to be much more effective. Mean values showed that the onset of bronchodilation and maximum effect with fenoterol, isoprenaline, and orciprenaline was quicker and stronger than after ipratropium bromide over the first 20 minutes. Following ipratropium bromide the single resistance diagrams of group B, with the exception of 4 patients, showed bronchodilation equal to that of group A and also to that obtained following adrenergics in group B. The patients apparently judged bronchodilation on the basis of the adrenergic side effects rather than by improvement of dyspnoea. There were 3 patients, however, who repeatedly showed better bronchodilation in response to adrenergics than parasympholytic agents, not depending of the way of application.

Aerosols↗

[Acute bronchodilator effect of chinoxaline, prednisolone, ipratropium bromide and fenoterol tested by whole-body plethysmography (author's transl)].

The acute bronchodilator effect of chinoxaline, prednisolone and ipratropium bromide was tested by whole-body plethysmography in 18 patients with chronic obstructive airway disease over a period of 60 min. The subsequent administration of fenoterol by a metered dose inhaler demonstrated the possibility of further bronchodilation. Chinoxaline (80 mg i.v.) was followed by a statistically-significant decrease in airway resistance to 82.66% of the baseline value after 5 min. (maximum reduction) and to 87.11% after 60 min.; fenoterol (0.4 mg = 2 puffs) caused a further marked decrease to 49.61% after 20 min. Prednisolone (250 mg i.v.) did not produce statistically-significant acute bronchodilation. Airway resistance decreased to a minimum level of 89.16% after 20 min. and to 90.77% after 60 min.; however, following fenoterol (0.4 mg = 2 puffs) the airway resistance was reduced to 45.72%. Ipratropium bromide inhalation (0.08 mg = 4 puffs) resulted in the greatest bronchodilatory response, with a statistically-significant effect from the 5th to the 60th min. Airway resistance was 64.66% after 5 min., 63.22% after 10 min., 58.94% after 20 min., 57.72% after 30 min. and 51.22% after 60 min. (maximum reduction); fenoterol (0.4 mg = 2 puffs) caused only a slight further decrease to 48.32%.

Adult↗

[Study of the influence of the beta-sympatholytic drug KO 1366 (Bunitrolol on lung function (author's transl)].

20 untreated outpatients suffering from chronic obstructive airway disease were tested with a new beta-sympatholytic agent, Kö 1366 (bunitrolol) or placebo in a randomized symptoms of bronchitis, but hacetylcholine inhalation was followed by severe bronchospastic hyperreactivity. The intravenous administration of 2.5 mg Kö 1366 resulted in a rapid and statistically significant (p less than 0.001) marked decrease in heart rate due to the beta-sympatholytic effect. Airway resistance, however, measured by whole-body plethysmography, was not affected. Kö 1366 can be regarded as a cardio-selective beta-sympatholytic drug in so far as i.v. administration is possible in patients with airway disease during a non-obstructive period. Moreover, should a bronchospastic reaction occur immediate control by inhalation of adrenergic or vagolytic drugs is possible.

Adult↗

[(Whole body plethysmographic studies on the bronchospasmolytic effect of injectabls drugs. Comparison of aminophylline, diprophylline and hexoprenaline)].

The bronchodilator effect of intravenously administered drugs was tested by whole bodyplethysmography in 24 patients with chronic obstructive airway disease over a period of 60 min. Subsequent to this, another bronchodilator was applied by a metered dose inhaler. Aminophylline (0,24 g i.v.) was followed by a decrease of airway resistance to a maximum of 73,04% of the base line value after 30 min. and to 76,33% after 60 min; inhalation of fenoterol (0,4 mg) caused a further decrease to 47,33% after 20 min. Diprophylline (0,28 gi.v.) produced only a slight decrease to a maximum of 95,75% after 20 min. and to 99,54% after 60 min.; fenoterol (0,4mg) reduced airway resistance to 55,29%. Hexoprenaline (0,005 mg i.v.) was followed by a decrease to a maximum of 74,71% after 5 min. and to 92,83% after 60 min.; ipratropiumbromide (0,08 mg) caused a further decrease to 54,92%. A considerable increase of heart rate, from 89,25/min. to 106,15/min. occurred only after hexoprenaline. For intravenous bronchodilator therapy we prefer aminophylline. Optimal bronchodilation however, was seen only after further application of fenoterol or ipratropiumbromide by a metered dose inhaler.

Adult↗

[Clinical testing of bronchospasmolytics in combined alternating test schedules].

NAB 365, a new beta2-adrenergic bronchodilator was tested in oral doses of 0.01, 0.02, 0.03 and 0.04 mg. An acute trial was carried out in outpatients suffering from chronic obstructive airways disease. Airway resistance was measured by bodyplethysmography. For doses from 0.02 to 0.04 mg NAB 365 a quick, dose related and statistically significant bronchodliation without remarkable side effects could be found. The application of Fenoterol and Sch 1000 (ipratropiumbromide) by a metered dose inhaler was followed by a further and finally equal bronchodilation. To avoid adrenergic side effects the combination of NAB 365 with Sch 1000 should be preferred to the combination of NAB 365 with Fenoterol.

Adrenergic beta-Agonists↗

[Combined administration of ipratropium bromide (sch 1000) and fenoterol in patients with chronic obstructive airway disease (author's transl)].

40 outpatients with chronic obstructive airway disease received the parasympatholytic bronchodilator ipratropium bromide (Sch 1000) and the sympathomimetic bronchodilator fenoterol from a metered dose inhaler. After evaluation of the initial values, first Sch 1000 was administered and 20 min. later airway resistance was measured, then fenoterol was given and a measurement was taken again 20 min. later. On the following day the aerosol inhalants were given in the reverse sequence. After the first inhalation 0.08 mg Sch 1000 proved to be an equally strong bronchodilator as 0.4 mg fenoterol and airway resistance was decreased to 52% and 55%, respectively of the initial value (p less than 0.001). The additional inhalation of the other bronchodilator caused a further slight decrease in airway resistance to a minimum of 47%, but was statistically significant (p less than 0.001) only in the case of the fenoterol/Sch 1000 sequence. The importance of bronchiolar tonus in regard to fluctuation of airway resistance and the possibility of a specific additive bronchodilatory effect of adrenergics and vagolytics is discussed.

Adult↗

[Body plethysmographic investigations with the new bronchodilator NAB365 (author's transl)].

NAB 365, a new beta2-adrenergic bronchodilator was tested in oral doses of 0,01, 0,02, 0,03, and 0,04 mg. An acute trial was carried out in outpatients, suffering from chronic obstructive airways disease. with doses of 0,02 and 0,04 mg NAB 365 a quick, dose related and statistically significant bronchodilation without remarkable side effects was found.

Bronchodilator Agents↗

[The effect of metered aerosols on bronchospasm induced by acetylcholine inhalation comparison of ipratropiumbromide (Sch 1000) and fenoterol (Berotec) (author's transl)].

Twenty patients with bronchoconstriction induced by inhaled acetylcholine were treated with Sch 1000 and Berotec comparatively. From the mean value diagrams a faster, stronger and more constant decrease of bronchial resistance due to Berotec inhalation can be recognized. The effect, however, is called in question by contrasting diagrams of single cases.

Acetylcholine↗