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At least 793 records · Page 44Linked to original sources
PubMed1975

[Clinical studies on the effect of drugs used in the treatment of angina].

The report is based on a four-centre study on 25 patients with coronary insufficiency (ECG signs). In random sequence the following were given to each patient: a nitrate (isosorbide dinitrate), carbocromene, practolol, and oxyphedrine. The initial criterion for inclusion was S-T depression of 0.2 mV on stepwise exercise (bicycle ergometry). S-T depression, systolic blood pressure and heart rate changes were used as criteria. For each drug there was an acute test and a long-term test of 12 days. The Friedman test was used for the statistical evaluation of the results. Isosorbide dinitrate decreased the extent of S-T depression in the acute tests while practolol did so in the long-term test. Practolol reduced systolic pressure on long-term administration, with no difference in the acute experiment. Heart rate was reduced by practolol both acutely and long-term. These results give no indication for any possible differential treatment of coronary insufficiency, but this may be due to the selection of patients in this study.

Adult↗
PubMed1978

[Indications and risks of anti-arrhythmia treatment with propafenone (author's transl)].

Propafenone, a new anti-arrhythmia drug, was given at an average dose of 70-140 mg (1-2 mg/kg body-weight) to 124 patients with various types of cardiac arrhythmias. It proved successful in patients with ectopic beats and tachycardias of atrial or ventricular origin. Ectopic beats were suppressed in 40 of 81 patients, while sinus rhythm was restored in 15 of 19 patients with paroxysmal tachycardias. On the other hand, sinus rhythm was restored in only 5 of 22 patients with atrial tachy-arrhythmias, while in most of the others in this group the heart rate decreased markedly during propafenone injection. The effect of propafenone was on atrial and ventricular myocardium and on the conduction system, lowering the discharge rate of sinus node and ectopic pacemakers. ECG signs of pre-excitation disappeared in 4 of 9 patients with WPW syndrome given the drug. Propafenone may prolong atrioventricular and intraventricular conduction, as well as cause a transitory decrease in cardiac function and a fall in systemic arterial blood pressure. It should, therefore, not be given to patients in severe heart failure, hypotension or shock, or with high-degree atrioventricular, intraventricular or sinoatrial block.

Adult↗
PubMed2005

13C-labelling of xanthohumol in hop cones (Humulus lupulus).

Biolabelling conditions in hop cones of xanthohumol (Xn) were studied by feeding [U-13C]glucose, [1-13C]glucose, [ring-13C6]phenylalanine, [2-13C]sodium acetate or [2-13C]malonic acid as biosynthetic precursors to hop sprouts. Quantitative 13C-NMR spectroscopic analysis of the resulting labelled Xn showed different labelling patterns and ratios depending on precursor and feeding concentrations. The highest incorporation rate was achieved with [U-13C]glucose (9.41 +/- 1.22 %). With [ring-13C6]phenylalanine only ring B was labelled (3.51 +/- 0.08 % enrichment). [2-13C]sodium acetate and [2-13C]malonic acid allowed labelling of the A-ring (1.82 +/- 0.02 % and 1.74 +/- 0.03 % enrichment). The specific labelling pattern of the prenyl side chain with [1-13C]glucose (2.36 +/- 0.27 % enrichment) confirmed the biosynthetic origin to be MEP pathway-derived. On the basis of these results radiolabelling of Xn will be performed for in vivo bioavailability studies.

Carbon Isotopes↗
PubMed2006

Influence of xanthohumol on the binding behavior of GABAA receptors and their lateral mobility at hippocampal neurons.

The influence of the xanthohumol from Humulus lupulus L. on the binding of muscimol-Alexa Fluor 532 (Mu-Alexa), a fluorescently labeled GABAA receptor agonist, was studied by fluorescence correlation spectroscopy. An incubation of hippocampal neurons with 75 nM of xanthohumol increased the specific Mu-Alexa binding by approximately 17%, which was selectively found in GABAA receptor Mu-Alexa complexes with hindered lateral mobility [D(bound2) = (0.11 +/- 0.03) microm2/s] as described with midazolam.

Animals↗
PubMed1990

Isoliquiritigenin: a new aldose reductase inhibitor from glycyrrhizae radix.

Traditionally in Japan, some kampo medicines (traditional oriental herbal prescriptions) have long been used for the treatment of diabetic neuropathy. We have found that some aldose reductase inhibitors are included among these drugs. We further investigated the components of glycyrrhizae radix, a constituent of some kampo medicines, and isolated six compounds (GUs 9-17). Among these, GU-17, identified as isoliquiritigenin, had the most potent aldose reductase inhibiting activity. Isoliquiritigenin inhibited rat lens aldose reductase with an IC50 of 3.2 x 10(-7) M, using DL-glyceraldehyde as a substrate. It inhibited sorbitol accumulation in human red blood cells in vitro, with an IC50 of 2.0 x 10(-6) M. Isoliquiritigenin, when administered via an intragastric tube to diabetic rats, suppressed sorbitol accumulation in the red blood cells, the sciatic nerve, and the lens as effectively as ONO-2235. These results suggest that isoliquiritigenin may be effective in preventing diabetic complications.

Aldehyde Reductase↗
PubMed1990

Antidepressant profile of bupropion and three metabolites in mice.

Bupropion is a novel antidepressant, distinct from tricyclic antidepressants both neurochemically and behaviorally. Bupropion forms several metabolites in both rodents and humans. Three chemically different molecules - BW 306, BW 494, and BW 287 - were selected. Comparative assessment of antidepressant activity of bupropion and its metabolites in mice, and pharmacological analysis of possible mechanisms of action of the parent drug and its metabolites (using interaction studies with pimozide, D,L-propranolol, and prazosin) were carried out. The results obtained show that: bupropion has a pharmacological spectrum in various animal models which predicts both antidepressant and stimulatory activity in man. BW 306 is the most active of the metabolites studied and, compared to bupropion, seems more "antidepressant" and less stimulant. BW 494, compared to bupropion or BW 306, has a lower degree of activity in various tests used to evaluate antidepressants. BW 287 has no effect in any of the tests used in this study. The interaction studies with pimozide, D,L-propranolol, and prazosin in the various tests have shown that: the stimulatory effect of bupropion, BW 306, and BW 494 is antagonized by both pimozide and prazosin. in the behavioral despair test, the reduction in the duration of immobility by bupropion and BW 494 is antagonized by pimozide, but not by prazosin or D,L-propranolol. the antagonism of reserpine-induced hypothermia by bupropion and BW 306 is significantly decreased by prazosin and D,L-propranolol, but not by pimozide. These data suggest that the clinical antidepressant profile (without a major stimulatory effect) observed in man after administration of bupropion is related to metabolite BW 306 and possibly to BW 494, rather than to bupropion itself.

Animals↗
PubMed1989

Lack of effect of the antidepressant compound bupropion on pineal indoleamines.

The effects of the antidepressant compound bupropion were studied on rat pineal indoleamines. A pharmacologically relevant dose of bupropion either acutely (20 mg/kg) or chronically (20 mg/kg/day for 12 days) had no significant effect on pineal melatonin synthesis or other pineal indoleamine concentrations. The significance of this finding is discussed in relation to the lack of effect of bupropion on beta-adrenergic receptors.

Animals↗
PubMedDate not supplied

[Wolff-Parkinson-White syndrome with paroxysmal supraventricular tachycardias of the fetus and the newborn--case report].

Paroxysmal supraventricular tachycardia causing an intrauterine congestive heart failure was diagnosed in a fetus at 33 week's gestation. After maternal digitalization the tachycardias and the signs of heart failure disappears. Postpartum a Wolff-Parkinson-White syndrome was recognised by electrocardiography. The paroxysmal supraventricular tachycardias of the newborn was terminated abruptly by intravenous application of propafenon. Recurrences were prevented by the oral administration of propafenon.

Adult↗
PubMed1985

[Idiopathic ventricular tachyarrhythmia. Spontaneous variability and effect of various antiarrhythmic agents].

20 patients with idiopathic complex ventricular arrhythmias received propafenone 450 mg/d, disopyramide 600 mg/d and metoprolol 100 mg/d. Before commencement of the 3-week treatment period the 95% normal range for spontaneous changes in ventricular extrasystoles (VES), as couplets and runs, were determined from three 24 h-ECG recordings in each patient under drug-free conditions. A drug effect was assumed when the rate of VES/24 h for the control period decreased by greater than or equal to 83.5% or increased by greater than or equal to 505% in the test period. The frequency dependent normal range for couplets varied between a decrease from 100% to 92% (greater than or equal to 16 to greater than or equal to 44/d) and an increase from 650% to 1000% (greater than or equal to 3 to greater than or equal to 38/d) and for runs between a decrease from 100% to 85% (greater than or equal to 6 to 32/d) and an increase from 600% to 1000% (greater than or equal to 1 to 14/d). A decrease in all rhythm disturbances under the action of the 3 drugs could be shown for the whole group (P less than 0.01). On the basis of the calculated normal range, ventricular extrasystoles in the patients decreased significantly by 26-37%, couplets by 13-33% and runs by 0-55% depending to the drug. A drug dependent arrhythmogenic effect occurred in 4 patients. A preference for one or other of the drugs could not be established statistically.

Adult↗
PubMed1984

[Cholestasis after antiarrhythmic therapy with propafenone].

Propafenone, three times 150 mg/d over 33 days and two years later at the same dosage over six days, was administered to an 84-year-old man with ventricular extrasystoles (Lown IVa). Both times intrahepatic biliary stasis occurred, presumably a sign of a drug-allergic hepatitis. All other possible causes in the differential diagnosis were excluded. The lymphocyte transformation test demonstrated in vitro propafenone-sensitive patient-lymphocytes.

Aged↗
PubMed1983

[Esophageal ulcer caused by mexiletine].

The anti-arrhythmic drug mexiletine caused an oesophageal ulcer, confirmed by endoscopy and biopsy, in a 72-year-old woman. This side-effect has not previously been published. The clinical course was similar to that observed after oesophageal ulceration caused by other drugs. An ulcer in the piriform recess also developed in a 63-year-old man who was taking both acetylsalicylic acid and mexiletine: it cleared up after mexiletine had been discontinued.

Aged↗
PubMed1982

[Propafenon and propranolol in the management of cardiac extrasystoles (author's transl)].

The anti-arrhythmic effectiveness of propafenon (3 x 150 mg daily) combined with propranolol (3 x 20 mg daily) was compared with that of each drug alone in 15 patients with stable ventricular and (or) supraventricular extrasystoles. The frequency of extrasystoles decreased on propafenon alone by 70% (P less than 0.05), without further decrease on additional propranolol administration. Propranolol alone on average caused no significant decrease infrequency (35%). The most important ECG changes with the combined treatment consisted of a definite increase in P-Q interval by an average of 25% (P less than 0.01) while with propafenon alone it was 13%, with propranolol alone 19% . Propafenon plus propranolol decreased heart rate by a mean of 17% (P less than 0.01). The additive effect of both substances can lead to an inhibition of atrioventricular conduction and of sinus node function.

Adult↗
PubMed1982

[The effect of anti-arrhythmic drugs on myocardial function (author's transl)].

In a randomized study the influence of anti-arrhythmic drugs on left ventricular myocardial function was tested. Propafenon, mexiletine, tocainide, disopyramide or placebo were given over seven days on top of basic treatment with digitalis, diuretics and nitrates. Propafenon, mexiletine, tocainide and disopyramide had negative inotropic effects of 16, 17, 19 to maximally 30%, respectively. Echocardiography was especially suitable for serial assessment of left ventricular failure. Propafenon, mexiletine and tocainide are the anti-arrhythmic drugs of choice in the treatment of cardiac arrhythmias. However, the at times marked decrease in contractility must be taken into account when the decision is made whether a given arrhythmia requires treatment or not.

Adult↗
PubMed1980

[Antiarrhythmic drugs in chronic ventricular extrasystole (author's transl)].

Several class I antiarrhythmic drugs were used in an intraindividual comparative study in 15 patients with chronic stable ventricular extrasystole of various origins. In a randomised sequence lidocaine, ajmalin and, in a cross-over double blind study with placebo, the new antiarrhythmic Org 6001 were tested. Propafenon was given as a final preparation. Each substance was administered parentally in therapeutic doses. A significant placebo effect could be excluded, baseline control values before administration of individual substances correlated well. Comparing mean values obtained over one hour before and after administration of the substance it was shown that the effectiveness of drugs decreased as follows: ajmalin, propafenon, lidocaine, Org 6001. Whereas suppression of extrasystole was most marked after ajmalin, propafenon showed the longest period of activity. After Org 6001 divergent activity of arrhythmia could be observed; in some patients good antiarrhythmic effects could be demonstrated. For evaluation of effectiveness and validity of new antiarrhythmic substances intraindividual comparison with placebo and well established standard antiarrhythmic drugs is advisable.

17-Ketosteroids↗
PubMed1980

[Combined use of propafenon and lidoflazine in chronic atrial fibrillation and flutter (author's transl)].

Forty-seven patients with chronic atrial fibrillation and (or) flutter in whom the clinical picture and the length of arrhythmia indicated that drug-mediated cardioversion should be tried were treated with a combination of lidoflazine and propafenon. The average daily dosage was 600 mg for propafenon and 180 mg for lidoflazine. Duration of treatment was limited to 8 days. Return to sinus rhythm was achieved in 34 patients. In comparison with monotherapy combined use of the drugs thus led to a clear-cut increase of the conversion rate. Dosage reduction of these differently acting substances decreases the risk of toxic side effects, particularly as both substances have different side effects which in part cancel each other out. It can be assumed that ventricular extrasystoles seen during treatment with lidoflazine as precursor of malignant tachycardia can be suppressed or eliminated by propafenon.

Atrial Fibrillation↗