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Biomedical subjects

G Weidinger

Publications and source records attributed to G Weidinger.

At least 73 records · Page 4Linked to original sources
PubMed1994

[Treatment of essential hypertension with the alpha-1 antagonist bunazosin retard. A multicenter, double-blind, placebo-controlled study].

In a randomised, placebo-controlled design 40 patients with moderately severe essential hypertension were treated with bunazosin (CAS 52712-76-2) retard in increasing doses ranging between 6 and 18 mg/day. In intervals of 14 days titration steps were made, the minimal period of treatment was 4 weeks. In 34 patients (80.6%) a blood pressure response could be achieved with Bunazosin retard alone, the rest of the patients needed the additional administration of 25 mg hydrochlorothiazide daily. In all actively treated patients diastolic blood pressure could be normalised (DBP < or = 90 mmHg). After 4 weeks the mean blood pressure was lowered in the Bunazosin group by 16.2 mmHg (diastolic) and 25 mmHg (systolic). The mean heart rate at rest remained almost constant. Bunazosin was generally well tolerated; only very few adverse events occurred, and no patient collapsed. Compared to placebo the orthostatic tolerance was not influenced by bunazosin retard. Only when changing from resting to standing position the rise in heart rate was slightly more pronounced under bunazosin. Also the physiological blood pressure profile under bunazosin remained unchanged during the orthostatic tests.

Adrenergic alpha-1 Receptor Antagonists↗
PubMed1994

Single daily administration of spirapril in the treatment of essential hypertension. A multicentre double-blind comparison of 1, 6, 12 and 24 mg of spirapril once daily.

A total of 171 male and female patients with mild-to-moderate hypertension [diastolic blood pressure (DBP) 100-115 mmHg] entered this randomized, double-blind, multicentre study. A 3-week placebo run-in period was followed by a 5-week active-treatment period during which patients received either 1, 6, 12 or 24 mg of spirpril once daily. Predose sitting blood pressure was taken in the morning by sphygmomanometer as well as by an automatic device (Tonoprint). Spirapril in doses of 6, 12 or 24 mg once daily significantly and similarly lowered systolic blood pressure (SBP) and DBP compared with 1 mg once daily. The rates of blood pressure normalization (DBP < or = 90 mmHg) were 12.5%, 37.5%, 30.8% and 28.9% with 1, 6, 12 and 24 mg, respectively. The percentage of patients experiencing a DBP reduction of at least 10 mmHg was 25.0%, 56.3%, 48.7% and 52.6% and 1, 6, 12 and 24 mg of spirapril, respectively. No serious or severe adverse events related or uncertain if related to the study medication were observed. The effective 6-mg dose was as well tolerated as the inefficacious 1-mg dose. In conclusion, in patients with mild-to-moderate essential hypertension, 6 mg of spirapril once daily is an efficacious and safe antihypertensive therapy with a favourable benefit-risk profile.

Adult↗
PubMed1994

Pharmacokinetics of spirapril and spiraprilat in patients with chronic renal failure.

In this single-blind trial with a 2-week placebo run-in followed by a 4-week active-treatment period, patients were given 6 mg of spirapril once daily. Forty-nine hypertensive men and women were recruited; all had pretreatment diastolic blood pressures (DBP) of 95-115 mmHg with varying degrees of renal impairment. Regression analysis of pharmacokinetic parameters C(max)ss (the maximum steady-state drug concentration in plasma during a dosing interval), Cl/f (total plasma clearance) and k (elimination rate constant) of spirapril on creatinine clearance (Clcr) showed that the pharmacokinetics of spirapril were not significantly influenced by the degree of renal impairment. C(max)ss values of spiraprilat, however, increased with decreasing Clcr, and AUC(l)ss (area under the concentration-time curve during a dosing interval) values also increased. Regression analysis of the pharmacokinetic parameters C(max)ss, Clm/fm (total plasma clearance) and lambda 1 (rate constant of the first disposition phase) of spiraprilat on Clcr showed that Clm/fm as well as lambda 1 were linearly correlated with Clcr (p < 0.01). However, the results indicate that, even when renal elimination is completely blocked, there is significant elimination of spiraprilat through a non-renal pathway. In conclusion, the risk of drug accumulation after multiple dosing is minimal as the presence of a substantial non-renal spiraprilat elimination was consistently demonstrated.

Adult↗
PubMed1991

[Therapy comparison between the combination hydergine/nifedipine and nifedipine alone in patients with isolated systolic hypertension].

The effect of Hydergine/Nifedipine (Pontuc) on blood pressure in supine or exercise blood pressure as well as subjective well-being was evaluated in a randomized, double-blind interindividual comparison with Nifedipine in 50 elderly out-patients (34 females, 16 males) with mostly pretreated isolated systolic hypertension. In addition to a nearly unchanged diastolic blood pressure during treatment the results prove that the drop in systolic blood pressure was statistically significant greater after treatment with Hydergine/Nifedipine and the normalization rate of the blood pressure was 81% in comparison to 69% after Nifedipine. Both drugs comparatively improved the subjective well-being of these geriatric patients. As drug specific adverse events flush symptoms were more frequent in the Nifedipine group, whereas in the Hydergine/Nifedipine group gastrointestinal symptoms occurred more often.

Aged↗
PubMed1990

Co-dergocrine mesylate inhibits the increase in plasma catecholamines caused by nifedipine in essential hypertension.

Co-dergocrine mesylate (Cod), which inhibits norepinephrine secretion by stimulating presynaptic dopamine receptors, and has no known metabolic side effect, has an additive antihypertensive effect to that of Nifedipine (Nif). Plasma norepinephrine, epinephrine, renin activity and aldosterone have been measured after acute administration of Nif and Cod alone and in combination to 18 patients with a diastolic blood pressure greater than 105 mmHg in a cross-over, randomized, double-blind study. Every patient received 4 mg Cod then 20 mg Nif, placebo then 20 mg Nif and 4 mg Cod then placebo. The second treatment was always given 1 h after the first medication. Blood pressure was measured before and every 15 min during the study period. Blood for measurement of catecholamines, aldosterone and renin activity was collected before medication, 1 h after the first dose and 90 min after the second treatment. Blood pressure was significantly lower (P less than 0.05) where Cod preceded Nif. Cod caused a significant decrease in plasma norepinephrine from 293 to 202 pg.ml-1 and in epinephrine from 67 to 55 pg.ml-1. The Nif-induced increase in norepinephrine from a pre-treatment value of 293 pg.ml-1 with preceding Cod to 331 pg.ml-1 was much less than the increase with placebo as premedication, from 284 to 440 pg.ml-1. Nif caused an increase in renin activity but no increase in aldosterone. Nif-related side effects, such as flushing and headache, occurred in 6 patients of whom 5 had no received Cod as premedication.(ABSTRACT TRUNCATED AT 250 WORDS)

Aldosterone↗
PubMed1990

Efficacy and tolerability of the new calcium antagonist isradipine in essential hypertension.

The antihypertensive efficacy and tolerability of the new calcium antagonist isradipine was assessed in 86 hypertensive patients who had pretreatment diastolic blood pressures (DBP) greater than or equal to 105 mm Hg and who were randomly allocated to a double-blind comparison of three different dosage regimens: 1.25 mg, 2.5 mg, and 5 mg b.i.d., and placebo. A 2-week run-in period was followed by a 4-week course of treatment. Isradipine reduced systolic and diastolic blood pressures dose-dependently; the normalization rate (DBP less than or equal to 90 mm Hg) was 5% with placebo and 29, 55, and 64% with isradipine 1.25, 2.5, and 5 mg b.i.d., respectively. The proportion of patients experiencing at least a 10 mm Hg reduction in sitting DBP was 29, 67, 86, and 91%, respectively. All three dosages proved to be significantly effective compared to placebo. Neither heart rate nor blood pressure regulation in orthostasis were influenced. The main side effects were headache, dizziness, and flushing; isradipine 1.25 and 2.5 mg b.i.d. were well tolerated (not significantly different from placebo). In conclusion, isradipine 2.5 mg b.i.d. appears to be the potential dose of first choice, exhibiting a favorable benefit-risk profile.

Blood Pressure↗
PubMed1990

Calcium antagonists as first-line antihypertensive agents: a placebo-controlled, comparative trial of isradipine and nifedipine.

The new calcium antagonist isradipine was compared with nifedipine retard in a multicenter, double-blind, placebo-controlled, randomized study involving 159 patients with mild hypertension. A 2-week run-in period was followed by a 6-week course of treatment with the possibility of dose doubling after 3 weeks, depending on blood pressure (BP) response (target diastolic BP less than 90 mm Hg). Systolic and diastolic BPs were reduced by isradipine (mean dose of 3.6 mg daily) from 151/101 to 136/89 mm Hg, by nifedipine (mean dose of 50 mg daily) from 155/101 to 144/90 mm Hg, and by placebo from 155/101 to 154/99 mm Hg. Normalization rates were 64% with isradipine, 56% with nifedipine, and 16% with placebo. Adverse events consisted mainly of flushing, headache, edema, and dizziness. Altogether, 8 patients receiving isradipine experienced adverse events in comparison to 21 taking nifedipine and 4 taking placebo. The superior tolerability of isradipine was paralleled by a significant improvement in the subjective well-being of the patients as assessed by the von Zerssen questionnaire (List of Complaints). With nifedipine and placebo, no statistically significant improvement was observed.

Blood Pressure↗
PubMed1989

The antimycotic drug terbinafine in contrast to ketoconazole lacks acute effects on the pituitary-testicular function of healthy men: a placebo-controlled double-blind trial.

Among the side-effects of the antimycotic drug ketoconazole, inhibition of testosterone biosynthesis is highly pronounced. The decrease in testosterone may cause impotence and gynecomastia, and this side-effect has been exploited in drug tests for the treatment of androgen-dependent tumours. Terbinafine, an allylamine derivate, from a new group of antifungal substances, did not show similar inhibiting effects on steroid synthesis in vitro and in vivo in animal experiments. In a double-blind, placebo-controlled study the influence of terbinafine and ketoconazole on the pituitary-testicular axis in normal young men were compared. Serial blood sampling for 12 h was followed by the ingestion of the placebo, ketoconazole (200 mg) or terbinafine (500 mg) on three different occassions in random order. Ketoconazole administration caused a steep decrease of serum testosterone reaching a nadir after 4-5 h. Simultaneously an increase in 17-hydroxyprogesterone occurred with peak values after 5 h. During 12 h after the administration of ketoconazole no changes in LH pulse frequency and amplitude were found, although testosterone serum levels were in the subnormal range for about 8-9 h. Terbinafine showed no effects on testosterone and 17-hydroxyprogesterone levels or on LH pulse frequency and amplitude. Estradiol, prolactin and FSH remained unchanged after ketoconazole and terbinafine ingestion compared with placebo treatment. The study confirms the acute effect of ketoconazole on serum testosterone and 17-hydroxyprogesterone, whereas terbinafine shows no acute influence on the pituitary-gonadal axis.

17-alpha-Hydroxyprogesterone↗
PubMed1987

E. coli maltodextrin phosphorylase: primary structure and deletion mapping of the C-terminal site.

The complete 796 residue amino acid sequence of maltodextrin phosphorylase was deduced from the E. coli malP nucleotide sequence. The calculated molecular weight of 90,500, including pyridoxal phosphate, is significantly larger than experimentally determined values. Enzymatically active and inactive mutants following deletion or exchange of up to 8 codons (7 amino acids) at the 3' end (C-terminus) confirm the size of the mature native enzyme and disclose the essential functional or structural role of the highly conserved C-terminal region of phosphorylases.

Amino Acid Sequence↗
PubMed1984

[The antifungal agent naftifin. Placebo-controlled therapeutic comparison in tinea pedis].

The antimycotic efficacy of Naftifine was compared with that of placebo in a double-blind randomized trial in 60 patients with Tinea pedum proved by culture and microscopic examination. Naftifine was significantly superior to placebo concerning the number of mycologically cured patients as well as the clinical response to therapy. At the end of the study all patients were cured by Naftifine, whereas no patient of the placebo group showed an improvement.

Administration, Topical↗
PubMed1984

[Central hemodynamics of antihypertensive agents. Studies on co-dergocrinmesylate].

The haemodynamic effects of a three-week-treatment with 4-8 mg co-dergocrinmesylate (Hydergin spezial) were investigated in 14 hypertensive patients with a mean age of 58 years and reduced ventricular function (exertional dyspnoea, enlarged cardiac opacity). Blood pressure values at rest and during physical exercise were reduced significantly. Marked cardiac relief was induced manifesting as decrease of enddiastolic and endsystolic volumes and at the same time as an increase of ejection fraction. Cardiac output remained largely constant, lowering of blood pressure was exclusively due to alteration of peripheral total vascular resistance. Cardiac frequency decreased significantly. There was no evidence of negative inotropic effects. Systolic wall tension as the main therapeutic target decreased at rest and during ergometry by 20% and 25%, respectively. Renal perfusion increased slightly, but significantly, in all patients.

Aged↗
PubMed1983

Cloning and expression in Escherichia coli and Bacillus subtilis of the hemolysin (cereolysin) determinant from Bacillus cereus.

From a cosmid gene bank of Bacillus cereus GP4 in Escherichia coli we isolated clones which, after several days of incubation, formed hemolysis zones on erythrocyte agar plates. These clones contained recombinant cosmids with B. cereus DNA insertions of varying lengths which shared some common restriction fragments. The smallest insertion was recloned as a PstI fragment into pJKK3-1, a shuttle vector which replicates in Bacillus subtilis and E. coli. When this recombinant plasmid (pJKK3-1 hly-1) was transformed into E. coli, it caused hemolysis on erythrocyte agar plates, but in liquid assays no external or internal hemolytic activity could be detected with the E. coli transformants. B. subtilis carrying the same plasmid exhibited hemolytic activity at levels comparable to those of the B. cereus donor strain. The hemolysin produced in B. subtilis seemed to be indistinguishable from cereolysin in its sensitivity to cholesterol, activation by dithiothreitol, and inactivation by antibodies raised against cereolysin. When the recombinant DNA carrying the cereolysin gene was used as a probe in hybridization experiments with chromosomal DNA from a streptolysin O-producing strain of Streptococcus pyogenes or from listeriolysin-producing strains of Listeria monocytogenes, no positive hybridization signals were obtained. These data suggest that the genes for these three SH-activated cytolysins do not have extended sequence homology.

Bacillus cereus↗
PubMed1983

[Effect of co-dergocrine mesylate on catecholamines and prolactin in elderly hypertensive patients].

The antihypertensive efficacy of co-dergocrine mesylate (a mixture of dihydroergocornine mesylate, dihydroergocristine mesylate, and alpha- and beta-dihydroergocryptine mesylates; Hydergin) and its effects on heart rate, plasma catecholamines, catecholamine excretion and plasma prolactin was tested in 12 elderly hypertensive patients. Co-dergocrine mesylate (6 mg or 12 mg, 1 or 2 tablets once a day) caused a significant reduction of the blood pressure during rest and under physical stress without a reactive increase of the heart rate. Plasma norepinephrine and prolactin as well as urinary excretion of norepinephrine and epinephrine were not affected by co-dergocrine mesylate. The therapeutic advantage of co-dergocrine mesylate for the treatment of hypertension in the elderly is discussed.

Aged↗