Arzneimittel Forsch
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Arzneimittel Forsch · Feb 1993
Randomized Controlled Trial Clinical Trial[The effect of molecular structure of hydroxyethyl starch on the elimination kinetics and fluidity of blood in human volunteers].
Influence of the Molecular Structure of Hydroxyethyl Starch on Elimination Kinetics and Blood Fluidity in Voluntary Subjects In a cross-over study 6 volunteers received an infusion of 500 ml hydroxyethyl starch of a batch with a high C2/C6-substitution ratio (10.8), or after a washout period of 3 months they received a batch with a low C2/C6-substitution ratio (5.8). The infusion solution was administered at random. The batches were identical as regards their physicochemical characteristics (HES 200/0.5 10%). ⋯ While the haematocrit decrease occurring 1 h after end of infusion is comparable, it keeps up for a longer time in case of a higher C2/C6-substitution ratio. The increase of plasma viscosity is more pronounced in case of a high C2/C6-substitution ratio. Clinical consequences are discussed.
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Arzneimittel Forsch · Sep 1991
General pharmacology of the novel angiotensin converting enzyme inhibitor benazepril hydrochloride. Effects on cardiovascular, visceral and renal functions and on hemodynamics.
The effects of benazepril hydrochloride (CGS 14824 A, CAS 86541-74-4), a novel angiotensin I converting enzyme inhibitor, on cardiovascular, visceral and renal functions and on hemodynamics, were studied in various experimental animals. Even at a high dose of 100 mg/kg p.o. benazepirl hydrochloride had no influence on the respiration, heart rate and ECG of normotensive anesthetized cats and, except at higher doses, had little effect on the contractile tension of mammalian isolated atrium, ileum, trachea, stomach fundus strips, vas deferens or uterus. Benazepril hydrochloride even at a high dose of 100 mg/kg p.o. had little effect on spontaneous uterine motility, charcoal transportation and gastrointestinal tract motility. ⋯ At a dose of 3 or 10 mg/kg.day p.o. for 4 weeks benazepril hydrochloride inhibited the increase in the excretion of urinary protein in DOCA/salt spontaneously hypertensive rats. It caused hemolysis at concentrations as high as 0.1-1% in rabbits, however, even at a high dose of 100 mg/kg p.o. it did not affect red blood cell fragility in rats, and, except at a high dose of 10(-4) g/ml, showed little effect on the platelet aggregation response induced by collagen or arachidonic acid in rabbits. From these results, benazepril hydrochloride is considered to be a safe and well-tolerated addition to the therapeutic armamentarium of cardiovascular drugs.
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Arzneimittel Forsch · Jun 1990
Pupillometry and radioreceptor binding. Semeiologic suggestions in the evaluation of the treatment with anticholinergic drugs.
In this study, a dynamic TV pupillometric system has been used to record the effects of the anticholinergic drug biperidene (Akineton) on pupil responsiveness to various types of stimuli. Plasma levels of the drug were evaluated by means of the radioreceptor binding technique at the same times of pupillometric monitoring. An excellent correlation was found between the effects of biperidene on pupil diameter after light and dark adaptation, light reflex and near vision reaction and the plasma levels of the drug. Radioreceptor binding and dynamic TV pupillometry represent useful tools to evaluate the possible alterations induced by drug therapy on the cholinergic system in man.
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Arzneimittel Forsch · Jun 1989
Influence of carbohydrates on the cytotoxicity of an aqueous mistletoe drug and of purified mistletoe lectins tested on human T-leukemia cells.
Partially and highly purified lectins from Viscum album L. (mistletoe) cause a dose-dependent decrease of viability of human leukemia cell cultures, MOLT-4, after 72 h treatment. The LC50 of the partially purified lectin was 27.8 ng/ml, of the highly purified lectin 1.3 ng/ml. Compared to the highly purified lectin a 140-fold higher protein concentration of an aqueous mistletoe drug was required to obtain similar cytotoxic effects on MOLT-4 cells. ⋯ The lectin fractions and the mistletoe drug inhibited protein synthesis of MOLT-4 cells stronger than DNA synthesis. Furthermore a subpopulation of MOLT-4, resistant to cytotoxic doses of both the mistletoe drug and the mistletoe lectins, was shown to exhibit a reduced amount of GalNAc and N-acetyl-D-glucosamine in their cellular glycoproteins which are probably responsible for the binding of the cytotoxic lectins. These results indicate that lectins are the main toxins in the mistletoe drug.
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Arzneimittel Forsch · Mar 1987
Randomized Controlled Trial Clinical TrialContinuous-plus-on-demand epidural infusion of buprenorphine versus morphine in postoperative treatment of pain. Postoperative epidural infusion of buprenorphine.
In a randomized, double-blind study, buprenorphine was compared with morphine in the treatment of pain after major abdominal operations by means of continuous-plus-on-demand epidural infusion for constant analgesia. The patients received bolus epidural injections of 0.15 mg buprenorphine or 2 mg morphine-HCl prior to an on-demand epidural infusion of 0.03% buprenorphine or 0.25% morphine HCl at a basal rate of 0.06 ml/h. ⋯ Under the treatment, no discomfort or side-effects necessitating treatment occurred. We conclude that buprenorphine is a useful substitute for morphine in the treatment of pain after major abdominal operations by continuous-plus-on-demand epidural infusion, and that the relative analgesic potency ratio of epidural buprenorphine is 8.