[Effectiveness and pharmacological effect of a new non-steroid drug tosiben in the treatment of rheumatic diseases].
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Arthritis, Rheumatoid↗
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The pharmacological effects of conjugates of pharmacologically active amines to complex or simple carriers: a new class of drug.
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Amines↗
Pharmacological effects of labetalol in man.
1 The pharmacological effects of labetalol have been studied in normal healthy subjects. The results of these studies are reviewed. 2 In the evaluation of the beta-adrenoreceptor-blocking effects of labetalol various indices of beta-adrenoceptor blockade in man were used. Labetalol administered orally and intravenously competitively antagonized the effects of isoprenaline on heart rate and diastolic blood pressure. The beta-adrenoceptor blockade induced was regarded as 'non-selective'. In addition, labetalol produced dose-related inhibitory effects on exercise-induced increases in heart rate any systolic blood pressure and similar dose-related inhibitory effects on the tachycardia induced by valsalva's manoeuvre. Labetalol had only a modest inhibitory effect on the tachycardia induced by tilting since blood pressure was reduced on a dose-related basis. 3 Labetalol was a specific competitive antagonist of the alpha-adrenoceptor agonist effects of systemically administered phenylephrine and locally infused noradrenaline. In addition, oral and intravenous administration of labetalol reduced systolic and diastolic blood pressure in the supine, standing and sitting positions. 4 The onset and duration of the alpha- and beta-antagonist effects of oral labetalol did not seem to be dissociated in time and there was a close correlation between the change in plasma concentration and pharmacological effects. 5 In comparative studies with propranolol, similar beta-antagonist effects were observed but propranolol was 4-6 times more potent weight for weight. Precise comparison, however, was complicated by the combined alpha- and beta -effects of labetalol, especially as the predominant effect of labetalol in normotensive subjects was to reduce blood pressure; whereas the predominant effect of propranolol was to reduce heart rate. In addition propranolol had inhibitory effects on ventilatory function in normal subjects, whereas labetalol in equivalent beta-adrenoreceptor-blocking doses did not. 6 From the details of the studies reviewed it was concluded that in man labetalol possesses combined alpha- and beta-adrenoreceptor antagonist properties.
Adrenergic alpha-Antagonists↗
[Pharmacological studies of Shikon and Tooki. (2) Pharmacological effects of the pigment components, Shikonin and acetylshikonin].
Pharmacological effects of Shikonin and Acetylshikonin, pigment components of Shikon were studied in mice, rats, guinea pigs and rabbits. The only difference between the chemical structures of the two pigments is that Acetylshikonin has the acetyl radical, while Shikonin does not. Though the activity was slightly different between the two compounds, the pharmacological effect of Shikonin was similar to that of Acetylshikonin. As the two pigments were extracted by ether from Shikon, systemic administration of these pigments showed the same effect as that of ether extract of Shikon as outlined in the first report(1). These compounds had no effect on blood coagulation, but inhibited the anticoagulant effect of heparin in rats. Topical application of both pigments (50 mg of 0.1% ointment) inhibited an increased vascular permeability and acute edema induced by histamine, anti-rat rabbit serum and heat. The activity was similar to that of 0.1% phenylbutazone ointment. On the other hand, these pigments increased proliferation of granuloma tissue in the cotton pellet method and promoted would healing in rats. The results suggest that Shiunko, a main prescription of Shikon, is an effective ointment for cutaneous injuries.
Analgesics↗
Disopyramide serum and pharmacologic effect kinetics applied to the assessment of bioavailability.
1 Serum, urine and pharmacologic effect (prolongation of the QT interval) kinetics of the antiarrhythmic disopyramide have been investigated in eight volunteers after intravenous administration (2 mg/kg) and oral administration (300 mg) of the two commercially available preparations, Rythmodan (Roussel Laboratories) and Norpace (Searle Laboratories). 2 An open one compartment body model adequately described the kinetics of disopyramide in serum and urine. 3 After intravenous administration, the following average pharmacokinetic parameters were found: biological half-life, 7.8 h; total clearance, 95 ml/min; renal clearance, 54 ml/min; apparent volume of distribution, 60 litres. 4 After oral Rythmodan and Norpace, serum concentration profiles and urinary excretion data revealed significant differences in rates of absorption, times required to achieve peak serum concentrations and biological half-lives. These differences were largely due to the relatively slow absorption characteristics of Norpace. 5 The absence of hysteresis in plots of QT prolongation against disopyramide serum concentration after oral administration indicated that serum and pharmacologic effect kinetics were indistinguishable within a kinetically equivalent compartment. 6 Analysis of both serum and urine data showed that while Norpace had a significantly higher degree of bioavailability (P less than 0.005), the 5--15% difference between the two formulations should not normally be of any clinical significance.
Administration, Oral↗
Relationship between plasma concentrations and pharmacological effects of labetalol.
In healthy normal subjects following the administration of labetalol the pharmacological effects were measured and compared with the plasma concentrations achieved. The inhibition of exercise induced tachycardia and inhibition of exercise induced increases in systolic pressure were significantly related to the administered dose of labetalol. Labetalol was rapidly absorbed from the gastrointestinal tract and peak plasma concentrations occurred two hours after oral administration. There was a linear correlation (r = 0.84) between the logarithm of the plasma concentration and the maximum inhibition of exercise tachycardia at two hours. After intravenous administration there was an immediate reduction in systolic and diastolic blood pressure with a concomitant small increase in heart rate. There was a rapid decline in the associated plasma concentration but the pharmacological effects were maintained in excess of two hours. Our findings are consistent with those of others who have studied the relationship between pharmacological events and plasma concentrations after single doses of other adrenoceptor blocking drugs.
Administration, Oral↗
Multiple receptor responses: a new concept to describe the relationship between pharmacological effects and pharmacokinetics of a drug: studies on clonidine in the rat and cat.
The time course of an observed pharmacological effect is affected not only by the kinetics of the drug levels at the site of action but also by parameters such as the slope and maximum effect of the functional relationship between drug level and response. Using clonidine as a test drug, it was found that the kinetics of its effects on blood pressure and pain responses cannot be described by the time course of clonidine levels in the blood, brain, or the hypothetical tissue compartment of the two-compartment characteristics of this drug. However, the results can be explained assuming that the observed pharmacological effects of a drug are composed of the sum of responses from at least two receptor sites with different slopes and maximal effects. The effect of intravenously administered clonidine on blood pressure in the rat was found to be related to the blood concentrations at least at two receptor sites with opposite effects, one leading to a hypertensive and the other to a hypotensive response. Predictions indicate that a maximum decrease of arterial blood pressure is obtained when the steady-state blood concentration of clonidine is about 1 ng/ml and that no effect is seen at 10 ng/ml. Higher levels will produce an increase of the pressure. The kinetics of the analgesic effect of clonidine in the rat could best be related to the brain levels if the observed effect was considered to be derived from the sum of activity at two receptor sites each producing analgesia. The kinetics of the effects of clonidine on the nictitating membrane of the cat was found to be determined by the kinetics of the drug in the peripheral compartment of the two-compartment open model. Consideration of multiple receptor responses is suggested for future studies on the relationship between the kinetics of drug levels and pharmacological responses.
Animals↗
The pharmacologic effects of furosemide therapy in the low-birth-weight infant.
The pharmacologic effects of furosemide were studied in six infants (mean gestation 30.7 weeks; mean birth weight 1,490 gm) at ages 10 to 57 days. Furosemide (for clinical indication, standardized at 1 mg/kg) was given intravenously over one minute; data were collected over the ensuing 24 hours. For three hours following furosemide administration, a significant diuresis was observed. Sodium excretion, percent fractional sodium excretion, and potassium excretion were significantly increased and urinary pH significantly decreased for six hours following the administration of furosemide. Creatinine and free water clearances were slightly elevated, although not significantly. Furosemide is an effective diuretic, the onset of pharmacologic action was within one hour, the peak action was sustained for three hours, and the duration of action was six hours. The net fluid, sodium, and potassium losses following a 1 mg/kg single dose were 28 ml, and 3.6 and 0.3 mEq/kg, respectively.
Furosemide↗
Pharmacological effects of phosphatidylserine liposomes: the role of lysophosphatidylserine.
1. Unique among the phospholipids, phosphatidylserine depresses brain energy metabolism when injected intravenously into mice in the form of sonicated liposomes. The possibility that this effect results from a metabolic transformation of phosphatidylserine is examined in this paper. 2. A strong enhancement of the phosphatidylserine effect is induced by the incubation of liposomes with rat serum. Similar phosphatidylserine activation is observed after the incubation of the phospholipid with purified phospholipase A2 from pancreas. In both cases phosphatidylserine is split into the deacylated derivative, lysophosphatidylserine. 3. Lysophosphatidylserine reproduces with greater efficacy the effect of phosphatidylserine on brain energy metabolism. Other lysophospholipids are not effective. 4. It is concluded that the pharmacological effects of phosphatidylserine liposomes is due to the generation of lysophosphatidylserine.
Animals↗
[Pharmacological effects of dobutamine and several catecholamines on various smooth muscles (author's transl)].
Pharmacological effects of dobutamine (DOB), a positive inotropic drug, on smooth muscles were compared with those of catecholamines such as norepinephrine (NE), epinephrine (E), isoproterenol (ISO) and dopamine (DA). DOB acted as a partial agonist and simultaneously as an antagonist on alpha-adrenergic receptors in the thoracic artery. Large doses of DOB induced uterine contraction in rabbits, but antagonised the contraction of the vas deferens of guinea pigs, as was induced by electrical stimulation. However, DOB showed a potent activity, similar to that seen with NE or E as an alpha-adrenergic agonist, on the portal vein. Doses of DOB required to produce a relaxation in the trachea of guinea pigs both in vitro and in vivo were 1/250 and 1/600 of ISO, respectively, and were considerably less regarding inhibition of uterine motility in rats. Inhibiting activity of DOB on the transport rate of intestinal contents in mice and gastro-intestinal motility of rabbits was much less than the activity seen with ISO, E and NE. Spasmolytic activity of DOB was also less than that of ISO, NE and E, but was more than that of DA. It is concluded that DOB is a more selective beta 1-agonist than ISO because of its weaker activity on alpha- and beta 2-receptors. The alpha-agonist activity of DOB in the portal vein was however, potent.
Animals↗
Major pharmacological effects of 6-methoxytetrahydro-beta-carboline, a drug elevating the tissue 5-hydroxytryptamine level.
Major pharmacological effects of 6-methoxy-1,2,3,4-tetrahydro-beta-carboline (6-methoxytryptoline, 6-MeOTHBC) are described. It seemed to have a weak effect of its own on 5-HT-receptors. It is concluded that most of the effects, like the increase of rectal temperature after peripheral administration and decrease and then increase after intrahypothalamic application as well as the antagonism of the group toxicity of amphetamine without effect on norepinephrine toxicity or barbiturate sleeping time, can result from the increase of tissue 5-HT-concentration and/or inhibition of 5-HT-uptake.
Acute Disease↗
[Experimental gingivitis as a model for the testing of the pharmacological effect in anti-inflammatory treatment of the gingiva].
This is a report concerning the feasibility of using gingivitis caused by neglect of usual oral hygiene for testing the pharmacological effects of anti-inflammatory agents. An unexpected difficulty is presented by the inability to reproduce the height of increase of the SB-index during repetition of the experiment after interruption of oral hygiene for one week.
Adult↗
Pharmacological effects of the giant African snail Achatina fulica.
The body fluid and tissue extract of the foot of Achatina fulica, the edible giant African snail, were investigated and quantified for pharmacological effects. Both reduced spontaneous locomotor activity in mice, protected them from death from amphetamine induced toxicity, prolonged hexobarbitone sleeping time and caused a depletion of catecholamines from various organs of the rat. From this a central depressant action combined with an antihypertensive effect is inferred. This is in keeping with the objectives of local traditional healers who use the snail on their patients. It is suggested that eledoison, a potent antihypotensive agent found in aquatic snails may also be present in terrestrial snails such as Achatina.
Animals↗
Pharmacokinetics and pharmacological effects of neostigmine in man.
1 The pharmacokinetics of neostigmine was studied in six patients during the reversal of neuromuscular block induced by tubocurarine chloride. The effect of the drug on neuromuscular function was simultaneously assessed by electromyography. 2 Neostigmine was rapidly eliminated from plasma after intravenous administration. The decline in the plasma concentration of the drug was invariably resolved into two exponential components. The fast disposition (distribution) half-life of the drug was invariably less than 1 min; the slow disposition (elimination) half-life ranged from 15.4--31.7 min. 3 Neostigmine usually increased the amplitude of the compound muscle action potential and diminished electromyographic decrement within 2 min of intravenous injection. The pharmacological effect of neostigmine was usually maximal between 7 and 15 min. There was an inverse relationship between the plasma concentration of the drug and the facilitation of neuromuscular transmission. 4 Red cell acetylcholinesterase activity was almost completely inhibited within 2--3 min of intravenous injection of neostigmine. Enzyme activity recovered to approximately 28% of control values by 30 min and to 55% by 60 min.
Acetylcholinesterase↗
Comparison of the pharmacological effects of epinephrine administered by the intravenous and endotracheal routes.
Epinephrine in various dosages was administered to anesthetized dogs by intravenous and endotracheal routes. Both methods produced measurable effects on heart rate, blood pressure, and respiration. Tachycardia occurred more rapidly after endotracheal administration than after intravenous administration. Respiration appeared to be supported more advantageously with the larger endotracheal dosages. The maximum blood pressure rise was delayed only 60 seconds by the endotracheal route. With an endotracheally administered dose of ten times the intravenous dose, equal responses in blood pressure were obtained. However, when equal doses are compared, there is only a two to three fold increase with the intravenous route. The endotracheal route may be less toxic at higher doses, affording greater safety when large amounts of epinephrine are used. It is concluded that endotracheally administered epinephrine produces significant pharmacologic effects in anesthetized dogs.
Animals↗
[Some pharmacologic effects of the "Styrax pill for coronary disease" and the pharmacological basis of a simplified styrax-borneol preparation (author's transl)].
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Animals↗
[Biological and pharmacological effects of carrageenan (author's transl)].
Carrageenan is sulfated polysaccharide which has been extensively used as emulsifier and thickening agent in the food industry, for its ability to induce acute inflammation in pharmacology and for its selectively toxic effect for macrophages in immunology. Carrageenan is a complex substance which displays various biological properties. The authors have shown the extent of these actions and reviewed the latest investigations on this subject.
Animals↗
Correlations between hydrophobicity and non-specific pharmacological effects of beta-adrenoceptor blocking agents.
It was the aim of this study to test whether the non-specific pharmacological activities of the beta-adrenergic blocking drugs can be predicted by estimation of the hydrophobicity of the compounds. Srong correlations were obtained between the octanol buffer partition coefficients and the ability of the drugs to decrease conduction velocity of the isolated frog heart, to raise the electrically induced ventricular fibrillation threshold in guinea pigs, and to depress ventricular contractility in the cat. The strong correlations between the partition coefficients and the pharmacological actions suggest that estimation of the hydrophobicity of the beta-adrenergic blocking drugs is suitable to predict the non-specific pharmacological properties.
Adrenergic beta-Antagonists↗