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PubMedDate not supplied

[Asarone and its biological properties].

In acute and chronic experiments on mice, rats, cats and rabbits in a wide range of tests, a study was conducted of the biological properties of alpha-asarone (1-propenyl-2,4,5- methoxybenzol)--etherophenol, isolated by the authors from the roots of Asarum europaeum. It was determined that the LD50 of asarone for mice in enteral administration was 417.6 mg/kg, in intra-abdominal--310 mg/kg. The preparation has quite diverse biological activity--tranquilizing, sedative, antiulcer, spasmolytic and antisclerosing. In its pharmacological properties the studied asarone is identical with asarone obtained from Acorus calamus and Guatteria.

Allylbenzene Derivatives↗

PubMed1979

[Spasm of the coronary arteries in acute myocardial infarct].

Emergency coronarography was performed in 36 patients with myocardial infarction. Spasms of the coronary artery supplying the area of the infarction were observed in some cases. The fact that the vessel was demonstrated along its entire length after 0.5 mg of nitroglycerine was placed under the tongue confirmed the existence of the spasm. In most patients with acute myocardial infarction the vessel supplying the area of the affected muscle has the appearance of a stump, i.e. its peripheral segments are not demonstrated. At the same time, in some patients, who died some time after the examination, anatomical study of the heart showed that these segments of the vessel were not occluded. Such an angiographic picture may also be explained by the spasm of the coronary arteries. The angiographic pattern of the coronary channel in patients with acute myocardial infarction suggests that coronarolytics and spasmolytics injected both intravenously and into the coronary vessel in coronarography may be used still more extensively.

Acute Disease↗

PubMed1979

[Pharmacological and toxicological study of turimycin].

Turimycin is characterised by low acute toxicity. Mean lethal doses for mouse and rat are 750 mg/kg body weight for intraperitoneal application of something in excess of 3,000 mg/kg for oral administration. The blood pressure of anaesthetised cats may be reduced by amounts depending on intravenous Turimycin doses (between 10 and 50 mg/kg). The hypotensive effect of Turimycin is attributable to its negative inotropic effect on the heart and its spasmolytic action on the unstriated muscles. Reversible reduction of urine and ion excretion of rat following intraperitoneal application of 50 mg/kg body weight of Turimycin is interpreted as a consequence of such action upon blood pressure. A preliminary study was conducted into dogs which had orally received daily Turimycin doses of 50 or 125 mg/kg body weight over twelve months. No substance-depending functional or morphological damage was recorded.

Animals↗

PubMed1979

[Rational combined X-ray examination of gallbladder and stomach (author's transl)].

X-ray examination of patients with upper abdominal symptoms has been performed up to now mostly as a sequence of separate procedures; instead, an integrated procedure is recommended: a plain film of the upper abdomen should be taken first; a routine oral cholecystogram in the lying position 12 hrs after intake of the contrast medium should be omitted-instead the gallbladder should be visualized fluoroscopically with the patient remaining in the standing position or lying, and films should be taken during visualization. X-ray examination of the stomach and duodenum may follow immediately thereupon, eventually as well during pharmacologically induced hypotony. Then a fatty meal may be given in order to stimulate contraction of the gallbladder; if spasmolytics have been given before, contraction however might be hampered. The diagnostic significance of fatty meals applied as a routine procedure in X-ray diagnosis of gallbladder function is considered to be limited; on the other hand this procedure may improve the diagnosis of the morphological situation.

Biliary Tract Diseases↗

PubMedDate not supplied

[Favorable effect of procaine administration in retrobulbar optic neuritis].

The author reports 12 cases of retrobulbar neuritis of recent onset in which intravenous procaine exerted unexpectedly an immediate favourable effect. The treatment consisted of intravenous drip infusion of 40 ml of 1% procaine in 400 ml of 5% glucose during 7 days. The author supposes that the therapeutic effect was due to the antiallgeric action of procaine (blocking of histaminergic receptors) and its spasmolytic influence.

Adolescent↗

PubMedDate not supplied

Antispasmodic activity of the tertiary base of Daucus carota, Linn. seeds.

A nitrogen containing base responding to Mayer's test and Dragendorff's reagent for tertiary bases has been isolated from the seeds of Daucus carota Linn. The effects of the base as its bromide have been studied on smooth muscles of ileum, uterus, blood vessels and trachea of different species of animals. The tertiary base has been found to have papaverine like nonspecific smooth muscle relaxant and spasmolytic activity, but its activity was found to be about one-tenth of that of papaverine.

Animals↗

PubMed1979

[Peripheral macro-and microcirculatory changes in acute arterial obstruction with papaverine and trental administration].

The effect of myotropic spasmolytic drugs--papaverine and trental was studied in 54 patients with acute arterial obstruction. After intravenous injections of papaverine 55.8% of the patients developed impairment of peripheral macrohemodynamics and 52.9%--of microcirculation. The injection of trental was followed by an improvement of peripheral macro-and microcirculation in 75% of cases.

Acute Disease↗

PubMed1979

Metabolism and kinetics of renal elimination of N-picolyl-3,5-dimethylbenzamides.

The metabolism and kinetics of renal elimination of N-(2-picolyl)-, N-(3-picolyl)- and N-(4-picolyl)-3,5-dimethylbenzamides were studied. These products have a depressive activity on the central nervous system, as well as an anti-inflammatory and spasmolytic activity. The elimination of the products N-(3-picolyl)- and N-(4-picolyl)-3,5-dimethylbenzamides includes a process of metabolic oxidization of the atom of pyridinic nitrogen with formation of the corresponding N-oxides as main products of its bio-transformation. The process of N-oxidization was not observed with the product N-(2-picolyl)-3,5-dimethyl-benzamide. The results showed that the renal elimination rate of the products studied is greater as the pyridinic nitrogen moves away from the amide group. In the biotransformation process of these products, there is an opposite effect, i.e., the formation of corresponding N-oxides is lower as the pyridinic nitrogen approaches the amide group.

Animals↗

PubMed1979

Pharmacological studies on new oncostatic acridine derivatives. I. Acute and subchronic action.

Preclinical pharmacological studies of two acridine derivatives, dihydrochloride N10-oxide 1-nitro-9-/3-dimethylaminopropylamino/-acridine (C-666) and dihydrochloride 1-nitro-9-[(2-dimethylamino)-1-methylethylamino]-acridine (C-829) are reported. Both compounds are characterized by biological activity, poor absorption from the gastrointestinal tract and local irritant action. Quality differences in an effect of both investigated acridine derivatives on the central nervous system were noted. C-666 proved to be deprived of the effect typical of the central component compounds while C-829 demonstrated mostly sedative activity. Clear dissociation in the effect of these both compounds was seen in in vitro experiments on isolated smooth muscle organs. C-666 acted spasmolytically on the motory action of intestine muscles while C-829 acted spastically. Both preparations had clearly hipotensic influence which can be due to the vascular effect and to their affinity with the intramyocardium transmitting system. Neither a distinctive effect on reproductivity of animals nor the teratogenic action were observed in the functional experiments.

Acridines↗

PubMed1979

[A successfully completed abdominal pregnancy].

The first pregnancy of a 22-year-old woman with somewhat more pronounced and prolonged symptoms of emersis gravidarum was followed up in the outpatient unit and was considered normal. The woman was admitted to the maternity ward 38 days before the term of labour because of painful abdominal cramps, vomiting and weakness. In the course of the first 17 days in hospital, the pregnancy was maintained by the use of spasmolytics but at that time it became clear on the basis of the symptoms, gynecological findings, and the gravidogram, that the case related to abdominal pregnancy. On the 18th day of hospitalization, laparotomy ws performed and a live, female, prematurely born baby, 2,450 g/45 cm, without any deformity, was delivered. The pregnancy was abdominal, with the nidation of the placenta at the right uterine horn. The placenta was completely removed. The girl is now 6 years old and her psychophysical development is normal, corresponding to her age.

Adult↗

PubMed1978

Antimotility and antisecretory activity of some aryl substituted amidinoureas.

A number of aryl substituted amidinoureas have been prepared and examined for their gastrointestinal spasmolytic, antimotility, antidiarrheal and antisecretory effects. In general, antisecretory and antimotility effects have been found to be associated with each other in these compounds. The structure-activity relationships found show that substitution of the aromatic ring in positions other than 2 and 6 correlates poorly with potency, and potency of such compounds is low. In contrast to this, 2,6-disubstitution confers high potency. The potency of 2,6-disubstituted compounds declines sharply with increasing weight of substitution of the amidinourea chain, with the important exception of the N-alkoxyamidinoureas. Increasing the molecular weight of an N-alkoxy substituent has a much less profound effect than the corresponding increase has in an N-alkyl substituent. High potency in an amidinourea may well be related to low basicity (or a high pKa value for its conjugate salt) but there is insufficient data to support this hypothesis fully. The actual tautomeric structure of an amidinourea probably affects its potency and this is discussed briefly.

Amidines↗

PubMed1979

[Pharmacological study on treptilamine in man/study on tolerability (author's transl)].

N,N-Diethyl-N-(2-[alpha(tricyclo[2,2,1,0(2,6]hept-3-ylidene)-benzyloxy]-ethyl)amine hydrochloride (treptilamine) which in experiments on animals showed distinct spasmolytic effects, has been investigated first in 6 volunteers with regard to compatibility using different doses p.o. and i.v. In connection with this previous study a double blind study including placebo was performed for verification of the observed effects. In the plot study 30, 40 and 50 mg were applied orally and 10, 15 and 20 mg treptilamine were used i.v. The double blind study was designed for 20 volunteers at dosages of 40 mg p.o. and 15 mg i.v. against placebo. In the pilot study systolic blood pressure decreased significantly 5 to 15 min after i.v. application of the substance for 5 or 30 min. The range of accommodation was restricted depending on the dose used. No alteration of circulation was observed after oral application at any dose. All volunteers felt tired. A significant decrease of systolic blood pressure (15 mmHg for 10 min immediately after application) occurred after 15 mg of substance were applied i.v. in the double blind study. No effect on circulation could be seen after placebo. The range of accommodation was restricted in a significant way both after i.v. application (40%) and after oral application (30%). Two of five volunteers recorded a burning sensation in the venous wall which was followed by drowsiness. One volunteer felt increasingly tired after oral application. No influence of the substance could be seen on the clinicochemical parameters examined.

Accommodation, Ocular↗

PubMedDate not supplied

[Pharmacological effects of the new psychotropic preparation, mebikar].

By its effects mebicar -- a derivative of bicyclic bis-ureas -- may be refered to psychotropic drugs occupying a middle position between tranquilizers and neuroleptics. The drug inhibits the orientation reaction in albino mice, potentiates the action of narcotic hypnotics, abolishes the conditioned reflex reaction of avoidance, displays central adrenolytic activity, interferes with the norepinephrine metabolism in the brain stem and modifies the permeability of the blood-encephalic barrier, like this is done by the known neuroleptics. The substance is little toxic, does not exert any direct spasmolytic action on the isolated organs.

Amphetamine↗

PubMed1984

[Adenosine-3',5'-monophosphate content and muscle tension in isolated coronary arteries under the effect of lanthanum ions].

According to experimental conditions lanthanum ions exert either relaxing or contracting actions on isolated bovine coronary arteries. Both the relaxing and the contracting effect were accompanied by an increase of the cAMP content. The enhancement of the cAMP level could be abolished by diisopropylfluorophosphate (DFP), an inhibitor of adenylate cyclase. The lanthanum-induced relaxation, however, was not influenced neither by DFP nor by the PDE-inhibitor methylisobutylxanthine. It is concluded that cAMP is not involved in the mechanism of La3+-induced relaxation. On La3+-contracted vessels isoprenaline, theophylline, papaverine and trapidil have a spasmolytic action that seems not to be mediated by cAMP.

1-Methyl-3-isobutylxanthine↗

PubMed1977

Synthesis and pharmacological testing on some theophylline esters.

Esters of theophylline-7-acetic acid with different amino alcohols were prepared as possible atropine substitutes, together with esters of some hydroxy acids with beta-hydroxyethyl theophylline. Moreover, esters possessing both theophyllinyl and piperazinyl moieties were prepared with the hope that their spasmolytic activity might be increased. Some of the prepared compounds proved to possess atropine-like activity.

Acetylcholine↗

PubMed1977

Pharmacological study of the activity of a group of piperizine esters and changes in action relative to their chemical structure.

A group of original symmetrical and asymmetrical piperazine compounds containing ester function have been synthesized and pharmacologically characterized. All compounds are pharmacologically active. Some relationships between their chemical structure and biological activity are discussed. Analgesic and coronary dilatory and especially spasmolytic effects are marked for all asymmetrical esters. A number of the compounds are interesting for further investigations relative to their possible application in medical practice.

Animals↗

PubMed1984

[Specific mechanism of action of calcium antagonists in the neutralization of experimental coronary spasms].

In vascular smooth muscle cells as in myocardial fibres, a transmembrane supply of Ca ions is required for activation of the contractile system. This is especially obvious in the vasculature of the great subepicardial coronary stem arteries which rapidly lose contractility upon extracellular Ca withdrawal. Consequently, in this special section of the coronary bed, even minute concentrations of calcium antagonists, by interference with transmembrane Ca++ influx, are capable of a spectacular suppression of contractile vascular smooth muscle performance. Moreover, in the extramural coronary vasculature - in contrast with most systemic arteries - the scope of the vasodilator and spasmolytic effects of calcium antagonists is particularly broad. This means that calcium antagonists produce a nearly uniform cessation of both tonic and phasic coronary responses regardless of whether different vasoconstrictors, receptors or pathways of Ca++ delivery are involved. Thus, our animal experiments as well as successful clinical trials highlight the outstanding efficacy of calcium antagonists in neutralizing all types of extramural coronary artery spasm. This action of calcium antagonists seems to be the predominant haemodynamic factor in relieving or preventing acute ischemic episodes especially in coronary heart disease with spastic components.

Acetylcholine↗

PubMed1983

What is preferable in unstable angina, beta-blockade or calcium-inhibition?

Nifedipine is a strong calcium antagonist; it blocks the excitation-contraction coupling, yet at therapeutic dosage levels it has few side effects. It is said that a single molecule of nifedipine can neutralize the effects of several thousand calcium ions in the excitation-process. Thus this agent reduces the ability of the cardiac cells to develop mechanical tension yet it does not affect electrical excitation. Calcium antagonists are also potent dilators, particularly of the arteries on the periphery of the human body and in the coronary arterial system. The basic mode of action is thought to be the same, i.e. reduction of the calcium transport, this time into the smooth muscle cells of the arterial wall, thus "forcing' the arteriole to dilate. The resultant action is a reduction in afterload, while there is an increase in perfusion of the coronary vascular bed. Thus there is a dual action, the one centrally, the other peripherally both of which will be particularly effective in patients with unstable angina (UA) in whom excess coronary vascular tone is suspected. Beta-blockers, particularly propranolol and metoprolol, with which we have the most experience, work via beta 2 adrenoceptor blockade in the heart. Cardiac frequency decreases, arrhythmias are suppressed, blood pressure may decrease, all reducing cardiac work. If in UA variations in coronary vascular tone and frank spasm do occur then is would be more logical to use Ca-antagonists instead of beta-blockade. Our clinical experience to date has not shown that patients with UA are worsened by propranolol or metoprolol but there are scores of clinical reports showing worsening of chest pain in Prinzmetal's syndrome, presumably because beta-blockade leads to excessive alpha-adrenergic vascular tone. On the other hand, in one year experience with 73 patients with UA, 52 did not experience relief from adequate beta-blockade until nifedipine was added. Within 2 hours, 42 of the 52 became asymptomatic--thus indicating that in UA the need for spasmolytic therapy prevails over the need for beta-blockade. In many cases of UA both drugs may have a place however, their exact relative value remains to be established.

Adrenergic beta-Antagonists↗