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PubMedDate not supplied

[Effect of the adrenaline, euphyllin, phentolamine and obzidan on serotonin bronchospasm in guinea pigs].

It has been shown in experiments on 81 guinea-pigs that variation of the functional status of alpha- and beta-adrenoreceptors produces a substantial effect on marked serotonin bronchospasm. The blockade of beta-adrenoreceptors with obsidan (1--2 mg/kg) increases the spasm of bronchial smooth muscles in response to serotonin (10 micrograms/kg). The alpha-adrenolytic phentolamine (2 mg/kg) and the myotropic spasmolytic euphylline (8 mg/kg) remove the hypersensitivity of the bronchi to serotonin 20 min after adrenaline administration and potentiate its protective effect in serotonin bronchospasm after administering the beta-adrenoblocker obsidan.

Adrenergic beta-Antagonists↗
PubMed1984

[Pharmacological studies of a new sleep-inducer, 1H-1,2,4-triazolyl benzophenone derivative (450191-S) (V). General pharmacological activities].

General pharmacological activities of 450191-S were studied in various species of animals and compared with those of reference benzodiazepines (BDZ). 450191-S at doses of 10 mg/kg slightly decreased (-5 degrees C) the rectal temperature of rabbits. 450191-S decreased respiratory and heart rates in anesthetized cats, but the effects were less than those of diazepam or triazolam. 450191-S increased respiratory and heart rates in conscious dogs, but had no effect on the blood pressure, electrocardiogram and autonomic nervous system in cats and dogs. The drug displayed a slight spasmolytic activity in the small intestine of guinea pigs and a slight inhibitory effect on isolated non-pregnant and pregnant uteri of rats. These effects were less than those of diazepam or nitrazepam. Below doses of 25 mg/kg, 450191-S did not affect urinary volume and electrolyte excretions in rats. It also decreased brain norepinephrine (NE) turnover rates in rats, but decreased NE and dopamine turnover rates in mice. These effects of 450191-S were less than those of nitrazepam. 450191-S was found to be minimally irritating to the ocular mucosa in rabbits and did not irritate the stomach and small intestine in rats. These effects were also compared with those of active metabolites of 450191-S, M-1, M-2, M-A, M-3 and M-4, and the superiority of the mother compound over its metabolites was clarified.

Animals↗
PubMed1982

Autacoid and autonomic reactivity of bovine and ovine bronchus: modifications by antigenic sensitization.

Spirally cut bronchial strips, prepared from three bovine (horse plasma-sensitized calves, control calves and adult cattle) and two ovine (horse plasma-sensitized and control sheep) animal groups were studied in isolated organ baths and their responses to standard autacoid and autonomic agents were compared. All bovine preparations contracted to carbachol greater than 5 HT greater than histamine and relaxed to isoproterenol greater than adrenaline greater than phenylephrine. Responses of ovine bronchus to the above agonists were similar to bovine except to histamine which caused relaxations. Atropine antagonized carbachol-induced contractions while the relaxant responses of bronchial strips to isoproterenol and adrenaline were inhibited by propranolol in both ruminant species. Contractile effects of histamine were sensitive to mepyramine whereas cimetidine inhibited histamine-induced relaxations of ovine bronchus. The bronchial strips prepared from horse plasma-sensitized calves and sheep exhibited a significant (p less than .05) hyperreactivity to carbachol. The relaxant responses of sensitized calf bronchus to isoproterenol and adrenaline were also significantly (p less than .05) impaired when compared with respective controls. It is concluded that hypersensitization with foreign antigens might exaggerate the airway reactivity by rendering them hyperreactive to spasmogenic and hyporeactive to spasmolytic stimulation.

Animals↗
PubMedDate not supplied

Analgesic activity and opiate receptor affinity of new derivatives of N-butylpiperidine.

The three newly synthesized derivatives of N-butylpiperidine 1-butyl-4-phenyl-4-isonicotinoylaminoethylpiperidine (BG 25), 1-buty-isonicotinoylpiperidine (BG 26) and N-(1-butyl-4-phenyl-4-piperidinoyl) tetrahydropapaverine (BG 9) were evaluated for analgesic activity and opiate receptor affinity. All the three compounds showed analgesic activity both in hot-plate and flinch-squeak-jump test in mice, BG 9 being the most potent. The affinity of the compounds to opiate receptor was moderate (in comparison with pentazocine): the affinity of BG 9 was much greater than that of BG 25 and BG 26. The compounds showed a pronounced inhibitory action in stimulated guinea-pig ileum preparation; this was reversible by naloxone. As evaluated on pA basis, all three investigated compounds showed moderate antagonistic activity. Also in this respect BG 9 was more active than the other two compounds. Cholinolytic and strong spasmolytic properties were observed in isolated rat ileum preparation for BG 9 only.

Analgesics↗
PubMed1984

Forskolin, adenylate cyclase, and cell physiology: an overview.

The potential of forskolin as a research tool is just beginning to be realized. Its use has revealed further subtleties to the control of cyclic AMP generation by adenylate cyclase in both solubilized and membrane preparations and in intact cells. It appears that an effect of forskolin will become one of the criteria for implicating adenylate cyclase in any physiological or biochemical response or, conversely, in ruling out an involvement of cyclic AMP. Clinical applications of forskolin as a hypotensive, spasmolytic, lipolytic, or antithrombotic agents or for the treatment of glaucoma or cardiac insufficiency remain other challenges for the future.

Adenylyl Cyclases↗
PubMed1983

[Clinical trial of the preparation Verbascan in treating gastrointestinal and biliary diseases].

The therapeutic results are presented from the peroral administration of the new Bulgarian preparation Verbascan (spasmolytic, cholinolytic and analgesic), 10 mg three times daily, to 50 patients: with duodenal ulcer--20, with cholelithiasis 10 and dyskinesia of biliary ducts and colon--10 each. In case of duodenal ulcer, the clinical symptoms were very well influenced after 20-day treatment in 65.5 per cent, well in 15.1 per cent, poorly--in 12.5 per cent and without effect in 12.5 per cent and the ulcer faded in 50 per cent, considerably reduced in size in 20 per cent and with no change--20 per cent of the treated (the effect on the ulcer was better, with statistical significance, as compared with the control placebo group). Gastric secretion was not substantially changed by the treatment carried out. The pain and dyspeptic complaints in cholelithiasis were favourably affected in 60 per cent of the treated but the peroral intake did not cope the cholelithiasis crises, rapidly and effectively. Verbascan eliminated and reduced the pains in half of the patients with dyskinesia of biliary ducts and colon, but it had no effect in the pains in the other halt. Verbascan was well tolerated, with no adverse effects, with a favourable ulceroprotective effect, hence it could be used in the treatment of the duodenal ulcer, cholelithiasis and dyskinesia of the biliary ducts and colon with moderate pains.

Alkaloids↗
PubMed1984

[Controlled clinical study on the efficacy of tiropramide hydrochloride in the treatment of irritable colon: comparison with octylonium bromide].

The effectiveness of a new calmodulin-independent spasmolytic, tiropramide hydrochloride, and octylonium bromide, an antispasmodic calmodulin-antagonist drug, was compared in a controlled trial performed in 60 patients with irritable bowel syndrome with spastic pattern. The effect of treatments was assessed according to the score reduction of following symptoms: abdominal pain, constipation, bloating and dyspepsia. Tiropramide hydrochloride administered at the daily dose of 300 mg for 30 days induced a faster and higher improvement than that observed during the administration of 120 mg daily of octylonium bromide. On 3rd and 5th day, treatment with tiropramide induced the relief of abdominal pain in a significantly greater percentage of patients (p less than 0.05). Besides, in the group of subjects treated with this drug the "pain" score was more markedly decreased. Furthermore, at the end of the study 88% of subjects treated with tiropramide and 47% with octylonium bromide had normal bowel habits. This difference was statistically significant (p less than 0.05). Both treatments are effective in reducing dyspeptic symptoms and bloating. We can conclude that tiropramide--having a significant antispasmodic effect combined with a regulating effect on bowel habits--besides eliminating spasm, would act by synchronizing and therefore normalizing the intestinal motility.

Adult↗
PubMed1984

[Venous tonus-modifying effect, pharmacokinetics and undesired effects of dihydroergotamine].

In the present review the clinical pharmacology of dihyroergotamine (DHE) is described. The decisive pharmacodynamic effect of DHE, i.e. the tonicization of the capacitance vessels leading to the acceleration of the venous backflow is described by the methods suitable for the detection of this activity in man. In the paragraph on pharmacokinetics the kinetic parameters of DHE at present known are discussed with regard to the usual forms of application. Emphasis is placed on the poor oral bioavailability of DHE as a result of a distinct first-pass metabolism in the liver. Taking into consideration several recently published cases of ergotism after prophylactic use of DHE, the ability of DHE is discussed to raise the peripheral resistance. The symptoms and the incidence of ergotism are reported on and reference is given to particular conditions which favour its occurrence. Among the measures of a medicamentous therapy of ergotism the use of drugs such as sodium nitroprusside and nitroglycerin which exert a direct spasmolytic effect on the vascular muscles is of special importance. Since DHE is at present the only medicament that possesses a reliable constrictor effect on the capacitance vessels, its clinical application demands special caution due to the narrow therapeutic margin of safety.

Administration, Oral↗
PubMed1984

[Modification of vasoconstriction in ischemically stressed and extracorporeally perfused dog kidneys by alpha adrenergic blockade with phenoxybenzamine].

Renal vasoconstriction was induced in mongrel dogs by clamping the pedicle for 30 min. After reestablishing the renal blood flow for 10 min, the kidneys were removed and flushed for 15 min with cooled Euro-Collins solution. As to estimate the spasmolytic effect of alpha adrenergic blockade with phenoxybenzamine (2 mg/kg) the left or right kidney was first flushed without post-ischemic blockade (control), whereas before nephrectomy of the remaining kidney the dogs received phenoxybenzamine. This was injected intravenously either immediately after the ischemia period maintaining the physiologic blood pressure by volume substitution (group 1) or without volumetric stabilization of the pressure (group 2) or 30 s before the harvesting procedure (group 3). The results showed that pretreatment with phenoxybenzamine in all groups caused a significant reduction of the renal vascular resistance and an improved microcirculation of the Collins solution during the isolated kidney perfusion as compared to the untreated kidneys. The vasodilatatoric effect markedly depends on the blood pressure during the reflow interval and on the time of bolus application before nephrectomy.

Angiography↗
PubMed1981

A comparative study of two parasympatholytic bronchodilator agents: ipratropium bromide and diphemanil methylsulfate.

Ipratropium and diphemanil are synthetic quaternary ammonium compounds with antimuscarinic properties. By using in vitro measurements of tension changes in isolated guinea-pig trachealis muscle strips and in vivo measurements of lung mechanics changes in anesthetized, vagotomized cats, the two drugs were compared in terms of their relative bronchodilator potency, mode of action and apparent site of activity in the bronchial tree. Ipratropium and diphemanil were about equipotent in antagonizing airway smooth muscle contraction induced by the cholinergic agonists, methacholine (in vitro) and carbachol (in vivo). When noncholinergic stimulation was used to augment smooth muscle tone, i.e., hypertonic potassium in the isolated preparations and serotonin in the vagotomized animals, only diphemanil exhibited significant bronchodilator activity. Simultaneous measurements of pulmonary resistance and dynamic compliance were used to partition in vivo bronchodilator effects between large and small airways. The parasympatholytic bronchodilator effects of both drugs were distributed uniformly along the bronchial tree, whereas the direct spasmolytic action of diphemanil appeared to manifest itself preferentially on large airways.

Animals↗
PubMed1978

[Complex conservative treatment of patients with chronic vertebral-basilar insufficiency against a background of cervical osteochondrosis].

The paper contains a description, concerning medicative treatment of 55 patients with chronic vertebro-basilar deficiency in cervical osteochondrosis. The purpose of this study was to remove irritation of the spinal plexus, insufficiency of the cerebral blood flow and secondary astheno-depressive conditions. The following measures were applied: physiotherapy (influences of sinusoidal modulated currents on the cervical part of the spine, massage), special medical gymnastics, drugs (vitamins of the B group, biogenic stimuli, spasmolytical and antihistamine drugs, tranquilizers) and psychotherapy. A comprehensive treatment leads to a steady improvment in 91% of the treated patients, and according to the REG data, to an activization of the blood supply in the zone of vascularization by spinal arteries, especially in the hemispheres with the largest initial blood repletion deficit.

Adult↗
PubMed1978

[Experience in treating vascular parkinsonism with metamysil].

The paper is concerned with a study of the effect of metamizil in 45 patients with different forms of vascular parkinsonism. It was established that metamizil exerts a positive effect on the development of neurological symptoms (rigidity, bradykinesia, tremor) in mild and moderately expressed degrees of lesions. In most of the cases the drugs appeared effective in doses of 0.001 g thrice daily, and in separate cases 0.001 g 6 times daily. In the majority of patients metazil was tolerated without significant side effects. In some patients the side effects (vertigo, dryness in the mouth) were slightly expressed. The effect of treatment was seen after 2 days up to 2 weeks and lasted during the whole course of treatment and sometimes after it. Metamizil possessing a moderate sedative action, as well as spasmolytical and hypotensive is indicated for patients with vascular parkinsonism.

Aged↗
PubMed1984

Experimental pharmacological study of three species from genus Salvia.

Fifteen extracts isolated from three species of genus Salvia were studied: two from Salvia officinalis, seven from Salvia triloba and six from Salvia verbenaca. Their effects on the blood pressure of cats and spontaneously hypertensive rats were examined. The smooth-muscle effects of the extracts were studied on isolated segments of guinea-pig ileum. The effects of some of the extracts on hexobarbital anaesthesia were investigated. Applied intravenously and duodenally, aqueous-alcohol extract of Salvia officinalis causes moderate but prolonged lowering of the blood pressure in cats. Decoction of Salvia triloba also possesses a similar effect (in experiments on spontaneously hypertensive rats). Most of the extracts isolated from Salvia officinalis and Salvia triloba inhibit to various degrees smooth-muscle contractions induced by acetylcholine, histamine, serotonin and BaCl2, whereas extracts of Salvia verbenaca usually potentiate them. Substances isolated from Salvia triloba prolong hexobarbital sleep. Future studies of substances isolated from Salvia officinalis and Salvia triloba are promising with a view to their spasmolytic and hypotensive actions. There exist marked interspecies differences in the pharmacological effects of biologically active substances isolated from genus Salvia.

Anesthesia↗
PubMed1978

The effect of papaverine on the contraction of the human gallbladder.

In a double-blind study, 40 mg of papaverine (Group I) or the same amount of placebo (1.0 ml of physiological saline, Group II)was injected intravenously in 19 patients to study the effect of papaverine on the contractility of the gallbladder in connection with routine oral cholecystography. In both groups a standard contraction meal (200 ml of cream) caused a significant contraction of the gallbladder (at 30 minutes). Thereafter, intravenously administered papaverine significantly inhibited further contraction caused by the fatty meal, but no significant dilatation was observed. This difference between the two groups lasted throughout the whole study period to 60 minutes after the drug administration. This time period mainly consisted of the distributional alpha-phase of the drug concentrations determined by gas chromatography in the serum. Because no dilation effect on the gallbladder was found, the clinical spasmolytic response to papaverine during an acute attack of pain in a patient with gallstones seems to be questionable.

Adult↗
PubMed1984

Antagonistic activity of verapamil and diltiazem against different intestinal smooth muscle stimuli.

Investigations in the isolated guinea-pig ileum have shown an almost equal inhibitory activity of verapamil and diltiazem against contractions elicited by histamine, 5-HT, acetylcholine and BaCl2. While dicycloverine (dicyclomine) has a specific anticholinergic action, no specific action against any of the stimulating compounds including BaCl2 could be differentiated. Verapamil and diltiazem seem to have good oral "unspecific" spasmolytic properties, which might be of clinical value. The results let us assume that the site of the calcium antagonists action of verapamil and diltiazem in the intestinal smooth muscle could be at a common entrance of Ca2+ released by receptor operating compounds and of Ba2+ into the cell or at structures from which BaCl2 as well as the other agonists release Ca2+.

Acetylcholine↗