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Two sets of phosphonic diethylester including a substituted benzylpiperazine moiety are synthesized. In spite of the spasmolytic or the calcium antagonistic potentialities of benzylpiperazine and phosphonic moieties, none of the six compounds, tested in vitro, exhibit any calcium antagonistic profile.
A report is given about the course of urolithiasis in 34 rams and 18 castrated billy-goats. Different therapeutic procedures of this disease are discussed. Concrements in the processus urethrae (n = 27) were removed by amputation of this organ. In animals with a further proximal situated urethral obstruction an ischiourethrostomy was done (n = 7). 21 animals were healed and 9 animals were sent home in an improved condition, but with urine leaking from an artificial opening. Complications as: hyperdistended and ruptured bladder (n = 9) or hydronephrosis caused by severe urine pressure were mostly seen when the diagnosis urolithiasis had been urine pressure were mostly seen when the diagnosis urolithiasis had been confirmed too late, or when the animals had been treated for several days only with analgetics or spasmolytics. Urine cellulitis of the ventral abdomen (n = 11) had not always a bad prognosis. 7 of 11 cases were healed.
Crude extract of Rubia cordifolia (RC) was tested in isolated tissue preparations for its possible calcium channel antagonistic activity. RC suppressed the spontaneous contractions of guinea-pig atria, rabbit jejunum and rat uterus in a concentration dependent manner (0.1-3 mg/ml). In rabbit aorta, it inhibited norepinephrine (10 microM) and KCl (80 mM) induced contractions. Replacement of physiological salt solution with calcium free solution abolished the spontaneous movements of rabbit jejunum. However, addition of calcium (25 micrograms/ml) in the tissue bath restored the spontaneous movements. When the tissues were pretreated with plant extract (1 mg/ml) or verapamil (0.5 microgram/ml), addition of calcium failed to restore spontaneous contractions. These results indicate that the plant extract exhibits spasmolytic activity similar to that of verapamil suggestive of presence of calcium channel blocker like constituent(s) in this plant.
59.4% of drugs allowed by current pharmaceutical nomenclature to be sold without prescriptions may cause side effects or have contraindications. Analgetics, spasmolytics, purgatives and non-steroidal anti-inflammatory drugs account for the bulk of side effects. 87% of over-the-counter drugs contain no information about possible adverse effects. Promoting awareness of the population of side effects of the drugs admitted to prescription-less sale should be considered as an urgent problem of pharmacy.
Inhaled beta-2-agonists are well established for the treatment of bronchial asthma. Treatment in childhood asthma has to take into account the longer night rests and intensive physical activity of the children. The new inhaled beta-2-agonist Formoterol meets these aspects because of the long lasting efficacy. In addition, compliance is increased by easy handling and rare application. Effects of Formoterol in children derived from several studies are presented. In single dose studies, Formoterol (12, 24 mcg) showed a rapid onset of action and in comparison to salbutamol and fenoterol a four-fold respectively two-fold longer lasting spasmolytic effect. The protective effect against unspecific stimuli was comparable but significantly longer. This protection was even more pronounced with a higher dose (24 micrograms). Long-term studies over three months showed that Formoterol (2 x 12 micrograms/day) improved lung function and asthmatic symptoms and protected against histamine and cold-air challenge throughout the study. Formoterol was well tolerated and additional medication could be reduced. Furthermore, we accomplished a high acceptance of treatment with Formoterol for both children and their parents.
Irritable bowel is a functional gastrointestinal disorder with chronic or relapsing symptoms of abdominal pain and impaired frequency and consistency of the faeces caused by obscure structural or biochemical deviations. The frequency of the condition in civilized countries is estimated to amount to 15-20% of the population and it accounts for 25-50% of all patients in gastroenterological ambulatory departments. From the clinical aspect the type with dominant diarrhoea, typically in the morning and very compelling, and the type with pain and constipation are known but even combinations of the two types are encountered. A psychosomatic disorder of the motility of the large bowel and its tonus is involved associated with enhanced pain perception. Despite great efforts to find aetiopathogenetic factors, knowledge still is at the level of obscure theories. The diagnosis is still established per exclusion after all organic causes are ruled out, i.e. we always have to differentiate between an irritable bowel from an irritated one. In therapy the patient's confidence in his doctor is most important and it is essential to gain the patient's active cooperation. In case of diarrhoea a low-residue diet is used, calcium carbonate, codeine, loperamide, conversely in constipation adequate dietary fibre, intake metoclopramide or cisapride. Pain is relieved by spasmolytics or Ca channel blockers in the smooth musculature of the large bowel. The associated dysbiosis is transformed into eubiosis by Lactobacillus or other bacterial products.
The article discusses the possibilities and tactics of radiologically-guided intravascular angioplasty in extended and combined occlusive-stenotic lesions of the lower limb arteries from experience gained in 116 intravascular dilatations in 78 patients. The authors show that it is really possible to perform catheter angioplasty in patients with extended and combined occlusive-stenotic lesions of arteries of the pelvis and lower limbs with compulsory use of spasmolytic and anticoagulant therapy during the operation and, in addition, also disaggregate therapy in the postoperative period. Extended occlusions of the femoral artery, beginning from the opening of the deep femoral artery, should be managed by a retrograde popliteal approach.
This paper presents the methods for galenical investigations of a new gastrotherapeutic preparation. The results and their possible relations to therapy are discussed. The preparation is presented a press-coated tablet. Its antacid characteristics concerning the rate of effectiveness, potency and duration are compared with leading brands on the German market. Pepsin inactivation together with the rapid liberation of the spasmolytic agent propantheline and the psychically stabilising agent peranzine are demonstrated. The results of the stability tests for the active ingredients and the in vitro availability are described. The new product is a gastrotherapeutic preparation, which fulfils all requirements for rapid action and reliable therapy.
Authors demonstrate 21 cases with primary dysmenorrhoea at girls aged 14-17 years, which were observed between 1989-1992 and present way of treatment. In their opinion administration of nonsteroid, antiphlogistic medicaments and the spasmolytics is the most effective method.
Under observation were 12 patients, in whom following paranephral novocain blockade subcapsular and paranephral hematomas, purulent paranephritis, abscesses and carbuncles of the kidneys developed. All patients were subjected to surgery. In such cases to eliminate renal colic it would be more safe to perform other kinds of theapeutic procedures (the injection of spasmolytic, the blockade after M. Ju. Lorin-Epshtein method, etc) which are not at all inferior in their effect to paranephral novocain blockade.
The microcirculatory state (by the method of conjunctival biomicroscopy) and ADP-induced platelet aggregation were examined in 42 patients with atherosclerotic and 34 patients with involutional depression both before and after the treatment which included vasoactive preparations and calcium antagonists. It was determined vascular and intravascular alterations predominance and increase of platelet aggregation in patients with atherosclerotic depression independently of leading syndrome, in patients with involutional depression with anxiety prevalence as well as in patients in stuporous state. The tendency was revealed of such disturbances increasing as for as psychosis was extended. Trental and Cavinton antiplatelet and spasmolytic properties were potentiated by inclusion of Corinfar in complex therapy and that promoted earlier microcirculatory alterations removal as well as aggregatograms and patient mental state normalization.
Experimental data on 116 adult mongrel dogs and clinical findings of 121 patients with complicated spinal injury who had been operated on at Moscow Clinical Hospital No. 67 which is a basis of the Clinic of Traumatology, Orthopedics and Military Surgery, I.M. Sechenov Moscow Medical Academy, underlay the authors' research material. Experimental studies of the impact of local cooling of the intact spinal marrow indicated that there were the least changes in the temperature range of +9 to +11 degrees C with a session lasting 2-3 hours. Experimental histological studies of nerve tissue with hemisection demonstrated that two-hour local hypothermal sessions at 2- or 3-hour intervals proved to be optimal within the first 2 postoperative days. Clinically, the intraoperative regional spinal cooling at the last stage showed a 1.5-2-fold reduction in blood loss and exerted a profound hemostatic effect. Its postoperative local cooling produced analgetic and spasmolytic effects and improved cerebral blood flow. The application of local spinal hypothermia by the procedure developed by the authors is within reach at any medical institution.
The inhibitory activity of O-carbamoyl acylhydroxymoylchlorides was studied on the purified specimens of acetylcholinesterase from human erythrocytes and butirylcholinesterase from the horse blood serum. The pharmacological activity of these compounds was studied on isolated organs of rats. It was shown that introduction of N-aryl substituent in carbamate molecule increases the anticholinesterase activity and efficacy of blocking the neuromuscular conductivity. However it significantly diminishes the spasmogenic effect of N-arylcarbamates on the ileum. An increase in N-arylcarbamate concentration to 0.02-0.04 mM and higher results in a spasmolytic effect on the ileum which can be attributed to their "side" calcium blocking action.
Previous reports have suggested a role played by peripheral benzodiazepine receptors (PBZ) in the regulation of calcium. The aid of this investigation was to evaluate the effects of Ro 5-4864 (PBZ agonist) and PK11195 (PBZ antagonist) in guinea pig trachea and their possible role in the regulation of calcium. Ro 5-4864 and PK 11195 showed spasmolytic effects on the contraction curve induced by acetylcholine. Moreover, Ro 5-4864, PK 11195 and diltiazem (a Ca2+ -antagonistic drug) shifted to the right the contraction curves induced by acetylcholine, potassium chloride (KCl), calcium chloride (CaCl2), or by Bay K 8644. These results demonstrate that the benzodiazepines and their antagonists may exhibit Ca2+ -antagonistic activity. Ro 5-4864 and PK 11195 may exert this effect at a site that is a component of, or is associated with, voltage operated calcium channels (VOC).
The application of human pediatric equipment for measuring respiratory function in nonhuman primates is rapidly gaining popularity in the evaluation of anti-asthma drugs. An important difference between primate procedures and the human clinical situation is the requirement for anesthesia for some techniques because of poor animal compliance. We studied the actions of three potential maintenance anesthetic agents-thiopental, saffan, and propofol-and their effects on a range of cardiovascular parameters under conditions of a broncho-provocation test in rhesus monkeys. The spasmolytic effect of saffan on bronchial smooth muscle was investigated in smooth muscle preparations in vitro and in the rhesus monkey in vivo. Thiopental proved to be a useful sedating agent for this application. Saffan proved to be a bronchodilator in vitro, but the sedative dose was lower than that required to induce appreciable bronchodilator activity in vivo. In comparison, propofol was not appropriate for this application because of the poor sedative effect at nonbronchodilator doses.
Renal colic arises in acute ureteral obstruction and indicates a sharp rise in intrapelvic pressure (up to 150 mm Hg). The diagnosis of renal colic is made basing on direct and indirect measurements of intrapelvic pressure. Ultrasound in renal colic detects dilatation of the calices and pelvis on the colic side, ureterolith can be also revealed by ultrasound. The authors used extracorporeal lithotripsy for fragmentation of the stone and colic relief in 68 patients. The colic stopped in all the cases. This method is extremely valuable in cases when spasmolytic and analgetic drugs, other conservative modalities fail.
31 patients with symptoms of acute renal colic were treated with diclofenac natrium. According to preliminary results this drug is more effective for relieving pain of acute renal colic than the traditional combination of spasmolytics and analgetics. This might be due to the blocking effect of diclofenac natrium on the renal PG synthesis and release, thus decreasing the diuresis. Side effects were minimal, as nausea, vomiting etc. Authors highly recommend this drug as the first choice of treatment in acute renal colic.
The trefoil peptides help to protect the lining of the gastrointestinal tract. They have two beneficial roles in the gastrointestinal tract: 1. In basal circumstances, they may play a role in mucus stabilisation. 2. When an acute injury occurs, their rapid upregulation is important in stimulating the repair process, particularly that of epithelial restitution. The trefoil peptide motif consists of a unique 'three-loop' structure formed by intrachain disulphide bonds. Three members of this family have been identified in humans; spasmolytic polypeptide, intestinal trefoil factor and pS2. The trefoil peptides are expressed by mucus-producing cells throughout the normal gastrointestinal tract in a site-specific manner. In addition, the production of all three trefoil peptides is ectopically expressed in cells surrounding areas of damage in conditions such as peptic ulceration and inflammatory bowel disease.