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PubMed1989

[Effect of cimetropium bromide in the treatment of colic in the first 3 months of life. Randomized study].

UNLABELLED: 20% of unweaned children aged below three months suffer from so-called gaseous colic. The effectiveness and tolerance of an antimuscarinic drug with high spasmolytic activity on the smooth visceral musculature, cimetropium bromide, has been evaluated, excluding cases of intolerance to cow's milk and other pathologies. 40 random patients of both sexes of average age 4.4 weeks (symptoms lasting for one week with crying fits lasting for more than 90 minutes consecutively, on at least 3 days a week) split into two groups of 20 patients each were studied. TREATMENT: A) 1.2 mg/kg 1 hour before bottle; B) 2.0 mg/kg 1 hour before bottle. Speedy reduction in the number of crying episodes (Group A: from 2.8 +/- 0.3 to 0.1 +/- 0.1; Group B: from 2.8 +/- 0.4 to 0.6 +/- 0.4; differences n.s.) and in their duration (Group A: 99 min +/- 10 min to 5 min +/- 3 min; Group B: from 121 min +/- 11 min to 15 min +/- 9 min; differences n.s.). The pharmacological treatment was considered: Group A: very good in 75% of cases; Group B: very good in 70% of cases. In Group B 4 episodes of stypsis occurred and these resolved immediately upon suspension of the drug. Given the equal effectiveness and better tolerance, the use of cimetropium bromide is recommended at the lower dosage.

Colic↗

PubMed1985

General pharmacology of the anxiolytic compound metaclazepam in comparison to other benzodiazepines.

7-Bromo-5-(2-chlorophenyl)-2,3-dihydro-2-(methoxymethyl)-1H-1,4- benzodiazepine X HCl (metaclazepam, KC-2547, Ka-2547, Talis) is a novel 1,4-benzodiazepine characterized by a high selectivity of its anxiolytic effects. The present experiments were performed to contribute to its general pharmacological profile and to evaluate possible risks especially on the cardiovascular field in comparison to standard benzodiazepines. The experiments were performed in guinea pig isolated ileal and papillary muscle preparations, anesthetized cats and dogs, conscious renal hypertensive (RHR) and pithed rats. At intravenous, intraduodenal and repeated oral administration of metaclazepam in anesthetized cats and dogs and RHR arterial hypotension, if any, occurred only at rather high dosages. Tilting experiments in dogs did not show any risk for postural hypotension due to metaclazepam. In guinea pig papillary muscles and in anesthetized dogs (i.v.), metaclazepam had a moderate negative inotropic effect. A diminution of stroke volume was seen only at high i.v. doses whereas cardiac output was maintained nearly constant by an increase in heart rate. In guinea pig papillary muscles metaclazepam, like diazepam, had only a tendency to prolong the refractory period. Unlike diazepam, i.v. metaclazepam had no relevant depressant effect on respiration in anesthetized cats. No specific interaction of metaclazepam with alpha- or beta-adrenoceptors was found in pithed rats and anesthetized cats. The papaverine-like, unspecific spasmolytic profile in the guinea pig isolated ileum suggests that metaclazepam has no relevant antimuscarinic properties. In anesthetized cats neither metaclazepam nor diazepam showed an effect on neuromuscular transmission; metaclazepam caused a markedly weaker inhibition of the polysynaptic linguomandibular reflex than diazepam and did not influence the monosynaptic patellar reflex. In conclusion, the results with metaclazepam did not indicate side effects limiting its therapeutic use as an anxiolytic. Its potential in producing untoward side effects on the cardiovascular and respiratory systems and its central muscle relaxant properties appear to be considerably weaker than with diazepam or bromazepam. Substantial overdosage may result in hypotension and/or impairment of cardiac contractility.

Animals↗

PubMed1987

[Status of postoperative pain therapy in West Germany. Results of a representative survey].

To determine how pain is assessed and managed in the early postoperative period, what the prescribing habits and general opinions on postoperative pain are, and what suggestions for future improvement could be made, questionnaires were sent to 430 anesthesia departments in the FRG. Of these, 188 were returned (38% response). Systemic treatment (opiates, major and minor tranquilizers, peripherally acting analgesics and spasmolytics) was preferred in most cases, although regional anesthesia/analgesia seems to be rather popular. Data are given not only for analgesic techniques, but also for the most frequently used drugs. The study highlighted deficiencies in communication between the anesthetic staff and the patients that resulted in poor assessment of acute pain problems. The findings indicate a need to document pain and pain relief more often and more precisely in order to improve postoperative pain control.

Analgesics↗

PubMed1985

[Differentiation of the effects of antispasmodic agents on the electromyogram of the sphincter of Oddi and the duodenum of the alert rabbit].

The electrical activity of the sphincter of Oddi and gastro-intestinal tract had been recorded on 21 negative atropineesterase conscious rabbits by means of chronically implanted electrodes located in the digestive wall. An analysis of the action of different spasmolytic and analgesic drugs was realized. Electromyograms of the sphincter of Oddi presented (a) isolated or in series spike potentials occurring independently of electrical activities of the duodenum (b) recurring spike potentials correlated with intestine spikes. The independent activity of the sphincter of Oddi was not controlled by the cholinergic system, contrary to the intestine-dependent activity (effect of the fempiverinium, atropine like drug). The pitofenone had inhibited the spike potentials of both the sphincter and intestine because its papaverinic effect. The noramidopyrine, analgesic drug without morphine-like effects, had induced activation and inhibition at low and high posology respectively.

Ampulla of Vater↗

PubMed1986

Management of irritable bowel syndrome.

Few drugs are of proven efficacy in irritable bowel syndrome. Bulking agents probably relieve constipation, spasmolytics may alleviate pain and antidiarrhoeals help control urgency and diarrhoea. With a combination of reassurance and therapeutic intervention up to 75% of patients can be expected to improve. For the 25% who do not, alternative therapies such as stress management, psychotherapy or hypnotherapy may prove effective.

Antidepressive Agents↗

PubMed1978

[General pharmacological studies on tramadol, a potent analgetic agent (author's transl)].

The general pharmacological properties of 1-(m-methoxyphenyl)-2-(dimethylaminomethyl)-cyclohexan-1-ol (tramadol; Tramal) are described and compared with those of other strong narcotic analgetics. In behavioral studies tramadol in high doses had a primarily stimulating effect in mice and rats and a sedative effect in rabbits and dogs. The Straub tail phenomenon, a reaction typical for mice administered morphine, was observed only after subtoxic doses of tramadol. In i.v. doses tramadol generally caused a weak central inhibition of non-stimulated and electrically stimulated brain activity in unanesthetized rabbits. Muscle tone and motor coordination in rats and mice were only slightly affected by the drug, in contrast to the effect of morphine. Unlike other strong analgesics tramadol in doses of 5--20 mg/kg i.v. did not cause respiratory depression and even clearly increased respiratory volume and rate in conscious rabbits and anesthetized dogs. In cats and dogs i.v. doses of tramadol up to 10 mg/kg were well tolerated in the cardiovascular system. Tramadol has a slight, papaverine-like spasmolytic effect and no effect on gastrointestinal motility or urinary and electrolyte excretion. The drug showed no antipyretic properties in rabbits. It inhibited edema in rats and guinea pigs but had no antiproliferative effect in the cotton pellet test in rats. Tramadol did not inhibit monoamine oxidase activity or cause enzyme induction in the rat liver.

Analgesics↗

PubMed1988

Historical aspects and applications of barbituric acid derivatives. A review.

This review considers the pharmacological and other applications of barbituric and 2-thiobarbituric acid derivatives. A chronological description about the discovery, structural studies and first clinical assays are given. Therapeutic expectations as anticonvulsant, antimicrobial, spasmolytic, antiinflammatory, antitumoral and some other effects of 5,5-disubstituted barbituric acids and alkylidene- or arylidenebarbituric acids are overviewed. A considerable amount of these types of compounds have been proposed as industrial dyes and pigments, photosensitizers and thermosensitive materials.

Animals↗

PubMed1987

[The pharmacology and pharmacokinetics of glycerol-2-nitrate].

Glyceryl 2-nitrate (G-2-N), which is the major metabolite of glyceryl trinitrate (GTN, Nitro Mack, glyceryl 1-nitrate (G-1-N) and isosorbide-5-nitrate (IS-5-N, Mono Mack) were examined in a comparative study. The haemodynamic and antianginal properties and the spasmolytic activity on blood vessels were investigated in the rat and dog. Also examined were the pharmacokinetics of G-2-N in the rat and of oral GTN in the dog. Strips of rat aorta contracted with potassium chloride or with norepinephrine were relaxed by G-2-N, but somewhat more weakly than with IS-5-N or G-1-N. After oral administration to the anaesthetized rat or to the conscious dog G-2-N exhibited antianginal and hypotensive activity for 6 h. The duration of action of orally administered GTN in the dog depended on the concentration used and was between 15 and 360 min. The half-life of elimination of G-2-N in the rat came to 2 h, and the substance was 100% bioavailable. The concentrations of G-2-N found in the walls of rat vena cava caudalis and rat aorta abdominalis were twice as high as those in blood or plasma. After oral administration of GTN to the conscious dog, G-2-N is the main metabolite, followed by G-1-N, glyceryl 1,2-dinitrate (1,2-GDN), and glyceryl 1,3-dinitrate (1,3-GDN). After a large oral dose of GTN (30 mg/kg), G-2-N contributes to the pharmacodynamic effect from the 3rd h or earlier.

Angina Pectoris↗

PubMed1988

[Reye-like syndrome following valproate therapy in an adult].

Three months after anticonvulsive regulation by means of the spasmolytic agent Convulsofin, a 46-year-old man suffered severe hepatosis, and when the preparation was discontinued he suffered a severe cerebral dysfunction. The clinical picture is interpreted as being "similar to the Reye syndrome", and distinctions between this and previously reported cases are noted. There has been very little observation of such complications among adult patients.

Chemical and Drug Induced Liver Injury↗

PubMed1988

General pharmacological properties of muroctasin.

General pharmacological effects of N2-[(N-acetyl-muramoyl)-L-alanyl-D-isoglutaminyl]-N6-stearoyl-L-ly sine MDP-Lys(L18), muroctasin) were examined and the following results were obtained. 1. Central nervous system: MDP-Lys(L18) had no effect on behavior, spontaneous motor activity, electroshock- and chemoshock-induced convulsions, hexobarbital sleeping time, pain threshold (mice), conditioned avoidance response (rats) at a dose of 0.4 mg/kg, s.c. and EEG as well as spinal reflex (cats) at a dose of 0.4 mg/kg, i.v. It produced a significant elevation in body temperature (rabbits) at doses of 13 micrograms/kg, s.c. and greater. 2. Respiratory and cardiovascular system (dogs): MDP-Lys(L18) did not show any significant effect on respiratory and cardiovascular functions at a dose of 0.4 mg/kg i.v. 3. Autonomic nervous system: MDP-Lys(L18) induced a miosis (rabbits) at doses of 13 micrograms/kg s.c. and greater. It did not affect norepinephrine-induced pressor and acetylcholine-induced depressor responses (dogs) and contraction of the nictitating membrane induced by electrical stimulation (cats) at a dose of 0.4 mg/kg i.v. 4. Smooth muscles: In the experiments using the isolated ileum, vas deferens, trachea (guinea pigs) and uterus (rats), MDP-Lys(L18) showed neither spasmogenic nor spasmolytic activity at a concentration of 4 x 10(-6) g/ml. Gastrointestinal propulsion (mice), gastric mucosa, gastric emptying rate and gastric secretion (rats) were not affected by this drug at a dose of 0.4 mg/kg s.c. MDP-Lys(L18) did not influence gastrointestinal motility (dogs) at a dose of 0.4 mg/kg, i.v. 5. Miscellaneous: MDP(L-18) suppressed carrageenan-induced edema (rats) at doses of 0.13 mg/kg s.c. and greater.(ABSTRACT TRUNCATED AT 250 WORDS)

Acetylmuramyl-Alanyl-Isoglutamine↗

PubMed1988

[Local hypothermia in the treatment of acute arterial occlusion of the extremities].

An experimental and clinical investigation of the possibility to use local hypothermia of the extremity in the complex treatment of its acute ischemia was performed. It was established that the local hypothermia could considerably improve tissue viability in the process of the extremity ischemia at the expense of spasmolytic, hypocoagulative, anesthetic effects and inhibition of metabolism. A conclusion is made that the local hypothermia should be used in the clinic for the improvement of results of treatment of patients with acute arterial obstruction of the lower extremities complicated by severe ischemia.

Acute Disease↗

PubMed1988

[Mesenterial infarct. New aspects of diagnosis and therapy].

Based on a retrospective analysis of 38 patients with mesenteric ischemia treated from 1981-1987, the current diagnostic and therapeutic concepts are presented. Embolic or thrombotic occlusions of the superior mesenteric artery prevailed (34 patients); venous thrombosis (4 patients) and non-occlusive disease (2 patients) occurred less frequent. Old age (70.6 years in average) and a long time interval between onset of symptoms and therapy (25.8 h in average) are responsible for the still high operative mortality (52.9% in the reported series). Of crucial importance is the early diagnosis within the first 6-12 hours, in which the ischemic bowel may mostly retain its viability. Since the application of transfemoral selective angiography or primary laparotomy however far more patients can be cured, compared to the results in earlier days. Especially in case of primary laparotomy the operative strategy aims in the exposition and inspection of the main trunk of the superior mesenteric artery and vein. Extensive ischemia of the intestines mandates, first of all, revascularization of the bowels. By means of exclusive vascular reconstruction or in combination with limited bowel resection (15 patients) the operative mortality could be reduced to 20%. For the intraoperative determination of intestinal viability the fluorescein test is of high reliability. New concepts in the management of mesenteric ischemia such as local arterial application of thrombolytics or spasmolytics open new approaches to improve the therapeutic results. Post-operative monitoring of serum-lactate in combination with clinical findings obviates routinely performed second-look operation.

Adult↗

PubMed1988

The effect of naftidrofuryl on PGF2 alpha, U 46.619, 5-HT and thromboxane A2 (TXA2) induced vasoconstriction.

This study was designed to investigate the effects of Naftidrofuryl on platelet function and vessel tone and additionally platelet vessel wall interactions. It is shown that Naftidrofuryl displays a spasmolytic activity against a variety of different vasoconstrictors, including 5-HT, PGF2 alpha, U 46.619 and KC1 and inhibits platelet secretion. These effects are observed at concentrations of the compound equal to or higher than 1 mumol/l and might contribute to the clinical efficacy of the drug.

15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5↗

PubMed1987

Influence of cartilage on reactivity and on the effectiveness of verapamil in guinea pig isolated airway smooth muscle.

The authors have examined the effects of cartilage removal on smooth muscle reactivity and the action of verapamil in guinea pig trachealis. In preparations devoid of cartilage, smooth muscle reactivity to both histamine and KCl was reduced. Reactivity to methacholine was unaffected by cartilage removal. In the absence of cartilage, verapamil had a greater depressant effect on the maximum responses to histamine and methacholine than in intact tissues. Similarly, verapamil was more potent against histamine- and methacholine-induced responses in the absence of cartilage where a greater shift to the right was seen in the concentration-response curves when compared with cartilage-containing controls. The spasmolytic action of verapamil on methacholine-induced responses was greater in the absence of cartilage and was greater than its antispasmogenic activity against methacholine (whether or not cartilage was present). Thus, cartilage removal reduces muscle reactivity and increases the potency of verapamil in guinea pig trachealis.

Animals↗

PubMed1987

Effectiveness of pinaverium bromide in the treatment of primitive biliary dyskinesia: 99mTc-P-IDA scintigraphic evaluation.

The 99mTc-P-IDA (technetium-p-iminodiacetic acid) hepatocholangiocholecystoscintigraphy is a diagnostic technique which allows information on the liver biligenetic and excretory capabilities to be obtained. It is, moreover, a test that mirrors closely the anatomic and functional conditions of the cholecyst and choledochus. In this study the authors wanted to verify whether pinaverium bromide, a drug with a documented musculotropic-spasmolytic activity, was able to induce changes in some abnormal instrumental parameters observed in 24 subjects with primitive biliary dyskinesia. The results revealed that the ti values, characteristically longer in those subjects, were significantly reduced in the group of patients treated with pinaverium bromide. On the contrary, in the group of patients treated with placebo, there was no change with respect to this parameter.

Adult↗

PubMed1979

[New developments in the field of bronchospasmolytics].

Bronchial obstruction is mainly treated by bronchospasmolytics. They have different sites of action and work either by stimulating the beta-adrenergic receptors (beta-sympathicomimetics), by inhibiting the phosphodiesterase (theophylline-derivatives) or by blocking the cholinergic receptors (anticholinergica). Beta-sympathicomimetics do not only act via the beta-receptors but also by inhibiting the degranulation of the mast cells and thus preventing the liberation of spasmogenic substances. A very promising development is ipratropium bromide, an anticholinergic with a spasmolytic effect as pronounced as that of a beta2-adrenergic substance but with hardly any adverse side-effect. Glucocorticoids which are highly effective in bronchial asthma were shown to have also an "permissive effect" towards beta-sympathicomimetics.

Adrenergic beta-Agonists↗

PubMed1988

[Disorders of regional blood circulation in systemic scleroderma: early diagnosis and possibility of its correction].

Clinical and instrumental manifestations of disorders of the regional blood circulation were studied in 47 patients with sclerodermia systematica. Hemodynamic changes of the lesser circulation were marked in patients under 44 with more active disease, longer disease duration, pulmonary pathology and cardiac decompensation. Sclerodermic vasculitis played the main role in lesser circulatory disorders. Additional factors were pulmonary and cardiac involvement and concomitant chronic nonspecific pulmonary diseases. Changes of intraorganic vessels and heart failure could result from hepatic circulatory disorders. The authors indicated a possibility of correction of pulmonary hypertension by combining the basic antirheumatic drugs with symptomatic therapy including spasmolytics and cardiac glycosides.

Adult↗

PubMed1988

[Histochemical quantification of muscular ischemia: effect of treatment with naftidrofuryl].

Evaluation of degree of muscle ischemia of a limb and its reversibility is a poorly resolved practical problem, and it has not been clarified whether vasodilatory and circulatory spasmolytic substances possess, in addition to an effect of increasing irrigation, any direct action on muscle cell energy metabolism. An experimental study used histochemical techniques to evaluate oxidative enzyme activity of tissues. The compound tetrazolium nitro-blue (NBT), when reduced by tissue dehydrogenases, has the property of producing a dense non-crystalline blue pigment designated "formazan". During muscle ischemia, the time of appearance of this reaction increases with degree of ischemia through the bias of the decrease or disappearance of succinate-dehydrogenases. Transient ischemia of hindpaw, over 3, 6, 9, 12, 15 and 18 hours, was provoked by tourniquet in 49 rats treated with a vasodilator (naftidrofuryl) and 21 untreated (control) rats. Spontaneous revascularization occurred after removal of the tourniquet. Muscles were studied by microsurgical removal of specimens on removal of tourniquet and 1 and 12 hours and 3, 7 and 14 days after its removal (fig. 1 and 2). Times for staining of muscles with tetrazolium were measured and curves of comparative times established (fig. 3 and 4). Histopathologic specimens were also obtained at the same periods (fig. 5, 6, 7). Results of histochemical studies with tetrazolium and with quantitative determination of degree of cellular anoxia showed the action of naftidrofuryl to be related to mitochondrial metabolism of skeletal muscle, specifically for succinate-dehydrogenase. Clinical application in the determination of therapy and of functional prognosis of an ischemic limb is a possibility by the use of the NBT test in vascular surgery.

Animals↗