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PubMedDate not supplied

[Marelin in the treatment of urolithiasis].

The paper provides the results of a study into a therapeutic effect produced by the Soviet agent Marelin used in the treatment of urolithiasis. The study was undertaken to examine 52 patients with severe nephrolithiasis, of them 33 had undergone an operation. The purpose of the study was to investigate spasmolytic, lithagogue, and anti-inflammatory effects of the drug, its impact on phosphorus and calcium exchange, uric acid metabolism, bacterial flora, urine excretion and pH. A pronounced spasmolytic effect was found almost in all the patients. Expelling of small concrements and fragments was observed in 14 cases, almost in all (80%) had crystallines of uric salts, mucus, and pus. Some of them had small calculi moved from the calyces and pelves into the ureter. No pathogenic urinary bacterial flora was found in 12.2% of the cases. Calciuria was normalized in 18 patients, reduced on an average of up to 5.2 mmol/l in 16. Phosphaturia (false or true) occurred in 20 of 52 patients, its severity diminished in two thirds of the cases. Hyperuricemia improved in 6 out of 13 patients who had oxalate calculi. With Marelin, diuresis increased in 48 of 52 patients by 25-30% and 10-20% within the first 2-9 days and the subsequent 20 days, respectively. There was a decrease in pH from 7.8 to 6.8 in some patients with urinary alkaline reaction. The findings suggest that Marelin should be recommended for its wide clinical application.

Chronic Disease↗
PubMedDate not supplied

Octylonium bromide, an antagonist of platelet-activating factor.

Octylonium bromide, a spasmolytic agent in clinical use for the treatment of increased tone and/or motility of the gastrointestinal tract, was examined for its ability to antagonize some biological actions of platelet-activating factor. It was found capable of inhibiting, in a concentration- or dose-dependent fashion, the platelet-activating factor-induced platelet aggregation of rabbit platelet-rich plasma, bronchoconstriction in guinea-pigs, hypotension in rats and lethality in mice, its potency being between 1/15 and 1/50 that of WEB 2086. On the other hand, octylonium bromide was not capable of inhibiting the platelet-activating factor-induced contraction of guinea-pig lung parenchymal strips, an effect which is inhibited by WEB 2086 only at high concentrations. It is worth mentioning that octylonium bromide antagonized endotoxin-induced gastrointestinal damage, known to be due to platelet-activating factor release, at doses comparable to those which exert a spasmolytic effect in man. The role of platelet-activating factor in human gastrointestinal disorders has not yet been clearly established and, therefore, the clinical implications of this property of octylonium bromide are at the moment unknown.

Animals↗
PubMed1989

[Indices of a threatened pregnancy in the first trimester].

Studies were carried out on 167 pregnant women, divided into 4 groups in accordance with the values of human chorionic gonadotropin (HCH). Fetal death was established by ultrasound in 41 of the pregnant women including all cases with HCG under 5000 IU, but it was also found in 19.18% of women with values of HCG over 10,000 IU. Pregnancy advanced unfavourably in other 16 pregnant women of altogether in 34.13%. Prognosis was unfavourable in the presence of decidual hematoma. The gestational sac was enlarged on the average. 1.3 mm per day in normal development. Treatment was made in two groups: with hormones, spasmolytics and vitamins and only with spasmolytics and vitamins. The results showed that progesterone preparations, used singly or in combination with estradiol, did not improve the results.

Chorionic Gonadotropin↗
PubMed1989

[Anesthesia in percutaneous extraction of concretions from the kidney].

The authors discuss the problem of the most suitable anaesthesia for percutaneous extraction of renal concrements. Based on 203 anaesthesias, they compare the combination of local anaesthesia with intravenous administration of ketamine with a tranquilizer, local anaesthesia with administration of phentanyl and a tranquillizer and local anesthesia with phentanyl and a analgetic-spasmolytic mixture. In the great majority of patients they prefer a combination of local anaesthesia and continuous administration of phentanyl and fractionated administration of an analgetic-spasmolytic mixture.

Adolescent↗
PubMed1988

R and S enantiomers of oxybutynin: pharmacological effects in guinea pig bladder and intestine.

Oxybutynin (Ditropan) is widely utilized in treatment of incontinence due to neurogenic bladder dysfunction. We prepared its R and S enantiomers and evaluated their antimuscarinic, Ca++-channel antagonistic and spasmolytic effects in guinea pig detrusor strips and ileal longitudinal muscle. Ussing chambers were used to assess inhibition of carbachol-induced mucosal Cl-secretion in vitro. The enantiomers and the racemate were also tested in in vivo preparations for local anesthetic activity and for antimuscarinic activity in the slow filling cystometrogram. Stereoselective antimuscarinic effects [R)OXY:(R/S)OXY:(S)OXY) were evident for isolated ileal longitudinal (0.12:1.0:4.5) and bladder detrusor muscle (0.5:1.0:13) isolated ileal mucosa (0.2:1:8.9) and acetylcholine stimulated phosphoinositide turn-over in vitro (0.24:1.0:39). Stereoselectivity was also evident for the volume-induced contractions of the cystometrogram in vivo (0.7:1:15). In contrast, no stereoselectivity was observed for Ca++-channel antagonism, spasmolytic and local anesthetic properties of (R/S)OXY and its enantiomers.

Anesthetics, Local↗
PubMed1977

[Therapeutic effectiveness of anticoagulants in the acute phase of cerebral infarction].

500 patients who were admitted to hospitals in acute phases of brain infarctions were treated by intravenous administrations of spasmolytical drugs. 518 patients with similar conditions, besides spasmolytical drugs received anticoagulants (heparin and phenilin). In patients with expressed neurological disorders treated by anticoagulants there was a highly significant improvement, including an increase of the percent of moderate improvement and a drop in the lethality, In those patients with mildly expressed neurological disorders who received anticoagulants an improvement was also marked, but not so distinctly. In cases with slight neurological disorders the different outcomes were not significant. The highest effectivesness of anticoagulants was marked in infarctions, due to thrombosis. The effectiveness indices in patients due to stenosis with angiospasms were not significant.

Acute Disease↗
PubMed1988

[The effects of noscapine and chlorpheniramine on physical dependence and antitussive activity of dihydrocodeine].

The effects of noscapine and chlorpheniramine on physical dependence liability and antitussive activity of dihydrocodeine, a narcotic antitussive, were studied. For developing physical dependence, male Sprague-Dawley rats were treated with dihydrocodeine (DC), noscapine (N), and chlorpheniramine (CP) singly or simultaneously admixed with food (drug-admixed food method (DAF): DC: 0.125, N: 0.25, CP: 0.05 mg/g of food, for 7 days) or were intermittently medicated for 3 days at one-hour intervals through an implanted intravenous cannula (infusion method: DC: 0.5-2, N: 1-4, CP: 0.2-0.8 mg/kg x 24 times/day). Subsequently, rats were treated with naloxone (0.5 mg/kg, sc) and checked for withdrawal signs during 3 hours. Naloxone-precipitated body weight loss of DC was suppressed by simultaneous administration of N or CP. In combined group of DC, N, and CP, withdrawal signs, such as body weight loss, body shakes, and diarrhea, were more remarkably suppressed. Papaverine, the same kind of spasmolytic as N, was tested by the same schedule of DAF. Papaverine did not suppress the naloxone-precipitated withdrawal signs of DC. These results suggest that suppressive effect of N is not due to its spasmolytic action. On the other hand, the cough reflex was induced by electric stimulation in guinea pigs and the fifty percent of antitussive dose (AtD50) was estimated in order to evaluate the influence of N and CP on antitussive effect of DC. N and CP did not change the antitussive effect of DC. These results may suggest that N and CP suppress the development of physical dependence of DC without diminishing the pharmacological effects of DC.

Animals↗
PubMed1986

[Effect of tiropramide on solid gastric emptying time in man].

The influence of Thyropramide, a recently developed spasmolytic on the gastric emptying times of a solid meal was assessed in 10 healthy subjects aged 23-54. Thyropramide (300 mg per diem for 3 days per os) does not significantly modify gastric emptying time compared to the placebo though a slight average increase in T 1/2 was noted. No side effects were noted during the study. Thyropramide therefore appears to have a spasmolytic effect on the large intestine without in any way influence the stomach either proximally or distally.

Adult↗
PubMed1985

[Improved blood flow in the organs and the prevention of thrombus formation with cold].

It has been established that tissue cooling to 15-20 degrees C brings about a short-term spasm of smooth muscles of the intestine, peripheral vessels and of the visceral vessels, replaced by an appreciable spasmolytic effect at the 5th-8th minute of hypothermia. The maximal hyperemia develops by the 15th-20th minute of the cooling and persists over the whole period of the cooling. It is assumed that inhibition of oxidative phosphorylation in the mitochondria of the smooth muscles underlies the spasmolytic action of cold. In addition, cold produces a marked hypocoagulation effect.

Animals↗
PubMed1978

[Studies on the pharmacodynamic activity of several drug solvents. 1st communication: Diethyleneglycol monoethylether, N,N-diethylacetamide, dimethylsufoxide (author's transl)].

The drug solvents diethyleneglycol monoethylether (Transcutol), N,N-diethylacetamide, and dimethylsulfoxide were examined for their pharmacodynamic properties in the following tests: i.p. toxicity, "sign pattern", inclined screen test, balance rod test, and potentiation of hexobarbitone sleeping time in mice, spasmolytic activity in the guinea pig isolated ileum, and cardiovascular studies in anaesthetized rats, cats and dogs including the i.v. toxicity. Except for the cat, N,N-diethylacetamide exhibited the highest toxicity; this solvent, too, was particularly potent in inducing behavioural changes and in potentiating hexobarbitone sleeping time. In the isolated ileum the solvents showed unspecific spasmolytic activities with histamine, carbachol, or BaCl2 as spasmogens. After i.v. administration in rats, cats, and dogs the solvents caused cardiovascular effects even in very low doses. Based on the pharmacodynamic properties doses are recommended for each solvent which should not be exceeded without control experiments in the laboratory routine. These tolerable doses do not only depend on the species but also on the test concerned.

Acetamides↗
PubMed1978

[Studies on the pharmacodynamic activity of several drug solvents. 2. Glycerin, N-(beta-hydroxyethyl)-lactamide, polyethylene glycol 400].

The drug solvents glycerin, N-(beta-hydroxyethyl)-lactamide, and polyethylene glycol 400 (Lutrol 9) were examined for their pharmacodynamic properties in the following tests: i.p. toxicity, "sign pattern", inclined screen test, balance rod test, and potentiation of hexobarbitone sleeping time in mice, spasmolytic activity in the guinea pig isolated ileum, and cardiovascular studies in anaesthetized rats, cats, and dogs including the i.v. toxicity. In mice and rats glycerin exhibited the highest tocicity as well as the greatest activity in potentiating hexobarbitone sleeping time. In the isolated ileum the solvents showed unspecific spasmolytic activities with histamine, carbachol, and BaCl2 as spasmogens. After i.v. administration in rats, cats, and dogs the solvents caused cardiovascular effects even in very low doses. Based on the pharmacodynamic properties, doses are recommended for each solvent which should not be exceeded without control experiments in the laboratory routine. These tolerable doses do not only depend on the species but also on the test concerned.

Animals↗
PubMed1984

Some pharmacological studies on a new tripeptide mustard.

The analgesic, spasmolytic, antiinflammatory, C.N.S., cardiovascular, respiratory, and anaphylactogenic activities of PTT-119 were investigated. PTT-119 possesses good peripheral but only slight central analgesic activity. It presents an interesting in vitro spasmolytic activity of non-competitive type against acetylcholine and histamine. PTT-119 is inactive in rat carrageenin oedema, on the C.N.S. of mice, on cardiovascular and respiratory parameters of cats, and in guinea-pig anaphylaxis.

Analgesics↗
PubMed1983

[Energetic metabolism of the placenta and vascular blood flow as criteria for the choice of drugs in risk pregnancy--results of our investigations].

Object of this paper was to estimate the vascular resistances of the placenta and the lactate/pyruvate-quotient influenced by 8 and 40 mu/min orciprenaline and 320 micrograms/min papaverine. 38 placentas were tested in extraorganic circulation. The content of lactic acid and pyruvic acid was determined in the perfusion solution flowing out of the umbilical vein. Pressure was registered with cymograph. Infusion of 8 micrograms/min orciprenaline diminishes the lactate/pyruvate-quotient and the vascular resistances. 40 micrograms/min orciprenaline causes spasm of placental vessels in the terminal phase of examination. In this group the processes of oxygenation were limited by the oxygen content in the perfusion solution. Papaverine turned the metabolism of the placenta to an anaerob way and the antispasmodic effect was shortlasting.--Therefore the drug effect results out of a metabolic and a spasmolytic component. In risk pregnancy there has to be considered in addition to the spasmolytic the metabolic effects, too.

Female↗
PubMedDate not supplied

The influence of a new antiarrhythmic drug, Craviten (M-71) on the circulatory system in cats.

Craviten, a newly synthesized ester of optically active 2-aminobutanol-1, produced in cats hypotension and inhibited excitability of sinus node and atrio-ventricular and intraventricular conduction. It acts as a spasmolytic on the isolated rabbit ileum, being approx. 100 times as potent as papaverine. Studies with drugs affecting the vegetative system indicate that the hypotensive and spasmolytic action of Craviten consists in a direct depressing action on smooth musculature.

Animals↗
PubMedDate not supplied

Pharmacological properties of Craviten (M-71).

The preparation Craviten (M-71) produced by POLFA Pharmaceutical Works in Cracow (2S, 2'S) N, N'-dimethyl-N, N'-bis-[1-(3',4',5'-trimethoxybenzoyloxy)-butyl]-2-ethylenediamine dihydrochloride) prevents and abolishes heart rhythm disturbance induced in the rat with BaCl2, CaCl2, adrenaline or aconitine. The doses effectively preventing arrhythmia development were in the range from 0.035 to 0.175 mg/kg. They are many times lower than the doses of lidocaine, hexobendine, procaine amide and D,L-propranolol producing a similar effect. Craviten has a much more favourable therapeutic index than these antiarrhythmic agents. Craviten causes sinus bradycardia and slows down myocardial conduction. It exerts a spasmolytic effect about 70 times as strong as papaverine. It has no influence on the central nervous system, on urine excretion, and after topical application it has no irritating or local anaesthetic effect. The 2R, 2'R isomer of Craviten has a similar profile of pharmacological action but its antiarrhythmic and spasmolytic effects are many times weaker.

Animals↗
PubMed1993

Hyperplastic polyps: a cell lineage which both synthesizes and secretes trefoil-peptides and has phenotypic similarity with the ulcer-associated cell lineage.

Hyperplastic polyps are common benign lesions of uncertain histogenesis, which occur in the colon in populations at risk for colorectal carcinoma. They contain neutral/MUC1 gene-related mucin which in turn is closely associated with the trefoil-peptide pS2, a major component of the ulcer-associated cell lineage, previously termed pseudopyloric metaplasia. We have examined 17 hyperplastic polyps for expression of the trefoil-peptides pS2 and human spasmolytic polypeptide by in situ hybridization and immunohistochemistry, as well as by using antisera to epidermal growth factor/urogastrone and its receptor and to epitopes of the product of the MUC1 gene to characterize any further similarity between these lesions and the ulcer-associated cell lineage and thus help elucidate the nature of the lesions. Our investigations show both human spasmolytic polypeptide and pS2 messenger RNA within the polyps, whereas only pS2 peptide could be demonstrated immunohistochemically. Epidermal growth factor/urogastrone, its receptor, and antisera to the MUC1 gene also showed widespread staining of these polyps. We suggest that hyperplastic polyps are formed of a lineage that both synthesizes and secretes trefoil-peptides and the MUC1 mucin and that hyperplastic polyps may be related to the phenotypically similar ulceration-associated cell lineage.

Cell Line↗
PubMed1993

Observer-blind study with metamizole versus tramadol and butylscopolamine in acute biliary colic pain.

To investigate the combined analgesic and spasmolytic effect of metamizole (dipyrone, Novalgin, CAS 68-89-3) this drug was compared with an opioid analgesic (tramadol) and a pure spasmolytic drug (butylscopolamine). In a multicentre, observer-blind, parallel-group study conducted in five German centres 74 patients suffering from "severe" or "excruciating" colic pain caused by a calculus in the bile duct were randomized to receive intravenously 2.5 g metamizole (25 patients), 100 mg tramadol (25 patients), or 20 mg butylscopolamine (24 patients). The three treatment groups were homogeneous for age, sex, height, weight and baseline pain intensity. Metamizole was significantly more effective in reducing pain than tramadol and butylscopolamine for the primary endpoint, pain intensity on a visual analogue scale (VAS) when evaluated as the area under the curve (AUC) from baseline to onset of analgesic action (p < 0.05) and the sum of pain intensity differences (SPID) for the observation period of 2 h (p < 0.005). The mean time until the onset of analgesic action occurred was shortest (p < 0.005) for metamizole (10.9 +/- 5.8 min) compared with tramadol (15.8 +/- 11.7 min) and butylscopolamine (25.6 +/- 24.3 min). Metamizole was also more effective for the secondary efficacy endpoint, pain intensity on a 5-point ordinal scale. In the patient's overall assessment of treatment efficacy at the end of the trial, metamizole was rated as the most effective drug (p < 0.005). Fewer patients in the metamizole (3) and the tramadol (1) groups than in the butylscopolamine group (8) needed a second injection of the "rescue" medication (p < 0.05).(ABSTRACT TRUNCATED AT 250 WORDS)

Aged↗
PubMed1993

Effects of terflavoxate on stimulated contractions of urinary bladder in vitro.

The antispasmodic activity of terflavoxate (CAS 86433-39-8), a flavone derivative with spasmolytic properties on the urinary tract, has been studied in vitro, in comparison to the most common drugs utilized in the therapy of overactive detrusor, namely flavoxate, oxybutynin, and terodiline. Terflavoxate showed affinity for bladder (and brain) muscarinic receptors at micromolar level, however, its activity on carbachol-induced contractions of rat bladder was clearly non competitive, indicating that the compound is devoid of functional antimuscarinic property. Moreover, the observation that unlike antimuscarinic drugs, terflavoxate inhibited by more than 50% field stimulation-induced contractions of rabbit bladder strips, indicates that mechanisms other than the anticholinergic one should be responsible for its smooth muscle relaxant properties. Terflavoxate, flavoxate, oxybutynin, and terodiline were equally effective in inhibiting the two components of K(+)-induced contractions, while nifedipine and nicardipine were more potent than the other compounds, and more effective in inhibiting tonic than phasic contractions. In addition, while nifedipine and nicardipine antagonized in a competitive manner calcium-induced contractions of potassium-depolarized bladder strips, the other spasmolytics behaved as mixed antagonists. Differences in calcium antagonistic properties between nifedipine and nicardipine on one side, and terflavoxate on the other, are further demonstrated by the data on binding experiments. Nevertheless, present results suggest that Ca(++)-antagonistic effects are mainly responsible for terflavoxate smooth muscle relaxant properties.

Animals↗