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PubMed1975

Pharmacological studies on 1-nitro-9-alkyl acridine derivatives. I. Acute and subchronic action.

Preclinical pharmacologic studies of two further acridine derivatives, 1-nitro-9-(diethylaminopropylamino)-acridine (C-410) and 1-nitro-9-(diethylaminoethylamino)-acridine (C-516) are reported. Both compounds are characterized by high toxicity, especially when injected intravenously, poor absorption from the gastrointestinal tract, and local irritant action. Local irritation can be partly alleviated by using phosphate buffer of pH 7.0 as solvent. Both preparations caused hemodynamic changes (hypotension) due to stimulation of the parasympathetic system (in cats), and higher doses showed direct action on the myocardium. Both preparations acted directly on smooth muscles, predominantly spastically (blood vessels, intestines in vivo and in vitro), and spasmolytically only on the smooth muscle of the urinary bladder in cats. Compound C-410 is deprived of a central component, and compound C-516 in most tests exhibited sedative properties. Despite moderate impairment of spermato- and spermiogenesis, neither of the compounds depressed reproductivity of the animals and no teratogenic action was observed.

Acridines↗
PubMed1975

[Discrepant findings between esophagoscopical and x-ray examination on the search for varicose veins of the esophagus (author's transl)].

In a comparising study of 191 liver-patients, who were laparoscopical and most of them histological examined, the results of registrated varicose veins of the esophagus by x-ray and fiber-esophagoscopical examination were compared. Between x-ray and esophagoscopical examination in our material was a discrepancy in 29,3% of the cases (suspect findings were counted positive). The question was posed, if the premedication with spasmolytical substances and tranquillizers gives the wellknown advantages for the esophagoscopical examination compared with the x-ray examination by relaxation of the esophaguswall and thereby combined with a better visuability of the varicose veins. In the proposed analysis showed still 19,9% of the cases a positive result by esophagoscopical examination by negative x-ray finding, and there was only in 9,4% of the cases a positive finding by x-ray examination by simultaneous negative esophagoscopical result. Other comparising studies by equal pharmacological conditions (premedication!) are urgently necessary to get better results of examination and perhaps to eliminate or at least reduce the discrepancies between endoscopical and x-ray examination.

Diagnostic Errors↗
PubMed2002

[Proper patient counseling, recommended nutrition, specific medication. The basics of irritable bowel syndrome therapy].

In the treatment of the irritable bowel syndrome, it is important to qualify unrealistic expectations with regard to treatment, at an early stage. The therapeutic spectrum encompasses establishment of good rapport between physician and patient, modification of life style, provision of good patient information, reassurance, coping strategies, and temporal restraints on medication. Depending on the leading symptoms, the latter may range from laxatives to probiotics, anticholinergics or spasmolytics, prokinetic and anti-diarrheal agents, to 5-HT3/HT4 receptor antagonists. In individual patients with frequently recurrent or permanent pain, the use of tricyclic antidepressants may be considered. Painkillers should be reserved for patients in whom other therapeutic strategies have failed.

Abdominal Pain↗
PubMedDate not supplied

[Diagnosis and results of treatment of congenital pyloric stenosis in children].

Results of treatment of congenital pylorostenosis in children during last 15 years were studied. There was established, that degree of hypotrophy increases proportionally to duration of vomitive period. Changes of clinical signs of illness due to depression of immune defence, observation by divisional pediatrician with administration of spasmolytic preparation constitute the causes of late hospitalization to unit of pediatric surgery. Late results of treatment witness, that timely performance of operation constitutes an effective method.

Female↗
PubMed2002

[Safety profile of NO-SPA].

The aim of the safety analysis performed by Chinoin Drug Safety Unit was to summarise the safety profile of NO-SPA (drotaverine hydrochloride), the Hungarian spasmolytic well known in Hungary and abroad. Authors collected the safety data from clinical studies between 1964-1998 for the determination of the adverse event frequency. Based on the data of 12111 patients treated with NO-SPA in 37 clinical trials 0.9% frequency of adverse events was found. The value indicates uncommon (0.1-1%) adverse event frequency according to the criteria for frequency categories. The benefit-risk ratio of NO-SPA is favourable, since the therapeutic effect does not include frequent adverse reaction occurrence.

Analgesics↗
PubMed1975

Chemical structure and pharmacological (curarizing) properties of various indole alkaloids extracted from an African Strychnos.

The chemical separation and identification of ten alkaloids extracted from the roots of Strychnos usambarensis are described. The elucidation of their structure by means of elementary analysis, I. R., U.V, and mass spectrometry allows their classification into bistertiary amines, hybrid and bisquaternary ammonium derivatives. This classification is reflected in the pharmacological properties. One of the tertiary amine alkaloids (usambarensine) presents atopine-like and spasmolytic activities while the bisquaternary ammonium compounds (dihydrotoxiferine, calebassine, C-curarine and afrocurarine) are competitive neuromuscular blocking agents.

Alkaloids↗
PubMed2002

[Clinical aspects of using pariet in treating chronic pancreatitis].

Three groups of patients were studied with the purpose of assessing the efficiency of the application of Pariet in the complex treatment of chronic pancreatitis. The first group (16 people) underwent conventional treatment (spasmolytics, enzymes, disintoxication therapy). In addition to conventional treatment, the second (22 people) and third (21 people) groups were administered Pariet (rabeprazole), 20 mg per day, or Quamatel (famotidine), 40 mg per day, respectively. The intragastric and intraduodenal pH was higher against the background of the treatment with Pariet than against the background of the application of Quamatel even within the first hours and days of treatment. A faster pain relief was observed in the second group of patients (p 0.05) than in the third one. According to the MRI data, the seven-day Pariet treatment of patients with chronic pancreatitis was accompanied by a reduction of the pancreas size, the diameter of the main pancreatic duct and the pancreatic edema. Thus, the application of Pariet in the complex treatment of chronic pancreatitis promotes a faster and more efficient pain relief and reduction of pancreatic edemas, as compared to the Quamatel therapy.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed1976

[Therapy of ulcus ventriculi with Caved-S. Use of the gastrocamera for diagnosis and control of therapy].

36 patients with a ventricular ulcer demonstrated by endoscopy and secured by histology, were given 2 tablets Caved-S 4 times a day for 4 weeks. Clinical parameters were subjective complaints, such as pain and heartburn, which after a relatively short time, many patients declared to have diminished or ceased completely. Objective parameters were endoscopic explorations before beginning of the treatment, i.e. gastroscopy and biopsy, examinations by gastro-camera and in some cases chromography to exclude a possible malignancy. The control examinations were performed almost exclusively by gastro-camera, and that after 2 and 4 weeks. The ulcer healing stage could be clearly defined after Ohmori and Miwa (1971), its localisation and size were also recorded. Altogether it can be said, that the preparation Caved-S, by a working-principle not as yet exactly defined in all details, effects rapid healing endoscopically provable, but that ulcers with a special localisation, e.g. in the angulus-area of the posterior wall, require a longer healing time according to expectation. Clinically relevant side effects were not observed. Thus it can be concluded that Caved-S is very suitable for the treatment of ventricular ulcers. The preparation has a spasmolytical component leading quickly to freedom from pain, and a protective component effecting a healing tendency which can be demonstrated by endoscopic methods. It must be said, however, that this protective healing-promoter factor has not yet been defined pharmacologically.

Aluminum Hydroxide↗
PubMed2003

The history of tocolysis.

In 1950, the World Health Organisation (WHO) defined prematurity as a birthweight of 2500 g or less and in 1961 as a gestational age of less than 37 weeks. The time in between marks an era in which there was growing recognition of the importance of gestational age at birth and how to influence it. The latter was facilitated too by the development of tocography, which permitted some semi-objective measurement of uterine contractility. Along with it, came a growing interest in agents that could control uterine contractility beyond the earlier classical approaches of hormones and gastrointestinal spasmolytics. Hence, the early 1960s saw much research interest in agents, such as nylidrine, isoxsuprine, and orciprenaline that could suppress uterine contractility as one of their many beta-agonist properties. Subsequently, two approaches would be used to shift the balance towards uterine function over and above the influence on other bodily functions. One consisted of supplementing these drugs with agents, such as calcium antagonists and beta-receptor blockers that were hoped to suppress non-uterine actions. The other was a search for drugs in the same class with greater uterospecificity and more selective binding to uterine as opposed to other receptors. Neither of these approaches has ever fully fulfilled the hopes that were pinned on them, but they resulted in the availability of a large number of agents to suppress uterine contractility. The advent of prostaglandins as regulators of uterine contractility and the ability to suppress their biosynthesis saw another range of attempts to suppress uterine activity. They included aspirin, sodium salicylate, flufenamic acid, sulindac and indomethacin, but some were clearly based on a defective understanding of how uterine prostaglandin synthesis can be influenced. In the meantime, a flurry of other agents came and went, often more than once, testifying to the ingenuity of clinicians in trying to solve a problem that is poorly understood. Some, such as relaxin and ethanol, came and disappeared. Others, such as calcium antagonists, entered the scene as protectors against the non-uterine effects of other agents, went, and re-entered the scene in their own right. Still others, such as magnesium sulphate, came, lingered around, and became credited with effects in preterm labour that do not depend on affecting uterine contractility. Amidst this all arose the term tocolysis, coined in 1964 by Mosler from the Greek stems 'tauomicronkappaomicronzeta' and 'lambdaupsilonepsiloniotanu', to epitomise all of this ingenuity.

Female↗
PubMed1992

Clinical profile of nicorandil: an overview of its hemodynamic properties and therapeutic efficacy.

Nicorandil is a new vasodilator agent. Efficacy and safety of nicorandil in the treatment of angina pectoris have been evaluated through an extensive clinical program with a total of 1,680 patients who received the product. Results of hemodynamic studies provide clear evidence of the vasodilatory effect of nicorandil. In a population of patients with normal left ventricular function, a reduction in preload was apparent from a decrease in left ventricular end-diastolic pressure from 7.4 +/- 1.7 to -3.2 +/- 1.5 mm Hg. Furthermore, nicorandil produced marked reductions in total peripheral resistance (19%) and aortic blood pressures with decreases in systolic pressure of 34% and in diastolic pressure of 21%. At antianginal doses, nicorandil has a coronary vasodilating effect as well as a balanced peripheral action that leads to decreases in both preload and afterload. Therefore, nicorandil affects two of the main hemodynamic determinants of oxygen demand without impairing myocardial contractility or atrioventricular conduction. In addition, its strong spasmolytic activity is of particular interest when dynamic coronary obstruction is considered. Nicorandil clearly has demonstrated K(+)-channel-opening activity. In addition, the range of plasma concentrations in humans at therapeutic doses is similar to that of experimental models in which the K(+)-channel activity has been determined. This mechanism of action may explain the different hemodynamic profiles of nicorandil and nitrates in humans. Nicorandil is an effective and potent antianginal agent at a dose of 10-40 mg, which in monotherapy controls 69-80% of patients with stable chronic angina. Comparative trials have shown that the efficacy of nicorandil compares with that of drugs from the main classes of antianginal drugs--beta-blockers (atenolol, propranolol) and a Ca2+ antagonist (diltiazem). Patients treated for as long as 3 months or 1 year have shown sustained efficacy with no evidence of development of tolerance to the drug. The long duration of action allows effective treatment with a well-tolerated b.i.d. regimen. At the recommended doses, the main side effects were limited to headaches. They usually occurred early in the course of treatment and can be diminished by a progressive titration. From the large safety data base, there is no evidence that nicorandil induced exacerbation of myocardial ischemia or abrupt withdrawal syndrome. Nicorandil does not adversely affect the lipid profile or the glucose level. As an antianginal drug with a novel mechanism of action, nicorandil provides a useful alternative to existing antianginal agents in the long-term management of patients with angina pectoris.

Diltiazem↗
PubMed2003

Physiological and chemical characteristics of antibacterial activity of pancreatic juice.

Attempts were made to find and characterize an antibacterial activity (ABA) factor in porcine pancreatic juice (PJ). Its isolation requires several steps. Since ABA factor was found to be heat resistant, the first step was heating for 30 min at 65 degrees C. Afterwards column chromatography, ethanol precipitation and polyacrylamide gel electrophoresis were involved. Finally, we obtained a pancreatic juice fraction with antibacterial activity against Escherichia coli strain AB1157. In the presence of this fraction the number of living bacterial cells in overnight culture decreased about 10,000 fold and a spot-test gave clearly positive results. The results of analysis suggest that the antibacterial factor is a polypeptide active in a pH range 8.0-8.5, that migrates in polyacrylamide gel electrophoresis as a band under 14,000 Da. Mass spectroscopy analysis of active fraction showed high concentration of porcine pancreatic spasmolytic polypeptide (PSP). In conclusion, a polypeptide controlling bacterial homeostasis has been found in the porcine pancreatic juice.

Animals↗
PubMed1992

[The efficacy of the conservative treatment of patients with acute appendicitis on board ships at sea].

Under study was efficiency of conservative treatment of 247 patients with acute appendicitis on ships in the sea depending on the age of patients, clinical manifestations of the disease, volume of medicamentous therapy and time of taking medical advice. It was established that conservative treatment is most effective if started within the first 6 hs from the beginning of the disease and antibiotics were used in combination with spasmolytics, antihistamines and sulfanilamides. Patients treated conservatively had pronounced inclinations to delimiting the inflammatory process in the abdominal cavity.

Acute Disease↗
PubMedDate not supplied

The effect of Salbupart on the value of placental perfusion pressure in extracorporeal experiment.

The purpose of the study was determination of the perfusion pressure as an expression of the resistance of placental vascular bed after administration of various doses of Salbupart. In a series of 29 experiments with extracorporeal perfusion of the fetal part of the placental from spontaneous labours after physiological pregnancy it was observed that the medicament given in one dose reduced the vascular resistance in the afterbirth. A beneficial spasmolytic effect of Salbupart may be expected in certain cases of pathological pregnancy associated with increased resting tonus of the placental vessels. The pharmacological management for stimulation of placental adenyl cyclase may be treated as supplementation of deficient endogenous catecholamines enhancing the adaptation mechanisms of the fetus and placenta.

Albuterol↗
PubMed1962

[Preliminary clinical study on the use of dihexyverine in obstetrics].

This study attempted to evaluate the effect of dihexyverine HCl (Metaspas), an anticholinergic and direct smooth muscle relaxant (spasmolytic), in shortening the first stage of labour. One hundred and five patients constituted the series: 31 were primiparae, 27 secundiparae and 47 multiparae. The majority of these (95) received one intramuscular injection (10 mg.) of dihexyverine. Alphaprodine (Nisentil), 40 mg., was administered in all but 10 cases, since dihexyverine has no analgesic action. Seventy-five control patients were used: 25 were primiparae, 25 secundiparae and 25 multiparae. Alphaprodine alone was administered to these control patients. The length of time for dilatation from 4 cm. to 10 cm. was the selected criterion. In the control group, the average time for complete cervical dilatation was 4 hours, 10 minutes. In the group treated by dihexyverine, complete dilatation was achieved in 1 hour, 16 minutes. On the average, the first stage of labour was 2 hours and 54 minutes shorter with dihexyverine; the clinical effect begins 10-30 minutes after administration. The only side effect encountered was a skin rash in one patient.

Alphaprodine↗
PubMed1992

[2-Amino-oxazoles as potential H-bonding agents in virostatic research. 4. Pharmacokinetics and pharmacologic-toxicologic profile of 2-guanidino-4,5-dipropyloxazole hydrochloride].

Out of the group of 2-amino-oxazoles 1 was found to be the most potent antiviral compound. Following p.o. or s.c. administration to rats, the 14C-labeled 1 was quickly and completely absorbed. The TRA was eliminated mainly via the kidneys and the liver with half-lives between 32 and 42 h. The acute pharmacodynamic effects of 1 were decrease of blood pressure, bradycardia, and inhibition of both gastric emptying and acid secretion. On smooth muscles spasmolytic and alpha-anti-adrenergic actions were predominant. After single administration the following MTD's were determined: 30 (mouse), 20 (rat), 10 mg/kg i.v. (pig), and 500 (mouse, rat), greater than 100 mg/kg p.o. (pig), respectively. In a subchronic toxicity study in rats, oral doses of 1 between 15 and 240 mg/kg given daily for 4 weeks were tolerated without any severe alterations related to the drug.

Administration, Oral↗
PubMed1992

[Cost-benefit analysis of a new treatment concept in patients with indwelling catheters].

An earlier and a new treatment concept for patients equipped with long-term indwelling bladder catheters were compared with regard to cost, expenditure of time, and equipment in a retrospective study involving 58 patients treated by the earlier concept and 60 treated by the new one. The new concept dispensed with the need for bladder irrigation and routine replacement of the indwelling catheters. Under the earlier concept, 18 indwelling catheter replacements and 53 bladder irrigations were required per patient and year during the years 1979/80. This compares with 6 indwelling catheter replacements and 0.05 bladder irrigations per patient and year for the years 1989/90 under the new concept. The use of analgesics and spasmolytics fell from 55 to 21 units per patient per year. Significantly fewer urinalyses were performed during 1989/90. The use of antibiotics remained unchanged. When compared with the earlier one, the new concept for the management of patients with indwelling catheters provides savings of 1265 minutes (21 hours) of nursing time and sFr. 405 for equipment per patient per year. Applied to our geriatric hospital (120 beds, 80 nursing staff), this translates into annual savings of one full nursing post and sFr. 34,000 for equipment.

Aged↗
PubMedDate not supplied

[The removal of calculi from the pelvic ureter by extracorporeal lithotripsy].

Using high-energy impulses from Dornier HM-3 lithotriptor, iliac ureteroliths were crushed in 18 patients for the period of 2.5 years. The mean age of the patients was 38 years. The lithotripsy was in all cases preceded by retrograde catheterization. Reposition of the stones was achieved in 6 patients. Prone-position lithotripsy was conducted in 12 patients. Specially designed support cushions helped to keep the patient in a steady position, speeded up the stones excretion, relaxed knee joints and reduced the exposure to the impulses. All the patients underwent antiinflammatory and spasmolytic therapy. The mean hospital stay reached 3.2 days. Good results were reported in 94.1% of those treated. Neither early nor long-term complications arose.

Adult↗