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PubMed2000

Inhibition of testosterone secretion by S-petasin in rat testicular interstitial cells.

S-petasin, a kind of sesquiterpene ester, is the anti-inflammatory ann analgesic component of the butterbur (Petasites hybridus). The clinical benefit of S-petasin is the spasmolytic activity, but its side effects on the reproductive endocrinology are not clear yet. The present study was to explore the effects of S-petasin on the secretion of testosterone in vivo and in vitro. We found that single intravenous injection of S-petasin (1 microg/kg) decreased basal plasma testosterone concentration in adult male rats. The enzymatically dispersed rat testicular interstitial cells were incubated with S-petasin (0-4.3 x 10(-5)M) in the presence or absence of human chorionic gonadotropin (hCG, 0.05 IU/ml), forskolin (adenylyl cyclase activator, 10(-5) M), and androstenedione (testosterone biosynthesis precursor, 10(-9) M) at 34 degrees C for 1 h. The concentrations of testosterone in the incubation medium were measured by radioimmunoassay. S-petasin at 4.3 x 10(-7) M was effective to reduce the basal and hCG-stimulated release of testosterone in rat testicular interstitial cells. The stimulatory effects of testosterone secretion induced by forskolin and androstenedione were significantly reduced by S-petasin at 4.3 x 10(-5) M and 4.3 x 10(-6) M, respectively. These results suggest that S-petasin inhibits the production of testosterone in rat testicular interstitial cells in part through diminishing the activities of adenylyl cyclase and 17-ketosteroid reductase.

17-Hydroxysteroid Dehydrogenases↗

PubMed2001

Estrogen derivative relaxes rabbit aorta via the endothelial receptor system.

BACKGROUND: It is well known that sexual hormones, in particular estrogens, may influence the cardiovascular system. Experimental and clinical studies have shown that estrogen directly or indirectly modulates the reactivity of vascular smooth muscle but at present the mechanism of action of this hormone has yet to be clarified. The aim of this study was to evaluate the vascular effects of a synthetic non-steroid estrogen, diethylstilbestrol, and the possible involvement of endothelial function. METHODS: We investigated, on aortic strips of a female rabbit, the inhibitory effects of diethylstilbestrol on the contractions induced by different spasmogenic agents, noradrenaline (10(-6) M), angiotensin II (10(-6) M), serotonin (10(-6) M), and KCl (10(-1) M). Some experiments were performed in high K+, Ca++-free solution. In some experiments endothelial function was abolished by mechanical ablation. Another series of experiments was incubated (30 min) with N(G)-monomethyl-L-arginine, which inhibits nitric oxide synthase or with tamoxifen, a specific antagonist of estrogen receptors. RESULTS: At doses from 10(-6) M to 10(-4) M, diethylstilbestrol showed an evident spasmolytic action on contractions induced by noradrenaline, angiotensin II and serotonin but no significant effect was observed on KCl spasm. The inhibitory response of diethylstilbestrol to increased vascular tone induced by noradrenaline disappeared when the endothelial function, validated by the acetylcholine test, was abolished by mechanical ablation. When tested in high K+, Ca++-free solution, diethylstilbestrol did not significantly shift the cumulative dose-response curve of calcium. In the experiments performed with N(G)-monomethyl-L-arginine, diethylstilbestrol failed to induce vasodilation suggesting that its action may be related to synthesis of nitric oxide. Moreover, in the presence of tamoxifen, diethylstilbestrol was unable to induce vasodilation. CONCLUSIONS: The early occurrence of vasodilation is in favor of a direct effect and seems to exclude a regulation of gene expression. These results suggest that estrogens may directly regulate vascular tone interacting with its specific endothelial cell receptors through the release of nitric oxide.

Animals↗

PubMed2000

[Treatment of irritable bowel syndrome with dicetelium and spasmomen].

The aim of the study was to compare clinical efficacy of new spasmolytics--pinaverium bromide (dicetel, Solvay Pharma) and otilonium bromide (spasmomen, Menarini-Berlin-Chemie)--in the treatment of irritable bowel syndrome. Effects appearing during the treatment with anxiolytic drug tofisopam (grandaxin, Egis) after using dicetel and spasmomen were also studied. The results indicate marked clinical efficiency of dicetel and spasmomen which improve vegetative functions and psychoemotional status. Grandaxin provides further improvement of clinical symptoms and additionally corrects psychoemotional status.

Adult↗

PubMed2000

[Treatment of hemorrhoids from the viewpoint of the gastroenterologist. Personal experience with the Ginkor Fort preparation].

Pathological changes in hemorhoid plexes are frequently occurring mainly in elderly. In development of this disease are mainly involved changes in the vessel wall, pressure changes in basin, disturbances in passage of stool and also infectious disease. Instead of the correction of the life-style in therapy are used locally-acting drugs whose basis are local anesthetics, spasmolytics, antiflogistics, antipruriginostics and corticoids in many combinations. The main aim of the orally administered drugs is influence of the vessel-wall tone, decrease of the capillary permeability, circulation betterment, decrease of the oedema and blockage of the inflammatory mediators. In the group of 45 patients is documented benefit in use of Gincor-fort in dose of 2 cps bid in first week and 2 cps daily in the second week of the treatment. We presume that this drug can influence all of above mentioned factors during the acute hemorrhoidal attack.

Acute Disease↗

PubMedDate not supplied

[Effect of nitroglycerin on the tonus of isolated coronary arteries].

It has established on isolated ring-like strips of large coronary arteries of the dog that spasmolytic effects of nitroglycerin are related to its antagonistic action on Ca2+ and are not completely pharmacomechanic. The action of nitroglycerin is not related to beta-adrenoreceptors of the coronary arteries and apparently is not mediated through an increase in the intracellular pool of cyclic AMP.

Animals↗

PubMed1999

[Omentoplasty in surgical management of postpulmonectomy pleural empyema].

A method of treating postpulmonectomy pleural empyema, practically implemented in this country for the first time, is described. Three patients are subjected to operation. Right pulmonectomy for lung cancer and chronic inflammatory process is done twice, and left pleuropulmonectomy for tuberculosis--once. Postpulmonectomy empyema persists in all three cases regardless of the adequate continuous suction drainage and intrapleural antiseptic management. Anaerobic and gram-negative flora is isolated. The size and location of the intrapleural cavity being cured are assayed by CT, thoracic ultrasonography and fistulography. In none of the patients is clinical and FBS evidence of bronchopleural fistula established. The operative procedure consists in resection of a 4 cm segment from the underlying rib in the drainage zone, and further cavity treatment under thorascopic control. Minor median laparotomy and skeletization of the greater omentum are performed preserving a major nutrient vessel depending on the location of the cavity. The omentum is drived into the pleural cavity through a parietal opening of the diaphragm, measuring 3-4 fingerbreadths. Pleural cavity drainage is carried out according to Redon. Two patients run an uneventful postoperative course. One female patient develops pylorospasm successfully cured by spasmolytic therapy and H2 blockers. CT and thoracic echography do not show presence of residual cavities. The patients are free of any complaints over periods ranging from 6 to 16 months postoperatively. The inference is reached that omentoplasty is a new method promoting successful elimination of both postpulmonectomy empyema, and other residual pleural cavities as well, with or without bronchopleural fistula.

Adult↗

PubMed1997

[Rolipram reversed salbutamol tolerance in guinea pig trachea].

Studies were carried out to examine the role of phosphodiesterase(PDE) III and PDE IV in the development of tachyphylaxis of isolated guinea pig trachea to beta 2 adrenoceptor agonists. Treating trachea with salbutamol(SB) 1 mumol.L-1 for 1 h produced a 5-fold rightward shift of the SB concentration-response curve for the spasmolytic effect against methacholine-induced bronchocontraction and decreased the maximum SB-induced relaxation by 30%, i.e. induced tolerance of airway response of SB in vitro. The PDE IV inhibitor rolipram (Rol, 1 mumol.L-1, IC50), but not the PDE III inhibitor siguazodan (SK&F 94836, 1 mumol.L-1, IC50), reversed the SB tolerance. However, the protein synthesis inhibitor cycloheximide(10 mumol.L-1) did not abolish the SB tolerance. These results indicate that the SB tolerance may be related to increase in PDE IV activity.

Adrenergic beta-Agonists↗

PubMed2001

Relaxant effect of 6-deoxyclitoriacetal on smooth muscle preparations.

The pharmacological effect of 6-deoxyclitoriacetal (6-DA), a rotenoid compound isolated from the roots of Clitoria macrophylla Wall. (Papilionaceae), was examined on different smooth muscle preparations. 6-Deoxyclitoriacetal 0.2 mg/ml produced a significant decrease in the spontaneous contraction of isolated rat uterus. It also suppressed the contraction induced by acetylcholine 5x10(-6) M and oxytocin 5x10(-3) IU/ml. The cumulative contractile responses of rat aortic strips caused by serotonin 10(-8)-10(-4) M and norepinephrine 10(-11)-10(-7) M were reduced by 6-DA 0.4 mg/ml. In calcium free Kreb's solution, 6-DA inhibited the aortic contraction produced by a cumulative dose of calcium chloride (0.1-30 mM). In guinea-pig ileum, 6-DA 0.15 mg/ml exerted the spasmolytic activity by inhibition of the contractile response evoked by various contractile agents e.g. acetylcholine 10(-9)-10(-5) M, serotonin 10(-9)-10(-5) M and histamine 10(-9)-10(-5) M. All of the results indicated that 6-DA could induce a smooth muscle relaxant effect by interference with intracellular calcium metabolism.

Animals↗

PubMed1975

The effect of methyl paraben on tracheal smooth muscle in vitro.

The widely used bacteriostatic preservative methyl paraben (M.P.) produced a concentration-dependent relaxation of the carbachol-contracted guinea pig trachea and the isolated rabbit jejunum. The relaxant effects on the trachea were not blocked by dl-propranolol and the responses on the rabbit jejunum were not blocked by bretylium tosylate which abolished the responses to sympathetic nerve stimulation. Sub-threshold concentrations of M.P. (130 muM) produced a marked and significant enhancement of the responses of the trachea to the three catecholamines dl-isoprenaline (I), 1-noradrenaline (N), 1-adrenaline (A), a slight but significant enhancement of the responses of the trachea to the two non-catechol beta sympathomimetics salbutamol (S), and orciprenaline (O), but no significant enhancement of the responses to aminophylline (AM). It is concluded that the relaxant effect of M.P. is characteristic of a "non-specific" spasmolytic and this is consistent with its reported local anaesthetic activity. In addition, the specific ability of M.P. to enhance responses to catecholamines suggests that it may be interacting with a mechanism responsible for catecholamine removal (i.e., tissue uptake or uptake 2). In view of the widespread use of M.P. in pharmaceutical preparations in concentrations often equivalent to or greater than those employed in the present investigation, the fact should be stressed that its presence should not be overlooked in the interpretation of experimental and clinical studies.

Animals↗

PubMedDate not supplied

Biliary Ascariasis in children.

BACKGROUND: Ascariasis is very common in this part of the world. Biliary Ascariasis is rare but is the commonest extra-intestinal complication. METHODS: This study was conducted At Ayub Teaching Hospital, Abbottabad, a tertiary care hospital. Five cases of biliary Ascariasis were studied from December 1999 to January 2001. History of passage of worms in stool or vomiting and abdominal pain was taken. After clinical evaluation, Stool Examination, Serum amylase, LFTs, and complete blood picture (CP) were done. Ultrasound abdomen was done as a basic tool for diagnosis. All cases were given Piperazine. Spasmolytics were also given to relax sphincter of oddi to release the worms. Surgical opinions were also taken for each case. RESULTS: About 80% Children were above 10 years of age. One case was 1 1/2 years old. Most common symptom was right upper quadrant abdominal pain. Previous history of passage of worms in stool and vomitus was also present. Two children developed complications of Biliary Ascariasis i.e., Cholecystitis and Portal empyema and responded to antibiotics. All children became symptom free in about 48 hours of treatment. Ultrasound was found to be a reliable, non-invasive, and quick tool for diagnosis and follow up.

Animals↗

PubMed2001

[Diagnosis and treatment of diffuse esophagospasm].

123 patients with diffuse esophagospasm were observed, including 56 (45.5%) with primary and 67 (55.5%) with secondary esophagospasm. Since 1986 due to unsatisfactory treatment results an original therapeutic complex including spasmolytics, neuroleptics, vitamins B, was used. In secondary esophagospasm therapy was complemented by pneumocardiodilatation, not more 5 sessions per course. Good and satisfactory clinical results were achieved in 30 (66.7%) patients with primary diffuse esophagospasm and in 45 (67.2%) patients with secondary esophagospasm.

Combined Modality Therapy↗

PubMed2002

[Irritable bowel syndrome: pathophysiology and (future) treatment options].

Abnormalities of intestinal motility, altered visceral perception and psychological influences are the most important factors in the pathogenesis of irritable bowel syndrome. Current pharmacological treatment options are limited and lack specificity. In the future, it is likely that a number of therapeutic agents with stronger spasmolytic effects (selective muscarinic receptor antagonists), more specific colokinetic properties (5-hydroxytryptamine (5HT)4 agonists) and a positive influence on visceral perception (serotonin (5HT3) receptor antagonists, kappa-agonists) will become available.

Analgesics, Non-Narcotic↗

PubMed2002

[Pharmacogenomics and pharmainformatics].

Pharmacogenomics is defined to identify the genes which are involved in determining the responsiveness and to distinguish responders and non-responders to a given drug. Genome sequencing, transcriptome and proteome analysis are of particular significance in pharmacogenomics. Sequencing is used to locate polymorphisms, and monitoring of gene expression can provide clue about the genomic response to disease and treatment. The transcriptome analysis can be done by methods of random cDNA sequencing (expressed sequence tag project, body map project, serial analysis of gene expression, et al), mRNA display (differential display, fluorescent differential display, RNA arbitraly primed PCR, molecular indexing, gene expression fingerprinting, et al) and differential hybridization(cDNA high density filter, cDNA microarray, oligomicrochip, et al). We used transcriptome analysis to identify therapeutic target genes by studying change of gene expression in animal models of cerebral vasospasm (1) and of hypoxia/ischemia and found novel drug target candidates through this pharmacogenomic strategy (2). We found remarkable up-regulation of heme oxygenase-1(HO-1) mRNA in the basilar artery and it might be closely related to the occurrence of delayed vasospasm after subarachnoid hemorrhage. In this report, we clearly demonstrate that intrathecal administration of antisense HO-1 oligodeoxynucleotide aggravates vasospasm, suggesting HO-1 gene induction has spasmolytic effects. Furthermore, we found the protective effects of HO-1 gene induction by endogenous or clinical compounds in cerebral vasospasm. Therapeutic gene induction of HO-1 could be a novel strategy for the prevention and treatment of Hb-induced pathologic conditions including delayed cerebral vasospasm. Our results suggest that the pharmacogenomic transcriptome analysis and pharmainformatics has the potential for strategy to define novel drug targets in various diseases (3). (1) J Clin Invest 104: 59-66, 1999. (2) J Biol Chem 276: 19921-19928, 2001. (3) J Cardiovasc Pharm 36: S1-S4, 2000.

Animals↗

PubMed1975

[Treatment of diabetic gangrene].

The results of treatment in 68 patients with vascular lesions of the lower limbs in diabetes mellitus are analysed. Fifty patients showed a necrotic and gangrenous stage of the disease. A grave form of diabetes was observed in half of them. In every case of diabetic angiopathy of the lower extremities vessels, irrespective of the gravity and stage of the process, insulinotherapy should be instituted. A complex therapy and preoperative management also include an adequate physiological diet, spasmolytics, vitamins, antibiotics according to an antibioticogram, and anticoagulants, local enzymotherapy, if indicated. In 13 cases spontaneous sequestration occurred, 31 patients were operated upon: sequestration--in 6, amputation--in 25. The operation was performed after elimination of auetonuria and ketonuria and reduction of hyperglycemia as low as 200 mg% (the latter was gained but not always). Recently, low amputations have been accomplished more frequently than before. No postoperative mortality was noted.

Adult↗

PubMed2002

[Acute renal insufficiency during pregnancy with acute pancreatitis].

According to current data the incidence of acute pancreatitis is from 1:1000 to 1:5000. Symptoms vary a lot, one of rare but most severe complications being acute renal failure. The case is a 24-year-old pregnant patients--30-th gestational week with symptoms of acute pancreatitis based most probably on hereditary hypertriglyceridemia and hypercholesterolemia. Parallel to acute inflammation of pancrease a hypercoagulation syndrome developed. It is possible that acute renal failure was caused by active thrombus formation. Because of danger for the life of mother and baby, an urgency preterm Cesarean Section was performed. Resussitation post-surgery care and drug therapy (lowmolecular anticoagulants, antibiotics, spasmolytics and analgetics, protease--inhibitors, inhibitors of protome pump, regulators and inhibitors of pancreas secretion normalize renal and pancreatic function if based on special dietary regimr. Coagulation status also normalizes.

Acute Disease↗

PubMed2002

[Hydrogen expandable implants in the treatment of stress incontinence in women--a pilot study].

OBJECTIVE: The aim of the study was to evaluate the use of new-type implants for the treatment of female urinary stress incontinence. The patients with intrinsic sphincter deficiency were also included, the other were after previous surgery for GSI. DESIGN: Original article. SETTING: Departments of Obstetrics and Gynaecology, Faculty Hospital Na Bulovce and General Faculty Hospital, 1. Faculty of Medicine, Charles University, Prague, Institute of Macromolecular Chemistry, Czech Academy of Science, Prague. METHODS: We operated 9 patients, two of them with type III (McGuire) urinary stress incontinence the rest after operations for GSI in general anesthesia. Six to nine hydrogel swelling implants were introduced into the submucosa of proximal urethra under the transrectal ultrasound guidance. We evaluated the effect 6 to 9 months after the operation. RESULTS: Two patient were dry (negative stress-test and pad-weight test), one patient had substantial improvement, 4 had mild improvement and 2 did not notice any change. We found de novo urge symptoms in four patients, two of them were of the motor type. CONCLUSION: The new type of implants reached the success rate of other currently used materials. The improvement of stress incontinence was on the cost of de novo urge symptoms in some patients. The urgency was successfully managed with spasmolytic drugs.

Female↗

PubMedDate not supplied

[Pharmacological properties of the alkaloid thalicmine].

In the course of tests conducted on anesthetized cats and dogs it was ascertained that starting with a dose of 0.5 mg/kg alkaloid talicmin depresses the tussal reflex and produces a hypotensive, spasmolytic and adrenolytic action.

Alkaloids↗

PubMedDate not supplied

Non-drug induced spasticity reduction achieved by coordination dynamic therapy in CNS injury.

In two patients with severe central nervous system (CNS) lesions it could be demonstrated that spasticity reduction can be achieved by the coordination dynamic therapy method without administration of spasmolytic drugs. The reduction of spasticity in the short- and long-term memory was measured with the coordination dynamic recording method. When performing rhythmic coordinated movements, the mainly extensor spasticity reduced in the first case in the short-term memory within 35 min of assisted exercising by approximately 68% (easy treatable case). In the second case spasticity reduced in the short-term memory within 58 min of exercising by 15 up to 28% and in the long-term memory within 6 months by 16% (difficult treatable case) as judged by the improvement of the coordination dynamics when exercising on the special coordination dynamic therapy device. Reduction of spasticity without administration of drugs could be achieved in all of the more than 100 patients undergoing coordination dynamic therapy.

Adolescent↗