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At least 1,765 records · Page 98Linked to original sources
PubMed1996

[Effects of histamine H2-receptor blockers and dalargin on reparative processes gastroduodenal mucosa in patients with duodenal ulcer].

The effect of synthetic opiate peptide dalargin, histamine H2-receptors blockers (cimetidin, famotidin) and combination of dalargin with famotidin on proliferative activity of gastroduodenal mucosal epithelium has been studied autoradiographically (3H-thymidine) in 75 patients with duodenal ulcer. Compared to spasmolytics and antacids, the studied drugs (dalargin, cimetidin and famotidin) significantly increased the number of DNA-synthetizing cells in the epithelium of fundal stomach, duodenal cap and ulcer borders. Maximal effect was noticed in combined use of dalargin and famotidin. A correlation existed between clinical and stimulating reparative effect of the drugs.

Adolescent↗
PubMed1997

Cerebrovascular selectivity and vasospasmolytic action of the novel calcium antagonist (+/-)-(E)-1-(3-fluoro-6, 11-dihydrodibenz[b,e]oxepin-11-yl)-4-(3-phenyl-2-propenyl)-piperazine dimaleate in isolated cerebral arteries of the rabbit and dog.

The cerebrovascular selectivity and vasospasmolytic action of AJ-3941 ((+/-)-(E)-1-(3-fluoro-6, 11-dihydrodibenz[b,e]oxepin-11-yl)-4-(3-phenyl-2-propenyl)-p iperazine dimaleate. CAS 143110-70-7), a new calcium antagonist, were studied in isolated rabbit and dog arterial preparations. In rabbit arterial ring preparations, AJ-3941 dose-dependently inhibited the contractions of various arteries caused by high K(+)-depolarization (high K+) and prostaglandin F2 alpha (PG). The inhibitory potency of AJ-3941 varied in different arteries, in descending order as follows: high K+: basilar > coronary > femoral > renal > mesenteric artery, PG: basilar > coronary > > femoral and renal artery. The median inhibitory concentration (IC50) in the basilar artery was over 40 times lower than that in the mesenteric or femoral artery for which the weakest inhibition in the examined arteries was observed. This selective action of AJ-3941 for cerebral artery was also observed in the frontal and middle cerebral arteries of dogs. The selectivity for the rabbit basilar artery was higher than those of flunarizine and nicardipine. Additionally, the contractile response of the rabbit basilar artery induced by phorbol 12,13-dibutyrate (PDBu), an activator of protein kinase C (PKC), was greater than those of the arteries examined such as the coronary, femoral and mesenteric arteries. The response in the basilar artery was greatly reduced in Ca(2+)-free medium, while this was not the case in other arteries. AJ-3941 as well as H-7, an inhibitor of PKC, potently inhibited PDBu-induced contractile response in the basilar artery in the presence, but not in the absence of Ca2+ in the medium, whereas the existing calcium antagonists, diltiazem and nicardipine, did not inhibit the contractile response in both conditions. These results suggest that the PKC-dependent system which is mediated by influx of extracellular Ca2+ profoundly contributes to the contraction of the cerebral artery and that the cerebroselective-vasodilating effect of AJ-3941 may depend, at least partly, on the inhibition of the PKC-mediated contractile response. In rabbit basilar arteries, AJ-3941 caused a dose-dependent inhibition of the contraction induced by various vasospasmogens, such as endothelin-1 (ET), arachidonic acid, 15-hydroperoxy-eicosatetraenoic acid and the thromboxane A2-mimetic U-46619. Furthermore, when isolated basilar arteries of the dog were perfused intraluminally with AJ-3941 at the concentration that inhibits high K(+)- or PG-induced contraction in the rabbit basilar artery, AJ-3941 effectively antagonized the vasospasm induced by extraluminal application of PG or ET. However, when flunarizine, nicardipine, diltiazem or verapamil was used for intraluminal perfusion of the same preparations, none of these drugs exerted spasmolytic effect. These results indicate that AJ-3941 has cerebrovascular selective-vasospasmolytic action, and consequently is thought to be effective in cerebrovascular disorder such as vasospasm following subarachnoid hemorrhage.

Animals↗
PubMed1996

[Lipid metabolism in women with threatened abortion].

The study group consisted of 130 subjects: 50 healthy nonpregnant, 35 healthy women in the I trimester of gestation (gestational age 6-15 weeks) and 45 patients with symptoms of threatened abortion (the same gestational age). In the latter group pain and bleeding ceased after hormonal treatment and spasmolytic drugs. Serum blood concentration of following compounds were determined: total lipids, LDL fraction, total cholesterol, phospholipids, triglycerides, HDL and LDL cholesterol fractions. Threatened abortion had changed lipids profile; diminished concentrations of LDL fraction, total cholesterol, LDL cholesterol fraction and phospholipids were observed. Levels of total lipids, phospholipids and triglycerides++ in blood serum of healthy pregnant women in the I trimester of gestation were higher than in nonpregnant women.

Abortion, Threatened↗
PubMed1976

[Pharmacological investigations with the combination sulfamoxole/trimethoprim, a new broadspectrum chemotherapeutic agent (author's transl)].

Investigations were conducted with the combination of N1-(4,5-dimethyl-2-oxazolyl)-sulfanilamide (sulfamoxole) and 2,4-diamino-5-(3,4,5-trimethoxy-benzyl)-pyrimidine (trimethoprim) (CN 3123, Nevin, Supristol) in a dose ratio of 5:1, with respect to pharmacological activity and possible side effects. The effects obtained with the combination CN 3123 were compared with those of the single substances. In a dose range comparable to that as used in clinical treatment, there were no effects on cardiovascular or respiratory functions, on functions of autonomic and central nervous system, on contractility of smooth muscles and on data of clinical chemistry such as urine and electrolyte excretion, blood sugar, blood coagulation and liver function tests. Doses which are 5 to 10 times higher than the initial dose or 10 to 20 times higher than the maintenance dose used in man caused an increase of urine and sodium excretion without influencing potassium and chloride output. There were no signs of sedation as alteration of motility or EEG patterns, but in mice and rats there was an increase in both duration and depth of anaesthesia caused by barbiturates or ether. Only in a dose range 30 to 40 times higher than the initial dose for man there were some slight alterations with respect to cardiovascular system and liver function tests. In vitro, with high concentrations of CN 3123 there was a weak, unspecific spasmolytic effect on the isolated ureter and an increase in the refractory period of the guinea pig atrium. There were no hints that the side effects seen with separate administration of high or very high doses of sulfamoxole or trimethoprim were increased or poteniated by their simultaneous administration. Slight side effects in animals were only observed with doses exceeding the tenfold of the doses for therapeutic use in men. Therefore, the therapeutic range of CN 3123 seems to be more than adequate.

Animals↗
PubMed1998

A fluid-filled condom causing intestinal obstruction: nonsurgical therapy of an ileus by ultrasound-guided transabdominal tapping.

Ingested foreign bodies are rare causes of intestinal obstruction in the adult. Condoms, if swallowed, are usually filled with drugs and found in body packers as a vehicle for drug smuggling. We report the case of 31-year-old male who presented with symptoms and signs of intestinal obstruction. He had swallowed a fluid-filled condom the day before. Ultrasonography of the abdomen revealed a fluid-filled foreign body within the small bowel. Due to radiological signs of an ileus and due to the fact that the patient's symptoms did not resolve after spasmolytic therapy the condom was tapped transcutaneously under ultrasonographical guidance. This procedure immediately relieved his symptoms. The further course was uneventful.

Abdominal Pain↗
PubMed1998

[The characteristics of the clinical manifestations and treatment of chronic obstructive bronchitis in patients with hepatobiliary system diseases and pseudoallergy].

Routine clinical, laboratory, instrumental and immunological examinations in 105 patients have established that hepatobiliary disorders occur 2.2 times more frequently in patients with chronic obstructive bronchitis (COB) and pseudoallergy than in those without pseudoallergy. To correct negative effects of pseudoallergy, conventional therapy was combined with enterosorbent polyphepan, spasmolytic nospa and cholagogic allochol used alone or in different combinations. The highest benefit for COB patients was achieved in using combination of polyphepan + nospa + allochol.

Adult↗
PubMed1998

The analgesic effect of intravenous tenoxicam in symptomatic treatment of biliary colic: a comparison with hyoscine N-butylbromide.

This was conducted to evaluate the analgesic effect of intravenous tenoxicam (non-steroidal anti-inflammatory drug) in the treatment of biliary colic pain and compared with spasmolytics. Thirtytwo patients (26 women, 6 men, mean age 47, range 38-55 years) with acute biliary colic were entered for study. They were allocated randomly to receive either tenoxicam 20 mg i.v. or hyoscine N-butylbromide 20 mg i.v. The patients recorded their pain severity on 5 point scale. The results showed that tenoxicam caused significant pain relief in 10 out of 16 patients at 30 min (mean pain score decreased from 2.75 +/- 0.93 to 0.49 +/- 0.51, p < 0.05) and in other 4 patients at 60 min (mean pain score decreased to 0.58 + 5.7, p < 0.05). None of these patients developed acute cholecystitis or pain relapse over a period of 24 h follow up. With use of hyoscine N-butylbromide, 7 out 16 patients had significant pain relief at 30 min (mean pain score decreased from 2.62 +/- 1.01 to 0.57 +/- 0.53, p < 0.05) and 3 other patients relieved at 60 min (mean pain score decreased to 0.66 +/- 0.57, p < 0.05). Four patients showed pain relapse within 24 h and needed pethidine-rescue treatment, two of them developed acute cholecystitis. Three out of 6 patients who showed no response to hyoscine N-butylbropmide and treated with 100 mg pethidine progressed to acute cholecystitis. We concluded that intravenous tenoxicam has rapid and prolong analgesic effects in the treatment of acute biliary colic as compared to hyoscine N-butylbroimde and it prevents the progression to acute cholecystitis.

Acute Disease↗
PubMed1998

[The use of Spasmomen (otilonium bromide) in pediatrics].

Spasmomen is an affective medicinal substance for treating functional pathologies of digestive organs in children. The above drug is well tolerated, with no adverse events or complications being associated with its intake. Spasmomen as a drug having spasmolytic effect can be recommended for use in pediatric practice for treating children in all age brackets.

Abdominal Pain↗
PubMed1998

Interference of myrtol standardized with inflammatory and allergic mediators.

Myrtol standardized (Gelomyrtol/Gelomyrtol forte) inhibits the activity of 5-lipoxygenase of human basophil and eosinophil leukocytes and the formation of leukotriene C4 as well as 1.8-cineole (eucalyptol). An increase of prostaglandins (PGE2) in mucous membranes of teat cisterns after topical administration of TPA (tetradecanoylphorbol-13-acetate) was inhibited. In vitro and in vivo studies revealed spasmolytic and broncholytic effects of Myrtol stand. After topical administration into the teat cisterns of the isolated bovine udder Myrtol stand. increased the surface temperature, comparable to effects of menthol.

Animals↗
PubMedDate not supplied

[Effect of imipramine and ftoracizin on platelet aggregation and smooth muscle contraction of the ureter].

The influence of the tricyclic antidepressants imipramine and ftoracizin on platelet aggregation and smooth muscle contractility was investigated in comparison with action of known smooth muscle relaxant and platelet aggregation inhibitor, papaverine. It has been shown that the tricyclic antidepressants possess potent spasmolytic activity but unlike papaverine have no effect on platelet aggregation. The biochemical mechanisms of the non-specific action of tricyclic antidepressants as well as some other structurally related-drugs are discussed.

Animals↗
PubMed1976

Pharmacological studies on a new 1-benzoyloxy-alkylaminocycloalkane derivative (YAU-17) with special reference to its mucosa anesthetic activity.

A new compound, dl-cis-1-benzoyloxy-2-dimethylamino-1,2,3,4-tetrahydronaphthalane (YAU-17) was found to produce sciatic nerve block, corneal and intradermal anesthesia in guinea-pigs, which markedly exceeded the effect of procaine and lidocaine. YAU-17, when given orally to mice, was much less toxic than any other drugs tested, though YAU-17 showed a considerably high acute toxicity by i.v. route. Oral administration of YAU-17 was effective in antagonizing the emetic response of dogs to intragastric phenylalanine isopropyl ester, but produced no distinct inhibition against vomiting elicited by oral copper sulfate. Furthermore, it possessed a spasmolytic activity which was comparable to that of papaverine, and showed an effect of suppressing the mucosal intrinsic reflex in the dog intestine. These pharmacological properties of YAU-17 were qualitatively similar to those of oxetacaine which was used as one of the reference compounds.

2-Naphthylamine↗