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PubMed1987

A potent hypotensive factor in chicken left ventricle.

Chicken artria and ventricles both have membrane-bound granules which resemble those containing atriopeptin (ANP) in mammals. However, nothing is known about the contents of the avian granules. A previous study in chickens showed that although extracts of whole chicken heart or synthetic rat ANP both caused profound hypotension, ANP caused both natriuresis and diuresis, while chicken heart extract did not. The present study sought to locate the region(s) of chicken heart containing the hypotensive activity, and to observe the effect on sodium and water excretion and blood pressure in rats. Acid extracts of either atrium, either ventricle, ventricular septum, skeletal muscle, and liver were identically prepared from chickens and rats. Extracts were adjusted to the same protein concentration and injected (0.15 ml/kg) into anesthetized Single Comb White Leghorn roosters. Mean arterial pressure (MAP) and the time for recovery were measured. The most potent extract from chicken hearts was from the left ventricle (-38 +/- 1 mm Hg, 149 +/- 9 sec to recover). All other extracts (including right ventricle) produced only small (10-20 mm Hg), short-lived (20-30 sec) decreases in MAP. In contrast, only rat atrial extracts evoked long-lasting hypotension (greater than 40 mm Hg, recovery time greater than 200 sec). A 30-min infusion of the most potent chicken extract (left ventricle, CLV) into rats produced a small but significant natriuresis and diuresis compared to the vehicle time control (P less than 0.05) and the hypotensive response to bolus injection was about one-third that seen in the chicken. The location of potent spasmolytic activity primarily in chicken left ventricle, the different avian renal responses to chicken heart extract and synthetic rat ANP (5), and the weak diuretic, natriuretic, and hypotensive effects of CLV extract in rats all suggest that the chicken heart substance may be different from mammalian ANP.

Animals↗

PubMed2005

Evaluation of contrast-enhanced helical hydro-CT in staging gastric cancer.

AIM: To discuss the helical computed tomography (CT) characteristics of gastric cancer and evaluate the diagnostic value of contrast-enhanced helical hydro-CT (HHCT) in staging gastric cancer. METHODS: A total of 50 patients with gastric cancer were included in this study. The CT findings in them were retrospectively analyzed and correlated with pathologic findings at surgery. All patients were preoperatively imaged by plain and contrast-enhanced helical CT after orally ingesting 1,000-1,500 mL water. Peristalsis was minimized by intra-venous administration of spasmolytics. RESULTS: The foci of gastric cancer became more prominent in all the 50 patients and showed strong enhancement in contrast-enhanced HHCT. The tumor was located at the gastric cardia in 14 cases, at the gastric fundus in 3 cases, at the gastric body in 8 cases, at the gastric antrum in 4 cases, at the gastric fundus and the body in 8 cases, at the gastric body and antrum in 11 cases, and at three segments of the stomach in 2 cases. The CT features of gastric cancer were focal or diffuse mural thickening, soft tissue mass, cancerous ulcer, stenosis of stomach, infiltration to adjacent tissues, lymph node and distant metastases. Strong contrast enhancement of the gastric wall was closely related to gastric cancer. The accuracy rate of contrast-enhanced HHCT in staging gastric cancer was 86% (43/50). The detection rate of lymph node metastases by CT was 60% (12/20). CONCLUSION: Contrast-enhanced HHCT is a reliable method to diagnose and stage gastric cancer.

Adenocarcinoma↗

PubMed2002

A review of the French maritime pine bark extract (Pycnogenol), a herbal medication with a diverse clinical pharmacology.

OBJECTIVES: An increasing body of evidence indicates that Pycnogenol (PYC), a standardized extract of French maritime pine bark, has favorable pharmacological properties. This is a review of studies with both PYC and components of the preparation, that have helped to elucidate target sites and possible mechanisms for activity in men. METHODS: Studies appearing in peer reviewed literature, as well as results presented at international meetings not yet available as published papers, are included in this review. Additional data from published sources in German and French languages that are not widely available are also included. RESULTS: Chemical identification studies showed that PYC is primarily composed of procyanidins and phenolic acids. Procyanidins are biopolymers of catechin and epicatechin subunits which are recognized as important constituents in human nutrition. PYC contains a wide variety of procyanidins that range from the monomeric catechin and taxifolin to oligomers with 7 or more flavonoid subunits. The phenolic acids are derivatives of benzoic and cinnamic acids. The ferulic acid and taxifolin components are rapidly absorbed and excreted as glucuronides or sulphates in men, whereas procyanidins are absorbed slowly and metabolized to valerolactones which are excreted as glucuronides. PYC has low acute and chronic toxicity with mild unwanted effects occurring in a small percentage of patients following oral administration. Clinical studies indicate that PYC is effective in the treatment of chronic venous insufficiency and retinal micro-hemorrhages. PYC protects against oxidative stress in several cell systems by doubling the intracellular synthesis of anti-oxidative enzymes and by acting as a potent scavenger of free radicals. Other anti-oxidant effects involve a role in the regeneration and protection of vitamin C and E. Anti-inflammatory activity has been demonstrated in vitro and in vivo in animals. Protection against UV-radiation-induced erythema was found in a clinical study following oral intake of PYC. In asthma patients symptom scores and circulating leukotrienes are reduced and lung function is improved. Immunomodulation has been observed in both animal models as well as in patients with Lupus erythematosus. PYC antagonizes the vasoconstriction caused by epinephrine and norepinephrine by increasing the activity of endothelial nitric oxide synthase. Dilation of the small blood vessels has been observed in patients with cardiovascular disease, whereas in smokers, PYC prevents smoking-induced platelet aggregation and reduces the concentration of thromboxane. The ability to inhibit angiotensin-converting enzyme is associated with a mild antihypertensive effect. PYC relieves premenstrual symptoms, including abdominal pain and this action may be associated with the spasmolytic action of some phenolic acids. An improvement in cognitive function has been observed in controlled animal experiments and these findings support anecdotal reports of improvement in ADHD patients taking PYC supplements. CONCLUSIONS: There is much evidence showing that PYC has beneficial effects on physiological functions. Results from ongoing clinical research are required to confirm and extend previous observations.

Antioxidants↗

PubMedDate not supplied

Central action of ergometrine.

Ergometrine, a spasmolytic which also stimulates dopamine receptors, was investigated as a potential central stimulant. It did not influence the locomotor activity of normal rats and mice, and in high doses even depressed it. The locomotor activity depressed by reserpine, spiroperidol, and pimozide was elevated by ergometrine. Ergometrine antagonized neuroleptic-induced catalepsy and abolished ptosis and hypothermia produced by reserpine. Given alone ergometrine depressed the body temperature in rats and mice, and this effect was abolished by pimozide in both species, and by spiroperidol and haloperidol in mice. The hypothermia was not antagonized by atropine. In several respects the central action of ergometrine resembles that of apomorphine.

Animals↗

PubMed1976

Pharmacology of dihydroxy-dibutylether, a specific choleretic drug.

The choleretic and the general pharmacological properties of dihydroxy-dibutyl ether (Discinil) were investigated in several animal species. Discinil (DHBE) increased the bile flow in conscious rats and dogs, after both oral and i.v. administration. A choleretic effect was also observed after i.v. injection into anaesthetized rats and guinea pigs. A dose-response relationship was always obtained, the threshold dose being 25--100 mg/kg. No evidence of tachyphylaxis was observed in rats after repeated treatments. The bile hyperflow was generally accompanied by an increased excretion of the total dry residue in guinea pigs and dogs. The choleretic effect in rats was still present after pretreatment with either DL-ethionine (causing parenchymal liver damage) or atropine (blocking the cholinergic control of bile production). At low doses (25--100 mg/kg i.v.) eliciting a definite choleretic response, DHBE did not show spasmogenic and spasmolytic effects in vivo on the smooth muscles of the gallbladder of guinea pigs and dogs, neither on the stomach and intestine of mice and dogs; while it constricted the pylorus sphincter of rats. At larger doses (200--400 mg/kg i.v.) the compound showed a mild relaxing activity on Oddi's sphincter of guinea pigs and a weak spasmogenic activity either on gall bladder or on small intestine. In vitro, it caused an unspecific antagonism against the spasm induced by acetylcholine, barium chloride, histamine, 5-hydroxytryptamine and norepinephrine. In anaesthetized rats, rabbits and dogs, DHBE caused a moderate and short-lasting hypotension, and tachycardia. The threshold doses for these effects were 2--4 times superior to those being choleretic. In conscious dogs, the compound was slightly hypertensive. DHBE did not provoke important respiratory and ECG changes, neither showed diuretic nor antiphlogistic effects.

Administration, Oral↗

PubMed1976

Synthesis and pharmacological study of diphenylalkylamines with cycloaliphatic residues. New coronary vasodilators.

The paper describes the synthesis and the pharmacological evaluation of some derivatives of prenylamine, all with a cycloaliphatic ring within or instead of the isopropylamine moiety. Their general formulas are: (C6H5)2CH-CH2-CH2-NH-CH-CH2-R CH2 (I) (C6H5)2CH-CH2-CH2-NH-R' (II) where R contains and R' is a cycloaliphatic ring. Several compounds and particularly those of formula (I), and of formula (II), where the alicyclic ring had a bulky substituent in para were more active than prenylamine as coronary vasodilators on isolated guinea-pig heart (Langendorff). The most interesting derivative was M.G. 8926 [N-(3,3-diphenylpropyl)-alpha-methyl-beta-cyclohexylethylamine], which was more active than prenylamine on Langendorff's heart and in enhancing the pressor response to catecholamines and inhibiting the isoprenaline induced hypotension. Moreover, it had almost the same effects as prenylamine as spasmolytic, local and general anesthetic, on heart rate and arterial pressure and against coronary spasm from pitressin.

Animals↗

PubMed1976

[On the mode of action of heptaminol (author's transl)].

The effect of heptaminol, an aliphatic amine with an alcoholic group on carbon 2, on sympathetic nerves and on isolated chromaffine granules was infestigated. In cats, heptaminol caused long-lasting, dose-dependent pressor effects accompanied by tachycardia and contractions of the nictitating membrane. In comparison with tyramine, heptaminol was 100 times less potent in increasing blood pressure and 10 times less effective in inducing contractions of the nictitating membrane. The rise in blood pressure as well as tachycardia and contraction of the nictitating membrane were diminished by cocaine. After pretreatment with cocaine, heptaminol in high doses caused short-lasting depressor effects. Also in rats the pressor effect of heptaminol was weaker but of longer duration than that of tyramine. The dose-response curve was depressed by pretreatment with reserpine. The tachycardia induced by heptaminol was markedly diminished after pretreatment with reserpine. After repeated injections heptaminol reduced the norepinephrine content of the rat heart by 20-40%, Tyramine and hexylamine were more effective than heptaminol in depleting the norepinephrine stores of the heart (50-60%). In fluorescence microscopic investigations on sympathetic nerves (rat iris) depleted of norepinephrine by reserpine, the uptake of alpha-methylnorepinephrine could be inhibited or prevented by heptaminol. The spontaneous release of catecholamines from isolated bovine chromaffine granules was enhanced (+30%) by heptaminol or methamphetamine in high concentrations. In lower concentrations, however, both drugs reduced the uptake of 14C-epinephrine in isolated medullary granules by 20-40%. In addition a non-specific papaverine-like spasmolytic effect of heptaminol could be demonstrated. The results suggest that heptaminol exerts its pharmacological action by interfering with release and uptake of norepinephrine.

Adrenal Medulla↗

PubMed1999

Identification of a metaplastic cell lineage associated with human gastric adenocarcinoma.

Metaplastic cell lineages arising in response to chronic injury are precursors for the evolution of dysplasia and adenocarcinoma. Although a subtype of intestinal metaplasia has been associated with gastric adenocarcinoma, the link between this lineage and the evolution of gastric adenocarcinoma has remained unclear. Wang et al (1998) have reported that an aberrant metaplastic cell lineage with morphological characteristics similar to Brunner's glands of the duodenum develops in the fundic mucosa of mice infected with Helicobacter felis. This metaplastic lineage expresses the trefoil peptide spasmolytic polypeptide (SP). Given the epidemiological association of Helicobacter species infection with gastric cancer, we hypothesized that this SP-expressing metaplastic (SPEM) lineage may represent a precursor to or appear commensurate with gastric adenocarcinoma. The SPEM lineage was present in 68% of fundic biopsies from patients with fundic Helicobacterpylori-associated gastritis, but was absent in biopsies of fundic mucosa from patients without H. pylori infection. In a review of archival samples from 22 resected gastric adenocarcinomas, we found the SPEM lineage in 91% of cases, typically located in mucosa adjacent to the carcinoma or areas of dysplasia. Importantly, 59% of resections showed SP immunoreactivity within dysplastic cells. These data indicate a strong association of the SPEM lineage with both chronic H. pylori infection and gastric adenocarcinoma.

Adenocarcinoma↗

PubMed1999

[Preterm premature rupture of membranes in the 19th week of pregnancy. A clinical case].

A case of premature rupture of membranes occurred at 19 weeks of pregnancy is reported. The patient underwent a genetic amniocentesis at 16 weeks of gestational age. During the hospitalization period, she presented amniotic fluid leakage responsible of olygohidramnios. She was treated with antibiotic, spasmolytic, tocolytic and cortisone therapy. All subsequent parameters were evaluated: blood cell count, heart rate frequency, body temperature. Ultrasound examinations were performed every two weeks. Cervical smears to detect infections were normal. Labour started at 28 weeks and the patient delivered spontaneously a 1010 g male baby, Apgar 4/8. The heaviest complication was a cerebral hemorrhage and the subsequent frontoparietal hematoma which progressively reduced. To date the neurological prognosis is good.

Amniocentesis↗

PubMed1999

[Treatment of different types of pain].

Accurate assessment of pain is the key to appropriate analgesia. This necessitates not only an understanding of the organic component, but also a comprehension of the role played by the mental, social and spiritual dimensions in the individual patient's suffering. It implies that the entire care team must be involved in pain management. The nature of a patient's pain is one predictor of the response to treatment. It is mainly characterized by its location, intensity, extent, timing and type (excessive nociception, neurogenic, or mixed), the circumstances in which it appears, and any accompanying signs. The choice of analgesic for treating pain due to excessive nociception was greatly facilitated by the introduction of the WHO three-step approach. Better knowledge of the pharmacological and pharmacokinetic properties of the different analgesics has contributed to increase their efficacy and tolerability. Certain types of pain of neurogenic origin respond poorly to both opiate and non opiate analgesics. They can be treated with other drugs whose mechanisms of action in pain relief are not fully understood. They include the following; antidepressants (amitriptyline, nortriptyline, desipramine and doxepine); anticonvulsants (carbamazepine, phenytoin, valporic acid and clonazepam); antiarrhythmic agents (lidocaine, mexiletine, flecainide and tocainide). The unwanted effects of these different treatments, together with psychological disturbances induced by the underlying disease, can call for the use of antiemetics, laxatives, spasmolytics, glucocorticoids and psychotropic agents (anxiolytics, neuroleptics and antidepressants). Finally, in many cases, better pain relief is obtained by combining drug-based therapy with other interventions such as radiation therapy, neurosurgery, and psychological/behavioral approaches. All these means must be chosen and used according to each individual patient's needs. Pain must be considered as a disease that can and must be eliminated or at least attenuated.

Analgesics, Non-Narcotic↗

PubMed1999

[Plantain (Plantago lanceolata L.): anti-inflammatory action in upper respiratory tract infections].

Plantain (Plantago lanceolata L.) is used for the therapy of infections of the upper respiratory airways. While only few clinical data are available, results of experimental research confirm e.g. antiinflammatory, spasmolytic and immunostimulatory actions. A positive benefit-risk-ratio allows the recommendation of plantain in moderate chronic irritative cough, also especially for children.

Adult↗

PubMed1999

[Pseudopolymorphism of NO-SPA, 1-(3,4-diethoxy-benzyl)-6,7-diethoxy-3,4-dihydro-isoquinoli ne hydrochloride].

The spasmolytic agent No-Spa, 1-(3,4-diethoxybenzyl)-6,7-diethoxy-3,4-dihydroisoquinoli ne hydrochloride (1) is a synthetic analogue of the naturally occurring alkaloid papaverine. (1) is prone to form stoichiometric crystalline solvates with a number of solvents causing technological and stability problem. Present paper describes the X-ray structure determination of the hemiethanol, hemibenzene and hemihydrochloride structures being the most important and interesting from both practical and theoretical point of view. The solvate formation is facilitated by the presence of the flexible ethoxy group encapsulating the solvent and by the quasi perpendicular position of the isoquinoline and phenyl group.

Crystallography, X-Ray↗

PubMed1999

Nifedipine is not feasible for biliary pain in patients with gallbladder stones.

OBJECTIVE: Biliary pain is generally treated with NSAIDs and spasmolytics, but some patients do not tolerate them. Nifedipine has been suggested to have some analgesic effect and it has been used successfully in many painful smooth muscle disorders. Our aim was to evaluate the effect of nifedipine for biliary colics and gallbladder volume. PATIENTS AND METHODS: Twenty-seven patients suffering from uncomplicated symptomatic gallbladder stones were prospectively randomized to receive either oral nifedipine (10 mg 3 times daily) or placebo in a double-blind manner. Liver chemistry and ultrasonography were examined before and after the 8-week study period. The patients completed each day a diary of their pain, headache, palpitation, burning feeling in skin, dizziness, and their use of painkillers. RESULTS: Biliary pain seemed to be less intensive and shorter in duration, but without statistical significance, whereas headache tended to be more common (p = 0.077) in nifedipine group than that in placebo group. This difference would have reached statistical significance with over 155 patients randomized. Overall additional drug use was similar in both groups, and was increased in nifedipine group for headache (p = 0.05). The fasting gallbladder volume tended to decrease (p = 0.085) during the nifedipine treatment but not with placebo. Serum liver chemistry remained within normal range. CONCLUSIONS: This small study shows that nifedipine may decrease slightly biliary pain intensity and duration, and contrary to previous findings in healthy volunteers, it seems to decrease resting gallbladder volume in patients with symptomatic uncomplicated gallbladder stones, but did not reduce the need of traditional pain medication partly because of increased need for headache. Thus it is not a feasible choice for routine use against biliary pain in symptomatic gallbladder stones, which is why the study was not continued to reach statistical significance in respect to biliary pain.

Adult↗

PubMed1999

[Drug treatment of gestational arterial hypertension in medical institutions of Russia (population study)].

AIM: To evaluate current situation with administration of drugs against gestational arterial hypertension (GAH) in medical institutions of Russia. MATERIALS AND METHODS: A population study in representative territories of European Russia has been performed to investigate current practice of GAH chemotherapy as compared to chronic arterial hypertension (CAH). RESULTS: In spite of shorter duration, GAH treatment employed two times greater amount of medicines per a course than chemotherapy of CAH. Injections and infusions were practiced in GAH 4.6 and 4.3 times more frequently than in CAH, respectively. Most popular drugs for injection were spasmolytics dibasol, papaverin solution, magnesium sulphate solution, for oral administration--clonidin. Specific antihypertensive medicines and beta-blockers dominated in CAH; infusions, sedatives and diuretics were used less frequently. In GAH infusions of plasma substitutes was widely practiced without adequate antihypertensive treatment. CONCLUSION: Management of pregnant women with hypertension overuses medicines. However, new effective antihypertensive medicines are not infrequently ignored. This fact can provoke further elevation of blood pressure and eventually result in preterm delivery. It is necessary to develop national standard of drug treatment of pregnant women with hypertension.

Academies and Institutes↗

PubMedDate not supplied

[A case of neurogenic dysphagia responding to nitrates].

We described a 47-year-old man with ischemic stroke who developed a brainstem syndrome with persistent dysphagia. He was fed by the nasogastric tube placed intermittently by himself for almost 7 months after the stroke. Elective feeding via percutaneous endoscopic gastrostomy (PEG) was not accepted by the patient. All treatment attempts with benzodiazepines, antidepressants and spasmolytic agents were unsuccessful. Videofluoroscopic investigation revealed excessive and long-lasting spasm of the upper esophageal sphincter which was associated with the massive aspiration of the contrast. The patient dramatically improved after treatment with nitroglycerin and long-acting nitrates with almost complete recovery of normal swallowing. A strikingly good effect of nitrates in the treatment of oropharyngeal dysphagia is emphasized by the authors.

Brain Ischemia↗

PubMed2000

[Endovascular occlusion and percutaneous treatment of vasospasm].

Current available minimal invasive endovascular technology allows for percutaneous treatment of cerebral aneurysms and of vasospasm, the associated disease fo cerebral arteries secondary to subarachnoid hemorrhage. Multicentric evaluation of standardized treatment techniques using platinum coils have shown that a high success rate is now obtained for certain forms of aneurysms, mostly those which have a small base (4 mm or less) of implantation of the vessel. Treatment of arterial vasospasm by techniques including angioplasty using soft silicon balloons, or intraarterial application of spasmolytics, or both may be very successful, when performed prior to establishment of irreversible ischemic damage to the brain tissue. An intensive patient monitoring during the posthemorrhagic period is therefore critical for the correct timing of such a procedures.

Constriction↗

PubMed2000

[Sulpiride treatment of irritable colon syndrome].

A blind placebo-controlled randomized trial was made of efficiency and safety of sulpirid compared to basic treatment in irritable colon syndrome (ICS). 40 patients over 18 years with ICS were randomized into two groups. Group 1 patients received sulpirid monotherapy (200-450 mg/day). Group 2 received basic therapy (combined treatment with spasmolytic, bacterial and cholagogic drugs). The treatment took 6 weeks. It was proved that sulpirid is more effective in ICS as it reduced the syndrome by 85% (basic therapy by 10%), relieved abdominalgia, anxiety, depression, corrected stool. As to disbacteriosis, sulpirid effect was weak. Tolerance of treatment in both groups was good. Side effects developed in 15% of group 1 patients and were easily corrected by lowering of the daily dose.

Adolescent↗

PubMed2000

[The immunomodulating properties of pharmacological preparations].

According to the analysis of literary data there are immunomodulating properties in the drugs that are used with different purposes: in tranquilizers, neuroleptics, stimulators of central nervous system, nonsteroid antiinflammatory agents, azole group, spasmolytics, sulphur and selenium compounds, blockers of calcic canals and other compounds. During the clinical application of pharmaceutic drugs it is necessary to consider their immunotropic properties as a side effect. Besides, the immunostimulating action of the above-mentioned compounds permits to use them in prophylaxis and treatment of different immunodeficient states.

Adjuvants, Immunologic↗