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PubMed1988

The effects of glucagon and glucagon-(1-21)-peptide on antroduodenal motility in healthy volunteers.

Since it has been argued that the spasmolytic effect of glucagon is related to the first 21 N-terminal amino acid residues, and not to the complete molecule, we have compared the effects of glucagon-(1-21)-peptide (G-(1-21) and glucagon on human antroduodenal motility. Glucagon and G-(1-21) were given as bolus injections to 30 healthy volunteers equally allocated into five groups. Each subject received two doses; one was placebo, 0.25, 0.5, 1.0 or 2.0 mg of glucagon, the other was an equimolar doses of G-(1-21) (placebo, 0.175, 0.35, 0.70 or 1.4 mg of G-1-21). The first injection was given during phase II of a migrating motility complex (MMC), and the next during the following phase II. Contractile activity was recorded using an oral tube with one sidehole positioned in the antrum and two in the duodenum. We confirmed that glucagon decreases the number of contractions in the antrum and duodenum and that normal phase II activity was restored within 20-40 minutes proportionally to the amount of the drug given. G-(1-21) did not change antroduodenal motility nor did it affect the phase II pattern in any of the groups. Neither were any side effects encountered. G-(1-21) does not seem to be an alternative to glucagon and other spasmolytic drugs for obtaining relaxation of the antroduodenal area.

Adult↗
PubMedDate not supplied

Perfusion--fixation of human kidneys for ultrastructural analysis.

Surgically removed human kidneys were fixed by vascular perfusion to improve the preservation of renal tissue and, in particular, the proximal tubules for electron microscopic analysis. Fifty kidneys with various pathologic changes were perfusion-fixed with glutaraldehyde under pressure control immediately after nephrectomy. A Tyrode solution containing a spasmolytic drug initiated the perfusion. The results demonstrate that large volumes of ultrastructurally well-preserved kidney tissue can be obtained in normal (nontumorous) parts of tumor kidneys as well as in kidneys with chronic nephropathy. Several factors improved the quality of fixation: (1) start of perfusion-fixation within 15 min after clamping of the renal vessels, (2) careful handling of the kidney during nephrectomy, (3) simultaneous clamping of the main renal vessels, and (4) employment of a spasmolytic drug. In comparison with tissue from immersion-fixed renal biopsies, perfusion-fixed kidneys represented an improved basis for ultrastructural investigations of normal or pathologically changed human kidney tissue.

Histological Techniques↗
PubMed1985

Cyanide and sulfide interact with nitrogenous compounds to influence the relaxation of various smooth muscles.

Sodium nitroprusside relaxed guinea pig ileum after the segment had been submaximally contracted by either histamine or acetylcholine, intact isolated rabbit gall bladder after submaximal contraction by either acetylcholine or cholecystokinin octapeptide, and rat pulmonary artery helical strips after submaximal contraction with norepinephrine. In each of these cases the relaxation produced by nitroprusside was at least partially reversed by the subsequent addition of excess sodium cyanide. Cyanide, however, in nontoxic concentrations did not reverse the spasmolytic effects of hydroxylamine hydrochloride, sodium azide, nitroglycerin, sodium nitrite, or nitric oxide hemoglobin on guinea pig ileum, nor did cyanide alone in the same concentrations have any effect. The similar interaction between nitroprusside and cyanide on rabbit aortic strips is not dependent on the presence of an intact endothelial cell layer. Also, on rabbit aortic strips and like cyanide, sodium sulfide reversed the spasmolytic effects of azide and hydroxylamine, but it had little or no effect on the relaxation induced by papaverine. Unlike cyanide, however, sulfide augmented the relaxation induced by nitroprusside, and it reversed the effects of nitric oxide hemoglobin, nitroglycerin, and nitrite. A direct chemical reaction between sulfide and nitroprusside may account for the difference between it and cyanide. Although evidence was obtained also for a direct chemical reaction between sulfide and norepinephrine, that reaction does not seem to have played a role in these results. These observations suggest the existence of at least three distinct subclasses of so-called nitric oxide vasodilators. At least in some cases cyanide and sulfide cannot be acting by the same mechanism in their modifications of the responses to the agonists.

Acetylcholine↗
PubMedDate not supplied

The efficacy and tolerability of triclabendazole in Cuban patients with latent and chronic Fasciola hepatica infection.

Current chemotherapy for the treatment of infections caused by the liver fluke Fasciola hepatica is not satisfactory. Therefore, the efficacy and tolerability of triclabendazole (TCZ) was assessed for this indication. Eighty-two patients (51 female, 31 male, age 15-81 yr, mean 42 yr) with chronic or latent F. hepatica infection refractory to previous anti-helminthic chemotherapy were enrolled in a 60-day open, non-comparative trial. Patients received 20 mg/kg TCZ as two doses of 10 mg/kg administered after food 12 hr apart. Efficacy of treatment was assessed by stool microscopy, determination of Fasciola excretory-secretory antigen (FES) in feces, and by ultrasonography (US) which were systematically performed pre-therapy and on Days 1-7, 15, 30, and 60 post-therapy. For continuous safety assessment, patients were hospitalized during the first week after therapy and then monitored at home for the appearance of any adverse events. Clinical chemistry and hematology tests were carried out on Days 1, 3, 7, 15, and 60, and whenever an adverse effect occurred possibly related to therapy. Seventy-one (92.2%) of the 77 patients who completed the 60-day follow-up period became egg-negative. Efficacy of therapy was supported by the disappearance or decrease of FES antigen and of ultrasonography abnormalities. In the 6 remaining patients, parasitological cure was achieved by another single TCZ dose of 10 mg/kg on Day 60. A total of 74 adverse events possibly related to therapy was reported by 54 patients. The most important adverse event was colic-like abdominal pain (40 patients [49%]) consistent with the expulsion of the parasite through the bile ducts as confirmed by US on Days 2-7. Most adverse events (53) were graded as mild, 20 as moderate, and only 1 as severe (a biliary colic responding to spasmolytic therapy within two hours). Triclabendazole 20 mg/kg is an effective therapy for the treatment of F. hepatica infection in patients who have failed to respond to other antihelminthic agents. Biliary colics reflecting the expulsion of dead or damaged parasites usually occur during Day 3-7 and respond well to spasmolytic therapy.

Adolescent↗
PubMed2002

[Spasticity treated with selective posterior rhizotomy].

BACKGROUND: Spasticity is often seen in patients with central nervous lesions. Some patients with severe spasticity are not optimally treated with physiotherapy and medication. MATERIAL AND METHODS: We present a case history of a 41-year-old woman with multiple sclerosis and severe painful spasticity in her lower limbs. Her spasticity did not respond to treatment with physiotherapy, spasmolytic medication, botulinum toxin A, intrathecal baclofen or epidural spinal cord stimulation. RESULT: The patient was treated with selective posterior rhizotomy S1-L1. Section of 60% of the rootlets on the right side and 40% on left the side resulted in a good outcome with less spasticity and pain. Finally her contractures were treated with tenotomy and myotomy, also with good functional result. INTERPRETATION: Patients suffering from severe painful spasticity and who do not respond to physiotherapy in combination with other spasmolytic medication should be considered for surgical treatment. In some patients posterior rhizotomy is the treatment of choice.

Adult↗
PubMed1992

Pharmacological screening of few new 2-(substituted acetyl) amino-5-alkyl-1,3,4-oxadiazoles.

Nine new 2-(substituted acetyl) amino-5-alkyl-1,3,4-oxadiazoles were synthesised and confirmed on the basis of IR and nitrogen analysis. These were screened for spasmolytic, anti-inflammatory and their effects on blood pressure after determining ALD50. Compounds GK-4 i.e. 2-(diethylaminoacetyl)- amino-5-methyl-1,3,4-oxadiazole and GK-8 i.e. 2-(din-propylamino acetyl)-amino-5-ethyl-1,3,4-oxadiazole were found to be spasmolytic. Compound GK-6 i.e. 2-(diethylaminoacetyl)-amino-5-n-propyl-1,3,4-oxadiazole was found to be a potent hypotensive agent with the effect lasting for more than two hours.

Animals↗
PubMed1992

[The otilonium bromide-benzodiazepine combination in the therapy of the irritable colon syndrome].

The irritable bowel syndrome is classified ad "disturbance of intestinal motility without an identifiable anatomic substrate". However, the clear etiopathogenetic implications of a psychosomatic nature complicate the search for an adequate therapeutic strategy. Based on this clinical experience, we set out to check the importance of a spasmolytic with a benzodiazepine and the tolerability of this type of combination. We therefore compared the results in 60 patients with irritable bowel syndrome of 8 weeks' treatment with tablets containing octylonium bromide (OB) 20 mg plus diazepam (DZ) 2 mg or OB 40 mg + 2 mg DZ. The doubling of the spasmolytic without increasing the daily dose of anxiolytic appeared to be useful for reducing the symptoms typical for the irritable bowel syndrome. In addition, the combination was found to be perfectly tolerated.

Adult↗
PubMed1992

[Otilonium bromide-diazepam in the treatment of the irritable colon. A controlled study versus otilonium bromide].

Octylonium bromide (OB) is a drug with spasmolytic properties acting selectively on the smooth muscle of the gastrointestinal tract by interfering with calcium mobilization from extra- and intra-cellular deposits. The etiopathogenetic implications of a psychosomatic nature of the irritable bowel syndrome amply justify the use of a spasmolytic (OB) with a benzodiazepine. In our study, we compared the combination OB + DZ (20 mg + 2 mg) T.I.D. versus OB alone (20 mg) in 30 patients suffering from irritable bowel syndrome. The double-blind study lasting 3 weeks was aimed at evaluating gastrointestinal symptoms (bowel motions, aspect of faeces, abdominal pain, pre-evacuation pain, bloating) during the three days preceding the study and during the last five days of treatment, as well as the anxiogenic situation as assessed by the STAI scale (State Tract Anxiety Inventory) before and at the end of the treatment period. The results obtained showed that both treatments considerably reduced gastrointestinal symptoms even though OB alone did not appear to be equally effective and the anxiety component was significantly reduced only by treatment with the combination. The absence of side effects and the perfect tolerability of both treatments showed the OB + D combination T.I.D. to be the treatment of choice for patients suffering from irritable bowel syndrome.

Adult↗
PubMed2004

[Profound study of respiratory biomechanics for diagnosis of chronic dust bronchitis].

Respiratory function studies play an important role in diagnosis of chronic dust bronchitis, both for the diagnosis verification and for determining the disease advance. The study is characterized by step-by-step assessment of respiratory function with body plethysmogram, flow/volume chart and bronchial spasmolytic test. Discrimination and regression analysis revealed leading functional parameters in chronic dust bronchitis: respiratory pathways resistance, pulmonary residual volume, bronchial spasmolytic test, forced vital lungs capacity, peak output flow.

Biomechanical Phenomena↗
PubMed2005

Nonocclusive radial artery injury resulting from transradial coronary interventions: radial artery IVUS.

OBJECTIVE: The purpose of the present study was to evaluate nonocclusive radial artery injury resulting from transradial access. BACKGROUND: The benefits of transradial access for coronary intervention have been well documented, but resulting intima-media hyperplasia could be a limitation. METHODS: Thirty patients undergoing transradial coronary intervention (Group A: 15 de novo procedures, Group B: 15 previous transradial procedures) underwent radial artery intravascular ultrasound (IVUS) before catheter insertion. IVUS abnormalities were evaluated in the 100 mm segment proximal to the access site using automatic pullback in the serial mode. A study segment was then selected for continuous cross-sectional recording to evaluate the effects of a spasmolytic cocktail on radial artery IVUS dimensions which were measured at baseline and at one-minute intervals after administration of 0.8 mg sublingual nitroglycerin (NTG) and 3 mg intra-arterial verapamil (V). Differences in the two groups were evaluated. RESULTS: Intimal hyperplasia and/or intima-media thickening was present in all patients in Group B. The baseline radial artery IVUS area was significantly smaller in Group B, despite the preponderance of males in this group (6.7 +/- 0.8 mm2 Group A versus 5.0 +/- 0.7 mm2 Group B; p < 0.01). Area increased significantly after NTG and V, but Group B area remained smaller than that of Group A. CONCLUSION: In patients with previous transradial access, evidence of nonocclusive injury can be demonstrated in the segment corresponding to the sheath location. Intimal hyperplasia was present and IVUS dimensions were significantly smaller, but the vasodilatory response to spasmolytic drugs was maintained.

Administration, Sublingual↗
PubMed1992

[Effect of pirenzepine on motility of Oddi's sphincter].

Pirenzepine (Gastrozepin) has a proven positive effect in the treatment of peptic ulcers by blocking the so called muscarinic acetylcholine receptors of the gastric glands. Reports of positive results with pirenzepine in the treatment of acute pancreatitis led to new discussions about its biological effects. It is thought that there are three ways by which pirenzepine acts in the pancreas. It decreases enzymatic secretion and it increases the secretion of sodium bicarbonate and water. Furthermore, it is said to have a spasmolytic effect on the sphincter of Oddi. To prove this spasmolytic effect we performed endoscopic manometry at the sphincter of Oddi with intubation of the pancreatic duct in 12 healthy patients. After two minutes of manometric registration of the normal sphincter activity 6 patients received 10 mg pirenzepine i.v. while a control group of 6 patients received 2 ml of 0.9% NaCl i.v. During the next 5 minutes the basal pressure of the sphincter, the amplitude of concentrations, as well as their frequency and duration were monitored. There were no changes noticed in the placebo group. However, pirenzepine caused a considerable decrease of the 4 manometric parameters of the sphincter of Oddi in all patients. Within 5 minutes the basal tonus fell from 14.3 +/- 5.1 mm of mercury to 9.0 +/- 6.0 (p less than 0.01). The frequency of contractions dropped from 5.8 +/- 2.7 per minute to 2.0 +/- 2.1 (p less than 0.05).(ABSTRACT TRUNCATED AT 250 WORDS)

Cholangiopancreatography, Endoscopic Retrograde↗
PubMed1991

Pharmacological studies on otilonium bromide.

Otilonium bromide (OB) is a quaternary ammonium compound characterized by a long aliphatic chain. Its chemical properties are responsible for both a poor penetration in CNS and a prolonged binding to cell membranes. OB is a spasmolytic agent which acts by modifying Ca++ fluxes from extra and intracellular sites. It has been documented that iv administration (10 mg/kg) of OB causes a marked reduction of colonic motility lasting from 2 to 3 hours, whereas an inhibition of upper GI motor activity is present only at higher dosages. In conclusion, OB seems to exert its activity mainly on distal GI tract, and its spasmolytic effect may be due to its ability to inhibit Ca++ fluxes and to a direct action of the drug on the contractile proteins of the smooth muscle.

Animals↗
PubMed1991

[Methods in individualized pharmacotherapy of diseases of the digestive and the respiratory systems in children].

The possibility to forecast pharmacotherapeutic effect in children with chronic diseases of breathing and digestion was studied. It was established that the use of pathogenic and associative markers, characteristic of the background state of a child as compared to individual peculiarities of pharmacokinetics and pharmacodynamics of a certain drug, will allow to forecast the efficiency of drug treatment of chronic diseases of breathing organs (bronchitis, pneumonia, asthmatic bronchitis) and digestion (gastritis, cholecystocholangitis). The use of aminophenazone marker in children with above mentioned pathology became the basis of research into efficiency of spasmolytics with similar type of metabolism (papaverini hydrochloridum, aminophyllinum, drotaverinum). Mathematic models of spasmolytics efficiency forecast was developed by many factor computer analysis.

Aminopyrine↗
PubMed1990

[The pharmacologic activity of p-substituted DL-2-phenylglycine octyl esters].

DL-2-phenylglycine octyl ester has antiphlogistic, analgesic and spasmolytic activities as shown in different animal models. The antiphlogistic effectiveness is changed only a little by the p-substitution at the phenyl ring, whereas the analgesic action is markedly influenced. Most of the substituted compounds are significantly more active than the unsubstituted ester. DL-2-(benzyloxyphenyl)glycine octyl ester is the most active compound, it has furthermore the highest therapeutic quotient. Using the i.p. application its efficacy exceeds that of acetylsalicylic acid, phenylbutazone and indometacin, respectively. The spasmolytic activity is differently changed by the substituents. The most active ester, DL-2-(p-methoxyphenyl)glycine octyl ester, is about two times more active than papaverine. In histamine induced spasm the effectiveness is low compared with the specific antagonist mepyramine. The results obtained show that the activities of the p-substituted DL-2-phenylglycine octyl esters are different with regard to the three investigated pharmacological properties.

Animals↗
PubMed1990

Pinacidil antagonism of endothelin-induced contractions of smooth muscle in the lungs: differences between tracheal and pulmonary artery preparations.

Contractions to endothelin and their reversal by pinacidil have been examined in isolated preparations of guinea pig and rat trachea and rat pulmonary artery. Indomethacin attenuated endothelin (less than or equal to 10 nM) on guinea pig trachea, but not on the rat tissues. This indicates that part of the effect of endothelin on guinea pig trachea is indirect and mediated by cyclooxygenase products. Endothelin (direct effects) was more potent on pulmonary artery than on guinea pig or rat trachea (negative log EC50 values: 8.42, 7.71 and 7.76, respectively) and was also a more effective spasmogen on pulmonary artery (maximum was the tissue maximum, i.e., greater than or equal to 80 mM K+) than on trachea (maximum was 60-70% of the tissue maximum to 10 microM carbachol). Pinacidil was less effective preventing (anti-spasmogenic) than reversing (spasmolytic) contractions to endothelin on either tissue type. This is compatible with different mechanisms for the initiation and maintenance of smooth muscle contraction in these tissues. As a spasmolytic against endothelin (0.03 microM), pinacidil was less potent on rat pulmonary artery than on guinea pig or rat trachea (negative log IC50 values: 4.45, 5.65 and 5.49, respectively). This may reflect 1) the greater tone induced by endothelin on pulmonary artery, 2) a smaller receptor reserve for endothelin in trachea and/or 3) a different mechanism whereby endothelin contracts pulmonary vascular smooth muscle compared with tracheal smooth muscle.

Animals↗
PubMed1990

Synthesis and pharmacological activity of 2-alkylthio substituted thieno[2,3-d]pyrimidine-4-one and 5H-pyrimido [5,4-b]indol-4-one.

Quaternary salts of several 2-alkylthio substituted derivatives of thieno [2,3-d]pyrimidin-4-one and 5H-pyrimido [5,4-b]indol-4-one with a basic group in position 2 of the alkyl chain were synthesized and screened for potential spasmolytic activity. These substances were prepared by condensation of the corresponding mercapto compounds with a 2-chloroalkyltertiary amine. The tertiary bases were quaternized with methyl iodide. Among the assayed compounds, the thieno [2-3-d]pyrimidin-4-one derivatives displayed a potent spasmolytic activity in the in vitro and in vivo assays.

Animals↗
PubMed1990

[Two cases of perioperative coronary vasospasm following ASD closure and OMC].

Two cases of perioperative coronary spasm following ASD closure and OMC are reported. A 36-year-old female had been diagnosed of vasospastic angina and another 47-year-old female patient was diagnosed of effort angina for 99% stenosis of the right ventricular branch preoperatively. Both patients suffered from coronary vasospastic attack and ventricular fibrillation several times within 17 hours postoperatively. Although the coronary dissolution was obtained finally following aggressive cardiac massage, administration of spasmolytic agents, such as NTG, lidocaine, DBcAMP and the start of IABP, the resolution was stormy due to the hemodynamic derangement. To prevent the coronary spastic episode, it is suggested, for patients of possible coronary spasm, to avoid arousal stimulation and to administer spasmolytic agents prophylactically within the first postoperative day.

Adult↗
PubMed1990

[The value of magnesium pyrrolidone carboxylate in true cervix dystocia. A double blind versus placebo study].

The efficacy of spasmolytics in cervix dystocia during labor is very contested. For this reason the authors studied the action of pyrrolidone carboxylate of magnesium for this indication in a double-blind versus placebo study (48 patients divided in two groups). Strict inclusion criteria and homogeneity of the two groups of patients allowed them to find out that the use of this particular magnesium salt reduced significantly the length of labor. Consequently the authors assess that spasmolytics work not only through their placebo effect, which is thought by some authors.

Adult↗