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1.
Rev. ciênc. farm. básica apl ; 41: [13], 01/01/2020. tab, graf
Article in English | LILACS | ID: biblio-1128583

ABSTRACT

Aim: Since other species of the Bignoniaceae Family presented of antispasmodic activity, it was decided, by chemotaxonomic criterion, to determine the antispasmodic activity of the leaves of Arrabidaea brachypoda. Methodology: the segments of the rat jejunum were suspended in glass vats containing specific saline solution, at an appropriate temperature, and after stabilization period, were stimulated by a contractile agent to observe the inhibitory or relaxing effect of EH-FAB. Results: EH-FAB showed the presence of 10 compounds, mainly rutin and it has an antispasmodic activity as it inhibits the phasic component and relaxes the tonic component of the contraction in isolated rat jejunum. To assess the mechanism of antispasmodic action, cumulative curves to the CCh were performed in which a non-competitive antagonism was observed, due to a displacement of the control curve to the right and reduction of the maximum contraction effect (Emax). Afterward, the participation of the calcium and/or potassium channels was evaluated by increasing the extracellular potassium, and it was observed that the EH-FAB relaxed the rat jejunum, suggesting the participation of the Ca2+ channels. To corroborate that hypothesis, the EH-FAB was tested against cumulative curves to Ca2+ in a free depolarizing solution of Ca2+, and it was observed that there was a shift of the curve to the right with a reduction in Emax. Conclusions: EH-FAB presents antispasmodic activity in isolated rat jejunum and it is suggested to block the influx of Ca2+ through voltage-gated calcium channels, signaling the therapeutic potential for the treatment of colic and/or diarrhea.(AU)


Subject(s)
Animals , Male , Rats , Parasympatholytics/therapeutic use , Plant Extracts/pharmacology , Calcium Channel Blockers/pharmacology , Bignoniaceae/chemistry , Potassium , Jejunum
2.
Evid. actual. práct. ambul ; 23(1): e002045, 2020. tab
Article in Spanish | LILACS | ID: biblio-1103172

ABSTRACT

Una mujer de 36 años, diagnosticada con síndrome de intestino irritable a predominio de diarrea (SII-D) acude a la consulta médica. Ella pregunta si el uso de probióticos sería útil para controlar los episodios de diarrea, ya que los fármacos con los que está siendo tratada no le resultan eficaces. Se realizó una búsqueda bibliográfica con el objetivo de en contrar evidencia en respuesta a su consulta, tras la cual se seleccionaron dos ensayos clínicos y una revisión sistemática. Se evidenciaron diversos resultados en cuanto al uso de probióticos en el SII-D y se discutieron los riesgos y beneficios del tratamiento, así como las implicancias en la vida de la paciente. (AU)


A 36-year-old woman diagnosed with diarrhea predominant irritable bowel syndrome (D-IBS) goes to meet the doctor. She raises whether the use of probiotics would be useful for controlling diarrhea episodes, since the drugs which she is being treated with, are not effective. A bibliographic search was conducted with the objective of finding evidence in response toher query. Two clinical trials and a systematic review were found. Variable results were found regarding the use of probioticsin D-IBS. The risks and benefits of the treatment were discussed, as well as the implications in the patient's lifestyle. (AU)


Subject(s)
Humans , Female , Adult , Probiotics/therapeutic use , Irritable Bowel Syndrome/therapy , Diarrhea/therapy , Parasympatholytics/therapeutic use , Quality of Life , Review Literature as Topic , Abdominal Pain/therapy , Cholestyramine Resin/therapeutic use , Clinical Trials as Topic , Probiotics/administration & dosage , Probiotics/adverse effects , Irritable Bowel Syndrome/diagnosis , Irritable Bowel Syndrome/etiology , Diarrhea/complications , Duration of Therapy , Gastrointestinal Motility/immunology , Intestinal Mucosa/immunology , Loperamide/therapeutic use , Antidepressive Agents/therapeutic use
3.
Rev. colomb. gastroenterol ; 34(3): 269-276, jul.-set. 2019.
Article in Spanish | LILACS | ID: biblio-1042814

ABSTRACT

Resumen El uso de los antiespasmódicos forma parte de la piedra angular del tratamiento en el síndrome de intestino irritable (SII), independientemente del subtipo. Consideramos relevante hacer una revisión de los medicamentos antiespasmódicos disponibles actualmente en Colombia, los cuales son usados crónicamente, de manera frecuente, en esta enfermedad.


Abstract Although antispasmodics are the cornerstone of treating irritable bowel syndrome, there are a number of antispasmodic medications currently available in Colombia. Since they are frequently used to treat this disease, we consider an evaluation of them to be important.


Subject(s)
Humans , Role , Therapeutics , Pharmaceutical Preparations , Irritable Bowel Syndrome , Parasympatholytics
4.
Neonatal Medicine ; : 67-71, 2019.
Article in Korean | WPRIM | ID: wpr-741661

ABSTRACT

Pylorospasm is a cause of delayed gastric emptying in young infants. As in patients with hypertrophic pyloric stenosis, most pylorospasm patients present with projectile vomiting. However, unlike that in case of hypertrophic pyloric stenosis, no persistent pyloric stenotic lesions are present. As such, follow-up using serial gastrointestinal fluoroscopy or ultrasonography can be helpful in diagnosing patients with clinical signs of gastroparesis. Most cases can be treated conservatively, but some patients require pharmacologic treatment. Antispasmodics have been proposed as a treatment for pylorospasm, but their use in neonates and infants has rarely been reported. Herein, we present a case of pylorospasm diagnosed in the neonatal period and successfully treated with intravenous atropine.


Subject(s)
Atropine , Fluoroscopy , Follow-Up Studies , Gastric Emptying , Gastroparesis , Humans , Infant , Infant, Newborn , Parasympatholytics , Pyloric Stenosis, Hypertrophic , Pylorus , Spasm , Ultrasonography , Vomiting
5.
Rev. peru. med. integr ; 4(4): 110-115, 2019. graf
Article in Spanish | MTYCI, LILACS, MTYCI | ID: biblio-1145704

ABSTRACT

Objetivo. El objetivo de este estudio fue investigar el potencial efecto antiespasmódico de Rubus roseus y Mentha pulegium en íleon aislado de cobayo (Cavia porcellus) Materiales y Métodos. Los segmentos de íleon se precontrajeron con acetilcolina (ACh; 4 × 10−6 M) y cloruro de potasio (KCl; 4 × 10-4 M) luego se evaluó la respuesta de los decoctos de Rubus roseus (Rr) Mentha pulegium (Mp) en el baño de órganos aislado en concentraciones crecientes (no acumulativas), como controles positivos se utilizaron nifedipino 5 × 10-8 M (antagonista de canales de Ca2+ voltaje dependientes); atropina sulfato 5,5 × 10-9 M (antagonista muscarínico no selectivo), y N-butilbromuro de hioscina 3 x 10-3 M (antagonista muscarínico M3 selectivo). Se cuantificó la amplitud y la frecuencia de contracción (durante diez minutos) después de la administración de los decoctos. Resultados. Los decoctos de Rubus roseus y Mentha pulegium reducen las contracciones inducidas por acetilcolina (p < 0,001) y KCl (p < 0,01) similares a nifedipino (Mp: 4 y 8 mg/mL); atropina sulfato (Rr: 0,2-4 mg/mL; Mp: 0,8 y 1,6 mg/mL) y N-butilbromuro de hioscina (Mp: 2,4 y 8 mg/mL). Por otro lado, ambos decoctos reducen la frecuencia de contracción inducidas por Ach (p < 0,001) y KCl (p < 0,001). Conclusión. Los decoctos de Rubus roseus y Mentha pulegium tienen efecto antiespasmódico en íleon aislado de cobayo (Cavia porcellus).


Objective. This study aimed to investigate the potential antispasmodic effect of Rubus roseus and Mentha pulegium on isolated guinea pig (Cavia porcellus) ileum. Materials and Methods. The ileum segments were pre-contracted with acetylcholine (ACh, 4 × 10-6 M) and potassium chloride (KCl, 4 × 10-4 M) then the response of the Rubus roseus (Rr) and Mentha pulegium (Mp) decocts was evaluated in the organ bath isolated in increasing concentrations (non-cumulative), as positive controls were used nifedipine 5 × 10-8 M (antagonist of voltage dependent Ca2+ channels) atropine sulfate 5,5 × 10-9 M (non-selective muscarinic antagonist) and 3 x 10-3 M hyoscine N-butylbromide (selective M3 muscarinic antagonist). The amplitude and the frequency of contraction were quantified (during 10 minutes) after the administration of the decocts. Results. The decocts of Rubus roseus and Mentha pulegium decrease the contractions induced by acetylcholine (p < 0.001) and KCl (p <0.01) comparable to nifedipine (Mp: 4 and 8 mg/mL), atropine sulfate (Rr: 0.2 - 4 mg/mL, Mp: 0.8 and 1.6 mg/mL) and hyoscine N-butylbromide (Mp: 2.4 and 8 mg/mL). On the other hand, both decocts reduce the frequency of contraction induced by Ach (p <0.001) and KCl (p <0.001). Conclusions. The decocts of Rubus roseus and Mentha pulegium have an antispasmodic effect on isolated guinea pig ileum (Cavia porcellus).


Subject(s)
Animals , Parasympatholytics , Mentha pulegium , Rubus , Plants, Medicinal , Guinea Pigs , Ileum , Medicine, Traditional
7.
Article in English | WPRIM | ID: wpr-716991

ABSTRACT

Chemodenervation with botulinum toxin (BTX) has been recommended for focal spasticity. BTX injection should be performed with caution in patients with bleeding disorders and/or receiving anticoagulation therapy. We present a case of BTX injection for post-stroke spasticity in a patient with hemophilia A who could not take oral spasmolytics due to chronic hepatitis C. To minimize the bleeding risk, we replaced factor VIII intravenously in accordance with the World Federation of Hemophilia guidelines for minor surgery. FVIII (3,000 IU) was administered 15 minutes before BTX injection. One day later, 2,000 IU was administered, and 2 days later, another 2,000 IU was administered. We performed the real-time Ultrasound-guided BTX injection three times, then spasticity and upper extremity function improved without adverse events. BTX injection can be considered as a treatment option for spasticity among patients with hemophilia.


Subject(s)
Botulinum Toxins , Factor VIII , Hemophilia A , Hemorrhage , Hepatitis C, Chronic , Humans , Minor Surgical Procedures , Muscle Spasticity , Nerve Block , Parasympatholytics , Stroke , Ultrasonography , Upper Extremity
8.
Article in Korean | WPRIM | ID: wpr-766517

ABSTRACT

Antispasmodics are effective in reducing abdominal pain and controlling spasm. Irritable bowel syndrome (IBS) patients have characteristic key factors such as intestinal motility disorder and visceral hypersensitivity. So antispasmodics have been used in the treatment of IBS for decades. Mebeverine blocks intestinal peristalsis but are not significantly better than placebo. Alverine citrate combined with simethicone is effective treatment option in IBS. Otilonium and pinaverium bromide are poorly absorbed agents, so they have mostly local effect with minimal systemic adverse events. Phloroglucinol controls acute exacerbation of abdominal pain effectively. Tiropramide reduce abdominal discomfort without serious adverse events. Fenoverine control spasm in spastic colon but does not affect normal contraction. Trimebutine have dual actions that it inhibits hyperactive colon and activates hypomotile colon. Each drug has advantages and disadvantages. Antispasmodics are considered as the first treatment option of pain-dominant IBS.


Subject(s)
Abdominal Pain , Citric Acid , Colon , Gastrointestinal Motility , Humans , Hypersensitivity , Irritable Bowel Syndrome , Muscle Spasticity , Parasympatholytics , Peristalsis , Phloroglucinol , Simethicone , Spasm , Trimebutine
9.
Int. j. morphol ; 35(2): 500-505, June 2017. ilus
Article in English | LILACS | ID: biblio-893011

ABSTRACT

Halphabarol, the active principle of Proximol, is the most potent of the four antispasmodics present in the national desert weed Cymbopogon proximus or ''Halfa Bar''. Halphabarol is of great value for the management of renal colic and in the expulsion of ureteric calculi as it causes dilation of the ureter below the site of calculus while active propulsion is maintained. Evaluation the congenital malformation of proximol in pregnant albino rats during gestation period. The virgin female rats were mated with male rats and the pregnant rats were orally administered a human equivalent dose (0.05 mg/kg) of Proximol from 5th-20th gestation day. At day 20 of pregnancy, all rats were anesthetized to obtained maternal and fetal data. The treatment group displayed some disorders, which can be summarized as growth retardation, external anomalies, embryonic resorption, and skeletal malformation. We concluded that the oral administration of Proximol resulted in embryonic abnormalities and skeletal malformations.


Halphabarol, el principio activo de Proximol, es el más potente de los cuatro antiespasmódicos presentes en la maleza desértica nacional "Cymbopogon proximus" o "Halfa Bar". Halphabarol es de gran utilidad para el manejo de cólicos renales y para la expulsión de cálculos ureterales, ya que causa la dilatación del uréter por debajo del sitio de cálculo mientras se mantiene el mecanismo de propulsión activa. Se realizó una evaluación de la malformación congénita por Proximol en ratas albinas gestantes durante el período de gestación. Las ratas fueron apareadas y a las ratas gestantes se les administró oralmente, del 5 al 20 día de gestación, una dosis de Proximol (0,05 mg / kg), equivalente a la dosis humana. Al día 20 de gestación, todas las ratas fueron anestesiadas para obtener datos maternos y fetales. El grupo de tratamiento mostró algunos trastornos, que pueden resumirse como retraso del crecimiento, anomalías externas, resorción embrionaria y malformación esquelética. Concluimos que la administración oral de Proximol resultó en anomalías embrionarias y malformaciones esqueléticas.


Subject(s)
Animals , Female , Pregnancy , Rats , Congenital Abnormalities/pathology , Cymbopogon , Parasympatholytics/toxicity , Plants, Medicinal/toxicity , Congenital Abnormalities/etiology , Fetus/drug effects , Fetus/pathology , Pregnancy, Animal/drug effects
10.
Article in English | WPRIM | ID: wpr-771016

ABSTRACT

Although methidathion is an organophosphate insecticide, it is different from the other organophosphates in terms of toxicity. Because of its relatively high fat solubility, the apparent volume of methidathion distribution throughout the body is very high, indicating that hemoperfusion is not effective in removing this organophosphate from the body. Redistribution of methidathion from fat to blood can also occur when plasma levels diminish. Additionally, acetylcholinesterase aging, which is the loss of an alkyl side chain that prevents reactivation by oximes, is very rapid so that the effective reactivation by oximes is thwarted. Thus, methidathion's effect on acetylcholinesterase inhibition is long lasting, particularly with a high dose. In addition to its parasympatholytic effect and ability to induce muscle paralysis, methidathion poisoning is associated with a profound and long-lasting circulatory collapse due to sympathetic ganglion blockade. This report presents the case of a 55-year-old man who accidentally ingested a high dose of methidathion. He later developed enteroinvasive aspergillosis infection-induced multiple bowel perforations on two separate occasions while on mechanical ventilator support, resulting in a fatal outcome. The renin-angiotensin axis activated by sympathetic ganglion blockade may have reduced the patient's splanchnic blood flow, contributing to translocation of endotoxin. Also, the effect of excessive acetylcholine on non-neuronal acetylcholine receptors may have contributed to the development of fatal enteroinvasive aspergillosis in this patient.


Subject(s)
Acetylcholine , Acetylcholinesterase , Aging , Aspergillosis , Fatal Outcome , Ganglia , Ganglia, Sympathetic , Hemoperfusion , Humans , Middle Aged , Organophosphate Poisoning , Organophosphates , Oximes , Paralysis , Parasympatholytics , Plasma , Poisoning , Receptors, Cholinergic , Shock , Solubility , Ventilators, Mechanical
11.
Article in English | WPRIM | ID: wpr-20754

ABSTRACT

Although methidathion is an organophosphate insecticide, it is different from the other organophosphates in terms of toxicity. Because of its relatively high fat solubility, the apparent volume of methidathion distribution throughout the body is very high, indicating that hemoperfusion is not effective in removing this organophosphate from the body. Redistribution of methidathion from fat to blood can also occur when plasma levels diminish. Additionally, acetylcholinesterase aging, which is the loss of an alkyl side chain that prevents reactivation by oximes, is very rapid so that the effective reactivation by oximes is thwarted. Thus, methidathion's effect on acetylcholinesterase inhibition is long lasting, particularly with a high dose. In addition to its parasympatholytic effect and ability to induce muscle paralysis, methidathion poisoning is associated with a profound and long-lasting circulatory collapse due to sympathetic ganglion blockade. This report presents the case of a 55-year-old man who accidentally ingested a high dose of methidathion. He later developed enteroinvasive aspergillosis infection-induced multiple bowel perforations on two separate occasions while on mechanical ventilator support, resulting in a fatal outcome. The renin-angiotensin axis activated by sympathetic ganglion blockade may have reduced the patient's splanchnic blood flow, contributing to translocation of endotoxin. Also, the effect of excessive acetylcholine on non-neuronal acetylcholine receptors may have contributed to the development of fatal enteroinvasive aspergillosis in this patient.


Subject(s)
Acetylcholine , Acetylcholinesterase , Aging , Aspergillosis , Fatal Outcome , Ganglia , Ganglia, Sympathetic , Hemoperfusion , Humans , Middle Aged , Organophosphate Poisoning , Organophosphates , Oximes , Paralysis , Parasympatholytics , Plasma , Poisoning , Receptors, Cholinergic , Shock , Solubility , Ventilators, Mechanical
12.
Article in Korean | WPRIM | ID: wpr-129458

ABSTRACT

Irritable bowel syndrome is a group of symptoms that includes abdominal pain and changes in the form and frequency of stool. Since its symptoms are usually long-lasting, the disease significantly degrades quality of life. Several pharmacological therapies have been suggested according to the type of symptoms (e.g., abdominal pain, constipation, or diarrhea). In order to control abdominal pain, smooth muscle antispasmodics, antidepressants including tricyclic antidepressants and selective serotonin reuptake inhibitors, or 5-HT3 antagonists can be used. To improve constipation, dietary fiber or laxatives, 5-HT4 agonists, and chloride channel activators are available. Opioid agonists, mixed opioid agonists/antagonists such as eluxadoline, and bile salt sequestrants can be considered for diarrhea. In addition, probiotics and non-absorbable oral antibiotics can be used for the normalization of the gut microbiome and the treatment of small intestinal bacterial overgrowth, respectively. It is necessary to understand the characteristics of each drug and their combinations, because any single regimen cannot improve all symptoms in patients with irritable bowel syndrome. In this review, the mechanisms of action, efficacy, and adverse events associated with drugs used for irritable bowel syndrome are summarized.


Subject(s)
Abdominal Pain , Anti-Bacterial Agents , Antidepressive Agents , Antidepressive Agents, Tricyclic , Bile , Chloride Channel Agonists , Constipation , Diarrhea , Dietary Fiber , Drug Therapy , Gastrointestinal Microbiome , Humans , Irritable Bowel Syndrome , Laxatives , Muscle, Smooth , Parasympatholytics , Probiotics , Quality of Life , Serotonin 5-HT3 Receptor Antagonists , Serotonin 5-HT4 Receptor Agonists , Serotonin Uptake Inhibitors
13.
Article in Korean | WPRIM | ID: wpr-129443

ABSTRACT

Irritable bowel syndrome is a group of symptoms that includes abdominal pain and changes in the form and frequency of stool. Since its symptoms are usually long-lasting, the disease significantly degrades quality of life. Several pharmacological therapies have been suggested according to the type of symptoms (e.g., abdominal pain, constipation, or diarrhea). In order to control abdominal pain, smooth muscle antispasmodics, antidepressants including tricyclic antidepressants and selective serotonin reuptake inhibitors, or 5-HT3 antagonists can be used. To improve constipation, dietary fiber or laxatives, 5-HT4 agonists, and chloride channel activators are available. Opioid agonists, mixed opioid agonists/antagonists such as eluxadoline, and bile salt sequestrants can be considered for diarrhea. In addition, probiotics and non-absorbable oral antibiotics can be used for the normalization of the gut microbiome and the treatment of small intestinal bacterial overgrowth, respectively. It is necessary to understand the characteristics of each drug and their combinations, because any single regimen cannot improve all symptoms in patients with irritable bowel syndrome. In this review, the mechanisms of action, efficacy, and adverse events associated with drugs used for irritable bowel syndrome are summarized.


Subject(s)
Abdominal Pain , Anti-Bacterial Agents , Antidepressive Agents , Antidepressive Agents, Tricyclic , Bile , Chloride Channel Agonists , Constipation , Diarrhea , Dietary Fiber , Drug Therapy , Gastrointestinal Microbiome , Humans , Irritable Bowel Syndrome , Laxatives , Muscle, Smooth , Parasympatholytics , Probiotics , Quality of Life , Serotonin 5-HT3 Receptor Antagonists , Serotonin 5-HT4 Receptor Agonists , Serotonin Uptake Inhibitors
14.
Braz. j. med. biol. res ; 49(2): e4800, 2016. tab, graf
Article in English | LILACS | ID: lil-766979

ABSTRACT

β-Citronellol is an alcoholic monoterpene found in essential oils such Cymbopogon citratus (a plant with antihypertensive properties). β-Citronellol can act against pathogenic microorganisms that affect airways and, in virtue of the popular use of β-citronellol-enriched essential oils in aromatherapy, we assessed its pharmacologic effects on the contractility of rat trachea. Contractions of isolated tracheal rings were recorded isometrically through a force transducer connected to a data-acquisition device. β-Citronellol relaxed sustained contractions induced by acetylcholine or high extracellular potassium, but half-maximal inhibitory concentrations (IC50) for K+-elicited stimuli were smaller than those for cholinergic contractions. It also inhibited contractions induced by electrical field stimulation or sodium orthovanadate with pharmacologic potency equivalent to that seen against acetylcholine-induced contractions. When contractions were evoked by selective recruitment of Ca2+ from the extracellular medium, β-citronellol preferentially inhibited contractions that involved voltage-operated (but not receptor-operated) pathways. β-Citronellol (but not verapamil) inhibited contractions induced by restoration of external Ca2+ levels after depleting internal Ca2+ stores with the concomitant presence of thapsigargin and recurrent challenge with acetylcholine. Treatment of tracheal rings with L-NAME, indomethacin or tetraethylammonium did not change the relaxing effects of β-citronellol. Inhibition of transient receptor potential vanilloid subtype 1 (TRPV1) or transient receptor potential ankyrin 1 (TRPA1) receptors with selective antagonists caused no change in the effects of β-citronellol. In conclusion, β-citronellol exerted inhibitory effects on rat tracheal rings, with predominant effects on contractions that recruit Ca2+ inflow towards the cytosol by voltage-gated pathways, whereas it appears less active against contractions elicited by receptor-operated Ca2+ channels.


Subject(s)
Animals , Male , Calcium Channel Blockers/pharmacology , Monoterpenes/pharmacology , Muscle Contraction/drug effects , Muscle, Smooth/drug effects , Trachea/drug effects , Analysis of Variance , Calcium Channel Blockers/administration & dosage , Enzyme Inhibitors/pharmacology , Indomethacin/pharmacology , Inhibitory Concentration 50 , Monoterpenes/administration & dosage , NG-Nitroarginine Methyl Ester/pharmacology , Parasympatholytics/administration & dosage , Rats, Wistar , Tetraethylammonium/pharmacology , Thapsigargin/pharmacology , Verapamil/pharmacology
15.
Clinical Endoscopy ; : 48-51, 2015.
Article in English | WPRIM | ID: wpr-55294

ABSTRACT

BACKGROUND/AIMS: Suppression of gastrointestinal (GI) peristalsis during GI endoscopy commonly requires antispasmodic agents such as hyoscine butylbromide, atropine, glucagon, and cimetropium bromide. This study examined the efficacy of oral phloroglucin for the suppression of peristalsis, its impact on patient compliance, and any associated complications, and compared it with intravenous or intramuscular cimetropium bromide administration. METHODS: This was a randomized, investigator-blind, prospective comparative study. A total of 172 patients were randomized into two groups according to the following medications administered prior to upper endoscopy: oral phloroglucin (group A, n=86), and cimetropium bromide (group B, n=86). The numbers and the degrees of peristalsis events at the antrum and second duodenal portion were assessed for 30 seconds. RESULTS: A significantly higher number of gastric peristalsis events was observed in group A (0.49 vs. 0.08, p<0.001), but the difference was not clinically significant. No significant difference between both groups was found in the occurrence of duodenal peristalsis events (1.79 vs. 1.63, p=0.569). The incidence of dry mouth was significantly higher with cimetropium bromide than with phloroglucin (50% vs. 15.1%, p<0.001). CONCLUSIONS: Oral phloroglucin can be used as an antispasmodic agent during upper endoscopy, and shows antispasmodic efficacy and adverse effects similar to those of cimetropium bromide.


Subject(s)
Atropine , Endoscopy , Endoscopy, Digestive System , Glucagon , Humans , Incidence , Mouth , Parasympatholytics , Patient Compliance , Peristalsis , Premedication , Prospective Studies , Scopolamine
16.
Intestinal Research ; : 306-312, 2015.
Article in English | WPRIM | ID: wpr-50554

ABSTRACT

Chronic diarrhea is usually associated with a number of non-infectious causes. When definitive treatment is unavailable, symptomatic drug therapy is indicated. Pharmacologic agents for chronic diarrhea include loperamide, 5-hydroxytryptamine type 3 (5-HT3) receptor antagonists, diosmectite, cholestyramine, probiotics, antispasmodics, rifaximin, and anti-inflammatory agents. Loperamide, a synthetic opiate agonist, decreases peristaltic activity and inhibits secretion, resulting in the reduction of fluid and electrolyte loss and an increase in stool consistency. Cholestyramine is a bile acid sequestrant that is generally considered as the first-line treatment for bile acid diarrhea. 5-HT3 receptor antagonists have significant benefits in patients with irritable bowel syndrome (IBS) with diarrhea. Ramosetron improves stool consistency as well as global IBS symptoms. Probiotics may have a role in the prevention of antibiotic-associated diarrhea. However, data on the role of probiotics in the treatment of chronic diarrhea are lacking. Diosmectite, an absorbent, can be used for the treatment of chronic functional diarrhea, radiation-induced diarrhea, and chemotherapy-induced diarrhea. Antispasmodics including alverine citrate, mebeverine, otilonium bromide, and pinaverium bromide are used for relieving diarrheal symptoms and abdominal pain. Rifaximin can be effective for chronic diarrhea associated with IBS and small intestinal bacterial overgrowth. Budesonide is effective in both lymphocytic colitis and collagenous colitis. The efficacy of mesalazine in microscopic colitis is weak or remains uncertain. Considering their mechanisms of action, these agents should be prescribed properly.


Subject(s)
Abdominal Pain , Anti-Inflammatory Agents , Bile , Budesonide , Cholestyramine Resin , Citric Acid , Colitis, Collagenous , Colitis, Lymphocytic , Colitis, Microscopic , Diarrhea , Drug Therapy , Humans , Irritable Bowel Syndrome , Loperamide , Mesalamine , Parasympatholytics , Probiotics , Receptors, Serotonin, 5-HT3 , Serotonin
17.
Biol. Res ; 48: 1-6, 2015. graf, tab
Article in English | LILACS | ID: biblio-950792

ABSTRACT

BACKGROUND: Ruta graveolens L. (R. graveolens) is a medicinal plant employed in non-traditional medicines that has various therapeutic properties, including anthelmintic, and vasodilatory actions, among others. We evaluated the trachea-relaxant effects of hydroalcoholic extract of R. graveolens against potassium chloride (KCl)- and carbachol-induced contraction of rat tracheal rings in an isolated organ bath. RESULTS: The results showed that the airway smooth muscle contraction induced by the depolarizing agent (KCl) and cholinergic agonist (carbachol) was markedly reduced by R. graveolens in a concentration-dependent manner, with maximum values of 109 ± 7.9 % and 118 ± 2.6 %, respectively (changes in tension expressed as positive percentages of change in proportion to maximum contraction), at the concentration of 45 µg/mL (half-maximal inhibitory concentration IC50: 35.5 µg/mL and 27.8 µg/mL for KCl- and carbachol-induced contraction, respectively). Additionally, the presence of R. graveolens produced rightward parallel displacement of carbachol dose-response curves and reduced over 35 % of the maximum smooth muscle contraction. CONCLUSIONS: The hydroalcoholic extract of R. graveolens exhibited relaxant activity on rat tracheal rings. The results suggest that the trachea-relaxant effect is mediated by a non-competitive antagonistic mechanism. More detailed studies are needed to identify the target of the inhibition, and to determine more precisely the pharmacological mechanisms involved in the observed biological effects.


Subject(s)
Animals , Rats , Parasympatholytics/pharmacology , Trachea/drug effects , Plant Extracts/pharmacology , Ruta/chemistry , Muscle, Smooth/drug effects , Neuromuscular Depolarizing Agents/pharmacology , Potassium Chloride/pharmacology , Furocoumarins/analysis , Quercetin/analysis , Rutin/analysis , Trachea/surgery , In Vitro Techniques , Carbachol/pharmacology , Plant Extracts/chemistry , Chromatography, Liquid , Rats, Sprague-Dawley , Cholinergic Agents/pharmacology , Inhibitory Concentration 50 , Plant Components, Aerial/chemistry , Muscle Contraction/drug effects , Muscle Tonus/drug effects
18.
Article in Chinese | WPRIM | ID: wpr-260304

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the impact of intestinal spasmolytic on colon polyps and adenoma detection rate during colonoscopy.</p><p><b>METHODS</b>Literatures related to the effect of intestinal spasmolytic on colon polyp or adenoma detection rate were retrieved from PubMed, Medline, EBSCO, High Wire Press, OVID, EMBASE, and the China National Knowledge Articles, etc. published before July 2014. Unified data were extracted by two researchers independently and organized using Jadad scale to evaluate the quality of the enrolled studies through Review manager 5.2 Meta-analysis software.</p><p><b>RESULTS</b>Six articles were enrolled with total 47,509 cases, including 16,867 cases in the scopolamine group and 30,642 cases in the placebo group. Meta analysis showed spasmolytic could increase the detective rate of polyps (OR=1.24, 95% CI:1.19-1.30), adenoma (OR=1.25, 95% CI:1.19-1.30) and high-risk adenoma (OR=1.22, 95% CI:1.16-1.29).</p><p><b>CONCLUSION</b>Using colonoscopy spasmolytic scopolamine can increase the detection rate of colonic polyp and adenoma.</p>


Subject(s)
Adenoma , China , Colonic Neoplasms , Colonic Polyps , Colonoscopy , Humans , Parasympatholytics
19.
Braz. dent. j ; 25(6): 554-560, Nov-Dec/2014. tab, graf
Article in English | LILACS | ID: lil-732259

ABSTRACT

The aim of this study was to assess, by the three-dimensional finite element method, the influence of crown-to-implant ratio and parafunctional occlusal loading on stress distribution in single external hexagon implant-supported prosthesis. Computer-aided design software was used to confection three models. Each model was composed of a block bone and an external hexagon implant (5x10.0 mm) with screw-retained implant prostheses, varying the height crown: 10, 12.5 and 15 mm. Finite element analysis software was used to generate the finite element mesh and to establish the loading and boundary conditions. Normal (200 N axial and 100 N oblique load) and parafunctional forces (1,000 N axial and 500 N oblique load) were applied. The results were visualized by von Mises and maximum principal stress. In comparison with the normal occlusal force, the parafunctional occlusal force induced an increase in stress concentration and magnitude on implant (platform and first threads) and screw (neck). The cortical bone showed the highest tensile stress under parafunctional force (oblique load). The stress concentration increased as the crown height increased. It was concluded that: increasing the C/I increased stress concentration in both implant components and cortical bone; parafunctional loading increased between 4-5 times the value of stresses in bone tissue compared with functional loading; the type of loading variation factor is more influential than the crown-to-implant factor.


O objetivo deste estudo foi avaliar, através do método dos elementos finitos tridimensionais, a influência do carregamento oclusal parafuncional e da altura da coroa na distribuição das tensões em próteses unitárias implantossuportadas de hexágono externo. Foram confeccionados três modelos com o auxílio de programas de desenho assistido. Cada modelo foi composto por um bloco ósseo da região molar mandibular, por um implante de tipo hexágono externo (5x10,0 mm) e por coroa com diferentes alturas: 10, 12,5 e 15 mm. Os modelos foram exportados para o programa de elementos finitos NEiNastran 9.0, para geração das malhas e estabelecer as condições de contorno. Aplicou-se uma carga funcional (200 N axial e 100 N oblíqua), bem como uma carga parafuncional (1.000 N axial e 500 N oblíqua). Os resultados foram visualizados por meio de mapas de Tensão de von Mises e mapas de Tensão Máxima Principal. O carregamento parafuncional induziu um aumento da área de distribuição e da magnitude das tensões no implante (plataforma e primeiras roscas) e parafuso (pescoço) em comparação com o carregamento funcional. A cortical óssea apresentou maiores áreas de tensão por tração sob carregamento parafuncional oblíquo. A concentração de tensões aumentou à medida que aumentou a altura da coroa. O aumento da altura da coroa induziu um aumento na concentração de tensões, tanto nos componentes do implante, quanto na cortical óssea; o carregamento parafuncional induziu um aumento entre 4-5 vezes da magnitude das tensões no tecido ósseo; o tipo de carregamento apresenta-se como um fator de variação mais influente do que a proporção coroa/implante.


Subject(s)
Animals , Male , Rats , Flavonoids/pharmacology , Hemodynamics/drug effects , Quercetin/pharmacology , /antagonists & inhibitors , Blood Pressure/drug effects , Dioxolanes/pharmacology , Heart Rate/drug effects , Infusions, Intravenous , Injections, Intravenous , Parasympatholytics , Quercetin/analogs & derivatives , Rats, Inbred Strains , Time Factors
20.
Braz. j. med. biol. res ; 47(10): 876-885, 10/2014. tab, graf
Article in English | LILACS | ID: lil-722165

ABSTRACT

The aim of the present study was to determine the mechanisms underlying the relaxant effect of adrenomedullin (AM) in rat cavernosal smooth muscle (CSM) and the expression of AM system components in this tissue. Functional assays using standard muscle bath procedures were performed in CSM isolated from male Wistar rats. Protein and mRNA levels of pre-pro-AM, calcitonin receptor-like receptor (CRLR), and Subtypes 1, 2 and 3 of the receptor activity-modifying protein (RAMP) family were assessed by Western immunoblotting and quantitative real-time polymerase chain reaction, respectively. Nitrate and 6-keto-prostaglandin F1α (6-keto-PGF1α; a stable product of prostacyclin) levels were determined using commercially available kits. Protein and mRNA of AM, CRLR, and RAMP 1, -2, and -3 were detected in rat CSM. Immunohistochemical assays demonstrated that AM and CRLR were expressed in rat CSM. AM relaxed CSM strips in a concentration-dependent manner. AM22-52, a selective antagonist for AM receptors, reduced the relaxation induced by AM. Conversely, CGRP8-37, a selective antagonist for calcitonin gene-related peptide receptors, did not affect AM-induced relaxation. Preincubation of CSM strips with NG-nitro-L-arginine-methyl-ester (L-NAME, nitric oxide synthase inhibitor), 1H-(1,2,4)oxadiazolo[4,3-a]quinoxalin-1-one (ODQ, quanylyl cyclase inhibitor), Rp-8-Br-PET-cGMPS (cGMP-dependent protein kinase inhibitor), SC560 [5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-trifluoromethyl pyrazole, selective cyclooxygenase-1 inhibitor], and 4-aminopyridine (voltage-dependent K+ channel blocker) reduced AM-induced relaxation. On the other hand, 7-nitroindazole (selective neuronal nitric oxide synthase inhibitor), wortmannin (phosphatidylinositol 3-kinase inhibitor), H89 (protein kinase A inhibitor), SQ22536 [9-(tetrahydro-2-furanyl)-9H-purin-6-amine, adenylate cyclase inhibitor], glibenclamide (selective blocker of ATP-sensitive K+ channels), and apamin (Ca2+-activated channel blocker) did not affect AM-induced relaxation. AM increased nitrate levels and 6-keto-PGF1α in rat CSM. The major new contribution of this research is that it demonstrated expression of AM and its receptor in rat CSM. Moreover, we provided evidence that AM-induced relaxation in this tissue is mediated by AM receptors by a mechanism that involves the nitric oxide-cGMP pathway, a vasodilator prostanoid, and the opening of voltage-dependent K+ channels.


Subject(s)
Animals , Male , Adrenomedullin/pharmacology , Calcitonin Receptor-Like Protein/analysis , Muscle, Smooth/drug effects , Parasympatholytics/pharmacology , Penis/drug effects , Vasodilator Agents/pharmacology , /pharmacology , /analysis , Adrenomedullin/genetics , Adrenomedullin/metabolism , Blotting, Western , Calcitonin Receptor-Like Protein/antagonists & inhibitors , Cyclic GMP-Dependent Protein Kinases/antagonists & inhibitors , Cyclooxygenase Inhibitors/pharmacology , Dose-Response Relationship, Drug , Enzyme Inhibitors/pharmacology , Immunohistochemistry , Indazoles/pharmacology , Muscle Relaxation , Muscle, Smooth/metabolism , Nitric Oxide Synthase/antagonists & inhibitors , Nitric Oxide/analysis , Nitric Oxide/analogs & derivatives , Penis/metabolism , Potassium Channels, Voltage-Gated/metabolism , Rats, Wistar , Real-Time Polymerase Chain Reaction , RNA, Messenger/metabolism , Receptor Activity-Modifying Protein 1/genetics , Receptor Activity-Modifying Protein 1/metabolism , /metabolism , /genetics , /metabolism , Receptors, Calcitonin Gene-Related Peptide/metabolism
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