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1.
Chinese Journal of Clinical Pharmacology and Therapeutics ; (12): 1153-1158, 2021.
Article in Chinese | WPRIM | ID: wpr-1014958

ABSTRACT

AIM: To observe the effect of acute normovolemic hemodilution (ANH) autologous blood transfusion on the EEG bispectral index and muscle relaxation in elderly patients undergoing orthopedic surgery to explore the influence of autologous blood transfusion containing anesthetic components on the quality and safety of postoperative anesthesia recovery. METHODS: Forty patients, aged 65-75, weighing 55-80 kg, ASA grade I-II, with an estimated intraoperative blood loss of more than 600 mL, were selected for elective orthopedic surgery. The patients were randomly divided into two groups (n=20): group A was given acute normovolemic hemodilution (ANH), and the target value of Hct was 28%-30% after induction of anesthesia; group B was the control group which was given routine fluid infusion during operation without ANH. Bispectral index (BIS), TOF values and plasma concentrations of propofol and cisatracurium were measured at the beginning of autotransfusion (T

2.
Bol. latinoam. Caribe plantas med. aromát ; 17(6): 610-618, nov. 2018. ilus, tab
Article in English | LILACS | ID: biblio-1007367

ABSTRACT

Peperomia hispidula (Sw.) A. Dietr. is used in Mexican traditional medicine for treating respiratory illnesses such as asthma. The latter disorder results from an excessive and inappropriate constriction of airway smooth muscle. The aim of the present study was to evaluate the relaxant activity of P. hispidula on isolated rat tracheal rings contracted with carbachol. The methyleugenol was identified as the main active constituent in the dichloromethane extract. To explore the possible mechanism of action, concentration-response curves were constructed in the presence and absence of propranolol (3 µM), indomethacin (10 µM), glibenclamide (1 µM), and L-NAME (300 µM), finding that neither reduced methyleugenol-induced smooth muscle relaxation. In conclusion, P. hispidula herein displayed relaxant activity on rat tracheal rings. The effect of methyleugenol, was probably not related to the activation of ß2-adrenoceptors, prostaglandins, K+ATP channels or nitric oxide.


Peperomia hispidula (Sw.) A. Dietr. es utilizada en la medicina tradicional mexicana para tratar enfermedades respiratorias como el asma. Este último trastorno es el resultado de una contracción excesiva e inapropiada del músculo liso de las vías respiratorias. El objetivo del presente estudio fue evaluar la actividad relajante de P. hispidula sobre anillos aislados de tráquea de rata contraídos con carbacol. El metileugenol fue identificado como el principal constituyente activo en el extracto de diclorometano. Para explorar el posible mecanismo de acción, se construyeron curvas concentración-respuesta en presencia y ausencia de propranolol (3 µM), indometacina (10 µM), glibenclamida (1 µM), y L-NAME (300 µM), encontrando que ninguno redujo la relajación del músculo liso inducida por metileugenol. En conclusión, P. hispidula muestra actividad relajante en anillos de tráquea de rata. El efecto de metileugenol, al parecer no está implicado con la activación de los receptores ß2-adrenérgicos, prostaglandinas, canales de K+ATP u óxido nítrico.


Subject(s)
Animals , Male , Rats , Trachea/drug effects , Eugenol/analogs & derivatives , Eugenol/pharmacology , Plant Extracts/pharmacology , Peperomia , Asthma/metabolism , Tracheal Stenosis/chemically induced , Eugenol/isolation & purification , Chromatography, High Pressure Liquid , Tandem Mass Spectrometry , Methylene Chloride/chemistry , Muscle Relaxation/drug effects
3.
Article in English | IMSEAR | ID: sea-180455

ABSTRACT

This study aims to investigate the mechanism of relaxant action of Ethyl 6-amino-5-cyano-2-methyl-4-(pyridin- 4-yl)- 4H-pyran-3-carboxylate (1) in in silico study and ex vivo tracheal rat rings pre-contracted with carbachol (1 µM). Compound 1 was more active than theophylline [a phosphodiesterases (PDE’s) inhibitor] used as positive control. Moreover, pretreatment with 1 significantly shifted to the right the carbachol-induced contraction and did not allow to reach the maximum effect (p< 0.001). In addition, compound 1 (96.30 µM) produces significant (100%) relaxant effect on the contraction induced by KCl (80mM), and the CaCl2-induced contraction was completely abolished by 1 as nifedipine does (a L-type calcium channel blocker), used as positive control (p< 0.001). Meanwhile, in the presence of isoproterenol (a β-adrenergic agonist), propranolol (a β-adrenergic antagonist), and K+ channel blocker 2-AP the relaxant curve was significantly modified (p< 0.05). Compound 1 was docked on an outer cavity located on the intracellular side of the human L-type calcium channel model and interacts in the following chains and residues: chain IP (G51, W52, T53, D54), IVP (R45, E50, A51, Q53, D54) and IS6 (W4, F7). In conclusion, ex vivo and in silico approaches suggest that compound 1 induces its relaxant effect mainly by calcium channel blockade, but other mechanisms like potassium channel and cAMP accumulation could be involved.

4.
Chinese journal of integrative medicine ; (12): 377-383, 2016.
Article in English | WPRIM | ID: wpr-310908

ABSTRACT

<p><b>OBJECTIVE</b>To examine the relaxant effects of hydro-ethanolic, macerated aqueous (MA) and lipidfree macerated aqueous (LFMA) extract of Tymus vulgaris on tracheal chains of guinea pigs.</p><p><b>METHODS</b>The relaxant effects of five cumulative concentrations of each extract (0.4, 0.8, 1.2, 1.6 and 2.0 g/100 mL) were compared with saline as negative control and five cumulative concentrations of theophylline (0.1, 0.2, 0.4, 0.6 and 0.8 mmol/L) on precontracted tracheal smooth muscle of guinea pig with 60 mmol/L KCl (group 1) and 10 µmol/L methacholine (group 2, n=6 for each group).</p><p><b>RESULTS</b>In group 1 all concentrations of theophylline, three higher concentrations of hydro-ethanolic, two concentrations of LFMA and last concentration of MA extracts showed significant relaxant effects compared with that of saline (P<0.05 or P<0.01). Two lower concentrations of LFMA and all concentrations of MA except higher one caused contraction compared with saline (P<0.05 or 0.01). In group 2 experiments, all concentrations of theophylline, hydro-ethanolic, MA and LFMA extracts showed significant relaxant effects compared to that of saline (P<0.05 or P<0.01). In both groups, the relaxant effect of all concentrations of hydro-ethanolic extract were significantly higher than most concentrations of others (P<0.05 or P<0.01). The relaxant effect of different concentrations of three extracts were significantly greater in group 2 compared with group 1 experiments (all P<0.01). There were significantly positive correlations between the relaxant effects and concentrations for theophylline and all extracts in both groups (P<0.05 or P<0.01).</p><p><b>CONCLUSION</b>Hydro-ethanolic extract has a potent weaker relaxant effect for other extracts from Tymus vulgaris on tracheal chains of guinea pigs.</p>


Subject(s)
Animals , Bronchodilator Agents , Pharmacology , Guinea Pigs , In Vitro Techniques , Lamiaceae , Chemistry , Lipids , Chemistry , Muscle Relaxation , Muscle, Smooth , Physiology , Plant Extracts , Pharmacology , Solubility , Solutions , Theophylline , Trachea , Physiology , Water , Chemistry
5.
Asian Pacific Journal of Tropical Medicine ; (12): 179-183, 2014.
Article in English | WPRIM | ID: wpr-819709

ABSTRACT

OBJECTIVE@#To assess the relaxant effect of several organic extracts obtained from Agastache mexicana (A. mexicana), Cochlospermum vitifolium (C. vitifolium), Cordia morelosana (C. morelosana), Lepechinia caulescens (L. caulescens) and Talauma mexicana (T. mexicana) used in Mexican traditional medicine for the treatment of several diseases.@*METHODS@#Extracts were obtained by maceration at room temperature using hexane, dichloromethane and methanol for each plant material. The organic extracts were evaluated ex vivo to determine their relaxant activity on the contractions induced by carbachol (cholinergic receptor agonist, 1 μ mol/L) in isolated rat tracheal rings.@*RESULTS@#A total of 15 extracts were evaluated (three for each species). All test samples showed significant relaxant effect, in a concentration-dependent manner, on the contractions induced by 1 μ mol/L carbachol, with exception of extracts from C. morelosana. Active extracts were less potent than theophylline [phosphodiesterase inhibitor, EC50: (28.79±0.82) μg/mL] that was used as positive control. Concentration-response curves revealed that the extracts with more significant effects were dichloromethanic extracts of T. mexicana [Emax: (103.03±3.32)% and EC50: (159.39±3.72) μg/mL) and C. vitifolium [Emax: (106.58±2.42)% and EC50: (219.54±7.61) μg/mL]. Finally, hexanic and dichloromethanic extracts from A. mexicana were fully effective but less potent than T. mexicana and C. vitifolium.@*CONCLUSIONS@#Less polar extracts obtained from A. mexicana, T. mexicana and C. vitifolium exhibited greater relaxant effect on tracheal rat rings, which allows us to suggest them as sources for the isolation of bioactive molecules with potential therapeutic value in the treatment of asthma.


Subject(s)
Animals , Male , Rats , Chemical Fractionation , Dose-Response Relationship, Drug , Medicine, Traditional , Mexico , Plant Extracts , Pharmacology , Plants, Medicinal , Chemistry , Rats, Wistar , Respiratory System Agents , Pharmacology , Trachea , Chemistry
6.
The Journal of The Japanese Society of Balneology, Climatology and Physical Medicine ; : 127-137, 2000.
Article in Japanese | WPRIM | ID: wpr-372823

ABSTRACT

Thirty-one outpatients with acute low back pain were all educated about activities of daily living. They also received spinal manipulation and SSP (TENS), and took NSAID for a certain period of time. Half of them were additionally exposed an electric field using HEAL THTRON, an electric field therapeutic decice, in order to analyze its efficacy.<br>The patients were randomly divided (non-blind test) into two groups. Those who received ordinary treatment were called the Non-HEALTHTRON group (NH-group); those who received HEALTHTRON treatment in addition to ordinary treatment were called the HEALTHTRON Treatment group (H-group). During the 15-day study period, the patients were subjected to a total of four electric field exposures using HEALTHTRON. Efficacy of the treatment was measured as an objective evaluation by measuring range of motion (ROM) using an inclinometer, and Peak torque and Total work using a dynamometer. A subjective evaluation was performed using the Oswestry Low Back Pain Disability Questionnaire, ADL pain questionnaire, Visual analog scale for Patient global assessment, VAS (Patient) and Visual analog scale for Physician global assessment, VAS (Physician). After ordinary treatment, significant improvement was found in all 31 patients with acute low back pain. The VAS (Physician), ADL pain questionnaire and ROM were more significantly improved in the H-group than in the NH-group.

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