• YAKHAK HOEJI
• /
• v.25 no.1
• /
• pp.27-35
• /
• 1981

Etomidoline is a new synthetic atropine-like drug. The present investigation aimed to study the combined effects of etomidoline and neofopam hydrochloride which has an analgesic and muscle relaxant activity, compared with the effects of each drugs. Acute toxicities (ID$_{50}$) in mouse were 132mg/Kg (p.o.) and 49mg/Kg (i.p.) when combination ratio of etomidoline and neofopam was 1:5 and 103 mg/Kg (p.o.) and 30mg/Kg (i.p.) with the ratio of 1:10. Etomidoline showed more potent anticholinergic effects than neofopam in the isolated rat intestine. Whereas, antibarium effects were twice as active with neofopam than with etomidoline. When etomidoline and neofopam were added in combination ratio of 1 : 5, papaverine-like avtivity was increased, but no changes of anticholinergic effect were observed. Analgesic effect was measured by the anti-writhing method of Whittle in mice. Both of the concurrent and single administration of etomidoline and nefopam reduced significantly the writhing number and the effect of the concurrent administration was more active than that of single, and 1 : 5 combination was slightly more potent than 1:10. Each drug or the combined drug was administered to mice and observed the change of the pupil size. Pupil sizes were increased with each drug and with combined drug, although there were no significant differences between the each group of drugs. However, those effects were less than that of atropine sulfate.e.

• YAKHAK HOEJI
• /
• v.50 no.4
• /
• pp.293-299
• /
• 2006

The aim of present study was to investigate the possible influence of Rho-kinase inhibition on the plant-derived estrogen-like compounds-induced arterial relaxation. Agonist- or depolarization-induced vascular smooth muscle contractions involve the activation of Rho-kinase pathway. However there are no reports addressing the question whether this pathway is involved in genistein-or daidzein-induced vascular relaxation in rat aortae precontracted with phenylephrine or thromboxane $A_2$ mimetic U-46619. We hypothesized that Rho-kinase inhibition plays a role in vascular relaxation evoked by genistein or daidzein in rat aortae. Endothelium-intact and denuded arterial rings from male Sprague-Dawley rats were used and isometric contractions were recorded using a computerized data acquisition system. Genistein concentration-dependently inhibited phenylephrine or thromboxane $A_2-induced$ contraction regardless of endothelial function. Surprisingly, in the agonists-induced contraction, similar results were also observed in aortae treated with daidzein, the inactive congener for protein tyrosine kinase inhibition, suggesting that Rho-kinase might act upstream of tyrosine kinases in phenylephrine-induced contraction. In conclusion, in the agonists-precontracted rat aortae, genistein and daidzein showed similar relaxant response regardless of tyrosine kinase inhibition or endothelial function.

• Journal of Pharmacopuncture
• /
• v.22 no.1
• /
• pp.7-15
• /
• 2019

Portulaca oleracea L. (PO) or Purslane is an annual grassy plant that is distributed in many parts of the world, especially the tropical and subtropical areas. PO has some pharmacological properties such as analgesic, antibacterial, skeletal muscle-relaxant, wound-healing, anti- inflammatory and a radical scavenger. This review article is focused on the anti-inflammatory, immuno-modulatory, anti-oxidant and anti-tumor activities of the PO. Anti-inflammatory, immuno-modulatory, anti-oxidant and Anti-tumor effects of PO were searched using various databases until the end of August 2018. The online literature was searched using PubMed, Science Direct, Scopus, Google Scholar and Web of Science. Our review showed that PO exerts its effects through anti-inflammatory properties and balancing the adaptive and innate immune system depending on situations. PO acts as immune-modulator and anti-oxidant agent in both inflammatory states by the dominance of Th2 response such as asthma, cancer and atopic dermatitis and evoked Th1 disorders including hepatitis and multiple sclerosis.

• Clinical and Experimental Pediatrics
• /
• v.46 no.2
• /
• pp.192-194
• /
• 2003

A neonate born at 38 gestational weeks was admitted due to generalized tonic-clonic seizure and cyanosis. The neonate was born six days previously at home through normal delivery and the umbilical cord was cut using scissors sterilized in boiling water. The neonate weighed 3,180 g at admission. Physical examination revealed cyanosis, opisthotonus, trismus and reactive muscle spasms. Laboratory exam, brain sonogram and EEG showed no significant abnormal findings. Based on her history and physical examination, the neonate was diagnosed with tetanus and put in an incubator isolated in a quiet, dark room. Treatment with tetanus human immunoglobulin along with antibiotics (penicillin G) were started immediately, and mechanical ventilation, administration of neuromuscular blocking agent and muscle relaxant were also started off. The frequency of seizure episode decreased gradually, and on the 32nd hospital day, mechanical ventilatory support was stopped along with extubation two days later. Thereafter, the neonate was in continuous generalized hypertonic state and showed feeding difficulty, but there was gradual improvement. She was dismissed on the 49th hospital day and is currently under OPD follow-up, doing well with no special problems. Respiratory management is critical to neonatal tetanus. We report here a case of tetanus treated with inhibition of self-respiration, neuromuscular blocker and application of ventilator, and present this method as a useful direction for future treatment of neonatal tetanus.

• Journal of Chest Surgery
• /
• v.28 no.8
• /
• pp.742-746
• /
• 1995

The present study was aimed at investigating possible transmitter mechanisms in the endothelial cell layer in regulating the tone of the vascular smooth muscle. The thoracic aorta was isolated from the anesthetized male white rabbits and its helical strips were prepared. Electrical field stimulation was delivered to platinum wire electrodes positioned parallel to the vessel segment preconstricted with phenylephrine [3.5x10-6 mol/L at a distance of 1.5-2.0 mm. The electrical stimulation [70 V, 5 msec, 0.5-200 Hz caused either relaxation only [34% or a biphasic response [prolonged relaxation following a weak and transient contraction, 66% . The relaxation response was frequency- dependent, and at 200 Hz a complete relaxation was noted. Mechanical rubbing of the endothelial layer abolished or greatly attenuated the relaxation. The relaxation was also markedly attenuated in the presence of NG-nitro- L-arginine methyl ester [10-3mol/L or procaine hydrochloride [3.5x10-4mol/L . Tetrodotoxin,guanethidine, atropine or indomethacin failed to block or enhance the relaxation response to electrical field stimulation. It is concluded that the vascular endothelium in the aorta contains diffusible substances that regulates the function of the smooth muscle layer, in which relaxation is more prominent than contraction. Their release by the electrical stimualtion in vitro may not involve classic neuronal transmitter release mechanisms or metabolism of arachidonic acids by cyclooxygenase. The release of the relaxing agents may require an increase in cytosolic calcium level. The chemical nature of the relaxant may be, to a large extent, nitric oxide.

• Journal of Pharmacopuncture
• /
• v.21 no.2
• /
• pp.70-75
• /
• 2018

Objective: Diseases of the respiratory system are one of the main causes of death and include situation such as chronic obstructive pulmonary disease, pneumonia or asthma. Medicinal plants have beneficial effects on multiple diseases include respiratory disorders like asthma and bronchitis. The aim of this study was to evaluate the effects of U. dioica and L. Album on tracheal smooth muscle contraction. Material and methods: Hydroalcoholic extracts of L. Album and U. Dioica aerial parts were prepared by maceration method and standardized based on their total phenol content. The effect of the extracts on the KCl-induced contraction of rat trachea was examined in an organ bath chamber. Data was analyzed with spss software 22. Results: The extract of L. Album (5 mg/ml), similar to theophylline (20 mM), significantly reduced the KCl-induced tracheal contraction. On the other hand, U. Dioica (1 mg/ml and 5 mg/ml) augmented the KCl-induced contraction. Conclusion: The relaxant effect of L. Album on the trachea makes it as a candidate for the managing patients with asthma and obstructive pulmonary diseases. But because of U. Dioica potential constrictive effect on the trachea it is suggested that patients avoid consuming it.

• Archives of Pharmacal Research
• /
• v.29 no.5
• /
• pp.400-404
• /
• 2006

This study examined the effect of Gamma-Amino butyric acid (GABA) and selective GABA receptor related drugs on the electrically stimulated relaxation in the lower esophageal sphincter muscle (LES) of a cat. Tetrodotoxin $(10^{-6}\;M)$ suppressed the electrically stimulated (0.5-5 Hz) relaxation of the LES. However, guanethidine $(10^{-6}\;M)$ and atropine $(10^{-6}\;M)$ had no effect indicating that the relaxations were neurally mediated via the nonadrenergic and noncholinergic (NANC) pathways. NG-nitro-L-arginine methyl ester ($10^{-4}M$, L-NAME) also inhibited the relaxant response but did not completely abolish the electrically stimulated relaxation with 60% inhibition, which suggests the involvement of nitric oxide as an inhibitory transmitter. This study examined the role of GABA, an inhibitory neurotransmitter, on neurally mediated LES relaxation. GABA ($10^{-3}-10^{-5}M$, non selective receptor agonist), muscimol ($10^{-3}-10^{-5}M$, GABA-A agonist), and baclofen ($10^{-3}-10^{-5}M$, GABA-B agonist) had no significant effect on the electrically stimulated relaxation. Moreover, bicuculline ($10^{-5}M$, GABA-A antagonist) and phaclofen ($10^{-5}M$, GABA-B antagonist) had no inhibitory effect on the electrically stimulated relaxation. This suggests that GABA and the GABA receptor are not involved in the electrically stimulated NANC relaxation in the cat LES.

• The Korean Journal of Pain
• /
• v.2 no.1
• /
• pp.66-71
• /
• 1989

It has been standard practice in many institutions to use a combination of a light general anesthesia and an epidural block for lower abdominal and pelvic surgery. This combination of a balanced anesthesia can provide various benefits to the patient such as less bleeding in the surgical field, the use of a lower concentration of general anesthetics, less muscle relaxant, and post operative pain management. However, there are several problems associated with hemodynamics such as bradycardia and hypotension etc. In order to block the pain of the high surgical area with a lumbar epidural puncture postoperatively, a large volume of local anesthetic is required and consequently an extensive blockade of sympathetic, sensory and motor functions can occur causing motor weakness, numbness and postural hypotension. Therefore, the patient is unable to have early ambulation postoperatively. In this study, thoracic epidural catheterization was undertaken to locate the tip of the catheter exactly at the surgical level for upper abdominal surgery, and was followed by general anesthesia. Twenty-one patients scheduled for upper abdominal surgery were selected. Fifteen of them had hepatobiliary operations and the remaining 6 had gastrectomies. Thoracic epidural punctures were performed mostly at T9-T10 (57.1%) and T8-T9. Neuromuscular blocking agents were not used in half of the cases and the, mean doses of relaxant were $3.5{\pm}1.0mg$ in gastrectomies, and $2.7{\pm}0.9mg$ in cases of hepatobiliary operation. Epidural morphine was injected 1 hour before the end of the operation for postoperative pain control. Eight patients did not require additional analgesics and the mean dose of epidural morphine was $2.2{\pm}0.9mg$, and 13 cases were given 0.125% epidural bupivacaine when patients complained of pain. Their initial doses of epidural morphine were $1.9{\pm}0.4mg$ and the mean duration of bupivacaine was 6 hours 20 minutes${\pm}40$ minutes. In conclusion. thoracic epidural analgesia is valuable to reduce postoperative pain in patients with upper abdominal surgery, However, it is not easy to maintain this balanced anesthesia with high epidural analgesia-and light general anesthesia for upper abdominal surgery because of marked hemodynamic changes. Therefore, further practice will be required.

• The Korean Journal of Physiology and Pharmacology
• /
• v.2 no.2
• /
• pp.251-260
• /
• 1998

Cromakalim (BRL 34915), known as an airway smooth muscle relaxant, inhibited the releases of mediators in the antigen-induced mast cell activation. It has been suggested that cromakalim, in part, inhibited mediator releases by inhibiting the initial increase of 1,2-diacylglycerol (DAG) produced by the activation of the other phospholipase system which is different from phosphatidylcholine-phospholipase D pathway. The aim of this study is to further examine the inhibitory mechanism of cromakalim on the mediator release in the mast cell activation. Guinea pig lung mast cells were purified by using enzyme digestion and percoll density gradient. In purified mast cells prelabeled with $[^3H]PIP_2$, phospholipase C (PLC) activity was assessed by the production of $[^3H]$insitol phosphates. Protein kinase C (PKC) activity was assessed by measuring the protein phosphorylated from mast cells prelabeled with $[{\gamma}-32P]ATP$, and Phospholipase $A_2\;(PLA_2)$ activity by measuring the lyso-phosphatidylcholine produced from mast cell prelabeled with 1-palmitoyl-2-arachidonyl $phosphatidyl-[^{14}C]choline$. Histamine was assayed by fluorometric analyzer, and leukotrienes by radioimmunoassay. The PLC activity was increased by activation of the passively sensitized mast cells. This increased PLC activity was decreased by cromakalim pretreatment. The PKC activity increased by the activation of the passively sensitized mast cells was decreased by calphostin C, staurosporine and cromakalim, respectively. The $PLA_2$ activity was increased in the activated mast cells. The pretreatment of cromakalim did not significantly decrease $PLA_2$ activity. These data show that cromakalim inhibits histamine release by continuously inhibiting signal transduction processes which is mediated via PLC pathway during mast cell activation, but that cromakalim does not affect $PLA_2$ activity related to leukotriene release.

• Journal of The Korean Society of Clinical Toxicology
• /
• v.1 no.1
• /
• pp.34-39
• /
• 2003

Carisoprodol (CSP) is commonly prescribed as a skeletal muscle relaxant. Recently, we encountered 7 suicidal cases in which carisoprodol was detected. We developed a rugged, sensitive, and specific method for the determination of CSP and meprobamate (MPB) by GC and GC/MS. Postmortem blood concentrations of CSP and MPB ranged 22.9-124.4 ,$\mu$g/ml and its metabolite, 26.8-144.5 ,$\mu$g/ml respectively. Among 7 cases studied, Only CSP was ingested in 4 cases and combination of CSP and dextromethorphan was ingested in 2 cases according to the case history and one case was with ethanol. The order of the tissue concentration of CSP and MPB was liver> kidney > brain, and the concentration of MPB was higher than that of CSP in all tissues. The MPB /CSP concentration ratios of urine, bile juice, liver, kidney, brain and blood were 15.7, 4.0, 1.2, 1.4, 1.4 and 1.0 respectively. There was a big difference in concentration of CSP and MPB in 7 cases due to differences in the amount of dose administered and time to death after dosing.