• Advances in Traditional Medicine
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• 제8권2호
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• pp.196-203
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• 2008

The methanol extract of the root of Artanema sesamoides Family Scrophuilariaceae (MEAS) was investigated for possible analgesic and anti-inflammatory effects in animals. Three models were used to study the extract effects on nociception, which were acetic acid-induced writhing response, hot-plate method and the tail flick test in mice. The antiinflammatory effects were evaluated using carrageenan, dextran, histamine and serotonin induced rat paw oedema (acute) and cotton pellet induced granuloma (chronic) models in rats. Results of the study revealed that the extract exhibited significant (P < 0.001) analgesic effect at a dose of 50, 100 and 200 mg/kg b.w p.o in mice in all the models. In acute model, the MEAS also exhibited significant (P < 0.001) antiinflammatory effect in all the above mentioned doses. In chronic model (cotton pellet induced granuloma) the MEAS 200 mg/kg and indomethacin 10 mg/kg showed that inhibition of granuloma formation 25.0% and 47.7% respectively (P < 0.001). The MEAS and indomethacin were effectively preventing the transudation of the fluid. Thus, the present study revealed that the methanol extract of the root of Artanema sesamoides exhibited significant analgesic and antiinflammatory activity.

• 한국임상약학회지
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• 제28권4호
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• pp.279-284
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• 2018

Objective: To compare the analgesic effects and adverse drug reactions (ADRs) of fentanyl intravenous patient-controlled analgesia (ivPCA) with nefopam, a centrally acting analgesic agent with demonstrated opioid sparing activity, as compared to ketorolac in a tertiary teaching hospital. Methods: A retrospective evaluation of electronic medical records was conducted on patient records including either nefopam or ketorolac with opioid ivPCA for post-operative pain management in general surgery department from January to December 2014. The status of pain control and ADRs were collected. Results: Out of 6,330 general surgery cases, nefopam was given in 153 prescriptions (6.9%) and ketorolac in 81 prescriptions (3.6%). The level of pain control was not different between two groups (70.9% vs. 75.3%; p = 0.51), but ADRs were more frequently reported in nefopam group (9.8% vs. 2.5%; p < 0.05). New ADRs of hot flushes (n = 1) and paresthesia in hands (n = 1) were reported in nefopam group and they were unlisted in the approved package insert. No serious ADRs were reported in both groups. Conclusion: Our findings presented that nefopam showed a similar analgesic effect and higher ADR rates compared to ketorolac as an adjuvant to fentanyl iv PCA for post-operative pain management in general surgery patients in South Korea.

• 약학회지
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• 제27권4호
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• pp.263-270
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• 1983

Effective BuOH fraction was extracted from Puerariae radix (Pueraria thunbergiana), and several pharmacological activities were examined. From several pharmacological examinations, it was found that BuOH fraction has an antipyretic activity against typhoid vaccine pyrexia in rabbit, a papaverine-like antispasmodic activity on isolated ileum and jejunum of rat, an analgesic effects on mice treated by 0.7% HAc, and an anti-inflammatory activity of carrageenin edema in rat. It was found that BuOH fraction has detoxication effects on acute and subacute toxic rat induced by alcohol in consequence of biochemical tests of serum. Therefore it was considered that BuOH fraction has preventive and therapeutic effects in alcohol intoxication.

• Biomolecules & Therapeutics
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• 제5권1호
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• pp.94-99
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• 1997

Capsaicin is known to be an analgesic agent, affecting the synthesis, storage, , transport and release of substance p, the principal neurotransmitter of pain from periphery to the central nervous system(CNS). DA-5018, a newly synthesized capsaicin derivative has shown potent analgesic effect comparable to that of morphine in various rat models of experimentally inducted acute pairs. In this study the mechanism of analgesic actlvity of DA-5018 was examined. First, the electrically-evoked contraction of guinea pig trachea was inhibited by DA-5018 and these inhibition was recovered by incubation with capsafepine(3$\muM$), capsaicin receptor antagonist and this result suggested that DA-5018 has affinity on capsaicin receptor. The correlation between the norciceptive threshold and the release of substance P was evaluated. In vivo perfusion of slices of the rat spinal cord with DA-5018(10, 100$\muM$) produced a significant increase of the release of substance P and this increase was less than that of capsaicin(10$\muM$). The norciceptive threshold of rat treated with DA-5018(1 mg/kg, p.o) in tall pinch test increased from 2.9$\pm$0.3 to 23.5 $\pm$6.61. Tail pinch latency increased to a maximun at 15 min after DA-5018 treatment and then declined to control values by 120 min. The capsaicin-evoked release ot substance P from the spinal cord slices of rat treated with DA-5018 reduced from 2.38$\pm$ 0.79 to 0.69$\pm$ 0.26 pg/mg wet weight. This reduction reached to a minium at 15 min after DA-5018 treatment and then recovered to control value by 120 min. These results mean that analgesic activity of DA-5018 is due to release of substance P The effect of DA-5018 cream on electrically-evoked neurogenic inflammation of rat saphenous nerve was compared with capsaicin (zostrix-HP). DA-5018 showed 34% inhibition of the neurogenic extravasation while capsaicin showed significant 67% inhibition. This result indicates that the potency of DA-5018 in the release of substance P is less than that of capsaicin. These results suggest that the release of substance P is partially involved in the mechanism of analgesic action of DA-50l8.

• 생약학회지
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• 제30권2호
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• pp.137-144
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• 1999

Torilin was isolated from haxane fraction of Torilis Fructus extract. Torilin produced inhibition of the acetic acid-induced and phenylquinone-induced writhing syndrome at the oral doses of 30 and 90 mg/kg in mice. It also increased the pain threshold at the oral doses of 30, 90 and 270 mg/kg in the tail pressure method and the Randall-Selitto method. However, it did not show a hypothermic action at the oral doses of 30 and 90 mg/kg in mice. The compound exhibited strong anticarrageenan activity at the oral doses of 90 and 270 mg/kg in rats, and had inhibitory effect on the vascular permeability at the oral doses of 30 and 90 mg/kg in mice. It also showed potent inhibition of leucocyte emigration in CMC-pouch at the doses of 3 and 9 mg/rat, sc. The acute toxicity of torilin was very weak: the $LD_{50}$ values were more than 5000 mg/kg, po and 2000 mg/kg, ip in mice. From the above mentioned results, it was suggested that torilin had potent analgesic and anti-inflammatory activities.

• 생약학회지
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• 제36권4호통권143호
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• pp.299-304
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• 2005

This study examined the antinociceptive properties of GCSB-5, a herbal formulation consisting of 6 Oriental herbs (Ledebouriellae Radix, Achyranthis Radix, Acanthopanacis Cortex, Cibotii Rhizoma, Glycine Semen, and Eucommiae Cortex) that are used in traditional medicine to treat various bone disorders, mainly of which involve analgesic processes. Peripheral and central analgesic models were established in experimental animals in order to evaluate the antinociceptive effects of the agent. GCSB-5 significantly inhibited the number of acetic-induced writhing (33.3%-34.3% inhibition at 100-600 mg/kg) but increased the pain threshold (38.0% increase at 300 mg/kg) in the Randall-Selitto test. However, GCSB-5 had no effect on the hot plate-induced nociception and hyperalgesia from the tail-pinch method. These results suggest that the antinociceptive effect of GCSB-5 may be mediated via peripheral mechanisms.

• 약학회지
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• 제25권1호
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• pp.27-35
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• 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.

• 약학회지
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• 제34권2호
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• pp.126-132
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• 1990

To enhance the activity of ibuprofen, amides of ibuprofen, 1-piperazinyl-2-(4-isobutylphenyl)propionamide(Ibu-P.A.) and 1-(4-methylpiperazinyl)-2-(4-isobutylphenyl)propionamide (Ibu-M.P.), were synthesized and the pharmaceutical properties and the pharmacological activities of the amides were studied. The lipid:water partition coefficients and pKa values were examined in vitro, and the antiinflammatory effect, analgesic effects, acute toxicity, and intestinal absorption were studied for the amides and compared with ibuprofen in vivo. The results are summarized as belows; 1) The lipid:water partition coefficients of Ibu-M.P. were higher than those of ibuprofen. 2) The calculated pKa values of ibuprofen and Ibu-M.P. were 5.49 and 8.66, respectively. 3) The antiinflammatory effects of ibuprofen, Ibu-P.A., and Ibu-M.P. were same intensity, but the duration of the effects of Ibu-P.A. and Ibu-M.P. were longer than that of ibuprofen. 4) The analgesic effect of Ibu-M.P. was more potent than those of ibuprofen and Ibu-P.A. in the acetic acid-induced writhing test. 5) The $LD_{50}$ was 495 mg/kg for ibuprofen, 187 mg/kg for Ibu-M.P., and over 1250 mg/kg for Ibu-P.A.. 6) The absorption rate constants(k) and half-life($t_{1/2}$) were 0.74($hr^{-1}$) and 0.94(hr) for ibuprofen, and 0.72 ($hr^{-1}$) and 0.96 (hr) respectively for Ibu-M.P..

• 대한한방내과학회지
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• 제19권2호
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• pp.88-106
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• 1998

This study was designed to elucidate the antiinflammatory, cardiovascular, antithrombotic, and analgesic effect of Sambitang. The antiinflammatory effects was measured by the method of carrageenin induced edema, protein leakage test using CMC-pouch, and the effect of Sambitang on the cardiovascular system was observed by the change of flow rate of Ringer solution in the vascular system in the ear of rabbit, and the contraction and dilatation of rat tail artery. Death rate, platelet aggregation, plasma coagulation activity was observed for the measurement of the anticoagurative effect of Sambitang, and the analgesic effect was measured by the acetic acid method and hot plate method. The result was as follows: 1. Sambitang administration, edema and protein leakage was significantly decreased. 2. The drug increased the auricular blood flow in rabbit. 3. The drug relaxed the artery contraction by pretreated norepinephrine in rat. 4. The drug inhibited the death rate of mouse which was led to thromboembo- lism by serotonin and collagen. 5. The drug inhibited the platelet aggregation in rat. 6. The drug prolonged the prothrombin time and activated partial thromboplastin time on the test of plasma coagulation factor activity in rat, but was not valuable. 7. The slight anagesic effect of Sambitang extract was confirmed by the observation of writhing syndrome, paw licking time, and escape time.

• 대한약학회:학술대회논문집
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• 대한약학회 2001년도 Proceedings of International Convention of the Pharmaceutical Society of Korea
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• pp.247.1-247.1
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• 2001