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Four Novel Synthetic Tryptamine Analogs Induce Head-Twitch Responses and Increase 5-HTR2a in the Prefrontal Cortex in Mice

  • Abiero, Arvie;Ryu, In Soo;Botanas, Chrislean Jun;Custodio, Raly James Perez;Sayson, Leandro Val;Kim, Mikyung;Lee, Hyun Jun;Kim, Hee Jin;Seo, Joung-Wook;Cho, Min Chang;Lee, Kun Won;Yoo, Sung Yeun;Jang, Choon-Gon;Lee, Yong Sup;Cheong, Jae Hoon
    • Biomolecules & Therapeutics
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    • v.28 no.1
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    • pp.83-91
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    • 2020
  • Tryptamines are monoamine alkaloids with hallucinogenic properties and are widely abused worldwide. To hasten the regulations of novel substances and predict their abuse potential, we designed and synthesized four novel synthetic tryptamine analogs: Pyrrolidino tryptamine hydrochloride (PYT HCl), Piperidino tryptamine hydrochloride (PIT HCl), N,N-dibutyl tryptamine hydrochloride (DBT HCl), and 2-Methyl tryptamine hydrochloride (2-MT HCl). Then, we evaluated their rewarding and reinforcing effects using the conditioned place preference (CPP) and self-administration (SA) paradigms. We conducted an open field test (OFT) to determine the effects of the novel compounds on locomotor activity. A head-twitch response (HTR) was also performed to characterize their hallucinogenic properties. Lastly, we examined the effects of the compounds on 5-HTR1a and 5-HTR2a in the prefrontal cortex using a quantitative real-time polymerase chain reaction (qRT-PCR) assay. None of the compounds induced CPP in mice or initiated SA in rats. PYT HCl and PIT HCl reduced the locomotor activity and elevated the 5-HTR1a mRNA levels in mice. Acute and repeated treatment with the novel tryptamines elicited HTR in mice. Furthermore, a drug challenge involving a 7-day abstinence from drug use produced higher HTR than acute and repeated treatments. Both the acute treatment and drug challenge increased the 5-HTR2a mRNA levels. Ketanserin blocked the induced HTR. Taken together, the findings suggest that PYT HCl, PIT HCl, DBT HCl, and 2-MT HCl produce hallucinogenic effects via 5-HTR2a stimulation, but may have low abuse potential.

A Literature Study on the Korean Acupuncture for the Treatment of Stroke (국내침구서적의 중풍치료에 관한 문헌 연구 - $\ll$치종지남(治腫指南)$gg$$\ll$동의보감(東醫寶鑑)$gg$$\ll$침구경험방(鍼灸經驗方)$gg$$\ll$교감 사암도인침법(校勘 舍岩道人鍼法)$gg$의 비교연구 -)

  • Han, Chang-Hyun;Park, Sang-Young;Ahn, Sang-Young;Kwon, Oh-Min;Ahn, Sang-Woo
    • Korean Journal of Acupuncture
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    • v.26 no.2
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    • pp.145-163
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    • 2009
  • Background : Stroke occurrences are prevalent and require intensive care for its treatment and rehabilitation. Acupuncture has been widely used in Korea throughout the history and provides an efficient method in the treatment of it. Objectives : To establish a distinctive and efficient acupuncture method for the treatment of stroke based in literature research. Method : We reviewed four Korean medical literature, $ll$治腫指南Guide to Swollen Sore Treatment$gg$, $ll$東醫寶鑑Treasured Mirror of Eastern Medicine$gg$, $ll$鍼灸經驗方Experiential Prescriptions of Acupuncture and Moxibustion$gg$, and $ll$舍岩鍼法Essential Rhymes on Acupuncture and Moxibustion by Master Sa-am$gg$, and analyzed the therapeutic characteristics in the treatment of stroke. Result : 1. In $ll$治腫指南Guide to Swollen Sore Treatment$gg$, various types of treatment can be found. Besides acupuncture, cupping, moxibustion with moxa tube, and bath therapy using Duchesneae Indicae Herba and Sal was applied. Needling in sublingual and vocal region, and also points like GB20, GB31, LI15, BL60, GV20, GV20, TE4, GB39, LU5, ST36, GB30 were frequently inserted. 2. In $ll$東醫寶鑑Treasured Mirror of Eastern Medicine$gg$, moxibustion treatment were in top priority. Points like GV20, LI15, LI11, GB31, ST36, GB39, LI4, GB20 pertinent to Governor, Conception, Gallbladder, Large Intestine, and Stomach meridian were most frequently needled. Selection of adjacent point was widely applied. 3. $ll$鍼灸經驗方Experiential Prescriptions of Acupuncture and Moxibustion$gg$ has some similarity compared to $ll$東醫寶鑑 Treasured Mirror of Eastern Medicine$gg$ in considering the moxa in top priority. But selected points far from the disease site. Main points were LI4, ST36, GB39, PC5, GV20, LI11, LR3, BL40, HT7. 4. $ll$校勘 舍岩道人鍼法Essential Rhymes on Acupuncture and Moxibustion by Master Sa-am$gg$ having the same content orders with $ll$鍼灸經驗方Experiential Prescriptions of Acupuncture and Moxibustion$gg$, it may had some influence from it. But the differences are also apparent. It emphasized in using mother-supplementing child-draining method, experiential prescriptions and visceral pattern identification. Conclusions : We could find various efficient methods through literature research of medical classics. This will not be limited in stroke alone but also will be applied in other diseases. This study will concurrently result in establishing distinctive therapeutic method characteristic of Korea.

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The effects of $\beta$-1,3/1,6-linked glucan in the diet on immune responses of olive flounder, Paralichthys olivaceus by oral admimistration ($\beta$-1,3 / 1,6-linked glucan 첨가사료가 넙치의 비특이적 면역반응에 미치는 영향)

  • Won, Gyeong-Mi;Kim, Su-Mi;Park, Su-Il
    • Journal of fish pathology
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    • v.17 no.1
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    • pp.29-38
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    • 2004
  • The effects of dietary $\beta$-1,3/1,6-linked glucan administration on nonspecific immune responses, hematology and disease resistance against Edwardsiella tarda in olive flounder, Paralichthys olivaceus were evaluated. Fish were fed the experimental diets supplemented with 0 %, 0.01 %, 0.05 %, 0.1 %, and 0.5 % of $\beta$-glucan to a commercial diet for 7 weeks. The test was performed in two ways such as fed on each $\beta$-glucan concentrations daily and every other week alternately. The body weight gain from the fish fed on daily the 0.05 % supplemented diet and fed on alternately the 0.1 % supplemented diet of $\beta$-glucan were significantly higher than the control. Both lysozyme activity and intracellular superoxide anion production of kidney phagocytes were higher in the all experimental groups than in the control. But there was no large difference in hematology among each group. The relative percent survival rate (RPS) after an artificial challenge with $4{\times}10^6$ cells of E. tarda per fish was higher than the control, except for that fed on daily the 0.01 % supplemented diet.

A Study on the Relation between Working Time and Tree Formal Characteristics (임업(林業)에서의 순수작업시간(純粹作業時間)과 임목형상조건(林木形狀條件)과의 관계연구(關係硏究))

  • Kang, Gun-Uh
    • Journal of Korean Society of Forest Science
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    • v.78 no.4
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    • pp.381-395
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    • 1989
  • The main purpose of this research is to provide scientific informations about standard wage and performance tariffs in forest management with special reference to working time for thinning. To identify relationships between net working time and tree characteristics, three geographically different sample plots were established at Yangsan, Bongpyung and Jinan and 460 oaks, 372 Japanese larches, 232 red pine and 240 pitch pine mere selected at each sample plots. The results of statistical analysis using multiple regression are as follows ; 1. Five independent variables of breast height diameter(DBH), mid-diameter(MD) large end diameter(LD), log-length(L), No. of branches(NOB) were stable independent of worker and tree species. 2. Comparing correlation coefficient of five independent variables, the best predictive variables, breast height diameter and No. of branches, were selected. Breast height diameter and No. of branches were identified as the most important independent variables in terms of effect on the dependent variable of the working time. 3. Comparing coefficient of determination (Rp) and residual mean square (MSEp), the best Linear regression equation for each tree species was selected as follower : $WT=a+b1{\times}NOB+b2{\times}DBF$ 4. Proportion of hang-up time to total working time in thinning were 66% in oak stand, 74%, in Japanese larch stand, 55%, in red pine stand and 52% in pitch pine stand, respectively. 5. Based on the best regression equation, a table of working time was made by strata of number of branches and breast height diameter. 6. Total working time using the best regression equation in Table 5 can be predicted in terms of felling time, limbing time, hang-up time, i.e., total working time increases by 11 to 13 seconds with every 1 centimeter increase in breast height diameter from 7 to 16 centimeter.

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A Literature Study on the Korean Acupuncture for Oral, Glottal, Labial and Dental diseases (구설순치(口舌脣齒)질환에 대한 한국 침구서적의 치료법 비교 연구)

  • Han, Chang-Hyun;Ahn, Sang-Young;Kwon, Oh-Min;Park, Sang-Young;Lee, Jeong-Hyeon;Ahn, Sang-Woo
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.23 no.1
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    • pp.182-198
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    • 2010
  • Background : The varieties of manifestations referred to oral, glottal, labial and dental diseases has been long complicated physicians in the efficient diagnosis and treatment of these diseases. Acupuncture has been widely used in Korea throughout the history and provides an efficient method in the treatment of them Objectives : Establish a distinctive and efficient acupuncture method for the treatment of oral, glottal, labial and dental diseases based in literature research Method : We reviewed four Korean medical literature, "Guide to Swollen Sore Treatment", "Treasured Mirror of Eastern Medicine", "Experiential Prescriptions of Acupuncture and Moxibustion", and "Essential Rhymes on Acupuncture and Moxibustion by Master Sa-am", and analyzed the therapeutic characteristics in the treatment of oral, glottal, labial and dental diseases Result : 1. According to "Guide to Swollen Sore Treatment", we could noted frequent application of blood letting methods in the affected area, then rinse ones mouth with salty water and further application of taro plaster. Also found acupuncture methods utilizing heated mole cricket or silkworm in the sublingual region. Regarding herbal method, Realgar was rubbed in the affected area. Mainly used acupuncture points in the treatment of oral, glottal, labial and dental diseases were GV20, GB20, LU5, and auricular anterior hairline 2. In "Treasured Mirror of Eastern Medicine", blood letting method in the sublingual region and burning needle searing method were the most frequently applied in the treatment of oral, glottal, labial and dental diseases. Moxibustion was also applied in the treatment of labial and dental diseases. Particularly, said to apply 3 moxa cones in ear zones of both sides, when no medicine is effective. This demonstrates how emphasized the importance of moxibustion in this kind of disease. Mainly used acupuncture points were GV16, CV24, LI4, EX-HN12, and EX-HN13 3. In "Experiential Prescriptions of Acupuncture and Moxibustion", no other methods beside wrist. Superstitious methods like applying moxibustion on the tooth picture drawn on the roofing tile need further confirmation. Mainly used acupuncture points were LI4, ST36, and HT7. 4. "Essential Rhymes on Acupuncture and Moxibustion by Master Sa-am", identified the cause of diseases according to visceral pattern identification. Stomach and Spleen in charge of vocal, lingual, and labial disease, Kidney for dental disease, and further scrutinizing identification according to Liver, Heart, Stomach, Lung, and Kidney manifestations. Used supplementation and draining needling methods of self meridians and other correlating meridians. Conclusions : After previous study on stroke and eye diseases, we could also find various efficient methods according to oral, glottal, labial and dental diseases, through literature research of korean medical classics. This study will concurrently result in establishing distinctive therapeutic method characteristic of Korea.

Antioxidant Activity and Cytotoxicity against Human Cancer Cells of Glycyrrhiza New Varieties : A Comparison with Glycyrrhiza Official Compendia (감초 신품종과 약전 수재 감초 추출물의 항산화 활성 및 암세포 독성 비교 연구)

  • Kim, Minhee;Kang, Myunghoon;Lee, Jeonghoon;Leem, Kang-Hyun;An, Hyo-Jin;Jin, Jong-Sik;Lee, Jong-Hyun;Chang, Jaeki;Seong, Shin;Kim, Wonnam
    • The Korea Journal of Herbology
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    • v.36 no.3
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    • pp.15-24
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    • 2021
  • Objectives : The Glycyrrhiza new varieties, WONGAM and SINWONGAM, were developed through interspecific cross between Glycyrrhiza glabra and Glycyrrhiza uralensis by the National Institute of Horticultural and Herbal Science, Rural Development Administration in Korea. This in vitro study was undertaken to compare the antioxidant and cytotoxic effects between Glycyrrhiza new varieties (WONGAM and SINWONGAM) and official compendia (Glycyrrhiza glabra and Glycyrrhiza uralensis). Methods : Antioxidant activity was determined by DPPH (1,1-diphenyl-2-picrylhy drazyl), ABTS (2,2-azino-bis (3-rthylbenz-thiazoline-6-sulfonic acid)) diammonium salt, Nitrite radical scavenging assay, and Reducing Power assay. Cytotoxicity was determined by MTT assay and cell morphology was observed by an inverted microscope. Results : The DPPH, ABTS, Nitrite radical scavenging activities and reducing power of Glycyrrhiza glabra, Glycyrrhiza uralensis, WONGAM, and SINWONGAM were evaluated at different concentrations (0, 10, 50, 100, 500, 1000 ㎍/㎖). Glycyrrhiza glabra, Glycyrrhiza uralensis, WONGAM, and SINWONGAM showed similar dose-dependent increase in antioxidant activities. The cytotoxic effects with increasing doses of Glycyrrhiza new varieties and official compendia did not differ in HCT116, HT29, A549, MDA-MB231, PC3, ACHN, and HeLa cells. However, significant difference in cytotoxicity were observed in AGS, MCF7 and Hep3B cells by Glycyrrhiza glabra, Glycyrrhiza uralensis, WONGAM, and SINWONGAM. Conclusions : These results showed that Glycyrrhiza new varieties and official compendia acts as a potent antioxidant. Also, the finding that equivalent cytotoxic potency was observed in a cell dependent manner. Our study suggests that Glycyrrhiza new varieties may offer a wide-variety of health benefits.

Study on the Anti-cancer, Anti-metastasis and Immune response improvement Effects of Aqua-acupuncture with Rubi Fructus infusion solution (항암(抗癌) 및 면역효과(免疫效果)에 복분자약침(覆盆子藥鍼)이 미치는 영향(影響))

  • Lee, Seon-Hee;Lee, Byung-Ryul
    • Journal of Acupuncture Research
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    • v.17 no.1
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    • pp.189-219
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    • 2000
  • To study the effects of anti-cancer, anti-metastasis and immune response improvement effects of aqua-acupuncture with Rubi Fructus infusion solution, we used Rubi Fructus infusion solution(taken by water-alcohol method) put into Chung-wan (CV12) and Chok-Samni(ST36) of BALB/c or C57BL/6 which are corresponding to humanbody. We observed the cytotoxicity, the effect on the expression of MMP-9 gene, the ability to control cancer cell proliferation, change of body weight, surviving number, median surviving time, increase of life span, changes in amount of leukocyte, erythrocyte, platelet, total protein, creatinine, glucose and LDH, weight of spleen, number of pulmonary colony, histological analysis on tissue metastasis of lung and liver, splenic cell proliferation, the expression of cytokine gene, the number of $CD4^+$, $CD8^+$, $CD19^+$ and NK cell, and concluded like this. The results were obtained as follows : 1. Effects of Anti-cancer 1) The cytotoxicity about B16-F10 cell line of $2^0$, $2^{-1}$, $2^{-2}$, $2^{-3}$, $2^{-5}$, $2^{-6}$, $2^{-7}$, $2^{-8}$ diluent groups in Rubi Fructus infusion solution treatment was inhibited significantly, compared with control group. 2) The cytotoxicity about HT1080 cell line of $2^0{\sim}2^{-8}$ diluent groups in Rubi Fructus infusion solution treatment was inhibited significantly, compared with control group. 3) The effect on expression of MMP-9 gene was inhibited significantly in all the sample groups, compared with control group. 4) The effect on the control-ability on the cancer cell proliferation showed cytotoxicity significantly in $2^0$, $2^{-1}$, $2^{-2}$, $2^{-3}$, $2^{-4}$, $2^{-5}$, $2^{-6}$, $2^{-7}$, diluent groups. 2. Effects of Anti-metastasis 1) S-180 cancer cell line transplants in BALB/c mice were inhibited significantly in weight increase in all the sample groups, compared with control group. The surviving number increased in almost sample groups, except one group put into Chok-Samni(ST36) with 20% Rubi Fructus infusion solution treatment group that showed same number of the control group. 2) S-180 cancer cell line transplants in BALB/c mice showed high MST significantly in almost sample groups, compared with control group. But one group put into Chok-Samni(ST36) with 20% Rubi Fructus infusion solution showed low MST than control group. 3) The group injected in vein with B16-F10 cancer cell line in C57BL/6 mice showed increased ILS than control group significantly in anti-metastasis test. 3. Effects of Immune response improvement 1) The group injected in vein with B16-F10 cancer cell line in C57BL/6 mice were increased significantly in the number of leukocyte and glucose, and decreased significantly in the amount of platelet and LDH, compared with control group. However, there's no significant increase or decrease in number of erythrocyte, total protein and creatinine. 2) We couldn't find any significant relation in spleen weight of the sample group. 3) In pulmonary colony, sample group was decreased significantly, compared with control group. 4) Histological analysis of sample group inhivited compared with that of control group in both of lung and liver. 5) In immune system, all the sample groups showed having more relevancy to the effect on splenic cell proliferation than normal group. 6) Cytokine gene increased in almost sample groups, except one group treated with $50{\mu}g/m{\ell}$ Rubi Fructus infusion solution on IL-12. 7) In flow cytometry there's no significant relation in number of $CD8^+$ cell, however, the number of $CD4^+$, $CD19^+$ cell and NK cell in sample group had more relation than in control group. Above the results showed that aqua-acupuncture of Rubi Fructus solution has effects of anti-cancer, and-metastasis and immune response improvement.

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Improvement of Reproductive Disturbances by In Vitro Fertilization and Spermatozoa Cryopreservation in a Mouse Strain Showing Behavior Abnormality Derived from Korean Wild Mouse (Mus musculus molossinus) (한국야생유래 행동이상 Mouse 에 있어서 체외수정에 의한 번식장애 개선과 정자의 동결보존)

  • 남윤이;김상근;김명수;이철호;최양규;현병화
    • Korean Journal of Animal Reproduction
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    • v.23 no.3
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    • pp.247-256
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    • 1999
  • The present study was performed to improve the reproductive disturbance as well as the elimination of microbiological contamination for animals bred under conventional conditions followed by in vitro fertilization and embryo transfer techniques including embryo and sperm freezing, using a mouse strain(M. m. molossinus-tt@Kist) showing the abnormal behavior disorder derived from Korean wild mice (Mus musculus molossinus). Moreover, hematological and serum biochemical analyses were also carried out to obtain the basic data of this mouse strain The results are summarized as follows: 1. In comparison with hematological data, the numbers of RBC and platelet of this mouse strain were appeared as the higher value those that of the same aged inbred strains such as BALB/c, DBA/2, C57BL/6 and C3H /Hen. However, no differences were found in values of WBC, Hb and Ht. Moreover, total cholesterol of this strain showed a low value but triglyceride, total protein and albumin values were similar as in inbred strains. 2. The average numbers of superovulated oocytes treated with 2.5/2.5 IU and 5.0/5.0 IU of PMSG/hCG were 11.6 and 12.7, respectively. The fertilization rates of 2.5/2.5 IU PMSG /hCG treatment(87.9%) was higher than 5.0/5.0 IU treatment(52.0%) (p<0.05) and the developmental rate of 2 cell stage embryos were 외 so appeared as higher value 99.0% and 90.6%, respectively. 3. The rates of in vitro fertilization treated with frozen sperm(24.8%) was significantly lower than of that fresh sperm(87.9%), (p<0.05). 4. The five, six and ten heads of offspring were obtained from frozen-thawed 2 cell embryos by in vitro fertilized, 2 cell embryos from in vitro fertilized by frozen-thawed spermatozoa. and 2 cell embryos by in vitro fertilization, respectively. These offspring developed the expected disease about 2 weeks after birth, which was confirmed that the disease character of this mutant mouse strain was reliably reproduced. 5. MHV(Mouse hepatitis virus) and Staphylococcus aureus were successfully eliminated from conventional animals by in vitro fertilization-embryo transfer and the use of SPF recipient animals.

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Short Tenn Reactions to Acupuncture Treatment and Adverse Events Following Acupuncture in Korea a Cross-sectional Survey of Patient Reports (침치료 직 후 자가 설문지를 이용한 침반응(針感)과 부작용에 대한 단면적 연구)

  • Park, Seong-Uk;Jung, Woo-Sang;Moon, Sang-Kwan;Ko, Chang-Nam;Cho, Ki-Ho;Kim, Young-Suk;Bae, Hyung-Sup;Park, Jung-Mi
    • The Journal of Korean Medicine
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    • v.28 no.2 s.70
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    • pp.66-79
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    • 2007
  • Objectives : To explore the type and frequency of short term reactions, de Qi associated with acupuncture treatment and to determine the incidence of adverse events following acupuncture in Korea. Subjects and methods : This study is a retrospective and cross-sectional survey of patient reports. 1095 subjects, 585 of out-patients of the Oriental Medicine of Stroke & Neurological Disorders Center, East-West NEO Medical Center of Kyunghee University and 510 of out-patients of the Department of Cardiovascular & Neurologic Diseases (Stoke Center), Hospital of Oriental Medicine, Kyunghee Medical Center, from June through November of 2006, who had acupuncture, gave informed consent and completed one survey form. On this form, patients were asked to report short term acupuncture reactions, de Qi, patient satisfaction measurement (using VAS), and adverse events relating to acupuncture treatment. The acupuncturists of this study are Korean Medicine Doctors (KMD) who had worked as practitioners for 3-30 years or more. Results : The average age of the 1095 subjects was 58 years old. Positive short term acupuncture reactions after treatment were reported by 878 (80.2%), negative short term acupuncture reactions by 75 (6.8%) and no reactions were reported by 142 (13.0%). The most common positive short term acupuncture reactions were feeling 'relaxed', 472 (43.1%), followed by feeling 'less pain' 90 (8.2%), 'energized' 16 ( 1.5%), 'tingling' 16 (1.5%), 'heat feeling or Cold feeling' 10 (0.9%), and others 274 (25.0%), respectively. Negative short term acupuncture reactions were feeling 'pain' 37 (3.4%), tiredness 24 (2.2%), dizziness 9 (0.8%), and others 5 (0.2%), respectively. Traditionally described needling sensations of de Qi refer to a patient's response to distention, pulling, soreness, heaviness, numbness. 39.7% of subjects reported de Qi during needling, experiencing 'distention' 333 (30.4%), 'soreness' 52 (4.7%), 'pulling' 22 (2.0%), 'heaviness' 18 (1.6%), and 'numbness' 10 (0.9%) respectively. Positive short term acupuncture reactions and de Qi rate were the highest in the less than 40 years group (83/96 86.5%, 50/96 52.1%). No acupuncture reactions were highly seen in the over 70 years old group (31/187, 16.6%). Patient satisfaction level using VAS was a comparatively high $72.9{\pm}19.9$. Adverse events were only bleeding in 92 (8.4%) of the total subjects. High sensitive acupoints were 95 points as GV26 (54 times), LI4 (54 times), ST36 (53 times), GB20 (37 times), HT8(34 times), LV3 (29 times), SI3 (29 times), and LI11 (27 times) in order. Main impressions were stroke patients 430 (16.9%), headache 185 (16.9%), hypertension 97 (8.9%), and dizziness 85 (7.8%). Conclusions : Although 8 different Korean Medicine Doctors participated in this research, we obtained similar results from each. There were no significantly different results between the two hospitals. Short term acupuncture reactions and de Qi were most related to age. Except for bleeding there were no adverse events relating to acupuncture treatment in this study. We consider acupuncture treatment as very safe depending on practitioners. Positive short term acupuncture reactions after treatment were 12 times higher than negative short term acupuncture reactions. Subjects were comparatively satisfied with acupuncture treatment.

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Antiemetic Effect of Dolasetron Mesylate in the Prevention of Acute and Delayed Nausea and Vomiting due to Moderately Emetogenic Chemotherapy (악성종양환자에서 중등도 이상의 오심, 구토를 유발하는 항암화학요법 시급성 및 지연성 오심, 구토의 예방에 대한 Dolasetron의 효과)

  • Kim, D.S.;Sung, H.Y.;Choi, K.M.;Paik, J.Y.;Roh, S.Y.;Moon, H.;Kim, C.C.;Hong, Y.S.
    • Journal of Hospice and Palliative Care
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    • v.7 no.2
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    • pp.248-257
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    • 2004
  • Purpose: To evaluate the efficacy of dolasetron mesylate in controlling nausea and vomiting in the first 24 hours and to extend these comparisons over the next 4 days in patients receiving moderately emetogenic chemotherapy. Methods: This was a single center, open-labeled study with single arm. Dolasetron (1.8 mg/kg) was given intravenously (I.V.) prechemotherapy with 10 mg of dexamethasone IV, followed 24 hours later by oral dolasetron (200 mg once daily) for the subsequent 4 days. The frequency of vomiting, severity of nausea and the presence of rescue antiemetics were assessed daily. Results: Of 30 patients enrolled, 28 were eligible and evaluable for the efficacy. Four out of 28 patients had complete control of nausea and vomiting without any rescue antiemetics through 5 days. The complete control got better as time went by with the rates of 17.9/46.4/42.9/53.6/60.7% on days 1 to 5. Vomiting was better controlled than nausea in both cisplatin-containing and non-containing chemotherapy. The adverse events were mild to moderate degrees of headache, diarrhea and fever, but were recovered spontaneously. Conclusion: Dolasetron was effective and safe for the control of nausea and vomiting in the patients with moderately emetogenic chemotherapeutic agents.

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