• Title/Summary/Keyword: (-)-ephedrine

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Evaluation on the Abuse Liability of Ephedrine Using Rats (흰쥐를 이용한 에페드린의 약물남용가능성 평가)

  • 류승렬;김혜진;홍진태;이종권;이선희;이병무;김부영
    • YAKHAK HOEJI
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    • v.43 no.5
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    • pp.682-688
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    • 1999
  • Abuse liability of ephedrine was investigated by measurement of locomotor activity and self-administration in Sprague-Dawley rats. Locomotor activity was determined in rats treated with 3, 10 and 30 mg/kg ephedrine for 14 days. Self-administration by ephedrine (0.23, 1 and 2.3 mg/kg) was examined in food-trained rats. We also examined effect of dopamine receptor antagonist (spiperone, $30{\;}\mu\textrm{g}/kg$) on the ephedrine-induced response of self-administration. Body weight was not statistically difference between control and ephedrine treatment group, but locomotor activity was dose-dependently increased. Self-administration for ephedrine was decreased in the early response (day 1 and 2) but the response was increased by higher dose of ephedrine. Self-administration was decreased by dopamine receptor antagonist (spiperone). These data showed that ephedrine increased locomotor activity and induced response of self-administration, and the effects of ephedrine were partially related to the dopaminergic system, which suggest the ephedrine may have abuse liability.

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Review on the Efficacy and Safety of Mahuang and Ephedrine in the Treatment of Obesity -Focused on RCT- (비만 치료에서 마황 및 에페드린의 유효성, 안전성에 대한 고찰 - RCT 연구를 중심으로 -)

  • Jo, Ga-Won;Ok, Ji-Myung;Kim, Seo-Young;Lim, Young-Woo
    • The Journal of Korean Medicine
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    • v.38 no.3
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    • pp.170-184
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    • 2017
  • Objectives: The objective of this study was to summarize randomized clinical trials (RCTs) that have assessed efficacy and safety of mahuang and ephedrine on treatment of obesity and to propose better process of study. Methods: NLM Medline (pubmed), the Cochrane library, Scopus, Science Direct, RISS, KISS were systemically searched for clinical trials investigating the efficacy, safety of mahuang and ephedrine on treatment of obesity from 2000 to 2017. Results: 16 RCTs met all the inclusion criteria. In most reports, mahuang and ephedrine significantly reduced body weight, body fat mass. There were no serious adverse events associated with mahuang and ephedrine in all studies. Conclusions: In appropriate dose of mahuang and ephedrine for healthy adult was safe, and weight loss effect of mahuang and ephedrine was better than control group. Improved clinical practice guidelines should be developed for safe use of mahuang and ephedrine.

Effect of Ephedrine on the Levels of Biogenic Amines and Their Metabolites in Rat Brain (Ephedrine이 뇌내 Biogenic Amine 함량에 미치는 영향)

  • Lee, Kyung-Eun
    • The Korean Journal of Pharmacology
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    • v.31 no.2
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    • pp.153-164
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    • 1995
  • Sympathomimetic amines, especially ephedrine, are a major ingredient in proprietary medications for symptomatic treatment of upper respiratory infections. Their frequent uses can lead to occasional instances of abuse and habituation. The clinical symptoms of ephedrine abuse are similar to that of amphetamine psychosis and resemble closely that of schizophrenia. Because both amphetamine psychosis and schizophrenia are thought to be mediated primarily through the action on catecholamines, ephedrine-induced changes of the biogenic amines can be suspected. However, there were few studies about the central effects of ephedrine because of the milder central action than peripheral. Therefore, the present investigation was undertaken to elucidate the relations between the effects of single or repeated administration of ephedrine on the regional levels of biogenic amines in rat brain and ephedrine-induced CNS stimulation. The male Sprague-Dawley rats weighing $100{\sim}200\;g$ were used. After single or repeated administrations of ephedrine, blocks of tissue were obtained from frontal cortex, corpus striatum, hippocampus, thalamus, hypothalamus, substantia nigra and cerebellum. The concentration of biogenic amines(norepinephrine, epinephrine, dopamine, 5-hydroxytryptamine(5-HT)) and their metabolites (3,4-dihydroxyphenylacetic acid (DOPAC), homovanillic acid(HVA), 5-hydroxyindoleacetic acid(5-HIAA)) were measured by means of high performance liquid chromatography-electrochemical detector(HPLC-ECD). The results obtained were as follows: 1) In the normal rat, the concentration of norepinephrine was the highest in hypothalamus. Dopamine, DOPAC and HVA were highest in corpus striatum, and 5-HT and 5-HIAA were highest in substantia nigra. Epinephrine was not detectable in any part of the brain tissue. 2) In a single administration of ephedrine, the concentration of DOPAC was decreased in corpus striatum. However, the other biogenic amines and their metabolites were not changed. 3) In repeated administration of ephedrine, the concentration of norepinephrine was decreased in all brain region checked. Dopamine was decreased in corpus striatum and substantia nigra and, increased in hypothalamus, and HVA was decreased in corpus striatum. 5-HT was decreased in all brain region except cerebellum and, 5-HIAA was decreased only in frontal cortex. The ratio of 5-HIAA/5-HT was increased in corpus striatum, thalamus, hypothalamus and substantia nigra. These data indicated that, although a single administration of ephedrine did not change the central neurotransmitters, repeated administration of ephedrine caused the decreases of norepinephrine and 5-HT in the most regions of brain, which may be responsible for the emergence of abnormal behavioral effect after ephedrine abuse.

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Prophylactic Intravenous Ephedrine Infusion during Spinal Anesthesia for Cesarean Section (제왕절개술을 위한 척추 마취시 Ephedrine의 예방적 정맥적주에 관한 연구)

  • Koo, Bon-Up
    • Journal of Yeungnam Medical Science
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    • v.8 no.1
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    • pp.72-78
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    • 1991
  • Ephedrine sulfate was administrated 30 healthy parturients undergoing elective repeat cesarean section under spinal anesthesia. Fifteen patients received ephedrine infusion (0.01% solution, beginning with approximately 5 mg/min) immediately after induction of spinal anesthesia to maintain maternal systolic blood pressure between 90% and 100% of the baseline systolic blood pressure (mean dose of ephedrine 31.6mg). Fifteen patients (contral group) received 20mg of ephedrine as an intravenous bolus, and additional 10mg increments, if neccessary, when systolic blood pressure decreased to 80% of the baseline systolic blood pressure (mean dose of ephedrine 26.8 mg). Nausea and/or vomiting occurred in seven women in the control group and one patient in the infusion group (p<0.001). Apgar scores, fetal blood gas tension, and time for onset of respiration was comparable in the two groups. The results suggest that prophylactic ephedrine infusion is safe and desirable in healthy parturients undergoing cesarean section under spinal anesthesia.

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Spectrophotometric Determination of Ephedrine Alkaloids by Charge-Transfer Complexation (전하이동 착물형성에 의한 Ephedrine Alkaloids의 분석화학적 연구)

  • 옥치완;백채선
    • YAKHAK HOEJI
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    • v.31 no.5
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    • pp.330-337
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    • 1987
  • The weak UV absorbing ephedrine alkaloids such as ephedrine, pseudoephedrine, methylephedrine and norephedrine could be analyzed by charge-transfer spectrophotometric method. The results obtained are summarized as follows: (1) It was possible to determine a weak UV absorbing ephedrine alkaloids using the intense charge-transfer UV bands in chloroform. (2) This method was suitable for the spectrophotometric determination of ephedrine alkaloids in mixed pharmaceutical preparation. (3) Linear relationship was found between absorbance and concentration in the range of 1.0$\times$$10^{-5}M$~5$\times$$10^{-5}M$ of ephedrine ($\varepsilon$= 2.72$\times$$10^{4}LM^{-1}cm^{-1}$ and pseudoephedrine ($\varepsilon$=2.84$\times$$10^{4]LM^{-1}cm^{-1}$), 1.0$\times$$10^{-5}M$~5$\times$$10^{-5}$M of methylephdrine ($\varepsilon$=1.68$\times$$10^{4}LM^{-1}cm^{-1}$) and 1/3$\times$$10^{-4}M$~4/3$\times$$10^{-4}M$ of norephedrine ($\varepsilon$=0.74$\times$$10^{4}LM^{-1}cm^{-1}$. (4) CT- complex of ephedrine, pseudoephedrine and methylephedrine has absorption maxima at 293nm and norephedrine have absorption maximum at 253nm. (5) CT-complexes were formed in a 1:1 ratio between ephedrine alkaloids and iodine in chloroform. (6) By UV, IR, and $^1H$-NMR spectra, it could be inferred that CT-complexes were formed by interaction between the basic nitrogen of ephedrine alkaloids as electron (n) donor and iodine as electron ($\sigma$) acceptor.

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Study on Isolative Determination Methylephedrine Hydrochloride and Ephedrine Hydrochloride in the Mixed Preparation (혼합제제중 Methylephedrine Hydrochloride와 Ephedrine Hydrochloride의 분리정량에 관한 연구)

  • Ko, In-Suk
    • Korean Journal of Pharmacognosy
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    • v.1 no.3
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    • pp.93-99
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    • 1970
  • There have been reported by several workers for the isolation and determination of the amine derivatives as Metbylephedrine Hydrochloride and Ephedrine Hydrochloride adopting neutralization method, steam distillation method, non-aqous titration method, ion-exchange resin method, titration method after acetylation, colorimetric method, gravimetric method, iodine titration method and gas chromatography. Those methods mentioned in above, can be practically applied for the sample which is not mixed one mith the other amine compounds. Presently, it has not shown on the isolative determination of the mixed sample of amine derivatives. In this paper, it is discussed on the isolative determination of Methylephedrine Hydrochloride as the tertiary amine compound and Ephedrine Hydrochloride as the secondary amine compound. According to the results of the experiment, it could be summarized as follows: 1. There is no time-variation on the color reaction of Methylephedrine Hydrochloride and Ephedrine Hydrochloride with the color reagent, bromcresolgreen. And Methylephedrine Hydrochloride and Ephedrine Hydrochloride, respectively, can be determined spectrophotometrically by means oft his color reaction. 2. For the isolation of Methylephedrine Hydrochloride and Ephedrine Hydrochloride from the mixed sample, Methylephedrine Hydrochloride can be eluted by chloroform, while Ephedrine Hydrochloride by the mixed solvent of chloroform and ethylalcohol (2:1), from the celite column adsorbed at pH6.4 followed by extraction with ether undersodium hydroxide alkali re action. 3. When the sample is mixed with quinine hydrochloride, dihydrocodeine bitartate, and noscapine, these mixed compounds can be eliminated by means of stram distillation. 4. When the sample is mixed with chlorpheniramine maleate, dextromethorphan hydrobromide and diphenhydramine hydrochloride, the mixed compounds can be eliminated by means of steam distillation and celite adsorption column chromatography, In conclusion, the isolative determination method for Methylephedrine Hydrochloride and Ephedrine Hydrochloride studied in this paper, indicates with the excellent reproducibility and accuracy.

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Simultaneous Determination of (+)-Pseudoephedrine and (-)-Ephedrine in Ephedra intermedia by HPLC-UV (HPLC-UV를 이용한 중마황의 (+)-Pseudoephedrine과 (-)-Ephedrine의 동시분석법 개발)

  • Jeong, Birang;Yoon, Yoosik;Shin, Soon Shik;Kwon, Yong Soo;Yang, Heejung
    • Korean Journal of Pharmacognosy
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    • v.48 no.1
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    • pp.93-96
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    • 2017
  • Ephedra alkaloids, (-)-ephedrine, (+)-pseudoephedrine, (-)-N-methylephedrine, (+)-N-methylpseudoephedrine, (-)-norephedrine and (+)-norpseudoephedrine, from ephedra herb are sympathomimetic agonists causing an increase of metabolism, blood pressure and perspiration. In this study, we developed the validation method of (+)-pseudoephedrine and (-)-ephedrine, two major ephedra alkaloids in Ephedra spp., by high-performance liquid chromatography-ultraviolet spectrometer (HPLC-UV). HPLC analysis was performed using a HECTOR-M C18 column operating at $35^{\circ}C$, and UV detection at 215nm. The mobile phase used a gradient flow with 25 mM SDS in water (A) and acetonitrile (B).

Stimultaneous Determination of Ephedrine Alkaloids in Ephedra sinica and Wolbigachul-tang by High Performance Liquid Chromatography (고성능 액체 크로마토그래피를 이용한 마황 및 월비가출탕 전탕액에서 에페드린류의 동시분석)

  • Song, Miyoung;Kim, Jung-Ok;Leem, HyunHee;Kim, Hojun
    • Journal of Korean Medicine for Obesity Research
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    • v.20 no.2
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    • pp.97-108
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    • 2020
  • Objectives: Ephedra sinica and Wolbigachul-tang which contains Ephedra sinica are used to treat obesity in Korean medicine. The aim of this study was to analyze the quantities of ephedrine alkaloids by high-performance liquid chromatography. Methods: The analysis was performed using a YMC-Triat C18 column with operating at 25℃, and UV detection at 210 nm. The mobile phase used a gradient flow with 0.1% H3PO4 in water and acetonitrile. Specificity, linearity, precision, accuracy, limit of detection, and limit of quantification were measured for validation anaylsis. This method was applied to analyze the quantities of ephedrine alkaloids in Ephedra sinica and Wolbigachul-tang. Results: The concentration per Ephedra sinica (gram) of ephedrine and pseudoephedrine in Ephedra sinica decoction are 4.74±0.22 mg and 2.19±0.10 mg, respectively and in Wolbigachul-tang decoction are 6.39±0.34 mg and 2.97±0.21 mg, respectively. The retention time of ephedrine was 23.6 min and that of pseudoephedrine was 25.8 min, and norephedrine and methylephedrine were not detected. Conclusions: In conclusion, analyzed the concentration of ephedrine alkaloids in Ephedra sinica and Wolbigachul-tang by the developed validation method.

A study on proper dosage of Ma-huang(麻黃) (마황(麻黃)의 적정 용량에 대한 고찰(考察))

  • Ryu, Hee-chang;Shin, Jeong-gyu
    • 대한상한금궤의학회지
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    • v.5 no.1
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    • pp.101-111
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    • 2013
  • Objective : The purpose of this study is to find out the proper dosage of Ma-huang for clinical use of Shanghanlun(傷寒論) Methods : To achive the purpose of this study, web-databases(pubmed, naver, google) were searched with the keywords including 'dose of Ma-huang Ephedra Ephedrine','dosage of Ma-huang Ephedra Ephedrine', and 'water extract of Ma-huang Ephedra'. The searched 30 papers and articles were reviewed. Results & Conclusions : 1. Proper dosage of Ma-huang 1) Adult: up to 9-12g/day 2) Adolescent: up to 6g/day 3) Hypertension disorder patient: up to 6g/day 4) lactating women: up to 6g/day 5) child: <2 years 0.7-2.5g/day, $${\geq_-}2$$ years 2.6-6g/day (Different from body weight) Although administration of Ma-huang to hypertension disorder patient, lactating women, child is safe on the paper, It is not recommended to these people because Ma-huang is one of toxic herbs. 2. Dosage form of Ma-huang There's no safety paper about pill or powdered Ma-huang(麻黃). There's not pill or powdered prescription of Ma-hunag in Shanghanlun(傷寒論), either. So it is recommended to administrate water exetract of Ma-huang.

Clinical Application of Ma Huang in the Obesity Treatment (비만처방에서 마황의 임상활용에 대한 고찰;용량, 효과, 부작용 등의 측면에서)

  • Song, Yun-Kyung;Lim, Hyung-Ho
    • Journal of Korean Medicine for Obesity Research
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    • v.7 no.1
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    • pp.1-7
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    • 2007
  • Background : Use of Ma Huang is controversial. Multiple reports of adverse effects led the U.S. Federal Drug Administration (FDA) to announce about prohibiting dietary supplements containing ephedrine alkaloids/Ma Huang. Objective : The objective of the study was to review the evidence from literature and rigorous clinical trials on the dosage, effectiveness, and adverse effects. Methods : Literature searches were conducted in U.S. FDA database after 2003 and digital Uibujeonok(醫部全錄). Hand searches of medical journal and bibliographies of identified articles were conducted. Results : Ma Huang has been used in Korean Oriental Medicine to treatment asthma and other ailments. Recently, Ephedrine/Ma Huang are used for weight loss or to enhance athletic performance in Europe and America, Korea. Ephedrine/Ma Huang are associated with increased risk of psychiatric, autonomic, or gastrointestinal symptoms, and heart palpitations. In addition to that, a risk of serious adverse events, including heart attack, stroke, epilepsy and psychiatric problem are also have been reported. Therefore, max dose of total alkaloids of ephedrine is studied in need of a specialist's part. Conclusion : In most reports, Ma Huang effectively promoted short-term weight loss and enhancement of athletic performance, But, safety with long-term use requires further investigation.

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