• Archives of Pharmacal Research
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• 제27권9호
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• pp.901-905
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• 2004

A rapid, sensitive and selective hydrophilic interaction liquid chromatography-tandem mass spectrometric(HILIC-MS/MS) method for the determination of tiapride in human plasma was developed. Tiapride and internal standard, metoclopramide were extracted from human plasma with dichloromethane at basic pH and analyzed on an Atlantis HILIC silica column with the mobile phase of acetonitrile-ammonium formate (190 mM, pH 3.0) (94：6, v/v). The ana-Iytes were detected using an electrospray ionization tandem mass spectrometry in the multi-ple-reaction-monitoring mode. The standard curve was linear (r＝0.999) over the concentration range of 1.00-200 ng/mL. The coefficient of variation and relative error for intra- and inter-assay at three QC levels were 6.4∼8.8％ and -2.0∼3.6％, respectively. The recoveries of tiapride ranged from 96.3 to 97.4％, with that of metoclopramide (internal standard) being 94.2％. The lower limit of quantification for tiapride was 1.00 ng/mL using 1 00 $\mu$L of plasma sample.

• Archives of Pharmacal Research
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• 제25권5호
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• pp.709-717
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• 2002

Hypoxemia is known to induce various physiological changes which can result in alteration in drug pharmacokinetics. To examine the effect of acute moderate hypoxemia on metoclopramide (MCP) pharmacokinetics, a continuous 14-hour infusion of MCP during a normoxemic, hypoxemic and subsequent normoxemic period was conducted in eight adult sheep. Arterial blood and urine samples were collected to examine the effects on the pharmacokinetics of MCP and its deethylated metabolites. MCP and its mono- and di-deethylated metabolites were quantitated using a GC/MS method. Steady-state concentrations of MCP were achieved in each of the three periods. During hypoxemia, MCP plasma steady-state concentration increased significantly from 50.72$\pm$1.06 to 63.62$\pm$1.79 ng/mL, and later decreased to 55.83$\pm$1.15 ng/mL during the post-hypoxemic recovery period. Total body clearance ($CL_{TB}$) of MCP was significantly decreased from 274.2$\pm$48.0 L/h to 205.40$\pm$28.2 L/h during hypoxemia, and later restored to 245.8$\pm$44.2 L/h during the post-hypoxemic period. Plasma mono-deethylated MCP concentration (32.78$\pm$1.73 ng/mL) also increased, compared to the control group (21.20$\\pm$1.39 ng/mL), during hypoxemia and subsequent normoxemic period. Renal excretion of MCP and its metabolites was also decreased during hypoxemia, while urine flow was increased with a concomitant decrease in urine osmolality. Thus, the results indicate that acute moderate hypoxemia affects MCP pharmacokinetics.

• 한국임상수의학회지
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• 제17권2호
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• pp.403-410
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• 2000

The Ultrasonographic method alas been widely applied to evaluating gastric motility with safety and reproducibility ill human medicine but few reference to its use in veterinary medicine is appeared. Therefore, in this study, the gastric motility was evaluated with ultrasonography by the cri-terion of mean cycle lime, short and lony axis and the area of pyloric antrum in dogs, fed with liquid of semisolid meals. Furthermore, the animals were evaluated for the effect of metoclopramide on the motility of pyloric antrum. Healthy 5 mongrel male dogs were fed with either 400 ml of milk a: a liquid meal or a mixed meal of 200 ml of milk with two pieces of bread as a semisolid meal. Mean cycle time of pyloric antrum of dogs was significantly delayed after feeding either of liquid and , semi- solid meals(P<0.05), alls it was returned to the fasting state at 60 min. after feeding of liquid meal and 160 min. after feeding of semisolid meal. Mean area of pyloric antrum of dogs was gradually decreased and was returned to the lasting state at 80 min. in doss fed liquid meal. but 1600 min. in dog\ulcorner fed semisolid meal. The administration of metoclopramide (1.0 mg/kg of of B.W.) accelerated the mean cycle time of pyloric antrum from 20 mill. to 60 min. after feeding of liquid meal and from 40 min. to 120 min. after feeding of semisolid meal. From this study, the ultrasonography was confirmed as a valuable diagnostic method leer evaluating the gastric motility and gastric area in dogs. It is non-invasive, safe and reproducible, and provides a method for the study of the effect of drugs and diseases states on gastric motility.

• 대한약리학회지
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• 제30권1호
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• pp.87-100
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• 1994

도파민 함유세포가 교감신경절에 존재하는 것으로 알려져 있으나, 말초에서 신경전달 물질로써 그의 역할과 작용기전에 대해서 아직까지 알려진 바가 많지 않다. 따라서 본 연구에서는 도파민 $D_2$-수용체의 선택적인 효능약으로 알려진 apomorphine이 흰쥐 적출 관류 부신에서 카테콜아민(CA)분비작용에 미치는 영향을 연구코자 시도하여 다음과 같은 연구결과를 얻었다. $10{\um}M\;Apomorphine$의 비교적 낮은 농도를 부신정맥내에 20분간 관류 하였을때 5.32mM ACh, 56mM KCl, $100{\mu}M$ DMPP 및 $100{\mu}M$ McN-A-343 등의 투여에 의한 CA 분비작용이 의의 있게 감소되었다. Apomorphine 농도를 $30{\mu}M$로 증가시켜 관류하였을때 상기약물에 의한 CA 분비작용은 더욱 억제되었으며 또한 Bay-K-8644에 의한 $100{\mu}M$의 고농도로 전처치 하였을때, ACh, excess $K^+$, DMPP 및 McN-A-343에 의한 CA분비작용은 현저히 차단되었다. 도파민 $D_2$-수용체 차단제인 metoclopramide $(30{\mu}M)$으로 20분간 관류 하였을때 ACh, DMPP 및 McN-A-343에 의한 CA 분비작용은 유의하게 억제된 효과를 나타내었으나 $excess\;{K^+}$에 의한 CA분비작용은 별다른 영향을 받지 않았다. 그러나 metoclopramide $(30{\mu}M)$ 존재하에서 $30{\mu}M$ apomorphine으로 20분간 전처치 하였을때 $excess{K^+}$ 뿐만 아니라 DMPP의 CA 분비작용은 별다른 변화를 받지 않았다. 이상과 같은 실험 연구결과를 종합하여 보면, apomorphine은 cholinergic receptor stimulation과 membrane depolarization에 의한 CA 분비작용을 용량의존적으로 억제하여, 이러한 작용은 억제성 도파민 수용체를 활성화 시킴으로써 흰쥐 부신 수질의 chromaffin cell 내로 칼슘의 유입을 억제하여 나타나는 것으로 사료된다.

• 약학회지
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• 제28권4호
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• pp.237-241
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• 1984

The effect of lofexidine, clonidine, and other drugs on castor oilinduced diarrhea in rats was investigated. Castor oil was administered orally and drugs were administered intraperitoneally. The results were as follows. 1. Lofexidine(0.1-43{\mu}mol$/kg) blocked dose dependently caster oil-induced diarrhea like clonidine, but its potency was weaker than that of clonidine, 1. Yohimbine (1-10{\mu}mol/kg$) antagonized the antidiarrheal action of lofexidine and clonidine. 3. Prazosin (3-30{\mu}mol/kg$) did not antagonize the antidiarrheal action of lofexidine and clonidine. 4. Metoclopramide, bromocriptine mesylate, and nadolol did not affect antidiarrheal action of lofexidine significantly. 5. Loperamid prolonged the antidiarrheal action of lofexidine.

• Journal of Dental Anesthesia and Pain Medicine
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• 제21권5호
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• pp.413-429
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• 2021

Background: Migraine headaches are the second leading cause of disability worldwide and are responsible for significant morbidity, reduction in the quality of life, and loss of productivity on a global scale. The purpose of this systematic review and meta-analysis was to evaluate the efficacy of ketamine on migraines and other primary headache disorders compared to placebo and other active interventions, such as midazolam, metoclopramide/diphenhydramine, and prochlorperazine/diphenhydramine. Methods: An electronic search of databases published up to February 2021, including Medline via PubMed, EMBASE, Web of Science, and Cochrane Library, a hand search of the bibliographies of the included studies, as well as literature and systematic reviews found through the search was conducted to identify randomized controlled trials (RCTs) investigating ketamine in the treatment of migraine/headache disorders compared to the placebo. The authors assessed the risk of bias according to the Cochrane Handbook guidelines. Results: The initial search strategy yielded 398 unduplicated references, which were independently assessed by three review authors. After evaluation, this number was reduced to five RCTs (two unclear risk of bias and three high risk of bias). The total number of patients in all the studies was 193. Due to the high risk of bias, small sample size, heterogeneity of the outcomes reported, and heterogeneity of the comparison groups, the quality of the evidence was very low. One RCT reported that intranasal ketamine was superior to intranasal midazolam in improving the aura attack severity, but not duration, while another reported that intranasal ketamine was not superior to metoclopramide and diphenhydramine in reducing the headache severity. In one trial, subcutaneous ketamine was superior to saline in migraine severity reduction; however, intravenous (I.V.) ketamine was inferior to I.V. prochlorperazine and diphenhydramine in another study. Conclusion: Further double-blind controlled studies are needed to assess the efficacy of ketamine in treating acute and chronic refractory migraines and other primary headaches using intranasal and subcutaneous routes. These studies should include a long-term follow-up and different ketamine dosages in diagnosed patients following international standards for diagnosing headache/migraine.

• Natural Product Sciences
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• 제12권1호
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• pp.55-61
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• 2006

A description of simple, isocratic and precise reversed phase HPLC methods is given for simultaneous quantification of pholcodine and ephedrine hydrochloride together with either carbinoxamine maleate or terfenadine in antitussive-antihistaminic oral pharmaceutical formulations. Separations were carried out on X-Terra and symmetry shield C18 column $(250\;{\times}\;4.6\;mm,\;5\;{\mu}m)$. The used isocratic elution systems were either $0.02\;M\;KH_2PO_4-acetonitrile$ in the ratio of 75 : 25 and pH adjusted to 7.70 with orthophosphoric acid or sodium hydroxide, for syrup (method A), or 0.02 octanesulphonic acid sodium salt solution-acetonitrile-acetic acid in the ratio of 75 : 25 : 0.5 for suspension (method B). The elution of both mixtures was achieved with a flow rate of 1 ml/min. Detection was carried out by UV absorbance at wavelengths of 220 and 250 nm for syrup and suspension, respectively. The quantification of the components in synthetic mixtures and actual syrup and suspension were calculated using the internal standard technique with metoclopramide HCl and codeine phosphate as internal standards (IS), respectively. The methods, for both mixtures, were validated and met all the requirements for the quality control analysis recommended by FDA and ICH.

• Clinical and Experimental Pediatrics
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• 제61권4호
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• pp.132-134
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• 2018

We report a unique case of intestinal duplication detected on posterior reversible encephalopathy syndrome (PRES) in a 13-year-old girl. She was admitted to the pediatric Emergency Department because of generalized seizures. Radiological assessment revealed a large, well-defined, thick-walled cystic lesion in the mid abdomen, suggestive of duplication cyst associated to a PRES. Exploration confirmed the diagnosis of ileal duplication cyst, and the mass was resected. The postoperative course was uneventful. Both hypertension and neurological dysfunction resolved after the mass resection. A follow-up brain magnetic resonance imaging was performed 9 months later and showed complete resolution of the cerebellar changes. Although extrinsic compression of the retroperitoneal structures has not been reported in the literature as a complication of duplication cyst, we strongly believe that this is the most logical and plausible hypothesis that would explain the pathogenesis of PRES in our patient.

• The Korean Journal of Pain
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• 제11권2호
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• pp.321-325
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• 1998

Most of the patients with pain resulting from advanced cancer need opioid for adequate analgesia. Various Methods of drug administration to control the pain have been developed. One of them, continuous administration of intravenous morphine is used for more effective pain control in the patient with severe pain that cannot be satisfactorily controlled by other Methods of morphine administration. But this is not a suitable method at home because of the possibility of serious infectious complications and the difficulty in managing intravenous access by untrained personnel. Continuous subcutaneous adminstration of drugs can not only overcome such disadvantages of continuous intravenous infusion but also get almost the same effect of pain control as continuous intravenous infusion, and allows opportunity to move freely and return home, improving quality of life. We used continuous subcutaneous morphine and metoclopramide in the patients with cancer pain via a portable PCA device, and accomplished satisfactory pain relief without significant side effect.

• The Korean Journal of Pain
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• 제9권1호
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• pp.178-182
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• 1996

Background: To evaluate the effect of prophylactic transdermal scopolamine in reducing nausea associated with postoperative epidural morphine. Methods: 30 healthy patients scheduled for cesarean section were given local anesthetics epidurally for surgical anesthesia. After delivery of the baby, transdermal scopolamine patch($Kimite^{(R)}$ Myung Moon Pharm. Co., Seoul, Korea) was applied to the study group(n=15) and placebo patch to the control group(n=15). Postoperative analgesia was provided soley with epidural morphine. Nausea was treated with metoclopramide. Results: During 24 hours postoperatively, the mean nausea score was significantly lower in the study group than in the control group. But the nausea incidence was not significantly different between the two groups. The mean number of times antiemetic drugs which were administered to patients were lower in the study group than in the control group($1.5{\pm}0.5$ vs $3.3{\pm}1.3$, p<0.05). Conclusion: Transdermal scopolamine patch provides antiemetic effect simply, continuously and safely, preventing nausea which could occur during administration of epidural morphine after cesarean section.