• The Korean Journal of Pain
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• v.2 no.1
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• pp.45-48
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• 1989

Trigeminal neuralgia is one of the diseases which cause most chronic and intractable pain on the facial area. Several drugs includding analgegics, anticonvulsants, tranquilizers, vitamins or hormonal preparations have been expected to be effective but no drug could effectively relieve the patients from the pain. The pain could be relieved by surgical neurectomy or neurolysis of the Gasserian ganglion or the involved branches with absolute alcohol alternatively. Surgical microvascular decompression may be performed if the pain resulted from compression of the nerve by adjucent arterial loops. 4 cases of trigeminal neuralgia are presented. They were treated with alcohol neurolysis of the involved peripheral nerves combined with or without carbamazepine and/or amitriptyline with favorable result of pain relief.

• 대한임상약리학회:학술대회논문집
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• 1994.12a
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• pp.25-25
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• 1994

• 대한임상약리학회:학술대회논문집
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• 1995.12a
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• pp.51-51
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• 1995

• 대한임상약리학회:학술대회논문집
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• 1996.12a
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• pp.27-27
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• 1996

• The Korean Journal of Physiology and Pharmacology
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• v.1 no.1
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• pp.13-17
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• 1997

Carbamazepine (CBZ), an anticonvulsant, has beeen reported to displace ligands at adenosine receptors. Several studies have demonstrated that as far as $A_2$adenosine receptors is concerned, CBZ acts as an antagonist. However, the situation with regard to Al receptors is less straightforward. In this study, we describe the effects of one-week CBZ treatment (25 mg/kg/day) on cerebrocortical $A_1$ adenosine receptors. $A_1$ adenosine receptor bindings as determined by using $[^3CH]DPCPX$ was not significantly altered in membranes prepared from CBZ-treated rats. However, there was a significant decrease in the $A_1$ adenosine receptor-mediated stimulation of $[^{35}S]GTP_{\gamma}S$ binding to cerebrocortical membranes prepared from CBZ-treated rats (20.0% decrease in basal activity; 17.8% decrease in maximal activity). The basal and $10^{-4}$ M forskolin-stimulated adenylyl cyclase activities were relatively unaffected by CBZ treatment, but 10 mM NaF-stimulated adenylyl cyclase activity was significantly reduced in CBZ-treated rats. It appears that one-week CBZ treatment caused an uncoupling of adenosine receptors from G proteins without alteration of $A_1$ adenosine receptor molecules, suggesting that CBZ acts as an agonist at $A_1$ adenosine receptors in rat brain.

• Polymer(Korea)
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• v.36 no.3
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• pp.332-337
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• 2012

The primary objective of this work is to find the properties of sustained release dissolution pattern depending on solubility of drugs, so venlafaxine HCl and carbamazepine tablets were made by using polymer wich various particle size. Hydroxy propyl methyl cellulose (HPMC) has been utilized in this study as an excipient that is one of the most widely used polymers for an oral sustained release formulation, and drug release pattern was strongly influenced by swelling rate depending on particle size of HPMC. Scanning electron microscope (SEM) was employed to investigate the surface of tablets with various HPMC particle size, and differential scanning calorimeter (DSC) was employed to investigate the crystallization of drugs in tablets. The release model equation was applied to analyze the main mechanism of drug release pattern. The results demonstrate that drug release pattern is controlled by the drug solubility and HPMC particle size.

• Korean Journal of Biological Psychiatry
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• v.7 no.1
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• pp.14-20
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• 2000

Recently atypical antipsychotics have been used as first line agent in the treatment of schizophrenia, and also played a significant role in the treatment of many kinds of psychiatric disorders. The pharmacokinetic and pharmacodynamic properties of these newer antipsychotics are well known through preclinical and early clinical trials. However, it is important to note the limitations of the results due to its relatively short experience. Clozapine is eliminated principally by the hepatic P450 1A2 and 3A4 cytochrome enzymes. 1A2 inducers such as carbamazepine and smoking can reduce its half-life, while 1A2 inhibitors such as SSRIs, especially fluvoxamine can increase its duration of action. Carbamazepine should be avoided in a patient on clozapine because of carbamazepine's potential effects on bone marrow. Benzodiazepines tend to increase the chances of sedation, delirium and respiratory depression. Risperidone is metabolized to 9-hydroxyriperidone by the hepatic P450 2D6 cytochrome enzymes. Fluoxetine and paroxetine, 2D6 inhibitors interfere with metabolism, but 9-hydroxyrisperidone has similar biological activity as parental drug, so it has little affect on the outcome. Olanzapine shows minimal capacity to inhibit cytochrome P450 isoenzymes and shows minimal chance of drug interaction. It is eliminated principally by the hepatic P450 1A2 and 2D6 cytochrome enzymes.

• Journal of Environmental Analysis, Health and Toxicology
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• v.21 no.4
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• pp.243-251
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• 2018

Pharmaceuticals in wastewater effluents have been recognized as emerging pollutants threatening freshwater organisms. To extend understanding for bioaccumulation and toxicity in those organisms, information on biotransformation products (or metabolites) and their metabolic pathway are crucial. The aim of the present study is to identify and elucidate metabolites of pharmaceuticals formed in exposed organisms using suspect and nontarget screening approach using LC-HRMS. As the target pharmaceuticals, carbamazepine, ketoprofen, metoprolol, propranolol, and verapamil were selected whereas Daphnia magna and Gammarus pulex were used as test organisms. After 24h exposure, metabolites formed in the organisms were identified using LC-HRMS. The structures of metabolites were elucidated via analysis of MS/MS fragment pattern and the comparison with fragment database. As the results, a total of 10 metabolites were identified for 5 parent compounds (C253/C356 for carbamazepine, K211 for ketoprofen, M256 for metoprolol, P218/P276/P306 for propranolol, V196/V291/V441 for verapamil). Among them, the presence of C253 and V291 was confirmed using standard materials. Most of the identified metabolites were formed through oxidative reactions such as hydroxylation, N-demethylation, and dealkylation. Cysteine conjugation (phase II reaction) metabolite (C356) for carbamazepine was found in daphnia. The metabolic pathway of verapamil showed similar metabolic pathways and metabolic pathways for both species. Although the toxicological information on the identified metabolites could not be confirmed, the molecular structure information of the proposed metabolites can be used for future evaluation and prediction of toxicity.

• Journal of Pharmaceutical Investigation
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• v.38 no.5
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• pp.335-342
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• 2008

The bioequivalence of two carbamazepine preparations was conducted. The in vivo bioequivalence study in 20 healthy male Korean volunteers was designed by using a single dose, randomized, 2-period crossover with a 3-weeks washout period between the doses. Prior to the in vivo study, an in vitro comparative dissolution test was performed by the paddle and basket method as described in the bioequivalence guidance of the Korea Food and Drug Administration (KFDA). Based on the similar dissolution pattern between two preparations in the dissolution test, the two formulations are demonstrated to be pharmaceutically equivalent. In addition, in vivo bioequivalence test was used to reconfirm the in vitro dissolution results. In the in vivo bioequivalence study, the plasma concentrations of carbamazepine up to 144 h after the administration were determined using a validated HPLC method with UV detection and the bioequivalence between the two drug products was assessed by statistical analysis of the log transformed mean ratios of $C_{max}$, $AUC_{0-t}$ and $AUC_{0-\infty}$. The mean maximum concentration ($C_{max}$) of the test and reference were found to be $1467.0{\pm}335.8\;ng/mL$ and $1465.9{\pm}310.3\;ng/mL$, respectively. The 90% confidence intervals (C.I.) of $C_{max}$ were in the range from 0.95 to 1.05. As for the $AUC_{0-t}$ and $AUC_{0-\infty}$, test values were $110027.1{\pm}27786.4\;ng/mL{\cdpt}h$, $128807.0{\pm}34563.2\;ng/mL{\cdot}h$ and $105473.6{\pm}26496.2\;ng/mL{\cdot}h$, $125448.5{\pm}35975.5\;ng/mL{\cdot}h$, respectively. The 90% C.I. of $AUC_{0-t}$ were 0.97 to 1.10 and of $AUC_{0-\infty}$, 0.99 to 1.09 and thus were within the log 0.8-log 1.25 interval proposed by the KFDA. A two-way ANOVA showed no significant difference between the two formulations. Based on these statistical analysis, it was concluded that the test formulation is bioequivalent to the reference.

• Journal of Korean Society of Environmental Engineers
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• v.39 no.7
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• pp.403-411
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• 2017

In this study, the occurrence and temporal variation of eight pharmaceuticals comprising antibiotics (clarithromycin, sulfathiazole, sulfamethazine, sulfamethoxazole, trimethoprim), scabicide (carbamazepine) and nonsteroidal anti-inflammatory drugs (acetylsalicylic acid, naproxen) in main stream and its tributary of the Nakdong River basin, were investigated. Concentrations of the target compounds ranged from $1.076{\mu}g/L$. The highest average concentration was observed for clarithromycin ($0.0316{\mu}g/L$), followed by sulfamethazine ($0.0170{\mu}g/L$), sulfamethoxazole ($0.0161{\mu}g/L$), naproxen ($0.0129{\mu}g/L$), carbamazepine ($0.0093{\mu}g/L$), acetylsalicylic acid ($0.0047{\mu}g/L$), sulfathiazole ($0.0024{\mu}g/L$) and trimethoprim ($0.0022{\mu}g/L$). The decreasing pattern of pharmaceutical concentrations was observed along with Nakdong River and the higher concentrations in downstream were observed than those in upstream. There was no temporal variation of the target compounds although the highest level was found in February. The calculated hazard quotients (HQs) for eight pharmaceuticals were below 1, indicating no environmental hazard in Nakdong River. However, further monitoring is still needed due to the other pharmaceuticals widely used in Korea.