• Analytical Science and Technology
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• v.20 no.2
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• pp.138-146
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• 2007

A simple and sensitive method for the determination of paroxetine in canine plasma was developed and validated by liquid-liquid extraction and liquid chromatography-tandem mass spectrometry (LC-/MS/MS). Fluoxetine was used as an internal standard. Paroxetine and internal standard in plasma samples were extracted using TBME (tert-butyl methyl ether). A centrifuged upper layer was then evaporated and reconstituted with mobile phase of 50% acetonitrile adjusted to pH 3 by formic acid. The reconstituted samples were injected into a Capcell Pak UG120 ($2.0{\times}150mm$, $5{\mu}m$) column. Using MS/MS with SRM (selective reaction monitoring) mode, the transitions (precursor to product) monitored were m/z $330{\rightarrow}192$ for paroxetine, and m/z $310{\rightarrow}148$ for internal standard. Linear detection responses were obtained for paroxetine concentration range of 0.02~5 ng/mL. A correlation coefficient of linear regression ($R^2$) was 0.9993. Detection of paroxetine in canine plasma was accurate and precise, with limit of quantification at 0.02 ng/mL. The method has been successfully applied to pharmacokinetic study of paroxetine in healthy beagle dogs.

• Korean Journal of Biological Psychiatry
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• v.3 no.2
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• pp.277-287
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• 1996

Objective : It has been proposed that cognition and related aspects of mental functioning are decreased in depression as well as in alcoholism. The objective of the study was to compare behavioral side effects of paroxetine and amitriptyline in depressed patients accompanied by alcoholism. The focused comparisons were drug effects concerning psychomotor performance, cognitive function, sleep and daytime sleepiness during the first 2 weeks of treatment. Methods : After an alcohol detoxification period(3 weeks) and a washout period(1 week), a total of 20 male inpatients with alcohol use disorder (DSM-IV), who also had a major depressive episode(DSM-IV), were treated double-blind with paroxetine 20mg/day(n=10) or amitriptyline 25mg/day(n=10) for 2 weeks. All patients were required to have a scare of at least 18 respectively on bath the Hamilton Rating Scale far Depression(HAM-D) and Beck Depression Inventory(BDI) at pre-drug baseline. Patients randomized to paroxetine received active medication in the morning and placebo in the evening whereas those randomized to amitriptyline received active medication in the evening and placebo in the morning. All patients performed the various tasks in a test battery at baseline and at days 3, 7 and 14. The test battery included : critical flicker fusion threshold for sensory information processing capacity : choice reaction time for gross psychomotor performance : tracking accuracy and latency of response to peripheral stimulus as a measure of line sensorimotor co-ordination and divided attention : digit symbol substitution as a measure of sustained attention and concentration. To rate perceived sleep and daytime sleepiness, 10cm line Visual analogue scales were employed at baseline and at days 3, 7 and 14. The subjective rating scales were adapted far this study from Leeds sleep Evaluation Questionnaire and Epworth Sleepiness Scale. In addition a comprehensive side effect assessment, using the UKU side effect rating scale, was carried out at baseline and at days 7 and 14. The efficacy of treatment was evaluated using HAM-D, BDI and clinical global impression far severity and improvement at days 7 and 14. Results : The pattern of results indicated thai paroxetine improved performance an mast of the lest variables and also improved sleep with no effect on daytime sleepiness aver the study period. In contrast, amitriptyline produced disruption of performance on same tests and improved sleep with increased daytime sleepiness in particular at day 3. On the UKU side effect rating scale, mare side effects were registered an amitriptyline. The therapeutic efficacy was observed in favor of paroxetine early in day 7. Conclusion : These results demonstrated thai paroxetine in much better than amitriptyline for the treatment of depressed patients accompained by alcoholism at least in terms of behavioral safety and tolerability, furthermore the results may assist in explaining the therapeutic outcome of paroxetine. For example, and earlier onset of antidepressant action of paroxetine may be caused by early improved cognitive function or by contributing to good compliance with treatment.

• Korean Journal of Biological Psychiatry
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• v.2 no.2
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• pp.205-217
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• 1995

In comparison with tricyclic antidepressants(TCAs), one of the most interesting characteristics of selective serotonin reuptake inhibitors(SSRIs) is its structural differences, reveals different pharmacological properties. The applications at the moment are most effective in clinical applications to depression. The limited result of the research to date on the various applications of SSRIs has not revealed the total potential and applicability of SSRIs. Therefore, attending physicians utilizing SSRIs do not know the full capabilities of the drug on patients and what the patients may reap in terms of benefit from its curing elements. Physicians must first try to understand the full potential of SSRIs and its potential applications for it to be effective on patients. recently, it has been determined that SSRIs and other drugs when administered together may be more effective in the healing process because SSRIs complements and aids in the enhancement and effect of the other drugs. This article is written to give attention to the reader of the pharmacological properties and the clinical use of SSRIs. It is the authors's hope that continuous research on the particular aspects of SSRIs can aid the clinicians in the use of this SSRIs.

• Journal of the Korean Applied Science and Technology
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• v.28 no.2
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• pp.170-177
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• 2011

Transdermal drug delivery(TDS) offers many important advantages. For instance, it is easy and painless, it protects the active compound from gastric enzymes, and it avoids the hepatic first-pass effect. Also, it is simple to terminate the therapy if any adverse or undesired effect occurs. But skin is a natural barrier, and only a few drugs can penetrate the skin easily and in sufficient quantities to be effective. Therefore, in recent years, numerous studies have been conducted in the area of penetration enhancement. The most commonly used transdermal system is the skin patch using various types of technologies. Compared with other method of dosage, it is possible to use for a long term. It is also possible to stop the drug dosage are stopped if the drug dosage lead to side effect. Polysaccharide, such as xanthan gum and algin were selected as base materials of TDS. Also, these polymers were characterized in terms of enhancers and drug contents. Among these polysaccharide, the permeation rate of Paroxetine such as lipophilic drug was the fastest in xanthan gum matrix in vitro. We used glycerin, PEG400 and PEG800 as enhancers. Since dermis has more water content(hydration) than the stratum corneum, skin permeation rate at steady state was highly influenced when PEG400 was more effective for lipophilic drug. Proper selection of the polymeric materials which resemble and enhance properties of the delivering drug was found to be important in controlling the skin permeation rate.

• 대한불안의학회:학술대회논문집
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• 2003.11a
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• pp.51-52
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• 2003

• 대한임상약리학회:학술대회논문집
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• 1997.12a
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• pp.42-42
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• 1997

• Anxiety and mood
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• v.3 no.2
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• pp.110-115
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• 2007

Objective : The authors examined the treatment response and remission rates in patients with panic disorder after short-term pharmacotherapy in an effort to determine the factors that can be used to predict remission in Korean patients with panic disorder. Methods : Sixty-one patients with panic disorder were recruited for participation in this study. The psychological symptoms of the patients were measured using the HAMA, HAMD, STAIS, STAIT, ASI and API at baseline and after 3 months of pharmacotherapy. Results : Patients with panic disorder showed significantly lower scores on all psychological measures after 3 months of pharmacotherapy with paroxetine. The remission rate was 44.3%, and the response rate was 54.1%. The remitters showed significantly lower HAMD, HAMA, STAIS, STAIT, and ASI scores than the non-remitters. Linear regression analysis revealed that the baseline HAMA, HAMD, and ASI scores could be used to predict the remission rate after controlling for age, sex and agoraphobia. Conclusion : Compared with previous reports, our study showed a similar remission rate in Korean patients with panic disorder. Lower baseline levels of anxiety, depression, and anxiety sensitivity were found to be predictors of treatment remission in panic disorder.

• Korean Journal of Biological Psychiatry
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• v.1 no.1
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• pp.88-97
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• 1994

Many evidences are compatible with the correlation between the inhibition of [$^3H$] imipramine([$^3H$]IMI) and [$^3H$]paroxetine([$^3H$]PAT) binding to the 5-hydroxytryptamine(5-HT) transporter complex and the 5-HT uptake of 5-HT neurons and platelets, and most antidepressants have been shown to inhibit the [$^3H$]IMI and [$^3H$]PAT binding and the neuronal 5-HT uptake. However, several paradoxical research findings led to doubt about the pharmacological significance of the [$^3H$]IMI and [$^3H$]PAT binding sites. This study was carried to clarify the correlation between the [$^3H$]IMI and [$^3H$]PAT binding parameters and the tissue 5-HT content or/and [$^3H$]5-HT uptake in the rabbit platelet, which contains 40 times ad much 5-HT as that of human platelet and shows the 10 fold higher $B_{max}$ of the 5-HT transporter binding to a 5-HT uptake inhibitor. The rabbits were treated for 28 days with amitriptyline(4mg/kg/day : AP), fluoxetine(0.5mg/kg/day : FO), and sertraline(0.5mg/kg/day : SA) via an Alzet osmotic pump implanted for constant infusion. The [$^3H$]IMI binding $B_{max}$ and $K_d$ of the rabbit platelets were $6.4{\pm}1.2$pmol/mg protein and $10.9{\pm}2.1$nM and those in the [$^3H$]PAT binding were $8.6{\pm}1.1$pmol/mg protein and $1.6{\pm}0.3$nM, respectively. AP slightly increased $B_{max}$ of [$^3H$]IMI binding and both [$^3H$]IMI binding and [$^3H$]PAT binding $K_d$, and i contrast, it slightly decreased $B_{max}$ of [$^3H$]PAT binding. FO Slightly increased $K_d$ of both and [$^3H$]IMI and [$^3H$]PAT binding and slightly decreased $B_{max}$ of [$^3H$]IMI and [$^3H$]PAT binding. SA produced the significant increase of [$^3H$]PAT binding $B_{max}$ and the slight increase of both [$^3H$]IMI and [$^3H$]PAT binding $K_d$ and in contrast, it slightly decreased $B_{max}$ and of [$^3H$]IMI binding. And, the $V_{max}$ and $K_m$ of platelet [$^3H$]5-HT uptake were $24.2{\pm}2.4$pmol/$10^8$ platelets/min and $3.3{\pm}0.3$nM, respectively. The $V_{max}$ was little affected by AP, FO, or SA, but the [$^3H$]5-HT uptake $K_m$ value was moderately increased by FO. However, the platelet 5-HT content was moderately decreased by all of the 5-HT uptake inhibitors used in this study. These results seem to be consistent with the allosterical and competitive interaction of 5-HT uptake inhibiting antidepressants with each other as well as 5-HT in the 5-HT transporter binding, and provide no support for the view that the potencies of 5-HT uptake inhibitors to inhibit the [$^3H$]IMI or [$^3H$]PAT binding with 5-HT transporter complex correlate with their antidepressant potencies.

• 대한임상약리학회:학술대회논문집
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• 1996.12a
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• pp.36-36
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• 1996

• Korean Journal of Psychosomatic Medicine
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• v.21 no.1
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• pp.3-10
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• 2013

Objectives : Many patients diagnosed with cancer suffer from various psychiatric symptoms such as depression, anxiety and insomnia as well as cancer itself. Patients with cancer are more vulnerable to possible adverse events of psychotropic medications. Although antidepressants are widely used among cancer patients, there is little information about tolerability of antidepressants. This study was conducted to compare tolerability of antidepressants in cancer patients referred for psychiatric consultation. Methods : The participants were cancer patients who had been referred to psychiatrist for their psychiatric symptoms. We retrospectively analyzed the data of patients diagnosed with cancer from 9 general hospitals in Korea. The discontinuation rate for a 6 months period after treatment initiation for three antidepressants(Escitalopram, Mirtazapine, Paroxetine) were compared. Results : Antidepressants were prescribed for 96.3% of subjects and Escitalopram 150(47.2%), Mirtazapine 92(28.9%) and Paroxetine 76(23.9%) were prescribed frequently in order There were no significant differences in discontinuation rates among the three antidepressants during the 6 month period after initiation of pharmacotherapy. But there was a difference in discontinuation rates between inpatients versus outpatients(p<0.0001). Conclusions : In a naturalistic setting for the antidepressant treatment for cancer patients, it seems that there are no differences in discontinuation rates among these three antidepressants. It is therefore essential that such interactions are carefully considered when treating patients of antidepressants who already have cancer.