• Korean Journal of Psychosomatic Medicine
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• v.19 no.2
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• pp.57-65
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• 2011

There are numerous drug interactions related to many psychotropic and cardiovascular medications. Firstly, the principles in predicting drug interactions are discussed. Cytochrome P (CYP) 450 plays a significant role in the metabolism of these drugs that are substrates, inhibitors, or inducers of CYP450 enzymes. The two most significant enzymes are CYP2D6 and CYP3A4. The ability of psychotropic drugs to act as inhibitors for the enzymes may lead to altered efficacy or toxicity of co-administered cardiovascular agents as a substrate for the enzymes. The following is also a review of the known interactions between many commonly prescribed cardiovascular agents and psychotropic drugs. Most beta blockers are metabolized by CYP2D6, which may lead to drug toxicity when they use in combination with potent CYP2D6 inhibitors including bupropion, chlorpromazine, haloperidol, selective serotonin reuptake inhibitors, and quinidine. Concomitant administration of lithium with angiotensin converting enzyme inhibitors, angiotensin receptor blockers, and diuretics may increase serum lithium concentrations and toxicity. Calcium channel blockers and cholesterol lowering agents are subject to interactions with potent inhibitors of CYP3A4, such as amiodarone, diltiazem, fluvoxamine, nefazodone, and verapamil. Prescribing antiarrhythmic drugs in conjunction with medications are known to prolong QT interval and/or inhibitors on a relevant CYP450 enzyme is generally not recommended, or needs watchful monitoring. Digoxin and warfarin also have warrant careful monitoring if co-administered with psychotropic drugs.

• Korean Journal of Biological Psychiatry
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• v.3 no.2
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• pp.251-257
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• 1996

Selective serotonin reuptake inhibitors(SSRIs), as haloperidol, ore metabolized in the cytochrome P450IID6. They can cause inhibition of metabolism of antipsychotics to elevate the serum level of antipsychotics and exacerbate the extrapyramidal symptoms when co-administered with antipsychotics. Among these SSRIs, there ore a few studies about paroxetine compared to fluoxetine or sertraline. In this study, we have intended to know the drug interaction of paroxetine and haloperidol when co-administered two drugs for the chronic schizophrenics by assessing the changes of positive, negative symptoms and extrapyramidal symptoms. for this purpose, we selected 29 subjects, the chronic schizophrenics with no physical problems. They were under maintenance therapy of haloperidol. They ore randomly assigned to placebo group(n=12) and drug group(n=17) by using double blind method. And then, placebo or paroxetine 20mg were administered to the subjects of each groups during 8 week period. We have assessed their psychopathology and extrapyramidal symptoms using Positive and Negative Syndrome Scale(PANSS), Hamilton Rating Scale lor Depression(HRSD), Simpson-Angus Scale at 0, 2, 4, 6, 8 weeks and serum haloperidol, reduced haloperidol levels at 0, 4, 8 weeks during the period. The results ore analysed by using repeated measure MANOVA. 27 subjects have completed the study during 8 weeks. among the subjects, 1) PANSS, HRSD ; no significant difference between groups. 2) Simpson-Angus Scale ; no significant change according to the time and no significant difference between the groups(no group and time effect). 3) Haloperidol and reduced haloperidol level ; no significant change. When co-administered paroxetine and haloperidol, there ore no significant changes of the psychopothology and no significant changes of the extrapyramidal symptoms. In this result, paroxetine seems to be not to affect the metabolism of haloperidol.

• The Korean Journal of Pain
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• v.28 no.1
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• pp.4-10
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• 2015

Etifoxine (etafenoxine, $Stresam^{(R)}$) is a non-benzodiazepine anxiolytic with an anticonvulsant effect. It was developed in the 1960s for anxiety disorders and is currently being studied for its ability to promote peripheral nerve healing and to treat chemotherapy-induced pain. In addition to being mediated by $GABA_A{\alpha}2$ receptors like benzodiazepines, etifoxine appears to produce anxiolytic effects directly by binding to ${\beta}2$ or ${\beta}3$ subunits of the $GABA_A$ receptor complex. It also modulates $GABA_A$ receptors indirectly via stimulation of neurosteroid production after etifoxine binds to the 18 kDa translocator protein (TSPO) of the outer mitochondrial membrane in the central and peripheral nervous systems, previously known as the peripheral benzodiazepine receptor (PBR). Therefore, the effects of etifoxine are not completely reversed by the benzodiazepine antagonist flumazenil. Etifoxine is used for various emotional and bodily reactions followed by anxiety. It is contraindicated in situations such as shock, severely impaired liver or kidney function, and severe respiratory failure. The average dosage is 150 mg per day for no more than 12 weeks. The most common adverse effect is drowsiness at the initial stage. It does not usually cause any withdrawal syndromes. In conclusion, etifoxine shows less adverse effects of anterograde amnesia, sedation, impaired psychomotor performance, and withdrawal syndromes than those of benzodiazepines. It potentiates $GABA_A$ receptor-function by a direct allosteric effect and by an indirect mechanism involving the activation of TSPO. It seems promising that non-benzodiazepine anxiolytics including etifoxine will replenish shortcomings of benzodiazepines and selective serotonin reuptake inhibitors according to animated studies related to TSPO.

• Development and Reproduction
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• v.6 no.2
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• pp.111-115
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• 2002

5-Hydroxytryptamine(5-HT; serotonin) system has been implicated in the modulation of male sexual behaviors and the secretion of reproductive hormones. In human males, selective serotonin re-uptake inhibitors(SSRIs) are known to improve the major male sexual dysfunction, premature ejaculation, through the central nervous system-mediated pathways. As numerous hormone and local factors, 5-HT may have peripheral role in the regulation of male sexual function. The expression of 5-HT receptor subtypes in the target tissue, however, has not been explored yet. The present study was undertaken to test whether the 5-HT receptor subtypes are expressed in the reproductive tissues of male rat, especially in ejaculatory machinery such as seminal vesicle and vas deferens. To do this, reverse transcription-polymerase chain reaction(RT-PCR) and Southern blot analysis were employed. The transcripts for the 1A, 1B and 2C subtypes of 5-HT receptor were amplified in all the tested tissues. The present study demonstrated the expression of 5-HT receptor in the rat ejaculatory machinery, suggesting that 5-HT may play a pivotal role in the male sexual function via not only central pathway but also peripheral route. Further study on the receptor subtype-specific effect and their harmonized mode of action will be needed to establish the understanding of ejaculation mechanism and drug design.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.3 no.1
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• pp.32-37
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• 2017

Cis-(1S,4S)-4-(3,4-dichlorophenyl)-1,2,3,4-tertrahydro-N-methyl-1-naphthalenamine (sertraline) hydrochloride from among selective serotonin reuptake inhibitors (SSRIs) is a treatment of major depression. For the differential diagnosis by metabolizing serotonin in a patient with neurological disorders, the radiolabeled $^{11}C$-sertraline was developed for non-invasive positron emission tomography in living brain and use the evaluation of new drug for SSRIs. We release the results of a fast and easy radiolabeling method applied a one-step loop method with $[^{11}C]CH_3OTf$ for routine clinical applications of $^{11}C$-sertraline. 1 mg of a precursor for $^{11}C$-sertraline in 0.1 mL DMF and $5{\mu}L$ of 1N NaOH, were injected into the loop of semi-prep high-performance liquid chromatography (HPLC). $[^{11}C]CH_3OTf$ was passed through the loop at room temperature (RT). The $^{11}C$-sertraline was separated by the semi-preparative HPLC. $^{11}C$-sertraline was eluted at 28.0 min was collected and evaluated by analytical HPLC and mass spectrometer. The total radiolabeling efficiency of $^{11}C$-sertraline was $30.7{\pm}8.7%$. The specific activity was $64.8{\pm}51.4GBq/{\mu}mol$. The radiochemical and chemical purities were higher than 99%. The mass spectrum of the product showed m/z peaks at 307.1 (M+1), indicating the mass of sertraline. By the one-step loop method with $[^{11}C]CH_3OTf$, $^{11}C$-sertraline could be quickly and easily prepared for clinical application.

• Korean Journal of Psychosomatic Medicine
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• v.11 no.1
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• pp.44-51
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• 2003

Objectives: Antidepressants are frequently associated with sexual dysfunction. Especially, there were few report of sexual dysfunction related with venlafaxine and mirtazapine in Korea. The purpose of this survey was to evaluate the frequency and nature of sexual dysfunction related with selective serotonin reuptake inhibitors(SSRIs), venlafaxine and mirtazapine by the use of specific questionaires. Methods: In one hundred twenty two patients, sexual dysfunction was investigated cross-sectionally by using The questionaires for sexual dysfunction, which includes questions about decreased libido, delayed orgasm or ejaculation, premature ejaculation or orgasm, absence of orgasm or ejaculation, erectile dysfunction in men/vaginal lubrication dysfunction in women, sexual pain and patient's tolerance of the sexual dysfunction. BDI was also measured. Sexual dysfunction was analyzed in association with the duration and the dose of medications and the severity of depression. Results: The incidence of sexual dysfunction during antidepressants use in our survey was 37.7%. There were no difference of incidence in sexes(p=.746). In comparison of paroxetine, venlafaxine and mirtazapine, there were no significant differences of the incidence(p=.065) and the severity of any type of sexual dysfunction. Conclusion: Although there were no significant differences of sexual dysfunction in our survey, sexual dysfunction may be closely associated with antidepressants. Further prospective study of sexual dysfunction should be needed.

• Korean Journal of Psychosomatic Medicine
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• v.9 no.2
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• pp.111-132
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• 2001

Depression in the medically ill is a common clinical problem that primary physicians and psychiatric consultants encounter. Treatment of such patients begins with a careful evaluation of the patient's medical and psychiatric conditions. The assessment of depression in the medical patients requires a multidimensional approach. Psychological instruments are also used as a method of assessment in these patients. First of all, what the therapists have to do is to find and remove organic causes. Psychosoical treatment includes dealing with the patient's resistance and despondency relevant to physical diseases. For biological treatment, it is important to select appropriate antidepressants. Therapists should be familiar with the side effects of the antidepressants as well as the patient's primary depressive symptoms, pharmacokinetics and pharmacodynamics of the available agents. In addition, special attention should be paid to the potential for drug-illness and drug-drug interactions. Tricyclic antidepressants can be still effectively used for patients with pain disorder, although a variety of new antidepressants such as selective serotonin reuptake inhibitors (SSRI), bupropion and venlafaxine could have more benefits in depression of the medically ill. However, electroconvulsive therapy can be recommended for refractory cases of depression in patients with medical illness.

• Korean Journal of Clinical Pharmacy
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• v.23 no.1
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• pp.33-41
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• 2013

Background: Prevalence of depression comorbid with neurologic disorders such as Alzheimer' disease (AD), Parkinson's disease (PD) and vascular dementia (VD) is higher than that of primary depression. Antidepressant medications, suggested by many researches for depression comorbid with neurologic disorders such as AD, PD and VD, are mainly selective serotonin reuptake inhibitors (SSRI). Objective: The primary objective of this study is the evaluation of antidepressant drug therapy for AD, PD and VD. Method: This study was a retrospective study based on medical records, carried out for 3 years and 6 months (Jan. 2007~Jul. 2010). Patients, diagnosed as comorbid depression through Beck Depression Inventory (BDI), Cornell Depression Scale (CDS), Geriatric Depression Scale (GDS) among neurologic out-patients of Chungnam National University Hospital because of AD, PD and VD, were selected. The results were evaluated by efficacy and safety of antidepressant drug therapy. Results: In result, the prescribing rates of antidepressants were 30%, 55% and 40% for each AD, PD and VD. Depression cure rates of patients receiving antidepressants vs patients not receiving antidepressants were 40% vs 39%, 33% vs 23% and 38% vs 30% for AD, PD and VD. The frequencies of prescriptoin of SSRI were 21%, 11% and 27% for each AD, PD and VD. The frequencies of prescriptoin of benzodiazepine (BZD) was 61%, 82% and 61% for each AD, PD and VD. The ratio of single BZD prescription was more than that of combination prescription of antidepressants. Tricyclic antidepressants (TCA) were rarely prescribed. The rate of patients with BZD-related side effects was 54%. The most frequent side effects of BZD were dizziness (30%), drowsiness (21%) and headache (16%). Side effects of SSRI were rare. Conclusion: In conclusion, the frequencies of prescription of antidepressants were not common for AD, PD and VD. There was little difference in depression cure rate between patient receiving antidepressants and not receiving. Even though SSRI has to be the highest priority of usage, the frequencies of prescription of SSRI were lower than those of BZD. Additional researches and efforts are required to improve antidepressant drug therapy for neurologic disorders such as AD, PD and VD.

• Korean Journal of Schizophrenia Research
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• v.22 no.2
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• pp.21-33
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• 2019

Objectives: The current study covers a secondary revision of the guidelines for the pharmacotherapy of schizophrenia issued by the Korean Medication Algorithm for Schizophrenia (KMAP-SCZ) 2001, specifically for co-existing symptoms and antipsychotics-related side-effects in schizophrenia patients. Methods: An expert consensus regarding the strategies of pharmacotherapy for positive symptoms of schizophrenia, co-existing symptoms of schizophrenia, and side-effect of antipsychotics in patients with schizophrenia was retrieved by responses obtained using a 30-item questionnaire. Results: For the co-existing symptoms, agitation could be treated with oral or intramuscular injection of benzodiazepine or antipsychotics; depressive symptoms with atypical antipsychotics and adjunctive use of antidepressant; obsessive-compulsive symptoms with selective serotonin reuptake inhibitors and antipsychotics other than clozapine and olanzapine; negative symptoms with atypical antipsychotics or antidepressants; higher risk of suicide with clozapine; comorbid substance abuse with use of naltrexone or bupropion/varenicline, respectively. For the antipsychotics-related side effects, anticholinergics (extrapyramidal symptom), propranolol and benzodiazepine (akathisia), topiramate or metformin (weight gain), change of antipsychotics to aripiprazole (hyperprolactinemia and prolonged QTc) or clozapine (tardive dyskinesia) could be used. Conclusion: Updated pharmacotherapy strategies for co-existing symptoms and antipsychotics-related side effects in schizophrenia patients as presented in KMAP-SCZ 2019 could help effective clinical decision making of psychiatrists as a preferable option.

• Korean Journal of Biological Psychiatry
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• v.14 no.2
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• pp.91-98
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• 2007

Objectives : Considering the impact of depressive illness on physical and mental health of both mother and fetus, specification of a treatment algorithm for depressive disorder during pregnancy is legitimated. This article provides a systemic review of treatments for depressive disorder during pregnancy and lactation. Methods : According to the search strategy of the Clinical Research Center for Depression of Korean Health 21 R & D Project, PubMed and EMBASE were searched using terms with regard to the treatment of depressive disorders during pregnancy and lactation. Reference lists of related reviews and studies were searched. In addition, relevant practice guidelines were searched using the PubMed. All identified clinical literatures were reviewed and summarized in a narrative manner. Results : Pharmacotherapy during pregnancy and lactation requires a comprehensive assessment of the risks and benefits of treatment for both mother and fetus or neonate. Recently, there is growing evidence that the use of tricyclic and selective serotonin reuptake inhibitors during pregnancy and lactation does not result in increased risks of teratogenicity. Treatment strategies are described according to the point of time of pregnancy or lactation. FDA categories for antidepressants during pregnancy and lactation are described. In addition, issues regarding to the electroconvulsive therapy and psychosocial treatment are discussed. Conclusion : The treatment option for depressive disorders during pregnancy and lactation depends on the severity of depressive illnesses of the individual patient. For mild to moderate depression, the non-pharmacological treatment should be considered first. For moderate to severe depression, pharmacotherapy should be administered in addition to the psychosocial treatment. ECT is recommended for depressive disorder of severe intensity. As the research knowledge is limited, the recommendations should based on the best judgement of psychiatrists.