Many psychotropic drugs are marketed and prescribed as a racemate form in a mixture of the stereoisomers. A chiral center or a center of unsaturation of carbon atoms in the chemical structures creates various stereoisomers of the psychotropic drugs, including antidepressants such as fluoxetine and venlafaxine, etc. The stereochemical significances of enantiomers on the pharmacokinetics and pharmacodynamics of several psychotropic drugs and their relationships with pharmacogenetic polymorphisms were reviewed. The single enantiomer drugs will be increasing more in the market shares replacing the racemic drugs by chiral switching, which is driven by the development of the analytical and preparative resolution techniques and will be of much benefit to the treatment from low dosages, simple dose-response curve, few adverse reactions, and so on.
Antidepressive Agents ; Carbon ; Fluoxetine ; Pharmacokinetics ; Psychotropic Drugs* ; Stereoisomerism ; Venlafaxine Hydrochloride

OBJECTIVE: The purpose of this study was to compare the efficacy and safety of escitalopram, paroxetine and venlafaxine in Korean patients with major depressive disorder (MDD). METHODS: A total of 449 Korean MDD patients were recruited in a six-week, randomized, rater-blinded, active-controlled trial and were evenly randomized to paroxetine, venlafaxine, or escitalopram treatment. RESULTS: When comparing the mean difference for the Montgomery-Åsberg Depression Rating Scale (MADRS) and the Hamilton Depression Rating Scale (HDRS) total scores during six weeks, paroxetine (−6.4±0.4, and −5.4±0.4, respectively) was found to be significantly superior to escitalopram (−3.7±0.5 and −3.1±0.4, respectively). Venlafaxine had a significantly lower MADRS total score (−5.4±0.4) than escitalopram. When adjusting baseline variables, the response, according to the MADRS and HDRS scores, in the paroxetine group was greater than that for the escitalopram group (odds ratio [OR]=2.43, 95% confidence interval [CI]=1.42–4.16 for MADRS; and OR=2.32, 95% CI=1.35–3.97 for HDRS) and the venlafaxine group (OR=1.94, 95% CI=1.17–3.21 for MADRS; and OR=1.71, 95% CI=1.03–2.83 for HDRS). Despite that the overall tolerability was high and similar among the three groups, a total of 268 subjects (59.7%) prematurely discontinued treatment, representing the main limitation of the present study. CONCLUSION: Although a low study completion rate limits generalizability, our findings suggest that paroxetine might be superior to escitalopram in Korean MDD patients. Further studies should be conducted to draw a definite conclusion.
Citalopram* ; Depression ; Depressive Disorder, Major* ; Humans ; Paroxetine* ; Venlafaxine Hydrochloride*

OBJECTIVE: During the transition to menopause, various symptoms including vasomotor symptoms and depressed mood lead to low quality of life. We investigated the effect of low-dose venlafaxine hydrochloride extended release on depressed mood and vasomotor symptoms of perimenopausal women. METHODS: 33 perimenopausal women fulfilling Diagnostic and Statistical Manual of Mental Disorders, fourth edition criteria for a depressive episode were enrolled between January 2014 and May 2014. Subjects were prescribed 37.5 mg/day or 75 mg/day venlafaxine hydrochloride according to clinician's judgement, and the dosages were maintained for 8 weeks. Depressed mood and other psychological difficulties were evaluated by using Hamilton Rating Scale for Depression (HAMD), Hamilton Rating Scale for Anxiety (HAMA), Clinical Global Impression-Severity. Climacteric symptoms including vasomotor symptoms were evaluated by using Greene Climacteric Scale (GCS). For statistical analysis, paired t-test was used. RESULTS: Significant decreases in HAMD, HAMA, GCS scores were observed after 2 weeks of treatment and the trends continued until the end of the study. The scores of HAMD significantly decreased, 28 of them reached remission (HAMD < or =7). The scores on vasomotor symptoms of GCS after 8 week treatment significantly decreased compared to baseline (13.1+/-5.0, p<0.01). CONCLUSION: These results suggest that venlafaxine hydrochloride is effective and tolerable treatment option for vasomotor symptoms and depressed mood in perimenopausal women. To validate our results, furthur studies with double-blind, placebo controlled will be needed.
Anxiety ; Climacteric ; Depression ; Diagnostic and Statistical Manual of Mental Disorders ; Female ; Humans ; Menopause ; Quality of Life ; Venlafaxine Hydrochloride

While in the past the almost sole availability of tricyclic antidepressants had limited antidepressant drug selection, newer drugs such as selective serotonin reuptake inhibitors, bupropion, mirtazapine and venlafaxine have vastly simplified treating depression in patients with medical illness. Appropriate selection of an antidepressant agent in medically ill patients requires a careful risk-benefit assessment of the antidepressant treatment considering the pharmacokinetic and pharmacodynamic properties of drugs, potential for drug interaction, the patient's general medical conditions, and primary symptoms of the patient's depression. The effective and safe approach to antidepressant treatment is to reduce initial dosage, to titrate upward more slowly, and to monitor closely adverse effects in patients with medical illness.
Antidepressive Agents, Tricyclic ; Bupropion ; Depression* ; Drug Interactions ; Humans ; Risk Assessment ; Serotonin Uptake Inhibitors ; Venlafaxine Hydrochloride

Depressive disorders often develop into chronic course and relapse of symptoms is prevalent. Long-term treatment with antidepressants consolidates the improvement of residual symptoms and prevents relapses and recurrences. In the long-term treatment, the long-term tolerability of antidepressant is a major factor which impact on the compliance and the success of treatment. Although new antidepressants have better side effect profiles than TCA and MAOI, the safety issues of the former are also a concern during continuation and maintenance phases of treatment. Nowadays, weight gain and sexual dysfunction are at a center of concern in this field. SSRI, venlafaxine and mirtazapine can cause weight gain in some patients. Many studies report that weight gain and sexual dysfunction cause significant sufferings and act as major reasons of non-compliance. Bupropion SR is a new antidepressants that has a unique pharmacological property. It produce neither substantial weight gain nor sexual side effect. It was also shown to be effective and well-tolerated in decreasing the risk for relapse of depression. So, Bupropion SR can be used preferentially as a first-line antidepressant or augmentation on other agents in the long-term treatment without significant weight gain and sexual side effects.
Antidepressive Agents* ; Bupropion* ; Compliance ; Depression ; Depressive Disorder ; Humans ; Recurrence ; Weight Gain ; Venlafaxine Hydrochloride

OBJECTIVE: The present study aimed to determine the intracellular action of the antidepressant, venlafaxine, in C6 glioma cells using heat shock protein 70 (HSP70) immunocytochemistry and HSP70 Western blots; HSP70 is known to be associated with stress and depression. METHODS: The extent of HSP70 expression was measured after rat C6 glioma cells were treated with 1) dexamethasone only, 2) venlafaxine only, 3) simultaneous venlafaxine and dexamethasone, or 4) dexamethasone after venlafaxine pretreatment. Dexamethasone (10 microM, 6 hours) did not affect the level of HSP70 expression relative to control. RESULTS: Short-term (1 hour) venlafaxine treatment significantly increased the level of HSP 70 expression. Simultaneous long-term (72 hours) venlafaxine and dexamethasone treatment significantly reduced the level of HSP70 expression. Dexamethasone treatment administered following long-term (24 and 72 hours) pretreatment with venlafaxine also significantly reduced the level of HSP70 expression. CONCLUSION: Short-term treatment with venlafaxine increases the expression of HSP70, but prolonged treatment with dexamethasone suppresses the venlafaxine-induced expression of HSP70. These findings suggest that HSP70 and dexamethasone play a significant role in the pathophysiology of depression.
Animals ; Cyclohexanols ; Depression ; Dexamethasone ; Glioma ; Heat-Shock Proteins ; HSP70 Heat-Shock Proteins ; Immunohistochemistry ; Rats ; Venlafaxine Hydrochloride

Recent studies have indicated that hyponatremia can be associated with antidepressants, and venlafaxine is a widely used serotonin norepinephrine reuptake inhibitor (SNRI) that has been reported to induce this electrolyte abnormality. A 76-year-old female patient was observed to have hyponatremia after an increase in the dosage of venlafaxine from 37.5 mg to 75 mg a day. Her electrolyte level normalized after the venlafaxine therapy was discontinued, but the abnormality recurred after therapy was resumed. A few case reports of hyponatremia associated with venlafaxine can be found in the literature. While the present case is consistent with previous reports, it is still remarkable due to the rapid development of the hyponatremia, which was 2 days in this patient versus several weeks in the other reported cases. Therefore, special attention is required for the use of venlafaxine, especially in elderly psychiatric patients and patients with a previous brain lesion.
Aged ; Antidepressive Agents ; Brain ; Cyclohexanols ; Female ; Humans ; Hyponatremia ; Norepinephrine ; Serotonin ; Venlafaxine Hydrochloride

Venlafaxine has a dose-dependant effect on blood pressure that is clinically significant at high dose. But the cases of hypertension associated with low dose venlafaxine have been rarely reported. We experienced a case of low dose venlafaxine-induced hypertension in a 53 year-old woman with major depressive disorder who has never been diagnosed as hypertension and other medical diseases. We started venlafaxine administration at a dose of 37.5 mg/day, and on the first day of venlafaxine administration, her blood pressure was abruptly elevated. Regardless of hypertension, venlafaxine was adjusted up to 112.5 mg/day for her depressive symptoms. Hypertension was continued, but not controlled by antihypertensive medication. We thought that she had a venlafaxine-induced hypertension, so we stopped this medication. Elevated blood pressure was normalized 2 days after stopping venlafaxine administration. Her blood pressure has been within normal range without antihypertensive medication for 9 months. So we report this case with the review of the literatures on the venlafaxine-induced hypertension.
Blood Pressure ; Depression ; Depressive Disorder, Major ; Female ; Humans ; Hypertension* ; Middle Aged ; Reference Values ; Venlafaxine Hydrochloride

Venlafaxine is a serotonergic and noradrenergic reuptake inhibitor which is used for the treatment of depression. We report a case of galactorrhea in a patient with major depressive disorder after starting treatment with venlafaxine. In particular, we discuss the course of hyper and normoprolactinemic galactorrhea. We managed this side effect initially by dose reduction and further by switching to essitalopram. Physicians should be aware of endocrinologic side effects such as galactorrhea during the serotonin and noradrenaline reuptake inhibitor treatment.
Depression ; Depressive Disorder, Major ; Female ; Galactorrhea* ; Humans ; Norepinephrine ; Pregnancy ; Prolactin ; Serotonin ; Venlafaxine Hydrochloride*

Authors report a case of hypertension associated with venlafaxine administration. A 52 years-old male patient with bipolar I disorder was hospitalized due to recently developed depressive symptoms. According to his past medical history, he had essential hypertension, which had been well controlled by intermittent antihypertensive therapy. He had no antihypertensive therapy for the last 3 years but maintained normal blood pressure. We started venlafaxine administration for his depressive symptoms and, after 9 days of venlafaxine administration, his blood pressure was abruptly elevated with nausea and headache at a dosage of 112.5mg/day. On 12th hospital day, this medication was adjusted up to 150mg/day. He showed no response to some conventional antihypertensive medications which had been effective for him. We thought that he had a hypertension associated with venlafaxine administration and decided to discontinue this medication. All the symptoms of elevated blood pressure, nausea and headache rapidly improved 4 days after stopping venlafaxine administration. It is necessary to assess blood pressure regularly in patients especially with past history of hypertension who take venlafaxine because of it's potential adverse effect of blood pressure increment. We recommend that dosage reduction or treatment discontinuation should be considered instantly when serious treatment-emergent hypertension with administration of venlafaxine developed.
Blood Pressure ; Depression ; Headache ; Humans ; Hypertension* ; Male ; Middle Aged ; Nausea ; Venlafaxine Hydrochloride