OBJECTIVETo synthesize venlafaxine with an improved novel method.

METHODSp-methoxypheny lethyl-acid was reacted with SOCl(2) to produce acyl chloride which was reacted with N,N-dimethylamine solution to get amide; then through Ivanov reaction and reduction by KBH(4)/BF(3).Et(2)O to yield venlafaxine.

RESULTVenlafaxine was successfully synthesized by using this method with an yield rate of 50.3%.

CONCLUSIONThe improved method is suitable for industrial production of venlafaxine.

Antidepressive Agents, Second-Generation ; chemical synthesis ; Cyclohexanols ; chemical synthesis ; Venlafaxine Hydrochloride

Acute Disease ; Antidepressive Agents, Second-Generation ; adverse effects ; Glaucoma, Angle-Closure ; chemically induced ; Humans ; Intraocular Pressure ; Venlafaxine Hydrochloride ; adverse effects

The aging process makes the changes of pharmacokinetics and pharmacodynamics of psychotropic drugs. The author discussed the biological treatment of geriatric mood disorders in this review. In the acute treatment of geriatric mood disorder, there are some different considerations about the biological treatment, such as the poor physical health, the high suicidal risk, the impaired judgment and reality testing, the likelihood of poor compliance, the impaired cognitive functioning, and the lack of social supports. Psychiatrists who prescribe for the mood disorder of the elderly must bear in mind the risks and benifits of pharmacotherpy in a view of pharmacokinetic and pharmacodynamics. The author reviewed the properties and cautions of the classical antidepressant TCAs and newer atypical antidepressants, such as trazodone and venlafaxine. And also the author reviewed the special situations in geriatric mood disorders, which are the delusional depression, the treatment-resistent depression, and the neuropsychiatric disorder.
Aged ; Aging ; Antidepressive Agents, Second-Generation ; Compliance ; Delusions ; Depression ; Humans ; Judgment ; Mood Disorders* ; Pharmacokinetics ; Psychiatry ; Psychotropic Drugs ; Reality Testing ; Trazodone ; Venlafaxine Hydrochloride

The aging process makes the changes of pharmacokinetics and pharmacodynamics of psychotropic drugs. The author discussed the biological treatment of geriatric mood disorders in this review. In the acute treatment of geriatric mood disorder, there are some different considerations about the biological treatment, such as the poor physical health, the high suicidal risk, the impaired judgment and reality testing, the likelihood of poor compliance, the impaired cognitive functioning, and the lack of social supports. Psychiatrists who prescribe for the mood disorder of the elderly must bear in mind the risks and benifits of pharmacotherpy in a view of pharmacokinetic and pharmacodynamics. The author reviewed the properties and cautions of the classical antidepressant TCAs and newer atypical antidepressants, such as trazodone and venlafaxine. And also the author reviewed the special situations in geriatric mood disorders, which are the delusional depression, the treatment-resistent depression, and the neuropsychiatric disorder.
Aged ; Aging ; Antidepressive Agents, Second-Generation ; Compliance ; Delusions ; Depression ; Humans ; Judgment ; Mood Disorders* ; Pharmacokinetics ; Psychiatry ; Psychotropic Drugs ; Reality Testing ; Trazodone ; Venlafaxine Hydrochloride

OBJECTIVETo compare the effect of electro-acupuncture (EA) and maprotiline (Map) in treating depression.

METHODSThirty patients of depression were treated with EA and 31 patients with Map orally taken respectively. The therapeutic effect and side-effect were evaluated by measurement of Hamilton Depression Rating Scale (HAMD), Self-Rating Scale for Depression (SDS), Self-Rating Scale for Anxiety (SAS), Clinical Global Impression Scale (CGI) and Asberg Rating Scale for side-effects (ARS) before treatment and on the day 14, 28 and 42 of the therapeutic course.

RESULTSAfter treatment, the scores of HAMD and SDS lowered significantly (P < 0.01) than before treatment, and with insignificant difference between the group (P > 0.05). For patients with somatic syndrome, the HAMD score decrease rate was obviously higher in the Map group than that in the EA group. However, for the patients with anxiety somatization syndrome, the score of SAS, ARS in the EA group were significantly lower than those in the Map group (P < 0.05). Moreover, the efficacy index was higher in the EA group (P < 0.01).

CONCLUSIONBoth EA and Map are effective in treating depression.

Acupuncture Therapy ; Adolescent ; Adult ; Antidepressive Agents, Second-Generation ; therapeutic use ; Depression ; therapy ; Electroacupuncture ; Female ; Humans ; Male ; Maprotiline ; therapeutic use ; Middle Aged

OBJECTIVETo study on clinical therapeutic effect and safety of electroacupuncture and Fluoxetine for treatment of mild or moderate depression with physical symptoms.

METHODSSeventy-five cases were randomly divided into a western medicine group (group A), an electroacupunctue group(group B) and an electroacupuncture plus medicine group (group C), 25 cases in each group. The group A were treated by oral Fluoxetine, 20 mg each day; the group B by electroacupuncture with Baihui (GV 20) and Yintang (EX-HN 3) selected as main points; the group C by oral administration of Fluoxetine plus electroacupunctue. HAMD depression scale was used for assessment of clinical therapeutic effect and TESS adverse reaction scale was used for adverse reactions.

RESULTSThe clinical effective rate was 78.3% in the group A, 82.6% in the group B and 91.7% in the group C, with significant differences between group C and A, group C and B (P < 0.05). Groups B and C had significant therapeutic effects in improvement of physical symptoms, and the adverse reaction of Fluoxetine in the group C was less than that in the group A.

CONCLUSIONElectroacupuncture can significantly improve physical symptoms and relieve adverse reactions of Fluoxetine. Electroacupuncture combined with Fluoxetine has a better therapeutic effect on depression with mild or moderate physical symptoms, with less adverse reactions.

Adult ; Antidepressive Agents, Second-Generation ; therapeutic use ; Combined Modality Therapy ; Depression ; therapy ; Electroacupuncture ; Female ; Fluoxetine ; therapeutic use ; Humans ; Male ; Middle Aged

OBJECTIVETo establish an liquid chromatography-mass spectrometry (HPLC-MS/MS)-based method for determining escitalopram in human plasma.

METHODSA liquid-liquid ether extraction approach was adopted using dextromethorphan as the internal standard. The Agilent ZORBAX SB-C18 (3.5 microm,2.1 x 150 mm) was used as the analytical column with acetonitrile-NH4AC buffer (70:30, V/V) as the mobile phase at the flow rate of 0.3 ml/min. The sample was ionized by electrospray ionization source in the triple quadruple tandem mass spectrometer, and the plasma escitalopram determined with a multiple reaction monitoring mode of m/z325.4-->109.4.

RESULTSThe linear range was 0.0866-64.13 microg/L (r=0.9965) for escitalopram in human plasma, with the absolute recovery between 64.98% and 78.72% and the within-day and between-day deviations less than 10%.

CONCLUSIONThe method is sensitive, accurate, rapid, specific and well applicable for clinical pharmacokinetics study of escitalopram.

Antidepressive Agents, Second-Generation ; blood ; pharmacokinetics ; Chromatography, High Pressure Liquid ; methods ; Citalopram ; blood ; pharmacokinetics ; Humans ; Sensitivity and Specificity ; Tandem Mass Spectrometry ; methods

OBJECTIVETo investigate the clinical efficacy, adverse reaction and safety of Jieyu pill (JYP) in treating depression.

METHODSThe randomized controlled trial was conducted in 28 patients in the treated group and 29 patients in the control group treated with maprotiline (Map). The efficacy of treatment was evaluated before treatment and 14, 28 and 42 days after treatment, with Hamilton depression rating scale (HAMD), self-rating scale for depression (SDS), self-rating scale for anxiety (SAS) and clinical global impression (CGI), the adverse reaction was assessed by Asberg Rating Scale (ARS).

RESULTSJYP was effective in treating depression, the markedly effective rate being 78.8%, corresponded to that of Map (82.8%, P > 0.05). After treatment, the scores assessed by HAMD, SDS and SAS were all lower than those before treatment (P < 0.01) respectively, but comparison between the two groups showed insignificant difference (P > 0.05). However, scores of ARS were significantly lower in the treated group than that in the control group, and the efficacy index of JYP was significantly higher than that of Map (P < 0.01).

CONCLUSIONJYP in treating depression shows the efficacy corresponded to that of Map and with less adverse reaction.

Adolescent ; Adult ; Aged ; Antidepressive Agents ; therapeutic use ; Antidepressive Agents, Second-Generation ; therapeutic use ; Depressive Disorder ; drug therapy ; Drug Therapy, Combination ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Humans ; Male ; Maprotiline ; therapeutic use ; Middle Aged ; Phytotherapy ; Psychiatric Status Rating Scales

The most common cardiovascular side effects of antidepressants are cardiac arrhythmias and orthostatic hypotension. Little is known, however, about the mechanisms by which these adverse reactions may occur, especially with regard to newer drugs such as fluoxetine. We hypothesized that these side effects may have an electrophysiological basis at the level of the cardiac myocyte. Thus, we investigated the effects of fluoxetine and other antidepressants on action potentials and ionic currents of rat ventricular myocytes using the amphotericin B perforated patch clamp technique. Fluoxetine (10 microM) prolonged the action potential duration (APD50) to 146.7 +/- 12.9% of control value without altering resting membrane potential. Fluoxetine and sertraline potently inhibited the L-type Ca2+ current (IC50 = 2.82 and 2.31 microM, respectively), but did not significantly modify the steady-state inactivation. Amitriptyline and imipramine had similar, but slightly weaker, effects (IC50 = 3.75 and 4.05 microM, respectively). Fluoxetine attenuated the peak transient outward K+ current and also altered current kinetics, as shown by accelerated decay. Fluoxetine did not change the voltage-dependence of the steady-state inactivation. Sertraline, amitriptyline and imipramine inhibited the transient outward K+ current with potencies very similar to fluoxetine. In contrast to the other antidepressants tested, trazodone weakly inhibited the Ca2+ and K+ currents and moclobemide had no detectable effect. Our comparative pharmacology data suggest that selective serotonin reuptake inhibitors, such as fluoxetine, are as potent as tricyclic antidepressants in inhibiting L-type Ca2+ and transient outward K+ currents. These inhibitory effects may contribute to cardiovascular complications such as arrhythmias and orthostatic hypotension.
Animal ; Antidepressive Agents, Second-Generation/pharmacology* ; Calcium Channels/drug effects* ; Calcium Channels, L-Type ; Electric Conductivity ; Fluoxetine/pharmacology* ; Male ; Myocardium/metabolism* ; Myocardium/cytology ; Potassium/physiology* ; Rats ; Rats, Sprague-Dawley ; Ventricular Function/physiology*

OBJECTIVETo explore the efficacy of jieyu granule (JG) combined Paroxetine in treating refractory depression (RD) patients of yin deficiency inner heat syndrome (YDIHS).

METHODSSeventy RD patients of YDIHS were randomly assigned to the experimental group (JG combined Paroxetine) and the control group (Chinese medical placebo combined Paroxetine), 35 cases in each group. Hamilt Depression Rating Scale and Hamilton Anxiety Scale were used before treatment, and at the weekend of the 2nd, 4th, and 8th week, respectively.

RESULTSIn the experimental group, 32 patients completed the trial and 3 patients dropped out. In the control group, 33 patients completed the trial and 2 patients dropped out. At the end of the 8th week of the treatment, the total score of Hamilt Depression Rating Scale was (14.75 +/- 7.85) in the experimental group, lower than that of the control group (19. 06 +/- 8. 31, P <0.05). At the end of the 2nd, 4th, and 8th week of the treatment, the score of Hamilton Anxiety Scale was 17.03 +/- 4.25, 14.50 +/- 5. 13, and 11.03 +/- 4.88, respectively in the experimental group, lower than that of the control group at each corresponding time point (19. 60 +/-3. 96, 17. 12 +/- 4.14, 14.64 +/- 4.47, P <0.05, P <0.01).

CONCLUSIONThe efficacy of JG combined Paroxetine for treating RD patients of YDIHS was superior to that of using Paroxetine alone.

Adult ; Antidepressive Agents, Second-Generation ; therapeutic use ; Depressive Disorder, Treatment-Resistant ; diagnosis ; drug therapy ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Humans ; Male ; Middle Aged ; Paroxetine ; therapeutic use ; Phytotherapy ; Treatment Outcome ; Yin Deficiency ; diagnosis ; drug therapy