SERTRALINE

This study explored microdosing methods for evaluating the distribution and pharmacokinetics (PK) of a central nervous system (CNS) drug candidate. We used sertraline as a model drug. In this open-label, one-arm, three-period, multiple-dosing study, 10 healthy male volunteers received 6-day administrations of sertraline at doses of 5, 25 or 50 mg/d in three different periods. Before the first dose of Period 1, and 24 h after the last dose of each period, an intravenous bolus of [11C]sertraline was injected for positron emission tomography (PET) scanning. After the sixth dose in each period, serial blood samples were collected at scheduled intervals over 48 h; then serum sertraline concentrations were determined with liquid chromatography-tandem mass spectrometry (LC-MS/MS). Sertraline was distributed in the brain within 20 min, and it was highly distributed in the putamen, cingulate, and thalamus. Linearity in steady-state Cmax and AUClast were observed in the 5 - 50 mg dose range. ...

Increasing multiple drug resistance of microorganisms to certain antibiotics is a major health problem of the current clinical practice. Therefore, development of novel broad
range antimicrobial agents and increasing efficiency of existing antibiotics are under great interest among scientists. Some psychotropic drugs not only reverse microbial antibiotic
resistance but also exhibit direct antimicrobial activity against several biological targets. In the present study, 16 different psychotropic drugs including sertraline, paroxetine,
aripiprazole, fluvoxamine, moclobemide, venlafaxine, mianserin, trazodone, mirtazapine, clomipramine,
alprazolam, escitalopram, citaloprame, fluoxetine, gabapentin and reboxetine have been examined for their antimicrobial properties against wide range of bacteria, yeast and fungi using disc-diffusion and micro-well dilution assays. The results revealed that except FOR gabapentin, venlafaxine, moclobemide and alprazolam,  the remaining drugs tested in this study showed various antimicrobial activities. Selective serotonin reuptake inhibitor group drugs including sertraline, paroxetine, fluvoxamine and fluoxetine displayed broad range
antibacterial activity compared to other psychotropic drugs. Among them, sertraline was also found to be effective against Candida albicans and Aspergillus niger. Exploring antimicrobial activities will increase the use and application of these psychotropic drugs in clinical approaches. However, in vivo studies and clinical trials are strictly required to evaluate efficiencies of these chemicals for the treatment of systemic microbial infections.

Recurrent unexpected syncope may have severe consequences and result in serious injury. This is especially the case in the immediate postpartum period when maternal syncope may have a disastrous effect on the infant as well as the mother. We report on 12 women who developed episodic hypotension resulting in syncope in the immediate postpartum period and describe the distinguishing characteristics of their presentation, tilt table results, and responses to therapy. Postpartum syncope represents a unique subgroup of syncopal patients who need to be recognized and treated in order to prevent potentially serious injury to both mother and infant.

Major depressive disorder is a highly prevalent and debilitating condition in youth, so developing efficient treatments is a priority for mental health professionals. Psychotherapy (i.e., cognitive behavioral therapy/CBT), pharmacotherapy (i.e., SSRI medication), and their combination have been shown to be effective in treating youth depression; however, the results are still mixed and there are few studies engaging multi-level analyses (i.e., subjective, cognitive, and biological). Therefore, the aims of this randomized control study (RCT) were both theoretical - integrating psychological and biological markers of depression in a multi-level outcome analysis - and practical - testing the generalizability of previous results on depressed Romanian youth population. Eighty-eight (N=88) depressed Romanian youths were randomly allocated to one of the three treatment arms: group Rational Emotive Behavior Therapy (REBT)/CBT (i.e., a form of CBT), pharmacotherapy (i.e., sertraline), and gr...

CUSP9 treatment protocol for recurrent glioblastoma was published one year ago. We now present a slight modification, designated CUSP9*. CUSP9* drugs--aprepitant, artesunate, auranofin, captopril, celecoxib, disulfiram, itraconazole, sertraline, ritonavir, are all widely approved by regulatory authorities, marketed for non-cancer indications. Each drug inhibits one or more important growth-enhancing pathways used by glioblastoma. By blocking survival paths, the aim is to render temozolomide, the current standard cytotoxic drug used in primary glioblastoma treatment, more effective. Although esthetically unpleasing to use so many drugs at once, the closely similar drugs of the original CUSP9 used together have been well-tolerated when given on a compassionate-use basis in the cases that have come to our attention so far. We expect similarly good tolerability for CUSP9*. The combined action of this suite of drugs blocks signaling at, or the activity of, AKT phosphorylation, aldehyde d...

To describe a case of a 65-year-old woman with persistent olfactory hallucination and delusional self-reference, successfully treated by aripiprazole augmentation of antidepressant therapy. Olfactory reference syndrome is a nosologic entity, which has been assimilated to various Diagnostic and Statistical Manual of Mental Disorder-IV-text revision codified diseases and several pharmacologic treatments have been proposed without a constant clinical response. Psychiatric, neurologic, neuropsychologic, imaging, and electroencephalogram data are reported. The patient showed a significant improvement with aripiprazole. We propose a pathophysiologic model of olfactory reference syndrome to explain the good response of our patient to aripiprazole. We hypothesize a disruption in the top-down regulation of the orbitofrontal cortex on the primary olfactory cortex and the olfactory bulb at the basis of the illness. Aripiprazole acting as a partial agonist of dopamine D2 receptors in the olfactory bulb compensates for the lack of modulation in this site, restoring the correct processing of olfactory information.

The determination of the new antidepressant drug sertraline and its main metabolite, desmethylsertraline, in human serum is described. A new solid-phase extraction method employing the dual functionality Clean Screen cartridge is presented followed by reversed-phase liquid chromatographic (LC) analysis. The sample preparation yielded extremely clean extracts and absolute recoveries in excess of 90% for both drugs from human serum. The response of the LC system was linear over the concentration range 0.01-2.5 mg/l for both sertraline and desmethylsertraline with a limit of detection of 0.01 mg/l. A gas chromatographic-mass spectrometric (GC-MS) system is also described should confirmation of the drugs be necessary.