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The effects of omeprazole, SCH 28080 and doxepin were studied on H+/K+-ATPase mediated H+ accumulation in parietal cell membrane vesicles. Omeprazole had no effect on the initial rate of H+ accumulation and the initial steady state concentration of H+; an inhibition was found after the vesicles were acidified. This inhibition was counteracted by the SH reducing agent dithioerythritol. SCH 28080 inhibited the initial rate of H+ accumulation and the steady state H+ concentration. The inhibitory effect of SCH 28080 was counteracted by KCl. Doxepin (3-100 microM) reduced the initial steady state H+ concentration. Doxepin concentrations lower than 0.5 microM had no such effect but dissipated the proton gradient after the vesicles were fully acidified. This doxepin effect was partially counteracted by KCl and was also obtained in vesicles in which the pump reaction was stopped by EDTA. These data show that (i) omeprazole is an acid-activated compound which interferes with SH groups of the H+/K+-ATPase localized inside the vesicles; (ii) SCH 28080 interferes with the K+ site of the H+/K+-ATPase; and (iii) doxepin interacts by a K+ antagonistic activity at the H+/K+-ATPase site and in addition by intravesicular neutralization and/or a protonophoric mechanism with the process of H+ formation.
In the area of Vienna, any person dying under questionable circumstances is examined at the Institute of Forensic Medicine, where the cause of death is determined by means of autopsy and chemical analysis. Our study on fatal intoxications was performed in the period between 1991 and 1997, when selective serotonin reuptake inhibitors (SSRIs) were establishing themselves on the market, reaching the top of prescription statistics. Tricyclic antidepressants (TCAs) were involved in 30 single- and 127 multiple-substance intoxications, with amitriptyline and doxepin being the most frequently used drugs. SSRIs were involved in five multiple-substance intoxications. The f-value, which refers to the number of deaths per million defined daily doses prescribed, was found to be significantly (P=0.001) higher in TCAs than in SSRIs. The f-value for the total group of all antidepressants declined significantly (P=0.05) during the observation period of 7 years. In conclusion, SSRIs turned out to be less toxic than TCAs, and the increasing use of new antidepressants did not coincide with an increased number of deaths caused by these drugs.
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An increased risk of ovarian cancer among users of antidepressants and benzodiazepines has been observed in some but not all prior studies. We examined these associations in a population-based case-control study.
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Histamine is a major neurotransmitter that plays important physiological roles (1, 2). There are four histamine receptor subtypes (H1 to H4) (3). Histamine H3 receptors (H3Rs) are presynaptic autoreceptors that negatively regulate the release of histamine and other neurotransmitters such as norepinephrine, GABA, dopamine, and acetylcholine in the central nervous system (CNS) (4). Consistent with the widespread projection of histaminergic neurons from the lateral hypothalamus, H3Rs are widely distributed in the CNS with high densities in the basal ganglia and are believed to play a variety of physiological roles, including regulation of feeding, arousal, cognition, pain, and endocrine systems (5-7). The H3Rs are also found in a wide variety of peripheral tissues (4). The H3Rs are GTP-binding-protein (G-protein)–coupled receptors that decrease Ca(2+) influx into the cell and inhibit adenylyl cyclase. Positron emission tomography (PET) and single-photon emission tomography of radioligands targeting histamine receptors allow visualization and analysis of histamine receptors in the human brain (8-10). [(11)C]Doxepin was synthesized and developed as a specific PET imaging agent for H1 receptors, showing strong and specific signals in the human brain (11). 3-(1H-Imidazol-4-yl)propyl-4-fluorobenzyl ether (fluoroproxyfan) was found to be a potent and selective H3R antagonist (10). [(18)F]Fluoroproxyfan was synthesized and evaluated as a specific PET imaging tool for H3Rs (12).
Situational in vivo exposure has been widely used in the treatment of agoraphobia. However, only a low to moderate proportion of individuals treated with this approach have shown a high level of therapeutic gain. The recent recognition of panic as central to the development and maintenance of a great many cases of agoraphobic avoidance suggests that treatments focused directly on panic may contribute to a more comprehensive approach to agoraphobia. The present single case demonstrates that whereas two modes of situational exposure produced only limited improvement an approach focused directly on panic had greater effectiveness. The specific effects of the treatment components within the panic control package are analyzed in detail.
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Many researchers have suggested that the glutamatergic system may be involved in the effects of antidepressant therapies. We investigated the effects of doxepin, imipramine, and fluoxetine on the excitatory amino acid transporter type 3 (EAAT3).
We searched the Cochrane Tobacco Addiction Group trials register which includes trials indexed in MEDLINE, EMBASE, SciSearch and PsycINFO, and other reviews and meeting abstracts, in March 2004.
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Molecular study of a cultured cell line.
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A semiautomatic extraction-fluorimetric method for the determination of tricyclic antidepressant drugs (TCAs) based in the formation of ion pairs with 9,10-dimethoxyanthracene-2-sulphonate (DMAS) has been developed. The aqueous solutions of the TCAs (imipramine, desipramine, amitriptyline, nortriptyline, clomipramine or doxepine) are injected into a carrier composed by DMAS in an acid medium and the ion pair formed is extracted into dichloromethane where the fluorescence is measured. An experimental design (Central Composite Design) together with the Response Surface Methodology has been used to find the optimal instrumental FIA and chemical variables. We have considered as the response function the product of the peak height by the sampling frequency. The calibration curves were linear over the working range (0.25-3.00mgL(-1)). The limits of detection were lower than 0.30mgL(-1). The method has been satisfactorily applied to the determination of imipramine, amitriptyline, clomipramine and doxepin in pharmaceutical preparations.
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There was no significant difference between the mean brain H1RO after levocetirizine administration (8.1%; 95% CI: -9.8 to 26.0%) and fexofenadine administration (-8.0%; 95% CI: -26.7 to 10.6%). Similarly, subjective sleepiness was not significantly different between the two antihistamines and placebo. Neither subjective sleepiness nor plasma concentrations was significantly correlated with the brain H1RO of the two antihistamines.
Stability of clonazepam, diazepam, haloperidol, and doxepin was determined in acidic solutions. In addition, determination of the kinetic and thermodynamic properties of this stability was carried out. Reaction rate constants (k), half-life times (t(0.1) and t(0.5)), and activation energy (Ea) were estimated for the drugs, which differed in polarity expressed with log P values. It was observed that estimated Ea values increased from 42.13 to 125.03 kJ/mol with an increase of lipophilicity (log P) beginning from the most hydrophilic drug (clonazepam, 2.70 log P) to the most lipophilic drug (doxepin, 4.10 log P). All degradation products were studied using an HPLC/electrospray ionization-MS technique in the positive ionization mode.
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A new pathophysiologically based classification of itch is proposed, which should help the clinician adopt a rational approach to diagnosis and management of generalized itch. Focusing on neurogenic itch (itch without visible rash), common causes are reviewed and guidelines for laboratory and radiologic investigation are proposed. A stepwise approach to the management of generalized itch resulting from systemic disease is recommended. Specifically, the relative merits of broad versus narrowband ultraviolet B (UVB) are discussed and the pros and cons of doxepin, opioid antagonists, and selective serotonin reuptake inhibitors (SSRIs) such as paroxetine are considered. Attention is drawn to some novel approaches, including bright-light phototherapy and molecular adsorbent recirculating system (MARS) for selected patients with intractable itch caused by hepatic failure, and mirtazapine for nocturnal itch.
Over recent years, the use of antidepressants for the symptomatic treatment of insomnia has grown substantially, but controlled studies are still lacking. Our study is the first investigation to prove objective efficacy and tolerability of low doses of a sedating antidepressant in a randomized, double-blind, and placebo-controlled manner in patients with primary insomnia.
These data substantiate the view that clinically relevant concentrations of neuroleptics and antidepressants can mediate changes in neuronal pHi, which may contribute to their pharmacological mode of action. Effects on pHi should be taken into account when therapeutic or even harmful effects of these drugs are evaluated.
Doxepin is a tricyclic antidepressant formulated as a mixture of E-(trans) and Z-(cis) stereoisomers. Cytochrome P450 2D6 (CYP2D6) catalyzes the hydroxylation of E-doxepin and E-N-desmethyldoxepin stereospecically. There is evidence that tricyclic antidepressants might inhibit CYP2D6 activity but there is no data about the influence of doxepin on CYP2D6.
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Effective migraine treatment is clearly the most cost-effective in terms of both direct and indirect costs. Patient education, behavior changes, and prudent medication selection can minimize costs. Low-dose aspirin may reduce headache frequency. Among the antidepressant medications used, amitriptyine 25 mg, 3 qhs ($4.16/month) and doxepin 25 mg, 3 qhs ($10.50/month) remain the standard. Imipramine (25 mg, 3 qhs ($3.75/month) is very inexpensive and should replace nortriptyline 25 mg, 3 qhs ($64.29/month) as a second-line agent. The specific serotonin reuptake inhibitors are expensive and have no proven effect for migraine prevention. Propranolol 80 mg bid ($7.80/month) is inexpensive and frequently a good choice among beta-blockers. Atenolol 100 mg qd ($27.50/month) is less expensive than long-acting propranolol 160 mg ($35.56/month) and nadolol 120 mg qd ($43.68/month) with equivalent effectiveness. It is thus recommended as the long-acting beta-blocker of choice. Sustained-release preparations of verapamil 240 mg qd ($31.98/month) are twice the cost and less well-absorbed than the standard preparation of 120 mg bid ($17.62/month). Better information is needed concerning effectiveness and optimal dosing of some older low-cost medications in the preventive treatment of migraine.
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Male Wistar rats received acute and four-week intraperitoneal injections of doxepin (3, 5, and 10 mg/kg) or its vehicle (0.9% saline). One hr after the last injection, animals were exposed to a 5 min swim stress session. In other cohorts of animals, the CB1 receptor antagonist AM251 (0.25, 0.5, and 1mg/kg) was injected 30 min before the administration of doxepin. Plasma corticosterone concentration was measured by enzyme-immunoassay at 45 min following stressing. 1, 5, and 12 hr after the last injection of doxepin, the contents of endocacannabinoids (anandamide and 2-arachidonylglycerol) within the lipid extracts of the prefrontal cortex, amygdala, hippocampus, and hypothalamus were determined using isotope-dilution liquid chromatography-mass spectrometry.
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1. The incorporation of 32Pi into 4 phospholipids of rat cortical synaptosomes was altered in the presence of carbachol (1 mM), viz. a decrease of phosphatidylinositol-4,5-bisphosphate and phosphatidyl-4-phosphate by 34 and 21%, and an increase of phosphatidylinositol and phosphatidic acid by 52 and 96% of basal controls respectively. 2. The IC30 values calculated from the dose-response curves for drugs affecting carbachol-induced 32Pi incorporation into these phospholipids, and [3H]QNB binding to the cortical synaptosomes were similar for the typical antimuscarinic agents (i.e. atropine, pirenzepine and trihexyphenidyl), and tricyclic antidepressants (i.e. amitriptyline, doxepin and imipramine) studied. 3. The IC30 values obtained for drugs affecting carbachol-induced 32Pi incorporation into these phospholipids, and high potassium-induced 45Ca2+-uptake by this preparation were similar for neuroselective calcium channel blockers (i.e. cinnarizine and flunarizine) studied. 4. Our results suggest that the neuroactive drugs studied can either act at, or beyond the receptor level, perhaps on the availability of calcium ion, to block carbachol-induced polyphosphoinositide turnover in rat cortical synaptosomes.
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Cases of profound hypoglycemia after the initiation of tricyclic antidepressant therapy in two patients taking sulfonylureas are described. To the authors' knowledge, this is the first report of a potential drug interaction between tricyclic antidepressants and sulfonylureas.
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The anticholinergic activity in serum of depressive patients receiving amitriptyline (50-300 mg/day) or doxepin (50-225 mg/day) was measured using a radioreceptor assay. In this method the membrane suspension prepared from rat brain was able to bind the potent muscarinic antagonist, quinuclidinyl benzilate. Using atropine as a standard, the antimuscarinic activity of several compounds can be measured in the serum of patients receiving drugs with anticholinergic effects or side-effects. The steady state serum levels of amitriptyline and doxepin and their desmethylated metabolites, nortriptyline and desmethyldoxepin were measured by radioimmunoassay in the same serum samples. The antimuscarinic activity in serum measured as atropine equivalents was 2.7 +/- 0.4 (S.E.M.) ng/ml in amitriptyline patients and 1.1 +/- 0.2 ng/ml in doxepin patients. There was a highly significant correlation (P less than 0.001) between amitriptyline (r = 0.92) and nortriptyline (r = 0.79) concentrations and serum antimuscarinic activity. The correlation was less clear, although statistically significant for doxepin (r = 0.42, P less than 0.05) and desmethyldoxepin (r = 0.58, P less than 0.01). The better correlation between serum drug levels and antimuscarinic activity in amitriptyline than in doxepin patients is probably due to the higher affinity of amitriptyline and its desmethylated metabolite to muscarinic receptors with the doses used in the present study. The method may have clinical applications e.g. in evaluation of excessive anticholinergic activity in patients.
Doxepin (1) did not have a robust effect on heart rate, (2) did not adversely affect left ventricular function, (3) did have a significant antiarrhythmic effect, (4) slowed cardiac conduction, and (5) caused a significant increase in orthostatic hypotension. Five (16%) of the 32 patients dropped out due to cardiovascular side effects. The overall dropout rate was 41%.
MEDLINE was searched for English-language papers published from 1953 to 2003, using the key words "tricyclic antidepressants (TCAs)," "amitriptyline," "amoxapine," "clomipramine," "desipramine," "doxepin," "imipramine," "lofepramine," "maprotiline," "nortriptyline," "protriptyline," and "trimipramine." The search was restricted to human studies. To estimate potential exposure to TCAs during pregnancy, data from the outpatient prescription drug database of Saskatchewan, Canada, were analyzed.
According to previous studies reporting the anesthetic/analgesic action of oral topical doxepin administration, this study evaluated a model of buccal permeation to determine the depth of delivery of doxepin into excised porcine buccal mucosa following topical application of a saturated aqueous doxepin solution. Buccal mucosa permeation studies were performed using Franz diffusion cells. Cumulative amounts of doxepin permeated were plotted as a function of time. Kinetic permeation parameters as flux (Js), lag time (Tl) and permeability coefficient (Kp) were calculated. Theoretical human plasmatic steady-state doxepin concentration and drug retained in the tissue were also determined in order to evaluate its potential therapeutic use, central or peripheral. Finally, a histological evaluation of the buccal mucosa was performed to test potential damage due to the permeation phenomenon. Obtained results showed a poor aqueous doxepin permeation through buccal mucosa membrane (median parameters Js=34.79 μg/h, Kp=0.49×10(-3)cm/h and Tl=2.8h). Predicted doxepin plasma concentrations would reach 46 ng/mL, far from the required to have central nervous system activity as tricyclic agent. However, median doxepin amount remaining in the mucosa membrane was 0.24 μg/cm(2)/μg tissue, which evidenced a reservoir function of the buccal mucosa. Histologically, no structural damage was observed in the tissues. This study lays the foundation for further research within this area with a view to potentially adopting alternative strategies for enhanced buccal absorption of doxepin in clinical practice.
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Two review authors independently performed study selection, data collection and risk of bias assessments.
In a randomized, double-blind safety and efficacy study, 50 patients with chronic pruritus were given either doxepin 10 mg/d or hydroxyzine 25 mg/d for 4 weeks. Pruritic score was calculated for each patient before treatment and 1 month after.
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This ongoing column is dedicated to the challenging clinical interface between psychiatry and primary care-two fields that are inexorably linked.Pain, including neuropathic pain, is a relatively common complaint in various clinical settings. Several antidepressants have been efficacious in the management of chronic neuropathic pain, including the tricyclic antidepressants (particularly the tertiary-amine subtypes, such as amitriptyline, doxepin, and imipramine) as well as venlafaxine, bupropion, and duloxetine. The selective serotonin reuptake inhibitors have either been less robust (paroxetine, citalopram) or lacked any efficacy at all (fluoxetine). In this article, we review these various medications and offer an interpretive comparison, as there are few head-to-head comparison studies.
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In a double-blind study on 40 outpatients (20 per group) suffering from endogenous and psychogenic depression of the anxious-agitated or inhibited form, trazodone was compared with doxepin to determine their efficacy and safety, and whether a single daily administration was adequate. Increasing doses of trazodone 50-200 mg and doxepin 25-100 mg were given once a day in the evening for a period of 5 weeks. Both drugs were found to be approximately equivalent as far as their antidepressive and anxiolytic effects and safety are concerned. Treatment with trazodone promises less risks according to the clinical experience described in the international literature. Administration once a day provides sufficient efficacy and safety.
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Carbon-11 labeled metabolites in human plasma were analyzed by high-performance liquid chromatography during positron emission tomography (PET) studies using the dopamine D2 ligand [11C]YM-09151-2 as well as the histamine H1 ligands [11C]doxepin and [11C]pyrilamine. For all the three tracers, blood clearance of the radioactivity was extremely rapid after an i.v. injection. The plasma protein-binding of [11C]YM-09151-2 and [11C]doxepin had protective effects upon the metabolic alteration of the ligands, whereas [11C]pyrilamine was free from the protein-binding and immediately degraded. The degradation of [11C]doxepin was more rapid in epileptic patients on medication than in normal subjects. These results indicate that analysis of metabolites in the plasma is necessary to determine the accurate arterial input function for quantitative PET measurement.