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PubMed2001

Sertraline, paroxetine, and venlafaxine in refugee posttraumatic stress disorder with depression symptoms.

Three new antidepressants were used in treating posttraumatic stress disorder (PTSD) and symptoms of depression in Bosnian refugees. Thirty-two Bosnian refugees seeking treatment at a mental health clinic participated in a case series study. All received open trials of Sertraline (n = 15), Paroxetine (n = 12), or Venlafaxine (n = 5), with standard clinical doses. Overall, Sertraline and Paroxetine produced statistically significant improvement at 6 weeks in PTSD symptom severity in depression, and in Global Assessment of Functioning. Venlafaxine produced improvement in PTSD symptom severity and in Global Assessment of Functioning, did not yield improvement in symptoms of major depressive disorder; and had a high rate of side effects. Notwithstanding improvement of symptoms, all 32 refugees remained PTSD positive at the diagnostic level at the 6-week follow-up.

Adult↗
PubMed2002

Can improvement in well-being and functioning be distinguished from depression improvement in antidepressant clinical trials?

The Inventory of General Life Functioning (GLF), a self-evaluation scale for patients, was developed for use in the National Institute of Mental Health Treatment of Depression Collaborative Research Program. The scale was designed to evaluate patient general well-being and functioning, areas not adequately covered by standard depression scales. We used the patient self-report version of the GLF in two imipramine-controlled clinical trials during the development of the antidepressant venlafaxine. In these double-blind studies, outpatients with depression received placebo (n = 158), venlafaxine (n = 152), or imipramine (n = 149) for up to 6 weeks. We examined the internal consistency and factor structure of the GLF, its correlation with standard depression rating scales, and its sensitivity to differential treatment effects. We found the scale to be internally consistent and moderately correlated with physician-rated measures of depression. A reported two-factor structure (general well-being and functioning) was evaluated by factor analysis. When analyses were restricted to patients who completed at least 4 weeks on therapy, the GLF displayed sensitivity to differential treatment effects. The GLF total and factor subscales demonstrated the superiority of an active therapy (venlafaxine) to placebo; the GLF factor and a 7-item subscale using only items derived from Dupuy's psychological general well-being index (PGWB) demonstrated an advantage for one active therapy (venlafaxine) over another (imipramine). The GLF is a useful complement to the standard depression rating scales because it may assess additional dimensions of the depressive syndrome.

Activities of Daily Living↗
PubMed2002

Long-term side effects of newer-generation antidepressants: SSRIS, venlafaxine, nefazodone, bupropion, and mirtazapine.

Anecdotal reports have suggested that the long-term use of selective serotonin reuptake inhibitors (SSRIs) may be associated with significant weight gain, sexual dysfunction, drug interactions, and discontinuation symptoms. Are these effects inevitable or can they be managed effectively with the appropriate interventions? In reviewing published, controlled clinical trials, it has been noted that many depressed patients experience weight gain during remission with or without treatment. Most antidepressants appear to produce a 3- to 4-kg weight gain after 6-12 months of therapy, which may be managed with nutritional counseling and exercise. The exception is mirtazapine, which appears to be associated with significant weight gain early in therapy. Antidepressant-induced sexual dysfunction is also common but may be managed with the addition of an antidote or substitution. Drug interactions are most common with fluvoxamine, nefazodone, and fluoxetine because these agents are more likely to affect the metabolism of commonly prescribed medications. It may be possible to prevent discontinuation symptoms with a cross taper to another antidepressant or by slowly tapering the antidepressant.

Antidepressive Agents, Second-Generation↗
PubMed2003

Differential metabolism of 1,8-cineole in insects.

In order to compare the metabolism of 1,8-cineole in the pyrgo beetle, Paropsisterna tigrina, three other herbivorous insect species, Faex nigroconspersa, Chrysophtharta bimaculata, and Oxyops vitiosa, were fed 1,8-cineole leaf diets. F. nigroconspersa adults excreted predominantly 9-hydroxy-1,8-cineole (36.2% of the volatile constituents) with some 2alpha-hydroxy-1,8-cineole (11.4%). In contrast, larvae excreted predominantly 2alpha-hydroxy-1,8-cineole (27.4%) and smaller proportions of 9-hydroxy-1,8-cineole (5.2%) and 3alpha-hydroxy-1,8-cineole (4.3%). C. bimaculata adults excreted predominantly 3alpha-hydroxy-1,8-cineole (16.5%). Oxyops vitiosa adults, on a lower 1,8-cineole diet, excreted predominantly 2alpha,9-dihydroxy-1,8-cineole (4.2%) and 2alpha-hydroxy-1,8-cineole (3.5%), with smaller proportions of 3alpha-hydroxy-1,8-cineole (1.1%) and 9-hydroxy-1,8-cineole (0.5%). This is the first reported occurrence of a dihydroxycineole as an insect metabolite. Gas chromatographic and mass spectral data for hydroxycineoles are recorded and interspecific metabolite variation discussed.

Animals↗
PubMed1997

Nonclassical and endogenous cannabinoids: effects on the ordering of brain membranes.

The effects of several nonclassical cannabinoids and the endogenous cannabinoid ligand, anandamide on the lipid ordering of rat brain synaptic plasma membranes (SPM) were examined and compared to delta 9-tetrahydrocannabinol (delta 9-THC). SPM order was determined using fluorescence polarization. All compounds tested affected membrane ordering. delta 9-THC, CP-55,940, CP-55,244 and WIN-55212 decreased lipid ordering in SPM. Some stereospecificity was observed with delta 9-THC and WIN-55212, but not other compounds. Anandamide also decreased lipid order as did its putative precursor, arachidonic acid. In contrast to these compounds, levonantradol increased SPM lipid order. Although all pharmacologically active cannabinoids affect SPM lipid order, potency on this measure does not correlate well with their pharmacological potency. The results of this study suggest that membrane perturbation (either increases or decreases in lipid order) may be a necessary characteristic for cannabinoid pharmacological activity, but it is not a primary or sufficient determinate of action for this class of drugs.

Analgesics↗
PubMed2003

Effects of two plant secondary metabolites, cineole and gallic acid, on nightly feeding patterns of the common brushtail possum.

We investigated effects of two plant secondary metabolites (PSMs), cineole and gallic acid, on the nightly feeding behavior of the common brushtail possum (Trichosurus vulpecula), a generalist folivore. We tested whether possums altered their feeding behavior in response to increasing levels of cineole, a dietary terpene. Possums were fed artificial diets containing three levels of cineole: zero (basal diet), medium (6.8% of total dry matter, DM), and high (15.3% DM). In another experiment, we introduced gallic acid, a dietary phenolic, into the diets. Possums were offered a Choice PSM diet (cineole and gallic acid diets simultaneously) or a No-Choice PSM diet (containing either cineole or gallic acid). Detoxification products of cineole and gallic acid were examined in urine to determine that different detoxification pathways were utilized in the elimination of each compound. With increasing cineole levels, possums ate less, had smaller feeding bouts, and had a lower rate of intake, but did not extend their total nightly feeding time. Possums offered the Choice PSM diet, compared with the No-Choice diets, ate more, had larger feeding bouts, and tended to increase their rate of intake. Results from the urinary analysis indicated that gallic acid and cineole were not involved in competing detoxification pathways in brushtail possums. There was also a significant sex effect: females ate more overall, ate more per feeding bout, and ate at a higher rate than males. These results indicate that PSMs not only constrain overall intake, but that possums alter their feeding behavior in response to them. Altered feeding patterns may reduce the negative influence of PSMs on intake.

Animals↗
PubMed1997

Once-daily venlafaxine extended release (XR) and venlafaxine immediate release (IR) in outpatients with major depression. Venlafaxine XR 208 Study Group.

This was a randomized, double-blind, placebo-controlled comparison of the efficacy and safety of once-daily venlafaxine extended release (XR) and venlafaxine immediate release (IR). Outpatients with DSM-III-R major depression were randomly assigned to venlafaxine XR, 75 mg once daily, venlafaxine IR, 37.5 mg twice daily, or placebo for a maximum of 12 weeks. If the response was inadequate after 2 weeks of treatment, the dosage of venlafaxine XR or IR could be increased to 150 mg daily. The primary efficacy variables were the 21-item Hamilton Depression (HAM-D) Rating Scale total score and depressed mood item, the Montgomery-Asberg Rating Scale (MADRS) total scores, and the Clinical Global Impressions (CGI) severity scale. Two hundred seventy-eight patients were evaluated for efficacy. Venlafaxine XR was significantly superior (p < 0.05) to placebo beginning at week 2 for the HAM-D, week 3 for the MADRS, and week 4 for the CGI severity. Similarly, venlafaxine IR was significantly superior (p < 0.05) to placebo beginning at week 2 on the HAM-D total and depressed mood item, week 3 on the MADRS total, and week 6 on the CGI severity scales. Venlafaxine XR exhibited superiority (p < 0.05) over venlafaxine IR at week 12 for all efficacy variables. The most common treatment-emergent adverse event with venlafaxine XR was nausea. The incidence of nausea was highest during the first 2 weeks with a low likelihood of developing nausea thereafter. The results of this study indicate that venlafaxine XR is safe, effective, and well tolerated for the treatment of major depression at once-daily doses ranging from 75 to 150 mg.

Adolescent↗
PubMed1997

Binding of aminoalkylindoles to noncannabinoid binding sites in NG108-15 cells.

1. Aminoalkylindoles, typified by WIN 55212-2, bind to G protein-coupled cannabinoid receptors in brain. Although cannabinoids inhibit adenylyl cyclase in NG108-15 neuroblastoma x glioma hybrid cells, cannabinoid receptor binding in these cells has not been described previously. This study compares pharmacological characteristics of [3H]WIN 55212-2 binding sites in rat cerebellar membranes and in NG108-15 membranes. 2. Although the KD of specified [3H]WIN 55212-2 binding was similar in brain and NG108-15 membranes, the Bmax was 10 times lower in NG108-15 than in cerebellar membranes. In both brain and NG108-15 membranes, aminoalkylindole analogues were relatively potent in displacing [3H]WIN 55212-2 binding. However, IC50 values for more traditional cannabinoids were significantly higher in NG108-15 membranes than in brain, e.g., the Ki values for CP55,940 were 1.2 nM in brain and > 5000nM in NG108-15 membranes. Moreover, sodium and GTP-gamma-S decreased [3H]WIN 55212-2 binding in brain but not in NG108-15 membranes. 3. These data suggest that WIN 55212-2 does not label traditional cannabinoid receptors in NG108-15 cells and that these novel aminoalkylindole binding sites are not coupled to G proteins.

Analgesics↗
PubMed2004

Constraint of feeding by chronic ingestion of 1,8-cineole in the brushtail possum (Trichosurus vulpecula).

Eucalyptus leaf-eating marsupials such as the brushtail possum (Trichosurus vulpecula) ingest large amounts of terpenes, especially 1,8-cineole (cineole)--the major component of many eucalyptus oils. Brushtail possums were acclimated to a non-Eucalyptus diet with increasing concentrations of cineole (0.5-4.0% wet weight) added over 18 d. We measured food and cineole consumption and urinary metabolites of cineole. Food intake decreased with cineole content, indicating that it was constrained by the maximum tolerable intake of cineole that was 3.8 +/- 0.2 g kg(-1) or 5.2 +/- 0.3 g kg(-0.75) (mean +/- SE, N = 6). The pattern of metabolites was similar at all cineole intakes (56% hydroxycineolic acids, 27% cineolic acids, 13% hydroxycineoles, and 4% dihydroxycineoles). In another experiment, possums maintained on artificial diet were abruptly presented with 4% cineole for 5 d. Food intake fell by 45 +/- 6% (mean +/- SE, N = 6) and mean cineole intake was 2.9 +/- 0.3 g kg(-1). There was evidence of induction of secondary oxidative pathways, as hydroxycineoles were the major metabolites (48% total) on the first day, but rapidly dropped to 15% on subsequent days as the acid metabolites increased. These findings indicate that ingestion of cineole is not constrained by selective saturation of individual enzymes involved in its multiple pathways of oxidation, but rather the total detoxification capacity appears to limit feeding on a cineole diet.

Animals↗
PubMed2004

Conduritols as oviposition stimulants for the danaid butterfly, Parantica sita, identified from a host plant, Marsdenia tomentosa.

Host-plant chemicals responsible for egg-laying by the chestnut tiger butterfly, Parantica sita, were identified from one of its hosts, Marsdenia tomentosa. Ovipositing females responded positively to a methanolic extract of the plant. Solvent partitioning of the extract and oviposition bioassays indicated that the active principle resided in the aqueous fraction. Further activity-directed fractionation of the water-soluble constituents by various forms of column chromatography led to the isolation of several saturated and unsaturated cyclitols together with their glycosides. Of these, conduritol A, a predominant cyclitol present in the plant, moderately stimulated oviposition, while conduritol F 2-O-glucoside, although present in a very small amount, evoked a stronger response from females than conduritol A when tested at the same dose. In contrast, its aglycone, conduritol F, which was also a trace component, was almost inactive by itself. However, the oviposition-stimulatory activity of conduritol A was significantly enhanced when tested in combination with a small quantity of conduritol F. Addition of a small quantity of conduritol F 2-O-glucoside to conduritol A resulted in a substantial elevation in female responses. Consequently, the synergistic action of a large amount of conduritol A and small amounts of co-occurring conduritol F and its glucoside can account for the stimulation of egg-laying by P. sita on M. tomentosa.

Animals↗
PubMed2004

Inhibition by anandamide and synthetic cannabimimetics of the release of [3H]D-aspartate and [3H]GABA from synaptosomes isolated from the rat hippocampus.

Cannabinoids (CB) can act as retrograde synaptic mediators of depolarization-induced suppression of inhibition or excitation in hippocampus. This mechanism may underlie the impairment of some cognitive processes produced by these compounds, including short-term memory formation in the hippocampus. In this study, we investigated several compounds known to interact with CB receptors, evaluating their effects on K(+)-evoked release of [3H]D-aspartate ([3H]D-ASP) and [3H]GABA from superfused synaptosomes isolated from the rat hippocampus. [3H]D-ASP and [3H]GABA release were inhibited to different degrees by the synthetic cannabinoids WIN 55,212-2; CP 55,940, and arachidonyl-2'-chloroethylamide/N-(2-chloroethyl)-5Z,8Z,11Z,14Z-eicosatetraenamide (ACEA), as well as by the endocannabinoids, anandamide (AEA), and 2-arachidonoylglycerol (2-AG). Both types of release were also inhibited by capsaicin. The inhibition produced by each of the cannabinoid compounds and capsaicin was unaffected by capsazepine or by the CB1-receptor antagonists AM-251 and SR141716A. The mechanism underlying AEA- and synthetic CB-induced inhibition of the release of [3H]GABA and [3H]D-ASP from rat hippocampal synaptosomes might not involve activation of presynaptic CB1 receptors.

Animals↗
PubMed2003

[Pharmacotherapy of generalized anxiety disorder: state of the art].

A large percentage of patients in primary care suffer from Generalized Anxiety Disorder (GAD). A task force of the Swiss GAD Society has reviewed the scientific literature and has developed treatment recommendations. Basic treatment, adjunctive treatment and therapy of specific problems like insomnia and comorbidities are differentiated. Newer antidepressants are recommended as basic treatment, especially venlafaxine and paroxetine, which are licensed for that indication.

Adolescent↗
PubMed2002

Achieving remission from depression with venlafaxine and venlafaxine extended release: a literature review of comparative studies with selective serotonin reuptake inhibitors.

OBJECTIVE: To evaluate data supporting the ability of venlafaxine, an antidepressant with a dual mechanism of action, to produce remission from depression. METHOD: Review of multicentre, double-blind, randomized studies comparing venlafaxine or venlafaxine extended release (XR) with a selective serotonin reuptake inhibitor (SSRI), using Hamilton Depression Rating Scale total scores in the range of < or = 7 and < 10 as the final outcome measure, to evaluate the ability of venlafaxine/venlafaxine XR to produce full remission from depression. RESULTS: Venlafaxine/venlafaxine XR demonstrated higher rates of remission than did the SSRIs and placebo. CONCLUSION: With full remission rather than response as the measure of outcome, venlafaxine/venlafaxine XR demonstrated more robust antidepressant efficacy than the SSRIs and placebo. This finding suggests that venlafaxine/venlafaxine XR are appropriate standard-of-care therapies for the treatment of patients with major depressive disorder.

Antidepressive Agents, Second-Generation↗
PubMed2003

Erotomania induced by venlafaxine: a case study.

OBJECTIVE: To describe a never previously reported case of erotomania induced by venlafaxine and highlight the effect of antidepressants on the dopaminergic system. METHOD: A case of erotomania is described. RESULT: Erotomania occurring in two separate occasions developed after treatment with high doses of venlafaxine. The episode remitted only after lowering the dose of the venlafaxine. CONCLUSION: Erotomania may occur with agents such as antidepressants. The dopamine neurotransmission of mood can provide further evidence for the development of newer classes of antidepressants.

Adult↗
PubMed2001

Pharmacological properties of cannabinoid receptors in the avian brain: similarity of rat and chicken cannabinoid1 receptor recognition sites and expression of cannabinoid2 receptor-like immunoreactivity in the embryonic chick brain.

The pharmacological properties of brain cannabinoid receptors were investigated in brains of 35 day-old chickens, since little is known about the avian cannabinoid system. The cannabinoid1 receptor-selective antagonist ligand [3H]SR 141716A bound to chicken brain membranes with K(D) and Bmax values of 0.92+/-0.28 nM and 790+/-58 fmol/mg protein, respectively. The binding was inhibited by CP 55,940 with a pI50 value of 7.63+/-0.14 and by a series of compounds with the order of potency CP 55,940>R(+)WIN 55,212-2>R-1 methanandamide approximately DAK. S(-)WIN 55,212-3 and AM404 were without inhibitory effect at 1 microM. Similar results were found for rat brain membranes. For both rat and chicken brain membranes, addition of the non-hydrolysable GTP analogues Gpp[NH]p and GTPgammaS shifted the CP 55,940 inhibition curve to the right, consistent with an intact coupling to G-proteins in the preparations. Fatty acid amidohydrolase in chicken brain membranes was less sensitive to inhibition by phenylmethylsulphonyl fluoride and arachidonoyl serotonin than its rodent equivalent. However, when fatty acid amidohydrolase activity in the preparations was reduced by use of a lower assay membrane concentration, anandamide was found to inhibit the binding of [3H]SR 141716A to chicken membranes with a pI50 value of 6.39+/-0.16. Using a novel antibody raised to amino acids 346-359 from the C-terminal tail of the human cannabinoid2 receptor, it was found that embryonic chick brain tissue (and embryonic chick neurones in primary culture) expressed a approximately 53 kDa immunoreactive band. This immunoreactivity, which was prevented by preincubation of the antibody with the immunising peptide, was also seen in cells expressing the recombinant human cannabinoid, receptor, but was not seen in adult chicken brain homogenates or in rat cerebellar homogenates. However, a "classical" cannabinoid2-receptor component of [3H]WIN 55212-2 binding (i.e. a fraction inhibited by low concentrations of the cannabinoid2-receptor-selective antagonist SR 144528) was not found.

Amidohydrolases↗
PubMed1997

(R)-methanandamide, but not anandamide, substitutes for delta 9-THC in a drug-discrimination procedure.

Fourteen male rats were trained to discriminate between injections of 2 mg/kg delta-9-tetrahydrocannabinol (delta 9-THC) and vehicle in a 2-lever operant drug-discrimination paradigm. Following training, substitution tests using a cumulative dosing procedure revealed that anandamide (0.5-16 mg/kg ip), the putative endogenous camabinoid receptor ligand, failed to generalize to the discriminative stimulus properties of the training dose of delta 9-THC. However, dose-dependent generalization to the delta 9-THC cue was observed following administration of both CP-55,940 (0.05-0.8 mg/kg ip), a synthetic cannabinoid, and (R)-methanandamide (0.5-8 mg/kg ip), a metabolically stable analog of anandamide. Collectively, these results demonstrate a cannabinoid-specific in vivo effect of an anandamide compound and suggest that the naturally occurring form of anandamide may be metabolized too rapidly to produce a cannabimimetic intercceptive state when administered peripherally.

Animals↗
PubMed2005

A redefinition of odor mixture quality.

Odor mixtures are perceived as different from (configural) or the same as (elemental) their components. Recent studies (L. M. Kay, C. A. Lowry, & H. A. Jacobs, 2003; C. Wiltrout, S. Dogra, & C. Linster, 2003) propose that component structural or perceptual similarities predict configural properties of binary mixtures. The authors evaluated this in rats using 4 binary mixtures with varying structural similarity (eucalyptol-benzaldehyde, eugenol-benzaldehyde, octanol-octanal, and [+/-]-limonene). The range of tested ratios for each mixture was determined by the components' vapor pressures. Three results are presented: (a) No mixture maintains purely elemental or configural properties for all concentration ratios, (b) structural similarity or dissimilarity does not predict configural or elemental perception, and (c) overshadowing is significant in responses to all odor sets. The authors offer more precise definitions of elemental and configural properties and overshadowing as they relate to odor mixture perception.

Animals↗