Bergamottin can be used to assess CYP3A-mediated intestinal first-pass metabolism without affecting P-glycoprotein-mediated efflux in rats.
Abstract
1. We investigated whether bergamottin would be useful for evaluating CYP3A-mediated intestinal metabolism in rats utilising its characteristics as a mechanism-based inhibitor of CYP3A. 2. Buspirone and fexofenadine, probe substrates of CYP3A and P-glycoprotein (P-gp), respectively, were orally co-administered to rats with bergamottin (2.5 mg/kg) or orally administered 2 h after bergamottin pre-treatment. The effect of bergamottin pre-treatment on hepatic CYP3A specifically was investigated with intravenous administration of buspirone. The kobs of bergamottin for CYP3A was calculated based on ...
Source: Xenobiotica - July 17, 2019 Category: Research Authors: Suzuki K, Taniyama K, Aoyama T, Watanabe Y Tags: Xenobiotica Source Type: research
Treatment of Sleep Bruxism With a Single Daily Dose of Buspirone in a 7-Year-Old Boy
We present a 7-year-old boy whose sleep bruxism symptoms disappeared with a single daily dose of buspirone treatment in this report. (Source: Clinical Neuropharmacology)
Source: Clinical Neuropharmacology - July 1, 2019 Category: Neurology Tags: Case Reports Source Type: research
Drugs for Anxiety Disorders
Date: August 12, 2019
Issue #:
1578Summary:
Anxiety disorders (generalized anxiety disorder, panic
disorder, social anxiety disorder, and various phobias)
are the most common form of psychiatric illness. They
can be treated effectively with cognitive behavioral
therapy (CBT) and/or pharmacotherapy. Obsessive-compulsive
disorder and posttraumatic stress
disorder are now considered separate entities in the
Diagnostic and Statistical Manual of Mental Disorders
(DSM-5); they can also be treated with CBT and many
of the same drugs. (Source: The Medical Letter)
Source: The Medical Letter - June 27, 2019 Category: Drugs & Pharmacology Authors: admin Tags: Alprazolam Amitriptyline Antidepressants Antihistamines Antipsychotics Atarax Ativan Beta blockers Buspirone Cannabidiol Celexa Chlordiazepoxide Cipralex Citalopram Clonazepam Clorazepate Cymbalta Diazepam Doxepin Dri Source Type: research
Human anxiety-specific “theta” occurs with selective stopping and localizes to right inferior frontal gyrus.
Anxiety disorders have high prevalence and generate major disability. But they have poor treatment targeting because psychiatry lacks diagnostic biomarkers. Right frontal goal-conflict-specific-rhythmicity (GCSR) in the simple stop signal task appears homologous to hippocampal “theta” as an anxiety-process biomarker but is weak and transient. An anticipatory response inhibition task (ARIT) elicits strong subjective conflict and so might generate stronger GCSR. Healthy participants provided EEG during an ARIT, which allowed direct comparison of selective (left, SG; right, GS), and nonselective (both, SS) handed stopping...
Source: Behavioral Neuroscience - June 20, 2019 Category: Neuroscience Source Type: research
The functional observational battery and modified Irwin test as global neurobehavioral assessments in the rat: Pharmacological validation data and a comparison of methods
ConclusionsBoth tests are ‘fit-for-purpose’ in detecting effects of candidate drugs on the nervous system. We would encourage the global safety pharmacology community to consider whether (a) the tests could be combined into one industry standard; (b) candidate drugs could be triaged according to CNS penetration, with the level of scrutiny in the CNS core battery assessment adjusted accordingly and (c) whether new home cage technology could be applied to semi-automate the preclinical neurobehavioral assessment. (Source: Journal of Pharmacological and Toxicological Methods)
Source: Journal of Pharmacological and Toxicological Methods - May 28, 2019 Category: Drugs & Pharmacology Source Type: research
Buspirone for the treatment of anxiety-related symptoms in Angelman syndrome: a case series
Conclusion
The findings of this study suggest that buspirone may be effective for the amelioration of behaviors related to anxiety in patients with AS, and well tolerated. Limitations include the open-label nature of these treatments, the small sample size and the absence of a control group. (Source: Psychiatric Genetics)
Source: Psychiatric Genetics - March 7, 2019 Category: Genetics & Stem Cells Tags: ORIGINAL ARTICLES Source Type: research
Buspirone Hydrochloride Loaded In Situ Nanovesicular Gel as an Anxiolytic Nasal Drug Delivery System: In Vitro and Animal Studies.
Abstract
Nasal nanovesicular gels of buspirone hydrochloride (BH) were prepared and characterized aiming for sustained delivery and enhancing bioavailability. Buspirone hydrochloride has low bioavailability of about 4% after oral administration due to first pass metabolism. Buspirone hydrochloride nanovesicles were formulated by thin film hydration method (TFH). The selected nanovesicular formulation was incorporated into two types of in situ gels (pH-induced and thermoreversible) using carbopol 974P and poloxamer 407 (P407), respectively, together with different mucoadhesive polymers. The in situ gels wer...
Source: AAPS PharmSciTech - March 3, 2019 Category: Drugs & Pharmacology Authors: Abdelnabi DM, Abdallah MH, Elghamry HA Tags: AAPS PharmSciTech Source Type: research
A Case of Buspirone Demonstrating Immediate and Sustained Benefit in a Man With Lifelong Non–Rapid-Eye-Movement Parasomnias
Conclusion
Buspirone can be considered an effective alternate treatment option for NREM parasomnias when other medications are not preferred or cannot be prescribed. (Source: Clinical Neuropharmacology)
Source: Clinical Neuropharmacology - March 1, 2019 Category: Neurology Tags: Case Reports Source Type: research
Buspirone for the treatment of anxiety-related symptoms in Angelman syndrome: a case series
Conclusion
The findings of this study suggest that buspirone may be effective for the amelioration of behaviors related to anxiety in patients with AS, and well tolerated. Limitations include the open-label nature of these treatments, the small sample size and the absence of a control group. (Source: Psychiatric Genetics)
Source: Psychiatric Genetics - February 26, 2019 Category: Genetics & Stem Cells Tags: ORIGINAL ARTICLES Source Type: research
sIs hippocampal theta frequency related to individual and sex differences in anxiety-like behaviour? An analysis in male and female Long-Evans rats.
Abstract
Hippocampal theta activity is a prominent slow (4-12 Hz) oscillatory activity pattern generated in the mammalian hippocampal formation. Based on evidence that anxiolytic drugs consistently decrease the frequency of hippocampal theta activity in rodents, hippocampal theta has been linked to anxiety states, leading to the influential theta suppression model of anxiolysis. Surprisingly, very few studies have examined whether hippocampal theta frequency relates to individual or sex differences in anxiety-like behaviour. Here, male and female rats were tested on the elevated plus maze (EPM) to quanti...
Source: Behavioural Brain Research - February 9, 2019 Category: Neurology Authors: Ou C, Dringenberg HC, Soutar CN Tags: Behav Brain Res Source Type: research
Pharmacological treatments for generalised anxiety disorder: a systematic review and network meta-analysis
This study is registered with PROSPERO, number CRD42018087106.FindingsStudies were published between Jan 1, 1994 and Aug 1, 2017, in which 1992 potential studies were screened for inclusion. This analysis is based on 89 trials, which included 25 441 patients randomly assigned to 22 different active drugs or placebo. Duloxetine (MD −3·13, 95% credible interval [CrI] −4·13 to −2·13), pregabalin (MD −2·79, 95% CrI −3·69 to −1·91), venlafaxine (MD −2·69, 95% CrI −3·50 to −1·89), and escitalopram (MD −2·45, 95% CrI −3·27 to −1·63) were more efficacious than placebo with relatively good acce...
Source: The Lancet - February 1, 2019 Category: General Medicine Source Type: research
Pharmacotherapies for cannabis dependence.
CONCLUSIONS: There is incomplete evidence for all of the pharmacotherapies investigated, and for many outcomes the quality of the evidence was low or very low. Findings indicate that SSRI antidepressants, mixed action antidepressants, bupropion, buspirone and atomoxetine are probably of little value in the treatment of cannabis dependence. Given the limited evidence of efficacy, THC preparations should be considered still experimental, with some positive effects on withdrawal symptoms and craving. The evidence base for the anticonvulsant gabapentin, oxytocin, and N-acetylcysteine is weak, but these medications are also wor...
Source: Cochrane Database of Systematic Reviews - January 28, 2019 Category: General Medicine Authors: Nielsen S, Gowing L, Sabioni P, Le Foll B Tags: Cochrane Database Syst Rev Source Type: research
Prenatal Stimulation of 5-HT 1A Receptors Improves Adaptive Behavior in Prenatally Stressed Rats
Various types of adaptive behavior during the prepubertal period were analyzed in the offspring of rats receiving chronic injections of serotonin (5-HT) reuptake inhibitor fluoxetine, 5-HT1A receptor agonist buspirone, or their combination starting from gestation day 9 and subjected to immobilization stress from the 15th day of pregnancy until delivery. Prenatal stress increased pain sensitivity, prolonged inflammatory pain response, and increased the levels of anxiety and depression. Chronic administration of drugs acting through 5-HT1A receptors to pregnant rats improved the studied behavioral parameters in their offspri...
Source: Bulletin of Experimental Biology and Medicine - January 18, 2019 Category: Biology Source Type: research
Monoaminergic system and depression
AbstractMajor depressive disorder is a severe, disabling disorder that affects around 4.7% of the population worldwide. Based on the monoaminergic hypothesis of depression, monoamine reuptake inhibitors have been developed as antidepressants and nowadays, they are used widely in clinical practice. However, these drugs have a limited efficacy and a slow onset of therapeutic action. Several strategies have been implemented to overcome these limitations, including switching to other drugs or introducing combined or augmentation therapies. In clinical practice, the most often used augmenting drugs are lithium, triiodothyronine...
Source: Cell and Tissue Research - January 10, 2019 Category: Cytology Source Type: research
Preparation and in vitro/in vivo evaluation of anastrozole reservoir-type intravaginal ring.
This report details the preparation of anastrozole (ATZ) reservoir-type intravaginal ring (IVR) and the detection the concentration of ATZ in Beagle dog plasma by liquid chromatography-tandem mass spectrometry (LC-MS/MS). An ATZ reservoir-type IVR which included ATZ silicone elastomer core and non-active silicone layer, was manufactured by reaction injection moulding at 80°C for 20 min. In vitro release experiment was performed under sink conditions and the samples are determined by high performance liquid chromatography (HPLC). A bioanalytical method has also been developed and validated for determination of ATZ in Beagl...
Source: Biomedical Chromatography : BMC - December 9, 2018 Category: Biomedical Science Authors: Xia L, Qiu S, Liu Z, Ning M Tags: Biomed Chromatogr Source Type: research
