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SedativeMuscle relaxantPharmacologicalReceptorsGamma-aminDiscontinuation of benzodiazepinesDepressantSedativesSerotoninBuspironeDrugsSedationDependenceOpiatesWithdrawalEfficacyHypnoticsChlordiazepoxideHypnoticMeprobamateDisorderSelectivityChlorideMaximalEffectsTranquilizerPanicClassDosageDrugFrequently
Sedative8
  • Per the Diagnostic and Statistical Manual of Mental Disorders, Fifth Edition, Text Revision (DSM-5-TR) , the appropriate diagnosis for a prolonged and problematic pattern of use of these substances would be "Sedative, Hypnotic, or Anxiolytic Use Disorder. (medscape.com)
  • Sonata (zaleplon) is a non-benzodiazepine sedative hypnotic drug used to treat insomnia. (rxlist.com)
  • The benzodiazepines (pronounced [ˌbɛnzoː.daɪˈæzəˌpiːn] , often abbreviated to "benzos" ) are a class of psychoactive drugs with varying hypnotic , sedative , anxiolytic , anticonvulsant , muscle relaxant and amnesic properties, which are mediated by slowing down the central nervous system . (wikidoc.org)
  • Their reduced intrinsic efficacy relative to full agonists such as diazepam resulted in an improved preclinical pharmacological profile in that there was a large window between anxiolytic and sedative doses and their dependence and abuse liabilities were much lower. (hhs.gov)
  • Belonging to the azaspirodecanedione drug class, 2 buspirone is a serotonin 5-HT 1A receptor agonist that is not chemically or pharmacologically related to benzodiazepines, barbiturates, and other sedative/anxiolytic drugs. (arlen.com.br)
  • Buspirone hydrochloride tablets, USP are an antianxiety agent that is not chemically or pharmacologically related to the benzodiazepines, barbiturates, or other sedative/anxiolytic drugs. (arlen.com.br)
  • Temazepam (trade name Restoril ) is a short-acting [3] psychoactive substance of the benzodiazepine class which produces anxiolytic, sedative, hypnotic, muscle relaxant, anticonvulsant , and amnesic effects. (psychonautwiki.org)
  • Subunit modulation of the GABA-BZ receptor chloride channel macromolecular complex is hypothesized to be responsible for some of the pharmacological properties of benzodiazepines, which include sedative, anxiolytic, muscle relaxant, and anticonvulsive effects in animal models. (healthyplace.com)
Muscle relaxant1
  • Tests revealed that the compound had hypnotic , anxiolytic and muscle relaxant effects. (wikidoc.org)
Pharmacological4
  • In addition to conventional psychotherapy models, psychiatrists worked on pharmacological therapies and consequently sedatives, anxiolytics, and hypnotics were created. (medscape.com)
  • Essential oils and the constituents in them exhibit different pharmacological activities, such as antinociceptive, anxiolytic-like, and anticonvulsant effects. (mdpi.com)
  • However, the advent of molecular genetic and pharmacological approaches has begun to delineate which GABA(A) receptor subtypes are associated with the various pharmacological effects of the non-selective BZs. (hhs.gov)
  • Its main pharmacological action is to increase the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABA A receptor. (psychonautwiki.org)
Receptors14
  • Trazodone - found in Sleep-T Synergy and Sleep-T Synergy Forte this antidepressant medication increases serotonin in the brain by preventing its reuptake and subsequent breakdown in brain cells and acts as an antagonist at 5-HT-2A/2C serotonin receptors. (victoryselect.com)
  • Benzodiazepines and barbiturates bind gamma-aminobutyric acid (GABA)-A receptors, increase the affinity of the receptor to GABA, and promote inhibitory neurotransmitter effects. (merckmanuals.com)
  • Some cross-tolerance exists between alcohol and sedatives, especially drugs that act on GABA-A receptors. (merckmanuals.com)
  • γ-Aminobutyric acid A (GABA A ) receptors (GABARs) are responsible for most fast inhibitory neurotransmission in the mammalian brain. (aspetjournals.org)
  • Although GABA activates synaptic (αβγ) GABA A receptors with high efficacy, partial agonist activation of αβγ isoforms and GABA activation of the primary extrasynaptic (αβδ) GABA A receptors are limited to low-efficacy activity, characterized by minimal desensitization and brief openings. (jneurosci.org)
  • Allosteric conversion of partial to full agonism may be a general mechanism for reversibly scaling the efficacy of GABA A receptors to endogenous partial agonists. (jneurosci.org)
  • It is even more intriguing to consider the potential plasticity of allosteric modulation given the observation of agonist-dependent functional properties of GABA A receptors. (jneurosci.org)
  • Non-selective benzodiazepine (BZ) binding-site full agonists, exemplified by diazepam, act by enhancing the inhibitory effects of GABA at GABA(A) receptors containing either an alpha1, -2, -3 or -5 subunit. (hhs.gov)
  • More specifically, the alpha2- and/or alpha3-containing GABA(A) receptors play a role in anxiety whereas the alpha1 subtype is involved in sedation, raising the possibility of a compound that selectively modulates alpha2- and/or alpha3-containing receptors but does not affect alpha1-containing receptors would be a non-sedating anxiolytic. (hhs.gov)
  • The benzodiazepine binding site of GABA(A) receptors as a target for the development of novel anxiolytics. (hhs.gov)
  • Activated postsynaptic 5-HT1A receptors promote hyperpolarization to released 5-HT on pyramidal neurons.8, The anxiolytic action of buspirone is mainly thought to arise from the interaction at presynaptic 5-HT1A autoreceptors. (arlen.com.br)
  • Benzodiazepines produce a variety of effects by binding to the benzodiazepine receptor site and magnifying the efficiency and effects of the neurotransmitter gamma aminobutyric acid (GABA) by acting on its receptors . (psychonautwiki.org)
  • The anticonvulsant properties of benzodiazepines may be, in part or entirely, due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors. (psychonautwiki.org)
  • Antagonist for the postsynaptic mesolimbic dopaminergic D2 receptors in the brain and decreases the release of hypothalamic and hypophyseal hormones. (essentialsofmedicine.com)
Gamma-amin4
Discontinuation of benzodiazepines2
  • Mr X was diagnosed with anxiolytic withdrawal due to recent abrupt discontinuation of benzodiazepines. (medscape.com)
  • It's worth noting that the sudden discontinuation of benzodiazepines can be potentially dangerous or life-threatening for individuals using regularly for extended periods of time, sometimes resulting in seizures or death. (psychonautwiki.org)
Depressant1
  • Midazolam is a short-acting benzodiazepine central nervous system (CNS) depressant. (nih.gov)
Sedatives2
Serotonin3
  • At low doses, trazodone appears to act as a serotonin antagonist and at higher doses as an agonist. (victoryselect.com)
  • Next, we'll take a look at each neurotransmitter system and examine how something other than serotonin, GABA, or glutamate may be causing your problem. (nootropicsexpert.com)
  • Arguably the most important advance in the pharmacotherapy of severe mental disorders in the last fifty years was the substitution of barbiturates with the clinically safer benzodiazepines and the introduction of the theory-driven selective serotonin reuptake inhibitors for the treatment of depression. (biomedcentral.com)
Buspirone3
Drugs3
  • Barbiturates Alcohol and illicit drugs are toxic to the placenta and developing fetus and can cause congenital syndromes and withdrawal symptoms. (merckmanuals.com)
  • The γ-aminobutyric acid A (GABA A ) receptor (GABAR) is a target for many clinically and experimentally important drugs. (aspetjournals.org)
  • Benzodiazepine drugs contain a benzene ring fused to a diazepine ring, which is a seven membered ring with the two nitrogen constituents located at R 1 and R 4 . (psychonautwiki.org)
Sedation3
  • Concomitant use of benzodiazepines and opioids may result in profound sedation, respiratory depression, coma, and death. (nih.gov)
  • However, despite their proven clinical anxiolytic efficacy, such compounds possess a relatively narrow window between doses that produce anxiolysis and those that cause sedation, and are also associated with physical dependence and a potential for abuse. (hhs.gov)
  • Clonazolam is described to be highly powerful, and concerns have been raised that clonazolam and flubromazolam in particular may pose comparatively higher harms than other designer benzodiazepines, due to their capacity to produce strong sedation and amnesia at oral doses of as little as 0.5 mg. (syntheticchemicallab.com)
Dependence3
  • Withdrawal and Detoxification from Benzodiazepine Dependence: A Potential Role for Clonazepam. (benzo.org.uk)
  • Anand KJS, Ingraham J. Tolerance, Dependence, and Strategies for Compassionate Withdrawal of Analgesics and Anxiolytics in the Pediatric ICU. (benzo.org.uk)
  • Dependence varies with the benzodiazepine used and with the user. (wikidoc.org)
Opiates1
Withdrawal3
Efficacy2
  • The newer GABA-effective hypnotics are the only medications with demonstrated effectiveness in treating chronic insomnia with the majority of evidence supporting treatment efficacy for cognitive-behavioral therapy and short acting GABA-receptor agonists. (springer.com)
  • We suggest that neurosteroids preferentially enhance low-efficacy GABA A receptor activity independent of subunit composition. (jneurosci.org)
Hypnotics1
  • The therapeutic value of these agents as anxiolytics and hypnotics has been well established, and they continue to serve an important role in managing many debilitating anxiety symptoms in the context of both psychiatric disorders and medical illness. (medscape.com)
Chlordiazepoxide4
  • [ 1 ] By 1959, the benzodiazepine chlordiazepoxide was created, giving rise to at least 3000 different benzodiazepines, of which 13 are currently marketed. (medscape.com)
  • The first benzodiazepine, chlordiazepoxide (Librium) was discovered serendipitously in 1954 by the Austrian scientist Leo Sternbach (1908-2005), working for the pharmaceutical company Hoffmann-La Roche . (wikidoc.org)
  • Three years later chlordiazepoxide was marketed as a therapeutic benzodiazepine medication under the brand name Librium. (wikidoc.org)
  • Following chlordiazepoxide in 1963 diazepam hit the market under the brand name Valium, followed by many further benzodiazepine compounds which were introduced over the subsequent years and decades. (wikidoc.org)
Hypnotic1
Meprobamate1
Disorder2
  • The status of these and other BZ site compounds with claimed, but often not explicitly stated, GABA(A) subtype selectivity (such as ELB-139 and ocinaplon) will be reviewed in relation to their development as non-sedating anxiolytics for the treatment of generalised anxiety disorder. (hhs.gov)
  • buy Clonazepam is a benzodiazepine that's prescribed for seizures, anxiety, panic disorder, and other conditions. (syntheticchemicallab.com)
Selectivity1
  • Many GABA A receptor modulators exhibit clear subunit selectivity ( Olsen and Macdonald, 2002 ). (jneurosci.org)
Chloride1
  • GABA opens chloride (Cl) channels, causing an influx of Cl ions. (medscape.com)
Maximal1
  • Amiloride acted primarily as a competitive antagonist, reducing the sensitivity of the receptor to GABA without affecting the maximal current amplitude. (aspetjournals.org)
Effects1
Tranquilizer1
Panic1
  • Benzodiazepines are also used to treat the panic that can be caused by hallucinogen intoxication. (wikidoc.org)
Class1
Dosage2
  • Midazolam hydrochloride injection is a water-soluble benzodiazepine available as a sterile, nonpyrogenic parenteral dosage form for intravenous or intramuscular injection. (nih.gov)
  • The use of benzodiazepines should therefore commence only after medical consultation and benzodiazepines should be prescribed the smallest dosage possible to provide an acceptable level of symptom relief. (wikidoc.org)
Drug1
  • Clonazolam powder also known as clonitrazolam is a benzodiazepine that has very little analysis done about its results and metabolism, and has been sold online as a designer drug. (syntheticchemicallab.com)
Frequently1