Benzodiazepine: Difference between revisions
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In [[pharmacology]], '''benzodiazepines''' are a class of [[medication]]s that are "a group of two-ring heterocyclic compounds consisting of a benzene ring fused to a diazepine ring."<ref>{{MeSH}}</ref> All benzodiazepines affect specific benzodiazepine receptors and modulate [[gamma-aminobutyric acid]]. Specific benzodiazepines also affect other neurotransmitters (e.g., [[clonazepam]] and [[alprazolam]] affect [[serotonin]]). | In [[pharmacology]], '''benzodiazepines''' are a class of [[medication]]s that are "a group of two-ring heterocyclic compounds consisting of a benzene ring fused to a diazepine ring."<ref>{{MeSH}}</ref> All benzodiazepines affect specific benzodiazepine receptors and modulate [[gamma-aminobutyric acid]]. Specific benzodiazepines also affect other neurotransmitters (e.g., [[clonazepam]] and [[alprazolam]] affect [[serotonin]]). Receptor relationships are quite complex and are discussed further below. | ||
Benzodiazepines are classifed as [[GABA modulator]]s, [[sedative]]s, and [[anti-anxiety agent]]s. Uses include the treatment of [[anxiety disorder]]s and [[alcohol withdrawal syndrome]]. Some are used as [[anticonvulsant]]s and to treat [[musculoskeletal spasticity]]. | Benzodiazepines are classifed as [[GABA modulator]]s, [[sedative]]s, and [[anti-anxiety agent]]s. Uses include the treatment of [[anxiety disorder]]s and [[alcohol withdrawal syndrome]]. Some are used as [[anticonvulsant]]s and to treat [[musculoskeletal spasticity]]. | ||
Examples are: | Examples are: | ||
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* [[Midazolam]] (Versed) | * [[Midazolam]] (Versed) | ||
* Triazolam | * Triazolam | ||
==Receptors== | |||
Part of the confusion in the receptors they affect come from the observation that what had previously been considered the GABA<sub>A</sub>-benzodiazepine-Cl<sup>-</sup> channel complex receptor has numerous sub-receptors, in five classes (α, β, γ, δ, ρ) with at least 16 subtypes. Benzodiazepine receptor type 1, for example, involves binding to α<sub>1</sub>, β<sub>2</sub> and γ<sub>2</sub>.<ref name=GG>{{citation | |||
| title = Goodman and Gilman's The Pharmacological Basis of Therapeutics | |||
| edition = Ninth Edition | |||
|date = 1996 | |||
| publisher = McGraw-Hill | |||
| contribution = Chapter 18, Drugs and the treatment of Psychiatric Disorders: Psychosis and Anxiety | |||
| author = Ross J. Baldessarini | |||
| editor = Joel G. Hardman ''et al.'' | |||
| isbn = 0070262667 | |||
}} pp. 421-434</ref> The interactions among GABA, benzodiazepines, and some other classes of drugs are even more complex, in that binding to one receptor type affects other receptors. For example, certain bindings to benzodiazepine receptors will increase the rate of opening of the GABA<sub>A</sub> receptor,<ref name=eMed-Tox>{{citation | |||
| title = Toxicity, Benzodiazepine | |||
| author = Robin Mantooth | |||
| date = 28 January 2010 | |||
| publisher = eMedicine | |||
| url = http://emedicine.medscape.com/article/813255-overview}}</ref> potentiating the effect of both endogenous GABA and GABA released by direct GABA agonists such as [[baclofen]]. | |||
==Clinical use== | |||
===Anxiety=== | |||
===Convulsive disorders=== | |||
===Musculoskeletal spasticity=== | |||
==Toxicity== | |||
==References== | ==References== | ||
{{reflist|2}} | |||
Revision as of 11:23, 4 June 2010
In pharmacology, benzodiazepines are a class of medications that are "a group of two-ring heterocyclic compounds consisting of a benzene ring fused to a diazepine ring."[1] All benzodiazepines affect specific benzodiazepine receptors and modulate gamma-aminobutyric acid. Specific benzodiazepines also affect other neurotransmitters (e.g., clonazepam and alprazolam affect serotonin). Receptor relationships are quite complex and are discussed further below.
Benzodiazepines are classifed as GABA modulators, sedatives, and anti-anxiety agents. Uses include the treatment of anxiety disorders and alcohol withdrawal syndrome. Some are used as anticonvulsants and to treat musculoskeletal spasticity.
Examples are:
- Alprazolam
- Benzodiazepinones
- Anthramycin
- Bromazepam
- Clonazepam
- Devazepide
- Diazepam (Valium)
- Flumazenil
- Flunitrazepam
- Flurazepam
- Lorazepam
- Nitrazepam
- Oxazepam
- Pirenzepine
- Prazepam
- Temazepam
- Chlordiazepoxide (Librium)
- Clorazepate dipotassium
- Estazolam
- Medazepam
- Midazolam (Versed)
- Triazolam
Receptors
Part of the confusion in the receptors they affect come from the observation that what had previously been considered the GABAA-benzodiazepine-Cl- channel complex receptor has numerous sub-receptors, in five classes (α, β, γ, δ, ρ) with at least 16 subtypes. Benzodiazepine receptor type 1, for example, involves binding to α1, β2 and γ2.[2] The interactions among GABA, benzodiazepines, and some other classes of drugs are even more complex, in that binding to one receptor type affects other receptors. For example, certain bindings to benzodiazepine receptors will increase the rate of opening of the GABAA receptor,[3] potentiating the effect of both endogenous GABA and GABA released by direct GABA agonists such as baclofen.
Clinical use
Anxiety
Convulsive disorders
Musculoskeletal spasticity
Toxicity
References
- ↑ Anonymous (2024), Benzodiazepine (English). Medical Subject Headings. U.S. National Library of Medicine.
- ↑ Ross J. Baldessarini (1996), Chapter 18, Drugs and the treatment of Psychiatric Disorders: Psychosis and Anxiety, in Joel G. Hardman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics (Ninth Edition ed.), McGraw-Hill, ISBN 0070262667 pp. 421-434
- ↑ Robin Mantooth (28 January 2010), Toxicity, Benzodiazepine, eMedicine