Category:Benzodiazepines
From Ganfyd
History
The original benzodiazepine, chlordiazepoxide, was first produced in 1954, but was not marketed for several years. Diazepam was first marketed in 1963. They were initially promoted as non-addictive substitutes for the barbiturates, but after several years their addictive potential became clear. They are not Soma, quite. Diazepam, lorazepam and temazepam, but not chlordiazepoxide are associated with an increased incidence of community acquired pneumonia[1].
Pharmacokinetics and pharmacodynamics
Potentiate the inhibitory neurotransmitter GABA, acting on benzodiazepine binding sites at GABA-ergic synapses.
Benzodiazepine binding has been classified into 3 subtypes:
- Omega-1 responsible for hypnotic effect associated with GABA-A receptors where the alpha subunit is α1[2].
- Omega-2 responsible for anxiolytic effect associated with GABA-A receptors where the alpha subunit is either α2 or α3 [3].
- Omega-3 responsible for muscle relaxant effect.
Benzodiazepines act on all three subtypes (cf z drugs none of which have action on Omega-3.)
There is also an outer mitochondrial membrane benzodiazepine receptor that appears to be a key factor in the flow of cholesterol into mitochondria permitting steroid hormone synthesis called BZRP and coded at 22q13.31[4].
She goes running for the shelter,
Of her mother's little helper 
-
Jagger, M 20th century
References
- ↑ The impact of benzodiazepines on occurrence of pneumonia and mortality from pneumonia: case-control and cohort study Thorax doi:10.1136/thoraxjnl-2012-202374
- ↑ Da Settimo F, Taliani S, Trincavelli ML, Montali M, Martini C. GABA A/Bz receptor subtypes as targets for selective drugs. Current medicinal chemistry. 2007; 14(25):2680-701.
- ↑ Da Settimo F, Taliani S, Trincavelli ML, Montali M, Martini C. GABA A/Bz receptor subtypes as targets for selective drugs. Current medicinal chemistry. 2007; 14(25):2680-701.
- ↑ Lin D, Chang YJ, Strauss JF, Miller WL. The human peripheral benzodiazepine receptor gene: cloning and characterization of alternative splicing in normal tissues and in a patient with congenital lipoid adrenal hyperplasia. Genomics. 1993 Dec; 18(3):643-50.
Pages in category "Benzodiazepines"
The following 13 pages are in this category, out of 13 total.
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DLMO |
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