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Its mechanism of action works by increasing the effect of the neurotransmitter gamma-aminobutyric acid (GABA). [20] Diazepam was patented in 1959 by Hoffmann-La Roche. [15] [22] [23] It has been one of the most frequently prescribed medications in the world since its launch in 1963. [15]
In terms of the mechanism of action of benzodiazepines, their similarities are too great to separate them into individual categories such as anxiolytic or hypnotic. For example, a hypnotic administered in low doses produces anxiety-relieving effects, whereas a benzodiazepine marketed as an anti-anxiety drug at higher doses induces sleep. [175]
Several efficient benzodiazepines offer choices about dosage form, length of action, metabolic interaction and safety. Benzodiazepines function by binding to the benzodiazepine site on most, but not all, GABA A receptors. GABA A modulation by benzodiazepine site agonists is self-limiting. The channel conductance is not higher in the presence of ...
The following benzodiazepines are used to treat status epilepticus: Diazepam (1963). Can be given rectally by trained care-givers. Midazolam (N/A). Increasingly being used as an alternative to diazepam. This water-soluble drug is squirted into the side of the mouth but not swallowed. It is rapidly absorbed by the buccal mucosa. Lorazepam (1972 ...
Benzodiazepines impair learning and memory via their action on benzodiazepine receptors, which causes a dysfunction in the cholinergic neuronal system in mice. [16] It was later found that impairment in learning was caused by an increase in benzodiazepine/GABA activity (and that benzodiazepines were not associated with the cholinergic system). [17]
Benzodiazepines share a similar mechanism of action with various sedative compounds that act by enhancing the GABA A receptor. Cross tolerance means that one drug will alleviate the withdrawal effects of another. It also means that tolerance of one drug will result in tolerance of another similarly-acting drug.