Pharmacology of Benzodiazepines - Mechanism of action , uses , side effects : Fmge and neet pg
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PHARMACOLOGY OF BENZODIAZEPINES
Mechanism of action โ Benzodiazepines bind to gamma-aminobutyric acid type A (GABAA) receptors, which are responsible for most of the inhibitory neurotransmission in the central nervous system and a major target of alcohol, barbiturates, muscle relaxants, and other medications with sedative effects. GABAA receptors are ligand-gated chloride ion channels. When GABA binds to these receptors, it increases the amount of chloride current generated by the receptor. Benzodiazepines augment GABAโs inhibitory effect by increasing the frequency of channel openings . This inhibitory effect leads to the anxiolytic, hypnotic, anticonvulsive, and muscle-relaxing properties of benzodiazepines.
Pharmacokinetics โ Benzodiazepines can be categorized into short (15 to 30 minutes), intermediate (30 to 60 minutes), and long-acting agents (one hour or longer). There are at least three determinants of the speed of action of benzodiazepines: half-life, rate of absorption, and lipophilicity. Half-life is determined by how the drug is metabolized and whether it has any active metabolites.
As an example, diazepam has a long half-life because it is oxidized by the liver (a relatively slower process) and is metabolized into oxazepam, which is an active anxiolytic.
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