Benzodiazepines Flashcards
What are the benzodiazepines?
Estazolam Quazepam Triazolam Flurazepam Temazepam
What are the general properties of BZDs?
replaced Barbs for treatment of insomnia & anxiety. suppress slow-wave sleep (SWS; stages 3&4 NREM) & REM sleep and prolong REM latency. Prolong Stage 2 sleep due to ↑ spindle density, ↓ sleep latency, ↑ total sleep time (TST). Acute withdrawal is associated with DECREASED TST as well as REM & SWS rebound.
What are The three groups that divides BZDs?
into 3 groups based on t1/2 duration: short-acting ( 24hr).
What is the mechanism of BZDs?
allosteric modulators of the GABAA receptor complex by increasing the frequency of the Cl- Channel openings in the presence of GABA and prolongs the miniature inhibitory postsynaptic currents
Describe GABAa receptors?
pentameric complex. 7 subunit families 18 subunits in the CNS
What is the major subtype combination in the CNS?
alpha1beta2gamma2- 60% of all GABAa receptors in the CNS
What is the function alpha 1 GABAa receptor?
Sedation, amnesia, anticonvulsant, ataxia & dependence liability
What is the function alpha 2 GABAa receptor?
Anxiolysis, myorelaxation
What is the function alpha 3 GABAa receptor?
Anxiolysis, myorelaxation, dopaminergic activity
What is the function alpha 5 GABAa receptor?
Memory performance (hippocampus