Drugs to treat Insomnia Flashcards
Barbiturates work how?
Modulate GABA receptors in the CNS.
They make GABA action last longer. At very high doses may activate GABA itself.
AE’s of barbiturates?
increase as the dosing gets higher, duh..,,Sedation, hypnosis, anesthesia, all the way to coma….This is why they are rarely used these days
Benzodiazepines do what
MODULATE GABA receptors….that is, they shift the dose response curve to the left meaning less GABA creates a greater action.
adverse effects of benzos
sedation, cognitive impairment, rebound insomnia with short acting drugs
Withdrawal symptoms of benzos
anxiety, irritability, restlessness, sleep apnea, respiratory depression
Benzos bind what subunit of the GABA receptor
alpha
different subgroups of binding sites for Benzos on the alpha subunit of GABA receptor
BZ1- sedation/amnesia
BZ2- anxiolysis
BZ3- myorelaxation/anticonvulsant
All benzos are ultimately eliminated how?
conjugated and then renally excreted
Know the benzo drugs
ok
Benzodiazepine receptor agonists can be used during pregnancy,,, they are cat c
ok
Flumazenil
Benzo antagonist. Reversal of sedation from benzo/benzo agonists. IV quick acting. causes abrupt awakening. Can cause seizure and withdrawl in chronic benzo users. Does not reverse sedation.
What does melatonin do
affects teh suprachiasmatic nucleus activity
Of the three melatonin receptors, which affect the sleep/wake cycle
MT-1 and 2