Pharm, sedatives/hypnotics, Kinder Flashcards
What benzos are used as sedatives
alprazolam clonazepam diazepam midazolam triazolam
benzo antagonist
flumazenil
barbituate used for sedative hypnotic
phenobarbital
mis sedative hypnotic drugs
busiprone eszopiclone ramelteon zaleplon zolpidem
misc sedative hypnotic drugs
busiprone eszopiclone ramelteon zaleplon zolpidem
sedative vs hypnotic
sedative: reduce anxiety and exerts calming effect
hypnotic: drowsiness and facilitates onset and maintenance of state of sleep
MAO benzos
promote binding of GABA to R
enhances GAG induced ion currents (inc freq Cl opening)
effects benzo as sedative/hypnotic
sedation, hypnosis, muscle relaxation, anxiolytic and anticonvulsant effects
MOA barbituate
bind GABA a R and potentiate Cl Ch (inc duration Cl opening)
effects barbituates as sedative/hypnotic
mild sedation to anesthesia
anxiolytic
hypnotic and anticonvulsant effects
MOA eszopiclone and zaleplon and zolpidem
agonist effects at benzo side on GABAa R
MOA remelteon
activate melatonin R MT1 MT2
MOA remelteon
activate melatonin R MT1 MT2
Absorption distribution sedative hypnotics
lipid solubility determines rates and rates of onset
all cross CNS, placental barrier and breast milk
metabolism benzos
hepatic
CYP3A4
which benzos more likely to cause excessive drowsiness
benzos with long half life
relative CI to benzos
hepatic insufficiency
metabolism barbituates
hepatic metabolism and excreted in urine as glucuronide conjugates
new hypnotic metabolism
CYP3A4
short half life
what can increase elimnatino of phenobarbital in urine
alkalinization
better choice benzo if have hepatic insufficiency
lorazepam and oxazepam
3 types binding sites of Benzos
agonist- facilitate GABA
antagonist- block actions benzo
inverse agonists- negative allosteric modulators– produce anxiety and seizures
what are the benzo agonists
benzos, eszoplicone, zalplon and zolpidem