sedatives Flashcards
CO toxicity treatment
remove from exposure and give high dose oxygen
zolpidem is a ___ derivative
imidazopyridine
zaleplon is a ____ derivative
pyrazolopyrimidine
ziprasidone class
antipsychotic
properties of sedatives/hypnotics:
duration of stage 2 NREM is ____ and the duration of REM is ____ and the duration of slow-wave sleep is ____
increased, decreased, decreased
tolerance to sedatives and hypnotics occurs after….
1-2weeks
true or false
sedatives/hypnotics should ONLY be used for short term treatment
true
true or false
barbituric acid itself is not pharmacologically active
true
barbiturate substitution – predict what will happen when C2 is replaced with sulfur instead of oxygen:
-lipid solubility?
-toxicity?
-electronegativity?
-onset of action?
this substitution is only used as what?
increased lipid solubility
increased toxicity
decreased electronegativity
increased onset of action
a pre-op sedative/hypnotic
C5 substitution of barbiturates with ___ or ____ is ESSENTIAL for hypnotic activity
alkyl or aryl
C5 phenyl group gives ____
increased length of C5 gives….
C5 PHENYL gives anticonvuldant activity
increase length gives hypnotic potency, and over 5-6 carbons increases anticonvulsant activity!
c1 sub with H, methyl or ethyl…
rapid action, and high incidences of excitatory phenomenon like tremors, involuntary movements
most important metabolism of barbiturates
C5 oxidation
molecular target of barbiturates
GABA ! - MOST well known inhibitory neurotransmitter
**absorption of barbiturates
generally well absorbed from the GI tract and the muscle
distribution of barbiturates
well distributed in all compartments – including the brain and potential fetues
3 ultra short acting barbiturates
methohexital
thiopental
pentobarbital
VERY lipid soluble
*mechanism of barbiturate tolerance
number of GABA receptors is reduced
___-___ times the therapeutic dose of barbiturates is the toxic dose
5-10x – not that much!!
15X IS DEATH
true or false
withdrawal from barbiturates is more dangerous than withdrawal from opiates
true
true or false
there is medication to treat barbiturate overdose
FALSE - there isn’t
what are the most important sedative hypnotics and why were they developed
benzodiazepines
to avoid the undesirable effects of barbiturates (abuse liability)
explain MOA barbiturates vs benzos
barb increase the duration of GABA channel openings
benzos increase the FREQUENCY of GABA channel openings
BOTH increase the receptor affinity for GABA
GABA receptor is a ___ channel
chloride
binding causes chloride to flow into the cell – hyperpolarization
overdose drug for benzos
flumazenil (but doesnt work for barbiturates!)
