B7-074 Anxiolytic and Sedative/Hypnotic Drugs Flashcards
bind to specific binding site on GABA-a receptor [2]
barbiturates
benzodiazepines (BZ)
facilitate GABA by increase Cl- opening time
barbiturates
barbiDURATes increase DURATion
barbiturates effects on CNS
complete CNS depression
can be exacerbated by alcohol use
barbiturates effects on cardiopulmonary system
medullary depression
(causes decreased respiration and blood pressure at anesthetic doses)
barbiturates effects on liver
P450s inducer
(decreases plasma levels of other drugs)
-tal
belong to what class of drugs?
barbiturates
phenobarbital, pentobarbital
barbituates she said to know [3]
phenobarbital (least lipophilic)
pentobarbital
thiopental (most lipophilic)
acute adverse effects of barbiturates
overdose
additive effects with other depressants
extreme medullary depression, no reversal agent
chronic effects of barbiturates [3]
tolerance
addiction
withdrawal
withdrawal from […] can cause seizures, hyperthermia, and cardiovascular collapse
barbiturates
metabolized in the liver via CYP450
barbiturates
increase likelihood of Cl- channel opening
benzodiazepines
FREZOdiazepines increase FREquency
act at a smaller subset of GABA receptors than barbiturates
benzodiazepines
CNS effects of benzodiazepines [5]
incomplete depressants
decreased anxiety
skeletal muscle relaxant
anticonvulsant
hypnotic
additive effect with barbiturates, alcohol
side effects benzodiazepines
sedation
amnesia
withdrawal
acute overdose of benzodiazepines can be treated with
flumazenil (antagonist)
-lam
-pam
what class are these?
benzodiazepines
short acting benzodiazepines [2]
midazolam (versed)
remimazolam
(2-4 hrs)
moderative acting benzodiazepines [3]
alprazolam
chlordiazepoxide
lorazepam
(10-14 hrs)
benzodiazepine often used for ACUTE panic attacks due to oral formulation
but can cause rebound anxiety
alprazolam
long acting benzodiazepines [1]
clonazepam (24 hrs)
(anti-convulsant)
very long acting benzodiazepines [1]
diazepam
benzodiazepine antagonist
flumazenil
fast acting benzodiazepine
date rape drug
flunitrazepam
highly protein bound but have very few drug interactions
benzodiazepines
BZ-1 agonists [2]
zolpidem
zaleplon
(non-benzodiazepine BZ agonists)
non-selective BZ agonist [1]
eszopiclone
(non-benzodiazepines BZ agonists)
side effects include abnormal thinking/behavior such as hallucinations, sleepwalking, and amnesia
non-benzodiazepines BZ agonist
(Z-…)
FA: anxiety, headaches, confusion
what contributes to the duration of long acting anxiolytics, like diazepam?
metabolites have anxiolytic activity
very long acting anxiolytic that does not tend to produce dry mouth or tachycardia
diazepam
what effects do barbituates have at sub-anesthetic doses?
no medullary depression
(no effect on resp/CV function)
orexin antagonist used as a hypnotic
suvorexant
used as prophylactic treatment in panic disorder
SSRIs
(due to increased synaptic availability of serotonin)
used to treat acute panic attacks
benzodiapezines
alprazolam specifically
benzodiazepine antagonist
flumazenil
flumazenil can be used in overdose of
benzodiazepines
non-benzodiazepine BZ1 agonist used as a hypnotic
zolpidem
zaleplon, esZopiclone as well
H1 antagonist that is a common OTC sedative
diphenhydramine
sedative that acts orexin antagonist
suvorexant
sedative that acts as an agonist at the MT1 and MT2 melatonin receptors
ramelteon
melatonin agonists
ramelteon
orally available benzo that is sufficiently fast acting to be used in treating panic attacks when they occur
alprazolam
non-depressant anxiolytic that is a partial agonist of 5-HT1A receptors
buspirone
onset of buspirone typically takes how long?
1-2 weeks of treatment
duration of action of lorazepam
intermediate
duration of action of diazepam
very long acting
(half life 43 hours)
rapidly and short acting benzo with profound amnestic effects
no clinical uses
flunitrazepam
(date rape drug)
short acting benzo administered IV as a preanesthetic and anesthetic agent
midalozam (versed)
partial agonist at 5-HT1A
slow onset of action 1-2 weeks
dysphoric at high doses
buspirone
used for generalized anxiety and as prophylaxis for panic disorder
SSRIs
H1 blocker
antipruritic, antiemetic
used pre and post operatively
hydroxyzine
melatonin receptor agonist indicated for insomnia with prolonged sleep onset
ramelteon
-rexants
orexin antagonists
block actions of orexins
indicated for difficulties with sleep onset and/or sleep maintenance
-rexants
H1 blocker
common OTC sedative
diphenhydramine
blocks 5-HT reuptake, H1, and a1 receptors
classified as antidepressant, but so sedating it’s used as a hypnotic
trazodone
benzo available in nasal spray for frequent seizure activity
midazolam
benzo that can cause rebound anxiety
alprazolam
[…] acting benzos are more likely to cause withdrawal symptoms
short
which benzo is used for it’s particularly amnestic side effects?
midazolam
increase the affinity of GABA receptors for GABA, increasing the likelihood of channel opening
benzo
which barbiturate is the most lipophilic, and therefore has the fastest CNS penetration and accumulates in adipose tissue?
thiopental
(phenobarbital is the least)
which barbiturate is the longest acting?
phenobarbital
which barbiturate is ultra short acting and available in IV formulation?
thiopental
(faster CNS penetration, most accumulation in adipose)
