Sedatives.Anticonvulsants.Antidepressants Flashcards
DOC for acute anxiety
benzodiazepines
DOC for GAD
benzodiazepines
buspirone
drugs used for panic disorder
SSRIs
drugs used for phobias
SSRIs
drugs used for OCD
SSRIs
drugs used for PTSD
antidepressants
drugs used for short term insomnia
sedative hypnotics
DOC for enuresis
TCA
major inhibitory neurotransmitter
GABA
what kind of channels associated with GABA receptors?
Cl-
hydroxyzine
antihistamine used as anti-anxiety med
drug that produces inhibition independent of GABA
barbituates
marked CNS depressant
causes euphoria
controlled drug
barbituate
drug used for induction of anesthesia
short-acting barbituate
thiopental
long-acting barbituates used for?
phenobarbital
anticonvulsants
kinetics of barbituates
induce CYP450s
liver metabolism
SEs of barbituates
CNS depression
paradoxical excitement
severe physio/psych dependence
CIs of barbituates
enhance porphyrin synthesis
pulmonary insufficiency
supra-additive effects (w/ other depressants)
pregnancy
withdrawal with barbituates?
yes
can be severe
toxicity of barbituates
low margin of safety with no ceiling effect
supra additive w/ other depressants
do we give stimulates with barbituate overdose?
no
increases mortality rate
how do we treat barbituate overdose?
diuresis and alkalization of the urine
benzos with no intermediate metabolites
lorazepam
oxazepam
metabolism of benzos
liver
CYP3A4
benzos with long duration
diazepam
flurazepam
benzos with intermediate duration of action
alprazolam
oxazepam/lorazepam
benzos with very short duration of action
midazolam
benzos: dependent or independent on GABA?
dependent
binds to receptors–increase affinity–prolonged action
benzos: ceiling effect?
yes
anxiety DOC
benzodiazepines
sedatives used for insomnia
flurazepam
temazepam
“hangover” effect
flurazepam
temazepam
sedatives/anxiolytics for status epilepticus
diazepam
lorazepam
what benzo can cause anterograde amnesia?
midazolam
used in prep for anesthesia
benzo used for mm relaxation
diazepam
what benzos are used to taper withdrawal?
chlordiazepoxide
diazepam
lorazepam
SE of benzos
CNS depression
paradoxical excitement
supra-additive
sleep related behaviors
disinhibition of suppressed behavior
benzos
especially in elderly
dependence with benzos?
yes but pts don’t usually increase dose
CIs for benzodiazepines
pregnancy
sleep apnea
elderly
withdrawal of benzos
abrupt discontinuation= rebound insomnia/anxiety= taper slowly
benzos ooverdose
generally safe= long deep sleep
benzodiazepine antagonist
flumazenil
reverses effects of benzos?
flumazenil
flumazenil SE
triggers withdrawal and seizures in patients who are physically dependent on benzos
CIs of flumazenil
hx of seizures
“Z”drugs
zolpidem
zaleplon
eszopiclone
effects of z drugs
sedative
no anxiolytic, convulsant, mm relaxant
MOA of Z drugs
bind to subtype of GABA receptor to increase GABA-medated inhibiton
use of z drugs?
insomnia
unique aspect of eszopiclone
long half-life=long-term treatment
what may increase half life of z drugs?
severe hepatic dz
SE of z drugs
GI CNS sleep-related behaviors rebound insomnia (after discontinuation) withdrawal sxs
suvorexant MOA
antagonist at orexin receptors
SE of suvorexant
HA
abnormal dreams
CI in pts with narcolepsy
suvorexant
melatonin analogue
ramelteon
how does ramelteon work?
promotes sleepiness w/o GABA effect
kinetics of ramelteon
addative sedation with other depressants
SE of ramelteon
drowsiness
dizziness
nausea
MOA of chloral hydrate
acts similarly to barbituates on GABA receptor
safety of chloral hydrate
low margin: high doses induce respiratory and vasomotor depression
long term SE of chloral hydrate
liver damage
fatal intoxication
benefit of chloral hydrate
cheap but not used often
buspirone MOA
partial agonist postsynaptic
full agonist at presynaptic
decreased 5-HT cell signaling/release
how long does it take to see buspirone effects?
2 weeks
additive effects with buspirone?
no
no mm relaxant, sedative, anticonvulsant properties
anxiolytic with low addiction potential
buspirone
jerking x60 sec
no LOC
simple partial seizure
impairment of consciousness <2 min
automatic mvmt-lip smacking, hand wringing
complex partial
loss of consciousness
originated from partial seizure
partial with secondary generalized tonic-clonic
loss of consciousness
tonic rigidity followed by tremor followed by clonic violent jerking
tonic clonic
staring
generally <30 sec
absence seizure
brief shock-like muscle contraction
myoclonic seizure
absence seizures associated with what channels?
voltage gated Ca channels
anticonvulsants that increase GABA transmission
phenobarbital
benzos
anticonvulsants that inhibit sodium channels
phenytoin
carbamazepine
lamotrigine
valporate
anticonvulsants that inhibit thalamic calcium channels
ethosuximide
valproic acid
which anticonvulsants induce CYP450s?
phenytoin
carbamaxepine
phenobarbital
phenytoin MOA
prolonging inactivation of Na channel
why is fosphenytoin IM injection?
water soluble
phenytoin elimination
first order at low levels then zero order at max capacity
drug interactions with phenytoin
warfarin
OCP
what increases metabolism of phenytoin?
carbamazapine
SE of phenytoin
gingival hyperplasia
hirstuism
teratogenic
DOC for partial seizures
carbamazepine
carbamazepine MOA
inhibits sodium channels– decreases transmitter release
other uses for carbamazepine
trigeminal neuralgia
bipolar d/o
pharmacokinetics of carbamazepine
induces liver enzymes–drug interactions
induces its own metabolism
drug interactions with carbamazapine
phenytoin
ethosuximide
valproic acid
what drugs inhibit carbamazaepine metabolism?
cimetidine
fluoxetine
isoniazid
erythromycin
SE of carabamazapine
GI double vision, ataxia blood dyscrasias teratogenic SJS
test for SJS
HLA-B1502
phenobarbital MOA
prolongs opening of GABAa receptor chloride channel
phenobarbital anticonvulsant uses
partial and generalized tonic-clonic
phenobarbital CI
pregnancy
lamotrigine MOA
inactivates voltage dependent Na channels
lamotrigine uses
partial seizures add on
absence seizures in children
SE of lamotrigine
dizzy, HA
teratogenic
hypersensitiivity
gabapentin MOA
GABA analogue
may increase GABA release
gabapentin use
adjunct for partial and generalized tonic-clonic
neuropathic pain
gabapentin SE
dizzy, drowsy ataxia, HA tremor weight gain teratogenic
pregabalin MOA
GABA analogue
binds to voltage-gated sodium channel-inhibt excitatory NT
pregabalin uses
anticonvulsant w/ sedative properties neuropathic pain fibromyalgia post-op pain pruritus restless leg syndrome
SE of pregabalin
peripheral edema dizzy fatigue weight gin xerostomia ataxia blurred vision GI Cat C
topiramate MOA
inhibits voltage-dependent Na channels– enhance GABA currents
topiramate use
broad spectrum
inhibit spread of seizures
SE of topiramate
dizziness sedaion nervous confusion Cat C decreased OCP
levetiraceam MOA
reduces glutamate release while increasing GABA release
levetiraceam use
partial, myoclonic, generalized tonic-clonic
SE of levetiraceam
dizziness
somnolence
ataxia
asthenia
tiagabine MOA
inhibits uptake of GABA
tiagabine use
adjunct for partial sizures
SE of tiagabine
nervousness
dizziness, tremor
Cat C
vigabatrin MOA
irreverisble inhibitor of GABA rransaminase which breaks down GABA
vigabatrin use
refrctory adult complex partial seizures
infantile spasm
SE of vigabatrin
constriction of visual field, retinal damage
drowsy
dizzy
weight gain
CI of vigabatrin
pre-existing mental illness
DOC for absence seizures
ethosuximide
ethosuximide MOA
reduces low threshold Ca2+ current in thalamus
SE of ethosuximide
GI
SJS
Cat C
valproic acid MOA
inhibits Na channels=increased GABA
valproic acid use
absence seizures
DOc for combo of absence and generalized tonic-clonic seizures
valproic acid
other uses for valproic acid
bipolar
migrain prophylaxis
SE of valproic acid
GI
hepatotoxicity
SJS
Cat D
CI of valproic acid
liver diz
drug interactions of valproic acid
inhibits own metabolism at low doses
inhibits metabolism of phenytoin, carbamazepine
clonazepam use
benzo
absence seizures
clonazepam SE
sedation
tolerance to antiseizure effect
drugs used for status epilepticus
diazepam
lorazepam
DOC for status epilepticus
diazepam
monoamine hypothesis of depression
enhancement of monoamine neurotransmission
neurotrophic hypothesis of depression
los of neutrophic agents contribute
BDNF
neuroendocrine hypothesis of depresion
dysregulation of the HPA axis
increased glucocorticoid release and decrease in brain glucocorticoid receptor activity
TCA MOA
inhibit uptake of Ne and 5HT
block muscarinic, alpha adrenergic and histamine receptors
tertiary amine TCA OMA
inhibit 5HT and Ne reuptake
secondary amine TCA MOA
more effect on NE reuptake
fewer CV effects, sedation
drug interactions with TCAs
common
metabolized by CYPs in liver
CNS SE of TCAs
drowsy, sedating
memory, cognition-anticholinergic effect
decreased seizure threshold
peripheral SE of TCAs
cardiac arrhythmias-TdP postural hypotension weight gain anticholinergic effects SIADH-hyponatremia sexual dysfunction
why is there postural hypotension with TCAs?
alpha1 blockade
uses of TCA
depression panic d/o chronic pain fibromyalgia enuresis
what can we use for enuresis?
imipramine
anticholinergic SE are more common with what TCAs?
tertiary
can TCAs be used in pregnancy?
yes
TCA overdose
very dangerous
TdP
severe hypotension
agitation
neuromuscular excitability
seizuresq
TdP
TCA Od
TCA drug interactions
serotonin syndrome w/ MOAI
fluoxetine (+other SSRIs) compete for metabolism=toxic levels
issues with TCA and SSRI together
compete for metabolism=toxic levels of TCA
TCA +sympathomimetic drugs
hypertension
TCAs and CNS depressants
potentiate sedation
restlessness mm twitching hyperreflexia sweating proceeds to hyperpyrexia, convulsions
serotonin syndrome
DOC for depression
SSRI–citalopram
SSRIs that inhibit CYP2D6
*fluoxetine
paroxetine
uses of SSRIs
depression panic d/o OCD social anxiety bulimia EtOHism
preferred SSRI in elderly
sertraline
issues with fluoxetine
inhibits CYP2D6
impairs BG in DM
agoraphobia DOC
SSRI
OCD DOC
paroxetine
social anxiety DOC
paroxetine
SE of SSRIs
Gi
CNS stimulation
sexual dysfunction/libido
photosensitivity
SSRIs with higher occurence of anxiety/insomnia
fluoxetine
sertaline
SSRI that may cuase sedation
paroxetine
drug interactions with SSRIs
serotonin syndrome- MAOI, St. johns Wort TCAs Warfarin phenytoin, carbamazapine beta blockers opioids
venlafaxine MOA
5HT and NE reuptake inhibitors
uses of venlafaxine
depression
neuropathic pain
post-menopausal hot flashes
duloxetine MOA
5HT and NE reuptake inhibitors
SE of duloxetine
hepatotoxicity
acute angle closure glaucoma
MAO A
metabolizes NE, 5HT and DA in CNS AND GI tract
MAO B
metabolizes DA in the CNS ONLY
GI effects: MAOA or MAOB?
MAO A
phenelzine MOA
inhibits both MAOA and MAOB
drug of last choice for depression
phenelzine
selegiline MOA
irreversibly inhibits only MAOB
use for selegiline
Parkinson’s
how long do MAOI effects last?
1-3 weeks after d/c because long half life and irreversible inhibition
SE of MAOI
HTN crisis
orthostatic hypotension
weight gain
anticholinergic effects
HTN crisis with MAOI
inhibition in GI tract=accumulation of tyramine–> release catecholamines–> crisis
how do we treat HTN crisis caused by MOAI?
alpha blocker
MAOI drug interactions
sympathomimetic–HTN
mepiridine, dextromethorphan, TCA, SSRI=serotonin syndrome
buproprion MOA
inhibits reuptake of DA
Zyban
extended release buproprion used for smoking cessation
SE of buproprion
seizures
mirtazapine
blocks presynaptic alpha2 receptors= increased release of NE and 5HT
mirtazapine SE
drowsiness-histamine blocker
atomoxetine MOA
SNRI
non-stimulant treatment for ADHD
atomoxetine
SE of atomoxetine
GI
insomnia
trazadone MOA
5 HT2a receptor antagonist
use of trazadone
often sleep aid or pain mgmt