psychopharm Flashcards
antipsychotic of choice in hx EPS
zyprexa
what % D2 blockade assoc w EPS vs clinical effect
80% vs 60-70
carbamazepine cardiac affect, conditions to avoid
slows conduction > avoid in AV block, sick sinus synd
carbamazepine effect on Na
SIADH –> hypoNa
atypical w highest risk EPS
risperdal
ALL antipsychotics block what receptors (to some degree)
HAM (+ D) histamine alpha1 muscarinic dopa
antipsychotic side effects from histamine blockade
sedation, wt gain
antipsychotic side effects from alpha1 blockade
sedation, dizziness, orthostatic hypotension
antipsychotic side effects from muscarinic blockade
sedation, dry mouth, constipation (anticholinergic)
antipsychotic side effects from dopa blockade
motor/EPS
amphetamine MoAs on DA (3)
1 competitively inhib DA presynaptic uptake by transporter
2 facilitates DA release from vesicles into cytoplasm & presynaptic neuron
3 promotes transporter-med reverse-transport of DA into cleft, indep of action-potential-ind vesicular release
–> inc extracell DA + longer DA rec signaling @striatum
class of mirtazapine
tetracyclic, NaSSA (noradrenergic & specific serotonergic antidepressant)
mirtazapine MoA
blocks presynaptic alpha2 rec –> 5HT1a activation & inc DA release
how does amiloride help w Li side effects
blocks Li entry thru Na channel of kidney –> reduces nephrogenic DI (polyuria 2/2 dec fluid resorption @distal tubules)
hypnotic to take in middle of night
zaleplon (shortest t1/2 1-2h)
ginkgo biloba indication + CI med
cognition/memory, warfarin
by what age is absorption & transportation of drugs same as adult
4mo
by what age are GFR & CYP metab same as adult
1yo
which CYP present at birth, last to develop
3A7 @birth (undetectable in adults), 1A2 last
CYP that metabolizes most drugs
3A4 (40-50%)
race most commonly affected by abnormal 2D6 metab & %
5-10% caucasians > AA > azns
galantamine MoA
reversible competitve inhib AChE + allosteric modulator of nicotinic AChRs
memantine MoA
glutamatergic NMDAR antag
effect of NSAIDs on Li
renal a constr –> dec Li clearance via renal excr –> inc serum lvl
sertraline CYP effect
> 100 inhib
MAOI MoA
inhib oxidative deamination of serotonin, NE, DA
MAOI HTN crisis mechanism
inhib tyramine metab @GI
t1/2 of Z drugs from shortest to longest
zaleplon 1-2h
zolpidem 2-3
eszopiclone 6
(ramelteon 1-3, temazepam 10-20, diazepam 40h)
Li lvl requiring HD in otherwise healthy pt
4-6
which SSRI would be most problemsatic with clozaril?
fluVOXamine (1a2 inhib)
initial side effects of high or low potency typical antipsychotics are similar to TCAs?
LOW (including wt gain)
EPS = HIGH potency!
rate of TD occurance in typical antipsychotics?
5% annually
what mechanisms contribute to sexual side effects of antipsychotics?
a1 rec, anticholinergic, antidopaminergic
increased risk of CV malformations with paxil vs other SSRIs
1.5-2x
what can be used to treat poor appetite as result of stimulant use?
cyproheptadine
how can cbz & vpa cause bleeding
thrombocytopenia/bone marrow suppression
which amphetamine isomer is most rapidly eliminated from body?
dextro-isomer in acidified urine
CBZ MoA
inhib voltgated & presynaptic Na channels > inhib glutamate release
topamax MoA
inhib Na channels, enhances GABAa rec, antag kainate @AMPA rec
VPA effect on GABA
INC
meds assoc w serotonin synd:
- antidepr/mood stab incl SSRIs, SNRIs, MAOIs, buspar, Li, CBZ, VPA
- amphetamines ie ecstasy
- analgesics ie flexeril, fentanyl, demerol, tramadol
- other: reglan, zofran, ergots, triptans, dexromethorphan, linezolid
most serious side effect of mirtazapine
agranulocytosis (1/1000), reversible
can also cause hypoNa, hypotension, neutropenia, urinary freq
Li effect on Na + how to correct
vs CBZ/VPA effect on Na
competes w ADH rec @kidney > inc water output (nephrogenic DI) > hyperNa
amiloride > blocks Li entry
CBZ/VPA > hypoNa
is Li like insulin or glucagon
insulin (lower bG > inc appetite > wt gain)
meds to tx NMS? benzo OD? opioid OD?
NMS: dantrolene
benzo: flumazenil
opioid: naloxone, naltrexone
indication/MoA for phentolamine
a1 blocker for extravasation of NE & HTN from pheo
buspar acts on what rec
5HT1a selective ptl agonist postsyn @raphe,cortex,hippocampus,ceruleus + inhib D2 presyn
topamax MoA for alcohol use do
in etoh use, GABA firing decd > disinhib/incd DA release from accumbens»_space; reinforcing etoh…disinhib GABA neurons @VTA mean its “hyperexcitable”
TPX incs GABA tone @accumbens > inhib GABA @VTA & antag glutamate > suppr etoh-ind DA release @ accumbens
meds assoc w inc risk depression: CV, repro, neuro, psych
CV: clonidine, hydralazine
repr: OCPs
neuro: amantadine, reserpine, levodopa
psych: benzos
ways to treat hypotension from MAOI
support hose, hydrate, salt, fludrocortisone, stimulants
serotonin synd sxs, cause, & resolution time
sensory change/paresthesias, sleep/vivid dreams, anxiety, agitation, flu like sxs, disequilib
dec synaptic serotonin
2w or 24h if restarted SSRI
clozapine OD
delirium, lethargy, hypotension, tachy, resp failure
a1 block (dizzy, sedation, hypotension), D2 block, M1 block (dry mouth, constip, sed), H1 block (sed, wt gain)
% pts who hypersalivate w clozaril
33%
prevalence of ebsteins anomaly w Li during pregn
1/1000 (compared to 1/20000)
trazodone MoA
active metab is agonist @5HT2A > ptl @2C, ptl @1A. it’s metabolized by CYP2D6 (actually blocked by traz @5HT2A/C)
+ selective inhib serotonin reuptake by brain presynaptosomes
benzo chemical structure determines what
t1/2 in body/metab
2keto: long t1/2 bc oxidation @liver slow
3hydroxy: shorter t1/2 bc conjug w glucuronide radical
triazolo: shorter t1/2 bc oxidized but ltd active metab
topamax MoA
inhib Na channels, enhances GABAa rec, antag subtype glutamate rec (kainate & AMPA)
VPA MoA
inc GABA
lamictal MoA
inhib volt gated Na channels & inhib glutamate
CBZ MoA
inhib volt gated & presyn Na channels
buspar MoA
5HT1A ptl agonist @postsyn hippocampus & cortex + full @presyn, D2/3/4 mild-mod ptl antag @presyn, a1 ptl ag
memantine MoA
NMDA rec antag (blocks glutamate overstim which can cause cytotoxicity & neuron death)
mirtazapine drug class
tetracyclic
doxepin drug class
TCA
is nicotine spray or inhaler faster to reach peak?
lozenge or gum?
how long does cigarette take?
SPRAY
LOZENGE
<1min (fastest)