med chem III quiz 6 anti-psychotics - hypnotics

first gen
phenothiazine
aliphatic
anit-emetic
ind - pediatric behavioral problems
high sedative effects

first gen
phenothiazine
piperazine
low sedative effects
50X more potent than chlorpromazine
prodrug ester

first gen
phenothiazine
piperazine
IV only
10X more potent than chlorpromazine
reduce dose for elderly

first gen
phenothiazine
piperazine
short term only
20X more potent than chlorpromazine

first gen
phenothiazine
piperazine
commonly used anti-emetic
suppositories as well
7.5X more potent than chlorpromazine

first gen
piperdine
prodrug discontinued
metabolite of thioridazine

first gen
phenothiazine
piperdine
parent drug
cardiotoxic agent
equipotent to chlorpromazine

first gen
thioxanthene
25X as potent than chlorpromazine
not for children <12

first gen
butyrophenone
DOC for tourette's
for PCP overdose
SE severe extrapyramidal effects
50X as potent as chlorpromazine

first gen
diphenylbutylpiperdine
ind - tourette's, not first line though
monitor ECG

may have a role in the tourette's syndrome

second gen
thienobenzodiazepine
ind - schizo, BPD, dementia related to alzheimers
oral disintegrating tabs
heavy sedation
less weight gain

second gen
dibenzothiazepine
multi receptor antagonist
no anticholinergic side effects
increased heart issues
less weight gain
extended release form

second gen
dibenzodiazpine
ind - if not responding to other agents
agranulocytopenia - must do blood work for refill
only dispense 1 week at a time
available through patient management system

second gen
benzisoxazole
ind - demential from alzheimers
      delay of relapse in long term Tx of schizo
no anticholinergic effects

second gen
benzthiazole
80 mg dose max --> QT elongation
metabolized by 3A4 & 1A2
no inhibition on CYP

second gen
agonist and antagonist properties
metabolized by 2D6
steady state reached in 14 days

second gen
benzisoxazole
active metabolite of risperidone
ER and injectable
antagonism of D₂ and 5HT_2A receptors
T1/2 - 23 hours, watch for accumulation in elderly

second gen
benzisoxazole
D₂ and 5HT_2A antagonism
alpha1 - antagonist --> titrate dose (severe orthostatic hypotension)

second gen
ind - acute adult schizo, bipolar 1 disorder
moa - very promiscuous
< 2% bioavailability orally
35% bioavailability sublingual

second gen
benzoisothiazol derivative
ind - adult schizo
black box warning - cerebrovascular AE
metabolized by 3A4

anti-psychotic
manic episodes
increase neutrophil count in chemo pts
competes with Mg possibly
watch for dehydration - toxic

1st drug for chorea
black box warning - increase risk of suicide
moa - reversible depletor of monoamines
         reversible VMAT2 inhibitor
significant CYP induction

increased Cu in the brain
treated with zinc acetate or D-penicillamine

anti-parkinson's
anti-cholinergic
not for children <3yo

anti-parkinson's
anticholinergic
idiopathic
T1/2 - 18-24 hours

antiparkinson's
anticholinergic
best tolerated in elderly with mild PK
lower incidence of peripheral SE

anitparkinson's
anticholinergic
quatenary
reduce other drugs dose when used adjunct

antiparkinsons
dopaminergic
direct agonist unstable photochemically

antiparkinson
dopaminergic
direct agonist D₃ & D₂ only
SE - hallucinations
      teratogenic
extensive 1A4 metabolism
restless leg syndrome
once daily Tx

antiparkinson
DOC - carbon monoxide poisoning
moa - produces increased dopamine release

antiparkinson
moa - dopamine agonist
use if unresponsive to levodopa
ergot

antiparkinsons
inhibits peripheral decarboxylase enzyme
does not cross BBB
SE - watch for blepharospasm

antiparkinsons
ind - relief of herpes zoster shingle pain and restless leg syndrome
prodrug converted in CNS
SE - dark urine and sweat

antiparkinson
used with wearing off syndrome
moa - selective and reversible inhibitor of COMT

antiparkinson
watch for fulminant liver failure
selective and reversible competitive inhibitor of COMT
metabolized by methyl hydroxylation and glucuronidation

antiparkinson
moa - irreversible monoamine oxidase type B suicide substrate inhibitor - CNS only enzyme

orally disintegrating MOA inhibitor

antiparkinson
adjunct or alone
irreversible MAO type B inhibitor
metabolized by 1A2
monitor for melanoma

combo product for parkinsons

possible used to slow the progression of parkinsons

antiparkinsons
used for end of dose wearing off episodes
used for severe emesis in poisoning cases
MOA - stimulates post synaptic D2 receptors
subQ only

antiparkinsons
non-ergot DA agonist
continuously delivered to avoid DA pulsation
transdermal

alzheimers
cholinesterase inhibitor
discontinued
monitor serum transaminase levels

alzheimers
cholinesterase inhibitor
centrally acting
has active metabolites
dose based on serum transaminase levels

alzheimers
cholinesterase inhibitor
centrally acting
metabolized by decarbamoylation
SE - N/V, anorexia and weight loss
transdermal patch available

alzheimers
first drug for severe stages
moa - blocks glutamate, uncompetitive open-channel antagonist
excreted unchanged in the urine

alzheimers
extracted from the bulbs of daffodil narcissus pseudonarcissus
cholinesterase inhibitor
metabolized by 2D6 & 3A4
SE - bradycardia

hypnotic
imidoazopyridine
ind - short term Tx of insomnia
MOA - modulation of GABA receptor
reduce dose in hepatic impairment

sublingual zolpidem

oral spray zolpidem

sublingual zolpidem for middle of the night awakening

hypnotic
pyrazolopyrimidine
short term management of insomnia
moa - specific binding to GABA omega1 receptor
japanese subjects have increased levels

hypnotic
ind - sedation of ICU pts
moa - relative selective alpha 2 agonist
injection only

hypnotic
hospital used
moa - similar to BZ's w/ less selectivity and higher abuse potential
CI in epileptics

benzo with shortest half life

benzo with longest half life

benzo with lowest hypnotic dose

benzo with quickest onset

benzo to be used if a full night sleep is obtained

first barb
can cause CNS depression and decreased IQ tests in kids
very long half life 50h

barb hypnotic
intermediate acting
onset of action 45 - 60 minutes
decrease dose in hepatic problems
T1/2 - 66-140 minutes

2 - barb sedative & hypnotic
short acting
onset of action 10-15 min.

pyrrolopyrazine derivative for insomnia
moa - allosterically coupled to BZ receptor
safer for long term use

idenofuran used of insomnia
moa - melatonin receptor agonist
ind - Tx of adults w/ trouble falling asleep
watch w/ hepatic deficiency

TCA for insomnia