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Neuro Exam 1
Lecture 6
51
Bartending
5th Grade
08/28/2013

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Term
definiton of a sedative drug
Definition
decreases pt acitivty and calms them
Term
defnition of a hypnotic
Definition
produces drowsiness like the onset of sleep
Term
how hard is it to rouse a person from the sleep due to a hypnotic?
Definition
very easy
Term
benzodiazepines target what drug system
Definition
GABA
Term
GABA is amde from what?
what is the converting enzyme?
Definition
glutamic acid
GAD(glut acid decarboxylase)
Term
which gaba receptor is ligand gated?
what ion does it increase? what does this cause?
Definition
A
Cl-> hyperpolarization
Term
which GABA receptor is metabotropic ?
where is it abdunant at in the body?
what substance does it decrease?
Definition
B
spine
NT release
Term
short lasting GABA A has high or low concentration?
Definition
higher inhibition abaility
Term
do BZs directly act on the GABA A receptor?
Definition
no!
Term
Gaba A receptor:
how many alpha subunits
beta?
gamma?
most common mammalian structure?
Definition
6
4
3
(A1)2(B2)2,(y1)
Term
BZs bind to which GABA alpha receptors?
which ones dont they bind to?
Definition
1,2,3,5
4,6
Term
GABA A alpha 6 receptors are found a lot where?
what does this control?
how do BZs affect motor control?
Definition
cerebellum
motor and balance
not at all
Term
what does the alpha 1 subunit control? -3
Definition
hynotic/sedation
anticonvulsant
antereograde amnesia
Term
what alpha subunit is resp for anxiolysis
Definition
alpha 2
Term
what is pi pi stacking
what is an example?
what amino acids form this?
Definition
weak bonding of parallels
multiple bonds are strong
DNA
aromatic: Phe, Tyr
Term
BZs are what kind of receptor mosulator of GABA?
this means?
Definition
a;llosteric
even at high doses they dont direct open the recpetor
Term
combo of BZ and _ can be lethal?
why?
Definition
alcohol
cause respiratoy depressoin
Term
what is the antidote for BZs?
what cna this drug not be an antidote for?-2
Definition
flumazenil
barbituates
ethanol
Term
BZs dont really affect what part of the sleep cycle?
Definition
REM
Term
which BZ is useful for status epilectus?
Definition
diazepam
Term
when do BZs have paradoxical effects
Definition
elderly pts
Term
pharmacological effects of BZs-4
Definition
sedation
reduced anxiety
anteretrgorade amnesia
reducded muscle tone
Term
PK of BZs-2
Definition
no effect on liver
usually long half life
Term
the metabolism of BZs invovles what 2 processes?
Definition
glucoronidation
excretion
Term
what is the BZ example most tlaked about?
Definition
Diazepam
Term
how do overdoses with BZs compares with barbituates and alcohol?
Definition
less dangerous
Term
ADEs of BZs -3
Definition
reduction of reaction time (traffic!)
ataxia/falls
addictive pro[perties
Term
what is the main addivtive properties?-2
which type of BZs have them more?
Definition
rebpound insomnia and anxiety
shjort acting
Term
whihc BZ is used for cocain withdrawal?
Definition
flunitrazepam
Term
BZs can also be used as?
Definition
date rapre drug (but no alcohol odor!)
Term
avoid using BZs with what type of ppl
Definition
former alcoholics
Term
withdrawal of BZs symptoms-2
Definition
tremor, dizzy
Term
long half life hypnotic BZs-2
Definition
flurazapem
quazepam
Term
short half lide hypnotic BZs-1
Definition
triazolam
Term
medium hal;f life BZs-2
what effect do they have?
Definition
estrazolam
temazepam
like a hangover
Term
what is the Z drug (non BZ)
what recpt is it more selective for?
what are other Z drugs like this
Definition
zolpidem
alpha 1
zaleplon
eszopiclone
Term
Zol[idem has mroe of this effect but less of this one?
what is its potential for abuse?
Definition
sedation
anxio;lytic
less than diazepam
Term
Z drugs are what kind of recpot modulators?
Definition
postive al;;lpsteric modulators (PAM)
Term
what Z drugs are alpha 1 selctive hypnotics?
what does this mean?
Definition
zaleplon
zolpidem
no withdrawal or depednce
Term
what barbituates where used for anesthesia?
how long are they effective for?
Definition
methohexital
thiopental
only few minutes
Term
what barbiutaes were used for pre OP sedation
Definition
amobarbital
pentobarbital
secobarbital
Term
which barbiutate was used for anticonvulsion
Definition
[phenobarbital
Term
at high doses barbituates CAN open GABA directly- what does this mean?
Definition
overdose is lethal!
Term
which type of dug class is strong inductioon of CYP 450s?
Definition
barbituates
Term
high doses of barbituaes does what? -2
Definition
respiratory and cariovasc depresison
Term
what effects do barbituates have? -3
what doesnt it have?-1
Definition
sedation, anticonvuls, REM supression
anxiolytic
Term
BZs are drug of chopice bc they have low/high therapuetic index?
Definition
high
Term
what drug is the agonist of melatonin
Definition
Ramelteon
Term
what does timulation of melatonin M! and MT2 recptors do?
Definition
induces sleep
Term
Ramelteon:
bioavilability? why? when is it 2x higher/?
primarly metab by what? so have to watch for this in what ppl?
Definition
1.8%; first pass metab; elderly
CYP1A2
smokers
Term
use melatonin to treat what?
what dont you use it for?
Definition
jet lag
imsonmia
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