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Exam 3
Lecture 9- Cocaine and stimulants
99
Astronomy
7th Grade
10/27/2013

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Term
behavioral stimualnts:3
Definition
cocaine
ritalin
amphetamines
Term
MOA of behaviroal stimualnts
Definition
increase NE and DA
Term
antidepressants-3
Definition
amitriptyline
imipramine
trnascyclopromine
Term
MOA of antidepressant-2
Definition
blockade of Ne/5HT reuptake
inhibit MAO (transcyclo)
Term
legal recreational drugs-2
Definition
nicotine
caffeine
Term
MOA of legal recreational drugs-2
Definition
stimulate ACh
block adneosine recptor
Term
psychostimulant effects-3
Definition
increased appeptie
elevated mood
increased motor activity
Term
high doses of psychostimulants causes
Definition
psychotic behavior
Term
low doses of spychostimulants alter what-
Definition
response to emergency situation
Term
*lots of ppl use cocaine daily, # has been stable over the yrs
Definition
Term
cocaine addicts are young or old
Definition
young (12-39)
Term
the risk of using cocaine vs those that actually do it is _ in middle schooler?
Definition
higher
Term
what are the 4 routes for cocaine
Definition
oral
intranasal/snorting
inhalation
IV/mainlining
Term
whihc route of cocaine doesnt give feeling of rush
Definition
oral/chewing
Term
intrnasal use of cocaine isnt absorbed well bc of-2
Definition
vasoconstriction
HCL salt
Term
cocaine easily passes what 2 barriers?
Definition
BBB
placenta
Term
what is the half life of cocaine?
Definition
30-90 minutes
Term
how is cocaine metab?
which is the active metab, major or minor?
Definition
liver
minor
Term
the major metabolite of cocaine is?
how long is it present in urine?
Definition
benzoylecgonine
3 days (in aucte users)
Term
the msall metaolite of cocaine is-
Definition
norcocaine
Term
3 main effects of cocaine
Definition
local anesthetic
blood vessel contrictor
psychostimulant (strong reinforcement)
Term
MOA of cocaine
Definition
block reuptake of Ne and DA
Term
cocaine increases DA where-2
Definition
ventral tegmental
N accumbens
Term
physiological repsonse of cocaine-2
Definition
tachycardia
pupillary dilation
Term
delayed effects of cocaine-
Definition
long lasting anxiety areter 60-90 min
Term
what is the main reason for craving more cocaine?
Definition
long lasting anxiety
Term
high doses of cocaine=
Definition
tremors/seizures
Term
toxic effects of cocaine-2
Definition
anxiety, sleep deprivation
Term
highdose/long term cocaine use= -2
Definition
dysphoria
schizo
Term
what are the fetal effects of cocaine? -2
Definition
ADHD
low toelrance for frustration
Term
cardio effects of cocaine-2
Definition
arrthymia, stroke
Term
what other drugs have cocaine like effects-4
Definition
methamphetamine
methylphenidate
pemoline
fenfluramine
Term
ampehtamine related drugs were indicated for 39 conditions like schizo, hiccups, etc
Definition
Term
amphetamines MOA
Definition
increase monoamines in synaptic cleft (DA, NE)
Term
at high doses amphetamines cna inhibit what?
Definition
MAO B
Term
main effects of ampehtamines at low doses-2
Definition
behavior and psychomotor stimulation
Term
amphetamine increase DA in the _ leads to -4
Definition
mesolimibc pathway
alertness, euphoria, mood elevate, reduce fatigue
Term
whcih drug class has a potent appetite supressant effect
Definition
ampehtamines
Term
in adults amphetamines cna have what affect?
in children?-2
Definition
increased aggressiveness
ADHD, inhibit aggression
Term
moderate dose of ampehtamine (20-50 mg)
results in-2
Definition
insomnia
stimulate respiration
Term
high doses of amphetamine (>50 mgs) results in-
Definition
ampehtatmine spychosis (acute schizo)
Term
chronic use of amphetamines results in-4
Definition
Da depletion
tyrosine hydroxylase depletion
loss of DA recpt
loss of resposnviness
Term
tolerance of ampehtamine is acocmpanied by-3
Definition
dysphoria
sedation
lethargy
Term
look at slide 19 for progression of substance abuse
Definition
Term
the #1 caffeine abuser drinks
Definition
energy drinks (can be 500 mg per can!)
Term
what was the energy drink that started it all?
Definition
red bull
Term
FDA OTC stimulants (including 100 mg of caffeine in NoDoz) must have this wanring?
Definition
dont give to children <12 yo
Term
what doesnt have the warning dose of caffine?
Definition
the 500 mg energy drink cans!
Term
blackout in a can=
how many of these is unsafe?
Definition
energy drink + alcohol
7
Term
MOA of caffeine at dose <15 mg/kg
Definition
antag of adenosnine recptors
Term
MOa of caffeine at high conc (>25 mg/kg)-3
Definition
inhibits PDE3
increases intracell Ca
Term
caffeine blocks what adeonisne recptors?
Definition
1 and 2!
Term
adenosine recpt 1 does-
Definition
decreases NT release
Term
adeosine 2 recptor does what?-2
Definition
increase GABA
decrease DA infinty
Term
caffeine is poor/well abrobed after PO?
Definition
well
Term
half life of caffeine in young na delderly?
Definition
2.5-4.5 hrs
Term
caffein PK effects are reduced in what ppl
why?
Definition
smokers
CYP 450 1A2 induced
Term
half life of caffeine is _ with oral contraceptives?
what about last trimester?
Definition
2x increase
15x increase
Term
peripheral affects of caffeine-2
Definition
bronchodilation
diuresis
Term
CNS effects of caffeine-2
Definition
alertness, congition
Term
symptoms of caffeine intoxication-3
what dose does it occur at?
Definition
restlessness, arrythmia
>250 mg
Term
caffeine withdrawal main symtpom?
Definition
headache
Term
can tolerance devlop in caffeine?
Definition
yes, but not all effects
Term
what is the #1 prevetnable cause of death in the US
Definition
death related to smoking
Term
was there a large decreas ein smokers in the past decade?
Definition
no
Term
how mnay compounds make up cigarette smoke?
how man are carcinogenic?
Definition
4000
40
Term
nicotine is readily abosorbed thru-3
Definition
skin
lungs
mucous membrane
Term
how mnay puffs of cig are needed to occupy brain nicotinic recpt
Definition
3
Term
1/2 life of nicotine
Definition
2 hrs
Term
what is majority of nicotine metab by?-2
what is it metab to?
Definition
aldehyde oxydase (liver) and CYPs
cotinine
Term
what is the half life of cotinine
Definition
24 hrs
Term
nicotine causes _ release where?
Definition
DA
nucelus accumbens
Term
where does nicotine bind to to release DA?
Definition
a4b2
Term
where does nicotine bind on glutamte recptors?
where are these recptors located
Definition
a7 nicotinc presynaptic recpt'
VTA
Term
nicotine also desentizes the _ recptors
where?
Definition
postsynaptic GABA
VTA interneurons
Term
nicotine raises DA where?
Definition
mesolimbic pathway
Term
nicotine causes _ of the a4b2 nicotinic ACh recpt?
normally these recept are
Definition
opening
in resting ststae
Term
how long does it take for re-sensitization of the nicotine recptorsnad withrdrawl craving>
Definition
45 min
Term
chronic desensitizaiton of nicotine recpt causes the recptors to upregulate and makes amplified cravings***
Definition
Term
smokers have lower levels of?
where at?-2
Definition
MAO B
brain and periphery
Term
nicotine actions on the CNS-
Definition
activate ACH= stimulation
Term
low dose nicotine effects-3
Definition
increased alertness
stimulate respiration
possible vomitting
Term
at high doses what does nicotine do
Definition
tremors/convulsions
Term
repeated exposure to nicotine leads to
Definition
tolerance/neuroadaptation
Term
nictoine affects what organ systems-5
Definition
CNS
peripheral
GI
cardiovasc
exocrine
Term
what does nicotine do to GI-3
Definition
N/V/diarrhea
Term
what does nicotine do to Cardiovasc system-3
Definition
increase HR/CO/O2 consupmtion
Term
wht does nicotine do to exocrine glands
Definition
inital stimulation, then inhibition
Term
what are adverse disease caused by smoking?
Definition
atherosclerosis
MI
lung cancer
Term
nicotine withdrawal symtpoms-3
Definition
anxiety
restlessness
wt gain
Term
with smoking, nicotine levels rise slow/quickly
Definition
quickly
Term
trnasdermal dlivery of nicotine deleviers what kind of nicotine?
what can this do?
what doesnt it do?-2
Definition
steady levels
desentize receptrs/releive craving
phasic bursts like cigs for DA to reinforce pleasure
cant eliminate all cravings
Term
what is the nicotinic partial agonist
Definition
varenicline
Term
partial nicotine agonists do what?
Definition
stabilze the nicotine receptors in an intermediate state
Term
ACh effect on nicotine recptrs
Definition
short pulses of DA release
Term
nicotine effects on nicotinic recptors
Definition
prolonged openein of channels til desensitize
Term
NPA action on nicotinic recpt
Definition
small increase in openeing of channels for sustained small amnt of DA release
Term
what is the DA and Ne reuptake inhibitor?
Definition
bupropion
Term
look at slide 51 for advt of NPAs and bupropion
Definition
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