cocaine Flashcards
what was the origional use of cocaine
as an anesthetic
what is the abuse potential for cocaine
high
what does cocaine do to mind (basic, 1 word)
euphoria
what is the main source of danger from cocaine
the cardiovascular effects
why does cocaine have the potential to cause damage to all organs (2)
lack of blood supply from vasoconstriction, increases blood clots
which country is Canadian’s major source of cocaine
colombia
how is most cocaine transported
in bricks of powder form
where does cocaine come from
coca plant
how do locals use the coca plant
they chew the leaves mixed with very basic substances to increase extraction(like lime)
how much paste comes from 500kg of coca leaves
1kg (0.2%)
how much paste comes from 5000kg of coca leaves
10kg (0.2%)
how do they extract active ingredients from coca leaves
add kerosene or gasoline
once the coca leaves and kerosene/gasoline are dried, what is left (and what is it made of)
cocaine paste, 75% cocaine but heavily contaminated with solvent
what is cocaine hydrochloride
when you add HCl to the paste
why do you want to make cocaine hydrochrolide (2)
because it makes it more easily transported and polar/water soluble
why is cocaine hydrochloride more water soluble
because HCl adds a charge (H+) so that makes it more water soluble
what are things that people cut cocaine with (add/ dilute to make more profit)
powdered milk, baby laxative, numbing anesthetics
what is levamisole
anti-helminthic drug given to cattle
what does levamisole do to the brain
mildly increase DA release
what does levamisole do to human body
cause purple discolouration and necrosis of tissue due to vasculitis
what is vasculitis
inflammation of vasculature
what % of cocaine is estimated (By DEA) to be contaminated
70%
why does levamisole make ears and tips of nose purple
because damages lining of vessels, RBC cant go in as easily, clots, immune response, no oxygen, tissues die (this happens a lot in extremities due to the fine vessels)
how fast is the onset when snorting cocaine
3-5 mins
how long do cocaine effects last when snorting
30-40 mins
how is cocaine absorbed when snorted
mucous membranes in nose
what happens to the nose of chronic snorters
why
the lose cartilage seperating nostrils
vasoconstriction + acidic erosion (hydrochoric acid of cocaine hydrochloride)
what is cocaine called when its in the form that can be snorted
cocaine hydrochloride
how fast is the onset when injecting cocaine
15-30 seconds
how long do cocaine effects last when injecting
10-20 mins
what are 2 dangers if the needle goes into an artery
severe vasoconstriction and necrosis
how does cocaine cause vasoconstriction (2)
prevention of NA uptake and decrease NO production
what happens if you try to smoke cocaine hydrochloride
it wont work
why cant you smoke cocaine hydrochloride
it will burn before it produces vapours so it is destroyed (both cocaine and HCL have pyrolysis at 195)
what is pyrolysis
degradation by heat
what temperature does cocaine pyrolysis happen
195
what temperature does HCl pyrolysis happen
195
what do you do if you wanna smoke cocaine hydrochloride
you want to convert it into a freebase form
what temperature does freebase cocaine vaporize at
98 degrees C
vaporizes before it burns
what are 4 steps to make freebase cocaine
- dissolve cocaine hydrochloride in water
- add base (ammonia)
- extract with ether (explosive, flammable)
- evaporate to dryness
what is the chemical reaction for making freebase
Coc-H+Cl- + NH3 –> Coc +NH4Cl
what are 2 ways to smoke cocaine
freebase and crack cocaine
how do you make crack cocaine (4 steps)
1-dissolve in water (low purity)
2-add baking soda (neutralize HCl)
3-heat
4-freebase will precipitate and be purified
is crack cocaine or freebase more pure
freebase
what is the chemical reaction for making crack cocaine
Coc-H+Cl- + NaCHO3 –> Coc +H2O + CO2 + NaCl
what is the onset effect for freebase and crack cocaine
6-10 seconds
what is the duration for freebase and crack cocaine
short, only a few mins
do people that smoke cocaine usually require repeated doses
yes
what is the major metabolite of cocaine
benzoylecgonine
what is benzoylecgonine
a major metabolite which appears within 4 hours of using cocaine
what is the metabolite of cocaine that is only found when taken with alcohol
cocaethylene
what is cocaethylene
metabolite of cocaine that is only found when taken with alcohol
what are 3 side effects of cocaethylene
potent vasoconstrictor, damage heart tissue
may enhance euphoria
what is methylecgonidine
pyrolysis metabolite that indicates that cocaine was smoked
which is the pyrolysis metabolite that indicates that cocaine was smoked
methylecgonidine
what are the 4 main cocaine metabolites
methylecgonidine
cocaethylene
benzoylecgonine
ecgonine methylester
can you get psychosis from cocaine
yes
what does cocaine do to your energy levels
increase
what does cocaine do to your euphoria
increase
what does cocaine do to your confidence
increase
what does cocaine do to your sexuality
hypersexual
what does cocaine do to mundane tasks
makes more pleasurable
what is the mechanism of action of cocaine (2) (physiologically, NOT IN BRAIN)
blocks sodium channels
stimulates sympathetic system
what does cocaine do to Na channels
blocks
what happens when Na channels are blocked by cocaine
prevents nerve conduction (no pain)
why can cocaine cause dysrhythmias
because blocking Na channels in the heart tissue inhibits depolarization
why can cocaine cause sympathetic stimulation
excess NT in synapse (DA NA A 5HT)
what does cocaine do to HR
increase
what does cocaine do to BP
increase
what does cocaine do to your weight
lose weight
what does cocaine do to sleep
insomnia
what does cocaine do to agitation levels
causes increase
what does cocaine do to DA in NAc
causes accumulation
what does cocaine do to transporter proteins that normally remove NTs
blocks
what does cocaine do to post synaptic receptors (2)
prolongs and greater stimulation
what are 2 important structural things in cocaine
why
the aromatic ring and amine group
mimics groups found in NTs like DA
why is the the aromatic ring and amine group important for the mechanism of action of cocaine
because they mimic the same groups found in DA and other NTs
which transporter does cocaine bind to and where
dopamine transporter, the same site as DA
what happens when cocaine binds to the DA transporter
it locks the transporter into a certain conformation so that it no longer is able to function (cant cycle through open and closed states)
what does DAT do normally
transports DA back into the presynaptic receptor to terminate the signal
what happens to presynaptic uptake of DA when cocaine is there
it is blocked
what happens do DA in synapse with cocaine present
it remains in the synapse
what happens to the signal when cocaine is present
it is prolonged
does cocaine influence phasic bursts of cocaine
no
does cocaine influence basal or phasic DA release
more so tonic because it just causes a massive buildup of DA
what happens to DA reusability with cocaine
its not reused as efficiently - you can run out of DA after a big binge
what happens to DA levels in the NAc with cocaine
increased
besides DAT, does cocaine effects other NT transporters
yes, noradrenaline and adrenaline and serotonin transporters are blocked too
what happens when you try to mimic cocaine effects with drugs that exclusively block DAT
you dont get the same effects (you need NA A 5HT)
is dopamine entirely responsible for the effects of cocaine by itself
no, you need NA A 5HT effects too
how do we know that NA and A are involved with cocaine too
because of cardiovascular effects - NA=hypertension, A=tachycardia
(more levels of them due to blockade of their transporter)
what happens to DAT activity in chronic users
it is increased
why can you be depressed in absense of cocaine
because DAT is increased so less DA in cleft
why is there an increased risk of stroke with cocaine
increase coagulation and impaired thrombosis (clot breakdown)
what is thrombosis
clot breakdown
what happens to HR and resp. with high acute doses + WHY
respiratory and circulatory failure due to effects on medulla
what is rhabdomyolysis
breakdown of muscle tissue
how does cocaine cause hyperthermia (2)
hyperactivity + vasoconstriction
what can hyperthermia cause
rhabdomyolysis
what does rhabdomyolysis cause (1 word)
myoglobinuria
what does myoglobinuria cause
kidney failure
what is myoglobinuria
myoglobin in urine
who gets psychosis with cocaine
chronic users of high doses
what is the increase of myocardial infarction within 1st hour after cocaine use
24 fold increase
what % of heart attacks between 18-45 year olds is cause by cocaine
25%
What does cocaine do to sympathetic output
increase
What does cocaine do to catecholamine release
increase
what 4 things happen with increased sympathetic output and catecholamines
increase HR and BP
coronary spams, vasoconstriction
what does increase HR and BP cause
increase O2 demand
what doe scoronary spams and vasoconstriction
decrease O2 supply
what happens with increased O2 demand and decreased O2 supply
ischemia and infarction
how does cocaine cause ischemia and infarction
sympathetic outflow, increase HR BP vasoconstrict/coronary spasm, more O2 demand less supply
what is ischemia
organ not getting enough oxygen to function
what is infarct
when parts of the heart dies off due to no oxygen - heart attack
what is withdrawal of cocaine like when compared to alcohol and sedatives
fairly mild
what is the most common characteristic of cocaine withdrawal
depression
what is “let down” from cocaine
when you feel depressed within 30 mins of cocaine use
what is “let down” severity linked to
dose and duration of use
what is the role of benzos in controlling acute symptoms
controlling agitation from acute intoxication
how do benzos help with acute cocaine
they decrease CNS effects and decrease NT release so that redeuces BP and HR
what 2 drug classes have been used to decrease acute cocaine mortality
benzos (52%) and antipsychotics (29%)
what is the first line of treatment for myocardial infarction
nitroglycerine
how does nitroglycerine work, mechanism of action
produces nitric oxide which is a vasodilator
how does nitroglycerine help the heart (3)
increases O2 to heart via vasodilation, reduces workload, reduces O2 consumption
what does cocaine do to NO production
inhibits!!!
how can you help treat hyperthermia with acute cocaine
cooling with ice water
what kind of drugs work well for decreasing the reward of cocaine
drugs that increase GABAergic activity
what does topirimate do
drug that enhances GABA-A receptor activity and inhibits glutamate receptor activity
what can topirimate do to cravings
reduce
