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Pmcol 305 > Cocaine > Flashcards

Cocaine Flashcards

1
Q

Three main consumable forms of cocaine

A

coca leaves
cocaine hydrochloride - white powder
free-base cocaine = crack

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2
Q

absorption

A

insufflation
inhalation of free-base smoke
injection

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3
Q

insufflation

A

absorbed through mucous membranes
~70% bioavailability
dissolves to pass membranes → creates HCl - corrosive to nasal structures
onset 3-5 min
duration 30-40 min

cocaine HCl pyrolyzes (breaks down with heat) before it vapourizes ~195 degrees

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4
Q

inhalation of free-base smoke

A

onset 6-10 sec
duration 5-30 min - intense
crack vapourizes at 98 degrees

lungs → left heart → brain = lots of drug fast into brain = greater euphoria

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5
Q

injection

A

onset 10-15 sec (longer than inhalation)
duration 10-20 min

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6
Q

metabolism

A

cocaine is hydrolyzed into benzoylecgonine within 4 hours of use - 40% degrades with exposure to water (spontaneously)

primarily liver CYP3A4
liver/plasma esterases generate ecgonine methylester (~35%)

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7
Q

methylecgonidine

A

by product of pyrolysis
metabolism of crack

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8
Q

co-administration of cocaine with alcohol

A

generates cocaethylene metabolite
both cocaine and cocaethylene are potent vasoconstrictors
= synergism - effect amplified

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9
Q

excretion

A

primarily kidneys
detectable in urine up to 4 days after use
2 weeks in chronic users

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10
Q

distribution

A

brain
spleen
kidney

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11
Q

acute effects

A

stimulant drug
= stimulating, invigorating
sympathomimetic → fight or flight
brain, heart, lungs, GI

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12
Q

physiological effects

A

anasthetic
dysrhythmias
sympathomimetic

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13
Q

anasthetic effect

A

blocks Na+ channels = blocks neurotransmission of afferent information → no pain

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14
Q

dysrhythmia

A

blockage of Na+ channels in heart alter rhythm

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15
Q

sympathomimetic effect

A

block reuptake of dopamine, serotonin, norepinephrine and epinephrine
increased heart rate, blood pressure
anorexia, insomnia, agitation, hyperthermia

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16
Q

effect on basal ganglia

A

repetitive, compulsive movements
stereotyped activity

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17
Q

effect on prefrontal cortex

A

influences planning, problem-solving, social behaviours

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18
Q

effect on nucleus accumbens

A

extremely rewarding
dopamine

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19
Q

effect on medulla

A

high dose can affect brain stem
respiratory and circulatory failure

20
Q

physiological mechanism

A

blocks transporter activity within synapses
leads to prolonged stimulation of post-synaptic nerves

aromatic ring and amine group mimic neurotransmitters

enhances VTA sensitivity to Glutamate and reward

21
Q

dopamine excess

A

in basal ganglia, prefrontal cortex, VTA,, and nucleus accumbens

22
Q

5-HT excess

A

underlies mood, sleep, appetite, and temperature dysregulation

23
Q

NE excess

A

underlies sympathomimetic effects

24
Q

acute adverse effects

A

irritability, hostility, anxiety, fear, restlessness
formication: delusion of crawling insects under skin
psychological events - depression, aggression, paranoia
increased acute infections in GI tract
nosebleeds
allergic reactions at injection sites, HIV

25
Q

potent vasoconstrictor

A

reduced blood flow causes tissue to die - can cause acute infections

26
Q

reinforcing mechanism of cocaine

A

blocks dopamine reuptake
keeps dopamine in synapse longer, enhancing levels

27
Q

dopamine transporter

A

dopamine triggers conformational change of transporter to allow it to move through

28
Q

mechanism of cocaine binding to dopamine transporter

A

cocaine binds to the same site as dopamine due to chemical mimicry
larger than DA - locks transporter in stable conformation = inactivation
not solely responsible for cocaine effects

29
Q

not just dopamine involved in cocaine mechanism

A

exclusive DAT blockers do not mimic cocaine effects

30
Q

cardiovascular effects

A

due to block of NE and EP reuptake
hypertension and heart rate

31
Q

effect on mood and appetite

A

due to 5-HT reuptake block

32
Q

cellular mechanisms of tolerance

A

exhaustion of dopamine biosynthetic pathways → depleted dopamine
= reduced euphoria
increase DAT efficiency to override blocking
phosphorylation to facilitate transport
in nucleus accumbens

internalization of D1 and D2 receptors via rapid mechanisms - shut off constant stimulation by removing receptors form membrane so they aren’t available to bind drug

33
Q

reverse tolerance

A

increased susceptibility to hyperthermia, convulsions, stereotyped movements

sensitization
down-regulated internalization after two weeks might cause D1 up-regulation
more receptors left functional - facilitate activity

basal ganglia and hypothalamus

34
Q

altered opioid-ergic signaling

A

tolerance
striatal dynorphin expression is induced (endogenous opioid)

35
Q

withdrawal

A

symptoms include depression, anxiety, appetite changes → all psychological
strong drug cue-associated cravings as long-term DAT efficiency increases

faster dopamine reuptake
decreased hedonic tone

relatively mild, ~ 30 min after use
exhausted DA circuits

36
Q

dependence

A

mild physical
intense psychological → hijacked reward pathway and circuit association
disincentivized addiction - anxiety, loss of motor control

37
Q

treating acute cocaine intoxication

A

drugs with opposite activity:
benzos
nitroglycerine
ice bath
butyrylcholinesterase

38
Q

benzos

A

control agitation and overstimulation
decrease bp and heart rate to counteract cardiac effects by decreasing NT release

39
Q

nitroglycerine

A

evokes NO production → counteract vasoconstrictive effects

40
Q

butyrylcholinesterase

A

experimental iv treatment
enzyme that degrades active chemical and causes rapid elimination of cocaine
extended enzyme half life 72+ hours

41
Q

maintaining abstinence

A

reduce drug cravings
topiramate - anti-seizure med that enhances GABAA receptor activity and inhibits Glu receptor activity

42
Q

long term consequences

A

cardiovascular disease
arrhythmias - arrest due to inhibited Na+ channels
constricts vessels
psychosis in high dose users
accelerated brain aging
rhabdomyolysis
increased stroke risk

43
Q

rhabdomyolysis

A

breakdown of muscle tissue due to hyperthermia (hypothalamus)
→ myoglobinuria and kidney failure

44
Q

increased stroke risk

A

increased blood coagulability
decreased fibrinolysis

45
Q

long-term brain effects

A

decreased brain volume and mass
reduced D2 expression in the striatum

Pmcol 305 (18 decks)

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