Cocaine Flashcards

1
Q

Is cocaine a CNS depressant or stimulant?

A

CNS stimulant

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2
Q

What are the forms of cocaine? (2)

A

Crack
Cocaine HCl powder

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3
Q

What locations does cocaine act? (3)

A
  • Local anesthetic, decreases axon signaling
  • Acts on the reuptake mechanism on nerve endings, psychoactive drug use
  • Affects reuptake of dopamine (addiction due to this), noradrenaline, serotonin
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4
Q

When was cocaine first used?

A

1844, natives chewed on the leaves of the coco plant

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5
Q

What was cocaine first used as a local anesthetic for?

A

The eye, dentists used it for teeth too

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6
Q

Where does cocaine come from now?

A

Mostly Columbia and South America

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7
Q

How is crack cocaine administered?

A

smoked

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8
Q

How is Cocaine HCl administered?

A

sniffed or injected

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9
Q

Pharmacodynamics of cocaine, what does it act on (2)?

A
  1. Blocks voltage-gated sodium channels – blocks axonal conduction (other sites, heart, conduction of electrical system, all excitable tissue)
  2. Blocks neurotransmitter reuptake
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10
Q
  1. Blocks neurotransmitter reuptake
A

a. Blocks reuptake of dopamine, noradrenaline, serotonin
b. Neurotransmitter/sodium symporter family (sympathetic nervous system is very active)
c. Effect in the reward pathway due to increase in dopamine, since reuptake is blocked

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11
Q
  1. Blocks voltage-gated sodium channels – blocks axonal conduction (other sites, heart, conduction of electrical system, all excitable tissue)
A

a. CNS: excitation (convulsions) then Inhibition (respiratory arrest)
b. Rapid administration may produce immediate death
c. Heart: Blocks the SA node or conduction causing cardiac arrest

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12
Q

Cocaine causes CNS excitation causing?

A

More blood flows to the heart and less to the intestines – fight or flight active
It is rarely used as a local anesthetic anymore

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13
Q

What are the main type of dopamine receptors affected by cocaine?

A

D2 receptors

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14
Q

administration (smoking or sniffing)?

A
  • Goes to heart then brain very quickly
  • No liver first pass
  • Blood from the lung does not go through the liver so it gets to the brain very fast
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15
Q

Administration (oral)?

A
  • First pass 75% metabolized, first used by natives of South America, the rise was very slow, not addictive
  • Absorption rapid at all parenteral sites (injection)
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16
Q

Is injection faster effect than sniffing?

A

yes, injection has a very fast absorption (a little faster than sniffing)

17
Q

What injury does nasal sniffing cause?

A

it causes intense vasoconstriction, nasal injury

18
Q

Distribution (where does cocaine go?)

A

Cocaine can go everywhere

19
Q

Distribution (does cocaine cross the BBB?)

A

It has no problem crossing the BBB

20
Q

How long does it take cocaine to reach the brain? Does it leave quickly?

A
  • Hits the brain quickly in about 6-7 minutes, then goes to other parts of the body
  • Leaves fast, therefore people take more hits
21
Q

Cocaine transesterification with ethanol causes?

A

toxic coca ethylene metabolite
o Toxicity similar to cocaine but worse
o Half life 3-5x cocaine
o Lethal dose is much lower
o Cardiac arrest is more common
o Chronic use: sever liver damage, cerebral damage

22
Q

Is excretion of metabolites fast?

A

No, metabolites can stay in the urine for days, cocaine metabolites can also be deposited in the hair

23
Q

What are the 2 big problems with cocaine use?

A
  1. cardiovascular
  2. CNS seizures
24
Q

Cardiovascular problems using cocaine?

A

a. Cardiac arrythmia, myocardial infarction
b. Ventricular fibrillation
c. Vasospasm (in brain too) constricted blood flow
d. Hypertension
e. Accelerated atherosclerosis
f. Stroke
g. Aneurysm (bulge in brain because of weak blood vessel)

25
Q

CNS problems using cocaine?

A

a. Agitated delirium
b. Subgroup of cocaine users
c. Dose not required high dose
d. Rapid and fatal
e. May involve variant D2 receptors linked to temperature control
f. The mechanism is not understood – no animal models
g. Hyperthermia - delirium and agitation - respiratory arrest – death

26
Q

Other problems using cocaine? (5)

A
  1. Acute pulmonary injury “crack lung”
  2. Death from trauma, murder, suicide, accidents, (get into more fights when angry)
  3. Chronic use – neuronal injury, excess dopamine is neurotoxic
  4. Fetal death abnormalities “crack babies” – fetal hypoxia, premature labor, vasoconstrictive effects of cocaine
  5. Cocaine-ethanol interaction
27
Q

How do dopamine receptors change during and after cocaine addiction?

A

Addiction: less dopamine receptors
Withdrawal: more receptors of a different type, less D2 receptors

28
Q

Withdrawal symptoms of cocaine?

A

Withdrawal – severe anxiety changes in noradrenaline system in brain
Block dopamine transporter, slow response, lower response to cocaine