Cocaine & Amphetamines Flashcards

1
Q

routes of administration for cocaine

A

ingested
injected - dissolve with water, better high than snorting and no numb. QUICKLY GOES AWAY
snorted - most popular: rapid onset and facial/nose numbness… numbness>euphoria
smoking crack
applied topically

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2
Q

duration of effect for cocaine powder

A

1-3 hrs

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3
Q

duration of effect for cocaine crack

A

5-30 minutes

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4
Q

duration of effect for cocaine amph

A

2-12 hours

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5
Q

NT directly affected by cocaine

A

dopamine, norepinephrine, and serotonin

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6
Q

how is the tolerance of cocaine

A

moderate
with some reverse tolerance

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7
Q

how is the physical dependance vs psychological dependence of cocaine

A

phys = moderate
psyc = high

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8
Q

what are the withdrawal symptoms from cocaine

A

depression, anxiety, drug craving, and binging (can lead to an acute tolerance)

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9
Q

what schedule is cocaine under

A

1

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10
Q

what kind of a stimulant is cocaine

A

psychomotor stimulant

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11
Q

cultural use of cocaine

A

was found in coca leaves growing in south america: chewed up.. slower onset but better endurance and alertness

  • coca leaves were an important in inca culture: religious ceremonies and currency
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12
Q

where in SA was cocaine found

A

mostly columbia, then peru and then bolivia

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13
Q

freuds use of cocaine: 1850s

A

he was an early advocate for it: depression, fatigue, indigestion, asthma, syphilis, autism, morphine addiction and alcoholism
- eventually opposed it

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14
Q

medicinal use of cocaine

A

“medical miracle”
- used as an anesthetic
- patented tonics and elixirs (coca cola in 1880)
- treatment for depression and morphine dependence

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15
Q

harrison narcotic act

A

prohibited coke being sold OTC in 1916
- allowed govt to track users and tax opium/heroin/cocaine

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16
Q

past recreational use of cocaine

A

1970/1980: cocaine use by snorting or IV injection increased due to rock bands popularity (edgy and cool)
1984: crack cocaine started
mid 1980s: US established harsh penalties for possession/distribution since crack cocaine started to get really popular

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17
Q

why was cocaine not initially seen as addictive

A

phys withdrawal symptoms were not as bad

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18
Q

modern day use of cocaine

A

coke is the 3rd highest drug used in Canada via the general population (15+)
- 1st is alc (78%), 2nd is weed (14.8%)

upward trend in coke use since 2013

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19
Q

how much of the general pop used coke in the past year

A

2.5%

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20
Q

current canadian penalties for coke

A

unlawful possession = fine up to $1000 or 6 months imprisonment
- bigger penalties for bigger quantities
- driving while impaired is a criminal offence

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21
Q

BC decriminalization pilot program

A

jan23-jan26
adults with less than 2.5g of CERTAIN illegal drugs arent subject to arrest or criminal charges and drugs are NOT seized

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22
Q

UNODC report on cocaine

A

united nations office on drugs and crime
- global estimate of cocaine use is 0.37%
- AUS = 2.5%
- USA = 2.4%
- UK = 2.3%
- CAN = 2.5%

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23
Q

coca leaf type of cocaine

A

natural, taken orally, has very little abuse potential

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24
Q

coca paste type of cocaine

A

from cocaine sulfate, smoked

25
Q

crack type of cocaine

A

freebase cocaine dissolved in baking soda
- converted from cocaine HCl

smoked, gives a faster and more intense high
*crack is less flammable than freebase

26
Q

cocaine type of cocaine

A

comes from cocaine hydrochloride (isolated from leaves)

snorted, cannot be smoked since it breaks down at high temps

27
Q

basic pharmacology of cocaine

A
  • cocaine extracted from coca leaves is converted to HCl salt and crystallized
  • can be turned back into smokeable cocaine via freebasing (crack)
28
Q

how to take cocaine HCl

A

it is water soluble therefor can be taken orally, intranasally, or IV injection

  • cannot be smoked
29
Q

cocaine HCl vs freebase (SR BOTD)

A

HCl
- isolated from coca leaves
- taken topically, via injection, orally, insufflation
- 70-75% bioavailability from snorting
- 10-30sec onset from snorting
- 10 min for peak brain levels from snorting
- 2 hour duration of action

crack
- converted from cocaine HCl via baking soda
- inhaled aka smoking
- 90% bioavailability from smoking
- 1-2 sec onset from smoking
- 8 sec for peak brain level from smoking
- 5-15min duration of action

30
Q

cocaine absorption: IV injection and smoking VS snorting and oral use

A

IV injection and smoking = extremely fast absorption

snorting and oral use = slow absorption

31
Q

why does cocaine quickly distribute through the body

A

because it is water and fat soluble and is able to pass through BBB rapidly
*can also pass through placenta

32
Q

how is cocaine metabolised

A

via the cytochrome P450 enzymes in liver
- there is individual variation in uptake and metabolism of cocaine

33
Q

cocaine half life vs major metabolites half life

A

c: 0.5-1.5hr
mm: 8ish hours

34
Q

cocaine elimination

A

Excreted in the
urine (mainly) - detectable for up to 3 days
sweat
saliva/blood - detectable for up to 2 days
breast milk

*metabolites are detectable in chronic users for up to 2 weeks

35
Q

what factors affect cocaine in the system

A

weight
frequency
dosage
persons metabolism

36
Q

which receptors does cocaine block and how

A

DA, NE, 5-HT: by inhibiting their membrane transporters

37
Q

which pathway is critical for the behavioral effects of psychostimulants

A

DA pathway
- mesolimbic DA system plays a role in
reinforcement and motivational mechanisms

38
Q

which ion channels does cocaine inhibit and how

A

inhibits voltage gated Na channels = blocks nerve conduction
- applied locally this acts as a local anesthetic

39
Q

which anesthetics were developed from cocaine

A

procaine aka novocaine
and lidocaine aka xylocaine

40
Q

animal study for cocaine and mice

A

genetically modified mice w a functional dopamine transporter that is INSENSITIVE to cocaine, fail to self admin the drug
- DATki mice:

41
Q

rats and cocaine: correlation of behavioral responses and individual differences
in neurochemistry

A

Rats that were naturally high cocaine responders (HCR) showed strong
locomotor responses in the open field (compared to LCR or control aka saline)
*around 90 min mark, HCR rats differed significantly from control and LCR

42
Q

why were LCR rats able to clear out DA more effectively than HCR

A

LCR have greater baseline DAT expression and were able to clear DA in the NAcc and dorsal striatum more effectively

43
Q

mechanism of cocaine (human studies) - what is used to study this

A

PET imaging is used to estimate DAT occupancy

44
Q

what does the intensity of the high depend on?

A

the amount of DAT occupancy AND the
rate at which occupancy occurs
(e.g., smoking will cause rapid occupancy)

45
Q

Sympathomimetic drugs produce?

A

symptoms of sympathetic nervous system activation

46
Q

ST effects of Sympathomimetic drugs

A

Constricted blood vessels, dilated pupils, increased body temperature, increased BP…

Feeling of euphoria, exhilaration, well-being

Increased wakefulness and alertness

Enhanced self-esteem, self-confidenct

47
Q

effects of cocaine as dose increases

A

Bizarre, erratic, violent behavior is possible

Restlessness, irritability, anxiety, panic, paranoia

Tremors, muscle twitches

High doses can be fatal (seizures, stroke, heart failure…)

48
Q

effects of extreme use of cocaine

A

heart problems, seizures, death and addiction

49
Q

unusual side effect of cocaine use

A

formication: delusional parasitosis
- a delusion that insects are crawling in and
under one’s skin

50
Q

LT effects of cocaine use

A

Cardiovascular effects

Seizures

Sexual dysfunction

Risk to nasal cavities if snorting

Risk to lungs if smoking

Risk of injury or infections from cracked pipes

51
Q

when are the severe effects of cocaine most likely

A

with high dosages and in chronic users

52
Q

cocaine dependence and misuse

A

most people who try it dont progress to misuse BUT for those that do: use escalates, binges are more common, ROA can switch from snorting to crack or IV injection

53
Q

cocaine tolerance and withdrawal symptoms

A

acute tolerance
- WD symptoms: phys symptoms are not life threatening but psych symptoms are compelling

54
Q

for cocaine tolerance/sensitization, what do we consider?

A

pattern of drug exposure, time since last dose, response being measured

E.g., tolerance to locomotor-stimulating effects; sensitization to stereotyped behaviours

55
Q

chronic cocaine use: Molecular adaptations in NAcc include

A

decreased DA synthesis

decreased DA release

less DAT binding

less D2/D3 receptor binding

56
Q

cocaine dependency causes..

A

cognitive deficits: impulse control, issues with
working memory, decision making, etc.

57
Q

brain parts affected by chronic cocaine use

A

inferior frontal AND temporal gyrus, insula, anterior cingulate gyrus, thalamus, dorsal striatum

58
Q

effects of chronic cocaine use

A

regular high dose use:
- strokes, seizures, perforation of nasal septum if its snorted
- panic attacks, paranoid psychosis