Exam 2: Cocaine

Question 1

produce modest stimulatory effects in the CNS

nicotine, caffeine, not scheduled

Answer 1

low-efficacy stimulants

Question 2

increase CNS activity by a significant amount
strong behavioral effects
addiction liability greater
abuse potential inc

Answer 2

high-efficacy stimulants

Question 3

cocaine

Answer 3

psychoactive substance extracted from leaves of coca plant

• coca leaves have 0.6-1.8% cocaine
• coca paste extracted from soaked and mashed leaves has 60-80% cocaine
• discovered and processed in 1860s

cocaine created from coca paste

Question 4

2nd most abused controlled substance

Answer 4

cocaine

Question 5

what schedule drug is cocaine

Answer 5

schedule 2 drug

• high potential for abuse
• known established medical uses
• severe psychological or physical dependence liability

Question 6

major current problem with cocaine

Answer 6

lack of purity!!
it is laced with ther substances only 50% is actually cocaine
- phentanol is a common laced substance - lethal = toxic

Question 7

forms of cocaine

Answer 7

cocaine salt, cocaine HCl : mixture of coca paste with HCl, readily water soluble

basic cocaine:
- freebase: dissolve cocaine HCl and ammonia, extract cocaine and ether (organic solvent)

crack: dissolve cocaine HCl mix with baking soda, heat, dry

Question 8

absorption of cocaine

Answer 8

route of administration:

• nasal (insufflation, snorting) - cocaine HCl
• IV injection, mainlined
• inhalation, smoking
• oral - rare since poor bioavailability

Question 9

nasal absorption of cocaine HCl

- bioavailability, onset of action, peak levels in brain, duration of action

Answer 9

bioavailability: 70%
onset: 30s-5min - snorting cocaine constricts blood vessels, slowing the absorption
peak in brain: 10-20 min
duration of action: 60-90 min

Question 10

injection absorption of cocaine HCl

bioavailability, onset of action, peak levels in brain, duration of action

Answer 10

bioavailability: 90%
onset: 10-60s
peak in brain: 3-5min
duration of action: 20-60 min

Question 11

another absorption f cocaine HCl besides nasal and injection

Answer 11

topical

Question 12

inhalation absorption - freebase/crack cocaine

bioavailability, onset of action, peak levels in brain, duration of action

Answer 12

bioavailability: 90%
onset: 1-2s
peak in brain: 10s-30min
duration of action: 5-15 min

Question 13

distribution of cocaine

Answer 13

cocaine = lipophillic - easily penetrates BBB and placental barrier

brain concentrations FAR exceed blood plasma levels
- important for addiction - bc of the speed

Question 14

metabolism of cocaine

Answer 14

rapidly broken down in about 2 hrs

by enzymes in BLOOD and liver into metabolites

Question 15

cocaine metabolites

Answer 15

benzoylecognine - broken down in bloodstream, inactive metabolite

ecgnonine methyl ester - broken down in liver - inactive metabolite

norcocaine - active metabolite broken down in liver - cytochrome p450s
- acute intoxication

Question 16

metabolism: alcohol and cocaine

Answer 16

alcohol slows cocaine metabolism

react together to form cocaethylene - greater effects than cocaine

Question 17

cocaethylene

Answer 17

• only known example where body forms new psychoactive compound from 2 others
• longer half life, but lower LD50
• more euphoria, increased cardiac toxicity
• seizures, liver damage, compromised immune system

Question 18

elimination of cocaine

Answer 18

-SLOWLY removed from brain but RAPIDLY removed from blood

1-5% excreted unchanged in urine

rapid fall of blood cocaine level: rush followed by a crash

Question 19

half lifes cocaine

IV, nasal, benzoylecognine

Answer 19

IV half life: 30-90min
Nasal: 30min-4.5 hr
Benzoylecognine: 14.5-52 hrs - detected in urine 2-3 days later if nasal, if chronic IV can detect for up to 10 days

Question 20

speed runs

Answer 20

to get the rush and avoid withdrawal
- short half life - snort every 40 min or inject every hr
=blood levels accummulate to toxic levels
- run continues until out of drug or something bad happens - seizure, overdose, heart stops

Question 21

eyes of a cocaine user

Answer 21

dilated!!!

sympathetic response

Question 22

stimulants are sympathomimetic - what does this mean?

Answer 22

they produce symptoms of sympathetic nervous system activation: dilated pupils, inc HR, vasoconstriction, hypertension, hyperthermia

low doses not harmful, high doses toxic or fatal

Question 23

what are some acute behavioral effects

Answer 23

feelings of exhilaration or euphoria
sense of wellbeing
inc alertness and energy
great self-confidence
inc aggression - not good impulse control 

immediately after smoking or IV: intense rush that is pleasurable
after oral or intranasal: euphoria without the rush - not as exhilarating

Question 24

behavioral effects of chronic cocaine use

Answer 24

panic attacks - sympathetic activation

temporary paranoid psychosis:

• hallucinations of touch, sight, taste, smell
• confusion, anxiety
• formication syndrome: people think bugs crawling all over their skin - may take chunks out of their skin

Question 25

physiological effects of chronic cocaine use

Answer 25

malnutrition and weight loss due to appetite suppression in sympathetic activation snorting: cocaine HCl - septal necrosis (tissue in nose dies off) or perforated septum (hole on inside of nose)

Question 26

vasoconstriction brain interrupts... which can lead to ....

Answer 26

blood flow to brain | stroke

Question 27

cocaine blocks what reuptake transporters

Answer 27

DA, NE, 5-HT

Question 28

cocaine has highest binding affinity for

Answer 28

5-HT | but DA is most important for reinforcing and addictive properties

Question 29

cocaine increases...

Answer 29

DA in the nucleus accumbens indirectly through PFC

Question 30

glutamate neurons in the PFC ecite

Answer 30

DA neurons in the VTA

Question 31

more NE leads to

Answer 31

inc glutamate and inc activation of VTW dopamine neurons

Question 32

what is PET imaging used for

Answer 32

estimates DAT occupancy by cocaine | once a certainminimum level is reached the subject may feel a high

Question 33

intensity of the high depends on

Answer 33

amount of DAT occupancy - rate at which DAT occupancy occurs - distribution speed - baseline level of DA activity in mesolimbic pathway

Question 34

increased NE levels activates

Answer 34

arousl centers and sympathetic nervous system - dilates pupils

Question 35

increased DA lvels associated with

Answer 35

euphoria, inc energym psychosis, sense of confidence

Question 36

at high concentrations, cocaine inhibits...

Answer 36

voltage gated NA channels in axons, blocking nerve conduction

Question 37

when cocaine is applied locally what does it act a

Answer 37

anesthetic | prevents transmission of signals along sensory nerves

Question 38

what two numbing agents were developed from cocaine

Answer 38

procaine (novacaine) and lidocaine (xylocaine)

Question 39

when using occaine most start by what route of administration

Answer 39

smoking

Question 40

abstinence syndroe and cocaine (3steps)

Answer 40

crash: user feels exhausted and depressed mood withdrawal: anhedonia, anergia, anxiety, crave cocaine extinction: symptoms subside

Question 41

intermittent access to self administered cocaine causes

Answer 41

behavioral sensitiztion instead of tolerance

Question 42

sensitization is more likely following _______ in brain as opposed to high, constant concentrations

Answer 42

repeated spikes

Question 43

disulfiram

Answer 43

used to treat alcoholism showing promise in clinicl trials since people frequently use cocaine and alcohol together it prevents conversion of DA to NE inc DA prevents cocaine cravings by blocking withdrawal effects

Question 44

cocaine vaccine

Answer 44

cocaine is attached to a toxin immune system produces antibodies aainst toxin and cocaine prevents cocaine from reaching brain no high - lose interest

Question 45

cognitive behavioral therapyy (CBT)

Answer 45

restrcting thught processes and training perso to avoid their triggers

Question 46

structural abnormalities in chronic cocaine users

Answer 46

``` PFC ACC insula dorsal striatum amygdala thalamus ```

Question 47

functional changes in chronic cocaine users

Answer 47

impulse control and working memory - PFC verbal learning an memory - temporal lobe performance on psychomotor tasks - dorsal striatum decision making - PFC