5 - Cocaine

Question 1

consumable forms

Answer 1

• coca leaves
• cocaine hydrochloride
• free-form cocaine (crack)

Question 2

insufflation

Answer 2

• 3-5 min on-set
• 30-40 min duration
• 70% bioavailability
• dissolution creates acid that is corrosive to nasal structures

Question 3

inhalation of free-based cocaine

Answer 3

• 6-10 sec on-set
• 5-30 min duration
• inhaled before it degrades (crack vapourizes at 98C)

Question 4

injection

Answer 4

• 10-15 sec on-set

- 10-20 min duration

Question 5

CYP3A4

Answer 5

liver enzyme that metabolizes cocaine

Question 6

benzoylecgonine

Answer 6

• metabolite

- 40% produced by hydrolysis (without enzyme) within 4 hours of use

Question 7

ecgonine methylester

Answer 7

liver plasma generated from cocaine

Question 8

cocaethylene

Answer 8

metabolite generated when cocaine is co-administered with alcohol

Question 9

methylecgonidine

Answer 9

by-product of pyrolysis (smoking cocaine)

Question 10

excretion

Answer 10

• detected in urine for up to 4 days
• detected in urine for up to 2 weeks in chronic users
• sweat
• saliva
• breast milk

Question 11

half-life

Answer 11

12 hrs

Question 12

effects of cocaine

Answer 12

sympathomimetic

Question 13

physiological effects

Answer 13

• blocks sodium channels to prevent pain, therefore it’s anaesthetic BUT can cause dysrhythmias
• excess DA, 5-HT, NE, EP stimulates sympathomimetic effect
• excess DA in BG causes repetitive and compulsive movements
• PFC is affected as there is changes in planning, problem-solving, and social behaviours
• excess DA in NAc results in high euphoria
• high doses can affect medulla resulting in respiratory and circulatory failure

Question 14

dysrhythmias

Answer 14

problems with heart rate/rhythym

Question 15

physiological mechanisms

Answer 15

• block transporters in synapse
• longer stimulation of post-synaptic nerves
• aromatic rings and amine group mimics NTs resulting in excess DA, 5-HT, NE, EP
• enhances VTA sensitivity to Glu and reward

Question 16

adverse effects

Answer 16

• irritability
• hostility
• anxiety/fear/paranoia
• restlessness
• fortification
• depression
• infections in GI tract
• nosebleeds
• allergic rxns at injection site

Question 17

dopamine transporter (DAT)

Answer 17

• locks transporter in a conformation that inactivates it-

Question 18

cardiovascular effects

Answer 18

NE and EP in synaptic cleft without reuptake results in hypertension and change in heart rate, respectively

Question 19

tolerance

Answer 19

• decreased DA levels due to increased DAT efficiency and D1 and D2 receptors’ internalization results in decreased euphoria
• increased dynorphin in striatum to counter cocaine effects
• intermittent use causes sensitization

Question 20

dynorphin

Answer 20

opioid released in striatum

Question 21

withdrawl

Answer 21

• depression
• appetite changes
• anxiety
• cue-associated cravings
• DAT efficiency increases

Question 22

dependance

Answer 22

• mild (most users do not become addicted)

- 10-15% of snorters become addicted

Question 23

treating cocaine intoxication

Answer 23

• benzos decrease NT release
• nitroglycerine counteract vasoconstriction
• ice bath decreases body temp.
• butyrylcholinesterase through IV eliminates cocaine

Question 24

consequences of cocaine

Answer 24

• 1/4 of heart attacks in 19-45 year olds
• organs will die due to vasoconstriction
• accelerated brain aging and psychosis
• breakdown of muscle tissue
• increased risk of stroke due to blood clots