Cocaine

Question 1

Active Ingredient Content

Answer 1

0.5-1% Cocaine

Paste: 60-80% concentrated

Question 2

Cocaine Forms - HCl Salt

Answer 2

H2O soluble - allows for rapid absorption via snorting or IV
25 mg/line
50-100mg/admin
Vulnerable to heat induced breakdown - can’t be smoked

Question 3

Cocaine Forms - “crack/rock” or Free Base

Answer 3

Not H2O soluble
Can smoke this form
Get 200mg/admin

Question 4

Absorption and Bioavailability of Cocaine

Answer 4

IV - fastest (2-5 mins)
Smoking (2-5 mins)
Snorting (45 mins to peak)
Oral - gut destroys it

Question 5

1/2 Life

Answer 5

30-90 mins

Rapidly and completely metabolized in plasma and liver

Question 6

Benzoyleconine

Answer 6

Inactive metabolite of cocaine that can be detected from 48 hours to 2 weeks (chronic users)
Can be used for drug tests

Question 7

Cocaethylene

Answer 7

Cocaine + Alcohol
active metabolite
1/2 life: 150 mins (3-5x of cocaine alone)
increases risk of dual dependency

Question 8

Mechanisms of Action

Answer 8

CNS stimulant
Anorectic
Psychomotor
Sympathomimetic
Schedule II drug

Question 9

Pharmacological Effects

Answer 9

Potent Local Anesthetic (blocks VG Na channels)
Vasoconstrictor
Pyschostimulant (behavioral addiction, reward and reinforcement, compulsive abuse)

Question 10

Cellular Mechanisms

Answer 10

Potentiates action of Monoamines (DA, NE, and 5-HT)

Inhibits VG Na channel

Question 11

Local Anesthetics

Answer 11

Procaine (novacaine) (inhibits VG Na channels)
Lidocaine
Xylocaine

Question 12

Effects of Cocaine on Monoamine Neurotransmission

Answer 12

Binds to monoamine transporter by competitive inhibition

• increased NT levels in synaptic cleft
• increased transmission at affected synapses

Question 13

Physiological Effects of Cocaine

Answer 13

Increased HR
Increased BP
Vasoconstriction
Bronchodilation
Increased Temp
Pupil Dilation
Decreased appetite
Increased plasma glucose
Fat Breakdown

Question 14

Effects on Attention

Answer 14

Increased alertness
Increased concentration
Decreases (postpones) fatigue

Question 15

Psychomotor Effects of Cocaine

Answer 15

Low doses - increased motor activity

Higher doses - stereotypies

Question 16

Acutely Toxic Dose of Cocaine

Answer 16

1-2 mg/kg

70-150 mg

Question 17

Cause of OD

Answer 17

Cardio - stroke/heart attack due to arrythmias, thrombosis or vasoconstriction
Seizure

Question 18

Progression of Effects with Continued Use for Cocaine AND Amphetamines

Answer 18

At first, euphoria, alertness, loss of anxiety
Then, more anxiety, less euphoria and increased fatigue
Then, Paranoia and sensory hallucinations

Question 19

Pathways Affected

Answer 19

NAc - DA activity here is involved with increased normal motor activity
Lesions - no cocaine induced increase in motor activity
(mesolimbic DA pathway)

Striatum - DA activity here is involved with stereotypies
Lesions - no stereotypies
(nigrostriatal pathway)

Question 20

Abstinence Syndrome - Crash

Answer 20

Extreme Exhaustion

Depressed mood

Question 21

Abstinence Syndrome - Withdrawal

Answer 21

Inability to experience normal pleasures
anxiety
lack of energy
craving

Question 22

Abstinence Syndrome - Extinction

Answer 22

Most symptoms subside

Craving is cue-induced

Question 23

Teratogenic Effects of Cocaine and Amphetamines

Answer 23

Teratogenic - causes abnormal fetal development/birth defects

Physiological Effects:
difficult labor
increased still births
increased premature deliveries
low birth weight
*microenephaly (small head size)
*specific organ problems (heart, CNS, renal, GI)
*rarer

Behavioral Effects:
Infants - more irritable and sensitive to stimuli
Toddlers - difficulty developing attachements and dealing with multiple stimuli, have a hard time with unstructured play, low tolerance for frustration, higher incidence of ADHD

Question 24

Damage to Brain

Answer 24

Dopaminergic pathways from the midbrain (substantia nigra, ventral tegmental area) to the striatum and nucleus accumbens
Thalamic Hemorrhages