Drugs of Abuse

Question 1

Mechanism of action of cocaine

Answer 1

Blocks reuptake of monoamines (especially dopamine)

Blockage of DA reuptake in the CNS related to rewarding effects

Question 2

Along with a drug of abuse, cocaine is a…

Answer 2

Local anesthetic

Blocks sodium channels

Question 3

Toxicities from cocaine include… (4)

Answer 3

Psychosis
Cardiovascular complications
Hepatotoxicity
Convulsions

Question 4

Effects of cocaine on the CV system

Answer 4

Increases heart rate, BP, and myocardial oxygen demand

Decreases oxygen supply by inducing coronary vasoconstriction, leading to myocardial ischemia

Question 5

4 ways to ingest cocaine

Answer 5

Orally
Inhalation
Injected (very fast effects)
Smoked (highly addictive)

Question 6

Which form of cocaine takes the longest time to onset?

Answer 6

Oral

Question 7

Which 2 forms of cocaine have the highest anticipated intoxication levels

Answer 7

IV

Smoked

Question 8

Cocaine causes a decreases in _____ in what part of the brain?

Answer 8

Decrease in glucose metabolism in the brain, especially in the frontal lobes

Question 9

3 ways amphetamines can be taken

Answer 9

Orally
Intravenously
Smoked

Question 10

Mechanism of action of amphetamines

Answer 10

At high concentrations it will compete for binding to the transporter but will also be transported into the terminal itself
Can bind to and inhibit the vesicular monoamine transporter
Dopamine cannot be repackaged into the vesicles, the intracellular concentration increases, and the amount of DA in the synapse increases

Question 11

Amphetamines can cause what symptoms

Answer 11

Fight or flight response
Alertness
Anxiety, severe apprehension, panic
Potent effects on DA in the reward center of the brain
Behavioral stereotypy (meaningless repetition of a single activity)

Question 12

Methamphetamine mechanism of action

Answer 12

Blocks DA reuptake and increases DA release

Question 13

Schedule 1 substances

Answer 13

No medical use

Highly addictive

Question 14

MDMA mechanism of action

Answer 14

Preferentially blocks the 5-HT transporter
Causes release of serotonin
Long term depletion of intracellular serotonin (24 hours - leads to depression, irritability)

Question 15

Acute toxic effects of MDMA

Answer 15

Hyperthermia

Dehydration

Question 16

When does serotonin syndrome occur

Answer 16

If MDMA is combined with other drugs that increase serotonin levels

Question 17

Symptoms of serotonin syndrome

Answer 17

Agitation or restlessness
Diarrhea
Fast heart beat
Hallucinations
Increased body temperature
Loss of coordination
Nausea
Overactive reflexes
Rapid changes in BP
Vomiting

Question 18

Hallucinogens

Answer 18

Alter consciousness
Distort perceptions
Also called psychomimetics
Do not induce dependence or tolerance
Do not stimulate dopamine release

Question 19

4 ways LSD can be taken

Answer 19

Orally
Inhalation
Injected
Transdermally

Question 20

LSD mechanism of action

Answer 20

Acts as agonist at 5-HT2a receptors
Modulates glutamate-mediated sensory, perceptual, affective, and cognitive processes
Increase glutamate release at cortical layer 5

Question 21

Phencyclidine and ketamine mechanism

Answer 21

Bind to NMDA-receptors as non-competitive antagonists and affect glutamate-mediated cortical neuron signaling
Work on interneurons that have NMDA receptors
Block the disinhibition of glutamate release

Question 22

2 major categories of hallucinogens based on the mechanisms

Answer 22

Partial agonists at 5-HT2a receptors (LSD, psilocybin, mescaline)
Block NMDA receptors (PCP, ketamine)

Question 23

The main psychoactive ingredient of cannabis is…

Answer 23

Delta 9 tetrahydrocannabinol

Question 24

4 ways to use cannabis

Answer 24

Smoked
Vaporizer
Oral
Sublingual

Question 25

First two endocannabinoids discovered

Answer 25

2-arachidonoylethanolamine (Anandamide, AEA) | 2-arachidonylglycerol

Question 26

Which cannabinoid holds the most promise for serious conditions?

Answer 26

Cannabadiol

Question 27

Cannabinoid binding and mechanism

Answer 27

Lipid soluble compounds that are released from post-synaptic membranes and diffuse back to pre-synaptic CB1 receptors Cause disinhibition of DA neurons by inhibiting the release of GABA

Question 28

Cannabinoids cause...

Answer 28

``` Euphoria Relaxation Increased appetite Prevent nausea Lower intraocular pressure ```

Question 29

Designer marijuana

Answer 29

Spice, K2 Do not contain tobacco or cannabis but produce similar effects to those of cannabis Contain synthetic cannabinoids that potently activate CB1 receptors

Question 30

What G protein do opioids act at?

Answer 30

Gi/o

Question 31

Mechanism of opioid action

Answer 31

In the ventral tegmental area Activation of mu opioid receptors selectively expressed on GABA neurons results in disinhibition of DA neurons and euphoria

Question 32

What channels are acted on from opioid receptors 1. At the presynaptic terminal 2. On the cell body

Answer 32

1. Cause the inhibition of Ca influx (get less GABA release) | 2. Enhance K efflux (hyperpolarization)

Question 33

Symptoms of opioid withdrawal

Answer 33

``` Yawning Sweating Weakness Nausea/vomiting Tremors Muscle jerks ```

Question 34

Methadone

Answer 34

Way to treat opioid withdrawal It is pharmacologically equivalent, but has a much longer half life to suppress withdrawal symptoms Can do slow dose withdrawal

Question 35

Naloxone

Answer 35

Opioid receptor antagonist | Precipitates withdrawal and abstinence syndrome in a dependent person

Question 36

Buprenorphine

Answer 36

Partial agonist at opioid receptor with high affinity Another way to treat opioid addiction (morphine) It competes at the same site, but still gives some efficacy Prevents the high, but also alleviates craving and drug seeking behaviour

Question 37

Which partial agonist is used to treat nicotine addiction

Answer 37

Varenicline

Question 38

Addiction is characterized by which 3 things?

Answer 38

Compulsive behaviour to take drug despite negative consequences Reinforcing behaviour (rewarding or pleasurable) Loss of control

Question 39

Acute effects of alcohol on 1. GABA receptors 2. Glutamate (NMDA receptors)

Answer 39

1. Activate | 2. Inhibit (non competitive antagonist)

Question 40

6 drugs that work on neurons in the nucleus accumbens

Answer 40

``` Opioids Cocaine Amphetamines Alcohol PCP Cannabinoids ```

Question 41

3 drugs that work in the ventral tegmental area

Answer 41

Nicotine Opioids Cannabinoids