Drugs of abuse II

Question 1

What are the clinical uses for benzos?

Answer 1

Anxiety, sleeping disorders, convulsions etc

Question 2

What is the MOA of benzos?

Answer 2

Positive modulators of GABA-(A) receptors (increased Cl influx)

Question 3

How do benzos cause the euphoric effect in the brain?

Answer 3

Inhibit the inhibitory interneurons that connect to dopaminergic neurons

Question 4

Why don’t benzos also affect the dopaminergic neurons in the VTA of the brain, since these neurons also have GABA-(A) receptors?

Answer 4

These receptors lack the alpha subunit, and are thus less responsive.

Question 5

What are the two most commonly abused benzos?

Answer 5

Diazepam

Alprazolam

Question 6

What is the “date rape” drug?

Answer 6

Flunitrazepam

Question 7

What is Flunitrazepam?

Answer 7

Roofies

Question 8

What is the antidote to benzos? MOA?

Answer 8

Flumazenil–GABA-(A) receptor antagonist

Question 9

Why aren’t barbiturates usually abused? Which one is usually abused?

Answer 9

Low margin of safety

Pentobarbital

Question 10

What is the MOA of barbiturates? How do these produce the increased dopamine in the VTA?

Answer 10

GABA-(A) receptor agonist

Inhibit inhibitory interneurons

Question 11

What is the street use for gamma-hydroxybutyric acid (GHB)?

Answer 11

Date rape drug

Question 12

What is the MOA of GHB?

Answer 12

GABA-(B) receptor agonist on inhibitory interneurons

Question 13

What is the relative risk of addiction for CNS stimulants?

Answer 13

5

Question 14

What is the MOA of cocaine in the CNS?

Answer 14

Inhibits the dopamine transporter (DAT) on synaptic terminals of dopaminergic neurons, causing increased synaptic dopamine and epi levels

Question 15

What is the MOA of cocaine in the PNS?

Answer 15

In the peripheral nervous system cocaine inhibits voltage-gated sodium
channels resulting in blocked initiation and conduction of action potentials  used as local
anesthetic.

Question 16

What is the street name for methylene dioxy-methyl amphetamine (MDMA)?

Answer 16

Ecstasy

Question 17

Amphetamine-like CNS stimulants are structurally similar to what endogenous molecule?

Answer 17

Epinepherine

Question 18

What is the metabolite that the liver turns EtOH and cocaine into?

Answer 18

Cocaethylene

Question 19

What has a longer half-life: cocaine or meth?

Answer 19

Meth, by a lot: 12 hours compared to 1 hour

Question 20

What is the MOA of amphetamines?

Answer 20

decreased re-uptake via DAT and inhibits VMAT, causing instant release of dopamine

Question 21

What are the major adverse effects of CNS stimulant abuse?

Answer 21

MI

Cerebrovascular hemorrhage

Question 22

What is the generic name for ritalin? MOA?

Answer 22

Methylphenidate

Amphetamine

Question 23

What is the MOA of MDMA?

Answer 23

Causes the release of 5HT vira the serotonin transporter (SERT)

Question 24

What are the side effects of MDMA?

Answer 24

Hyperthermia
Dehydration secondary to all night dance party

Hyponatremia if too much water

Question 25

What are the long term effects of MDMA use?

Answer 25

Neurological problems d/t permanent serotonin depletion

Question 26

What are the long term effects of psychostimulant use?

Answer 26

Paranoid schizophrenia

Question 27

What is the relative risk of addiction with psychedelics (hallucinogens)?

Answer 27

1

Question 28

What is lysergic acid diethylamide (LSD)?

Answer 28

Ergot alkaloid

Question 29

What are the eye findings of LSD use?

Answer 29

Dilation

Question 30

What is psilocybin? MOA?

Answer 30

Hallucinogenic found in mushrooms. Converted into psilocin.

Question 31

What is the MOA of hallucinogens?

Answer 31

Increased glutamate release in the cortex, via thalamic excitation, and targeting of 5HT-2 receptors.

Question 32

What is the major risk with hallucinogenic use?

Answer 32

Risk to self and others

Question 33

What are the 5HT-2 receptor G protein?

Answer 33

Gq

Question 34

What are the flashbacks with hallucinogens?

Answer 34

Reproduction of visual effects of prior LSD trips years after use

Question 35

Why do hallucinogens pose such a low addictive rate?

Answer 35

Not much effect on dopamine release in the VTA

Question 36

What are the four hallucinogenic drugs?

Answer 36

LSD Psilocybin Ketamine PCP

Question 37

What is the MOA of ketamine?

Answer 37

Block the NMDA type glutamate receptors in the cortex and limbic system, causing a decrease of excitation in these areas

Question 38

What is the MOA of PCP?

Answer 38

Block the NMDA type glutamate receptors in the cortex and limbic system, causing a decrease of excitation in these areas

Question 39

What is the clinical use for ketamine?

Answer 39

Anesthetic

Question 40

What is the relative risk of addiction for opioids?

Answer 40

4

Question 41

What are the four most commonly abused opioids?

Answer 41

Codeine Heroin Morphine Oxycodone

Question 42

What is the MOA of opioids? (2)

Answer 42

Inhibition of GABAergic neurons via activation of mu-opioid receptors in the VTA, causing euphoria Inhibit kappa-opioid receptors, causing dysphoria

Question 43

What is the emergency antidote for opioid use? MOA?

Answer 43

Naloxone mu-opioid receptor competitive antagonist

Question 44

What is the NON-emergency antidote for opioid use? MOA?

Answer 44

Naltrexone mu-opioid receptor competitive antagonist

Question 45

What is methadone, and what is it used for?

Answer 45

Long acting opioid agonist (not as powerful) to reduce withdrawal symptoms

Question 46

What is opioid abstinence syndrome?

Answer 46

Opioid withdrawal

Question 47

What is codeine metabolized to?

Answer 47

Morphine

Question 48

What is the MOA of THC?

Answer 48

Inhibition of GABAergic | interneurons on dopaminergic neurons

Question 49

What is dronabinol?

Answer 49

medicinal cannabinoid approved for medical use

Question 50

What are the two synthetic cannabinoids that are approved for medical use?

Answer 50

Dronabinol | Nabilone

Question 51

What is the relative risk for addiction of the cannabinoids?

Answer 51

2

Question 52

What is the MOA of nicotine on the VTA?

Answer 52

Activates nicotinic receptors on dopaminergic neurons

Question 53

What are the two drugs used to treat nicotine addiction?

Answer 53

Bupropion | Varenicline

Question 54

What is the MOA of varenicline?

Answer 54

High-affinity nAChRs agonists | that compete for binding with nicotine