6 - Amphetamines

Question 1

ephedra sinica

Answer 1

what amphetamine was derived from

Question 2

Ma huang

Answer 2

ephedra used as traditional Chinese medicine

Question 3

Lazar Edelano

Answer 3

synthesized alpha-methylphenethylamine (amphetamine)

Question 4

L-AMPH

Answer 4

• methyl in to the page
• raises bp
• opens passages
• causes headaches

Question 5

D-AMPH

Answer 5

• methyl coming out of the page
• raises bp
• opens passages
• causes headaches
• elevates mood
• enhances energy

Question 6

methamphetamine

Answer 6

increased lipid solubility therefore an increase in potency

Question 7

making meth

Answer 7

• Nagai synthesis
• reductive amination
• Leuckart synthesis

Question 8

Nagai synthesis

Answer 8

pseudoephedrine/ephedrine from OTC used to synthesize meth

Question 9

reductive amination

Answer 9

add methylamine to phenylacetone

Question 10

Leuckart synthesis

Answer 10

add methylamine to phenylacetone

Question 11

structure of AMPH vs METH

Answer 11

meth has an extra methyl group than amph

Question 12

ice

Answer 12

• smokeable meth with a half-life of 12 hrs

- 70-100% bioavailability

Question 13

CYP2D6

Answer 13

liver enzyme that metabolized amph and meth

Question 14

stimulants in AMPH and METH

Answer 14

• 4-hydroxyamphetamine (4-HA)

- norephedrine

Question 15

4-HA

Answer 15

• activates trace amino acid receptor (TAAR)
• stimulates norephedrine release
• inihibits monoamine oxidase (MOA)

Question 16

trace amino acid receptor (TAAR)

Answer 16

intracellular GPCR that reverses DAT activity

Question 17

monoamine oxidase (MOA)

Answer 17

degrades NTs (5-HT, DA, NE)

Question 18

acute effects

Answer 18

• euphoria
• energy
• decreased appetite
• sympathomimetic
• formication
• punding (meaningless behaviour)

Question 19

AMPHs mechanism

Answer 19

1. AMPH enters presynaptic cell and blocks DAT
2. VMAT stores AMPH in vesicles
3. AMPH blocks MOA by binding to it
4. DA released into cytoplasm
5. AMPH binds to TAAR which reverses DAT activity

Question 20

AMPH vs cocaine mechanism

Answer 20

• AMPH is a smaller molecule, therefore it can fit in the transporter
• AMPH forms a complex with TAAR

Question 21

adverse effects

Answer 21

• contaminants

- combining with other drugs to increase effect

Question 22

tolerance

Answer 22

• DA. 5-HT, and NE displacement from terminals

- reduces DAT function

Question 23

withdrawl

Answer 23

• cravings
• depression
• lethargy
• muscle pain
• emotional volatility

Question 24

withdrawl period

Answer 24

can last up to 12 months due to permanent damage

Question 25

dependance

Answer 25

reduced receptors for DA, NE

Question 26

TAAR1 agonists

Answer 26

reduce the effects of AMPH

Question 27

long-term consequences

Answer 27

• weight loss
• skin breaking
• sores
• tooth decay
• jaw grinding
• corrosive contaminants from ice
• reduced saliva production
• sensitization
• unprovoked aggression
• suicical/homicidal
• damage to DA, 5-HT, NE terminals
• stresses neurons (apoptosis) therefore brain damage

Question 28

neuron loss in limbic system

Answer 28

• reduced volume indicated reduced neurons
• word recall issues observed due to loss in neurons in the hippocampus
• more susceptible to Parkinson’s due to loss of DA neurons
• reactive oxygen species production and stress due to calcium influx from nAChR activation