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PMCOL 305 > Amphetamines > Flashcards

Amphetamines Flashcards

1
Q

What is Ma huang?

A

A traditional Chinese medicine herb that has been used therapeutically for 5000 years

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2
Q

Who is Lazar Edeleanu?

A

He synthesized alpha-methylphenethylamine (amphetamine) in 1887 to treat asthma

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3
Q

What does L-amphetamine do?

A

Raises BP, opens nasal passages, causes headaches

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4
Q

What does D-amphetamine do?

A

Has the same effects as L-form but also elevates mood and enhances energy

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5
Q

Why does meth have increased potency and brain effects in relation to L-amphetamine and D-amphetamine?

A

Increased lipid solubility due to the addition of a methyl group
Easier to enter the BBB

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6
Q

What can meth be made from?

A

Pseudoephedrine or ephedrine from over-the-counter decongestants
Commercial phenylacetone

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7
Q

What is the process to make meth from decongestants?

A

Nagai synthesis

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8
Q

What are the processes to make meth from commercial phenylacetone?

A

Reductive amination or Leuckart synthesis

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9
Q

Why are amphetamines able to bind to neurotransmitter transporters?

A

Because of their chemical similarity to catecholeamines

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10
Q

What comprises the catecholamine nucleus?

A

A phenolic group with 2 hydroxyl groups

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11
Q

How AMPHs be absorbed?

A

Ingested, injected, snorted, or smoked

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12
Q

What is ice?

A

HCl salt which is smokeable meth

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13
Q

What is the half-life of ice?

A

12 hours

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14
Q

What is the bioavailability of ice?

A

Effectively absorbed from the GI tract, 70-100% bioavailability

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15
Q

Does meth or cocaine last longer in the blood?

A

Meth lasts much longer than cocaine

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16
Q

Where are AMPHs distributed?

A

Brain, lungs, liver, kidney, spleen

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17
Q

What is the onset of AMPHs?

A

30-120 minutes

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18
Q

Where are AMPHs excreted?

A

Kidneys, sweat, saliva

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19
Q

What metabolizes meth?

A

Liver CYP2D6

20
Q

How is meth metabolized?

A

Meth is broken down into 4-HA and norephedrine which are stimulants
4-HA activates trace amino associated receptor (TAAR) which stimulates NE release and inhibits monoamine oxidase

21
Q

What is TAAR?

A

An intracellular GPCR

22
Q

What does MAO do?

A

Degrades monoamine NTs like DA, NE, 5HT

23
Q

What does CYP2D6*10 do?

A

It reduces the rate of metabolism, dopamine and other excitatory NTs last longer in the system

24
Q

What are the acute effects of AMPHs?

A

Euphoria, energy, aggression, grandiosity, decreased appetite
Sympathomimetic effects (NE)
Delusional parasitosis and perceptual disturbances ( increased 5HT release)
Locomotor activity (increased DA)

25
Q

What is punding?

A

At high doses, causes repetitive meaningless behaviours because too much DA leads to less movement selectivity in the basal ganglia

26
Q

What do AMPHs do to NTs?

A

Elevates the ability of DA, NE, 5HT

27
Q

Do AMPHs require DA-ergic neuron firing?

A

No, DAT transporter brings meth into nerve endings and also enter by diffusion (VMAT pumps)

28
Q

What is the mechanism of AMPHs at the synapse?

A

AMPH binds to DAT and enters the terminal
VMAT transports AMPH into storage vesicles which displaces DA into the cytoplasm
MAO is bound by AMPH and can’t degrade DA
AMPH-TAAR complex and cytoplasmic DA build-up reverse DAT, DA leaks across synapse resulting in a DA spike

29
Q

How do AMPH mechanisms differ from cocaine?

A

Smaller structure allows the transporter to complete transport
AMPH activates TAAR (activates phosphorylation-dependent signalling) that targets DAT which reverses transport

30
Q

What are the adverse effects of the acute use of AMPHs?

A

Poisoning from contaminants
Combining with other drugs can enhance stimulant effects (MAO inhibitors)

31
Q

How is AMPH tolerance achieved?

A

Depletion of DA, 5HT, NE via displacement of these NTs from terminals
Inhibition of tyrosine hydroxylase to reduce synthesis of DA and NE
Acute dosing reduces DAT function = reduced effects

32
Q

What are the symptoms of AMPH withdrawal?

A

Physical and psychological
Cravings, depression, lethargy, muscle pain, abnormal sleep, anhedonia, emotional volatility

33
Q

How long can AMPH withdrawal last?

A

Depends on dosing
Can last 12 months due to permanent damage

34
Q

How do users become dependent on AMPH?

A

Chronic AMPH dosing causes reduced cell-surface expression of transporters for DA and NE

35
Q

What occurs upstream of reduced transporter expression?

A

TAAR activation

36
Q

What are TAAR1 knockout mice more sensitive to?

A

DA activation

37
Q

What do TAAR1 agonists do?

A

Reduce effects of AMPHs

38
Q

What are the long-term consequences of AMPH use?

A

Weight loss
Skin breakdown
Sores, picking
Poor oral hygiene, tooth decay, jaw grinding (meth mouth)
Contaminants may be corrosive
Reduced saliva production

39
Q

What are the psychological effects of long-term AMPH use?

A

Psychological effects are exaggerated, sensitization
Unprovoked aggression, homicidal/suicidal thoughts, extreme anxiety

40
Q

Where is DA depletion significant after long-term use of AMPH?

A

Areas of the brain responsible for movement, memory, and decision making

41
Q

What kind of damage is done to DA, NE, 5HT terminals after long-term AMPH use?

A

When cells recover from MAO inhibition, elevated DA metabolism results in reactive species formation
Excitotoxicity stresses neurons and kills them, brain damage

42
Q

What underlies long-term symptoms of AMPH use?

A

Neuron loss in the limbic system

43
Q

Where is neuron loss most significant due to AMPH use?

A

In the cingulate gyrus

44
Q

What do hippocampal neuronal loss correlate with in meth users?

A

Word-recall issues

45
Q

What are meth users 75% more likely to develop?

A

Parkinson’s disease due to the death of DA-ergic neurons

PMCOL 305 (18 decks)

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