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PSYCH 478 > Amphetamine > Flashcards

Amphetamine Flashcards

1
Q

true or false - enactogens are readily absorbed from GI

A

true

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2
Q

does enactogens affect plasma levels

A

yes they peak after 2 hours

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3
Q

how is enactogen metabolized

A

through the liver by CYP450

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4
Q

where does MDMA have increased activity

A

at seratonergic neurons

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5
Q

_______ and stimulant effects are modulated by __

A

sympathomimetic ; NE

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6
Q

reinforcing effects are modulated by _____

A

dopamine

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7
Q

MDMA increased what hormone levels

A

oxytocin

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8
Q

what are the adverse effects of enactogens

A

increased HR, tremors and sweating and hypothermia

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9
Q

what is trismus

A

tightening of jaw muscles

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10
Q

what is bruxism

A

grinding teeth

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11
Q

true or false - trismus is a stereotypes behavior

A

false - bruxism

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12
Q

true or false - hyperthemia from MDMA can be fatal

A

true

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13
Q

true or false - there re serious withdrawal symptoms from MDMA

A

false - not medically serious

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14
Q

the crash of MDMA is similar to what other drug

A

cocaine

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15
Q

what are some persistent effects from MDMA use

A
  • > decreased 5-HIAA in csf
    -> decreased 5-HT transporter binding
    -> decreased hormone response to seratonergic challenge
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16
Q

Amphetamines are a large class of _________
originally based on the naturally occurring _____________.

A

stimulants; ephedrine

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17
Q

Amphetamine first synthesized in 1887, brought
to market in 1930s as ___________ as a
___________.

A

benzedrine; decongestant

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18
Q

What is the parent compound to the class of amphetamines?

A

dopamine

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19
Q

How are amphetamines administered? Which is the most common therapeutic route? Which is susceptible to binge use?

A
  • oral = therapeutic
  • IV or inhalant = binge
20
Q

What is the half-life of amphetamines? Is this shorter or longer than cocaine?

A

7-30 hours; longer than cocaine

21
Q

TRUE or FALSE: Amphetamine and methamphetamine are used
interchangeably in clinical context

22
Q

methamphetamine vs methamphetamine HCl

A
  • methamphetamine: more potent; higher BBB permeability; illicit use
  • methamphetamine HCl: smoking (crystal meth)
23
Q

What are the behavioural effects of amphetamines (other than psychosis, punding, and formication)?

A
  • euphoria or exhilaration
  • heightened alertness
  • increased confidence
  • reduced fatigue (insomnia)
  • improved performance on repetitive psychomotor tasks (Stereotyped behaviour)
  • enhanced athletic performance
24
Q

Describe psychosis induced by amphetamine administration.

A
  • Drug-induced, particularly in chronic users
  • Indistinguishable from schizophrenia
  • Use precipitates psychosis in schizophrenia
  • Can persist beyond periods of intoxication
25
What is punding?
stereotyped behaviours
26
Describe punding induced by amphetamines.
- useless repetitive tasks - abstain from eating, drinking, bathroom breaks - irritated or angry if interrupted
27
Describe formication induced by amphetamines.
- feeling of insects crawling on skin - common to pick at skin as a result
28
Which nerve terminals do amphetamines act at? Which NTs are affected?
- catecholaminergic nerve terminals - dopamine, norepinephrine (and 5-HT)
29
Amphetamine have lesser effects on 5-HT except ____________ amphetamines.
enactogenic
30
What are the 4 mechanisms by which amphetamines increase catecholamine release?
1. competitive inhibition of DAT/NET 2. exchange transport at VMAT 3. altered catecholamine transport via TAAR1 signalling 4. MAO inhibition
31
How does amphetamine competitive inhibition of DAT/NET increase catecholamines?
- dopamine and amphetamine are both substrates for DAT - amphetamine competes with dopamine transport --> elevated synaptic dopamine
32
Describe how amphetamine exchange transport at VMAT increases chatecholamines.
- amphetamine is substrate for VMAT/VMAT2 - amphetamines transported through VMAT by EXCHANGE WITH INTRAVESICULAR DOPAMINE (i.e. dopamine goes out of vesicles, into synaptic terminal)
33
How does amphetamine activation of TAAR1 lead to increased catecholamines?
- amphetamines bind intracellular receptor (Gs/Gq) involved in monoamine regulation - TAAR1 - TAAR1 --> PKC --> phos DAT --> dopamine EFFLUX --> non-competitive reuptake inhibition
34
Provide a summary for how amphetamines increase catecholamines.
- competitively inhibit reuptake through DAT - increase cytosolic dopamine levels by exchange transport at VMAT - increases DAT internalization and induces dopamine efflux by activating TAAR1 - inhibit MAO (at high dose), decreasing intracellular dopamine breakdown
35
Describe persistne effects of amphetamine use.
- prolonged use --> psychosis - hallucinations and paranoia (resembling schizophrenia) - can occur outside of intoxication in chronic users
36
In animals, methamphetamine doses result in long-lasting decreases in ______, ___________, and _______ in the striatum.
DA; tyrosine hydroxylase; DAT
37
review slide 13 image
go look
38
What form of amphetamins is in common use?
pseudoephedrine
39
Why does smoking methamphetamine HCl degrade tooth enamel? What is this exacerbated by?
- highly acidic; reduced self-care in heavy abusers - exacerbated by sympathomimetic and stereotypic effects (decreased salivation, dehydration, teeth grinding)
40
What are some clinical uses of amphetamines? Which is most common? Which form is illicit?
- narcolepsy - ADHD (most common) - nootropic; improve studying (illicit)
41
What is ADHD characterized by?
- increased locomotor activity and distractibility - difficult in sustained attention - high impulsivity - excessive motor activity
42
Why are psychomotor stimulants effective in treating ADHD?
- ADHD may occur through excessive DAT activity --> dopamine insufficiency - DAT density increased in ADHD adults - genetic evidence links some cases with polymorphism in the DAT gene
43
What is an example of an enactogenic amphetamine? What behavioural effects are seen?
- MDMA - communicative, introspective, empathic
44
Where are enactogens readily absorbed from? When do plasma levels peak? What is the half-life? What enzyme does liver metabolism occur by?
- GI - peak after 2 hours - half-life of 8 hours - CYP450 2D6
45
What are the drug effects of enactogens?
*Euphoria * Increased wakefulness * Increased endurance * Sense of well-being, sociability, and extraversion * Sense of closeness, tolerance, and empathy to others * Sexual arousal

PSYCH 478 (28 decks)

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