amphetamines Flashcards

1
Q

where are amphetamines derived from

A

chinese medicine herb ma huang (5000 years)

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2
Q

who is credited with synthesizing AMPH and when

A

lazar edeleanu, 1885

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3
Q

what are the effects of L-amphetamine

A

raises BP
opens nasal passages
causes headache

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4
Q

what are the effects of D-amphetamine

A

same as L-amphetamine
also enhances mood and energy

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5
Q

how does meth have increased potency and brain effects?

A

lipid solubility

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6
Q

what are the 2 ways of synthesizing meth

A

pseudoephedrine (hydroiodic acid + red phosphorus) - nagai

from phenyl acetone (lamarck or reductive amination)

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7
Q

how are AMPHs absorbed

A

smoking injection snorting ingesting

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8
Q

what is the smokeable version of meth & what is its half life

A

ice, 12 hours

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9
Q

how is ice absorbed & what is its bioavailability

A

GI tract 70-100

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10
Q

what metabolizes meth and AMPH

A

cyp2d6 in liver

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11
Q

what are the stimulants that AMPH is metabolized into

A

4HA and NE

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12
Q

what does 4-HA act

A

inhibit MAO and activate TAAR and stimulate NE

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13
Q

what is the enzyme that reduces rate and what is the demographic distribution of its effect

A

cyp2d6*10
10% caucasions, 75% east asians

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14
Q

how is AMPH/METH distributed?

A

brain lungs liver kidney spleen

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15
Q

what is the onset of AMPH/METH

A

30-120 min

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16
Q

what is the half life of METH

A

12+ hr half- life 10-20 hours

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17
Q

what is the half life of AMPH?

A

11 hr half life, 3-12 hr

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18
Q

how is METH/AMPH excreted?

A

kidney sweat saliva

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19
Q

what are the acute affects of AMPHs

A

euphoria, energy, aggression, grandiositty, decreased appetite

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20
Q

what causes the sympathiomimetic effects of AMPH?

21
Q

what causes the delusional parasitosis and perceptual disturbances of AMPHs?

22
Q

what causes the strange locomotor activity of AMPHs

A

increased DA

23
Q

which area of the brain controls selection of action of movement?

A

basal ganglia

24
Q

what is punding`

A

at high doses of AMPH, repetitive meaningless behaviors

25
does AMPH require DA-ergic neuron firing
nah
26
what brings meth into nerve terminals
DAT or diffusion
27
what pumps meth into storage vesicles
VMAT
28
what does AMPH increase the availability of
DA, NE, 5HT
29
where does AMPH cause a DA surge
NAc, basal ganglia
30
what are the 3 main mechanisms of AMPH
blocks reuptake & reverses transporter increase release into synapse inhibit MAO
31
what reverses DAT
AMPH-TAAR complex and DA build-up
32
how does AMPH mechanism differ from cocaine?
smaller structure allows transporter to complete transport intracellular GPCR TAAR
33
how does TAAR work?
acttivates phosphorylation depdent signaling that targets DAT
34
how can AMPH cause poisoning
contaminants
35
how does tolerance form for AMPH
DA, 5HT and NE depletion via displacement of these NTs from terminals inhibition of tyrosine hydroxylase reducing DAT function
36
how long does tolerance last for AMPH
days or weeks
37
what is the withdrawal for AMPH
physical and psychological craving, depression, lethargy msucle pain, abnormal sleeping patterns, anhedonia
38
how does dependence occur for AMPH
reduced cell surface expression for DA and NE
39
where does TAAR activation occur with respect to reduced transporter expression
upsteeam
40
what can reduce the effect of AMPH
TAAR1 agonists
41
what kind of mice are more sensitive to DA activation
TTAR1 knockout mice
42
what are the 3 main physical long term consequences `
weight loss, skin breakdown, sores/picking
43
how does AMPH cause decreased saliva?
alpha 1 on vessels , alpha2 on salivary glands
44
how does AMPH cause brain damage?
excitotoxicity stresses neurons and induces cell death
45
what happens as cells recover from MAO inhibition
elevated DA metabolism results in reactive species formation which damages cell membrane proteins and mito
46
how is damage measured
reduced volume/ reduced neurons
47
where is the most significant loss of neurons in the brain
cingulate gyrus
48
which losses correlate to word-recall issues in long-term METH users
hippocampal
49
how much more likely are METH users to develop Parkinsons
75%