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PMCOL 305 > amphetamines > Flashcards

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?

A

NE

21
Q

what causes the delusional parasitosis and perceptual disturbances of AMPHs?

A

5HT

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
Q

does AMPH require DA-ergic neuron firing

A

nah

26
Q

what brings meth into nerve terminals

A

DAT or diffusion

27
Q

what pumps meth into storage vesicles

A

VMAT

28
Q

what does AMPH increase the availability of

A

DA, NE, 5HT

29
Q

where does AMPH cause a DA surge

A

NAc, basal ganglia

30
Q

what are the 3 main mechanisms of AMPH

A

blocks reuptake & reverses transporter
increase release into synapse
inhibit MAO

31
Q

what reverses DAT

A

AMPH-TAAR complex and DA build-up

32
Q

how does AMPH mechanism differ from cocaine?

A

smaller structure allows transporter to complete transport
intracellular GPCR TAAR

33
Q

how does TAAR work?

A

acttivates phosphorylation depdent signaling that targets DAT

34
Q

how can AMPH cause poisoning

A

contaminants

35
Q

how does tolerance form for AMPH

A

DA, 5HT and NE depletion via displacement of these NTs from terminals
inhibition of tyrosine hydroxylase
reducing DAT function

36
Q

how long does tolerance last for AMPH

A

days or weeks

37
Q

what is the withdrawal for AMPH

A

physical and psychological
craving, depression, lethargy msucle pain, abnormal sleeping patterns, anhedonia

38
Q

how does dependence occur for AMPH

A

reduced cell surface expression for DA and NE

39
Q

where does TAAR activation occur with respect to reduced transporter expression

A

upsteeam

40
Q

what can reduce the effect of AMPH

A

TAAR1 agonists

41
Q

what kind of mice are more sensitive to DA activation

A

TTAR1 knockout mice

42
Q

what are the 3 main physical long term consequences `

A

weight loss, skin breakdown, sores/picking

43
Q

how does AMPH cause decreased saliva?

A

alpha 1 on vessels , alpha2 on salivary glands

44
Q

how does AMPH cause brain damage?

A

excitotoxicity stresses neurons and induces cell death

45
Q

what happens as cells recover from MAO inhibition

A

elevated DA metabolism results in reactive species formation which damages cell membrane proteins and mito

46
Q

how is damage measured

A

reduced volume/ reduced neurons

47
Q

where is the most significant loss of neurons in the brain

A

cingulate gyrus

48
Q

which losses correlate to word-recall issues in long-term METH users

A

hippocampal

49
Q

how much more likely are METH users to develop Parkinsons

A

75%

PMCOL 305 (19 decks)

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