psychostimulants 2 Flashcards

1
Q

Dexedrine names

A

Chemical - (S)-1-phenylpropan-2-amine
Generic-dextroamphetamine
Trade- Dexedrine

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2
Q

Benzedrine

A

dextrolevoamphetamine

  • Racemic
  • Least potent
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3
Q

dexedrine

A

dextroamphetamine

Active isomer

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4
Q

Desoxyn

A

methamphetamine

-most potent in CNS

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5
Q

Amphetamine administration

A

All Forms
-oral

Methamphetamine

  • Intranasal
  • Intravenous
  • Inhalation
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6
Q

Amphetamine weak base absorbtion

A
  • increasing GI Absorbtion with Increasing PH

- Rapid Absorbtion by inhalation

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7
Q

Amphetamine onset and duration of action

A

Oral:
Onset in 30 minutes, duration 6 hours

Inhalation:
Onset in seconds, Duration 15 minutes

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8
Q

Amphetamine distribution

A

crosses the blood brain barrier

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9
Q

amphetamine metabolism

A

Via liver

First order

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10
Q

Amphetamine Elimination

A
  • Increased excretion at lower renal pH

- Antacids Decrease Excretion, Increase Duration

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11
Q

Amphetamine Half-Life

A
  • 6-36 hours Depending on Renal pH

- Metabolites Persist up to 3-5 days After Last Administration, much longer in heavy users

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12
Q

Amphetamine action at synapse

A
  • Enhances release of catecholamines
  • Blocks reuptake of catecholamines
  • inhibits monamine oxidase (MAO)
  • Agonist at Catecholamine Receptors
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13
Q

Amphetamine synapse stimulation

A

1) enters Neuron via Reuptake
2) Forces DA/NE from Vesicles
3) Inhibits MAO to Reduce DA/NE Breakdown
4) Reverses Transport of DA/NE into Synapse

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14
Q

MicroDialysis

A

Measurement of Transmitters and their Metabolites in specific Brain regions of behaving rats

-Amphetamine increases Extracellular NE and Da in Prefrontal Cortex

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15
Q

Amphetamine therapeutic usis

A

approved:
Narcolepsy
ADHD

off label:
Obesity
Depression

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16
Q

Attention Deficit Hyperactivity Disorder (ADHD)

subtypes

A
  • ADHD - Predominantly inattentive
  • ADHD - Hyperactive / Impulsive
  • ADHD - Combined
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17
Q

Attention ADHD: possible disfunctions

A

Frontal lobe
-Executive Functions and Working Memory

Executive functions (Right Prefrontal Cortex)

  • attention
  • planning
  • impulse control
  • mental flexibility
  • monitoring actions
  • PreFrontalCortex lesions (Right)
  • Distractibility
  • Disorganization
  • Impulsivity
  • Perseveration
  • Forgetfulness
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18
Q

Prefrontal Cortex inhibition

A
confers inhibition on other brain regions
-Motor and premotor cortices
-Basal Ganglia:
Striatum (caudate)
Subthalamic nucleus

Cerebellum via pons

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19
Q

psychostimulants effects on add

A

reset the balance of noradrenergic and dopaminergic neurotransmission in the prefrontal cortex
NE - alpha2A receptors
DA - D1 receptors

Too little alpha2A/D1 ratio leads to drowsiness
-to high ratio leads to stress, misguided attention/responses, Mental Inflexibility, stimulus bound

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20
Q

Attention Deficit Hyperactivity Disorder treatment formulations:
Amphetamines

A

Dexedrine- dextroamphetamine (1-3)

Adderall - amphetamine salts(1-3)

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21
Q

Attention Deficit Hyperactivity Disorder treatment formulations:
methylphenidates

A

Ritaline - Methylphenidate(2)
Concerta - Methylphenidate ER (1)
Daytrana - methylphenidate ER(1)

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22
Q

Attention Deficit Hyperactivity Disorder treatment formulations:
Strattera

A

Atomoxetine

  • non-stimulant
  • noradrenertic reuptake blocker
  • Somewhat less effective than psychostimulants
  • lower risk of abuse
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23
Q

Attention Deficit Hyperactivity Disorder treatment formulations:
vyvanse

A

Vyvanse - lisdexamfetamine (1)

  • Prodrug
  • Converted to D-amphetamine
  • Longer duration of action
  • Lower risk of abuse
24
Q

ADHD psychostimulant therapeutic effects

A
  • improve attention span and focus
  • increase ability to follow directions
  • decrease distractibility
  • decrease impulsivity, stubbornness, aggression
25
Q

Psychostimulant ADHD side effects

A
  • increased heart rate and blood pressure
  • Dizziness, headache
  • Insomnia
  • Poor appetite, weight loss
  • Suppressed growth
  • abuse potential
26
Q

ephedrine

A

amphetamine-like
(ma huang)
stimulant, anti-asthma

27
Q

fenfluramine

A

serotonergic

weight control

28
Q

phenylephrine

A

alpha1 agonist

decongestant

29
Q

Bath salts

A

cathinone (Khat extract)
synthetic cathinones
amphetamine-like structure
Amphetamine-like effects

30
Q

Drug Tolerance

A

reduced effect of a drug after repeated administration

increased dose restores original effect

Tolerance Varies with drug

Tolerance varies with drug effect

31
Q

mechanisms of tolerance

A

metabolic tolerance (dispositional)

Celllular Tolerance (Pharmacodynamic)

Behavioral Tolerance

Contextual Tolerance (Situational)

32
Q

Metabolic tolerance

A

increase in metabolism

33
Q

Cellular Tolerance

A

Pharmacodynamic

34
Q

Behavioral tolerance

A

functioning in presence of drug

35
Q

Contextual Tolerance

A

Context in which drug is taken induces tolerance

36
Q

psychostimulant tolerance

A

Rapidly forming

Slowly or not Forming

Reverse Tolerance (sensitization)

37
Q

psychostimulant Rapidly Forming Tolerance

A

Appetite suppression

Euphoria

Cardiovascular Effects

Lethal Effects

38
Q

Psychostimulant Slowly or Not Forming Tolerance

A

Effect on Narcolepsy

Effects on ADHD

39
Q

psychostimulant Reverse Tolerance

A

Seizures

Locomotion

40
Q

Drug dependence

A

physical dependence

psychological dependence

41
Q

physical dependence

A

withdrawal syndrome

opposite of acute effects

42
Q

psychological dependence

A

Reinforcing effect of Drug

“Drug Craving”

43
Q

Psychostimulant physical Dependence

A

Fatigue and exhaustion

Prolonged sleep

Depression or Crash

Intense Hunger

44
Q

Psychostimulant psychological dependence

A

Extremely powerful
intense craving
anhedonia (inability to feel pleasure)
self administration

45
Q

Cocaine ratings

A

Withdrawal: 3.5 to 4

Reinforcement: 1

1 is most serious, 6 is least serious

46
Q

models of drug dependence

A

physical dependence

positive reinforcement
incentive sensitization

47
Q

physical dependence model (Wikler)

A

physical withdrawal maintains dependence.

initial drug use
-
repeated drug use
-
physical dependence
-
Attempts at abstinence
-
Withdrawal symptoms
-
relapse

Then goes back up to attempts at abstinence

48
Q

Positive Reinforcement Model (Koob)

A

Reinforcement maintains dependence

initial drug use
-
positive reinforcement
-
repeated drug use
-
Attempts at abstinence
-
Compulsive desire to re-experience drug-induced euphoria
-
relapse

then goes back up to attempts at abstinence

49
Q

Positive reinforcement

A

Dopamine activity is what is reinforcing

50
Q

Cocaine Mesolimbic Pathway (DA)

A

Cocaine blocks DA reuptake amphetamine Stimulates DA release

Nucleus accumbens

51
Q

incensitive sensitivation model summary

A

brain becomes sensitized to effects of drugs
increased dopamine activity increases salience of rewarding stimuli
alters brain structure

52
Q

incentive sensitivation model

A
initial drug use
-
positive reinforcement
-
repeated drug use
-
Sensitization of drug "wanting" but not drug "liking"
-Attempts at abstinence
-
Compulsive desire for the drug due to a sensitized incentive salience system
-
relapse

then goes back to attempts at abstinence

53
Q

brain changing model

A
repeated drug administration
-
transcription factors
-
gene expression
-
Dendritic remodeling in Nucleus Accumbens
-
Drug Addiction
54
Q

neurotoxicity in striatum

A

amphetamine use leads to neurotoxicity of Dopamine transporter neuronws in striatum
-less afferents to striatum

55
Q

meth mouth

A

dry mouth
clenching
poor dental hygiene