dextrolevoamphetamine - Racemic - Least potent

psychostimulants 2 Flashcards by Harris Jordan

Dexedrine names

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

How well did you know this?

Not at all

Perfectly

Benzedrine

dextrolevoamphetamine

Racemic
Least potent

How well did you know this?

Not at all

Perfectly

dexedrine

dextroamphetamine

Active isomer

How well did you know this?

Not at all

Perfectly

Desoxyn

methamphetamine

-most potent in CNS

How well did you know this?

Not at all

Perfectly

Amphetamine administration

All Forms
-oral

Methamphetamine

Intranasal
Intravenous
Inhalation

How well did you know this?

Not at all

Perfectly

Amphetamine weak base absorbtion

increasing GI Absorbtion with Increasing PH

- Rapid Absorbtion by inhalation

How well did you know this?

Not at all

Perfectly

Amphetamine onset and duration of action

Oral:
Onset in 30 minutes, duration 6 hours

Inhalation:
Onset in seconds, Duration 15 minutes

How well did you know this?

Not at all

Perfectly

Amphetamine distribution

crosses the blood brain barrier

How well did you know this?

Not at all

Perfectly

amphetamine metabolism

Via liver

First order

How well did you know this?

Not at all

Perfectly

Amphetamine Elimination

Increased excretion at lower renal pH

- Antacids Decrease Excretion, Increase Duration

How well did you know this?

Not at all

Perfectly

Amphetamine Half-Life

6-36 hours Depending on Renal pH

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

How well did you know this?

Not at all

Perfectly

Amphetamine action at synapse

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

How well did you know this?

Not at all

Perfectly

Amphetamine synapse stimulation

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

How well did you know this?

Not at all

Perfectly

MicroDialysis

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

-Amphetamine increases Extracellular NE and Da in Prefrontal Cortex

How well did you know this?

Not at all

Perfectly

Amphetamine therapeutic usis

approved:
Narcolepsy
ADHD

off label:
Obesity
Depression

How well did you know this?

Not at all

Perfectly

Attention Deficit Hyperactivity Disorder (ADHD)

subtypes

ADHD - Predominantly inattentive
ADHD - Hyperactive / Impulsive
ADHD - Combined

How well did you know this?

Not at all

Perfectly

Attention ADHD: possible disfunctions

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

How well did you know this?

Not at all

Perfectly

Prefrontal Cortex inhibition

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

Cerebellum via pons

How well did you know this?

Not at all

Perfectly

psychostimulants effects on add

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

How well did you know this?

Not at all

Perfectly

Attention Deficit Hyperactivity Disorder treatment formulations:
Amphetamines

Dexedrine- dextroamphetamine (1-3)

Adderall - amphetamine salts(1-3)

How well did you know this?

Not at all

Perfectly

Attention Deficit Hyperactivity Disorder treatment formulations:
methylphenidates

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

How well did you know this?

Not at all

Perfectly

Attention Deficit Hyperactivity Disorder treatment formulations:
Strattera

Atomoxetine

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

How well did you know this?

Not at all

Perfectly

Attention Deficit Hyperactivity Disorder treatment formulations:
vyvanse

Study These Flashcards

Vyvanse - lisdexamfetamine (1)

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

ADHD psychostimulant therapeutic effects

Study These Flashcards

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

Psychostimulant ADHD side effects

- increased heart rate and blood pressure - Dizziness, headache - Insomnia - Poor appetite, weight loss - Suppressed growth - abuse potential

ephedrine

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

fenfluramine

serotonergic | weight control

phenylephrine

alpha1 agonist | decongestant

Bath salts

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

Drug Tolerance

reduced effect of a drug after repeated administration increased dose restores original effect Tolerance Varies with drug Tolerance varies with drug effect

mechanisms of tolerance

metabolic tolerance (dispositional) Celllular Tolerance (Pharmacodynamic) Behavioral Tolerance Contextual Tolerance (Situational)

Metabolic tolerance

increase in metabolism

Cellular Tolerance

Pharmacodynamic

Behavioral tolerance

functioning in presence of drug

Contextual Tolerance

Context in which drug is taken induces tolerance

psychostimulant tolerance

Rapidly forming Slowly or not Forming Reverse Tolerance (sensitization)

psychostimulant Rapidly Forming Tolerance

Appetite suppression Euphoria Cardiovascular Effects Lethal Effects

Psychostimulant Slowly or Not Forming Tolerance

Effect on Narcolepsy | Effects on ADHD

psychostimulant Reverse Tolerance

Seizures | Locomotion

Drug dependence

physical dependence psychological dependence

physical dependence

withdrawal syndrome opposite of acute effects

psychological dependence

Reinforcing effect of Drug | "Drug Craving"

Psychostimulant physical Dependence

Fatigue and exhaustion Prolonged sleep Depression or Crash Intense Hunger

Psychostimulant psychological dependence

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

Cocaine ratings

Withdrawal: 3.5 to 4 Reinforcement: 1 1 is most serious, 6 is least serious

models of drug dependence

physical dependence positive reinforcement incentive sensitization

physical dependence model (Wikler)

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

Positive Reinforcement Model (Koob)

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

Positive reinforcement

Dopamine activity is what is reinforcing

Cocaine Mesolimbic Pathway (DA)

Cocaine blocks DA reuptake amphetamine Stimulates DA release Ventral Tegmental Area - Nucleus accumbens

incensitive sensitivation model summary

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

incentive sensitivation model

``` 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

brain changing model

``` repeated drug administration - transcription factors - gene expression - Dendritic remodeling in Nucleus Accumbens - Drug Addiction ```

neurotoxicity in striatum

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

meth mouth

dry mouth clenching poor dental hygiene

psychostimulants 2 Flashcards

(55 cards)