Psychostimulants Flashcards

1
Q

psychostimulants

A
  • cocaine
  • amphetamines
  • khat
  • caffeine
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2
Q

Cocaine Origin

A
  • Erythroxylon Coca, the coca bush
  • coke, snow
  • South America
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3
Q

cocaine history

A
  • andes
  • ancient civilizations (incas: anesthetic effect)
  • spanish conquistadores 16th century
  • 1800s explorers: to europe and north america
  • 1880’s medical use: freud, panacea, coca-cola (9mg coke)
  • reports of addiction: popularity
  • 1914: Harrison Narcotics Act
  • 1970s: celebrities
  • 1980’s: smokable forms
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4
Q

Harrison Narcotics Act

A
  • 1914

- amphetamines turned out to be worse then cocaine, so people went back to coke use

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5
Q

cocaine clinical use

A
  • local anaesthetic: blocks sodium (NA+) channels
  • vasoconstrictor, tightens blood vessels: eye and nasal surgery
  • appetite suppressant
  • schedule II: very rare and declining use in medicine
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6
Q

cocaine, chemical composition

A
  • white powder
  • extracted by crushing leaves with hydrochloric acid: cocaine hydrochloride
  • water soluble: doesn’t cross membranes well
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7
Q

cocaine routes of administration

A
  • snorted: intranasal, good blood supply (10-15 minutes), no first pass effect or enzymes
  • damage of the septum because coke cuts off blood supply
  • buccal, gums
  • dissolved in water and injected:
  • oral: enzymes, first pass effect good bioavailability but risk for heart attack
  • cannot be smoked
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8
Q

other forms of cocaine

A
  • crack
  • freebase
  • other forms can be smoked, cocaine hydrochloride not
  • other forms are not water soluble
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9
Q

freebase cocaine

A
  • cocaine hydrochloride treated with amonia (base) and then dry to evaporade
  • solid
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10
Q

crack cocaine

A
  • cocaine hydrochloride treated with baking soda (base) and then heated
  • solid: rocks
  • won’t dissolve in nose anymore
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11
Q

differences of freebase and crack cocaine

A
  • intense rush: much faster and more addictive
  • uncharged, lipophilic: cross membranes and BBB more easily
  • much lower temperature of vaporisation, doesn’t burn away like reg. coke
  • smokable: huge surface area, effects within seconds
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12
Q

amphetamines general

A
  • 1930’s: labs needed, therefore relative recent
  • amphetamine (benzedrine: bennies)
  • dextroamphetamine (dexedrine: dexies)
  • historically: treat cold and sinus symptoms (vasoconstrictor effect), stimulate wakefulness and alertness
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13
Q

amphetamines current medical use

A
  • schedule II
  • anti-obesity
  • narcolepsy
  • ADHD
  • only work while taking them: built up tolerance
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14
Q

methamphetamine

A
  • Meta: CH3: more lipidic, more powerful and addictive

- Desoxyn: schedule II, ADHD, obesity (not really prescribed anymore)

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15
Q

illegal methamphetamine

A
  • crystal meth (ice)
  • smoked, snorted, iv
  • start: west coast
  • biker drug to club drug
  • making crystal meth: illegal labs (turn ephidrine, pseudoephidrine into meth: cough syrups)
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16
Q

MDMA

A
  • Methylenedioxymethamphetamine
  • ecstasy, molly
  • stimulant and psychedelic: alter reality with serotonin pathways
17
Q

stimulants cycle

A
  • cocaine: 1800’s
  • amphetamine: end of 1800’s, WWII, 1930-60’s (boom)
  • amphetamine was prescribed to treat heroin addiction
  • 1970’s return of cocaine
  • 1980 methamphetamine
18
Q

absorption stimulants

A
  • intranasal: 10-20 minutes
  • iv: secs
  • smoke: secs
19
Q

metabolism stimulants

A
  • cocaine: rapid, short acting, effects last 20-80 min
  • amphetamine: slower metabolism, 4-12 hours
  • cocaine, amphetamines and metabolites of either can be detected in the urine for 2-3 days
20
Q

mechanisms of stimulant action

A
  • affect monoamines (NT in limbic system): dopamine, serotonin, norepinephrine
  • block re-uptake of monoamines: block pumps for re-uptake, especially with dopamine
  • amphetamines also release dopamine
  • mesolimbic dopaminergenic pathway: pleasure and reward
  • high doses = psychosis
21
Q

behavioural effects: low and moderate doses

A
  • behavioural effect: party drugs
    + mood elevation
    + talkativeness, sociability, confidence
    + alertness and arousal (insomnia)
    + physical endurance and strength (norepinephrine)
  • decrease in performance of complex tasks and reasoning
  • state dependent learning: learned something on coke, will remember better on coke
22
Q

Sympathomimetics (NE): low and moderate doses

A
  • fight or flight response
  • increased heart rate and vasoconstriction
  • increased breathing
  • dilated pupils
  • dry mouth
23
Q

Anoerectic effects: low and moderate doses

A
  • abused for weight loss
24
Q

acute effects: high doses / overdose

A
  • stimulant psychosis
  • organic psychosis: treat with dopamine antagonist
  • metamphetamine: direct toxicity to dopamine neurons
  • paranoid delusions
  • aggression
  • hallucinations
  • compulsive stereotyped behavior
  • death: heart attack, stroke, seizures
25
Q

toxic effects: methamphetamine

A
  • psychosis
  • CV effects
  • meth mouth: unique to metamphetamine: directly toxic to dopaminergic neurons
26
Q

chronic effects

A
  • tolerance: acute, protracted tolerance
27
Q

dependence

A
  • no physical withdrawal syndrome

- psychological withdrawal syndrome: dysphoria, depression, anxiety, physical weakness, compulsive craving for the drug

28
Q

withdrawal

A
  • two phases: comedown, crash / withdrawal
  • even after single session
  • chronic users: stronger and longer effect
  • dopamine-depletion hypothesis
  • avoid withdrawal: reason to keep taking the drug
29
Q

cocaine / crack babies

A
  • high risk pregnancy
  • lower birth weight
  • higher mortality
  • maternal neglect, environment
  • low IQ scores
30
Q

ADHD

A
  • attention deficit/hyperactivity disorder

- triad: inattention, hyperactivity, impulsivity

31
Q

ADHD medication

A
  • amphetamine derivatives
  • ritalin
  • amphetamine mixture: adderall
  • paradoxical effect of stimulants: no
  • improvement of activity in frontal lobe: improve focus, calming effect in ADHD children
32
Q

ADHD drugs side effects

A
  • CNS stimulation
  • weight loss
  • CV effects
33
Q

Khat

A
  • Catha edulis: east africa
  • bath salts
  • legal high: designer drugs
  • synthetic cathinones (mephedrone)
  • amphetamine-like effects
34
Q

Caffeine

A
  • worlds favorite drug
  • antagonist of adenosine
  • dangerous to mix with alcohol since one might feel not as drunk as they are
35
Q

caffeine pharmacology

A
  • antagonist of adenosine receptors
  • adenosine receptors: protect the brain from working too hard: these receptors are blocked
  • adenosine: gets us to sleep, tiring effect
36
Q

caffeine acute effects

A
  • caffeinism: cardiac effects, anxiety
37
Q

caffeine chronic effects

A

more gastric acids

38
Q

caffeine tolerance and withdrawal

A
  • fast tolerance to sleep disruption
  • low tolerance to stimulating effects
  • withdrawal: mild, wear off quickly, fatigue