Psychostimulants Flashcards
1
Q
psychostimulants
A
- cocaine
- amphetamines
- khat
- caffeine
2
Q
Cocaine Origin
A
- Erythroxylon Coca, the coca bush
- coke, snow
- South America
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
4
Q
Harrison Narcotics Act
A
- 1914
- amphetamines turned out to be worse then cocaine, so people went back to coke use
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
6
Q
cocaine, chemical composition
A
- white powder
- extracted by crushing leaves with hydrochloric acid: cocaine hydrochloride
- water soluble: doesn’t cross membranes well
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
8
Q
other forms of cocaine
A
- crack
- freebase
- other forms can be smoked, cocaine hydrochloride not
- other forms are not water soluble
9
Q
freebase cocaine
A
- cocaine hydrochloride treated with amonia (base) and then dry to evaporade
- solid
10
Q
crack cocaine
A
- cocaine hydrochloride treated with baking soda (base) and then heated
- solid: rocks
- won’t dissolve in nose anymore
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
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
13
Q
amphetamines current medical use
A
- schedule II
- anti-obesity
- narcolepsy
- ADHD
- only work while taking them: built up tolerance
14
Q
methamphetamine
A
- Meta: CH3: more lipidic, more powerful and addictive
- Desoxyn: schedule II, ADHD, obesity (not really prescribed anymore)
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)
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
toxic effects: methamphetamine
- psychosis
- CV effects
- meth mouth: unique to metamphetamine: directly toxic to dopaminergic neurons
26
chronic effects
- tolerance: acute, protracted tolerance
27
dependence
- no physical withdrawal syndrome
| - psychological withdrawal syndrome: dysphoria, depression, anxiety, physical weakness, compulsive craving for the drug
28
withdrawal
- 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
cocaine / crack babies
- high risk pregnancy
- lower birth weight
- higher mortality
- maternal neglect, environment
- low IQ scores
30
ADHD
- attention deficit/hyperactivity disorder
| - triad: inattention, hyperactivity, impulsivity
31
ADHD medication
- 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
ADHD drugs side effects
- CNS stimulation
- weight loss
- CV effects
33
Khat
- Catha edulis: east africa
- bath salts
- legal high: designer drugs
- synthetic cathinones (mephedrone)
- amphetamine-like effects
34
Caffeine
- worlds favorite drug
- antagonist of adenosine
- dangerous to mix with alcohol since one might feel not as drunk as they are
35
caffeine pharmacology
- 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
caffeine acute effects
- caffeinism: cardiac effects, anxiety
37
caffeine chronic effects
more gastric acids
38
caffeine tolerance and withdrawal
- fast tolerance to sleep disruption
- low tolerance to stimulating effects
- withdrawal: mild, wear off quickly, fatigue
