t- cocaine amphetamine methylphenidate Flashcards

1
Q

absorption

A

amphetamines used medically are always given orally

when used recreationally can be smoked, snorted or injected

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2
Q

methamphetamine

A

highest potential for abuse- BBB, not degraded by MAO and is therefor more potent and faster acting

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3
Q

cathinone

A
chewing leaves of Khat shrub
absorbped fast into muscous membrane and stomach 
euphoric effects 
methcaninone- snorted or IV 
- less potent so requires higher doses
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4
Q

coca–> cocaine

A

sulfate paste- first, lime water and kerosine
HCL salt- KPO4, kerosine, alcohol
impurities
free base or crystalized crack- has to be smoked

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5
Q

distribution

A

all cross BBB and distribute to organs
amphetamines- highest concentration in kidney and lungs
peaks in 9 mins
cocaine- concentrates more in the brain and peaks faster (4.5 mins)
methylphenidate- peaks in 1 hour orally or 8-20 mins injected

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6
Q

elminiation

A

amphetamine reabsorption depends on pH of urine
acidic urine decreases half life and basic prolongs
methamphetamine is not altered by repeated use meaning that it may be pharmakodynamic
cocaine- half life only 60 mins

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7
Q

monoamine release

A

MAO and COMT affect monoamine release
reabsorption achieved by monamine transporters MAT
MATs are Na/Cl dependant substrate specific membrane transporters
VMAT packages monamines in vesicles

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8
Q

cocaine on DAT (MAT and VMAT)

A

competitive reuptake inhibitors or ereuptake blockers Binds to receptor site
leaves dopamine in synaptic cleft and exert larger effect on post synaptic neuron

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9
Q

bupropion

A

similar potency to cocaine and methylphenidate to DA system but doesnt increase drug liking and may produce adverse affects

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10
Q

cocaine as DAT inverse agonist

A

modify the conformation of DAT in a different way
binds to a different binding site than dopamine
triggers outward conformation change that allows reverse transport of dopamine into the cleft

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11
Q

amphetamine as a competitive transporter DAT NET and SERT

A
  • bind to same site as monoamine, most potent inhibitors of NET - increasing extracellular concentrations
  • also enter vesicles through VMAT preventing transmitters from being packaged causing transmitter to be released into the cleft
  • competitive substrate releasing agent- dispalce monoamine from presynaptic neuron
  • MAO inhibitor
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12
Q

cathinone as a competitive antagonist

A

strongly binds to NET and DAT but not SERT
structurally similar to amphetamines
2-3x less potent

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13
Q

psychomotor stimulant effects on human body

A

elevate heart rate, bp, increase temperature, vasodilation, bronchodilation, decrease food consumption (not well understood)

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14
Q

punding

A

repetitive performance of some act for an etended period of time
- users ground up amphetamine like drug and injected for a rush

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15
Q

amphetamine subjective effects

A

positive: clear mind, high spirits, decrease in fatigue, increase in energy, desire to accomplish things
negative: anxiety
intense feelings of euphoria or rushes

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16
Q

discrimination

A

participants could discriminate amphetamines between benzos but not between eachother

17
Q

effects on sleep, sensation and performance

A
  • prevent fatigue, increase alertness, energy and attention can cause insomnia
  • lower threshold and increase visual/auditory acuity
  • increase athletic abilitys, decrease driving ability
18
Q

ADHD treatment

A

drugs target DA and NE which are dysfuncitonal
negative feedback reduces DA and dampens DA signalling
also dampen background noise & amplify task related

19
Q

run abstininece cycle

A

cocaine taken in large quantities than a period of abstinince

20
Q

harmful effects

A

cocaine- mild jaundice from liver damage, binges
methyl- headache, dizziness, pain, naesua (non life threatening)
methamphetamine- much more dangerous

21
Q

amphetamine neurotoxicity

A

brain damage to many different areas - dopamine and serotonin related

22
Q

monoamine psychosis

A

high doses over extended periods of time can elicit psychosis
indistinguishible froms schizophrenia
formication- bugs crawling all over

23
Q

sex drive - cocaine and khat

A

low doses may increase sexual pleasure
high doses may decrease amd disrupt
KHAT- inhitially increases but after continued use decraeses

24
Q

stimulant overdose

A

coke- initial excitment followed by severe headche nausea vomitting and convulsions
meth- dilated pupils, shivering, high fever, hypertension
most result from organ failure, pulmonary congestion CV hemorrhage or heart failure

25
Q

tolerance

A

stimulants show acute tolerance
coke out: loses ability to cause rushes and improve mood
no tolerance to cardiovascular effects

26
Q

withdrawal

A

coke- high followed by a crash but not typical withdrawal

meth- lack of sleep and deficits

27
Q

pharmacotherapies

A
modafil
buproprion
methylphenidate 
oral d-amphetamine
naltrexone
28
Q

vaccine

A

stimulate immune system to produce antibodies to bind to cocaine molecules
in stages of testing