t- cocaine amphetamine methylphenidate Flashcards
absorption
amphetamines used medically are always given orally
when used recreationally can be smoked, snorted or injected
methamphetamine
highest potential for abuse- BBB, not degraded by MAO and is therefor more potent and faster acting
cathinone
chewing leaves of Khat shrub absorbped fast into muscous membrane and stomach euphoric effects methcaninone- snorted or IV - less potent so requires higher doses
coca–> cocaine
sulfate paste- first, lime water and kerosine
HCL salt- KPO4, kerosine, alcohol
impurities
free base or crystalized crack- has to be smoked
distribution
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
elminiation
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
monoamine release
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
cocaine on DAT (MAT and VMAT)
competitive reuptake inhibitors or ereuptake blockers Binds to receptor site
leaves dopamine in synaptic cleft and exert larger effect on post synaptic neuron
bupropion
similar potency to cocaine and methylphenidate to DA system but doesnt increase drug liking and may produce adverse affects
cocaine as DAT inverse agonist
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
amphetamine as a competitive transporter DAT NET and SERT
- 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
cathinone as a competitive antagonist
strongly binds to NET and DAT but not SERT
structurally similar to amphetamines
2-3x less potent
psychomotor stimulant effects on human body
elevate heart rate, bp, increase temperature, vasodilation, bronchodilation, decrease food consumption (not well understood)
punding
repetitive performance of some act for an etended period of time
- users ground up amphetamine like drug and injected for a rush
amphetamine subjective effects
positive: clear mind, high spirits, decrease in fatigue, increase in energy, desire to accomplish things
negative: anxiety
intense feelings of euphoria or rushes