Stimulant Pharma Flashcards
PLANT DERIVED STIMULANTS
cocaine
ephedra
khat
SYNTHETIC STIMULANTS
amphetamine
methamphetamine
canthinone
COCAINE METABOLITES
- > benzoylecgonine
- >ecgonine methyl ester
COCAINE METABOLISM
ESTERASE
by carboxylesterases in the liver and by butyrylcholinesterase in the liver, plasma, brain, lung and other
remaining 5% is N-demthylated to norcocaine by CYP3A4 enzyme of cytochrome P450 system
AMPHETAMINE METABOLISM
- DEAMINATION TO INACTIVE
- OXIDATION TO NOREPHEDRINE AND OTHER ACTIVE
- PARA-HYDROXYLATION TO ACTIVE
amphetamine is N-demethylated metabolite of methamphetamine
STIMULANT DRUG DRUG INTERACTION
MAO inhibitor within two weeks
also caution with TCA’s (block synaptic reuptake of catecholamines)
STIMULANT MECHANISM
enhance extracellular concentrations of monoamine nurotransmitters (DA. NA, 5-HT3) by disrupting plasma membrane transporters
cocaine and methylphenidate - reuptake blockers (transporter blockers)
amphetamine and phentermine - releasers (transporter substrates)
MONOAMINE NEUROTRANSMITTERS
dopamine, noradrenaline and serotonin