Exam 2: Amphetamines Flashcards
what neurotransmitter are amphetamines structurally related to?
dopamine
two similar plant compounds
cathinone: suburb native to East Africa and Arabia
ephedrine: from herb used in chinese medicine for years
amphetamines original purposes
asthma, alertness in wars, narcolepsy, hyperactivity in children
what schedule drug are amphetamines
schedule 2 - has some instrumental use
federal laws limited ingredients inmethamphetamine…
pseudophedrine cold medicine
anhydrous ammonia fertilizer
types of amphetamines
D-amphetamine (Dexedrine): more potent than L amphetamie
L-amphetamine (Benzedrine): less potent than D-amphetamnie
what is methamphetamine commonly found as
odorless, white or off-white, bitter tasting powder
found in pills, capsules, larger crystals
currently do people use more amphetamines or methamphetamines?
amphetamines
what gender is more likely to use methamphetamine and become dependent
females
route of administration of amphetamines
oral
snorted, injected smoked - most common ones
absorption of amphetamines
water soluble, well absorbed into blood
GI tract-slow
IV-rapid
distribution of amphetamines
most organs - highest uptake in lungs and liver
highly liophillic -crosses BBB
methamphetamine gets into brain quicker than either type of amphetamine
metabolism of amphetamines
NOT completely broken down
in liver by CYP4502D6
in brain by monoamine oxidase (MAO)
major and minor metabolites for methamphetamine
major: amphetamine
minor: 4-hydroxymethamphetamine
metabolites for amphetamines
major: 4-hydroxymethamphetamine
p-hydroxymethamphetamine - potent hallucinogen
excretion of amphetamines
half life 6-12 hrs
rate of excretion influenced by pH of urine
high pH = longer time for elimination - meth quicker since more basic
kidneys
amphetamines compared to cocaine
amphetamines have longer half life - 12 hrs and longer drug actions - 10 hrs
what do amphetamines stimulate the release and block uptake of
catecholamines in CNS
amphetamines block and reverse function of what transporters
monoamine transporters (DAT, NET, SERT) and VMAT2
neurotoxicity of methamphetamine
damage and depletion of DA and 5-HT neurons!!!
10% loss of brain tissue in limbic system
nigrostriatal DA neurons destroyed - inc risk for PD
what neurotransmitter increases body T and has appetite effects
serotonin
people with methamphetamine abuse or dependence have deficits in what?
motor and cognition
behavioral effects: immediately after IV vs oral
IV: intense rush that is pleasurable
oral: euphoria but no rush
acute behavioral effects of amphetamines
nervousness, anxiety, panic
punding - purposeless prolonged and repetitive behaviors (nail biting)
insomnia
reduced appetite
stomach cramps
physical damage as result of chronic use
cardio and pulmonary dysfunction (heart attack, stroke, inflammation of heart)
tooth decay (meth mouth)
psychological effects of chronic use
amphetamine psychosis: [paranoia, visual and tactile hallucinations (formication)
anxiety, OCD - punding
methylphenidate
trade name: ritalin
schedule 2 drug
hyperactivity disorders, narcolepsy, depression, coma, ADHD!!!
absorption of methylphenidate
orally - most common if instrumental use
nasal, IV
metabolism of Ritalin
broken by liver to make water soluble into ritalinic acid
excretion of Ritalin
half life about 3.5 hrs range 2-8hrs
less in kids - 2-5hrs
urine
pharmacodynamics of Ritalin
DAT and NET reuptake blocker
behavioral effects of ritalin
inc arousal, alertness, moood
inc focus
high doses lead to anxiety
PFC and ADHD
normal PFC
alpha 2A receptors: enhance sensory signals (inc signal)
D1 receptors: decrease irrelevant signals (reduce noise)
both to help focus
in ADHD patients - PFC
PFC dysfunction, low levels of DA and NE so giving low levels of stiumlant can help bring these levels up
abuse potential of Ritalin
lower abuse potential than cocaine, amphetamiens, methamphetamines when used instrumentally
