Amphetamines Flashcards
What is the difference between amphetamines and methamphetamines?
They are both a stimulant, but meth enters the brain more rapidly
True or false: amphetamines effects are similar to those of cocaine?
True, sensations of well-being, profound euphoria and illusion of invincibility, suppression of fatigue and increased alertness
What is the natural source of amphetamines?
Trick question, there is no natural source, they are purely synthetic. Was originally synthesized for a new asthma medication
What other uses for amphetamines were there?
Weight loss, depression, asthma, stimulant (for pilots and soldiers), narcolepsy (still used for today), ADHD
What NT have a similar backbone to meth and amphetamines?
Noradrenaline and dopamine
Why is meth the drug of choice now other other amphetamines?
Has an extra methyl group that makes it easier to enter the brain quicker and is harder to metabolize - profound euphoria
What is a common starting point for meth synthesized?
Pseudo ephedrine from cold remedies
How much waste is usually produce for 1 kg of product?
5-7kg of waste (lithium, sodium, phosphorous, ammonia
Are amphetamines longer or shorter lasting compared to cocaine?
Longer lasting, not administered as frequently
Do amphetamines produce higher dopamine releases than cocaine or less? By how much?
Yes, amphetamines have over 1000% of basal release in the NA, and only about 400% when taking cocaine
What is the enzyme that metabolizes amphetamines in the liver?
CYP2D6
What are the metabolites of amphetamine and of meth?
Amph: norephedrine, and 4-hydroxyamphetamine
Meth: 4-hydroxymethamphetamine and norephedrine, and 4-hydroxyamphetamine.
These metabolites can stimulate the periphery NS themselves
What is the mechanism for amphetamines?
Amphetamine ENTERS (unlike cocaine, where it blocks from the outside) the presynaptic terminal through two ways: 1. diffusion through the membrane and 2. transportation by DAT. But like cocaine, it prevents the re uptake of dopamine, noradrenaline and serotonin
How does dopamine accumulate in the system?
It floods the cleft because AMPH enters the vessibles in the pre membrane and causes them to spew out all their dopamine, AMPH inhibits MAO to prevent the degrading of dopamine, AMPH reverses the DAT transporters and pushes dopamine from pre membrane into the cleft and also dopamine diffuses across the pre membrane
True or False: amphetamines don’t need stimulation of the presynaptic cell to get activation of post synaptic receptors
True, depolarization of pre membrane doesn’t need to occur for the release of dopamine into the cleft
How does methamphetamines and amphetamines reverse the DAT receptor?
They bind to and strongly activate the intracellular receptor called Trace Amine Associated Receptor (TAAR)
What happens when tolerance occurs when using AMPH?
The enzyme involved in synthesis pathway for dopamine and noradrenaline, tyrosine hydrozylase, is inhibited. Acutely and chronically, DAT function decreases (less sensitive to dopamine, unlike cocaine), and there is less cell surface expression
Are AMPH very damaging to the brain?
Yes, shown that dopaminergic, noradrenergic and serotinergic terminal are reduced. Also, excess glutamate release causes excess dopamine and toxic environment that leads to neuronal death–> excitotoxicity
Brain damage from AMPH is similar to what disease? Can AMPH cause this disease?
Parkinson’s Disease, and evidence has shown that there is a 76% increased risk in developing Parkinson’s in meth users, but not cocaine users
What are some of the negative psychological effects?
Unprovoked aggression, feeling of being indestructible (grandiosity), hallucinations and paranoia, delusions of parasitosis, pounding (repeated meaningless behaviours)…
Describe some of the physiological behaviours:
Sympathetic stimulation, increased heart rate and BP, insomnia, tremors, headaches, hyperthermia, meth mouth, skin disorders, renal and hepatic failure, strokes and seizures
How severe are the withdrawal symptoms?
Anhedonia (inability to feel pleasure), fatigue, mood volatility, vegetative state and increase craving. Usually symptoms are very long lasting, often at least 12 months. If dopaminergic neutrons were destroyed, its unlikely they will recover completely.
