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Lecture 13

PSYT 301 Lecture Notes - Lecture 13: Levamisole, Benzoylecgonine, Piperazine


Department
Psychiatry
Course Code
PSYT 301
Professor
Kathryn Gill
Lecture
13

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Lecture 13: Stimulants continued
- new psychoactive substances (NPS): designer drugs, herbal highs, synthetic drugs
- most new substances that are being detected are synthetic cathinones,
synthetic cannabinoids, also seizures of amphetamine stimulants, tryptamine,
piperazine and PCP analogues, phenylamines
- synthetic cathinones: bath salts derived from African plant Khat -- labelled as
not for human consumption (actual content are not very well known, could be
anything)
- mephedrone: similar psychoactive effects to cocaine/other stimulant
- many people that buy cocaine might not even have cocaine in the sample, cut with
multiple toxic substances including levamisole (a deworming agent that causes
necrosis, aim to mask the adulteration)
- MDMA or ecstasy is one of the most adulterated drugs, caffeine, “others”
Cocaine metabolism:
- normally cocaine is degraded by plasma or liver esterases to benzoylecgonine (50%-
70%), inactive in dopamine uptake, non active metabolite
- in the presence of alcohol, cocaine is degraded by carboxyl esterase to
cocaethylene, a pharmacologically active cocaine metabolite
- compared to cocaine it has a equal affinity for the dopamine transporter,
lower LD50, greater effects on BP and HR, greater hepatotoxicity, and a
longer half-life
- easier to overdose on it -- a lower amount will lead to a 50% death rate
- increased cardiovascular and subjective effects
Amphetamines:
- benzedrine, dexedrine, methedrine, methylphenidate, MDMA
- effects vary in the PNS, depending on the tissue distribution of alpha and beta
adrenergic receptors
- relax smooth muscle in bronchioles leading to bronchioles dilation, but constrict
peripheral blood vessels leading to increased HR and BP
- methamphetamine is more commonly abused due to the fast route of administration
(smoking - ~10s), large bioavailability, fat soluble, passes BBB very easily
- first anti asthmatic
- heavy amphetamine and cocaine use can lead to psychotic symptoms
- similar in structure to dopamine, norepinephrine, epinephrine
- methamphetamine can be converted to crystalline form to be smoke
- long half-life (~12 hrs), long lasting, intense and persistent drug action
- heavy use can produce acute delusional and psychotic behaviour which is
dose-dependent
- increases risk for stroke, heart attack and aortic tears
- ice is to meth as crack is to cocaine
- substantiated evidence has shown that meth can lower brain volumes, all
across the brain
- height of american epidemic (1967) when 31 million prescriptions for diet pills were
filled, and meth was readily available by prescription, in 1970 FDA restricted legal
use to the treatment of narcolepsy, hyperactivity in children (ritalin) and weight
reduction
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