PLANT STIMULANTS- AMPHETAMINES AND CONVULSANTS Flashcards
6 questions
______: two species of perennial low shrubs
native to Eastern Asia
Ma Huang- ancient Chinese name
known to ancient Greeks and Romans
active secondary product: ephedrine (amphetamine-like compound)
powerful CNS stimulant
anti-histaminic
synthetic amphetamines replaced the natural product- Pseudoephedrine the new active compound (stereoisomer of ephedrine)
became popular “herbal remedy” and “supplement”
amphetamine/benzedrine, methamphetamine, MDMA, ketamine, esketamine, methylphenidate, fenfluramine-phentermine all come from _____
ephedra
T/F: there are other members of Ephedra genus in Asia and NA but they are not used medicinally
true!
T/F: all Ephedra species have wiry stiff twigs and highly reduced leaves, because they grow in dry, desert-like conditions
true
records of Ephedra use in China date back how many years?
4000 years! used in tonics and teas to improve circulation, increase blood pressure, raise heart rate, promote perspiration, reduce fever, also as an antihistamine! natural decongestant and cough remedy as well
what is the active secondary product of ephedra?
ephedrine
amphetamine-like compound, first isolated by Japanese scientist
_______ is a powerful CNS stimulant, increases blood pressure and raises heart rate
also anti-histaminic
ephedrine
when the west “discovered” the uses of ephedra (increases blood pressure and raises heart rate,
also anti-histaminic) their demand from China greatly increased, by 1940 over ___ million pounds of Ephedra twigs were being imported into the US from China
one million
_____ was used in western medicine to dilate the pupil, increase blood pressure, treat asthma/hay fever, counteract overdoses of depressant drugs (alcohol/morphine/etc.)
ephedra
by the ____, semi-synthetic analogues (synthetic amphetamines) had replaced natural Ephedra
1950s
_____ are stimulants that reduce fatigue by temporarily increasing overall mental and physical activity, speech, concentration
they mimic neurotransmitters (mostly dopamine, but also serotonin) and therefore stimulate the CNS
amphetamines
_______: stereoisomer of ephedrine, is a common ingredient in OTC medicines
pseudoephedrine
Ephedra contains pseudoephedrine, but todays synthetic is obtained by yeast fermentation of dextrose in the presence of enzymes and benzaldehyde
why is pseudoephedrine used in the illicit drug trade?
its easily reduced to methamphetamine and oxidized to methcathinone
why did Ephedra become a “herbal remedy” and weight loss supplement in the 90s?
it increases body metabolism and temp
it was also sold as something to improve athletic performance
adverse effects of Ephedra include…
hypertension, heart palpitations, rapid heartbeat, strokes and seizures
sometimes acute psychosis, when combined with other things
when was Ephedra use banned? both commercially and tested in athletes?
2004
however, Canada had been calling for its ban since 2002
_____/____: “pep pills”
ephedrine-based semi-synthetic
introduced commercially in 1932
used widely by German troops in WWII and later Allied soldiers, Japanese factory workers
caused the first recorded stimulant abuse epidemic, after it was dumped on the open market after the war
lasted until 1958, when governments made it illegal, still widely used after as a decongestant in the 60s but was banned again
continues to be used in oral decongestants, diet pills, and bodybuilding aids
amphetamine, benzedrine
______: “speed”
semi-synthetic amphetamine
produced in 1929 through simple reduction of ephedrine… but MUCH more potent and addictive
methamphetamine
________: “ectasy”
derivative of methamphetamine
high doses cause depression, memory loss, insomnia
overdose results in impaired breathing, heart attack, kidney failure
was promoted as a psychotherapeutic drug, but by the 80s became a street drug
might be useful in treating severe cases of PTSD in small doses (in stage III clinical trials!)
MDMA
______: amphetamine derivative
general anaesthetic
dissociative drug, trance-like state with sedative/analgesic effects
NMDA receptor antagonist, results in rapid increase in glutamate, also increase dopamine activity in the brain
small doses can treat severe, treatment-resistant depression
ketamine
____: stereoisomer of ketamine
in a nose spray that was recently approved to treat clinical depression
esketamine
________: (Ritalin)
synthetic ephedrine
calms hyperactive children
methylphenidate
_____: used in 90s to promote weight loss
banned in 1997 following research showing it causes major heart valve problems
also addictive, and can cause psychoses
fenfluramine-phentermine (fen-phen)
______: small deciduous tree
native to SE Asia and Northern Australia
close relative to SA Curare
powerful muscle convulsant
active principle: strychnine (alkaloid), highest concentration in seeds/bark/whole fruit
highly poisonous (homicide/arrow poison)
cause initial agitation then uncontrolled muscle spasms and convulsions
high doses cause collapse of vital organ systems
effective nervous system stimulant at low doses!
recommended to cure fevers/snakebites, stimulate GI tract, improve blood circulation and treat nervous conditions… rarely used today because much safer alternatives are available
strychnine, nux-vomica