PLANT DEPRESSANTS: TRANQUILIZERS AND OPIATES Flashcards
8 questions
______: small evergreen shrub
contains reserpine which revolutionized treatment of schizophrenia and hypertension
promoted as tranquilizing agent for mild to moderate anxiety in 1953, but was discouraged when reports of extreme fatigue and depression were linked to its use
indian snakeroot
______: small shrub
native to South Pacific Islands
exists ONLY as cultigen, numerous sterile polyploid cultivars (nearly 250 types are recognized on Vanuatu ALONE)
must be propagated clonally
religious and ceremonial significance to South Pacific Islanders, used to communicate with spirits and gods
used socially to relax, induce sleep, relieve pain, treat anxiety and insomnia, treats rheumatism, menstrual problems, venereal diseases, tuberculosis
rootstock contains active principles: can be harnessed in two ways (chewing or grating method)
active principles: kavalactones, 18 related compounds (ex: kavain)
kava
where was kava first domesticated? how many types of kava are recognized there?
Vanuatu around 3000 years ago, over 250 types are recognized!
T/F: cultivars are sterile
true! kava is sterile and must be reproduced clonally
what are the two different ways kava rootstock is prepared:
chewing method: root broken into small pieces, chewed into soft mass, mixed with cold water/coconut milk, strained and then drunk a few hours later
grating method: root is grated and mascerated in cold water/coconut milk, filtered then drunk
chewing kava is said to have stronger narcotic and depressant effect
grating gives milder tonic to treat sick/convalescent
what is the pharmacology of kava? symptoms?
18 related compounds called kavalactones, and other secondary products
kavalactones have muscle-relaxing anti-spasmodic effects
symptoms include: mild muscle paralysis, decreased rapidity but increased force of heart rate, initially stimulates but then depresses respiration
T/F: unlike alcohol, kava does not impair altertness significantly
true
whole extracts of _____ have hypnotic-sedative, analgesic, psychotropic effects
higher doses produce hypnotic effect
kava
kava is recommended for treatment of…
non-psychotic anxiety symptoms
such as nervous tension, stress, agitation, insomnia
said to be as effective as many synthetic depressants but with fewer side effects
constant and heavy use of kava can result in…
scaly skin eruptions which are alleviated by abstinance
T/F: kava and alcohol can be taken together
no! both depressants, so they have an additive effect… they should never be taken together
why is kava banned in some European countries?
people using kava as a dietary supplement have experienced liver toxicity (rare), popular thought is that toxicity is not from kava root but rather something else (use of ethanol for water-extraction in prep)
in Canada, there was a “stop-sale” order in 2002 but its not enforced and kava can still be bought
_____: robust annual plant
member of Poppy family
native to Southwest Asia
often claimed to be worlds oldest narcotic
addictive properties were well known but caused little concern
Arabic traders introduced it to India and China ~1000 years ago
Hong Kong was yielded to Britain over fights to ban opium from China
made from milky sap of green fruit (capsule) that dries into brown gummy substance- contains at least 25 related opiate alkaloids
morphine, noscapine, papverine, and thebaine- exert their effect on opiate receptors of CNS
most common opiate present is morphine- powerful analgesic, hypnotic, narcotic
heroin derived from morphine (combined morphine and acetic acid)
majority of global production occurs in “Golden Triangle”… Myanmar, Laos, Thailand
plantations also present in Colombia, Mexico, Central/SA countries
opium poppy
its claimed that _____ is the world’s oldest known narcotic… because of its presence on Sumerian medical clay tablets
opium poppy
however, many scholars believe that tablet was referring to a non-narcotic species of poppy
_____ was used in Mycenaean funeral rites (1500-1100 BCE) in Greece… even evidence that it was used in burial chambers in Spain 4500 years ago!
opium poppy
there were many images of Persephone (goddess of fertility) holding opium poppies… why?
Mycenaean opium cults were centerred around worship of fertility goddess
where was the first evidence of the narcotic use of opium? ivory pipes and other opium smoking equipment found
3500 years ago in Mediterranian Islands of Cyprus and Crete
opium use was described by Galen (Roman), Islamic medicine spread its use to the Arabian peninsula, then later to India and China… when was the use of opium popularized (brought) to Renaissance Europe? it was apparently unknown to Medieval Europe at this time!
spread to Renaissance Europe around 1500… by the 19th century, opium was entirely legal and absolutely integral to everyday life
its addictive effects were known, but no one cared!
T/F: its estimated that 1 in 400 people in the US were addicted to opium by 1900
true!
explain the history behind opium use in China
Arabic traders introduced its use 1000 years ago
Chinese smoked it with tobacco, but then tobacco was banned by last Ming emporer… so opium content shot up in mixture (eventually only pure opium used)
its use was made illegal in 1729 but millions were still addicted
British re-introduced opium use in 1781
by the 1830s British East India Company had monopolized opium trade (but still illegal in China!)
to combat this, British and American ships smuggled opium into China at the port of Canton
smuggling heavily drained Chinese economy, First Opium War started by Chinese gov.
British fought the Chinese over opium trade, ending with China ceding Hong Kong to the British and giving them all trading rights with China (including opium!)
Second Opium War weakened Chinese even more
opium smoking remained constant until Communist regime in late 1940s
in 1838 alone, ____ million kgs of opium was smuggled into China
2.5 million kgs
by early 20th century, an estimated ____ of the population in China was addicted to opium
one-quarter
when did the British-Indian opium trade end? after pressure from Chinese and British governments
1913
how is traditional opium produced? what are the steps of production?
sharp knife cuts open green fruit (capsule) when petals fall… milky sap leaks for around 10 days then dries to brown gummy substance (pure, raw opium)
collected raw opium contains __ related opiate alkaloids
25
what are the most important opiate alkaloids in opium?
morphine (4-21%)
noscapine (4-8%)
papaverine (0.5-2.5%)
thebaine (0.5-2%)
how do opiate alkaloids exert their effect? what does it result in (symptoms)?
exert effect on opiate receptors of CNS
decreases awareness of pain, depress respiratory/heart rates
stops digestion (decreases secretion of digestive juices)
results in total satisfaction (reduces stress, tension, depression, panic)
the most common opiate alkaloid of opium is ___
morphine
absorbed easily by injection/orally
super addictive, first shown by soldiers in wars
when morphine was boiled with acetic acid in 1874, the semi-synthetic diacetylmorphine was produced… otherwise known as _____
heroin
marketed as harmless, non-addictive substitute to morphine… LOL
why is heroin so much more addictive than morphine?
two acetyl groups increase solubility… makes it 3x more potent
because heroin is so much more addictive than morphine, it has gnarly withdrawal symptoms. people often continue taking it not to search the high, but to avoid going into withdrawal. how long do these symptoms last?
24-36 hours of intense withdrawal
semi-synthetic ____, derived from morphine, still used into terminal cancer patients
hydromorphone
semi-synthetic _____ is structurally similar to morphine & other opiates, but it actually reverses the effect of opiates on the respiratory/CNS
used to counter opioid overdose
naloxone
____, synthetic opiate, administered to overcome addiction to heroin and other opioids
also addictive, but less debilitating
methadone
methadone is taken as a heroin substitute in stages of increasing dosage
initial ___-___ mg to combat cravings for heroin
___-__ as a higher maintenance dose to prevent severe withdrawal symptoms
10-50 mg
80-140 mg
____, semi-synthetic derived from morphine/thebaine
mild analgesic, used as cough suppressant, pain control
potentially addictive so its a controlled substance in US… but low doses can be bought OTC in Canada
codeine
_____, semi-synthetic from thebaine
treats and manages moderate-severe pain
potentially addictive, abuse has become increasingly common recently
oxycodone
codeine, oxycodone, and other opiate drugs are semi-synthesized from raw opium produced legally where?
Turkey, India, France, Australia
_____: potent synthetic opiate
effective analgesic and anaesthetic
introduced to western medicine in 60s, widely used by 90s
50-100 times more potent than morphine (some analogues are 500x+!!)
devastating addictive properties, extreme potency results in many drug overdoses
fentanyl
the vast majority of opium production is illicit… occurring where?
Afghanistan and “Golden Triangle”- Myanmar, Laos, Thailand
the Taliban banned opium production but today _____ is the major global source of illicit heroin
Afghanistan
because of demand in North America for opium and its synthetics… there are opium poppy plantations in which two countries + more, established by cartels
Colombia and Mexico
plus other Central/South American countries
