PLANT DEPRESSANTS: TRANQUILIZERS AND OPIATES

Question 1

______: 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

Answer 1

indian snakeroot

Question 2

______: 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)

Answer 2

kava

Question 3

where was kava first domesticated? how many types of kava are recognized there?

Answer 3

Vanuatu around 3000 years ago, over 250 types are recognized!

Question 4

T/F: cultivars are sterile

Answer 4

true! kava is sterile and must be reproduced clonally

Question 5

what are the two different ways kava rootstock is prepared:

Answer 5

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

Question 6

what is the pharmacology of kava? symptoms?

Answer 6

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

Question 7

T/F: unlike alcohol, kava does not impair altertness significantly

Answer 7

true

Question 8

whole extracts of _____ have hypnotic-sedative, analgesic, psychotropic effects

higher doses produce hypnotic effect

Answer 8

kava

Question 9

kava is recommended for treatment of…

Answer 9

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

Question 10

constant and heavy use of kava can result in…

Answer 10

scaly skin eruptions which are alleviated by abstinance

Question 11

T/F: kava and alcohol can be taken together

Answer 11

no! both depressants, so they have an additive effect… they should never be taken together

Question 12

why is kava banned in some European countries?

Answer 12

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

Question 13

_____: 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

Answer 13

opium poppy

Question 14

its claimed that _____ is the world’s oldest known narcotic… because of its presence on Sumerian medical clay tablets

Answer 14

opium poppy

however, many scholars believe that tablet was referring to a non-narcotic species of poppy

Question 15

_____ 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!

Answer 15

opium poppy

Question 16

there were many images of Persephone (goddess of fertility) holding opium poppies… why?

Answer 16

Mycenaean opium cults were centerred around worship of fertility goddess

Question 17

where was the first evidence of the narcotic use of opium? ivory pipes and other opium smoking equipment found

Answer 17

3500 years ago in Mediterranian Islands of Cyprus and Crete

Question 18

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!

Answer 18

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!

Question 19

T/F: its estimated that 1 in 400 people in the US were addicted to opium by 1900

Answer 19

true!

Question 20

explain the history behind opium use in China

Answer 20

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

Question 21

in 1838 alone, ____ million kgs of opium was smuggled into China

Answer 21

2.5 million kgs

Question 22

by early 20th century, an estimated ____ of the population in China was addicted to opium

Answer 22

one-quarter

Question 23

when did the British-Indian opium trade end? after pressure from Chinese and British governments

Answer 23

1913

Question 24

how is traditional opium produced? what are the steps of production?

Answer 24

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)

Question 25

collected raw opium contains __ related opiate alkaloids

Answer 25

25

Question 26

what are the most important opiate alkaloids in opium?

Answer 26

morphine (4-21%)
noscapine (4-8%)
papaverine (0.5-2.5%)
thebaine (0.5-2%)

Question 27

how do opiate alkaloids exert their effect? what does it result in (symptoms)?

Answer 27

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)

Question 28

the most common opiate alkaloid of opium is ___

Answer 28

morphine
absorbed easily by injection/orally
super addictive, first shown by soldiers in wars

Question 29

when morphine was boiled with acetic acid in 1874, the semi-synthetic diacetylmorphine was produced… otherwise known as _____

Answer 29

heroin

marketed as harmless, non-addictive substitute to morphine… LOL

Question 30

why is heroin so much more addictive than morphine?

Answer 30

two acetyl groups increase solubility… makes it 3x more potent

Question 31

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?

Answer 31

24-36 hours of intense withdrawal

Question 32

semi-synthetic ____, derived from morphine, still used into terminal cancer patients

Answer 32

hydromorphone

Question 33

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

Answer 33

naloxone

Question 34

____, synthetic opiate, administered to overcome addiction to heroin and other opioids
also addictive, but less debilitating

Answer 34

methadone

Question 35

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

Answer 35

10-50 mg

80-140 mg

Question 36

____, 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

Answer 36

codeine

Question 37

_____, semi-synthetic from thebaine
treats and manages moderate-severe pain
potentially addictive, abuse has become increasingly common recently

Answer 37

oxycodone

Question 38

codeine, oxycodone, and other opiate drugs are semi-synthesized from raw opium produced legally where?

Answer 38

Turkey, India, France, Australia

Question 39

_____: 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

Answer 39

fentanyl

Question 40

the vast majority of opium production is illicit… occurring where?

Answer 40

Afghanistan and “Golden Triangle”- Myanmar, Laos, Thailand

Question 41

the Taliban banned opium production but today _____ is the major global source of illicit heroin

Answer 41

Afghanistan

Question 42

because of demand in North America for opium and its synthetics… there are opium poppy plantations in which two countries + more, established by cartels

Answer 42

Colombia and Mexico

plus other Central/South American countries