Opiods 1 Flashcards
What are opiates
opiate refers only to naturally occurring drugs or drugs derived from naturally occurring compounds
Opiates include codeine and morphine
What are opioids
opioid is a term used to describe compounds both natural and synthetic that have properties similar to opium or morphine
opiate refers only to naturally occurring drugs or drugs derived from naturally occurring compounds
as clinical agents, renowned as powerful analgesics
have a dramatic effect on the affective component of
pain (anxiety, worry, uneasiness etc)
referred to as narcotics (causes sleep)
What are some other names for opioids
China white, smack, scag, junk, dope
What is the psychological disorder of pain
Being aware of pain but not caring
Wha are some of the legal uses of opioids
morphine is the gold standard of pain killers
in Canada, morphine is prescription only, tightly regulated
codeine found in small amounts in OTC medica&ons
heroin illegal except for experimental use
Why do those using opioids for pain typically not get addicted
pattern of high use with high pain, will decrease dose when pain diminishes
What percentage of users are estimated to become addicted
estimated that 2 - 6% of all long-term users may become addicted
What is the main source of opium
main source is a particular poppy, Papaver somniferum
opium is in the sap of the plant
plant makes drug in only 10 days of its life cycle
between petals dropping and seed pod maturing
Explain the labour intensive process if harvesting opium
workers scratch the seed pods in the evening so that white sap (latex) oozes out overnight
it oxidizes into brown gummy substance black tar opium
scrape it off by hand and compress it
this is opium
What country is the major source of opioids
Aphganistan
What is in opium?
a mixture of narcotic and non-narcotic alkaloids
two major narcotic components are morphine (from Morpheus the Greek god of sleep) (10%) and codeine (0.5%) (Greek for poppy head)
What is morphine 10 fold more potent than
morphine is 10-fold more potent than opium
Explain what codeine is converted to in the liver and what happens if enzymes are deficient or overactive
codeine converted to morphine in the liver and brain
if enzyme is deficient, ( 6-10% of caucasians) codeine codeine produces no effect
if overactive usually because of multiple copies of the gene (2% of popula&on), can get morphine intoxication from codeine use
What is heroin
in 1874, two acetyl groups were added to morphine by Bayer giving diacetylmorphine
given brand name Heroin (from heroish, german for heroic): feel invincible/heroic after use
Explain the significance if the structure of heroine
two acetyl groups make heroin 10 times more lipid soluble than morphine and 3 times more potent:
gets to the brain faster and in higher concentrations
acetyl groups metabolically removed once in brain - converted into morphine which is then able to bind to receptors
Explain the deacetylation of heroin: why it occurs and the products
in the brain, one acetyl group at a &me is quickly removed
get mixture of 6-monoacetyl- morphine (6-MAM) and 3-monoacetylmorphine (3-MAM)
6-MAM binds to mu receptors and is psychoac&ve, 3- MAM does not
both then converted into morphine
6-MAM can only be produced from heroin and so is used in legal cases to prove heroin use
Explain heroin purity over the years
in North America in the 1970s, heroin was 4-6% pure
rest (94 - 96%) was something else
in the 1980s to early 1990s, was 25%
in 2006, 30 - 36%
some samples now 90% with most in a range from 7 - 75%
it is now cheaper for higher purity - more danger for addiction and overdose
What is oxycodone
oxycodone - one of the most abused prescription analgesics
What is oxycodone called when mixed with acetomenophine vs aspirin
Percocet, Percodan
Synergistic effect on pain control
What is OxyContin
OxyContin is a tablet that contains many times the amount of oxycodone as a regular tablet - it was designed as a time-release formula - now a highly sought-after drug of abuse
What is hydrocodone
hydrocodone (Vicodin, Lortab) is another prescription drug commonly abused
What is OxyNeo
Last year, a new version of slow-release oxycodone was brought to market
OxyNeo replaced OxyContin
Pills contain polyethylene oxide, a hydrophilic polymer
OxyNeo is formulated so that if user tries to crush it, instead of a powder, it forms a gummy gel if exposed to fluid
Some evidence that demand for it has gone down
But also evidence that abusers are switching to heroin and other opioids
What does recent data suggest about opioid anise particularly in relation to heroin
recent data shows a substan&al increase in opioid abuse
mostly due to prescrip&on (PO) opioids
in fact, heroin use has decreased in Canada
ratio of PO opioid:heroin abuse was 3:1 in Canadian cites
What is Canada ranked in global prescription opioid consumption
Canada ranked first globally for PO hydromorphone (Dilaudid) consumption per capita and second for oxycodone consumption per capita
A study found that 4 out of every 5 patients seeking help at a Toronto methadone clinic were abusing PO opioids
What is methadone
A safer opioid used to ween people off heroion
What are the death tolls since the introduction of OxyContin
with the introduc&on of oxycon&n:
opioid-related deaths increased 41%
oxycodone-related deaths increased by 416%
What is fentanyl
Synthetic opioid
fentanyl is used primarily as a surgical anaesthetic but also in lollipops and skin patches
less euphoria, more analgesia compared to heroin
100 times as potent as morphine due to high
lipophilicity
short duration is useful in surgery, but may increase addictive potential
lethal in individuals who think they are injecting heroin
recent number of deaths due to heroin being cut with fentanyl - LD50 may be ten &mes lower than for heroin
What is the street name for mixtures if heroin and fentanyl
MAC-22, “magic” “the bomb” are street names for potent mixture of heroin and fentanyl
What are the general opioid abuse effects
intense euphoria, drowsiness, mental clouding, sleepy sensation “nodding”
a “rush” when taken IV, large amount enters brain rapidly - “body orgasm” effect followed by sedation (hour or so)
analgesia may last 3 to 5 hours
in some people, see a stimulant effect
What are the classic physiological effects of opioids
constriction of pupils (except meperidine/demerol) due to agonist effects on mu and kappa receptors in oculomotor nucleus important diagnosis tool in overdose as most other causes of coma produce pupillary dilation
nausea and vomiting (via the chemoreceptor trigger zone in a region of the medulla - the area postrema)
lowering of blood pressure (medulla effect)
vasodilation may lead to profuse sweating
histamine release - hypotension, bronchoconstriction, itching
What are the effects of opioids on mu receptors
opioids are notorious for depressing respiration via ac&va&on of mu receptors even at therapeutic doses
associated with decrease in sensitivity to arterial CO2 and inhibition of respiratory rhythm generator in the medulla
most deaths due to asphyxiation
What are the effects of opioids on digestive system
disrupts coordination of digestive system so food passes slowly
(anti-diarrheal) by activating mu opioid receptors in gastrointestinal tract and in the CNS
results in increased muscular tone but less motility
Explain the oral route if heroin and morphine
heroin and morphine are weak bases that become ionized in acid stomach
not well absorbed from GI
heroin is 100 times less effective when given orally compared to IV
oral route also has major first pass metabolism
suppository form can be used to mostly avoid this
Explain how heroin is smoked
higher purity heroin has allowed for smoking to become a viable alternative
chasing the dragon
pure heroin is heated on tin foil until it
vaporizes
user chases the smoke with a tube and inhales
17 - 63% of heated heroin is vaporized
can also use pipes to smoke it
Explain how heroin is injected
to inject, heroin usually mixed with water in a spoon
lemon juice or something acidic may be added to help dissolve it
heat it to help dissolve and warm it to body temp
sometimes drawn up through cotton ball to “filter out impurities, bacteria and viruses”
heroin can also be snorted (morphine cannot)
Explain the problems with injecting heroin
“track marks” are the scars le^ by frequent injec&ons, especially with dull reused needles
mul&ple injec&ons result in collapsed veins due to scarring
crushed pills seem especially dangerous to vein health due to fillers
addicts frequently need to find new veins in which to inject
seems especially bad with black tar heroin, a crude, gummy preparation from Mexico, Afghanistan
blood is rerouted through deeper, smaller veins
What is Krokodil
A drug that surfaced in Russia several years ago
Codeine, red phosphorous, gasoline, iodine and
hydrochloric acid used to generate desmorphine
Final product is an unfiltered suspension
Injected IV
Immediate damage to blood vessels, muscle, bones
Produces abscesses, gangrene, large-scale necrosis – crocodile-like skin is produced
Called “the drug that eats junkies”
What is doda
doda is a powder made from grinding poppy heads
typically made into a tea and used by workers to get a burst of energy (which seem paradoxical to known effects)
popular with South Asian communi&es
can be just as addictive and dangerous as any other opioid even though it is a very crude prepara&on
in 2009, Edmonton had huge bust - 70 kg
