Opiods 1 Flashcards

0
Q

What are opiates

A

 opiate refers only to naturally occurring drugs or drugs derived from naturally occurring compounds
Opiates include codeine and morphine

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1
Q

What are opioids

A

 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)

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2
Q

What are some other names for opioids

A

 China white, smack, scag, junk, dope

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3
Q

What is the psychological disorder of pain

A

Being aware of pain but not caring

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4
Q

Wha are some of the legal uses of opioids

A

 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

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5
Q

Why do those using opioids for pain typically not get addicted

A

 pattern of high use with high pain, will decrease dose when pain diminishes

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6
Q

What percentage of users are estimated to become addicted

A

 estimated that 2 - 6% of all long-term users may become addicted

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7
Q

What is the main source of opium

A

 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

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8
Q

Explain the labour intensive process if harvesting opium

A

 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

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9
Q

What country is the major source of opioids

A

Aphganistan

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10
Q

What is in opium?

A

 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)

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11
Q

What is morphine 10 fold more potent than

A

 morphine is 10-fold more potent than opium

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12
Q

Explain what codeine is converted to in the liver and what happens if enzymes are deficient or overactive

A

 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

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13
Q

What is heroin

A

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

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14
Q

Explain the significance if the structure of heroine

A

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

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15
Q

Explain the deacetylation of heroin: why it occurs and the products

A

 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

16
Q

Explain heroin purity over the years

A

 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

17
Q

What is oxycodone

A

oxycodone - one of the most abused prescription analgesics

18
Q

What is oxycodone called when mixed with acetomenophine vs aspirin

A

Percocet, Percodan

Synergistic effect on pain control

19
Q

What is OxyContin

A

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

20
Q

What is hydrocodone

A

hydrocodone (Vicodin, Lortab) is another prescription drug commonly abused

21
Q

What is OxyNeo

A

 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

22
Q

What does recent data suggest about opioid anise particularly in relation to heroin

A

 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

23
Q

What is Canada ranked in global prescription opioid consumption

A

 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

24
Q

What is methadone

A

A safer opioid used to ween people off heroion

25
Q

What are the death tolls since the introduction of OxyContin

A

 with the introduc&on of oxycon&n:
 opioid-related deaths increased 41%
 oxycodone-related deaths increased by 416%

26
Q

What is fentanyl

A

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

27
Q

What is the street name for mixtures if heroin and fentanyl

A

MAC-22, “magic” “the bomb” are street names for potent mixture of heroin and fentanyl

28
Q

What are the general opioid abuse effects

A

 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

29
Q

What are the classic physiological effects of opioids

A

 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

30
Q

What are the effects of opioids on mu receptors

A

 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

31
Q

What are the effects of opioids on digestive system

A

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

32
Q

Explain the oral route if heroin and morphine

A

 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

33
Q

Explain how heroin is smoked

A

 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

34
Q

Explain how heroin is injected

A

 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)

35
Q

Explain the problems with injecting heroin

A

 “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

36
Q

What is Krokodil

A

 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”

37
Q

What is doda

A

 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