Lecture 25- Opiates and Weed Flashcards
1
Q
Major medical use- Opiates
Pain relief
A
- Pain control without loss of consciousness
- NSAIDs (ex. ibuprofen) not as effective as opioids, sometimes not enough for severe pain
- Heroin is Schedule 1 drug… some opioids that are just as addictive or potentially worse are acceptable to use
2
Q
Major medical use- Opiates
End-Stage Cancer
A
- tolerance not as concerning
- administration w low-dose Naltrexone
3
Q
Major medical use- Opiates
Other ways opiates can help medically
A
- diarrhea- severe
- cough (dextromethorphan)- sold over the coutner in cough syrups
- Opiod use disorder- methadone and buprenorphine
4
Q
Is heroin/opiod analgesics lethal?
A
- relatively safe- organs not damaged, destroyed, or threatened by even a lifetime of narcotic addiction
- concern is related to rise in use of opioids in the last decade
5
Q
What makes heroin/opioid analgesics dangerous?
A
- Small therapeutic window (small ratio between effective dose and lethal dose)
- Toxic substances often used to dilute
- Often taken with other misused drugs- synergistic actions can contribute to the overdose deaths
- unstable levels of tolerance
6
Q
What is the point of replacement therapy?
A
- to use different opiod with different PK to help cravings/withdrawal
- these will not get the person high
7
Q
Replacement Therapy
Methadone
A
- a tool-not the answer
- doses are individualized
- Methadone clinics in China-ppl w opioid use disorder cdan go to a clinic daily to get methadone
8
Q
What does methadone increase?
A
abstinence rates
9
Q
What does methadone decrease?
A
- Crime rates
- HIV rates
- mortality
10
Q
Replacement therapy
Buprenorphine (Suboxone)
A
- Some of the best qualities of both Methadone and Naloxone
- partial agonist/antagonist
- lowers withdrawal and craving effects
- only produces partial opioid effect
11
Q
Heroin at receptor
A
full agonist
12
Q
Buprenorphine (Suboxone) at receptor
A
- partial agonist (blocks the receptor but does not work/fit 100%)
13
Q
Naloxone (Narcan) at receptor level
A
- antagonist
- fits into receptor but does not produce an effect- prevents an effect from occuring
- overall, reverses effects of opioids
14
Q
Cannabis Sativa plant info
A
- translates to “intoxicant” in Portuguese
- Marijuana- leafy portion
- Hashish- dust/resin for protecting the plant
15
Q
Marijuana Earliest uses
A
- Stone age (10,000 years ago): pots and household items made from cannabis fibers
- Shen Nung (mythical Emperor, 2800 BC)- used for sedation, analgesia, illness, evil spirits, psychoactive effects (purportedly used medically)
16
Q
Early use internationally
India
A
- weed spread to surrounding countries including india
- India used for religious uses- included as a sacred plant in one of oldest Hinduism books
17
Q
Early use internationally
Middle east and North Africa
A
- Hashish identified around 900 AD
- speed up childbirth
18
Q
Early use internationally
Western civilization (1800s)
A
- Medical applications
- Rheumatism, pain, rabies, convulsions, cholera, neuralgia, gout rheumnatism, hysteria, depression, insanity, stomach pain, discomfort, restlessness, coughs, asthma
19
Q
Early use internationally
Mental Illness
A
- Dr. Jacques Moreau believed marijuana could be used for mental illness
- “The Hashish Club” in France- descriptions of effects written by Theophile Gautier
20
Q
Marijuana Tax Act of 1937
A
- Government an media trying to advertise and suggest that marijuana use led to people doing awful things like murdering family members
- “Reefer Madness”-movie in 1930s anti-marijuana
21
Q
LaGuardia Committee Report
A
- Multidisciplinary experts started to investigate if the terrible effects of weed use were actually true
- Found marijuant not to particularly harmful w/ no association to aggresssion, violence, and belligerence, contrary to media depictions
- Did note: mental confusion, excited delirium, laughter, and anxiety
22
Q
US National Academy of Science
A
- Found that weed can be used as pain treatment, nausea, vomiting, and appetite stimulation
23
Q
What are some reasons people use weed?
A
- To relax
- pain relief
- for fun
- to be social
- to be creative
- to improve sex
- to sleep
- etc.
24
Q
Percieved risk and marijuana use
A
- As perceived risk has decreased, past year use has increased
25
Absoprtion- what ways do people take in weed?
* ingested in liquid/food form in India centuries ago- slow PK
* leaves can be chewed
* smoking (most common), quickest absorption is through lungs (smoked or vaped)
26
What ways do people smoke weed?
* joint: cigarette form
* blunt: emptied out cigar w some tobacco effects
* vapor: water pipes/bongs/electronic devices
27
Absorption- time
* peak effect is in around 30 minutes
* Effects last around 2-4 hours
28
Factors that influence marijuana absorption
* cannabis potency
* time smoke is in lungs
* only around 20% of active ingredient in joint is absorbed
29
Weed- ADMET- Distribution
* Highly lipid-soluble (lipid-philic)
* Gets trapped (deposited) in various fatty tissues throughout the body, making it detectable for long time periods
* Certain compounds still detectable even if blood levels are 0!!
30
Weed- ADMET- Metabolism
* by liver and other organs
* into less active products
31
Weed- ADMET- Elimination
* slowly through feces/urine (1/2 live is around 1 week)
* some metabolites detected up to 30 days following single use- in urine for several weeks following chronic use
32
# chemical makeup
How many unique compounds are in weed?
>400 individual unique compounds in the plant
33
# chemical makeup
Cannabinoids
* >60 compounds in weed grouped as cannabinoids
* Delta-9-tetrahydrocannabinol (THC) is primary psychoactive compound
* Other cannabinboids (cannabidiol and cannabinol) can produce effects but are not psychoactive on their own
34
THC isolation
* delta-9-tetrahydrocannabinol isolated in 1964 in Israel by Drs. Gaoni and Mechoulam
35
# Chemical makeup
Potency
* highly variable
* Highest in Sinsemilla (seedless)- around 10-30% thc
* lower in US grown- 8-10% now (but around 2% in 1980)
* concentration has risen over decades
36
# Chemical makeup
Hash oil (processed)
* more potent than marijuana foliage
* upwards of 60% but typically around 20%
37
Cannabinoid receptor type 1 (CB1)
* mainly found in CNS (hippocampus, cerebellum, and cerebrum)
* metabotropic
38
Cannabinoid receptor type 2
* CB2
* mainly found in periphery/immune system (spleen, tonsillar, and immune cells)
39
Endocannabinoids
* Endogenous cannabinoids: anandamide ("bliss"), 2-arachidonoyl-glycerol (2-AG)
* fatty acids
* synthesized postsynaptically
* cannabinoid receptors are found presynaptically
* retrograde transmission
