Exam 3 Flashcards
(94 cards)
1
Q
Explain Centrally Acting Opiates/ Opioids
Introduction
A
- Opiates a large group of naturally occurring compounds from opium, the latex from the opium poppy
- Main psychoactive opiates in opium are: Morphine, Codeine, Thebaine
- Afghanistan largest illegal producer of opium
- India, Turkey, and Australia largest legal producers
- Lethbridge Opium production (Same conditions to grow opium)
- Opium used as far back as 5,000 BCE
- Used in ancient Asia, Egypt, Arabia, Greece, Rome
- Introduced to western medicine 1500s
- Morphine isolated from opium in 1805 and codeine isolated in 1832
- Opium often combined with alcohol to laudanum
- 1/400 North Americans addicted in early 1900s (women and children)
2
Q
The latex from the opium poppy is what?
A
Papaver Somniferum
3
Q
Opium was historically used for…
A
- Pain relief, surgical analgesia, insomia, depression, and diarrhea
- Religious and ritualistic context
- Suicide and executions (combined with hemlock)
- Recreational use
4
Q
Women and children were
A
addicted to opiates and opium
5
Q
Opiates/ Opioids used for executions was combined with…
A
Hemlock
6
Q
Mrs. Winslow’s Soothing Syrup AKA
A
Baby Killer (1tsp fatal)
7
Q
1895-1915 state provincial laws
A
eliminated the over-the-counter availabilty of opiates and opioids
8
Q
Recreational use of opioids in Canada was made illegal in
A
1908
9
Q
Recreational use of opium was made illegal in the U.S. in
A
1914
10
Q
Why was recreational use of opium made illegal?
A
Addiction concerns and widespread use amongst immigrant chinese labourers and increasing recreational use in non-chinese
11
Q
Opioids are…
A
Synthetic
12
Q
Opiates are…
A
Natural (Codeine, Morphine, Thebine)
13
Q
First Synthetic Opioid
A
Heroin
14
Q
Heroin
A
- Made form morphine 1874
- Reaches brain faster, 2-3 times more potent than morphine
- Introduced as a substitute for codeine and morphine to suppress coughing from tuberculosis and pneumonia
- Mistakenly believed to have fewer side effects
15
Q
Oxycodone
A
- OcyContin, Percocet
- Thebaine
- 1916
16
Q
Hydromorphone
A
- Dilaudid
- From Morphine (Kadrian)
- 1922
17
Q
Methadone
A
- Synthetic Opioid
- 1939
18
Q
Pethidine
A
- Demerol
- Synthetic opioid
- 1939
19
Q
Pentazocine
A
- Talwin
- 1959
20
Q
Fentanyl
A
- Sublimaze
- 1959
21
Q
Naloxone
A
- Narcan
- 1961
22
Q
Naltrexone
A
- Trexan
- ReVia
- 1965
23
Q
Loperamide
A
- Imodium
- 1969
24
Q
Buprenorphine
A
- Suboxone
- 1969
25
Carfentanil
- 1974
26
Modern Uses of Opiates and Opioids
- Pain relief
- Coughing
- Diarrhea
- Anesthesia
- Opiate/ Opioid addiction (drug substitute)
- Opiate/ Opioid O.D.
- Alcohol, Gambling addiction (anti-craving-)
- Executions (U.S.)
- Chemical Weapons
- Euphoria (Recreational use and abuse)
27
What is used for U.S. executions (Modern)
Fentanyl combined with potassium chloride to stop heart
28
Opiates/ Opiods are taken
Orally, Intravenously (Mainlined), intramuscular, subcutaneous, smoked, snorted
29
True or False: More absortion when taken orally because it is lipid soluble
False
| Less complete absorption when taken orally because tends to be lipid ins
30
What is the Neuromechanism of Opiates?
Mimics endogenous and natural opioids. Endogenous opioids are distributed throughout the Central Nervous System, particularly in areas that involve pain like spinal chord and midbrain, and mood (limbic system), also found in stomach and intestines
31
What endogenous/ natural opioids are mimicked?
| fins
endorphins, dysnorphins, and enkephalins
32
Natural Opioids function as...
| Neuro
Neurotransmitters, neurohormones, and neuroegulators
33
True or False: Overall role of opioids/ opiates are complex and not well understood
True
34
Body releases...
| Exercise and Stress
Cortisol toincrease glucose in blood to aid muscles
35
Brain releases...
| Exercise and Stress
BNDF to protect neurons from cortisol and stimulate neuronal growth for learning, memory, and thinking
Endorphins and endocannabinoids to block pain
36
What happens after exercise ends?
- Cortisol returns to normal levels
- Endorphins, endocannbainoids, and BDNF still elevated
- Produces a sense of well-being
37
12 hours of mood elevation can be achieved by
a 20 minute work-out
38
Name the 4 types of opioid receptors
- Mu (euphoria
- Kappa
- Delta
- NOP
39
What is the primary effect of the opioid receptor?
activation is reduction or inhibition of neurotransmission, particularly neurotransmitter release
40
Spinal chord
Inhibit substance P release
41
Ventral Tegmental Area
Inhibits GABA neurons thus disinhibiting dopaminergic neurons and increasing dopamine input in nucleus accumbens
42
Main Effects of Opioids and Opiates
| Physical
- Analgesia
- Relief of anxiety, euphoria, lose all concerns
- Decreased respiration (including coughing)
- Constipation
- Reduced Sex Drive
- Decreased pupil size
- Mental clouding, drowsiness
43
What is a less effective non-opiate alternative?
Dextromethorphan
44
Thousands of Overdose Deaths/ Year
- Respiratory suppression
- 80% associated with other drugs (stimulants and alcohol)
- Increasing since 2000, peak during pandemic (2020-2021)
45
Highest Opioid Death Rates in Canada
- Fentanyl and Carfentanil users
- Yukon, British Columbia, Alberta
- Young and Middle-Aged males
- Indigenous
- Stimulant users (cocaine and meth)
46
True or False: Lethbridge does not have the highest death rate per capita in North America
False they have the highest
47
What is the fatal dose of fentanyl
2mg or 2000mcg
48
fatal dose of carfentanil
0.02mg or 20mcg
49
Opiates/ opioids differ in ____ degree pass through blood-brain barier, which opioid receptor they act on, whether they are agonists or antagonists, and duration
Potency
50
Opioids are mostly metabolized by...
The liver and excreted by kidneys
51
Opioids and Opiates for pain, sedation, and coughing
- Codeine
- Morphine
- Pentazocine
- Oxycodone
- Hydromorphone
- Heroin/ Diamorphine
- Fentanyl
- Carfentanil
52
Opiates and Opioids for Addiction
- Buprenorphine
- Naltrexone
- Naloxone
53
Opiates and Opioids for Diarrhea
Loperamide
54
Long-Term Effects of Occasional Opioid Use
- Not associated with long-term effects
55
Long-Term Effects of Reccurent Opioid Use
- Profound tolerance and strong physical and psychological dependence
- Crime
- Severe withdrawal symptoms (excitation, nausea, insomnia, hypersensitivity to pain, rarely fatal)
- Constipation, indigestion, nausea
- Increased risk of sexual dysfunction, fatigue, depression, sleep apnea, neuropsychological deficits, increased sensitivity to pain due to neuroadaptation
- Use of needles can lead to vein collapse, hepatitis, blood poisoning, AIDS (unclean needles)
56
Harm Minimization for Opioid/ Opiate Use
- Supervised injection sites
- ARCHES
57
Periferally Acting Analgesics
- Often subclassified into NSAIDs and atipyretics
- Most common are aspirin, acetaminophen, ibuprofen, naproxen, and voltarin
- Most widely used medications in the world
- All but acetaminophen work primarily on the body and peripheral nervous system
- For pain, inflammation, fever, differences between them in efficacy profile
- More effective for pain when combined with caffeine
- Increased risk for gastrointestinal bleedin, stroke, and heart attack, adverse effects on kidneys and liver
- Fatal in large doses
- Inhibit enzymes related to prostaglandins
- Minimal tolerance and dependence
- Most available over the counter
58
What are prostaglandins
Lipids having hormone-like effects to mediate pain, inflammation and fever
59
Aspirin
- Found in willobark and spiraea
- Used for pain and fever for thousands of years
- Most commonly used peripherally acting analgesic
- No cardiovascular risk other than PAA, daily low dose helps to stop blood clots and prevent heart attacks
- Useful in preventing certain cancers (colorectal)
- Increases risk of gastrointestinal bleeding and kidney problems
- Shouldn't be given to children and teens. Associated with Reye Syndrome
60
What is Reye Syndrome?
A brain disease associate with aspirin in children and teens
61
Acetaminophen
- Tylenol
- 1955
- Less risk of gastrointestinal bleeding
- Higher risk of liver damage and fatal OD due to liver failure (500 deaths/ year U.S.)
- Not effective for inflammation, less effective for pain relief
- Increase cardiovascular problems and kidney damage
- Unlike other analgesics effects mostly in Central Nervous System
62
Ibuprofen
- 1974 (relatively new)
- Gastrointestinal irritation (less than aspirin), increased cardiovascular risk, increased risk of kidney damage
- May help prevent Parkinson's
63
Naproxen
- 1976 (relatively new)
- Longer duration than other peripherally acting analgesics
- Low risk of cardiovascular problems
- Increased risk of gastrointestinal bleeding and kindey problems
64
What are Psychotherapeutic Drugs?
- Exotic compounds also prescribed in historical times for mental disorders
- Most operated via placebo effect
- Exception; Opium, Alcohol, Cannabis, Willow bark
65
morphine
| 1804
Pain, depression, and insomnia
66
Chloroform & Ether
| 1840s
Pain
67
Aspirin
| 1899
Pain
68
Phenobarbital
| 1912
Seizures
69
Amphetamines
| 1935
Narcolepsy, Depression
70
Lithium
| 1949
Mania
71
Chlorpromazine
| 1953
Schizophrenia
72
MAOI
| 1957
Depression
73
Tricyclic Antidepressants
| 1957
OCD, Anxiety, Depression
74
I-Dopa
| 1961
Parkinson's Disease
75
Diazepam
| 1968
Anxiety
76
Naltrexone
1894
77
1980s
- New Antidepressants
- Antianxiety
- Antipsychotics
78
1987
Prozac/ Fluoxetine
79
2006
Varenicline (Champix)
80
Current Prevalence of Mental Health Medication
- Significant increase in rx psychotropics in past 30 years
- Primarily due to increased use of antidepressants
- Signficant increase in children and adolescents as well (mostly due to stimulant medication for ADHD), although this has leveled off recently
- Billions currently spent on antidepressants, antianxiety, antipsychotics, and stimulant drugs
81
In 2019, adults...
- 14% rx opiate/ opioid
- 11% rx sedative
- 10% antidepressant
- 2% rx stimulant
82
Increase of Psychotropic use due to...
- Family physicians being main mental health practitioners
- Quick fix
- Short-term effectiveness
- Wide range of mental health conditions that can be treated
- Mild to short-term side effects
83
6% of U.S. adults were prescribed psychotropic medication in...
1990
84
What is an issue with the increase of psychiatric drugs?
- Increasing the chronicity of mental health problems
- Very difficult to withdraw from the drug
85
Demographic Correlates of Mental Health Medication Usage
- Higher in Western countries
- Higher in North America compared the Europe
- Higher in females
- Higher in whites
86
Psychotropics are the first line treatment for...
- Bipolar types I and II
- Schizophrenia
- Severe depression
87
Psychotropics also effective in short-term for other mental heath problems. However...
Long-term mental health tends to be worse compared to people who have went to psychotherapy or received no medication at all
88
Psychotherapeutic drugs should always be...
The last resort
89
Physicians refer to...
Compendium of Pharmaceuticals and Specialties (CPS)
90
ADHD medications
- Methylphenidate (Ritalin, Concerta)
- Amphetamines (Dexedrine, Vyvanse)
| Both medications have 1/day administration
91
How does ADHD medication work?
- Increases on-task behaviour and decreases disruptive behaviour
- Equivocal impacts of academic achievement
92
Side Effects of ADHD Medication
- Appetite suppression
- Insomnia
- Small growth retardation
- Motor and vocal tics, may produce permanent tics
- 1.5% risk of psychosis
- Abuse potential
93
New formulation of Vyvanse
Converted to dextroamphetamine after enzymatic break-down in red blood cells
94
