Introduction Flashcards

1
Q

Drug

A

Chemical compound that may affect psychological, physiological and behavioural processes

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2
Q

Psychoactive effects and examples

A

Changes in cognitive, behavioural, or motor processes
ie. euphoria, hallucinations, increased libido, altered time perception

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3
Q

Why can the categorization of drugs be complex?

A

Most drugs have the ability to “act like” or produce effects similar to a different class of drugs based on the dosage

example: MDMA can act as a stimulant in low doses and a hallucinogenic in high doses

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4
Q
A
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5
Q

Common Categories of Drugs

A
  • Alcohol
  • Cannabis
  • Caffeine (and minor stimulants)
  • Nicotine
  • Major Stimulants (cocaine, amphetamines)
  • Hallucinogens
  • Sedative-Hypnotics (anti-anxiety)
  • Inhalants
  • Opiates
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6
Q

History of Drugs: What drugs did they have in the BC days?

A
  • earliest was 10000 BC evidence of fermented alcoholic beverages
  • Cholinergic Hallucinogens
  • First stimulant - ma huang
  • Cannabis identified for psychoactive properties
  • Opium
  • Chewing coca leaves
  • discovery of tea, oldest caffeine beverage
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7
Q

History of Drugs 1600’s

A
  • cannabis introduced to Canada/US for hemp use
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8
Q

History of Drugs 1700s

A
  • England faces a gin epidemic
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9
Q

History of Drugs 1800s

A
  • Opium wars between Britain and China
  • Cocaine isolated from coca leaves by Albert Neimann
  • Heroin synthesized by C.R Alder Wright
  • Cigarette rolling machine, tobacco use becomes widespread
  • Rise of patent medicine containing drugs like cocaine and opium
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10
Q

History of drugs 1900s

A
  • Early 1900s: Development of sedative-hypnotic barbituates
  • Early: Criminalization of drug use begins in Canada/US
  • 1919-1931: Alcohol prohibition era in US, Canada for some of that time
  • 1930s: Amphetamines became popular
  • 1943: LSD Discovered by Albert Hoffman
  • 1960s: Benzodiazepines introduced as primary anxiolytics, Surgeon general report on smoking - usage declines steadily
  • 1980s: Crack cocaine makes headlines
  • 1990s: Methamphetamine epidemic begins
  • 2000s: Synthetic cannabanoids and cathinones emerge, cannabis legalization progresses
  • 2010s: Opiate crisis escalate due to overperscribing, appearance of fentanyl
  • 2013: DSM V introduces new conceptualization of substance use disorders, including gambling addiction
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11
Q

What are the 2 major surveys on drug use we talked about and who do they sample

A
  • Ontario Student Drug Use and Health Survey: Grades 7-12
  • Canadian Tobacco, Alcohol and Drugs Survey: Sample of all Canadians 15+
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12
Q

What % of Canadians will develop a substance abuse disorder at some point?

A

20%

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13
Q

How many deaths annually in Canada linked to drug use

A

67,000

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14
Q

What % of Canadians 15+ have consumed alcohol in the past year

A

80%

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15
Q

What % of Canadians aged 15+ exceeded the 2011 Low Risk Alcohol Drinking Guidelines

A

20%

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16
Q

What % Canadians aged 15+ are current smokers, and what % have tried e-cigarettes? (same %)

A

15%

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17
Q

What % Canadians aged 15+ used cannabis in the past year?
What is the % difference between those born in Canada and not born in Canada?

A

20% overall
30% for those born in canada
15% for those not born in Canada

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18
Q

What % of Canadians aged 15+ reported using at least one illegal drug like cocaine, MDMA, or heroin in the past year?

A

3%

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19
Q

What were the 2011Low Risk Alcohol Guidelines? What were the CCSA Alcohol Guidelines in 2021?

A

2011 Low Risk Alcohol Guidelines
* no more than 2 standard drinks per day or 10 per week for females
* no more than 3 standard drinks per day or 15 per week for males

2021 CCSA Guidelines
* 2 standard drinks per week or less - not likely to have any adverse consequences
* 3-6 standard drinks per week - increased risk of adverse consequences
* 7+ standard drinks per week - substantial risk of adverse consewuences
* More than 2 drinks per occassion is associated with increased risk

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20
Q

Drug Names: Most Drugs have 4 Names which are:

A
  • The chemical name: describes the molecular structure and functional groups (ie. caffeine is 1,3,7 trimethylxanthine
  • Generic Name (Non-Proprietary Name): Official medical name for the drug, any company can use the name in marketing (ie. diazepam, fluoxetine)
  • Trade Name (Proprietary Name): a brand name owned by a company (ie. valium, prozac)
  • Street Name: Usually derived from the trade name, physical characteristics, or effects of the drug (ie. The love drug, bennies for benzodiaxepines)
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21
Q

What are pharmacokinetics?

A

A series of steps that describe the process of drugs entering the body, getting absorbed, circulating through the body, getting metablolized, and exiting the body

1. Administration: Process of introducing the drug to the body (ie. taking a pill, snorting something)
2. Absorption:T he drug gets absorbed into the bloodstream
3. Distribution: The drug spreads through the body via the circulatory system
4. Metabolism: The drug is processed and broken down, usually to an inactive form
5. Elimination: The drug and its metabolites are expelled from the body

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22
Q

Pharmacodynamics

A

The process of the drug interacting with receptors (its target) which results in the drug’s therapeutic effects

23
Q

4 Common Routes (Methods) of Administration

A
  • Oral
  • Absorption across mucous membrane
  • Inhalants
  • Injection
24
Q

Orally Administered Drugs:

What is the process?

Why can drugs lose efficacy when it is administered orally?

A
  • Drugs are swallowed and go to stomach (an acidic environment)
  • Most drugs are alkaline so they get ionized in acidic environment (stomach)
  • Ionized = Charged. Ionized chemicals cannot absorb easily, therefore the alkaline drugs cannot be absorbed from the stomach
  • Alkaline drugs also get easily destroyed and broken down in acidic environments, so some of the drug gets destroyed in the stomach
  • The portion of the drug that survives until it gets to the small intestine can be absorbed into the bloodstream because the small intestine is more alkaline, so they will unionize.

The portion of the drug that was lost becuase it was destroyed in the stomach was metabolised before it even reached the body, making the drug less effective.

25
Q

Administration Across Mucous Membranes:

What is this method of admin? Which membranes does this refer to?

A

Drugs can be introduced through the body through mucous membranes in the:
* nose (snorting)
* eyes
* vagina
* rectum
* skin (dermal absorption)

26
Q

Examples of accidental and intentional absorption across mucous membrane

A

Accidental:
* women in which trials may have been experiencing effects because of chemicals they absorbed vaginally
* LSD effects accidentally discovered by Albert Hoffman through dermal absorption
* workers exposed to pesticides

Intentional:
* snorting something
* nicotine patch
* Nicotine and caffeine chewing gum absorbed through membranes in the mouth

27
Q

Inhalants:

Why is this known as an effective way to administer a drug?

How long until it reaches the brain?

Why is it the fastest way to administer a drug?

What are 2 street terms related to inhalants

What is the downside of inhalants?

A
  • effective because you absorb all of the drug unlike orally where some is lost
  • fastest because it goes from the lungs straight to general circulation: IV is slightly longer because goes from site of injection to one side of heart, to lungs, other side of heart then general circulation - inhalants bypass this initial circulatory process.
  • The time to reach the brain is about 8 seconds
  • Downside is lung damage

2 terms related to inhalants:
“Huffing” and “Bagging”

28
Q

Injection:

What are the types of injection? How fast is the absorptio using each method of injection based on blood flow?

A
  • Intraveneous (IV): injecting directly into bloodstream (this makes blood flow irrelevant to speedf absorption because drug is immediately available system-wide) - Called “Mainlining” in drug subculture
  • Intraperitoneal (IP): Injection into paritoneal cavity, often used in research because it has large blood supply therefore rapid absorption
  • Intramuscular (IM): Injecting into the muscle tissue; moderate absorption rate due to decent blood flow
  • Subcutaneous (SC): Injecting into the skin - slowest due to less blood flow - Called “Skin Popping” for illicit admin
29
Q

How does blood flow affect rate of absorption of injected drugs?

A

The blood flow at the site of the injection will determine how fast the drug is absorbed into blood stream circulation.

More blood flow at site of injection = faster absorption

(Does not matter for IV injection becuase it is injected directly into the bloodstream)

30
Q

Describe the curves of each of the 4 methods of admin on a graph that has
x axis: Time after administration
y axis: concentration of drug in brain (effects of drug)

A
  • Inhalants: Fastest to brain therefore steepest slope and peak is leftmost - second highest peak
  • Injection: Second fastest, second steepest slope, peak is second to left - most effective with highest peak
  • Snorting: effects start slow, then increase faster to the peak, then decrease faster, then decrease slower. Peak is second lowest and second to right (peak time happens second latest). Effects last for longer than inhalants and injection
  • Injestion: Slowest onset, steady increase in effect, slope is the least steep, decrease happens a faster than increase but slope still not steep. Peak is the lowest of all of the methods. However, it stretches out over the x axis the most, so the total time of experiencing effects is the longest
31
Q

Describe how the ionization of acidic or alkaline drugs depends on their environment.

A
  • Alkaline drugs are more ionized in acidic environments, less so in alkaline environments
  • Weak acid drugs are more ionized in alkaline environments and less so in acidic environments

(The drug will be less ionized (charged) in environment type the same as its own ph)

32
Q

Describe the distribution process

A
  • absorbed and distributed based on the blood flow of in the area where the drug is administered.
  • entire volume of blood typically circulated every 1 minute, so drug is rapidly circulated to its potential action sites
33
Q

Which type of molecule (ionized vs. non-ionized) is not easily absorbed? Why?

A
  • Ionized (charged) molecules are not easily absorbed because they do not easily pass through the lipid membrane
  • Non-ionized molecules are more easily absorbed because they are more lipid soluble therefore pass through lipid membrane more easily
34
Q

How does lipid solubility of molecules affect absorption and distribution?

A
  • Molecules that are more lipid soluble can pass through lipid membranes easier, therefore they can be absorbed more easily
  • Lipid solubility is important for a drug to be able to pass through the blood-brain barrier
  • Therefore lipid soluble drugs can exert their effects faster and more effectively
35
Q

Describe the Blood-Brain Barrier (what it lets through and what it doesn’t)

Why is this selective permeability of the blood-brain barrier important?

A
  • restricts the diffusion of large or highly charged molecules (big or ionized molecules no get through)
  • more permeable to lipid soluble or un-ionized particles (they can go through)
  • This selective permeability is important for protecting brain against potential toxins while also allowing essential substances to pass through
36
Q

What is the placental barrier? Do drugs pass through this barrier?

A
  • Placental barrier (between fetus and mom)
  • placenta filters blood supplies of fetus and mom
  • allows significant transfers of drugs from mom to fetus
  • in some cases, concentration of the drug in fetal blood can be higher than in the mother’s soon after administration
37
Q

What is receptor binding?

A
  • Drugs exert their effects by interacting with receptors in target tissues.
  • The binding involves electrical charge interactions between the drug and the receptor.
38
Q

How is receptor binding related to effectiveness of a drug?

A

effectiveness of a drug is proportional to how many receptors it occupies.

39
Q

What is an agonist?

A
  • a drug that mimics the action of a neurotransmitter
  • they activate receptors
  • they can cause more neurotransmitters to be released (increasing their presence and activity)
  • they can block neurotransmitter reuptake (allowing them to be active for longer)

(neurotransmitter is like a key, receptor is like a lock - the neurotransmitter fits into the receptor and causes an effect - agonists act like neurotransmitters and bind into the receptors in the same way)

40
Q

What is an antagonist?

What is an example?

A
  • a drug that reduces the effect of neurotransmitters
  • it does this by occupying their receptors without activating them (like a key that fits into the lock without turning it - they just sit there and don’t cause an action)
  • Nolaxone is an example of an antagonist - an opiate receptor antagonist that can block the effect of opiates
41
Q

What is competitive binding?

(does the stronger or weaker agonist win the receptor site?)

A
  • various drugs can compete for the same receptor sites
  • a weaker agonist can prevent a stronger agonist from binding to a receptor site
  • therefore a weaker agonist can block or reduce the effects of a stronger agonist
42
Q

How can the understanding of competitive binding help in therapeutic applications?

A
  • we can use a weaker agonist to block or reduce the effect of a stronger agonist, making them not feel the effects of the stronger one as much, therefore reducing overall impact on the user
  • and helping in withdrawal symptoms
43
Q

What are the factors that affect entry of a drug into circulation?

A
  • local blood flow at the site of administration
  • the solubility of a drug (lipid or water solubility)
  • Route of administration
  • molecular formation of the drug
44
Q

What determines a drug’s efficacy/potency

A

the extent and nature of receptor binding

45
Q

is receptor binding reated to pharmacokinetics or pharmacodynamics?

A

receptor binding is a crucial process in pharmacodynamics

Pharmacodynamics are about how the drug affects the body (the effects it produces caused by receptor binding)

46
Q

What is the Dose Response Curve (DRC)

What is on the x and y axis?

A
  • x axis: Dose
  • y axis: effect of dose (as % of subjects showing the effect)
  • Allows for comparing of drugs
  • More potent drugs have curves more to the left (less dose for same effect)
47
Q

What is the shape of a typical Dose Response Curve (DRC)? What would it mean if the curve was shifted to the right?

A
  • durg effect increases with dose until it plateaus
  • if a curve shifted to the right, then a higher dose would be needed for same effect
  • this could indicate development of tolerance or other factors that decrease drug sensitivity
48
Q

What is ED50

A

The dose at which 50% of the population exhibits the drug’s desired effect.

A standard measure of a drug’s potency

49
Q

What is LD50

A

The dose at which the drug is lethal for 50% of the population

Used to assess toxicity of a drug

50
Q

What is therapeutic index (TI)?

A

The ratio of LD50 to ED50 (ratio of lethal to half the people to desired effect for half the people)

Higher TI indicates greater safety margin between the effective and lethal dose

LD50/ED50

51
Q

What is Margin of Safety?

A

Calculated as the ratio of LD1 (dose lethal to 1% of the population) to ED99 (effective dose for 99% of the population)

a more conservative safety measure than TI

LD1/ED99

52
Q

Why is there more than one Dose Response Curve for each drug?

A

Dose response curve measures dose vs. effect

since there is more than one effect of each drug, each drug will have more than one dose response curve (for each effect)

53
Q

Which one will always be greater: Margin of safety or Therapeutic Index? Why?

A

Margin of safety will always be smaller than therapeutic index

because margin of safety is a more conservative estimate of safety of the drug

54
Q
A