EXAM 1 Flashcards

(115 cards)

1
Q

What is Drug Addiction?

A

A complex disorder characterized by poor decision making and pathological use of psychoactive drugs that leads to poor social/personal health

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2
Q

What is drug addiction?

A

It is a complex disorder lead by poor decision making and pathological use of psychoactive drugs that leads to poor social/personal health

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2
Q

Why it is that Aspirin becomes “trapped” in the blood
after it moves from the stomach?

A

Aspirin moves from the gut to progressively higher pH body compartments and becomes highly ionized in neutral pH blood.

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2
Q

Why are drugs of abuse often inhaled or injected?

A

Results in the most rapid accumulation of high doses of drug in the brain to produce the greatest euphoric effects

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2
Q

Routes of Administration: Why does it matter?

A

Depending on objective; if it is for high and fast peak or steady state

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2
Q

What is is difference in applications of drugs for recreational usage vs. medical uses?

A

Medical use: maintain the minimum effective concentration, over a long time period

Rec use: Highest effect, quickly high quickly low

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2
Q

Imagine 2 agonist drugs used to treat pain. Compound A
is highly effective pain reliever used for post-operative analgesia,
although pain relief is observed only at doses > 5mg/kg. Compound B
is a drug of the same class and exhibits pain relief at 1mg/kg, but has
more modest effects on overall pain thresholds, even at very high
doses. Imagine the dose-response functions for these two
compounds. How would we describe these compounds’ efficacy and
potency in relation to one another?

A

Compound A has higher efficacy
Compound B has higher potentcy

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3
Q

What is potency?

A

How much drug is needed to produce an effect; on the x-axis; how potent a drug needs to me

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4
Q

What if efficacy?

A

maximum effect that can be produced by a drug; y-axis; highest peak on drug

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5
Q

What are partial agonists?

A

Drugs with intermediate levels of intrinsic activity at a receptor
(compared to “full agonist”)

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6
Q

Example of a partial agonist

A

Buprenorphine

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7
Q

What are the two properties of a drug that can modulate its efficacy?

A
  1. Mechanism of Action
  2. Intrinsic Activity
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8
Q

Why do some drugs have higher efficacy than others?

A

The may act on different receptors; less intrinsic activity at the same receptor

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9
Q

Explain the effect of tolerance on a dose-response curve.
What are 2 processes that lead to tolerance?

A
  1. Right shift in dose curve
  2. Learning, homeostatic /enzyme induction (pharmacokinetic ), changes in
    receptor number/location (pharmacodynamic)
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10
Q

Changes in a dose curve with tolerance?

A

Curve shifts to the right

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11
Q

What is the difference between negative reinforcement and punishment?

A

Negative Reinforcement is taking something away from a system and punishment is adding something to the system to stop a behavior.

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12
Q

A rat was previously trained to self administer heroin. In a new
experiment, that same rat exhibits an exaggerated locomotor
response to an amphetamine injection. What is this effect on the
response to amphetamine an example of?

A

Cross-Sensitization: Previous exposure to one drug emphasizes the effect of a second, novel drug on a particular response

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13
Q

What is sensitization?

A

Can occur from many factors including metabolic

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14
Q

Example of sensitization

A

Heavy Alcohol use leads to reduced capacity to metabolize alc

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15
Q

When can cross-sensitization occur?

A

-between drugs (coke and amphetamine)
- between drugs and stress

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16
Q

What is a conditioned reinforcer?

A

a neutral stimulus that acquires reinforcing properties from its association w/ a primary reinforcers

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17
Q

Drugs can be classified in many ways, including what they do, where
they act, and what they are derived from. Give an example of a
natural, semi-synthetic, and synthetic analgesic.

A

Opium/morphine, heroin, fentanyl

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18
Q

We discussed 2 key enzymes in the metabolism of alcohol. Which
contributes to sex differences in alcohol tolerance, and which directly
controls how bad of a hangover someone gets?

A

enzyme to contribute to sex differences: alcohol dehydrogenase – women have less than men

enzyme to contribute to hangover: aldehyde dehydrogenase

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19
Q

What is the major difference between the synthesis of
classical and non-classical neurotransmitters?

A

Classical: Has dietary precursor; synapse at A.T

Non-Classical: New protein synthesis ;Synapse in Soma then travel down A.T

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20
What is the difference between a competitive and non-competitive antagonist? Relate to response curve
competitive must fight to bind to receptor and non -competitive binds elsewhere onto molecule On a response curve: Comp = shifts to the right Non-Comp = lowers the curve
21
What is an autoreceptor?
Receptors on a terminal where the same NT binds
21
We talked about a lot of different self-administration procedures, which best captures the behavioral and pharmaco-kinetic profile of drug abuse?
Intermittent Access(IntA) self administration procedure
21
Which of the two major types of synapses do drugs of abuse typically act on?
Chemical synapses
21
What are the two major types of synapses in the brain?
Electrical and Chemical
22
Starting with the binding of a neurotransmitter to a Gs- coupled GPCR, describe the pathway leading to a change in gene transcription.
The catalytic subunit of PKA can cross the nuclear membrane to phosphorylate CREB to increase/decrease transcription of certain genes
22
Where are neurotransmitters stored after synthesis, but before release?
Vesicles
23
Psychopharmacology
Influence of drugs on behavior and psychological function
23
Pharmacology
Brand of medicine that deals with the uses, effects, and modes of action of drugs
24
What is a Drug?
A substance that is used primarily to bring about a change in some existing process or state, be in psychological, physiological or biochemical Chemical entity or mixture alters biological function outside the maintenance of normal health
24
Neuropsychopharmacology
Influence of drugs on brain, behavior and psychological function
25
Neuropharmacology
Influence of drugs on brain function
26
What are the ways to name and classify drugs?
1.By Source (e.g. manmade or natural) 2. Therapeutic Use (e.g. analgesic) 3.Mechanism of Action (e.g opioid receptor) 4.Chemical Structure 5.Legal / Social status
26
What are the naturally occuring drugs and where do they come from?
1. Opium from unripe seed pods of opium poppy 2. Cocaine, from the leaves of the coca plant 3. Ephedrine, extracted from Ephedra plant
27
What are some semisynthetic drugs?
1. Heroin from Morphine 2. LSD from grain ergot fungus
28
What are some synthetic drugs?
Fentanyl (synthetic opioid) Amphetamine (powerful stimulant) MDMA (Ecstasy: stimulant+ hallucinogen)
29
Analgesics
Morphine Codine
29
What are the Stimulants?
-Amphe -Coke -Nic
29
What are the three main questions of pharmacokinetics?
How much drug? How Fast? How long to activate?
29
Drug Schedule #1
substances that have no accepted medical use and high abuse potential
29
What are the CNS depressants?
Barbiturates and alcohol
29
Hallucinogens
LSD and Psilocybin
30
Drug Schedule #4
Even lower abuse potential than 3
30
Drug Schedule #2
Substances that have a high abuse potential w/ severe psych or physical dependence liability
30
Drug Schedule #3
Substances with lower abuse potential than 1 and 2
31
Drug Schedule #5
Contain limited amounts of narcotics and used for medical use.
31
Cons of Oral Admin
First pass metabolism -- the amount of drug that gets lost in stomach acid before it goes into blood (Poor control)
32
Pharmacokinetics
the life and movement of a drug from its site of action till excretion
32
What is the most common route of administration?
Oral (PO)
32
Pros of Oral Administration
Easy and more accessible Slow and steady concentration (No spikes)
33
ALL Routes of Admin
Oral, IV, IM, SC, Inhale, Topical, Transdermal, Intranasal
33
Non-invasive routes of drug administration
Oral Nasal -- up nose Sublingual -- under tongue Rectal -- Up anus Transdermal Inhale -- smoking
33
What if Half-Life in terms of drugs?
Time for plasma drug conc to fall to half of peak level
33
Subcutaneous Injection (SC)
Needle under skin, not into muscle In the skin layer(epithelium)
33
Intramuscular Injections (IM)
Into Muscle (absorbed faster -- more in blood)
33
Intravenous Injection (IV)
Into Vein -- directly into circulatory system
33
where doesn't the IV dyes spread e
CSF and Brain
33
How did the BBB arise?
Distinct properties of brain capillaries
33
What are the different routes of administration in order from highest peak to lowest (refer to graph)
Inhalation>Injection>Snorting/Sniffing>ingestion
34
Degree of Ionization
More ionized = less lipid soluble = less absorption = less effect
34
Brain Caplilaries
More selective (through lipid-soluble molecules)
34
What kind of drug can pass the lipid bilayer?
-Lipid soluble, neutral, small molecules
35
Other factors that affect rate of absorption
-Blood circulation at the site of administration -Surface area available for absorption -Amount of drug destroyed immediately (e.g. by stomach acids) -Extent of binding to inactive sites (depot binding
36
Pharmacodynamics
Subfield of pharmacology dealing with “the study of the biochemical effects of drugs and their mechanism of action
37
What is a Drug receptor?
the molecule(s) a drug (or other ligand) interacts with, to initiate its biological effects
38
What is the Law of Mass Action?
Maximal effect when all receptors are occupied; larger drug doses have a larger effect up to a certain point
39
What are Agonists?
A drug that binds to a receptor and has a biological effect
40
Do Agonists have intrinsic activity?
Yes
41
What are Antagonists?
They bind to receptors; have no intrinsic activity
41
What are the two characteristics of agonists?
potency and efficacy(max effect)
42
Why do some drugs have a higher potency than others?
- access of drugs to brain -- if it is lipophilic or not - some drugs have a higher affinity than others
43
True or False: Higher intrinsic activity = higher efficacy
True
44
Agonist vs. Antagonist
Agonist -- makes something happen antagonist -- blocks activity making no reaction
45
What are the forms of tolerance?
Acute, Protracted, Cross
45
What are inverse agonists?
If a drug reduces the ligand bonding activity
45
If drug effect gets bigger, it is...
Sensitization
45
If drug effect gets smaller it is....
Tolerance
46
What is Acute Tolerence?
Drug effect decreases rapidly - within a single session
47
What is Protracted Tolerance?
Drug effect decreases w/ repeated administration
48
What is cross tolerance?
Drug effect decreases with repeated administration of another drug
49
Mechanisms of Tolerance
Pharmacokinetic/Metabolic; Pharmacodynamic
50
What is dependence?
After tolerance, stopping the drug results in withdrawal - used instead of addiction
51
Significant characteristics of tolerance
- reversible when drug use stops - dependent on drug dose, frequency and environment - can happen rapidly, over long periods or never
52
Withdrawal results in
opposite feelings from what the drug does
53
With Sensitization the curve shifts...
to the left
54
Behavioral Pharmacology
The study between the physiological actions of drugs and their effects on behavior and psychological function
55
What are Unconditioned effects of drugs?
how drugs affect a wide range of naturally- occurring behaviors (lab experiments)
56
Conditioned effects of drugs
Train animals to perform tasks; examine how motivated the animals are to work for drugs
57
What is Drug Discrimination?
A method to ask animals about the interoceptive cues associated with diff drugs(how it feels)
58
Fixed Ratio
Reinforcement after every n responses ex. reward after every 5 responses
59
Fixed Interval
Reinforcement for the first press after a fixed delay
60
Advantages of a progressive ratio schedule?
Dose response is easier to interpret than FR1 Readily compare different drugs
61
Limitations to progressive ratio schedules
Just one data point
62
Long Access Models (LgA)
Administration for six hours a day Result: Use becomes excessive and uncontrolled
63
Short Access(ShA)
2 hour sessions
64
Synapse
Site of action for most psychoactive drugs
65
Are electrical synapses bidirectional?
Yes
66
Steps in chemical synaptic transmission
1. Synthesis 2. Transport 3. Storage 4. Release 5. Receptor binding 6. Inactivation
67
Steps in Secretion
1. Open Ca channels 2. Influx of Ca 3. Bind to Ca calmodulin 4. phosphorylation of proteins 5. proteins move into vesicles 6. exocytosis
68
What is the most toxic substance on Earth?
Botox
69
How do NT move/travel?
Diffusion
70
Terminating synaptic transmission: two ways
Enzymatic degradation Reuptake
71
Where do drugs act on the neuron
Outside on he receptors (Ligand binding)
72
Two Classes of NT receptors
Ionotropic (ligand gated ion channels) Metabotropic (G-protein-coupled receptors)
73
What are allosteric modulators
They can bind to receptors, alone have no effect but can modify action of agonist
74
Ligand-Gated Channels effects
fast and rapidly reversible
75
how many genes code for GPCrs
one gene; 7 segments; slower than ionotropic receptors
76
G-protein process
1. Receptor binds to ligand 2. Activates effector enzyme adenylyl cyclase 3. Converts to cAMP 4. Activates PKA 5. Phosphorylation 6. Response
77
How does it differ from signaling from the membrane to nucleus? (in gpcrs)
Will phosphorylate CREB to increase transcription of certain genes
78
Second messengers can alter gene regulation
True
79
Drugs can also have epigenetic effects
True --- can change gene expression for a lifetime