EXAM 1 Flashcards

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
Q

What is the difference between a competitive and non-competitive
antagonist? Relate to response curve

A

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

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21
Q

What is an autoreceptor?

A

Receptors on a terminal where the same NT binds

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21
Q

We talked about a lot of different self-administration procedures,
which best captures the behavioral and pharmaco-kinetic profile of
drug abuse?

A

Intermittent Access(IntA) self administration procedure

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21
Q

Which of the two major types of synapses do drugs of abuse typically act on?

A

Chemical synapses

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21
Q

What are the two major types of synapses in the
brain?

A

Electrical and Chemical

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22
Q

Starting with the binding of a neurotransmitter to a Gs-
coupled GPCR, describe the pathway leading to a
change in gene transcription.

A

The catalytic subunit of
PKA can cross the
nuclear membrane to phosphorylate CREB to increase/decrease transcription of certain genes

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22
Q

Where are neurotransmitters stored after synthesis, but before release?

A

Vesicles

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23
Q

Psychopharmacology

A

Influence of drugs on behavior and psychological function

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23
Q

Pharmacology

A

Brand of medicine that deals with the uses, effects, and modes of action of drugs

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24
Q

What is a Drug?

A

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

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24
Q

Neuropsychopharmacology

A

Influence of drugs on brain, behavior and psychological function

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25
Q

Neuropharmacology

A

Influence of drugs on brain function

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26
Q

What are the ways to name and classify drugs?

A

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

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26
Q

What are the naturally occuring drugs and where do they come from?

A
  1. Opium from unripe seed pods of opium poppy
  2. Cocaine, from the leaves of the coca plant
  3. Ephedrine, extracted from Ephedra plant
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27
Q

What are some semisynthetic drugs?

A
  1. Heroin from Morphine
  2. LSD from grain ergot fungus
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28
Q

What are some synthetic drugs?

A

Fentanyl (synthetic opioid)
Amphetamine (powerful stimulant)
MDMA (Ecstasy: stimulant+ hallucinogen)

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29
Q

Analgesics

A

Morphine
Codine

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29
Q

What are the Stimulants?

A

-Amphe
-Coke
-Nic

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29
Q

What are the three main questions of pharmacokinetics?

A

How much drug?
How Fast?
How long to activate?

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29
Q

Drug Schedule #1

A

substances that have no accepted medical use and high abuse potential

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29
Q

What are the CNS depressants?

A

Barbiturates and alcohol

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29
Q

Hallucinogens

A

LSD and Psilocybin

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30
Q

Drug Schedule #4

A

Even lower abuse potential than 3

30
Q

Drug Schedule #2

A

Substances that have a high abuse potential w/ severe psych or physical dependence liability

30
Q

Drug Schedule #3

A

Substances with lower abuse potential than 1 and 2

31
Q

Drug Schedule #5

A

Contain limited amounts of narcotics and used for medical use.

31
Q

Cons of Oral Admin

A

First pass metabolism – the amount of drug that gets lost in stomach acid before it goes into blood
(Poor control)

32
Q

Pharmacokinetics

A

the life and movement of a drug from its site of action till excretion

32
Q

What is the most common route of administration?

A

Oral (PO)

32
Q

Pros of Oral Administration

A

Easy and more accessible
Slow and steady concentration (No spikes)

33
Q

ALL Routes of Admin

A

Oral, IV, IM, SC, Inhale, Topical, Transdermal, Intranasal

33
Q

Non-invasive routes of drug administration

A

Oral
Nasal – up nose
Sublingual – under tongue
Rectal – Up anus
Transdermal
Inhale – smoking

33
Q

What if Half-Life in terms of drugs?

A

Time for plasma drug conc to fall to half of peak level

33
Q

Subcutaneous Injection (SC)

A

Needle under skin, not into muscle
In the skin layer(epithelium)

33
Q

Intramuscular Injections (IM)

A

Into Muscle (absorbed faster – more in blood)

33
Q

Intravenous Injection (IV)

A

Into Vein – directly into circulatory system

33
Q

where doesn’t the IV dyes spread e

A

CSF and Brain

33
Q

How did the BBB arise?

A

Distinct properties of brain capillaries

33
Q

What are the different routes of administration in order from highest peak to lowest (refer to graph)

A

Inhalation>Injection>Snorting/Sniffing>ingestion

34
Q

Degree of Ionization

A

More ionized = less lipid soluble = less absorption = less effect

34
Q

Brain Caplilaries

A

More selective (through lipid-soluble molecules)

34
Q

What kind of drug can pass the lipid bilayer?

A

-Lipid soluble, neutral, small molecules

35
Q

Other factors that affect rate of absorption

A

-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
Q

Pharmacodynamics

A

Subfield of pharmacology dealing with “the study of the biochemical effects of drugs and their mechanism of action

37
Q

What is a Drug receptor?

A

the molecule(s) a drug (or other ligand) interacts with, to initiate its biological effects

38
Q

What is the Law of Mass Action?

A

Maximal effect when all receptors are occupied; larger drug doses have a larger effect up to a certain point

39
Q

What are Agonists?

A

A drug that binds to a receptor and has a biological effect

40
Q

Do Agonists have intrinsic activity?

A

Yes

41
Q

What are Antagonists?

A

They bind to receptors; have no intrinsic activity

41
Q

What are the two characteristics of agonists?

A

potency and efficacy(max effect)

42
Q

Why do some drugs have a higher potency than others?

A
  • access of drugs to brain – if it is lipophilic or not
  • some drugs have a higher affinity than others
43
Q

True or False: Higher intrinsic activity = higher efficacy

A

True

44
Q

Agonist vs. Antagonist

A

Agonist – makes something happen
antagonist – blocks activity making no reaction

45
Q

What are the forms of tolerance?

A

Acute, Protracted, Cross

45
Q

What are inverse agonists?

A

If a drug reduces the ligand bonding activity

45
Q

If drug effect gets bigger, it is…

A

Sensitization

45
Q

If drug effect gets smaller it is….

A

Tolerance

46
Q

What is Acute Tolerence?

A

Drug effect decreases rapidly - within a single session

47
Q

What is Protracted Tolerance?

A

Drug effect decreases w/ repeated administration

48
Q

What is cross tolerance?

A

Drug effect decreases with repeated administration of another drug

49
Q

Mechanisms of Tolerance

A

Pharmacokinetic/Metabolic; Pharmacodynamic

50
Q

What is dependence?

A

After tolerance, stopping the drug results in withdrawal
- used instead of addiction

51
Q

Significant characteristics of tolerance

A
  • reversible when drug use stops
  • dependent on drug dose, frequency and environment
  • can happen rapidly, over long periods or never
52
Q

Withdrawal results in

A

opposite feelings from what the drug does

53
Q

With Sensitization the curve shifts…

A

to the left

54
Q

Behavioral Pharmacology

A

The study between the physiological actions of drugs and their effects on behavior and psychological function

55
Q

What are Unconditioned effects of drugs?

A

how drugs affect a wide range of naturally- occurring behaviors (lab experiments)

56
Q

Conditioned effects of drugs

A

Train animals to perform tasks; examine how motivated the animals are to work for drugs

57
Q

What is Drug Discrimination?

A

A method to ask animals about the interoceptive cues associated with diff drugs(how it feels)

58
Q

Fixed Ratio

A

Reinforcement after every n responses

ex. reward after every 5 responses

59
Q

Fixed Interval

A

Reinforcement for the first press after a fixed delay

60
Q

Advantages of a progressive ratio schedule?

A

Dose response is easier to interpret than FR1
Readily compare different drugs

61
Q

Limitations to progressive ratio schedules

A

Just one data point

62
Q

Long Access Models (LgA)

A

Administration for six hours a day
Result: Use becomes excessive and uncontrolled

63
Q

Short Access(ShA)

A

2 hour sessions

64
Q

Synapse

A

Site of action for most psychoactive drugs

65
Q

Are electrical synapses bidirectional?

A

Yes

66
Q

Steps in chemical synaptic transmission

A
  1. Synthesis
  2. Transport
  3. Storage
  4. Release
  5. Receptor binding
  6. Inactivation
67
Q

Steps in Secretion

A
  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
Q

What is the most toxic substance on Earth?

A

Botox

69
Q

How do NT move/travel?

A

Diffusion

70
Q

Terminating synaptic transmission: two ways

A

Enzymatic degradation
Reuptake

71
Q

Where do drugs act on the neuron

A

Outside on he receptors (Ligand binding)

72
Q

Two Classes of NT receptors

A

Ionotropic (ligand gated ion channels)
Metabotropic (G-protein-coupled receptors)

73
Q

What are allosteric modulators

A

They can bind to receptors, alone have no effect but can modify action of agonist

74
Q

Ligand-Gated Channels effects

A

fast and rapidly reversible

75
Q

how many genes code for GPCrs

A

one gene; 7 segments; slower than ionotropic receptors

76
Q

G-protein process

A
  1. Receptor binds to ligand
  2. Activates effector enzyme adenylyl cyclase
  3. Converts to cAMP
  4. Activates PKA
  5. Phosphorylation
  6. Response
77
Q

How does it differ from signaling from the membrane to nucleus? (in gpcrs)

A

Will phosphorylate CREB to increase transcription of certain genes

78
Q

Second messengers can alter gene regulation

A

True

79
Q

Drugs can also have epigenetic effects

A

True — can change gene expression for a lifetime