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CEP > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What is pharmacology good for

A

How to categorise drugs
Quantify drug action
Proper dosing
Benefits of drugs and side effects

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2
Q

What is pharmacology

A

The study of mechanism of DRUG ACTION
Effects of drug on body

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3
Q

What is a drug

A

Active ingredient of medicine
Any substance that interacts with a biological system and changes it

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4
Q

Drugs that produce their effects not by binding to receptor but due to their physicochemical properties

A

Antacids
Laxatives
Heavy metal antidotes
Osmotic diuretics
General anaesthetics

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5
Q

Potency

A

-Measure of drug activity
-Highly potent drug is only required in a very small dose
-potency is related to affinity

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6
Q

Types of specificity of drugs

A
  • Biological specificity (receptor wise)
  • Chemical specificity (drug wise)
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7
Q

How are drugs categorised? (7)

A
  • Chemical nature of drug
  • Symptoms/ disease in which they are used
  • Organ system affected
  • Receptor
  • Duration of action
  • Generations
  • Route of administration
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8
Q

Receptor concept

A
  • Drugs produce their effects by combining with their specific receptor sites in cells
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9
Q

What is a pharmacological
receptor?

A
  • any molecule to which a drug binds, thus initiating an effector mechanism leading to a specific pharmacologic response
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10
Q

What is affinity?

A

The binding strength of the drug receptor interaction or the likelihood of binding

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11
Q

What is the Endocrinological pathway of a drug

A
  1. Hormone producing cell
  2. Body
  3. Target cell
  4. Receptor
  5. Biological effect
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12
Q

Pharmacological pathway:

A
  • Drug
  • GI tract
  • target cell
  • receptor
  • biological effect
  • Health improvement
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13
Q

Endocrinological definition of a receptor

A

For a hormone a receptor is a biomolecule they have to bind to to exert their biological function

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14
Q

What is the nature of drug?

A

Anything that causes a physiological effect, when interacting with a drug’s receptor

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15
Q

Quantitive pharmacology?

A

Based on the assumption that drugs act by entering into a simple chemical relation with certain receptors in cells

Simple relation between the amount of drugs fixed by these receptors and the action produced

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16
Q

relationship between drug concentration and response?

A

Relationship is
–Continuous
–Saturating
–Exhibits threshold

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17
Q

What is assumed about the response (y axis) on the graph

A

That response is equal to the concentration of drug receptor complexes

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18
Q

What is Emax

A

The maximal response that the drug can produce

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19
Q

What shape curve does a log graph produce

A

Sigmoid curve

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20
Q

What is EC50?

A

The conc/ dose needed to produce 50% maximal response
= potency

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21
Q

Why is a graph useful?

A

Useful as it compares drugs that qualitatively have the same effect

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22
Q

Drug efficacy?

A

Maximal response a drug can produce once bound to receptor

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23
Q

What is an agonist?

A

Binds to receptor and produces a response

Possess affinity and efficacy

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24
Q

Antagonist

A

Bind to a receptor but do not produce a response

Prevent agonist binding and so block the response to an agonist

Possess affinity but not efficacy

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25
Q

What is Emax dependent on?

A
  1. Intrinsic activity. Ability of agonist to activate receptor.
  2. Agonist-receptor complexes. Depends on dose.
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26
Q

Full agonist?

A

100% Emax
Not all receptors need to be bound

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27
Q

Partial agonists?

A

All receptors occupied
But due to low intrinsic activity
Submaximal response

28
Q

What happens when a full agonist and partial agonist compete?

A
  • Full agonist will displace partial agonist and still achieve Emax
  • Curve displace to the RHS and Ec50 increases
  • FA potency decreases but efficacy same
29
Q

Competitive antagonists

A

Bind reversibly to receptor site
Don’t activate receptor
Inhibition of receptor can be overcome by more agonists

30
Q

Non competitive antagonists?

A

changes shape of receptor
Irreversible (covalent bond) / dissociates very slowly
Emax reduced and decreases agonist efficacy without affecting potency

31
Q

What is Kd

A

Numerically equal to the concentration of drug required to occupy 50% of sites at eqm

The higher the affinity the lower the Kd

32
Q

What is he difference between EC50 and Kd?

A

EC50 is the model free equivalent of a Kd value

33
Q

What is an endogenous agonist?

A

compound naturally produced by the body which binds to and activates a receptor

34
Q

What is the difference between an antagonist and an inhibitor?

A

An inhibitor is blocking the action of an enzyme which catalyzes a reaction.

An antagonist blocks the site of a receptor so that the receptor can’t respond to an appropriate stimulus.

35
Q

What are dirty drugs?

A

Bind to a receptor but also does other unwanted things

Sometimes beneficial “wanted side effects”

that means two different dosings of the same drug are actually
equivalent to TWO different drugs

36
Q

How do Steroid hormones act as dirty drugs?

A

At by binding to intracellular nuclear receptors but also activate membrane bound GPCRs

The effects of steroids often result from the interplay of the two mechanisms

37
Q

Examples of different drug receptors types:

A
  1. Enzymes
  2. Ion channels
  3. Transporters (pumps, transport proteins)
  4. “Physiological” receptors - receptors for hormones/ NT
38
Q

Types of agonists

A

Full inverse agonist
Partial inverse agonist
Silent antagonist
Partial agonist
Full agonist
Super agonist

39
Q

Ways of regulating cell function?

A
  1. Altered membrane potential
  2. Altered enzyme activity
  3. Altered gene expression
  4. Most drugs affect cell function via physiological receptors
40
Q

How drugs produce effects by binding to receptors?

A

Drug Agonism

A drug or substance that binds to a receptor inside a cell or on its surface and causes the same action as the substance that normally binds to the receptor

41
Q

How drugs block effects by binding to receptors- ways in which effects are blocked or reduced?

A

Antagonism
Desensitisation

42
Q

Patch clamp technique?

A

Makes response quantifiable
Electrode and micropipette inside of cell

43
Q

Inverse agonists?

A

Have negative efficacy

44
Q

What are spare receptors?

A

When there are more receptors present than are required to produce a maximal response when a ligand binds to them.

45
Q

Super agonists

A

Highly efficacious agonists
Can produce maximal response from cell without binding to all of the available receptors

46
Q

Partial agonist?

A

Low efficacy
Cannot produce cells maximal response
Even when they’ve bound to all receptors

47
Q

Example of an advantage of partial agonists

A

Buprenorphine is an opioid used to treat opioid addiction
Moderate acute and chronic pain
Less toxic as only partial

48
Q

Competitive antagonists

A

binds to the same site as the agonist but does not activate it, thus blocks the agonist’s action

49
Q

How are irreversible antagonists evidence of spare receptors?

A

may still see full biological effect even though there are irreversible agonists
Some receptor blocked by irreversible antagonists but agonist can bind to other receptors

50
Q

Types of antagonism

A

Competitive antagonists
Irreversible antagonists
Allosteric antagonists (non competitive)
Channel blockers
Physiological antagonists

51
Q

What is a protein degradation inducer

A

Same as a irreversible antagonist

52
Q

Allosteric antagonists

A

Bind reversibly at a diff distinct site from agonist
Decrease agonists affinity
Reduce likelihood of agonist binding

53
Q

Channel blockers

A

Bind inside the channel and prevent passage of ions
Binding of channel blockers enhanced by receptor activation

54
Q

Physiological antagonists

A

Antagonise the physiological effect of some agonists but via different mechanisms

55
Q

Response to drug may decrease due to:

A
  1. Desensitisation
  2. Tolerance
  3. Drug resistance
56
Q

Receptor classification based on:

A
  1. The basis of the selective action of the drug
  2. According to transmitter or hormone they interact with
    e.g. acetylcholine receptors
57
Q

Transmitters may act at more than one receptor? True or false

A

True. Completely diff receptor with same molecular function
ACh receptors:
1. Muscarinic
2. Nicotinic

Only after high affinity muscarinic ones has been poisoned do the low affinity nicotinic ACh receptors become visible

58
Q

Describe AChR?

A

5 SUBUNITS
2 ACh binding sites

59
Q

Muscarinic AChR structure?

A

G protein coupled receptor

60
Q

Names of receptor super families?

A
  1. Integral ion channels
  2. Integral tyrosine kinases
  3. Steroid receptors (nuclear receptors)
  4. G protein coupled receptors
  5. Cytokine receptors
61
Q

Integral ion channels?

A

Nicotinic receptor
Sit in extracellular membrane
Can open and close
Specific

62
Q

Integral tyrosine kinase receptor?

A

E.g. insulin receptor
No pore
Tyrosine in cytoplasmic domain trans phosphorylated by partner receptor
Allows propagation of signal via activated proteins

63
Q

Steroid receptor

A

E.g. Oestrogen receptor
Act in nucleus but located in cytoplasm
Ligand binding domain has folding sensor
Steroid hormone binds - folded
Dna binding domain allows binding to genes

64
Q

G protein coupled receptors mechanism?

A
  1. Iigand binds
  2. Conformational change
  3. Alpha subunit (GTP) dissociates from beta and gamma
  4. Alpha activated other proteins
  5. Signalling cascade (adenylyl cyclase - 2nd messenger)
  6. GTP hydrolyses into GDP
65
Q

Why is G protein coupled receptors 7 helices?

A

Sterics- more compact

66
Q

What are the 3 G subunits?

A

Gs
Gi
Gq

67
Q

Cytokine receptors?

A

E.g. Prolactin receptor
Binds to protein hormones
Big extracellular domain
Kinases bound non covalently to cytoplasmic domain
Dimerisation activates receptor

CEP (12 decks)

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