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Pharmacology Flashcards

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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
What is Emax dependent on?
1. Intrinsic activity. Ability of agonist to activate receptor. 2. Agonist-receptor complexes. Depends on dose.
26
Full agonist?
100% Emax Not all receptors need to be bound
27
Partial agonists?
All receptors occupied But due to low intrinsic activity Submaximal response
28
What happens when a full agonist and partial agonist compete?
- 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
Competitive antagonists
Bind reversibly to receptor site Don’t activate receptor Inhibition of receptor can be overcome by more agonists
30
Non competitive antagonists?
changes shape of receptor Irreversible (covalent bond) / dissociates very slowly Emax reduced and decreases agonist efficacy without affecting potency
31
What is Kd
Numerically equal to the concentration of drug required to occupy 50% of sites at eqm The higher the affinity the lower the Kd
32
What is he difference between EC50 and Kd?
EC50 is the model free equivalent of a Kd value
33
What is an endogenous agonist?
compound naturally produced by the body which binds to and activates a receptor
34
What is the difference between an antagonist and an inhibitor?
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
What are dirty drugs?
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
How do Steroid hormones act as dirty drugs?
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
Examples of different drug receptors types:
1. Enzymes 2. Ion channels 3. Transporters (pumps, transport proteins) 4. “Physiological” receptors - receptors for hormones/ NT
38
Types of agonists
Full inverse agonist Partial inverse agonist Silent antagonist Partial agonist Full agonist Super agonist
39
Ways of regulating cell function?
1. Altered membrane potential 2. Altered enzyme activity 3. Altered gene expression 4. Most drugs affect cell function via physiological receptors
40
How drugs produce effects by binding to receptors?
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
How drugs block effects by binding to receptors- ways in which effects are blocked or reduced?
Antagonism Desensitisation
42
Patch clamp technique?
Makes response quantifiable Electrode and micropipette inside of cell
43
Inverse agonists?
Have negative efficacy
44
What are spare receptors?
When there are more receptors present than are required to produce a maximal response when a ligand binds to them.
45
Super agonists
Highly efficacious agonists Can produce maximal response from cell without binding to all of the available receptors
46
Partial agonist?
Low efficacy Cannot produce cells maximal response Even when they’ve bound to all receptors
47
Example of an advantage of partial agonists
Buprenorphine is an opioid used to treat opioid addiction Moderate acute and chronic pain Less toxic as only partial
48
Competitive antagonists
binds to the same site as the agonist but does not activate it, thus blocks the agonist's action
49
How are irreversible antagonists evidence of spare receptors?
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
Types of antagonism
Competitive antagonists Irreversible antagonists Allosteric antagonists (non competitive) Channel blockers Physiological antagonists
51
What is a protein degradation inducer
Same as a irreversible antagonist
52
Allosteric antagonists
Bind reversibly at a diff distinct site from agonist Decrease agonists affinity Reduce likelihood of agonist binding
53
Channel blockers
Bind inside the channel and prevent passage of ions Binding of channel blockers enhanced by receptor activation
54
Physiological antagonists
Antagonise the physiological effect of some agonists but via different mechanisms
55
Response to drug may decrease due to:
1. Desensitisation 2. Tolerance 3. Drug resistance
56
Receptor classification based on:
1. The basis of the selective action of the drug 2. According to transmitter or hormone they interact with e.g. acetylcholine receptors
57
Transmitters may act at more than one receptor? True or false
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
Describe AChR?
5 SUBUNITS 2 ACh binding sites
59
Muscarinic AChR structure?
G protein coupled receptor
60
Names of receptor super families?
1. Integral ion channels 2. Integral tyrosine kinases 3. Steroid receptors (nuclear receptors) 4. G protein coupled receptors 5. Cytokine receptors
61
Integral ion channels?
Nicotinic receptor Sit in extracellular membrane Can open and close Specific
62
Integral tyrosine kinase receptor?
E.g. insulin receptor No pore Tyrosine in cytoplasmic domain trans phosphorylated by partner receptor Allows propagation of signal via activated proteins
63
Steroid receptor
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
G protein coupled receptors mechanism?
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
Why is G protein coupled receptors 7 helices?
Sterics- more compact
66
What are the 3 G subunits?
Gs Gi Gq
67
Cytokine receptors?
E.g. Prolactin receptor Binds to protein hormones Big extracellular domain Kinases bound non covalently to cytoplasmic domain Dimerisation activates receptor

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