DRUG TARGETS - AGONISTS AND ANTAGONISTS Flashcards

You may prefer our related Brainscape-certified flashcards:
1
Q

Define Pharmacology

A

The study of drugs on living systems

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Define Pharmacodynamics

A

The mechanisms of drug action which explains variations in drug responses, adverse drug reactions and drug-drug interaction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Define Pharmacokinetics

A

It is the absorption, distribution, metabolism and excretion of drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Define agonist

A

A drug that binds to a receptor and produces an effect that mimics the repose to a neurotransmitter, hormone etc

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What type of activity can agonist drugs have

A

They have both affinity and intrinsic activity (efficacY)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Define partial agonist

A

Cannot produce a maximum effect even though all receptors may be occupied

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What is the difference between partial and full agonists

A

The efficacy of a partial agonist is less than that of a full agonist

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Define antagonist

A

A drug that decreases the action of another drug or endogenous ligand

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What type of activity do classic antagonist drugs have

A

Classic competitive antagonists have affinity for the receptor but no intrinsic activity.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

In order to assert an effect what must a drug do

A

Bind to a specific protein on living tissues

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Why can side effects occur when taking a drug

A

As the protein that a drug can bind to may be present in the body other than the intended site

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Which proteins can drugs target in the body

A
  1. Enzymes
  2. Transporters
  3. Ion channels
  4. Receptors
  5. DNA and RNA
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What are receptor operated ion channels

A

Those which require the binding of drugs to open their gate letting ions flow in or out of the cell across cell membranes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Name a complex receptor

A

G protein coupled receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

How many domains do G protein coupled receptors

A

Can have 7 domains that span the cell membrane

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What happens when GTP binds

A

Intracellularly, three subunits interact when GTP binds due to the action of other enzymes or ion channels inside the cells

17
Q

How do nuclear receptors work

A

The ligand has to enter the cell to bind inside to its receptor

18
Q

What happens when nuclear receptors are activated

A

The ligand-receptor complex binds to a specific DNA sequence in the nucleus
This alters the gene expression

19
Q

Do G protein couples receptors respond faster or nuclear receptors

A

G protein couples receptors respond faster

But nuclear receptors have a longer lasting affect

20
Q

Name some factors that can affect the effectiveness of a drug

A
  1. Genetics
  2. Age
  3. Diet
  4. Existence of disease
  5. Drug-drug interactions
21
Q

What is the therapeutic index

A

The ‘window of activity’ where it can be said that the benefits outweigh the risks

22
Q

What does it mean when a drug has a narrow therapeutic index

A

Means the toxicity or adverse drug reactions occur when the recommended maximal dose in the blood is exceeded

23
Q

What does it mean when a drug has a BROAD therapeutic index

A

Means that the maximum blood level lays comfortably between that which is needed to induce therapeutic effect and that which would risk inducing serious toxicity

24
Q

What does NNT stand for when looking at drug effectiveness

A

Number needed to treat

25
Q

What is the number needed to treat (NNT)

A

The number of people you need to give a drug to for one single person to prevent an adverse outcome from the disease you are treating

26
Q

What does an NNT of 5 means

A

NNT of 5 means 5 people will receive the drug before 1 of them benefits

27
Q

Do we want the NNT high or low

A

as low as possible

28
Q

What can happen to drug response as time goes by

A

It can change- patients can become desensitised or even supersensitised

29
Q

What can recurrent dosing with an agonist drug lead to

A

Tolerence or tachyphylaxis

30
Q

What is tolerance

A

A diminished repose occurring over days to weeks

31
Q

What is tachyphylaxis

A

The same effect as tolerance but it develops rapidly after a small number of doses only

32
Q

What can long term treatment with an antagonist lead to

A

Super sensitivity by changes in the number of receptors

33
Q

What are biologics

A

Biopharmaceutical agents with immunomodulatory properties

34
Q

What are biologics used in

A

Used for inflammatory chronic or malignant disease

35
Q

What are biologics made up of

A

A variety of active agents including proteins, monoclonal antibodies and fusion protein

36
Q

Give examples of biologics

A

Insulin
Erythropoietin
Infliximab