Pharmacology

Question 1

Define pharmacology

Answer 1

The study of substances that interact with living systems, usually through binding with regulatory molecules.

Either through enhancing or inhibiting a process. In terms of drugs, there is usually a mimicking of natural processes

Question 2

Define a drug

Answer 2

Any substance that interacts with a molecule or protein that plays a regulatory role in living systems

Question 3

Name an example of an endogenous drug

Answer 3

Hormones (neurotransmitters)

Question 3

What is a receptor?

Answer 3

A region of tissue or molecule that responds to a specific neurotransmitter, hormone, antigen or other substance.

Usually a protein.

Question 4

What are the names of agonists in terms of their level of activity?

Answer 4

Full agonist
Co-agonist
Selective agonist
Partial agonist
Inverse agonist
Superagonist
Irreversible agonist

Question 5

What is an endogenous ligand?

Answer 5

A ligand produced by the body and not administered by drugs

Question 6

What is an agonist?

Answer 6

Any drug that binds to a receptor and activates it. It mimics the endogenous ligands in the body.

When a ligand leaves it usually deactivates the receptor and stops the effect.

Some ligands cause covalent changes and keep the receptor permanently activated

Question 7

What are the 4 main types of receptors?

Answer 7

Ligand gated ion channels
G protein coupled receptors
Receptor tyrosine kinases (enzyme linked),
Nuclear receptors

Question 8

What is a full agonist?

Answer 8

A full agonist is a chemical or drug that binds to a receptor and activates it causing an enhanced response

It mimics the endogenous ligand exactly with the same affinity and same response

Question 9

What is a partial agonist?

Answer 9

A partial agonist is an agonist that binds to the receptor active site but is unable to cause the maximal response even if all the receptors are occupied

They usually have a lower affinity for the receptor and so don’t bind as strongly as the full agonist

Question 10

Compare partial and full agonists

Answer 10

Partial agonists have a lower affinity for the receptor compared to full agonists

Partial agonists at lower doses produce a greater response but can never reach the maximal response

Partial agonists have a wider therapeutic window and are safer to give to patients

Question 11

How do you figure out the volume of distribution?

Answer 11

Volume of distribution = total amount of drug / plasma concentration

Question 12

What happens when a drug is bound to a protein?

Answer 12

It becomes pharmacologically inactive

A drug needs to be free onto

Can’t be administration, distributed, metabolised, excreted (ADME)

Question 13

What is efficacy?

Answer 13

K

Question 15

What is potency?

Answer 15

K

Question 16

What is a non competitive antagonist?

Answer 16

K

Question 17

What is a competitive antagonist?

Answer 17

K

Question 18

How do G protein coupled receptors work?

Answer 18

Agonist causes a conformational change

Question 19

What are the properties of the G Protein coupled receptors?

Answer 19

Receptor binding point

7 transmembrane spanning domains

Question 20

How do ligand gated ion channels work?

Answer 20

There is a change in the cells electrical activity as a ligand binds which brings about a conformational change and then the specific ions that it is sensitive to can pass through along it’s concentration gradient

Question 21

What kind of a channel is NMDA?

Answer 21

Ca2+

Question 22

What kind of a channel is GABA?

Answer 22

Cl-

Question 23

What kind of receptors are common in the Nervous system?

Answer 23

Ligand gated ion channels

Question 24

How do tyrosine kinase receptors work?

Answer 24

Phosphorylation of the 2 tyrosine dimers on the membrane

Question 25

How do nuclear receptors work?

Answer 25

K

Question 26

Which type of receptors are the slowest?

Answer 26

Nuclear receptors

Question 27

What is the order of action of the four main classes of receptors? State the general time period

Answer 27

Ligand gated ion channels (milliseconds)
GPCR (seconds)
Receptor tyrosine kinase (minutes to hours)
Nuclear receptor (hours)

Question 28

What factors do you have to consider in drug design?

Answer 28

K

Question 29

What is tachyphylaxis?

Answer 29

Acute tolerance

Question 30

What is tolerance?

Answer 30

K

Question 31

What is buccal delivery?

Answer 31

Spray

Mucoadhesive

Question 32

What is intravenous delivery and what is it’s bioavailability?

Answer 32

Injection

100%

Question 33

Name different type of drug administration

Answer 33

Oral
Intravenous
Intramuscular
Subcutaneously
Rectum
Inhalation
Transdermal
Topical
Sublingual

Question 34

Why is the oral bioavailability low?

Answer 34

Some of it goes to the fat, plasma, muscle

Question 35

How long do orally administrated take to work?

Answer 35

5-30 minutes

Question 36

What does sublingual administration mean and how does it work, how long does it take?

Answer 36

Taking a drug under the tongue
Bypasses the 1st pass metabolism (the liver) and enters the systemic blood directly
2-3 minutes

Question 37

What does transdermal administration mean and give an example?

Answer 37

Applied to skin
Crosses the skin to enter systemic blood supply
Nicotine patches

Question 38

Define clinical pharmacology

Answer 38

K

Question 39

Define a medicine

Answer 39

K

Question 40

Define therapeutics

Answer 40

K

Question 41

Explain 1st order metabolism

Answer 41

K

Question 42

Explain zero order metabolism

Answer 42

I