PED1003/L01 Intro to Drug Action

Question 1

Define pharmacology.

Answer 1

What the drug does to the body
What the body does to the drug

Question 2

Where do drugs typically come from? (2)

Answer 2

Plants or fungi

Question 3

Where is aspirin derived from?

Answer 3

Willow tree bark

Question 4

Where is morphine derived from?

Answer 4

Opium poppy

Question 5

Where is psilocybin derived from?

Answer 5

‘Magic’ mushroom

Question 6

How are synthetic drugs created in the laboratory? (3)

Answer 6

Novel medicinal chemistry
Identical to natural compounds (mimics)
Derived from natural compounds

Question 7

Define pharmacodynamics.

Answer 7

The effect of the drug on the body

Question 8

What molecular interactions does pharmacodynamics focus on? (3)

Answer 8

Targets for drug action
How drugs act at target
How drug produces action within cell

Question 9

How is the influence of drug concentration on magnitude of response shown?

Answer 9

Graphically with dose-effect relationships

Question 10

What does study of pharmacodynamics allow?

Answer 10

Determine appropriate dose range for patients
Compare efficacy and safety of one drug to another

Question 11

What is the distance between 2 lines on a dose-response curve called?

Answer 11

Therapeutic window

Question 12

Define pharmacokinetics.

Answer 12

The effect of the body on the drug

Question 13

Give the phases involved in pharmacokinetics. (4)

Answer 13

Absorption into blood
Distribution into ICF and ECFs of tissues
Metabolism - inactivation through enzymes
Excretion through urine, bile or faeces

Question 14

What does study of pharmacokinetics allow? (3)

Answer 14

Determination of:
Route of administration
Frequency of dosing
Treatment duration

Question 15

Give 3 other considerations of drugs.

Answer 15

Hydrophobicity
Ionisation of drug (pKa)
Conformation of target
Stereochemistry of drug

Question 16

Give 3 targets for drug action.

Answer 16

Receptors
Ion channels
Carrier molecules
Enzymes

Question 17

What is the drug target of salbutamol?

Answer 17

B2 adrenoreceptor
For asthma

Question 18

What is the drug target for lidocaine?

Answer 18

Voltage-gated sodium ion channel
Local anaesthetic

Question 19

What is the drug target for aspirin?

Answer 19

Cyclooxygenase
Analgesic

Question 20

What is the drug target for omeprazole?

Answer 20

Proton pump
Anti-ulcer

Question 21

Give 2 factors that alter drug interaction with targets.

Answer 21

Shape
Charge distribution

Question 22

Explain the difference between an agonist and an antagonist.

Answer 22

Agonists act as a pseudosubstrate
Antagonists inhibit

Question 23

How do many diseases arise?

Answer 23

Abherrant cell signalling

Question 24

Briefly describe how an antagonist works.

Answer 24

Binds to a receptor which inhibits agonist response/blocks binding

Question 25

Give the 4 receptor sub-types.

Answer 25

Ligand-gated ion channels G-protein coupled Enzyme (kinase) linked receptors Intracellular receptors

Question 26

Describe the effects of benxodiazepine on GABA receptors. (4)

Answer 26

Binds to allosteric site Alters structure of receptor GABA binds Enhances the effects of GABA

Question 27

What do all adrenoreceptors have in common?

Answer 27

All subunits activated by adrenaline/noradrenaline

Question 28

Describe the function of a1 adrenoreceptors.

Answer 28

Activates PLC Vasoconstriction

Question 29

Describe the function of a2 adrenoreceptors.

Answer 29

Inhibit adenylyl cyclase Auto-inhibition of neurotransmitter release

Question 30

Describe the function of B1&2 adrenoreceptors.

Answer 30

Stimulate adenylyl cyclase B1 - accelerated HR B2 - bronchodilation

Question 31

Briefly describe the action of receptor tyrosine kinases.

Answer 31

Ligand binding Dimerisation Autophosphorylation

Question 32

Give 2 examples of nuclear oestrogen receptor substrates.

Answer 32

Estradiol Tamoxifen

Question 33

Describe class I nuclear receptors. (3)

Answer 33

Located in cytoplasm Form homodimers Ligands are endocrine

Question 34

Describe class II nuclear receptors. (3)

Answer 34

Present in nucleus Form heterodimers Ligands are lipids