Wk 9

Question 1

What is pharmacology?

Answer 1

The study of all aspects relating to drugs or medicine.

Question 2

What is pharmacodynamics?

Answer 2

The action of the drug (how drugs affect the body).

Question 3

What are the two types of pharmacodynamics?

Answer 3

1. Qualitative aspects (how do they produce their effects?, targets)
2. Quantitative aspects (magnitude of response)

Question 4

What is pharmacokinetics?

Answer 4

The fate of the drug (how the body affects drugs? absorption, distribution).

Question 5

What is pharmacotherapeutics?

Answer 5

The use of the drug treatment.

Question 6

What is a side-effect?

Answer 6

A drug effect that is NOT the primary purpose for giving the drug (desirable or undesirable).

Question 7

What is an adverse drug reaction?

Answer 7

Unintended and undesirable response to a drug.

Question 8

What is pharmacy?

Answer 8

Branch dealing with manufacture, preparation and dispensing of drugs.

Question 9

What is pharmaceutics?

Answer 9

Preparation and dispensing of drugs.

Question 10

What is formulation?

Answer 10

Form in which the drug is administered.

Question 11

What is indication?

Answer 11

The illness or disorder that the drug is used for.

Question 12

What is contraindication?

Answer 12

Situation/condition where drug should NOT be used or with caution.

Question 13

What are the 3 names used for each drug?

Answer 13

1. Chemical name
2. Approved (generic) name
3. Proprietary (brand) name

Question 14

What are the stages of drug development?

Answer 14

1. Drug discovery (target selection)
2. Preclinical development (short-term toxicology)

Clinical Development:
3. Phase I (small # of subjects)
4. Phase II (long-term toxicology)
5. Phase III (large # of subjects)

6. Regulatory approval (submission)
7. Phase IV (post marketing surveillance)

Question 15

What are the 3 molecular targets for drugs?

Answer 15

1. Proteins (channel-linked receptors, GPCR, kinase-linked receptors, nuclear receptors)
2. Nucleic Acids
3. Miscellaneous targets

Question 16

What are the 4 types of receptors?

Answer 16

1. Channel-linked receptors
2. GPCR
3. Kinase-linked receptors
4. Nuclear receptors

Question 17

What are channel-linked receptors?

Answer 17

• located at membrane
• ion channel effector
• direct coupling
• responds in milliseconds
• e.g. glutamate, GABA A

Question 18

What are GPCR?

Answer 18

• located at membrane
• enzyme/ion channel effector
• coupling via G protein
• responds in seconds
• e.g. adrenoceptors, opiates

Question 19

What are kinase-linked receptors?

Answer 19

• located at membrane
• enzyme phosphorylation effector
• direct coupling (dimerization)
• responds in minutes
• e.g. insulin receptor, growth factors

Question 20

What are nuclear receptors?

Answer 20

• located at nucleus
• gene transcription effector
• coupling via response elements
• responds in hours
• e.g. steroid, hormone

Question 21

What are the 3 drugs that are acting at receptors?

Answer 21

1. Agonists
2. Antagonists
3. Allosteric modulators

Question 22

What is an agonist?

Answer 22

ACTIVATE target receptor
- mimic endogenous (internal) messengers
- affinity & efficacy for receptor

Question 23

What is an antagonist?

Answer 23

BLOCK target receptor
- prevent signal being sent
- only affinity for receptor

Question 24

What are allosteric modulators?

Answer 24

• drugs that act on modulatory site of receptor
• control response to endogenous chemical

Question 25

What is affinity?

Answer 25

The ability of a drug to BIND to a receptor.
high affinity = strong binding

Question 26

What is efficacy?

Answer 26

Once bound to receptor, the ability to ACTIVATE receptor and produce RESPONSE.

Question 27

What is the relationship between drug concentration and effect?

Answer 27

The HIGHER the drug concentration, the MORE rapid the effect is to a certain level.

Question 28

What is agonist potency?

Answer 28

Concentration that produces a certain pharmacological response.

More potent = given response at lower dose

Question 29

What is the commonly used measure of agonist potency?

Answer 29

EC50
conc. of agonist which produces 50% of the maximal response.

Question 30

What is the difference between full and partial agonists?

Answer 30

Full agonists - can achieve maximal response (high efficacy)

Partial agonists - can never achieve maximal response even at high conc. (low efficacy)

*same affinity for receptor

Question 31

What is constitutive activity?

Answer 31

Receptor is active without ligand binding (car is on but just idling).

Question 32

What are inverse agonists?

Answer 32

• decrease constitutive activity
• NEVER completely stops it

Question 33

What is a receptor antagonist?

Answer 33

Prevent or reduces the action of agonist drugs at the same receptors.

Question 34

What are the two types of antagonism?

Answer 34

1. Competitive (agonist & antagonist bind at same site on receptor)
   - Reversible (can overcome effect of antagonist)
   - Irreversible (can NOT overcome effect of antagonist)
2. Non-competitive (binds to receptor at different side to agonist)