Introduction to Pharmacology

Question 1

What is pharmacodynamics?

Answer 1

What a drug does to a body (Drug Action)

Question 2

What is Pharmacokinetics?

Answer 2

What the body does to a drug (Drug Handling)

Question 3

What medicines were used up until the 19th century? What were the issues with this?

Answer 3

Herbal remedies such as the bark of the white willow tree.
- Unpredictable amounts of the drug within it
- Hundreds of unwanted contaminants

Question 4

What were the three steps for the creation of aspirin?

Answer 4

1853: Chemical structure of salicylic acid is determined, chemically synthesises acetylsalicylic acid. However it was ineffective and toxic.
1897: Aspirin created with no contaminants, more efficacy and less toxicity.
1971: Researched published describing aspirins mechanism of action.

Question 5

Where do drugs act?

Answer 5

Receptors, usually located in membranes or cytoplasm.

Question 6

What is the term for when a drug reaches its maximum reaction?

Answer 6

When a drug reaches its maximum Dose Dependent Response it is called a Saturable Maximum Response.

Question 7

Why are log graphs used for dose response curves?

Answer 7

1. Related compounds give parallel curves
2. Potencies are easily determined
3. Linear between 20-80% of maximum response
4. Displays entire concentration range
5. Effects of antagonists shown

Question 8

What are covalent and non covalent drugs?

Answer 8

Covalent = Reversible
Non-Covalent = Irreversible

Question 9

What is the most ideal selectivity of a drug?

Answer 9

• Very. Not just for a transmitter or enzyme but for the interaction of that with a particular tissue.
• However most drugs have multiple actions (side effects such as morphine and constipation)

Question 10

What is the meaning of potency?

Answer 10

The concentration of a drug that is required to give a response. For example 500mg of paracetamol is much less strong than 500mg of morphine.

Question 11

What is efficacy/intrinsic activity?

Answer 11

How big the response of the drug is. Does it make your head not hurty or does it make you completely unconscious? rather important to know.

Question 12

What is an Agonist drug?

Answer 12

A drug that produces a response by binding and inducing a change to an active configuration.

Question 13

What is an Antagonist drug?

Answer 13

A drug that blocks a response by binding to the same sites but does not induce an active conformation. By binding, it prevents access to the agonist.

Question 14

What is a physiological antagonist drug?

Answer 14

Agents which have mutually antagonistic responses but act through different receptors.

Question 15

What is a pharmacological antagonist drug?

Answer 15

A drug which prevents the action of an agonist at its receptor.

Question 16

What do full agonist drugs show on a dose response curve?

Answer 16

Parallel shifts = All have the same maximum effect/efficacy, but at different doses.

Question 17

What do partial agonist drugs show on a dose response curve?

Answer 17

One will have a lower maximum response/efficacy and they wont be parallel.

Question 18

What are competitive antagonist drugs?

Answer 18

Drugs binding to the same receptor that have no change in maximum response and give a parallel shift to the right.
- Includes partial agonists

Question 19

What are the characteristics of an Irreversible antagonist?

Answer 19

• Covalently bind to the agonist binding site
• Effect cant be overcome by addition of more agonist
• Reduces maximum response

Question 20

What is acetylcholine activated by?

Answer 20

Nicotine. NOT MUSCARINE. However it is a natural agonist at both types of receptors (important because this gives the possibility of selectively targeting a receptor subtype)

Question 21

Describe a muscarinic receptor.

Answer 21

G-Protein coupled
- Intestinal smooth muscle, heart, blood vessels, salivary glands, CNS

Question 22

Describe a nicotinic receptor.

Answer 22

Ligand-gated ion channels
- Skeletal muscle, ganglia, CNS
- Pentameric structure many different subunits (8 α and 4 β which have different channel opening times)

Question 23

Describe an insulin receptor.

Answer 23

• A tyrosine kinase receptor
• Binding of insulin causes conformation change, activating tyrosine kinase catalytic domain.
• Found on most cells in the human body.

Question 24

Describe a Glucocorticoids Receptor.

Answer 24

• Nuclear receptor.
• Intracellular receptors = transcription factors.
• Found in brain, liver, muscle, immune system and fat cells.