Introduction to Pharmacology

Question 1

What is Thermodynamics?

Answer 1

The effect a drug has on the body (biological effects and mechanisms)

Question 2

What is Pharmacokinetics?

Answer 2

How the body responds to the drug.

Question 3

Name X3 Drug Targets

Answer 3

• Proteins
• DNA
• RNA

Question 4

What are Agonistic Drugs?

Answer 4

Mimics a neurotransmitter and binds to a receptor to activate and produce a cellular response.

Question 5

Explain the X3 step how an Agonistic drug functions.

Answer 5

1) Agonist binds to receptor, this is reversible. (Binding step)
2) Receptor undergoes a conformational. (Affinity Steps)
3) Change in receptor conformation which activates the receptor. This is temporary.

Question 6

Are Agonistic and Antagonistic drugs effects reversible?

Answer 6

-YES

Question 7

What X2 Features does Agonistic drugs have?

Answer 7

• Efficacy

- Affinity

Question 8

What is Efficacy?

Answer 8

• The ability a drug has to evoke a cellular response

- (‘e’-effect)

Question 9

What is Affinity?

Answer 9

• This is attraction between receptors and ligand (drugs)

- Determined by the chemical bonds between ligands and receptors.

Question 10

What are Antagonistic Drugs?

Answer 10

-1) Bind to receptors (reversible) and block them. DO NOT ACTIVATE

Question 11

Why do Antagonists not have Efficacy?

Answer 11

-They do NOT evoke e cellular response because they bind rot the receptor and block binding-No response occurs

Question 12

What x2 types of graphs can show relationship between concentration and dose?

Answer 12

• Sigmoidal

- Hyperbolic- Logarithmic (more accurate)

Question 13

Compare the Efficacies between Partial and Full Agonists

Answer 13

Partial-Low Efficacy

Full-High Efficacy

Question 14

What is drug potency?

Answer 14

The amount of a drug that is needed to produce a given effect

Question 15

What is Reversible Competitive Antagonism?

Answer 15

-When Antagonist drug blocking effect can be overcome by increasing the concentration of the Agonist drug.

Question 16

What is the name of the site where Competitive Antagonists and Agonist drugs bind?

Answer 16

-Orthosteric Site

Question 17

Where do Non-Competitive Antagonistic Drugs bind?

Answer 17

• Separate site

- Allosteric site

Question 18

What X2 things happen to a curve graph when Competitive and Non-Competitive Antagonists bind?

Answer 18

Competitive- Parallel shift to RIGHT (competitive- always right :)
Non-Competitive- Depresses the slope

Question 19

What affect does increasing concentration of an Agonist?

Answer 19

-Shifts curve to the RIGHT

Question 20

What effect does increasing concentration of a Competitive Antagonist and Non-Competitive have?

Answer 20

Competitive-Shifts more to the right

Non-Competitive- Depresses slope further

Question 21

What do Hydrophilic Signalling Molecules include?

Answer 21

neurotransmitters, hormones, endogenous molecules, peptides etc.

Question 22

What are Ligand-Gated Ion Channels?

Answer 22

Open in response to ligand binding

-Transmembrane Proteins

Question 23

What are G-Protein Coupled Receptors (GPCRs)?

Answer 23

Targeted by ‘Therapeutic Agents’-drugs

• Signal via Secondary Messenger Systems
• inbox for messages in the form of light energy, peptides, lipids, sugars, and proteins.

Question 24

What are Kinase-Linked Receptors?

Answer 24

uses second messenger signaling that triggers a cascade of cellular events.

Question 25

What are Nucleated Receptors?

Answer 25

- In nucleus - Slow timescale-hours/days - Alter gene expression

Question 26

What type of channel are Voltage Gated Ion Channels: ?

Answer 26

- Ligand Gated | - Opne in response to voltage

Question 27

How do G-Protein Coupled Receptors control effector activity?

Answer 27

-Secondary Messenger Systems

Question 28

How are G-Protein Coupled Receptors linked to Secondary Messenger Systems?

Answer 28

-Intermediate-G-Proteins

Question 29

What type of protein are receptors?

Answer 29

-Integral

Question 30

What is the structure of a receptor's polypeptide and what terminus to they possess?

Answer 30

- NH2 and COOH Termini | - Single Polypeptide Chain

Question 31

Wha is the structure of a G-Protein Coupled Receptor?

Answer 31

Polypeptide chain is connected to X7 transmembrane spans- are 3 intracellular AND 3 extracellular connecting loops

Question 32

What is the result when G-Protein Coupled Receptors are activated and what is this process called?

Answer 32

- Activation of G-Proteins | - G-Cycle

Question 33

What are the X3 G-Protein sub-units?

Answer 33

Alpha, Beta and Gamma

Question 34

What type of protein are G-Proteins?

Answer 34

-Peripheral (Outside)

Question 35

What do G-Proteins called and act as when activated?

Answer 35

- Intermediate-G-Proteins | - Intermediate between G-Protein Coupled Receptors and Effectors

Question 36

Explain what happens in the G-Cycle

Answer 36

Active State: - Alpha sub-unit dissociates off from polypeptide - GTP binds to Alpha sub-unit - GDP dissociates off (not-needed) Deactivation of GCPRs: - Agonist dissociates off from receptor - Signalling can continue because G-Protein has been already activated - Alpha sub-units acts as an enzyme and breaks the GTP that’s is attached > GDP +Pi - Signal now turned off - Alpha sub unit re-joins polypeptide - G Cycle is COMPLETE!

Question 37

Are receptors used as signalling pathways?

Answer 37

- YES | - Bind to signalling molecules to form signalling pathway

Question 38

What type of signalling molecules are Steroid Hormones?

Answer 38

-Hydrophobic

Question 39

What type of cascade is formed by Kinase-Linked receptors once bound to hydrophilic signalling molecules-causing Phosphorylation ?

Answer 39

- Phosphorylation cascade | - As kinase enzymes trigger phosphorylation

Question 40

How do Nucleated Receptors Signal?

Answer 40

- This causes dissociation of Inhibitory HSP protein - Hydrophilic and receptor complex moves to the nucleus and form a ‘Dimer’ (two receptors joint) - and binds to HREs (Hormone Response Elements)

Question 41

What does 'Transpressed' and 'Transactivated' mean in Transcription?

Answer 41

-Switched on= Transactivated | Switched off =Transpressed

Question 42

What type of factors are Nucleated Receptors

Answer 42

- Transcription Factors | - Control DNA Transcription