Lecture 3

Question 1

What is the difference between pharmacology and pharmacy?

Answer 1

Pharmacology: Study of mechanics by which drugs (biologically active compounds) affect the function of living systems.
Pharmacy: Study of formulation, dispensing and dosing

Question 2

What are receptors?

Answer 2

Proteins which recognize and bind ‘chemical mediators/ messengers’

Question 3

What are examples of chemical mediators?

Answer 3

hormones, neurotransmitters, antibodies

Question 4

What is the main function of receptors?

Answer 4

regulation of cellular processes

Question 5

What are the two types of cellular processes?

Answer 5

1. hormone recognition and binding

2. intracellular signal generation

Question 6

What are current proteins targeted by small molecule drugs?

Answer 6

1. ST/Y kinases 22%
2. GPCRs 15%
3. Cation channels 5%
4. Ser proteases (trypsin) 4%
5. Protein phosphatases 4%

Question 7

How much of drugs interfere with the function of receptors involved in chemical communication?

Answer 7

40%

Question 8

What are subclasses of receptors classified by structure?

Answer 8

1. carriers/transporters
2. enzymes
3. ion channels

Question 9

How many types of receptors are there?

Answer 9

1000

Question 10

What is an example of receptors that bind to different ligands?

Answer 10

Muscarinic ACh receptors

Ligands: ACh and nicotine

Question 11

What is an example of an accessory protein that binds to enzymes?

Answer 11

ATP

Question 12

What are drugs that bind to a receptor producing a response by mimicking the effect of chemical mediators?

Answer 12

Agonists

Question 13

What are examples of agonists?

Answer 13

Morphine, pilocarpine

Question 14

What is a poppy derived drug that interacts with pain-sensory neurons which mimics endorphins.

Answer 14

Morphine

Question 15

What is a side-effect of morphine?

Answer 15

Addiction from constant stimulus

Question 16

What does pilocarpine bind to?

Answer 16

Muscarinic ACh receptors in ANS

Question 17

What is an antagonist?

Answer 17

Drugs that prevent the response of an agonist

Question 18

What is an example of an antagonist?

Answer 18

atropine

Question 19

What is atropine an antagonist to?

Answer 19

pilocarpine

Question 20

What are examples of drugs which target ion channels?

Answer 20

Lignocaine, apamin, nifedipine ariloride

Question 21

Where is lignocaine found in?

Answer 21

Strepsils

Question 22

What is lignocaine?

Answer 22

Local anesthetic

Question 23

How does lignocaine work?

Answer 23

Binds to voltage gated sodium channels to stop their activity and prevent pain information inflammation, then pain nerve ending activation doesn’t reach CNS.

Question 24

Where is apamin found?

Answer 24

bees

Question 25

How does apamin work?

Answer 25

Blocks activity of voltage gated potassium channels so that pain nerve endings fire more AP

Question 26

What type of substance is nifidepine?

Answer 26

dihydropyridines

Question 27

What does nifidepine do?

Answer 27

Counteracts hypertension

Question 28

How does nifidepine work?

Answer 28

Blocks voltage gated calcium channels in smooth muscle lining arteries which reduces resistance to bring down hypertension

Question 29

Where does ariloride (an ENAC) work?

Answer 29

Kidneys

Question 30

What are examples of drugs which target enzymes?

Answer 30

acetylsalicylic acid, pargyline (and clorgyline), captopril

Question 31

Where is acetylsalicylic acid found?

Answer 31

aspirin

Question 32

Which enzymes does acetylsalicylic acid target to?

Answer 32

COX and MAO

Question 33

What does COX do?

Answer 33

Reduces pain associated with inflammation

Question 34

What does MAO do?

Answer 34

Breaks down noradrenaline, adrenaline

Question 35

What does Pargyline do?

Answer 35

Inhibits MAO against hypertension as a treatment against depression

Question 36

Where does pargyline affect?

Answer 36

CNS - unwanted side effects in CNS and PNS cannot be

Question 37

What is captopril?

Answer 37

ACE inhibitors

Question 38

What is captopril used for?

Answer 38

Treatment for hypertension

Question 39

How does captopril work?

Answer 39

Increases angiotensin by acting on an enzyme

Question 40

What are types of drugs that target transporters?

Answer 40

1. some need ATP and some need solutes 2. prevents action potential 3. may be hijacked and transport is utilized to get into cells

Question 41

What are examples of drugs that target transporters?

Answer 41

fluoxetine (prozac), Digoxin

Question 42

What is fluoxetine (prozac)?

Answer 42

It is a widely prescribed antidepressant more specific to the CNS

Question 43

What transmitters does fluoxetine target?

Answer 43

5-HT, serotonin

Question 44

How does fluoxetine work?

Answer 44

It blocks transport of serotonin so that it builds up outside of neurons to ctivate receptors for happiness

Question 45

Where is digoxin found?

Answer 45

In foxgloves

Question 46

What transporter does digoxin target?

Answer 46

Na/K transporter (exchanger)

Question 47

How does digoxin work?

Answer 47

1. Na in heart muscle builds up 2. Ca builds up in heart 3. Strength of contractility increases 4. Prolongs action potential

Question 48

What is a receptor superfamily?

Answer 48

Receptors which have similar structural features

Question 49

How many receptor superfamilies are there?

Answer 49

4: Ligand-gated ion channels (ionotropic receptors) G-protein-coupled receptors (metabotropic receptors) Kinase-linked receptors Nuclear receptors

Question 50

Which receptor superfamilies are found on the cell surface?

Answer 50

All except nuclear receptors

Question 51

How many hydrophobic amino acid segments are there in transmembrane spanning receptor proteins?

Answer 51

20-25

Question 52

Many drugs act via the _ domain.

Answer 52

ligand binding

Question 53

Nuclear receptors are DNA-linked. What does this mean?

Answer 53

They regulate gene transcription and the ligand must be able to cross the plasma membrane