1. Introductory pharmacology

Question 1

What is a drug?

Answer 1

A drug is “any chemical which affects physiological function in a specific way”

Question 2

What is pharmacology?

Answer 2

How the function of living things is altered by chemical agents

Question 3

What is the ending ‘PRIL’ representative of?

Answer 3

Angiotensin converting enzyme inhibitors - they block the synthesis of vasoconstrictor peptide angiotensin 2. Prevents the constriction of blood vessels.

Question 4

What is the first source of drugs?

Answer 4

Individual chemicals purified from cells and tissues. e.g. plants

Question 5

Where does atropine come from?

Answer 5

Atropa belladona

Question 6

Where does morphine come from?

Answer 6

Papaver somniferum

Question 7

What is another source of drugs?

Answer 7

Individual chemicals purified from cells and tissues e.g amphibians, reptiles etc

Question 8

What can be derived from pigs?

Answer 8

Porcine insulin

Question 9

Where does streptokinase come from?

Answer 9

Haemolytic bacteria

Question 10

What is another source of drugs? and give examples

Answer 10

Chemical synthesis by pharmaceutical industry e.g. ephedrine paved the way for salbutamol.

Question 11

What is another source of drugs? and give examples

Answer 11

Chemical synthesis by the pharmaceutical industry e.g. drug discoveries

Question 12

What is the fifth source of drugs and give examples

Answer 12

Large scale production of recombinant human proteins, e.g. , human insulin. And antibodies to human proteins e.g. cytokine mediators for treating inflammatory disease.

Question 13

What ways do most drugs bind?

Answer 13

Reversibly via ionic bonds. Van Der Waals are also a factor.

Question 14

What can happen when you take drugs.

Answer 14

They cause a desired effect in one target but can cause an adverse effect in the same target but in a different area.

Question 15

In practice what are drugs?

Answer 15

Selective rather than specific - which means unwanted effects are common.

Question 16

How should you think of drugs?

Answer 16

They’re like the ball you push shapes into, some shapes can fit in the other holes although they will not be as good a fit they will still fit. Thats how adverse affects come about.

Question 17

What are the molecular targets for drug action?

Answer 17

Proteins 
- ion channels 
- membrane transporters 
- enzymes 
- non-cellular proteins 
- receptors 
Nucleic acids 
Miscellaneous targets

Question 18

What are the different types of ion channels are drug targets?

Answer 18

Blockers
Allosteric modulators
- Inhibitor
- Facilitor

Question 19

What do blockers do and whats some examples?

Answer 19

They physically block the open ion channels. E.g. lidocaine - local anaesthetic. Blocks the Na+ ion channel therefore no action potentials can be produced.

Question 20

What do allosteric modulators do?

Answer 20

They chase a shape change in channel proteins on binding elsewhere on the protein.

Question 21

What is the difference between an allosteric inhibitor and facilitator?

Answer 21

Inhibitors cause less ions to enter - less response and facilitator cause more ions to enter - greater response

Question 22

What is an inhibitor modulator - Amlodopine

Answer 22

Treats hypertensions, angina pectoris. Blocks electrically gated Ca2+ ion channels. It dilates blood vessels causing blood pressure to reduce and coronary muscle relaxation. This means coronary blood flow is increased and more oxygen gets to the heart.

Question 23

What is a facilitator modulator - Benzodiazepine

Answer 23

Binds to GABA(a) to enhance channel opening by GABA. The increased Cl- conductance reduces neuronal excitability.

Question 24

What is GABA?

Answer 24

An inhibitory neurotransmitter, therefore is you increase the incidence of GABA it becomes less inhibitory.

Question 25

What are two examples of membrane transporters as drug targets?

Answer 25

Inhibitors and false substrates

Question 26

What do inhibitors do? e.g.

Answer 26

They block the transport mechanism. E.g. furosemide. It is a loop diuretic which prevents NaCl reabsorption in the thick ascending loop of henle. Therefore more urine is produced. It does this by inhibiting the Na+/K+/2Cl- co transporters in the luminal membrane combining with the chloride binding site.

Question 27

How do false substrates work? e.g. Amphetamine

Answer 27

Accumulation of the false substrate competes with and prevents the movement of the natural substrate. Amphetamine is a better competitor for the NA binding site.

Question 28

What are two examples of enzymes as drug targets?

Answer 28

Inhibitors and pro-drugs

Question 29

What is an example of an enzyme inhibitor?

Answer 29

Binds to substrate site (reversibly or irreversibly), or allosteric regulatory site, or disrupt enzyme integrity.
E.g. lisinopril which targets ACE, thus reduces the constrictor angiotensin 2

Question 30

What are pro-drugs?

Answer 30

They first require conversion by an enzyme to form the active form. e.g. perindopril - ACE inhibitor - that is converted to the active form perindoprilat

Question 31

What are some non-cellular proteins as drug targets?

Answer 31

Antibodies to inflammatory protein mediators e.g. infliximab for rheumatoid arthritis and inflammatory bowel disease.
e.g. Heparin - anticoagulant - activates anti-thrombin 3 in blood which inhibits the clotting cascade

Question 32

Who are nucleic acids a target for drug action

Answer 32

Cisplatin is an anti-cancer drug which covalently cross links DNA and prevents replication, transcription and prepare. Therefore promoting cell death.

Question 33

What is an antacid

Answer 33

Non-protein target for drug action, neutralise gastric acid.

Question 34

What else can drugs target?

Answer 34

Antibiotics etc used in the prevention or treatment of infections.