Introduction

Question 1

what are opium alkaloids used for

Answer 1

• obtained from the latex of papaver somniferum
• known for its analgesic and sedating properties

Question 2

give examples of opium alkaloids

Answer 2

• morphine
• codeine
• noscapine

Question 3

what is the activity of morphine

Answer 3

• analgesic
• antitussive
• reduced gastric motility
• respiratory depressant

Question 4

when was the hypodermic syringe invented

Answer 4

1853
- increased medical use of opium
- challenges in formulation and sterility

Question 5

what year was insulin first used to treat diabetes

Answer 5

1922

Question 6

what year was the first vaccine for influenza discovered

Answer 6

1945

Question 7

when was paracetamol first sold as an analgesic in UK

Answer 7

1956

Question 8

what does the traditional approach to drug discovery involve

Answer 8

1. isolation and purification of active substance
2. structural modifications to active substance
   3.screening of groups of molecules

Question 9

what does the traditional drug discovery process involve

Answer 9

1. test molecule is synthesised on mg to g scale
2. sent for bioassay testing
3. data returned and analysed
4. structural changes made and new molecule synthesises and tested

Question 10

what does the modern drug discovery process involve

Answer 10

1. target identification
2. target validation
3. lead discovery
4. lead optimisation
5. pharmacological and toxicological profiling
6. formulation development
7. marketing authorisation

Question 11

what are the most common human target classes

Answer 11

• G protein coupled receptors
• enzymes
• transporters
• nuclear receptors

Question 12

what does the search for new drug targets require

Answer 12

1. knowledge of physiology/pathology- elucidation of biochemical pathways and regulatory systems
2. knowledge of mechanisms of actions of drugs, poisons, toxins and venoms
3. structural similarities in biomolecules suggesting new targets
4. genomics- search for new receptors, enzymes, ion channels on the basis of amino acid sequence homology with similar known targets

Question 13

what is needed to exploit a drug target

Answer 13

1. need information on:
   - structural nature of target
   - possible mechanism of interaction between target and potential drugs
2. need to develop an assay that accurately measures the activity of the target
   - dose dependent response
   - capable of comparison with other ligands