L2 Sources of drugs and their nature

• What are the three critical areas at the intersection of the modern pharmaceutical industry?


  Biomedical sciences, chemistry, and therapeutics
• In what year did Paul Ehrlich show that syphilis can be treated with arsenical compounds?


  1909
• What was the first sulphonamide antibacterial developed by the Bayer company?


  Prontosil
• What significant era in drug development occurred during the 1960s, 70s, and 80s?


  The era of rational drug design
• Who led the era of rational drug design?

  Sir James Black
• What revolutionized the drug discovery process in the 1990s?

  Techniques such as high throughput screening and combinatorial chemistry
• What happened to Thalidomide in 1961?


  It was withdrawn
• What significant scientific milestone occurred in 2002?


  The human genome was mapped
• What is the focus of basic research in universities regarding drug discovery?

  It leads to a better understanding of physiology and disease mechanisms
• What is identified during the drug discovery process?


  Potential drug targets, usually proteins that play a crucial role in a disease
• What hypothesis is generated in the drug discovery process?


  A drug that acts on a target to change its activity will be effective in treating the disease
• What is an example of the drug discovery process involving adrenaline?


  • Adrenaline relaxes smooth muscle in the airway (bronchodilation)
  • Asthma causes bronchoconstriction
  • Target: Beta receptor on bronchial smooth muscle
  • Hypothesis: A drug mimicking adrenaline will relieve asthma symptoms
• What are some considerations during the drug development process?

  Safety, ethical issues, intellectual property, and cost
• What are the steps involved in drug discovery?

  1. Hypothesis
  2. Assay systems
  3. Natural products
  4. Compound libraries
  5. Combinatorial chemistry
  6. Potential drugs
  7. Animal models
  8. Active chemicals
  9. Chemical optimisation
• What do pharmaceutical companies build up to aid drug discovery?


  Huge chemical libraries containing millions of chemical compounds
• What is the challenge in screening chemical libraries?


  How to screen many compounds to see if they have the desired action
• What is high-throughput screening?


  A method to quickly identify compounds with required biological activity
• How does combinatorial chemistry work?


  • Reacts attachment points with different substituents
  • Increases the number of potential compounds
  • Example: 2 attachment points with 3 substituents yields 9 compounds
  • Example: 3 attachment points with 8 substituents yields 512 compounds
• What is the benzodiazepine skeleton used for?


  It is the basis for numerous anxiolytic and hypnotic drugs
• What is the purpose of assay techniques in drug discovery?


  To identify potential drugs from chemical libraries
• What is the purpose of Phase I clinical trials?


  To check for safety and tolerability in healthy volunteers
• How many patients are typically involved in Phase IIa trials?


  50-200 patients
• What is the primary purpose of Phase II clinical trials?


  To evaluate the drug's effectiveness and safety compared to current treatments
• What is the role of drug regulatory bodies?


  To oversee the approval and monitoring of drugs
• What is the purpose of Phase IV clinical trials?


  To monitor long-term effects and drug interactions after market release
• What is pharmacovigilance?


  Monitoring the safety of a drug after it has been licensed
• What does the "Yellow Card" system in the UK monitor?


  Adverse effects and drug interactions post-market