Summary: Pl2201

Read the summary and the most important questions on PL2201

• 1 General Principles of Pharmacology

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• List the desirable properties of drugs

  1. Specific action 
  2. Potent (only need small dosage for wanted effect) 
  3. Appropriate duration of action 
  4. Easy to administer/convenient for patient 
  5. Minimal side-effects/toxicity at therapeutic doses
  6. Low cost = ready availability

• List the undesirable properties of drugs

  1. Adverse effects 
  2. High dose needed
  3. Organ toxicity 
  4. Teratogenic 
  5. Difficult to administer 
  6. Poor tissue access (needs higher dose) 
  7. Expensive = poor availability

• What are the defining characteristics of drug-receptor interaction

  1. Based on 3D-fit = lock and key model
  2. Involves chemical interactions 
  3. Usually reversible

• Is covalent or non-covalent bond preferred for drug-receptor interaction?

  Non-covalent bond is preferred for drug-receptor interaction because they are much more reversible than covalently bonded drug and receptor

• What motion allows drugs to bind to receptors?

  Random/Brownian motion because drugs don't know where it is supposed to go, so they will only interact when they reach their destination. 

• What is Ka (affinity) equivalent to?

  Ka = concentration of drugs needed to bind to 50% of available receptors at equilibrium

• What does [D] near receptor determine?

  Response

• What makes [DR] proportional to [D] and [R]?

  Dynamic equilibrium = constant binding and dissociation of drugs and receptors

• What is proportional to the size of a cell response?

  Proportion of time a receptor molecule spends in the DR form is proportional to the size of a cell response

• What reduces the time each ligand spends receptor-bound?

  Competition of 2 ligands for a same binding site on a receptor