Discuss the impact of drug binding on receptors
View the conformational change of shape caused by endogenous substrate binding
Receptors exist as inactive, active, or desensitized
Discuss drug (ligand) and receptor binding.
Describe/define free receptor and occupied
Explain how increase in drug concentration or receptor concentration will increase the effect of a drug.
Use the mathematical dissociation formula to demonstrate the relationship
Read and discuss a paper which focused on the physiology and pharmacology of prostaglandin and thromboxane synthesis. The pathway of synthesis from arachidonic acid to prostaglandin and thromboxane and the cyclooxygenase enzyme required.
Discuss the action of thromboxane in clot formation, and how aspirin inhibits the COX2 enzyme required, thereby acting to prevent clot formation.
Examine how drug-receptor binding results from multiple chemical interactions between molecules.
Define and explain binding affinity
Read article on prostaglandins
Examine the binding effect by sterio isomers.
Use images to define and explain sterio-isomerism.
Discuss dextro and levo forms of certain drugs, and why one form is more active than another. Use warfarin and methorphan as examples. Levomethorphan is a strong opiate analgesic while dextromethorphan (DM) is a powerful cough suppressant. Think Robitussin DM.
Discuss drug binding and conformation of the receptor shape.
Discuss receptor binding sites. Show from a sketch the binding of histamine to the specific receptor.
Discuss the unique chemical characteristics determined by the specific amino acids which make up the protein receptor
Define and discuss affinity.
Define and discuss inactive receptors. Us aspirin as an example of a drug which irreversibly attaches to a specific receptor which allows the production of prostaglandins and anti inflammatory responses.
Stress that receptor binding sites are highly specific.
Discuss the question "why does one drug affect cardiac function while another affects kidney function.
Discuss the answer in terms of drug-receptor interactions
Discuss the specificity of the receptors based on their protein structures
Display a diagram of the 4 different protein structures.
Indicate why small drug molecules bind better to macromolecular receptors
Indicate that the shape determines its function and location.
Define a drug and discuss bioactive species-
Define pharmaceuticals-
List all the parameters which pharmacology encompasses-
Discuss pharmacodynamics and pharmacokinetics-
Explain "ADME" and the derivation from the Greek for pharmacology-
Discuss which areas of science are important to the study off pharmacology. These include biology, chemistry, anatomy and physiology and medicine.
Indicate that the science is concerned with:
1) drug action
2) the interaction that occurs between a living organism and chemicals which affect behavior.
Hand out information sheets which will be used in the discussion of the history of pharmacology
Session Minutes
45
Minutes Student Attended
45
Lesson Comments
Nina seemed upbeat and very relaxed. It was good to deal with her this way.
With the use of a video, the major developments in the theory of the atom was shown in graphic form. The modern Bohr atom and atomic cloud theory were also examined. These were used to reinforce the development of the theories which will allow us to move forward to the next unit.
Session Minutes
60
Minutes Student Attended
60
Lesson Comments
Nicole exhibited wonderful insight as the theories progressed. She pointed out that each scientist built on the work of the previous scientist, and was able to discuss it insightfully