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10 Cards in this Set
- Front
- Back
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What is a chemical antagonism? |
When one drug antagonises the action of another by chemically combining with it |
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What is physiological antagonism? |
When two drugs counteract each other by producing opposing effects in different receptors |
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What is pharmacological antagonism? |
When antagonist binds to a receptor and Stops an agonist binding the same receptor types |
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How do you measure the antagonist affinity in the lab? |
Construct an agonist concentration response curve Then add a concentration of antagonists and see what happens to the curve |
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What happens by increasing the agonist concentration? |
It will restore the response |
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What are the principles of competitive antagonism ? |
Antagonist interact with a receptor according to the law of mass action Antagonist had an affinity for the receptor There is competition between the antagonist and agonist for the receptor The effect of the antagonist is surmountable ie. Adding increasing concentrations of agonist will restore the response to original value |
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What is the Gaddum equation |
PA=XA/XA+KA(1+XB/KB) |
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What is non competitive antagonism? |
Antagonists that act at sites other than the agonist binding site are classified as non competitive antagonists These drugs like irreversible competitive antagonists produce non parallel rightward shifts of agonists concentration response curves |
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What are allosteric modulators ? |
Competitive antagonists bind to the orthosteric site Allosteric modulators bind to an allosteric site And be negative Or positive or neither Can effect the binding smog the agonist or efficacy of the agonist |
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Why might allosteric modulations be good drugs? |
Lots of variation easier to Anne a selective modulator Modulators don’t tend to block the receptor competently so less likely tk have severe side effects |
