Pharmacodynamics: drug binding to receptors & their effects on the body
Affinity: ability of drug to bind to receptor
o Closer to Y axis = higher affinity
Higher Ka (Association constant/ affinity) most likely means lower
dose and frequency
Potency: quantity of drug required to achieve desired effect
o Closer to Y axis = higher potency
Efficacy: how well a drug produces a response
o Maximal height
Graded dose-response curve: increasing response to increasing dose
o Efficacy
Quantal dose-effect curve: proportion of population will respond to drug at
given dosages
o Closer to Y axis = higher potency
Steep slope: little dose increase has large response (risk of toxicity)
Partial agonist vs full agonist:
o Full agonist: maximal effect which is measured by intrinsic activity
o Partial agonist: does activate receptors, but cant elicit maximal response
Can’t compare potency/ affinity
Although they occupy the receptors equally the full agonist will
have higher level of efficacy, but sometimes there are unwanted
effects
Competitive (reversible) antagonist:
o Block receptors of drug, but can be kick off by increasing the drug
Parallel shift right
Non-Competitive (irreversible) antagonist:
o Block receptors of drug & cant be kicked off
Non-parallel shift down & to the right
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, *** If EC50 is less than Kd, we know that the drug can produce 50% of its
maximal effects while occupying less than 50% of the receptors ***
Suppose we have a drug with an EC50 value of 1 mole/liter and a Kd value of 2
moles/liter.
o This drug can produce 50% of its maximal effect at a concentration that is
one-half the concentration necessary to occupy 50% of the receptors.
*** Indicates that the number of receptors present exceeds
the number needed to produce the maximal effect ***
Potentiation: 2 or more drugs/agents together are more potent than
the drugs individually.
o Curve moves left
Quantal (All or None) Dose Response Curve: describes the
distribution of MINIMUM doses of a drug required to produce a
response for a group of people
Toxicity & Therapeutic Index (TI): reality safety of a drug
o TI = Toxic Dose 50
Effective Dose 50
G-Coupled Protein Receptor Cascade (2 pathways)
This study source was downloaded by 100000868424010 from CourseHero.com on 06-20-2024 12:45:33 GMT -05:00
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