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Terms in this set (17)
Therapeutic Index = LD50/ED50. The farther apart the curves are for effective and lethal dose range, the safer the drug will be.
Drug reactivity Terms:
Hyperreactivity: the usual effect at lower than norm doses. Happens in skinny people, low metabolism, and lots of receptors or coupling of receptors.
Hyporeactivity: the usual effect at higher than norm doses.
Happens in fat people, high metabolism, and fewer receptors.
Tolerance is a type of hyporeactivity from previous exposure to a drug (think of a druggy).
Tachyphylaxis is a type of tolerance that develops after only a few doses of a drug.
Drugs are never specific in their actions, they are...
side effects are...
1) a consequence of the primary action of the drug
2) dose dependent
3) can be produced because of a separate property of the drug (like acting on more than one target)
What is toxicity? How is it corrected?
Toxicity is an extension of the desired effect. It is correct by LOWERING the dosage.
What does the biological activity of a drug usually correlate with?
Its chemical structure.
True or false? Drugs impart new function to a cell or tissue.
Drugs only modify the existing condition. They DO NOT impart a new function.
What are two levels of mechanisms of action that drugs participate in?
Physiological level: effects on cells and tissues....stimulation, depression, initiation of response, alteration of response.
Biochemical level: Interaction with enzymes, other proteins, DNA, RNA, cell membrane constituents.
Most drug receptors are ...
Macromolecules like proteins, nucleoproteins, and enzymes. Some drugs though have relatively nonspecific interactions.
What are four variations in response to drugs that can happen at a receptor level?
-alterations in [drug] acting on the receptor
-variations in [endogenous ligand] for a receptor
-alteration in number, subtype, or function of a receptor
-changes in levels of secondary messengers
What type of curve results from plotting a dose vs response on:
- hyperbolic curve
-symmetrical sigmoid curve
What are the four characterizing parameters of dose-response curves?
-potency:shown on the dose axis (x axis)
-slope: big changes if steep, smaller changes if gradual
-maximal efficacy (same as maximal effect)
-variability: vertical bracket is the range of effects from a given does administered to a group.....horizontal bracket is the range of doses required to produce a specific response in a group of individuals
Terms for receptor interactions and effects:
Full agonists: bind preferentially to the activated receptor. They produce the maximal possible response.
Partial agonists: result in less than maximally activated receptor population
Antagonists: bind to either the active or inactive form of receptor so the equilibrium results in the same number of activated and inactivated receptors sooooo there is NO OVERALL EFFECT.
Inverse agonist: favor equilibrium that makes the overall receptor population become inactive. It would produce the opposite effect of an agonist.
Name the parts of the simple formulation of agonist-receptor interaction.
Receptor Occupancy x Efficacy x Receptor Number
The maximal effect of a drug depends on its concentration and fraction receptor occupancy.
Antagonists can inhibit....
What are two types of antagonists? What is their effect and what do they look like on a curve?
Antagonists can interact with a receptor to inhibit the action of the agonist.
Competitive antagonists (equilibrium competitive or reversible competitive): shift the does response curve to the right....in other words they decrease potency.
Non-competitive (non-equilibrium or irreversible competitive): shift the dose response curve to the right and reduce the maximal effect/efficacy. These types reduce the number of available receptors.
Spare receptors are demonstrated by...
non-competitive antagonists irreversibly blocking a major part of the receptors, but maximal response to the agonist still being possible. As you increase the concentration of non-competitive antagonists, the maximal effect/efficacy starts to decrease as the antagonist binds more of the spare receptor population.
Distinguish between potency and efficacy.
Potency: how much drug is required to produce a certain effect.
Efficacy: the maximum effect a drug can produce.
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