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30 Cards in this Set

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Antagonist
Drugs that decrease the actions of another drug or endogenous ligand; reverses or blocks the effect of an agonist and makes the agonist less potent; "blockers"; has no actions of its own and produces no efect by themselves; has no efficacy
Competitive Antagonist
Competes for the same binding sites as the agonist; can displace the agonist from the binding site if the affinity is > than the agonist; the agonist can reach 100% biological response if the agonists's concentration or affinity is sufficient; the duration of action is dependent on the 1/2 life
Example: Nalaxon vs. morphine
Non-competitive Antagonist
Permanently and strongly bind to a different receptor site than the agonist in order to reduce or block the effect of the agonist; the agonist will never reach 100% biological response; the Kd of the agonist will not change; the Emax decreases
Allosteric Modulators
Bind to a different receptor than the agonist and either inhibit or enhance the action of the agonist.
Binding
Causes: (1) Conformational change in the receptor which leads to immediate functional changes, (2) inhibition of action by covering an active receptor site, (3) Coupling (deals with tranduction) -- the drug produces a change in the receptor, the association with proteins results in the clinical effects; the physiologic and chemical processes that occur as a result of binding; it often occurs extra-cellularly -- the act of coupling allows extra-cellular messages to be transmitted to intracellular organelles which control cell function
Pharmacology
What the drug does to the body; including interaction @ the receptor sites and drug effects on the target organs.
Efficacy
The response produced by the drug.
Maximum Efficacy
The maximum response the drug illicits (when all the receptors are saturated)
Potency
The amount of drug given to produce a response
ED50
The dose required for 50% of people to exhibit the desired response.
LD50
The dose required for 50% of people to exhibit lethal effects.
Therapeutic Index
A crude measurement of drug safety based on animal toxicity data.
Therapeutic Window
The safe and effective dose range
Affinity
The degree of attraction that a drug has for the receptor site
Kd
The dissociation constant; a measure of affinity; indicates drug potency
Emax
The drug concentration that produces the maximal effect.
EC50
The drug concentration that produces 1/2 the maximal effect; EC50 = Kd
Bioavailability
The rate and extent to which a drug is absorbed or is otherwise available to the treatment site in the body.
Receptor
A protein molecule of the cell where binding occurs
Agonist
An exogenous or endogenous compound that binds to the receptor, causing a change in the receptor and resulting in a biological response
Saturability
A finite number of receptors on a cell; a filling up of receptors; maximal response when fully saturated.
Simple Occupance Theory
The maximal drug response when all receptors are occupied/saturated (after that point, increasing the drug concentration will not increase the response
Reversibility
The ability of the ligand receptor to associate and dissassociate
Idiosyncratic Drug Response
A response that is infrequently observed; often caused by genetic differences in drug metabolism or immunologic mechanisms.
Example: a drug is given with a resulting reaction in someone able to tolerate it previously
Hyporeactive/Hyperreactive Responses
Responses to a drug that are > or < than one would expect to see in the population.
Tolerance
A decrease in responsiveness of a drug over time.
Example: narcotic analgesics
Tachyphylaxis
A decrease in the responsiveness of a drug rapidly with continued administration.
Example: Transdermal NTG
Homeostatic Reserve
Modulation of the response by compensating for the drug's effect.
Example: The elderly have a decreased homeostatic reserve.
Up-Regulation
An increased number of receptors; occurs with the administration of an antagonist resulting in an increase in the total number of receptors; must be weaned slowly from the antagonist.
Example: A sudden discontinuing of beta-blockers results in rebound HTN due to large influx of agonist in increasing number of receptors
Down-Regulation
A decreased number of receptors from the administration of agonist decrease in coupling of receptors; is clinically seen as drug tolerance -- the client will require an increased dose of medication.