pharmacology
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| Pharmacodynamics | the study of the biochemical and physiologic effects of drugs and the molecular mechanisms by which effects are produced
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| The dose- response relationship is | graded. The response becomes progressively larger with increasing dosage
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| Maximal efficacy | is the most intense effect a drug can produce
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| A drug with a very high maximal efficacy is not always most desirable as | the intensity of the drug response must be matched to the patient's needs.
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| potency | is defined as the amount of a drug that must be given to elicit an effect
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| It is important to note that the potency of a drug implies nothing about it's | maximal efficacy
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| A receptor | can be defined as any functional macro- molecule in a cell to which a drug binds to produce its effects
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| Binding of a drug to its receptor is usually | reversible
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| the receptors through which drugs act are | normal points of control for physiologic processes
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| under physiologic conditions, receptor function is regulated by | molecules supplied by the body
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| All that drugs can do at receptors is | mimic or block the body's own regulatory molecules
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| Because drug action is limited to mimicking or blocking the body's own regulatory molecules, | drugs cannot give cells NEW functions. Only alter the rate of pre-existing capabilities.
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| Drugs produce their therapeutic effects by | helping the body use its pre-existing capabilities to the patient's best advantage.
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| It should be possible to synthesize drugs that can | alter the rate of any biologic process for which receptors exist
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| The four primary families of receptors are | 1.) cell membrane- embedded enzymes, 2.) ligand- gated ion channels, 3.) G- protein- coupled receptor systems and 4.) transcription factors
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| Selective Drug Action is possible largely because drugs act | through specific receptors
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| If a drug interacts with only one type of receptor and that receptor regulates just a few processes | the drug will have limited effects
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| Selectivity does not guarantee | safety
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| affinity | the strength of the attraction between a drug and its receptor
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| Drugs with high affinity are | very potent
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| intrinsic Activity | the ability of a drug to activate a receptor upon binding
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| drugs with high intrinsic activity have high | maximal efficacy
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| Agonist | are molecules that activate receptors
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| Agonists have both | affinity and high intrinsic activity.
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| Affinity and high intrinsic activity allows agaonists | bind to receptors and activate that receptor after binding
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| Antagonists produce their effects by | preventing receptor activation by endogenous regulatory molecules and drugs
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| Antagonists have affinity for receptors but lack of intrinsic activity prevents | the bound antagonists from causing receptor activation
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| If no agonist is present | administration of a antagonists has no observable effect
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| Antagonists are subdivided to two major classes | noncompetitive antagonists and competitive antagonists
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| Noncompetitive antagonists | bind irreversibly to a receptor
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| Competitive Antagonists | Bind reversibly to a receptor
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| Partial agonists have only moderate intrinsic activity | which meancs their maximal efficacy is lower than that of full agonists.
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| (desensitized) When the receptor continually exposed to an agonist,the cell... | becomes less responsive
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| Desensitized | refractory, (down regulation)
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| Continuous exposure to antagonists causes | the cell to become hyper sensitive (super-sensitive)
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| Most effects from drugs results from | drug receptor interactions
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| Other ways that drugs effects arise | physical or chemical interactions with other small molecules
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| The dose required to produce a therapeutic response can | vary substantially from patient to patient
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| The average effective dose (ED50) | is the dose required to produce a defined therapeutic response in 50% of the population
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| Standard dose | ED50
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| After a patient's response to standard dose has been evaluated, subsequent doses are | altered accordingly
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| Because drug responses are not completely predictable, the nurse must evaluate the patient to determine | if more or less of the medication has been administered.
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| Therapeutic Index | LD50:ED50
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