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Chapter 5 pharmaco
pharmacology
Question | Answer |
---|---|
Pharmacodynamics | the study of the biochemical and physiologic effects of drugs and the molecular mechanisms by which effects are produced |
The dose- response relationship is | graded. The response becomes progressively larger with increasing dosage |
Maximal efficacy | is the most intense effect a drug can produce |
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. |
potency | is defined as the amount of a drug that must be given to elicit an effect |
It is important to note that the potency of a drug implies nothing about it's | maximal efficacy |
A receptor | can be defined as any functional macro- molecule in a cell to which a drug binds to produce its effects |
Binding of a drug to its receptor is usually | reversible |
the receptors through which drugs act are | normal points of control for physiologic processes |
under physiologic conditions, receptor function is regulated by | molecules supplied by the body |
All that drugs can do at receptors is | mimic or block the body's own regulatory molecules |
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. |
Drugs produce their therapeutic effects by | helping the body use its pre-existing capabilities to the patient's best advantage. |
It should be possible to synthesize drugs that can | alter the rate of any biologic process for which receptors exist |
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 |
Selective Drug Action is possible largely because drugs act | through specific receptors |
If a drug interacts with only one type of receptor and that receptor regulates just a few processes | the drug will have limited effects |
Selectivity does not guarantee | safety |
affinity | the strength of the attraction between a drug and its receptor |
Drugs with high affinity are | very potent |
intrinsic Activity | the ability of a drug to activate a receptor upon binding |
drugs with high intrinsic activity have high | maximal efficacy |
Agonist | are molecules that activate receptors |
Agonists have both | affinity and high intrinsic activity. |
Affinity and high intrinsic activity allows agaonists | bind to receptors and activate that receptor after binding |
Antagonists produce their effects by | preventing receptor activation by endogenous regulatory molecules and drugs |
Antagonists have affinity for receptors but lack of intrinsic activity prevents | the bound antagonists from causing receptor activation |
If no agonist is present | administration of a antagonists has no observable effect |
Antagonists are subdivided to two major classes | noncompetitive antagonists and competitive antagonists |
Noncompetitive antagonists | bind irreversibly to a receptor |
Competitive Antagonists | Bind reversibly to a receptor |
Partial agonists have only moderate intrinsic activity | which meancs their maximal efficacy is lower than that of full agonists. |
(desensitized) When the receptor continually exposed to an agonist,the cell... | becomes less responsive |
Desensitized | refractory, (down regulation) |
Continuous exposure to antagonists causes | the cell to become hyper sensitive (super-sensitive) |
Most effects from drugs results from | drug receptor interactions |
Other ways that drugs effects arise | physical or chemical interactions with other small molecules |
The dose required to produce a therapeutic response can | vary substantially from patient to patient |
The average effective dose (ED50) | is the dose required to produce a defined therapeutic response in 50% of the population |
Standard dose | ED50 |
After a patient's response to standard dose has been evaluated, subsequent doses are | altered accordingly |
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. |
Therapeutic Index | LD50:ED50 |