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37 Cards in this Set

  • Front
  • Back
• Pharmacodynamics is the study of:
the biochemical and physiologic effects of drugs and the molecular mechanisms by which those effects are produced.
• For most drugs, the dose-response relationship is graded. This means:
the response gets more intense with increasing dosage.
• Maximal efficacy is defined as:
the biggest effect a drug can produce.
• Although efficacy is important, there are many situations in which a drug with relatively low efficacy is:
preferable to a drug with very high efficacy.
• A potent drug is simply a drug that:
produces its effects at low doses. As a rule, potency is not important
• Potency and efficacy are independent qualities.
Drug A can be more effective than drug B even though drug B may be more potent. Also, drugs A and B can be equally effective, although one may be more potent than the other.
• A receptor can be defined as:
any functional macromolecule in a cell to which a drug binds to produce its effects
• Binding of drugs to their receptors is:
almost always 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 action of 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.
Rather, drugs can only alter the rate of pre-existing processes
There are four primary families of receptors:
cell membrane-embedded enzymes, ligand-gated ion channels,
G protein-coupled receptor systems, and transcription factors
• Receptors make selective drug action possible, therefore:
If a drug interacts with only one type of receptor, and if that receptor type regulates just a few processes, then the effects of the drug will be relatively selective.
• If a drug interacts with only one type of receptor, but that receptor type regulates multiple processes, then:
the effects of the drug will be nonselective
If a drug interacts with multiple receptors
its effects will be nonselective.
Selectivity does not guarantee:
safety.
The term affinity refers to :
the strength of the attraction between a drug and its receptor
• Drugs with high affinity have:
high relative potency.
• The term intrinsic activity refers to:
the ability of a drug to activate receptors.
• Drugs with high intrinsic activity have:
high maximal efficacy.
• Agonists are:
molecules that activate receptors
• In terms of the modified occupancy theory, agonists have:
both affinity and high intrinsic activity. Affinity allows them to bind to receptors, whereas intrinsic activity allows them to activate the receptor after binding.
• Antagonists are drugs that:
prevent receptor activation by endogenous regulatory molecules and by other drugs.
• Antagonists can be subdivided into two major classes:
(1) noncompetitive antagonists and
(2) competitive antagonists.

Most antagonists are competitive.
• Noncompetitive antagonists bind:
irreversibly to receptors.
• Competitive antagonists bind:
reversibly to receptors.
• In terms of the modified occupancy theory, antagonists have:
affinity for receptors but no intrinsic activity. Affinity allows the antagonist to bind to receptors, but lack of intrinsic activity prevents the bound antagonist from causing receptor activation.
• Antagonists have no observable effects in the absence of:
agonists.
• Partial agonists have only moderate:
intrinsic activity.
Hence their maximal efficacy is lower than that of full agonists.
• Partial agonists can act as agonists if
there is no full agonist present
Partial agonists can act as antagonists if:
a full agonist is present.
• Continuous exposure of cells to agonists can result in:
receptor desensitization (aka refractoriness or down-regulation).
continuous exposure of cells to antagonists can result in:
hypersensitivity (aka supersensitivity).
• The ED50 is defined as:
the dose required to produce a defined therapeutic response in 50% of the population
• An average effective dose (ED50) is perfect for some people, insufficient for others, and excessive for still others.:
Because drug responses are not completely predictable, you must look at the patient (and not some drug reference book) to determine if dosage is appropriate.
• The therapeutic index—defined as the LD50:ED50 ratio—is:
a measure of a drug’s safety.
Drugs with a high therapeutic index are safe. Drugs with a low therapeutic index are not safe.
• Because of variability in responses, nurses, patients, and other concerned individuals must evaluate:
actual responses and be prepared to inform the prescriber about these responses so that proper adjustments in dosage can be made.