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pharm chapter 5
| Question | Answer |
|---|---|
| define pharmodynamics? | -its the study of what drugs do to the body and how they do it. |
| explain the dose-response relationship and its phases | 1: occurs at low doses, the curve is flat since the doses are too low to elicit a measurable response 2: increase in dose causes increase in response, its a graded response 3: an increase in doesn't cause an increase in response |
| define potency | -it is the amount of drug that is given to elicit an effect -potency of a drug implies nothing about its maximal efficacy -high potency; produces higher effects not necessarily need lower doses to achieve it |
| t/f binding of drug to its receptor is irreversible | F |
| what are the four primary receptor families | 1) cell membrane-embedded enzymes 2) ligand-gated ion channels, 3) G-protein-coupled receptors 4) transcription factors |
| define cell membrabe-embedded enzyme receptors | -they span the cell membrane -ligand binding domain located on cell surface -enzyme catalytic site is inside -response to actuvation of these receptors happens in secs Isulin ex of endodogenous ligands that works through this receptor |
| what is the main function of ligand-gated ion channels and where are they located | -control flow of ions into/out of cells, -each ligand gate is specific to ion -span the cell membrane -binding of endogenous ligand to receptor causes flow of ion into or out of cell -activation/response fast -nt like acetycholine and GABA use this |
| what are the three parts of the G protein-coupled receptor | -the receptor -G protein (binds GTP) -an effector (an ion channel or an enzyme) |
| what is the main difference between transcription factors and other receptors? | 1) TF are found w/in the cells instead of the surface 2) respose to activation of these receptors are delayed -TF found on DNA in cell nucleus & they regulate protein synthesis -the whole process may take hrs-days |
| T/F TF are activated by only lipid soluble ligands | T -since TF are intracellular, they are only activated by lipid ligands that are able to cross the cell membrane |
| why is it that drugs interact with certain receptors and not all? | because of the lock and key analogy -it must have the shape complementary to the receptor, it also needs to have the correct charges postions at the correct site to interact with the receptor |
| what are the two theories for drug receptor interaction? | 1) the simple occupancy theory 2) the modified occupancy theory -they explain dose-response relationships and ability of drugs to mimic or block actions of endogenous regulatory molecules |
| what are the two ideas that the simple occupancy theory state?SOT | 1) the intensity of the response to a drug is proportional to the # of receptors occupied by that drug 2) maximal response will occur when all available receptors have been occupied |
| 9what are the assumptions that SOT make | assumes all drugs acting at a particular receptor are identical with respect to the ability to bind to the receptor & the ability to influence receptor function once binding has taken place. The modified occupancy theory is diff |
| what is the modified occupancy theory | looks at 1) affinity-> strength of attraction bet drug and receptor reflected in potency, need little to bind or need a lot of drug to bind 2) intrinsic->ability of drug to activate receptor after binding reflected in maximal efficacy-> |
| Drugs that mimic body's own regulatory molecules are called ____________ | Agonist--> have high intrinsic activity and affinity |
| Drugs that block actions of endogenous regulators are __________________-- | antagonists--> have no effect of their own on receptor function, they do prevent activation of receptors by agonists |
| Drugs that mimic actions of endogenous regulatory molecules but produce an intermediate intensity response _____________ | partial agonist--> the maximal effect that it produces is lower than a full agonist since it only has moderate intrinsic activity -can act as an agonist and antagonist ie: pentszocine |
| T/F response to an antagonist is determined by how much agonist is present | T if there is no agonist present, administration of an antagnoist will have no observable effect and vice versa |
| what are the two classes for antagonists | 1) competitive(most are this) and 2) noncompetitive 1) bind reversibly -2) bind irreversibly to receptors and they reduce the maximal response since there will be a decrease in receptors available for agonist |
| define effective dose (ED) | the dose that is required to produce a defined therapeutic response in 50% of the population. |
| what is the therapeutic index? | measure of the drugs safety ratio of drugs lethal dose (LD) to its effective dose |
Created by:
Jaspritk
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