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36 Cards in this Set
- Front
- Back
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Affinity |
ability of the agonist molecule to bind to receptors |
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Efficacy |
Abiltiy of an agonist molecule to cause a response |
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Competitive antagonism |
Antagonist and agonist compete; antagonist keeps agonist from binding to cell receptors, but there are usually some receptor sites left on a cell for the agonist to bind to NOT PERMANENT: the antagonist will eventually leave the cell and the agonist will bind; reversible |
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Noncompetitive Antagonism |
Rare; tight; long-lasting (permanent) blockade produced by antagonsit cannot be overcome. Few clinical agents are noncompetitive (e.g., nerve gas) antagonist may bind to receptor next to the agonst receptor and change the shape of the agonsit receptor so that the cell doesn't recognize the agonist. |
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Biochemical antagonism |
the process by which one drug decreases the amount of another drug that is available w/in the body to produce an effect. May be d/t ability of drug to decrease absorption, increase excretion, or alter metabolsim of other drug. e.g., antacids |
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Chemical antagonism |
inhibtition/total loss of a dru'gs action as a result of its chemical interaction w/another substance. e.g., drugs affected by food: tetracyclin & Ca++, NTG comes w/its own tubing b/c it binds w/other IV tubing |
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Physiologic antagonism |
2 agonists act w/diff receptors and their effects cancel each other e.g., Epi (incr. HR) + Ach (decr. HR) |
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Direct physical or chemical |
Not on a cell antacids chemically neutralize stomach acid; osmotic diuretics have physical action of increasing osmotic pressure |
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Action on or near a cell |
Action is on or in cells but no receptor e.g., general anesthetics alter electric properties of nerve cells CA drugs alter metabolism of chemicals essential for cell function Penicillin alters cell metabolism of bacterial cells |
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selective toxicity |
ideal drug acts only on the system which you want to effect e.g., Penicillin acts only on bacterial cells. Thus, low toxicity. CA drugs act on enzyme processes that occur in all cells --> high toxicity |
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drug potency |
relative amts needed to cause an effect way to compare drugs of same class |
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drug efficacy |
maximum response drug can get |
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pharmacogenomics |
differences in sensitivity and resistance the study of role of inherited and acquired genetic variation in drug response |
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Factors that alter drug response: |
1. Gender 2. Genetics 3. Pathophysiology 4. Diet 5. Circadian Rhythms 6. Drug hx 7. Psychosocial 8. Drug administration 9. Body build 10. Age |
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allergy |
an immune response involving antigen-antibody rxn. Usually requires previous exposure; such is not always obvious; could be environmental to related chemical. |
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idiosyncratic reaction |
highly unusual and unpredictable; genetically determined |
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cumulative effects |
increasing response to repeated doses of a drug that occurs when the rate of administration exceeds the rate of metabolism or excretion. As blood level rises, toxicity may occur. |
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toxicity |
poisoning; may be reversible or not |
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tolerance |
an increased dose of a drug is needed to cause a response equal to the response produced by a lower dose before tolerance developed |
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tachyphylaxis |
tolerance after only one/two doses |
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tissue damage |
local or systemic; gastric irritation from ASA. ototoxicity |
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carcinogenesis |
from tobacco, asbestos |
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teratogenesis |
production of physical defects in the fetus |
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mutagenesis |
production of chromosomal abnormalities that manifest in offspring |
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drug fever |
a febrile response that coincides temporally with the admin of a drug and disappears after discontinuation of the offending agent |
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Pregnancy Category A |
no risk to fetus |
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Pregnancy Category B |
Probably no risk to fetus -animal studies indicate no risk to fetus and no adequate or well-controlled studies in pregnant women OR -animal studies show adverse effect, but adequate & well-controlled studies in pregnant women demonstrate no risks |
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Pregnancy Category C |
Risk in animals -animal studies report adverse effects on the fetus and there are no adequate and well-controlled studies in humans OR -no animal studies have been done and there are no adequate and well-controlled studies in pregnant women |
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Pregnancy Category D |
Risk in humans but the potential benefit may warrant the use of these drugs in pregnant women, if safer drugs are not available or ineffective e.g.,epileptic drugs for the mom harm fetus but seizures also harm the fetus |
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Pregnancy Category X |
NEVER GIVE TO PREGNANT WOMEN -fetal abnormalities reported and positive evidence of fetal risk in humans is available form animal and/or human studies. The risks involved clearly outweigh the potential benefits. |
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Addition effects |
when 2 drugs w/the same mechanism of action are taken and the result is equal to the effects of either drug given alone in higher doses. (1+1=2) e.g., tylenol 325 + codeine 30 = Cod 60 or tylenol 650 |
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Synergistic effects |
2 drugs have a greater combined effect than the sum of the separate action of each single drug (1+1=3) e.g., ETOH & CNS depressants |
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antagonistic effects |
combination of drugs create less of an effect than that produced when either drug is given alone (2+2=1) e.g., levodopa and B6 |
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Alterations in absorption |
one drug can change rate or extent of absorption of the other; if extent is changed- don't give together |
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alterations in distribution |
changes in protein binding e.g., coumadin and ASA |
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alterations in metabolism and excretion |
barbiturates stimulate hepatic enzymes --> increase metabolism and excretion of other drugs --> decrease therapeutic effects. -If excretion alone is changed it can lead to toxicity. (drug accumulation) |
