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24 Cards in this Set
- Front
- Back
link between phrmacokinetics and pharmacodynamics?
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concentration: pharmacokinetics = dose-concentration and pharmacodynamics = concentration-effect
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definition of drug absorption?
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passage of drug from site of administration into circulation
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>80% of prescribed drugs are what class?
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enteral
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what drug characteristics are important to drugs administered orally?
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surface area, pH, particle size
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what drug characteristics are important to drugs administered sublingually?
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lipid solubility and pH
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what is main disadvantage of orally administered drugs?
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first pass effect may be significant
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advantages of IV administration?
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direct, easy to control dose for drugs with narrow margin of safety (small therapeutic range), reach desired blood level, for drugs which cannot be tolerated by other routes
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possible adverse effects of IV administration?
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anaphylactic reactions, embolism, hemolysis or agglutination of blood, infection
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what form of drug administration follows first order kinetics?
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intramuscular
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what is intramuscular drug administration limited by?
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blood flow, ionization, lipid solubility, molecular size
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what are limitations to subcutaneous drug administration?
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absorption may be retarded by cooling, vasoconstriction
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where is intrathecal injected to?
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subarachnoid space
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what limits pulmonary drug administration?
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particle sizes >2 microm is probably not absorbed
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requirements and advantages of topical application of drug?
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highly lipid soluble substances can be absorbed slowly through the skin
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how is lipid solubility determined?
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by lipid (oil)/water partition coefficient
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what does a higher oil/water partition coefficient indicate?
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hydrophobic and will more easily pass through biological membranes
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what does the degree of ionization depend on and what is the consequence?
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depend on pKa of drug and pH of the environment --> only nonionized particles can pass through membranes
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how can drugs move across cell membranes?
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passive diffusion, facilitated diffusion, active transport, endocytosis, exocytosis
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fick's law of diffusion defines flux as a function of what for passive diffusion?
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concentration gradietn, area, permeability coefficient, and thickness
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what does the pH partition hypothesis suggest?
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ion trapping mechanism due to differing pHs of body causing drug to exist in either nonionized or ionized form, which dictate if the drug will be able to cross the biological membranes
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for drugs with similar pKa, what can influence the amount of drug absorbed?
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increased lipid solubility results in greater absorption
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consequences of first pass effect?
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significantly decreased bioavailability of orally administered drugs and large individual variation in plasma concentration
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how does oral administration differ from sublingual/buccal and rectal administration of drug?
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blood from the intestinal mucosa drains into the liver via the hepatic portal system, whereas the blood from the mouth and rectum drains into the systemic circulation
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which drugs have poor availability when given orally due to first pass effect?
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acetylsalicyclic acid, chlorpromazine, desipramine, isoproterenol, propranolol, lidocaine, meperidine, methylphenidate, morphine, salicylamide, nitroglycerin, nortriptyline, pentazocine, propoxyphen
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