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26 Cards in this Set
- Front
- Back
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What is the chemical name of a drug mean?
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Name the medicinal chemist uses to refer to it.
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What is the code name?
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Chosen by manufacturer during drug development usually are unaware of the drug name?
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What is the proprietary name?
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Also chosen by the manufacturer for marketing purposes..also referred to as brand or trade name
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Official name
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assigned by the US Adopted Name Council
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Generic name
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Offical, nonproprietary name
used after patent loss |
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What are some of the physiochemical properties of drug molecules?
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Small MW..stability in vitro and in vivo
solubillity in H2O and oil 3-D structure ionizable groups |
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What is Lipophilicity?
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Solubility in lipid relative to water
Measured by oil/water partition coefficient * ability a drug has to diffuse into cell |
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What is Pharmacodynamics?
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Study of biologic effects produced by chemicals, the site at which and mechanism by which the biologic effects are produced ; the fate of a chemical agent in the body: its absorption, distribution, elimination, and the factors which influence the safety and effectiveness of an agent.
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What is Pharmacokinetics?
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The time course of:
absorption distribution elimination Factors that modify pharmacokinetic phenomenon |
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What are the objectives of PK analysis?
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predict time course of drug effect
predict concentration at site of action characterize absorption, distribution, elimination kinetics dose/species dependence |
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What are the four types of biotransport?
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passive diffusion
filtration carrier-mediated transport receptor-mediated endocytosis |
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Explain passive diffusion
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Passage through lipid cell membrane by dissolution in membrane
*rate dependent of concentration gradient *obeys first-order kinetics |
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Explain filtration
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Transport of substance in bulk flow of aqueous fluid
*Rate dependent on: -hydrostatic pressure -mw, size, charge, and binding to excluded macromolecules -tissue porosity |
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Explain carrier-mediated transport
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involves saturable kinetics, substrate competition, and tissue differences in expression of carriers
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What are two types of drug transporters
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Multidrug resistance p-glycoproteins
Mulidrug restistance associated proteins |
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What is the MDR p-Gylcoprotein?
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PM protein that can pum drugs inside the cell out...
Why cancerous cells stop responding to chemotherapy. |
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Drug transporters are usually located?
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Intestinal mucosa
hepatocyte proximal renal tube brain: choroid plexus, vascular endothelium |
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What is receptor mediated endocytosis?
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Internalization into PM
Important in selective tissue uptake Rate dependent of receptor expression and membrane insertion Saturable kinetics |
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What is absorption kinetics?
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Time between absorption and distribution
Characterization by: half-life percent dose absorbed (bioavailabililty) |
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Describe route of administration intravenously
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100% bioavilability---all of dose in plasma compartment
rate dependent on technique importance of sterility |
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Describe route of administration subcutaneously
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-Uptake of high mw cmps into lymphatics
absorption is slow -blood flow is rate-limiting factor for some drugs -improved bioavailability over oral route for some drugs |
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Describe route of administration inhalation
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rapid absorption of gases and vapors due to:
-high pulmonary blood flow -low diffusional distance from avelous to blood -route for localized delievery of drugs with actions in pulmonary tissue |
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describe route of topical administration
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absorption through skin slow due to surface layers of dead, keratinized cells
-drugs with sufficeint lipophilicity and potency may have systemic clinical efficacy upon topical application in transdermal patch |
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What is enteral administration?
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pertains to administratin of drugs into any part of the gastrointenstinal tract..oral, sublingual, rectal
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Describe the route of oral administration
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Bioavailiability may be low due to: mucosa as barrier
or first pass effect: absorbed drug passes via portal circulation through liver which may clear substantial fraction and thus decresase bioavailability... |
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Two important factors of absorption are:
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half-life
bioavailability |
