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26 Cards in this Set

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What is the chemical name of a drug mean?
Name the medicinal chemist uses to refer to it.
What is the code name?
Chosen by manufacturer during drug development usually are unaware of the drug name?
What is the proprietary name?
Also chosen by the manufacturer for marketing purposes..also referred to as brand or trade name
Official name
assigned by the US Adopted Name Council
Generic name
Offical, nonproprietary name
used after patent loss
What are some of the physiochemical properties of drug molecules?
Small MW..stability in vitro and in vivo
solubillity in H2O and oil
3-D structure
ionizable groups
What is Lipophilicity?
Solubility in lipid relative to water
Measured by oil/water partition coefficient
* ability a drug has to diffuse into cell
What is Pharmacodynamics?
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.
What is Pharmacokinetics?
The time course of:
absorption
distribution
elimination
Factors that modify pharmacokinetic phenomenon
What are the objectives of PK analysis?
predict time course of drug effect
predict concentration at site of action
characterize absorption, distribution, elimination kinetics
dose/species dependence
What are the four types of biotransport?
passive diffusion
filtration
carrier-mediated transport
receptor-mediated endocytosis
Explain passive diffusion
Passage through lipid cell membrane by dissolution in membrane
*rate dependent of concentration gradient
*obeys first-order kinetics
Explain filtration
Transport of substance in bulk flow of aqueous fluid
*Rate dependent on:
-hydrostatic pressure
-mw, size, charge, and binding to
excluded macromolecules
-tissue porosity
Explain carrier-mediated transport
involves saturable kinetics, substrate competition, and tissue differences in expression of carriers
What are two types of drug transporters
Multidrug resistance p-glycoproteins
Mulidrug restistance associated proteins
What is the MDR p-Gylcoprotein?
PM protein that can pum drugs inside the cell out...
Why cancerous cells stop responding to chemotherapy.
Drug transporters are usually located?
Intestinal mucosa
hepatocyte
proximal renal tube
brain: choroid plexus, vascular endothelium
What is receptor mediated endocytosis?
Internalization into PM
Important in selective tissue uptake
Rate dependent of receptor expression and membrane insertion
Saturable kinetics
What is absorption kinetics?
Time between absorption and distribution
Characterization by:
half-life
percent dose absorbed (bioavailabililty)
Describe route of administration intravenously
100% bioavilability---all of dose in plasma compartment
rate dependent on technique
importance of sterility
Describe route of administration subcutaneously
-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
Describe route of administration inhalation
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
describe route of topical administration
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
What is enteral administration?
pertains to administratin of drugs into any part of the gastrointenstinal tract..oral, sublingual, rectal
Describe the route of oral administration
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...
Two important factors of absorption are:
half-life
bioavailability