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60 Cards in this Set

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what is pharmacology
body of knowledge concerned with the action of chemicals on biologic systems
what is medical pharmacology
area of pharmacology concerned with the use of chemicals in the prevention, diagnosis, and treatment of disease especially in humans
what is toxicology
area of pharmacology concerned with the undesirable effects of chemicals on biologic systems
how do drugs vary
in size from MW 7 (lithium) to over MW 50,000 (thrombolytic enzymes).
what is MW 7
lithium
what is MW 50,000
thromolytic enzymes
the majority of drugs have molecular weights between what range
100-1000
how to drugs bind to receptors
chemical bonds
what are the different types of chemical bonds
covalent, electrostatic, hydrogen, van del Waals, hydrophobic bonds
what is a covalent bond
very strong bond
what is a electrostatic bond
weaker than covalent bond
what bond interactions are weak
hydrogen, van der Waals, and hydrophobic bonds
the specifc nature of the drug is of less practical importance than what
the fact that drugs that bind through weak bonds to their receptors are generally more selective than drugs that bind by means of very strong bonds (b/c weak bonds require a very precise fit of the drug to its receptor if an interaction is to occur)
weak bonds require what for an interaction to occur
a very precise fit of the drug to its receptor if an interaction is to occur
wwhat is permeation
movement of drug molecules into and within the biologic environment
what are the different types of permeation
aqueous diffusion, lipid diffusion, transport by carrier proteins, endocytosis,
what is aqueous diffusion
movement of molecules through the watery extracellular and intracellular spaces
what is lipid diffusion
Passive movement of molecules across lipid membranes
Fick's law governs what
aqueous and lipid diffusion
Fick's law does not govern what
transport by special carrier proteins
what is endocytosis
occurs through binding to receptors on cell membranes with subsequent internalization by infolding of that area of membrane
what is Fick's law of diffusion
Predicts the rate of movement of molecules across a barrier
what is the formula for Fick's law
concentration gradient (C1 – C2), and permeability coefficient for the drug and the area and thickness of the barrier are used to compute the rate, as follows:
Rate = (C1 –C2) X Perm coef/Thickness X Area
what does Fick's law quantify
observation that drug absorption is faster from organs with a large surface area and from organs with a thin membrane barrier
Log is equal to what in the Henderson Hasselbach equations
pKa-pH
is log protonated or unporotonated
either
weak bases are ionized when
when they are protonated
weak acids are not ionized when
when they are protonated
when acids are protonated what happens
they are not ionized
when bases are protonated what happens
they are ionized
what determines the ratio of the protonated to unprotonated form
pH of the medium
the pH of the medium determines what
the ratio of the protonated to unprotonated form
what are the routes of drug administration
oral, IV, sub Q, buccal and sublingual, rectal, inhalation, topical, transdermal,
what are the characteristics of oral administration
offers convenience, but absorption may be slower and less complete than when parenteral routes are used. Ingested drugs are subject to the first pass effect.
what are the characteristics of IV administration
instantaneous and complete absorption. Potentially more dangerous
what are the characteristics of sub Q administration
slower absorption than intramuscular route. Avoids first pass metabolism
what are the characteristics of buccal and sublingual administration
permits direct absorption into the systemic venous circulation. Avoids first-pass effect
what are the characteristics of rectal administration
partial avoidance of first pass effect.
what are the characteristics of inhalation administration
Results in rapid absorption. Particularly convenient for drugs that are gases at room temperature
what are the characteristics of topical administration
application to skin or mucous membrane for local effect
what are the characteristics of transdermal administration
application to the skin for systemic effect
in regards to absorption what will high blood flow do
maintains a high drug depot-to-blood concentration gradient and thus maximizes absorption
in regards to absorption what will concentration changes do
higher the concentration of the drug at the site of administration, the faster the absorption
what are the determinants of distribution
size of organ, blood flow, solubility, binding, metabolism, elimination
in regards to determinant of distribution what will the size of the organ do
large organs such as skeletal muscle can take up a large amount of drug because the concentration in the muscle tissue remains low even after large amounts of drug have been transferred
in regards to determinant of distribution what will blood flow do
determine rate of uptake. Well perfused tissues will achieve high tissue concentrations rapidly
in regards to determinant of distribution what will solubility do
Lipid soluble drugs will distribute rapidly into organs with a high lipid content such as the brain
in regards to determinant of distribution what will binding do
binding of a drug to a macro-molecule in a compartment will tend to increase the drug’s concentration in that compartment
in regards to determinant of distribution what will metabolism do
terminate action of many drugs before they are excreted by actively metabolizing them to biologically inactive derivatives
what is inactive as it is administered and must be metabolized in the body to become active
prodrug
true or false: Some drugs are not modified by the body; they continue to act until excreted
true
true or false: elimination is the same as excretion
false
how do elimination and excretion differ
A drug may be eliminated by metabolism long before the modified molecules are excreted from the body
what is the first order of elimination
the rate of elimination is proportionate to the concentration of the drug. The half-life of elimination is constant regardless of the amount of drug in the body
what is zero elimination
the rate of elimination is constant regardless of the concentration of the drug
what can zero elimnation occur with
ethanol, aspirin, and phenytoin at high doses
what are the various drug preparations
solutions and suspensions (syrups, elixirs, parental)
what is the syrup preparation
sweetened aqueous solution
what is the elixir preparation
sweetened alcoholic solution
what is the parental preparation
sterile (IV)