Term
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Definition
| genome-wide comparisions of individuals to determine how one affects pharmacological function and therapeutic response |
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Term
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Definition
| variation in DNA sequence and the effect on pharmacokinetics or pharmacodynamics - for specific determination of individual drug effects |
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Definition
| use of drugs in the treatment of disease |
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Term
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Definition
| novel use of antibodies, target delivery, gene therapy |
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Term
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Definition
| study of drug safety - adverse drug reactions and other effects of drugs on people (ADRs are the 5th leading cause of death of people in the states |
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Definition
| study of adverse effects of drugs and toxins |
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Term
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Definition
| any substance that is a food or part of alleging to provide health benefits |
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Definition
| non-nutrient chemical that has function in the body |
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Term
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Definition
| through a membrane of the body (buccal, sublingual, rectal, oral) |
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Term
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Definition
| intravascular, intramuscular, subcutaneous |
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Term
| 4 steps of pharmacokinetics |
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Definition
ADME
absorption
distribution
metabolism
excretion |
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Term
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Definition
most passive diffusion
some facilitated diffusion
active transport
endocytosis - large proteins |
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Term
| oil/water partition coefficient |
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Definition
| amount of drug in the oil versus water. the higher the number the greater membrane permeability and the higher intake through the stomach |
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Term
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Definition
| high pH protonates the acid and de-ionizes it |
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Term
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Definition
| higher the pH the base is protonated and the base is ionized |
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Term
| effect of pH (H-H formula) |
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Definition
| log ([HA]/[A-]) = pKa - pH |
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Term
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Definition
| major location of absorption due to surface area and pH (bases) |
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Term
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Definition
| amount of absorbed drug that is metabolized in the liver - most for oral due to gut wall and liver |
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Term
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Definition
| fraction of administered drug that meets the systemic circulation as a percent of what was injected |
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Term
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Definition
| leaving of the blood to the tissues; flow, protein binding, permeability and size are factors |
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Term
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Definition
| albumin, determines freedom of drugs in serum, the most tightly bound drug will out compete and will drive the free concentration of the drug higher in the blood |
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Term
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Definition
plasma only (4 L)
extracellular fluid (14 L)
intracellular fluid (42 L)
VERY Hydrophobic (volume depends on how much effective volume there is compared to amount left in blood) |
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Term
| distribution determination |
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Definition
is it eliminated? or metabolized?
if neither then there is an equilibration period (distribution phase) |
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Term
| distribution w/ elimination |
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Definition
| log scale the concentration axis and take x intercept to determine the hypothetical distribution concentration (with elimination there is a constant logarithmic excretion to account for) - allows determination of the distribution volume |
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Term
| biotransformation kinetics |
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Definition
v=vmax*[C]/Km when there is low concentration
v= vmax when there is a high concentration
major purpose is to allow for excretion |
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Term
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Definition
| substance occuring naturally in the body |
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Term
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Definition
phase 1 - small functional group changes (still active)
phase 2 - large conjucation products (inactive) |
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Term
| biotransformation phase 1 reactions |
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Definition
| oxidative, hydrolytic, reductive |
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Term
| biotransformation phase II reactions |
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Definition
| glucuronidation; sulfation; acetylation; methylation; conjugation with GSH and AAs |
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Term
| give one example of a phase II biotransformation enzyme and cofactor |
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Definition
| UDP-glucuronosyltransferase (UDP-GT); UDP-glucoronic acid |
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Term
| individual genetic variations |
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Definition
| inherited variation and polymorphisms |
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Term
| name two drugs that have genetically affect actions |
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Definition
| succinylcholine, NAT2 effect on isoniazid metabolism |
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Term
| race changes in metabolism/action |
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Definition
| BiDil is more active in heart failure for African Americans than other races |
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Term
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Definition
| smoking induces P450, grapefruit juice inhibits P450 |
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Term
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Definition
| glumerular filtration + active tubular secretion - pass-reabsorption = excretion; pH can determine this process both in the lumen and the blood |
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Term
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Definition
| can be enterohepatically recycled; not as common as renal |
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Term
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Definition
| pumps foreign substances out of cells in the GI epithelium using 2 ATPs, an inherent protective mechanism |
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Term
| drug effects on p-glycoprotein pump |
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Definition
induction - heightens activity of pump (St. John's Wart)
inhibition (quinidine) |
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Term
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Definition
| when displaced with a competitor (sulfonamides)bilirubin is removed and can promote toxicity |
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Term
| what is the proper nomenclature for cytochromes? |
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Definition
| CYP + Arabic Number + Letter + Arabic Number |
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Term
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Definition
| xenobiotic transformation, synthesis of sterols and vitamins |
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Term
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Definition
UM - ultra-fast metabolizer
EM - extensive
IM - intermediate
PM - poor
when inhibited type is changed to a lower level |
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Term
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Definition
| largest subfamily, expressed in Liver and intestine |
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Term
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Definition
women not tested well
after two weeks the enzymes are active and progress into adolescence - decline into old age |
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Term
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Definition
zoles, grapefruite juice and other inhibitors prevent metabolism of this drug; causes myolysis - requires choice of best type of this class
lower amount of treatment till the drug that interacts with it is not used anymore |
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Term
| non-depolarizing agents - neuromuscular |
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Definition
| competitive antagonist: -curium, -curonium, Tubocurarine |
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