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Pharmacokinetics Bioavailability
bioavailability
19
Other
Graduate
11/05/2012

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Term
F
Definition
Is fraction of drug absorbed into the systemic system circulation
F≤1
Systemic absorption
Term
Ff
Definition
absorption through the gut lumen (intestine)
Term
Fg
Definition
absorption through gut wall (gut)
Term
Fh
Definition
absorption into the systemic circulation after first-pass hepatic metabolism
Term
Bioavailability
Definition
measure of how much drug given orally will be absorbed into the systemic circulation.
Term
What influences how much drug is absorbed systemically?
Definition
absorption through the gut lumen and wall, and first-pass hepatic metabolism
Term
Duodenum
Definition
primary site for drug absorption
increased surface area
pancreatic enzymes
primary site for pro-drug cleavage to activate drug
Term
microvilli
Definition
increase surface area by 600X
Term
pancreatic enzymes
Definition
degrade protein and carbohydrates
insulin
Term
examples of pro-drugs to active drugs
Definition
enalapril (vasotec) to enalaprilat
valacyclovir (valtrex) to acyclovir
Term
rectum
Definition
3 main vessels for systemic absorption
Term
two sites of absorption
Definition
duodenum
rectum
Term
mesalamine
Definition
recatlly: 10-35% absorption
orally: 20-30% absorption
Term
acetaminophen
Definition
rectally: variable
orally: rapid
Term
giving a drug by IV admin means ___ is in the systemic circulation
Definition
100%
Term
giving a drug by PO administration means that _______ will be absorbed into the systemic circulation.
Definition
0% to 100%
Term
IV dose ______________ than your PO dose to achieve the same systemic exposure
Definition
will never be greater
Term
approach 1
Definition
(%)(PO dose) = IV dose
Term
approach 2
Definition
1 mg PO = (% bioavail)mg IV
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