T2

Question 1

pharmacokinetics

Answer 1

what the body does to the drug

Question 2

pharmacokinetic parameters

Answer 2

absorption
distribution
metabolism
elimination

Question 3

molecular weight

Answer 3

MW between 100-1000 readily diffuse
MW >1000 do not and may require facilitated diffusion or active transport

Question 4

lipid solubility

Answer 4

lipid soluble drugs (lipophilic) pass through cell membranes more easily than water soluble drugs (hydrophilic)
hydrophilic drugs typically require transporter proteins or channels for facilitated transport

Question 5

protein binding

Answer 5

when a drug is bound to proteins, a large complex forms that is unable to cross cell membranes, only unbound (free) drug molecules can cross

Question 6

drugs that exhibit low protein binding are generally

Answer 6

more easily transported than highly protein bound drugs

Question 7

drugs with reversible protein binding

Answer 7

weaker bonds form drug-protein complex
inactive and unable to cross cell membranes when bound
bonds are not permanent, and drug can be released as free-drugs

Question 8

drugs with irreversible protein binding

Answer 8

strong bonds form drug-protein complex
permanently inactive and unlikely to be transported once bound

Question 9

more non-ionized drug in solution will cause

Answer 9

drug absoprtion

Question 10

more ionized drug in solution will cause

Answer 10

drug accumulation

Question 11

non-ionized

Answer 11

lipid soluble, able to cross membrane barriers easily

Question 12

ionized

Answer 12

water soluble, poorly crosses membrane barrier

Question 13

dissociation constant (pKa)

Answer 13

defined as the pH at which the ionized and non-ionized forms are equal, classifies a drug as a weak acid or weak base

Question 14

pH of the environment determines

Answer 14

amount of drug that will be ionized or non-ionized

Question 15

when pKa of the drug = pH of the environment

Answer 15

there are equal amounts of ionized and non-ionized drugs in solution

Question 16

weak acids and weak bases have better absorption

Answer 16

weak acids better in acidic solution
weak bases better in alkaline solution

Question 17

weak acids and weak bases have better elimination

Answer 17

weak acids have better elimination in alkaline solution
weak bases have better elimination in acidic solution

Question 18

weak acid pH of solution < pKa of the drug

Answer 18

drug is more likely to be absorbed

Question 19

weak acid pH of solution > pKa of the drug

Answer 19

drug more likely to accumulate

Question 20

weak base pH of solution < pKa of the drug

Answer 20

drug is more likely to accumulate

Question 21

weak base pH of solution > pKa of the drug

Answer 21

drug is more likely to be absorbed

Question 22

paracellular transport

Answer 22

passage of solutes and fluids through the intracellular space between adjacent cells
occurs in epithelial and endothelial tissues
tight junctions: specialized protein complexes that seal intercellular space
allow for selective permeability (CNS-blood brain barrier)

Question 23

passive diffusion

Answer 23

major absorption process for small, lipid-soluble, nonionized medications

Question 24

facilitated diffusion via solute carrier (SLC) transporter

Answer 24

used for large, water-soluble, or polar medications
saturable process

Question 25

active transport key characteristics

Answer 25

energy requirement saturability selectivity competitive inhibition

Question 26

primary active transport couples with

Answer 26

ATP hydrolysis

Question 27

ATP binding cassette (ABC) transporters

Answer 27

rely on ATP hydrolysis to actively pump substrate across membranes against the concentration gradient

Question 28

sodium/potassium-ATPase

Answer 28

rely on ATP hydrolysis for ion exchange

Question 29

secondary active transport

Answer 29

transport of one solute is energetically driven by the transport of another solute symporters and antiporters

Question 30

symporters

Answer 30

ions move in the same direction sodium/glucose transporter

Question 31

antiporters

Answer 31

ions move in opposite directions sodium/calciu exchanger

Question 32

routes of administration

Answer 32

oral, IM, IV, inhalation, intranasal, subcutaneous, rectal, transdermal, sublingual

Question 33

route of administration bypassing absorption

Answer 33

intravenous

Question 34

factors impacting absorption

Answer 34

surface area of tissue blood flow to the site of absorption pH of the environment physical state of the drug drug concentration at the site of absorption

Question 35

surface area

Answer 35

greater surface area at the site of administration allows for increased absorption

Question 36

optimum site of oral drug absorption

Answer 36

duodenum due to immense surface area

Question 37

blood supply in terms of transport and distribution

Answer 37

greater blood supply allows for quicker transport of drug from the site of administration into the bloodstream greater blood supply = faster and easier distribution

Question 38

factors impacting rate and extent of distribution

Answer 38

size (MW) and polarity (degree of ionization) of the medication blood supply to tissues degree of protein binding drug volume of distribution

Question 39

organs in order of greatest to least amount of blood flow

Answer 39

liver - 1500 mL/min kidneys - 1100 mL/min muscle - 900 mL/min brain - 800 mL/min heart - 250 mL/min adipose - 250 mL/min

Question 40

protein binding in plasma and tissues

Answer 40

typically reversible but may be irreversible

Question 41

high plasma protein binding =

Answer 41

lower concentration of drug in tissues/site of action only unbound drugs can readily diffuse longer time for elimination may limit drug transport metabolism reduced

Question 42

high tissue protein binding =

Answer 42

accumulation and that tissue can act as a reservoir most common in bone and fat due to limited blood supply may limit elimination

Question 43

volume of distribution

Answer 43

measure of apparent space in the body available to contain drug

Question 44

small Vd

Answer 44

<3L, drug remains mostly in the plasma

Question 45

moderate Vd

Answer 45

> 16L, drug distributes to plasma and interstitial fluids

Question 46

large Vd

Answer 46

> 46L, drug distributes to all body compartments

Question 47

metabolites

Answer 47

usually polar and water-soluble which are more readily eliminated

Question 48

active drug

Answer 48

drug that is active on administration breaks down into inactive or less active metabolites via metabolism

Question 49

prodrug

Answer 49

drug that is inactive on administration but is converted to an active compound via metabolism

Question 50

sites of metabolism

Answer 50

liver: cytochrome P450 enzymes intestines lungs kidneys

Question 51

first pass effect

Answer 51

portal vein delivers blood from the GI tract to the liver before it circulates to the rest of the body once in the liver, metabolism occurs

Question 52

drugs with extensive first-pass effect have

Answer 52

smaller amounts of drug reaching systemic circulation and therefore less drug will reach its target

Question 53

routes of administration that bypass first pass effect

Answer 53

IV IM transdermal sublingual inhalation

Question 54

metabolic reactions phase I

Answer 54

cytochrome P450 enzymes catalyze reaction oxidation, hydrolysis, reduction

Question 55

metabolic reaction phase II

Answer 55

conjugation of medication of metabolite with another compound methyl acetyl sulfa glutathione glucuronic acid

Question 56

routes of excretion

Answer 56

renal (urine) liver (bile) GI tract (feces) lungs (exhalation)