drug metabolism and elimination

Question 1

true or false. only drugs that are free and unbound from plasma protiens can be absorbed

Answer 1

true

Question 2

albumin binds to what

Answer 2

warfarin and aspirin

Question 3

albumin binding to aspirin is an example of what

Answer 3

a drug drug interaction

Question 4

blood flow, organ size affect what

Answer 4

distribution - more blood flow into the organ, the more medication, the bigger the organ , the more blood flow there is, thus more meducation

Question 5

blood brain barrier

Answer 5

possesses p-glycoprotiens which prevent some drugs from crossing biological membranes

Question 6

what do p-glycoprotiens do?

Answer 6

they adhere to drugs stopping them from crossing biological membranes

Question 7

fetal placental barrier

Answer 7

prevents drugs from affecting the fetus

Question 8

what mechanical barriers have p-glycoprotiens

Answer 8

BBB, fetal-placenta, liver, epithelial

Question 9

parenteral route distribution

Answer 9

bloodstream –> tissue

Question 10

oral administration distribution

Answer 10

liver - hepatic portal –> systemic circulation

Question 11

first pass effect

Answer 11

this means that always the forst part of a drug is going to be metabolized in the liver and is no longer available

Question 12

how is to bioavilablilty of a drug affected by the metabolism of the liver?

Answer 12

the bioavailability of the drug is reduced

Question 13

what routes of administration are affected by the first pass affect

Answer 13

oral and rectal

Question 14

what is metabolism

Answer 14

process by which drugs are biotransformed into water soluble compounds that are easily secreted by the kidneys

Question 15

the water-soluble metabolites from the liver are what?

Answer 15

inactive

Question 16

hepatic drug metabolism is crucial for what

Answer 16

terminating the drug action and facilitates the elimination of drug molecules from the body

Question 17

what converts lipid soluble drugs into water soluble metabolites

Answer 17

metabolism

Question 18

the kidneys can only excrete what substances

Answer 18

water soluble

Question 19

what are phase one reactions

Answer 19

theses reactions are hydrolysis, oxidation, reduction

Question 20

how do phase one reactions work?

Answer 20

they convert non-polar molecules into polar molcules via the addition of a polar funcitonal group

Question 21

most important phase one reaction

Answer 21

oxidation

Question 22

cytochrome p-450 enzymes do what

Answer 22

replace a -CH or -NH group in a molecule with an -OH

Question 23

what enzymes replace a -ch or -nh group in a molecule with an -oh group

Answer 23

cytochrome p450 enzymes

Question 24

cytochrome p448 enzymes

Answer 24

insert an oxygen atom between two carbons that are connected by a double bond

Question 25

what enzymes insert an oxygen atom between two carbons that are connected by a double bond

Answer 25

cytochrome p448

Question 26

what can activites can inhibit cytochrome enzymes

Answer 26

smoking and grapefruit juice

Question 27

what drugs can induce or inhibit the synthesis of oxidation enzymes - CYP - 450

Answer 27

rifampin and erythromyocin

Question 28

rifampin

Answer 28

increases the synthesis of CYP enzymes, effecting the metabolism of the medications

Question 29

what drug causes the increased metabolism and decreased plasma concentration of co-administered drugs

Answer 29

rifampin

Question 30

what drug can make things like birth control, antidepessants less effective?

Answer 30

rifampin

Question 31

erythromycin

Answer 31

inhibits the activity of CYP enzymes

Question 32

what inhibits the activity of the CYP enzymes

Answer 32

erytromycin

Question 33

aldehyde oxidase and liver alcohol dehydrogenase

Answer 33

can oxidize alcohol

Question 34

monoamine oxidase

Answer 34

metabolize things like dopamine and serotonin

Question 35

phase two reactions do what?

Answer 35

they form a highly water soluble metabolite

Question 36

what drug isnt rendered inactive after phase two conjugation

Answer 36

morphine

Question 37

glucuronyl transferase

Answer 37

replaces an -oh or -sh group with glucuronic acid

Question 38

n- acetyltrasnferase

Answer 38

replaces an -oh, -sh, -nh2 group with acetate

Question 39

sulfotrasnferase

Answer 39

adds a sulfate group replacing -oh

Question 40

glutathione s-transferase

Answer 40

forms an adduct between the drug and glutathione

Question 41

forming an adduct means

Answer 41

you are almost adding a molecule onto another

Question 42

where do the reactions occur in acetaminophen?

Answer 42

sulfation, oxidation, glucuronidation

Question 43

the oxidation of acetaminophen causes what

Answer 43

it causes the molecule to be unstable resulting in a spontaneous reaction

Question 44

what does the spontaneous reaction of acetaminophen result in

Answer 44

another phase two reaction of glutathione s-transferase

Question 45

in the situation of an acetaminophen overdose, what enzyme stops irreversible damage to the liver?

Answer 45

glutathione

Question 46

NAPQI combined with sulfahydryl causes what

Answer 46

causes cell death

Question 47

what is administered in acetaminophen overdose

Answer 47

acetylcysteine

Question 48

what is acetylcysteine

Answer 48

this is a compound that works just like glutathione, it binds to NAPQI and prevents damage to hepatocytes

Question 49

excretion is done by

Answer 49

kidneys

Question 50

in order for drugs to be excreted what must the drugs be

Answer 50

must be ionized and polar

Question 51

true or false, polarity of drugs can be manipulated by shifting pH of urine

Answer 51

true

Question 52

where do drugs that are more fat soluble excreted through

Answer 52

the intestines

Question 53

what drugs can experience intra-hepatic absorption

Answer 53

fat soluble