Exam 1; Metabolism and Excretion

Question 1

In general, the action of the drug is terminated by what

Answer 1

its metabolism

Question 2

Which drugs are not terminated by its metabolism

Answer 2

prodrugs; they are inactive when given and are activated in the body

Question 3

What are four sites of drug metabolism

Answer 3

skin
lungs
kidney
small intestine

Question 4

What is the main organ (primary site) of drug metabolism

Answer 4

the liver

Question 5

This is when an oral drug gets absorbed by the small intestine and travels to the liver via the portal system

Answer 5

first pass metabolism

Question 6

If a drug is rapidly metabolized (nitroglycerin, morphine), it will not what

Answer 6

reach the circulation

Question 7

The smooth endoplasmic reticulum of the liver cells contains a complex of enzymes referred to as what

Answer 7

cytochrome P450 (CYP)

Question 8

What is the most significant form of CYP

Answer 8

CYP3A4; involved in more than 50% of the metabolism of drugs we talk about

Question 9

CYPs catalyze what type of reactions

Answer 9

oxidation reactions

Question 10

When CYP oxidizes a drug, what occurs?

Answer 10

the drug becomes more polar, which increases water solubility and makes it more readily excreted by the kidney

Question 11

CYPs can be both induced and inhibited by what

Answer 11

environmental factors

Question 12

What are some inhibitors of CYP

Answer 12

grapefruit juice
some antibacterials
some antifungals

Question 13

What are some activators of CYP

Answer 13

phenytan and phenoharbitol
St. Johns
rifampin

Question 14

What happens to the concentration of the drug upon inhibition or activation of CYP

Answer 14

inhibition of CYP = concentration of drug increases

activation of CYP = concentration of drug decreases

Question 15

CYP450 is responsible for what percentage of phase 1 reactions

Answer 15

75%

Question 16

Oxidation of the drug molecule forms what

Answer 16

a polar group like -OH or the removal of a non-polar group

Question 17

This is the addition of -OH to a molecule

Answer 17

hydroxylation

Question 18

What are four CYP450 phase 1 reactions besides hydroxylation

Answer 18

N-oxidation
S-oxidation
N-dealkylation
O-dealyklation

Question 19

What are four non-CYP450 phase 1 reactions

Answer 19

deamination
hydrolysis; esterases
peptidases
phosphatases

Question 20

What is the purpose of the phase II reactions

Answer 20

“finisher”

add a moiety to the drug (large molecule

Question 21

What five endogenous molecule groups can be added to a drug during phase II

Answer 21

acetyl group
glucuronic acid
methyl group
sulfate grouo
amino acid (like glycine)

Question 22

What is the primary organ of drug excretion

Answer 22

the kidney

Question 23

The more polar molecules will or will not be excreted via the kidney

Answer 23

will

Question 24

the more polar molecule will or will not stay in the urine and be excreted

Answer 24

will

Question 25

The more non-ionized molecule will or will not be resorbed from urine

Answer 25

will

Question 26

HA ⇆ H+ - A- | this means what

Answer 26

if you acidify the urine, this will allow the drug to stay in the body

Question 27

In what other ways can the drugs be excreted

Answer 27

feces lung sweat breast milk

Question 28

What are three factors that can alter absorption

Answer 28

time of day; before during or after meals age (older cannot metabolism as readily) environment (other drugs taken)

Question 29

What are three factors that can alter distribution of the drug in the body

Answer 29

body size and fat gender other drug interactions

Question 30

What are two enzymes that can be genetically different that can alter metabolism/excretion

Answer 30

CYP450 | plasma cholinesterases

Question 31

This enzyme is necessary for maintaining RBS integrity; deficiency can lead to RBC hemolysis

Answer 31

glucose-6-phosphate dehydrogenase

Question 32

This acetylator can slow metabolism

Answer 32

procainamide

Question 33

This acetylator can cause a lupus-like syndrome

Answer 33

hydralazine

Question 34

What four things can alter metabolism and excretion

Answer 34

age (infants and elderly) route of administration star of disease/pregnancy exposure to drugs (especially those affecting P450)

Question 35

What are the four phases of new drug testing

Answer 35

animal testing | phase 1-3

Question 36

This phase of new drug testing is dose dependent effect in normal and healthy humans

Answer 36

phase 1 (after animal testing)

Question 37

This phase of new drug testing is in a small number of patients with the target disease

Answer 37

phase 2

Question 38

This phase of new drug testing is in a large number of patients with the target disease

Answer 38

phase three

Question 39

How long and how much money does it cost for a drug to enter the market

Answer 39

8-9 years | 1 billion dollars

Question 40

This FDA category regarding pregnant women taking drugs is when there is no risk

Answer 40

A

Question 41

This FDA category regarding pregnant women taking drugs is when there is no risk in animals, but humans have not been tested

Answer 41

B

Question 42

This FDA category regarding pregnant women taking drugs is when risk cannot be ruled out (humans not tested) but the benefit is greater than the risk

Answer 42

C

Question 43

This FDA category regarding pregnant women taking drugs is when there is risk but also benefit; the risk = benefit treat the patient, may worry about the fetus

Answer 43

D

Question 44

This FDA category regarding pregnant women taking drugs is when there is a severe risk; drug is contraindicated; the risk is more than the benefit

Answer 44

X