Exam 1; Metabolism and Excretion Flashcards Preview

AU14 Pharmacology > Exam 1; Metabolism and Excretion > Flashcards

Flashcards in Exam 1; Metabolism and Excretion Deck (44):
1

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

its metabolism

2

Which drugs are not terminated by its metabolism

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

3

What are four sites of drug metabolism

skin
lungs
kidney
small intestine

4

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

the liver

5

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

first pass metabolism

6

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

reach the circulation

7

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

cytochrome P450 (CYP)

8

What is the most significant form of CYP

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

9

CYPs catalyze what type of reactions

oxidation reactions

10

When CYP oxidizes a drug, what occurs?

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

11

CYPs can be both induced and inhibited by what

environmental factors

12

What are some inhibitors of CYP

grapefruit juice
some antibacterials
some antifungals

13

What are some activators of CYP

phenytan and phenoharbitol
St. Johns
rifampin

14

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

inhibition of CYP = concentration of drug increases
activation of CYP = concentration of drug decreases

15

CYP450 is responsible for what percentage of phase 1 reactions

75%

16

Oxidation of the drug molecule forms what

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

17

This is the addition of -OH to a molecule

hydroxylation

18

What are four CYP450 phase 1 reactions besides hydroxylation

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

19

What are four non-CYP450 phase 1 reactions

deamination
hydrolysis; esterases
peptidases
phosphatases

20

What is the purpose of the phase II reactions

"finisher"
add a moiety to the drug (large molecule

21

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

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

22

What is the primary organ of drug excretion

the kidney

23

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

will

24

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

will

25

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

will

26

HA ⇆ H+ - A-
this means what

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

27

In what other ways can the drugs be excreted

feces
lung
sweat
breast milk

28

What are three factors that can alter absorption

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

29

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

body size and fat
gender
other drug interactions

30

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

CYP450
plasma cholinesterases

31

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

glucose-6-phosphate dehydrogenase

32

This acetylator can slow metabolism

procainamide

33

This acetylator can cause a lupus-like syndrome

hydralazine

34

What four things can alter metabolism and excretion

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

35

What are the four phases of new drug testing

animal testing
phase 1-3

36

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

phase 1 (after animal testing)

37

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

phase 2

38

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

phase three

39

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

8-9 years
1 billion dollars

40

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

A

41

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

B

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

C

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

D

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

X