Pharmacokinetics COPY COPY

Question 1

ADME concept (4)

Answer 1

Absorption, Distribution, Metabolism, Excretion

Question 2

This term describes what the body does to the drug.

Answer 2

Pharmacokinetics

Question 3

What are the main steps of pharmacokinetics?

Answer 3

1.) absorption 2.) Distribution 3.) Elimination

Question 4

This term describes when the drug is acting on the body

Answer 4

pharmacodynamics

Question 5

What are the ways to administer drugs? (6)

Answer 5

1. ) oral or rectal
2. ) percutaneous
3. ) intravenous
4. ) intramuscular
5. ) intrathecal
6. ) Inhalation

Question 6

How are drugs eliminated in the body? (5)

Answer 6

1. ) urine
2. ) feces
3. ) milk, sweat
4. ) expired air

Question 7

What factors affect oral absorption? (4)

Answer 7

1. ) Disintegration
2. ) Drug in small particles
3. ) Dissolution
4. ) Drug in solution

Question 8

What part of the body are drugs maximally absorbed?

Answer 8

small intestine

Question 9

what makes the small intestine the best place for maximal absorption?

Answer 9

large surface area allows more blood to flow

Question 10

What factors affect gastric emptying? (6)

Answer 10

1. ) volume of meal
2. )meal composition
3. )viscosity,
4. )osmotic pressure,
5. ) position
6. ) drugs

Question 11

What factors slow gastric emptying?

Answer 11

high meal fat content, increased viscosity, increased osmotic pressure, opioids, anticholinergics, ethanol, bile salts and acidification

Question 12

What factors influence drug absorption? (8)

Answer 12

1. ) Molecular weight
2. ) Blood flow
3. ) solubility
4. ) concentration
5. ) Disintegration and dissolution
6. ) partition coefficient
7. ) transporters
8. ) pH partition theory

Question 13

What are the non-oral routes of drug administration? (6)

Answer 13

1. ) sublingual (under the tongue)
2. ) rectal
3. ) pulmonary
4. ) subcutaneous
5. ) intramuscular
6. ) intravenous

Question 14

What types of non-oral routes of drug administration are perfusion- rate limited?

Answer 14

subcutaneous and intramuscular

Question 15

phenomenon of drug metabolism when the drug concentration is greatly reduced before entering systemic circulation

Answer 15

First pass effect

Question 16

the fraction of lost drug during the process of absorption related to liver and gut wall clearance

Answer 16

first pass

Question 17

How do you recognize a drug with a first pass clearance?

Answer 17

Look at the F value

Question 18

If F=1 what is its first pass clearance?

Answer 18

there is NO first pass clearance

Question 19

True/False: If a drug has a much larger oral dose than intravenously, there is a first pass clearance.

Answer 19

TRUE

Question 20

How can you describe drug absorption? (2)

Answer 20

1. ) the EXTENT or total amount of drug entering systemic circulation
2. ) the RATE or how quickly the drug enters the systemic circulation

Question 21

Rate and extent to which the active ingredient or active moiety is absorbed from a drug product and which becomes systemically available

Answer 21

Bioavailability

Question 22

How would you determine rate if given a graph?

Answer 22

Tmax and Cpmax values

Question 23

How would you determine extent if given a graph?

Answer 23

AUC (area under the curve)

Question 24

A higher peak on a graph of generic vs. brand would indicate ____.

Answer 24

a higher/faster rate of absorption

Question 25

True/False: A higher AUC yields a higher extent or total amount of drug absorbed.

Answer 25

TRUE

Question 26

Fraction of drug administered which becomes systemically available. Comparing an oral dose to and intravenous dose of a drug.

Answer 26

Absolute Bioavailability

Question 27

If a drug is not absorbed at all, what would the absolute bioavailability be?

Answer 27

0

Question 28

If a drug has a F= <1 value what has to happen?

Answer 28

a larger oral dose has to be given compared to the intravenous dose

Question 29

used to determine bioequivalence or when 2 orally administered drugs are being compared

Answer 29

relative bioavailability

Question 30

represents how extensively the drug distributes in the body

Answer 30

volume of distribution (Vd)

Question 31

What would a drug with a large volume of distribution indicate?

Answer 31

they are bound, and stored somewhere and lipid soluble. They do NOT stay in the blood.

Question 32

What are the factors that affect drug distribution between body compartments? (5)

Answer 32

1. ) tissue differences contribute to differences in blood perfusion 2. ) presence of disease states 3. ) degree of drug lipid solubility 4. ) extent of drug protein binding 5. ) regional differences in pH

Question 33

What determines the size of the loading dose?

Answer 33

concentration and volume of distribution

Question 34

allows you to rapidly achieve the therapeutic concentration of a drug

Answer 34

loading dose

Question 35

If a drug with a F= 0.5 value is given, what effect would this have on the loading dose?

Answer 35

the loading dose would be TWICE as much than an IV.

Question 36

True/False: Loading dose is dependent on clearance.

Answer 36

FALSE; not dependent on clearance

Question 37

What are the targets for drug action?

Answer 37

Receptor Transporters Ion Channels Enzymes Hit the drug action target just RITE.

Question 38

Why are receptors important in drug action?

Answer 38

- Largely determine quantitive relationship b/w drug dose and effectivity - Determine selectivity and antagonist effects

Question 39

Compare and contrast the two dose-response relationships types.

Answer 39

Graded is a sigmoidal curve that tells us the max efficacy while quantal is a bell-shaped graph that tells us about variability. They BOTH tell us about potency and selectivity.

Question 40

What is the effective dose? (ED50)

Answer 40

The concentration resulting in 50% of the maximal response.

Question 41

What are the x and y axis for graded and quantal? For graded if curve is shifted to the left then the drug is less or more potent?

Answer 41

Graded is response vs dose Quantal is frequency (% asleep or wake) vs dose More potent!

Question 42

What is Ti? If I have a high Ti then do I have to think when dosing? How do I find on graph

Answer 42

Ti=therapeutic index= LD50/ED50. It is a ratio at which 50% of subjects experience the toxic dose and 50% experience the therapeutic dose. Cumulative percents.

Question 43

What is the difference between potency and efficacy?

Answer 43

Potency is relative compares two drugs doses to another in producing the desired effect. Efficacy is the ability of a drug to effect and is described as maximal effect for a drug ( how wide and how tall in a d-r graph)

Question 44

Oral dose being MUCH larger than parenteral indicates...

Answer 44

First pass. Oral has to compensate for lost drug.

Question 45

Define Tachyphylaxis

Answer 45

Rapid or acute tolerance (example: nitroglycerin)

Question 46

Define Tolerance. Dose-response curve shifts left or right?

Answer 46

hyporeactivity from chronic drug exposure ( slower to get and slow to get rid of). Cross-tolerance also is a factor, for example, alcohol and benzodiazepines. Sh

Question 47

What is the difference between antagonist and inverse agonist? What is the difference between full and partial efficacy?

Answer 47

Antagonist zero efficacy while Inverse decreases efficacy. full and partial agonist are positive efficacy BUT partial will never reach the max efficacy that full agonist does. Note: partial can knock off full agonists.

Question 48

Where does the antagonist bind on the receptor? What are the two types?

Answer 48

to the active site of the receptor. reversible and irreversible antagonists.