Pharmacokinetics

Question 1

List the routes of administration of a drug

Answer 1

1) absorption
2) distribution
3) metabolism (biotransformation)
4) elimination

(ADME)

Question 2

The movement of a drug from the site of administration into the blood

Answer 2

Absorption

Question 3

Term that describes how once in the blood, the drug moves to various parts of the body

Answer 3

Distribution

Question 4

Term used for when the drug is converted to a form that is more readily eliminated

Answer 4

Metabolism (biotransformation)

Question 5

Metabolism or excretion of the drug from the body

Answer 5

Elimination

Question 6

When does the drug move from pharmacokinetics to pharmacodynamics

Answer 6

When the drug reaches it’s site of action and when it starts showing an effect because it starts binding to receptors

Question 7

What route of administration is convenient, but slower and less complete than parenteral (around the GI tract) forms?

Answer 7

Oral

Question 8

What are ingested drugs subject to?

Answer 8

First-pass effect (portal circulation)

Question 9

What is the first-pass effect?

Answer 9

Blood from the GI tract passes through the liver before entering other organs; during the first pass through the liver, some or nearly all of a drug can be metabolized to an inactive or less active derivative; as a result, some drugs are useless when given orally

Question 10

What does it mean for a drug to be parenteral?

Answer 10

Around the GI tract (ex: IV)

Question 11

What is the difference between oral administration and IV administration when it comes to over-dosing?

Answer 11

Oral: have time to combat it b/c it has to make it through the system first
IV: don’t have time to combat it

Question 12

What part of the body is the major site of absorption following oral administration? Why?

Answer 12

Intestines because they have a lot of surface area

Question 13

What route of administration means in the pouch between the cheek and gums, and permits direct absorption into the systemic venous circulation (can be fast or slow)

Answer 13

Buccal

Question 14

What route of administration is under the tongue and permits direct absorption into the systemic venous circulation?

Answer 14

Sublingual

Question 15

What is an example of a sublingual route of administration?

Answer 15

Nitroglycerin for angina

Question 16

What route of administration is good for a patient who is nauseous or vomiting, and is formulated as a suppository?

Answer 16

Rectal

Question 17

What route of administration is often faster with absorption and more complete than with oral, and can be given in large volume?

Answer 17

Intramuscular

Question 18

What are the compartments in intramuscular absorption?

Answer 18

Compartment 1 = muscle

Compartment 2 = blood

Question 19

What route of administration offers slower absorption than the intramuscular route due to more vasculature, but large volume doses are feasible

Answer 19

Subcutaneous

Question 20

What is an example of subcutaneous administration?

Answer 20

Insulin

Question 21

What route of administration does not involve absorption (bioavailability is 100% = measures how much of your dose got into the blood), and can be dangerous b/c of the high blood levels that are produced if administration is too rapid

Answer 21

Intravenous (IV)

Question 22

How many compartments are involved with IV?

Answer 22

1 = blood

Question 23

What route of administration offers delivery closest to the target tissue, providing the most rapid absorption because of the large surface area available?

Answer 23

Inhalation (due to the alveoli)

Question 24

What route of administration includes any application to the skin or the mucous membranes of the eye, nose, throat, airway, or vagina for LOCAL effect; the rate of absorption is usually slower than any of the other routes

Answer 24

Topical

Question 25

Where is one place that we never want topical administration to reach?

Answer 25

The blood

Question 26

What is an example that you would need topical administration for?

Answer 26

Rash

Question 27

What route of administration involves application to the skin for SYSTEMIC effects; absorption usually occurs very slowly, but the first-pass effect is avoided (absorption is ALWAYS involved); drug must be potent

Answer 27

Transdermal

Question 28

Example of transdermal administration

Answer 28

Nicotinic patch

Question 29

What are the 3 types of administration that are parenteral (around the GI tract)?

Answer 29

IV (intravenous)
IM (intramuscular)
SC (subcutaneous)

Question 30

Can a system that doesn’t use a carrier be saturated?

Answer 30

Nope

Question 31

Most common type of drug movement in the body?

Answer 31

Passive diffusion

Question 32

Drug movement in the body that is driven by concentration gradient across a membrane;
No carrier
Not saturable
Low structural specificity

Answer 32

Passive diffusion

Question 33

Drug movement in the body that is driven by concentration gradient
Involves specific carrier proteins
Is saturable
No energy is required

Answer 33

Facilitated diffusion

Question 34

Drug movement in the body that moves against a concentration gradient
Involves specific carrier proteins
Is saturable
Needs ATP

Answer 34

Active transport

Question 35

What are the 2 things you have to decide on in order to figure out the drug movement in the body

Answer 35

1) Does it need a carrier? (saturable or not?)

2) Did it need energy?

Question 36

Given the example:
Give certain amount of drug and that drug moves into the cells. Then give more of that drug and more of it moves into the cells. Then give even more and even more moves into cells. If every time I give more drugs and more movement occurs, this shows what?

Answer 36

The drug is not saturated, which means that it is using passive diffusion

Question 37

Given the example:
You used a drug to inhibit ATP. If you stop ATP production, and the drug stops moving, then what type of movement is the drug using?

Answer 37

Active transport

Question 38

Given the example:
You used a drug to inhibit ATP. If you stop ATP production, and the drug continues to move, then what type of movement is the drug using?

Answer 38

Facilitated diffusion