Basic Principles of Pharmacology

Question 1

pharmacokinetics

Answer 1

How drugs move through the body (moves)

Question 2

pharmacodynamics

Answer 2

the effects of drugs and the mechanism of their action (effects)

Question 3

4 parts of taking medicine

Answer 3

Absorption, distribution, metabolism and excretion

Question 4

AUC/MIC, T>MIC, Cmax/MIC

Answer 4

?

Question 5

P-glycoprotein inhibitors

Answer 5

?

Question 6

Therapeutic drug monitoring: Drugs that exhibit narrow therapeutic indices

Answer 6

?

Question 7

Therapeutic drug monitoring: Timing of appropriate serum drug levels

Answer 7

?

Question 8

Absorption-

Answer 8

movement of the drug from its site of administration into the blood

Question 9

3 Factors that affect absorption

Answer 9

1. Route of administration can effect
2. Bioavailability
3. Concentration

Question 10

Factors that affect absorption: Route of administration can effect 4 things

Answer 10

Compliance, bioavailability, onset of action and duration of action

Question 11

Factors that affect absorption: Bioavailability

Answer 11

The percentage of administered drug that enters the blood

Question 12

Factors that affect absorption: Concentration

Answer 12

Higher concentration of drug at site of action may increase absorption

Question 13

Rectal administration may be useful in

Answer 13

presence of nausea, vomiting, pediatric

Question 14

Topical administration includes skin,

Answer 14

lungs, eyes, ears, nasal

Question 15

Factors that affect absorption: Bioavailability: If bioavailability is low,

Answer 15

higher doses may be required

Question 16

Factors that affect absorption: Concentration: Rapid absorption may lead to

Answer 16

higher concentrations/ peaks

Question 17

Distribution-

Answer 17

the process of drugs moving throughout the body after absorption

Question 18

Factors that affect distribution: 4 things

Answer 18

• Size of the organ
• Blood flow (well perfused tissue tend to have higher tissue concentrations)
• Solubility
• Binding (highly plasma protein bound drugs stay in the vascular compartment)

Question 19

Factors that affect distribution: explain the effect of binding

Answer 19

highly plasma protein bound drugs stay in the vascular compartment

Question 20

Factors that affect distribution: explain the effect of Blood flow

Answer 20

well perfused tissue tend to have higher tissue concentrations

Question 21

Metabolism occurs primarily

Answer 21

in the liver

Question 22

Metabolism can ___ the action of the drug

Answer 22

activate or terminate the action of the drug

Question 23

Metabolism some drugs are metabolized and converted to an ____ metabolite before excretion

Answer 23

inactive

Question 24

Some drugs are metabolized and converted to an inactive metabolite before excretion. 2 example:

Answer 24

Sympathomimetics, phenothiazines

Question 25

Prodrugs are

Answer 25

inactive until they are metabolized in the body

Question 26

Prodrugs: 2 example

Answer 26

Levodopa, minoxidil

Question 27

Unlike prodrugs, Other drugs are

Answer 27

active when administered and have active metabolites

Question 28

Unlike prodrugs, Other drugs are active when administered and have active metabolites. 2 examples:

Answer 28

Morphine, benzodiazepines

Question 29

Unlike prodrugs, Other drugs are active when administered and have active metabolites. There are also drugs that

Answer 29

do not get metabolized and remain active until excretion

Question 30

There are drugs that do not get metabolized and remain active until excretion, for example

Answer 30

Lithium

Question 31

Excretion (for MOST drugs) occurs primarily in the

Answer 31

kidneys

Question 32

Volatile anesthetic gases are excreted primarily by the

Answer 32

lungs (unlike most other drugs that are done by the kidneys)

Question 33

Drugs that are not metabolized-> excretion is the mode of elimination

Answer 33

?

Question 34

Metabolism is often needed to ensure

Answer 34

elimination of drugs and to facilitate excretion

Question 35

Metabolism: Phase I reactions

Answer 35

Converts parent drug to a more polar (water-soluble) form

Question 36

Metabolism: Phase 2 reactions

Answer 36

Increase water solubility by conjugation of the drug molecule with a polar moiety

Question 37

Glucuronate, acetate, or sulfate

Answer 37

?

Question 38

CYP isoenzymes

Answer 38

?

Question 39

P-glycoprotein

Answer 39

An ATP-dependent transport molecule that expels drug molecules from the cytoplasm into the extracellular space.

Question 40

Drug-receptor binding is r____, s___, and g____

Answer 40

reversible, selective and graded

Question 41

Drug-receptor binding: The higher the number of drug bound receptors,

Answer 41

the greater the pharmacological response

Question 42

Drugs that are bound to the receptors may be: (3 things)

Answer 42

Agonists, Partial agonists, Antagonists

Question 43

Agonists

Answer 43

a drug capable of activating the receptor upon binding to it

Question 44

Partial agonists

Answer 44

Produces less than the full effect

Question 45

In the presence of a full agonist, the partial agonist

Answer 45

acts as an inhibitor

Question 46

A pharmacological antagonist interacts with

Answer 46

the same receptor as the drug it is meant to inhibit

Question 47

Dose-response curve

Answer 47

depicts the relationship between the drug dose and magnitude of effect

Question 48

Dose-response curve: Doses below the curve

Answer 48

do not produce a pharmacological response

Question 49

Dose-response curve: Doses above the curve

Answer 49

do not produce much additional pharmacological response

Question 50

Dose-response curve: Therapeutic index (TI) is

Answer 50

the ratio between the lethal dose (LD) and the effective dose (ED). The larger the ratio, the safer the drug.

Question 51

Therapeutic index (TI) is the ratio between the lethal dose (LD) and the effective dose (ED). The larger the ratio,

Answer 51

the safer the drug. (larger means you have more room to mistake, therefore safer)

Question 52

Loading doses may help achieve therapeutic drug levels...

Answer 52

quicker

Question 53

Generally takes ___ half-lives of the drug to achieve steady state

Answer 53

4 ½ - 5

Question 54

Steady state

Answer 54

when the amount of drug going in equals the amount of drug going out to keep the blood levels “steady”

Question 55

When should serum drug levels for TDM should be taken

Answer 55

after steady state is achieved

Question 56

Many drugs that have a narrow therapeutic index may require TDM. 3 examples:

Answer 56

Digoxin, aminoglycosides, lithium

Question 57

Drug - Drug Interactions: Enzyme induction: Produces

Answer 57

an increased rate and extent of metabolism of drugs

Question 58

Drug - Drug Interactions: Enzyme induction: Produces an increased rate and extent of metabolism of drugs. often associated with

Answer 58

cytochrome P450 enzymes

Question 59

Drug - Drug Interactions: Enzyme induction: Drugs that increase enzyme activity are known as

Answer 59

inducers

Question 60

Drug - Drug Interactions: Enzyme Inhibition: The inhibitors of drug metabolism include, but are not limited to,

Answer 60

grapefruit juice*, amiodarone, and protease inhibitors

Question 61

Drug - Drug Interactions: Enzyme induction: Since inducers increase metabolism,

Answer 61

less drug becomes available → decreased drug effect

Question 62

Drug - Drug Interactions: P-glycoprotein inhibitors: Drugs that inhibit P-glycoprotein

Answer 62

increase bioavailability of the drug and can result in toxic levels of drugs when given at normal dosages.

Question 63

Drug - Drug Interactions: P-glycoprotein inhibitors: P-glycoprotein inhibitors include

Answer 63

Verapamil, grapefruit juice*

Question 64

Drug - Drug Interactions: P-glycoprotein inhibitors: Drugs that can become toxic when given with a P-glycoprotein inhibitor

Answer 64

Digoxin, cyclosporine

Question 65

Drug - Drug Interactions: P-glycoprotein inhibitors: Furanocoumarin

Answer 65

is the component in grapefruit juice that is responsible for these effects