Pharmacotherapeutics, Pharmacokinetics, & Pharmacodynamics Contd

Front 1

2nd process of pharmacodynamics

Back 1

Distribution

Front 2

The distribution of a drug throughout the body depends on three factors:

Back 2

1. the drug’s ability to leave the blood

2. blood flow to the tissues

3. the drug’s ability to enter cells.

Front 3

There are two conditions that low blood flow can affect the outcome of the drug action:

Back 3

Abscess
Tumor

Front 4

Protein-Binding affects the ____ of a drug. When_____ to protein, it is unable to pass though the capillary walls.
The bonds will dissolve in time, and the drug molecules will become free and ______.

Back 4

distribution

bound

active

Front 5

Do highly protein bound drugs have longer or shorter durations of action?

Back 5

Longer duration

Front 6

Protein-binding- drugs circulate in the plasma either ___ or ____ to plasma proteins (usually _____)

Back 6

bound

unbound

albumin

Front 7

Albumin is a ____ molecule and because of this, albumin always remains in the blood stream.

Back 7

large

Front 8

The degree to which Protein-binding- drugs are bound is determined by the ____ between albumin and the drug. It is represented by ____.

Back 8

attraction

percentages

Front 9

How does the Blood-Brain Barrier work?

Back 9

It is a highly selective protective mechanism.
The cells of the CNS system have very tight capillary walls that limit movements of drug molecules into drug tissues.

Front 10

Metabolism of drugs occurs primarily in the ____.

Back 10

liver

Front 11

A product of metabolism is called a _______.

Back 11

metabolite

Front 12

HEPATIC FIRST-PASS EFFECT

Back 12

initial biotransformation of a drug that produces altered (usually less) pharmacologically active molecules. As drugs are metabolized through the liver the loss of effectiveness is called the first-pass effect.

Front 13

Drugs that experience a high first-pass effect may need _____ oral doses to achieve a therapeutic level of circulating drug.

Back 13

higher

Front 14

A drug given via the ___ route may be extensively metabolized or broken down by the liver before reaching the systemic circulation (high first-pass effect).

Back 14

oral

Front 15

First pass _______ may significantly limit the drugs effect.

Back 15

metabolism

Front 16

Drugs given ____ bypass the liver, preventing the first-pass effect from taking place, and more drug reaches the circulation.

Back 16

IV

Front 17

Example of a drug with a high first pass metabolism?

Back 17

Nitroglycerin

Front 18

What are the routes that bypass the liver (dodge the first pass effect)?

Back 18

Everything besides PO!!

Front 19

Liver metabolism is predominantly achieved by specific ___ ____.

Back 19

liver enzymes

Front 20

The microsomal enzymes in the liver that are responsible for liver metabolism are called the ______ ____ ________.

Back 20

cytochrome P-450 system

Front 21

The enzyme ______ is the most common and is responsible for the metabolism of most drugs.

Back 21

CYP3A4

Front 22

Some drugs either induce or inhibit the P-450 system, altering _______ of other drugs.

Back 22

metabolism

Front 23

When a large quantity of one of the P-450 system enzymes is present, more _____ can occur through this pathway.

Back 23

metabolism

Front 24

An increase in metabolism rapidly ________ the amount of circulating drug.

Back 24

decreases

Front 25

Drugs that induce a hepatic enzyme will cause ____ metabolism to occur, which will rapidly _____ the amount of active circulating drug.

Back 25

more

decrease

Front 26

Drugs that inhibit a hepatic enzyme will cause ____ metabolism to occur, which will rapidly _____ the amount of active circulating drug.

Back 26

less

increase

Front 27

What is one common drug that potentially INHIBITS the p450 enzymes?

Back 27

grapefruit juice

Front 28

What is one common drug that potentially INCREASES the activity of P450 enzymes?

Back 28

tobacco

Front 29

_______ is the process of removing a drug, or its metabolites, from the body.

Back 29

Excretion

Front 30

The most common route for drug excretion is through the ______.

Back 30

urine

Front 31

Diseases and pathophysiologic changes in the kidney decrease the effectiveness of the kidney in drug ____.

Back 31

excretion

Front 32

3 processes are involved in renal excretion of drugs.

Back 32

1. glomerular filtration.

2. passive tubular reabsorption.

3. active tubular secretion.

Front 33

glomerular filtration

Back 33

Most drug particles pass easily through the spaces of the capillary walls into the urine in the proximal tubule.

Front 34

passive tubular reabsorption

Back 34

The drug particles will try to move from the area of greater concentration to that of lesser concentration.

Front 35

active tubular secretion

Back 35

Active transport systems in the renal tubule work to move some drugs from the blood and into the urine.

Front 36

Drug excretion can be increased if the ____ of the urine encourages the drug to become an ion.

Back 36

pH

Front 37

Overuse of the active transport system also affects _____.

Back 37

excretion

Front 38

2 drugs can be given together to deliberately slow the rate of _______ of one or both of the drugs.

Back 38

excretion

Front 39

The ____-____ if the combined process of both metabolism and excretion

Back 39

Half-Life

Front 40

Half-Life

Back 40

The time it takes for ½ the drug concentration to be eliminated from the body

Front 41

In one half-life, a set _____ of the drug molecules present in the blood will be eliminated, not an absolute set number of drug molecules.

Back 41

percentage

Front 42

Steady State

Back 42

The point at which the amount of drug being administered and the amount being eliminated are equal

Front 43

At ____ to _____ half-lives, steady state is achieved.

Back 43

four to five

Front 44

The full ____________ response of a particular drug dose is measured when the drug has achieved steady state.

Back 44

pharmacotherapeutic

Front 45

Steady state will never equal ____

Back 45

100%

Front 46

Onset

Back 46

time it takes to reach minimum effective concentration

Front 47

Peak

Back 47

time it takes to reach highest blood or plasma concentration

Front 48

Duration

Back 48

length of time the drug has a pharmacologic effect

Front 49

This rate is called “clearance” or “clearance rate of the drug”

Back 49

Rate at which drug molecules disappear from the circulatory system

Front 50

Renal excretion and hepatic metabolism are the major modes of _______.

Back 50

clearance

Front 51

____________ is the biologic, chemical, and physiologic actions of a particular drug within the body.

Back 51

Pharmacodynamics

Front 52

Drugs cannot create new responses in the body; they can only ___ __, ___ ___, ______, or _____ a response that the body is inherently capable of producing.

Back 52

turn on, turn off, promote, or block

Front 53

At the ____ ____, the drug is able to stimulate the cell to act in a way that the cell is designed to act.

Back 53

receptor site

Front 54

Each type of receptor is responsible for producing a particular effect in the cell.
An ______ causes the cell to act. An _______ or blocker prevents something
else from attaching to the cell blocking and action.

Back 54

AGONIST

ANTAGONIST

Front 55

Single-occupancy theory

Back 55

The intensity of the body’s response to the drug is directly related to the number of receptors occupied by the drug.
The maximum response occurs when all of the receptors have drug molecules attached.

Front 56

Modified occupancy theory

Back 56

Different drugs have different strengths of attractions, or affinity, for receptor sites.
Once a drug is attached to a receptor, it has different abilities to stimulate the receptor.

Front 57

Receptors are not static.
Continual stimulation from an agonist usually makes the drug ___ _____.

Back 57

less effective.

Front 58

Continual blockage from an antagonist usually makes the drug ___ likely to react.

Back 58

more

Front 59

Drugs exert their effect by reacting _____ or _______ with other molecules in the body.

Back 59

physically

chemically

Front 60

Potency and Efficacy

Back 60

The level of the drug needed in the body to produce an effect

Front 61

Maintenance dose

Back 61

daily dose

Front 62

Loading dose

Back 62

larger than usual dose to reach an therapeutic effect quicker

Front 63

Therapeutic index

Back 63

The difference between an effective dose and a toxic dose

Front 64

minimum effective concentration

Back 64

Certain level of drug must be present in the body to have any effect

Front 65

The amount of a drug that must be given in order to produce a particular response is called the ______ of a drug.

Back 65

potency

Front 66

How well a drug produces its desired effect is called ______.

Back 66

efficacy

Front 67

The dose that is given consistently over time is called the _____ _______.

Back 67

maintenance dose

Front 68

Patients who are started on drug therapy using the standard maintenance dose arrive at steady state after ______ half-lives.

Back 68

4-5

Front 69

The loading dose is computed so that after some of the drug is eliminated, the drug concentration in the body is still in the ______ range.

Back 69

therapeutic

Front 70

The point at which the dose would be fatal in 50% of the population receiving that dose is called lethal dose 50% (_____).

Back 70

LD50

Front 71

The relation of ED50 to LD50 is called the ____ ______.

Back 71

therapeutic index

Front 72

As drug levels within the body increase, the patient is more likely to experience____ _____ from drug therapy.

Back 72

adverse effects

Front 73

To help determine whether a drug’s dose is sufficient to be in the therapeutic range, but not so high as to cause adverse effects, ____ ____ of the drug are often measured.

Back 73

blood levels

Front 74

The therapeutic range can only be considered an _______.

Back 74

average

Front 75

All drugs have some type of adverse effect(s). True or False?

Back 75

True

Front 76

An ____ _____ of drug therapy is usually an undesirable effect other than the intended therapeutic effect.

Back 76

adverse effect

Front 77

A ___ _____ occurs when two drugs or a drug and another element have an effect on each other.

Back 77

drug interaction

Front 78

An allergic response is a(an) ____ _____ response.

Back 78

immune system

Front 79

After an allergic response to a drug, the ____-_____ response happens when the drug is taken again.

Back 79

antigen–antibody

Front 80

After an allergic response, ymptoms may become more _____ each time the drug is introduced into the body.

Back 80

severe

Front 81

The most serious allergic response is called_________.

Back 81

anaphylaxis

Front 82

_________ responses are unusual and in fact may be the opposite of what is anticipated.

Back 82

Idiosyncratic

Front 83

Which of the following is not a symptom of anaphylaxis?
A. Bronchospasms
B. Vasodilation
C. Convulsions
D. Urticaria

Back 83

D. Urticaria

Front 84

Neurotoxicity

Back 84

Signs and symptoms: drowsiness, auditory and visual disturbances, and seizures.

Front 85

Hepatotoxicity

Back 85

If liver damage occurs, the drug will not be metabolized as efficiently.

Front 86

Nephrotoxicity

Back 86

Signs and symptoms: decreased urinary output, elevated blood urea nitrogen, increased serum creatinine, altered acid-base balance, and electrolyte imbalances.

Front 87

Ototoxicity

Back 87

Signs and symptoms: tinnitus, hearing loss, light-headedness, vertigo, and nausea.

Front 88

Cardiotoxicity

Back 88

Signs and symptoms: irregularities in conduction, heart failure, and damage to the myocardium.

Front 89

Immunotoxicity

Back 89

Signs and symptoms: immunosuppression.

Front 90

Additive Effect

Back 90

An effect in which two substances or actions used in combination produce a total effect the same as the sum of the individual effects. (1+1=2)

Front 91

Synergistic Effect

Back 91

occurs when 2 or more "unlike" drugs are used together to produce a combined effect, and the outcome is a drug effect greater than either drug's activity alone (1+1=3)

Front 92

Potentiated Effect

Back 92

an interaction in which the effect of only one of the to drugs is increased. (1/2+1=2)

Front 93

Antagonistic Effect

Back 93

the opposite of synergistic effect. Results in an effect that is less than the effect of either drug alone because the 2nd drug either diminishes or cancels the effect of the 1st drug. (1+1=0)

Front 94

5 key categories to look at when assessing Core Pt. Variables

Back 94

health status
lifespan and gender
lifestyle, diet, and habits
environment
culture and inherited traits

Front 95

bioavailability

Back 95

term used to describe the fraction of the administered dose that reaches the systemic circulation and produces effects

Front 96

IV drugs have ___% bioavailability

Back 96

100%

Front 97

Bioequivalent

Back 97

2 drugs that ahve the same bioavailability (both drugs absorbed into circulation system in identical amounts and with same absorption rates)

Front 98

How do you maximize therapeutic effects and minimize adverse effects?

Back 98

Check pts history, constant evaluation, admin drugs correctly, etc.