Orientation to Pharmacology Flashcards

1
Q

What is pharmacokinetics ?

A

The body’s effect on drugs - involves drug absorption, drug distribution, drug metabolism and drug excretion

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2
Q

What is pharmacodynamics?

A

This is the impact of drugs on the body

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3
Q

What are the three properties of an ideal drug?

A

Effectiveness, Safety, and Selectivity

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4
Q

Is there such a thing as an ideal drug?

A

No- there is no ideal drug that does not cause any side effects.

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5
Q

What is the most important property a drug can have?

A

Effectiveness - the drug elicits the response for which it is given

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6
Q

What is the therapeutic objective ?

A

The objective of drug therapy is to provide maximum benefit with minimal harm

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7
Q

Drug _______ , ________, and ____________________ are important determinants of drug responses.

A

dosage; route; timing of administration

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8
Q

Pharmacokinetic processes determine how much of an administration dose gets to its ______________

A

sites of action

4 major pharmacokinetic processes-
ADME

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9
Q

Once a drug has reached its site of action, pharmacodynamic processes determine _________ and ________________ of the ___________.

A

nature; intensity; response

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10
Q

In most cases the initial step leading to a response is the ______________ of a drug to its _____________

A

binding; receptor. This is followed by a sequence of events that ultimately leads to a response

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11
Q

Characteristics unique to each ______________ can influence the _____________ and ____________________ processes and by doing so can help determine the ________________ to a drug

A

patient; pharmacokinetic; pharmacodynamic; patients response

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12
Q

Sources of individual variation when it comes to the patients response to a drug

A

Drug interactions, age, gender, weight, pathologic variables especially the diminished function of the kidneys and liver, the major organs of drug elimination and genetic variables

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13
Q

Genetic factors can alter the _____________ of drugs and can predispose the patient to unique _________ dr

A

metabolism; drug reactions

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14
Q

No two patients will response identically to the same drug regimen. True or false.

A

true - everyone is different and genetically unique

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15
Q

To achieve the ___________, we must tailor drug therapy to the _________________.

A

therapeutic objective; individual

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16
Q

Our ultimate concern when administering a drug is _________________

A

the intensity of the response

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17
Q

The intensity of the response is determined by the _______________ of a drug at its ______________-

A

concentration; sites of action

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18
Q

What are factors that determine the intensity of drug responses ?

A

Administration
Pharmacokinetics
Pharmacodynamics
Sources of Individual Variation

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19
Q

Important events will take place after the ________________ is delivered and these must be __________ to.

A

Medication; responded

Remember the MLB pitcher analogy that likened the nurses response to medication administration and response to a pitcher throwing a pitch and anticipating what would happen next

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20
Q

What is the role of the FDA in drug regulation and safety?

A

The FDA regulates the pharmaceutical industry by approving drugs for marketing and use. Its aim is to make drugs safer, more effective and more affordable. It advances public health and aids public in getting accurate science based information.
It also provides rigorous oversight of drug safety after a drug has been approved.

The FDA regulates: 
Foods
Dietary Supplements
Drugs
Prescription and Non-prescription
Biologics
Vaccines
Blood and Blood products
Medical Devices
Tongue depressors
Bed pans
Heart Pace makers
Electronic: Products that give off radiation
Xray equipment
Cosmetics
Veterinary Products
Tobacco Products
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21
Q

What is the most reliable way to objectively assess drug therapies ?

A

Randomized Controlled Trials

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22
Q

What are OTC agents ?

What is CAM ?

A

Over the Counter agents such as vitamins and supplements

they are the most common form of Complementary and Alternative Medicine

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23
Q

Commonly used dietary supplements include

A
Cranberry Juice
Echinacea
Garlic
Ginger Root
Ginkgo Biloba
Green Tea
Probiotics
St. John’s Wort
Valerian Root
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24
Q

FDA regulations for dietary supplements

A

dietary supplements do not have to be approved by the FDA
Manufacturer must notify the FDA of efficacy claims
Has authority to intervene if supplement becomes harmful
Only after it has been released for marketing

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25
Q

What does pharmacokinetics determine ?

A

How much of an administered drug gets to its sites of action

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26
Q

Drug absorption factors

A

Rate of Dissolution- before a drug can be absorbed, it must first be dissolved; drugs with rapid dissolution have a faster onset than drugs with a slow dissolution

Surface Area: major determinant of rate of absorption; the larger the surface area, the faster the absorption

Blood Flow:drugs are absorbed most rapidly from sites where blood flow is high

Lipid Solubility: highly soluble drugs are absorbed more rapidly than drugs whose lipid solubility is low; lipid-soluble drugs can readily cross membranes, whereas low lipid-soluble drugs cannot

pH Partitioning

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27
Q

What are the different absorption patterns for IV, IM, SQ and Oral routes ?

A

IV is instantaneous absorption
IM and SQ are both relatively more rapid in being absorbed
Oral absorption is slowest

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28
Q

What is the distribution of the drug determined by?

A

Blood flow to tissues
Ability to exit the vascular system
Ability to enter the cell

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29
Q

What is an abscess ?

A

A puss filled pocket with no internal blood flow- antibiotics would not reach the bacteria there and would not prove effective unless the abscess is drained

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30
Q

Tumors have _________________ ______________ supply, which would affect drug therapy.

A

limited blood

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31
Q

Factors affecting the passage of the drug through the cell membrane

A

Lipid solubility

presence of a transport system

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32
Q

What is metabolism defined as for drugs ?

Where does most drug metabolism take place ?

A

The enzymatic alteration of a drug structure

Most drug metabolism takes place in the liver

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33
Q

To directly penetrate membranes ….. a drug must be

A

lipid soluble

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34
Q

What organ accounts for the majority of drug excretion ?

A

The kidneys
Glomerular Filtration
Passive Tubule Reabsorption
Active Tubular Secretion

Drugs are removed from the body through urine (renal excretion) and sweat, bile, saliva, breast milk and expired air (all non renal excretion methods)

Decreased kidney function = delayed excretion

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35
Q

Compare effect of healthy kidneys on drug’s duration of action with that of failing kidneys

A

Healthy kidneys will limit the duration of action of many drugs while failing kidneys result in an increase in the duration and intensity of drug responses

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36
Q

Drugs must cross cell membranes by what 3 ways ?

A
  1. Through Channels or Pores
  2. Aid of a Transport System
  3. Direct Penetration of a Membrane
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37
Q

Very few _________ cross membranes via ________________ because of how small they are; only the smallest of compounds pass through these channels; some of these compounds include: ________________

A

drugs; channels/pores; SODIUM and POTASSIUM

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38
Q

What do transport systems of cells do ?

A

Move drugs from one side of the cell membrane to the other

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39
Q

Will transport systems carry any drug ?

A

No they are selective; it is dependent on the drugs structure

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40
Q

What is one of the most important transporters of the cell?

A

P Glycoprotein

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41
Q

What is P Glycoprotein ?

A

a multi-drug transporter protein; It carries many drugs out of cells and can be found in many cells in the LIVER, KIDNEY, PLACENTA, INTESTINES, CAPILLARIES OF THE BRAIN

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42
Q

Discuss the action of P Glycoprotein within different organs in the body

A

In the liver P-glycoprotein transports drugs into bile for excretion
In the kidneys P-glycoprotein pumps drugs into the urine for excretion
In the placenta P-glycoprotein transports drugs back into maternal blood to reduce fetal drug exposure
In the intestines P-glycoprotein transports blood into the intestinal lumen reducing drug absorption into the blood
In the brain capillaries, P-glycoprotein pumps drugs into the blood thereby limiting access to the brain

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43
Q

Parenteral Routes of Administration

A

Subcutaneous
Intramuscular
Intravenous

44
Q

Other routes of Administration

A
Oral 
Aural
Ocular
Inhaled
Topical
Transdermal
Suppositories (Rectal or Vaginal)
45
Q

Absorption pattern of IM route

A

Rapid-w/ water soluble drugs

Slow-w/ poorly soluble drugs

46
Q

Absorption pattern of oral route

A

Slow and Variable

47
Q

Distribution is defined as …………….

A

the movement of drugs throughout the body -

drugs move from the blood into the tissues and cells

48
Q

Abcesses and tumors affect ___________________ because there is _________________

A

drug distribution; low blood flow

49
Q

Blood Flow of Tumors

A

Solid tumors have limited blood supply, central blood flow is markedly decreased, though the outer region has high blood flow; Achievement of high drug levels deep inside the tumor is not achieved making them highly resistant to drug therapy

50
Q

What is necessary in order for drugs to undergo metabolism and excretion ?

A

They must exit the vascular system

51
Q

Drugs in the vascular system leave the blood at

A

Capillary beds
Through the blood-brain barrier
Placental drug transfer
Protein binding

52
Q

How can drugs leave typical capillary beds ?

A

By passing between the spaces between capillary cells that make up the vessel, rather than pass through them.

53
Q

Some drugs must enter cells to reach their __________________

A

sites of action

54
Q

All drugs must enter cells in order to undergo __________________ & ________________.

A

metabolism & excretion

55
Q

Factors that determine the ability of the drug to enter the cell

A

Lipid Solubility
Transport Proteins
Both

56
Q

How is metabolism defined ?

A

The enzymatic alteration of drug structure

57
Q

Most drug metabolism takes place where?

A

In the liver

58
Q

What is the most important consequence of drug metabolism ?

A

Renal drug excretion

59
Q

Are the kidneys able to excrete drugs that are highly lipid soluble ?

A

No, they are not

60
Q

How does metabolism accelerate renal drug excretion?

A

By changing highly lipid soluble drugs into more hydrophilic, water soluble substances that are more easily and rapidly excreted by the kidneys.

61
Q

Drug metabolism can convert pharmacologically active compounds to _________________-

A

inactive forms

62
Q

Metabolism can increased the ________________ of some drugs.

A

Effectiveness

the conversion of codeine to morphine - morphine has much greater analgesic effects

63
Q

What does activation of prodrugs means ?

A

A inactive form of a drug is administered which then undergoes metabolic changes to become an active form

64
Q

By converting drugs into inactive forms, metabolism can decrease ________________

A

toxicity

65
Q

Metabolism can increase ________________ by converting relatively safe compounds into forms that are ________________-

A

the potential for harm; toxic

66
Q

Special Considerations in Drug Metabolism: Age

A

Infants are especially at an increased risk for drug sensitivity because liver’s drug metabolizing capabilities are not fully developed until 1 year after birth.

Older adults also are at increased risk of toxicity because their ability to metabolize drugs is commonly decreased.

67
Q

Drugs may be P450 __________, P450 enzyme ____________ and P450 enzyme ___________.

A

substrates; inducers; inhibitors

68
Q

What are drugs that are metabolized by P450 enzymes called ?

A

Substrates

69
Q

True or false- a drug can be both an inducer and a substrate……

A

True….. If the drug is both an inducer and a substrate, by stimulating the liver to produce more drug metabolizing enzymes, the drug can increase the rate of its own metabolism, thereby necessitating an increase in its dosage to maintain therapeutic effects.

70
Q

True or false …. the induction of drug metabolizing enzymes can decrease the metabolism of other substrates used concurrently, allowing for no changes in their dosages to keep levels steady.

A

False….. the induction of drug metabolizing enzymes can accelerate the metabolism of other substrates used concurrently, necessitating an increase in their dosages

71
Q

What are inhibitors as it relates to metabolism ?

A

Drugs that act on the liver to decrease rates of drug metabolism.

72
Q

What is one therapeutic effect of inhibitor drugs on metabolism ?

A

Because they slow the rate of drug metabolism, it is possible that other drugs used concurrently can reach toxic levels or have adverse effects.
The active accumulation of a drug due to the slower metabolism must be carefully monitored.

73
Q

The first pass effect refers to the

A

rapid hepatic enzyme inactivation of certain oral drugs - as a result, a dosage may have no therapeutic effect. In order to bypass this, drugs that are rapidly inactivated by hepatic enzymes can be administered through another route or their dosage is increased to counteract the first pass effect.

74
Q

How can nutritional status affect the rates of drug metabolism?

A

Certain cofactors are needed by hepatic drug metabolizing enzymes in order to function. A malnourished patient may be deficient in some of these cofactors, thereby compromising drug metabolism.

75
Q

How can competition between drugs affect their metabolism?

A

Two drugs that are metabolized by the same metabolic pathway may be competing with each other for metabolism. Since there are winners and losers, one drug may be metabolized more slowly than the other.

Therefore, drug levels must be monitored for toxicity because the one that has a decreased rate of metabolism may accumulate to dangerous levels.

76
Q

Drugs can be excreted through the

A

urine, bile, sweat, breast milk, saliva and expired air

77
Q

Urinary excretion is the net result of what 3 processes ………….

A

glomerular filtration
passive tubular reabsorption
active tubular secretion

78
Q

When two drugs are taken together what can happen?

A

one may alter the absorption, distribution, metabolism or excretion of the other

Altered Absorption: May be enhanced or reduced
Altered Distribution: Competition for protein binding and alteration of extracellular pH
Altered Metabolism: Increase or decrease metabolism of other drug
Altered Excretion: One drug can alter the renal excretion of another

79
Q

Why do clinicians monitor plasma drug levels in efforts to regulate drug responses ?

A

It has been shown that there is a direct correlation between therapeutic and toxic responses and plasma drug levels.

More often than not, it is a practical impossibility to measure drug concentrations at sites of action

80
Q

Which two plasma drug levels are of special importance?

A

The minimum effective concentration and the toxic concentration

81
Q

What is the MEC?

A

The minimum effective concentration is defined as the plasma drug level below which therapeutic effects will not occur.

Example: any dose of warfarin below ______ will have no therapeutic effect

82
Q

How is toxic concentration defined ?

A

When drug levels within the plasma climb too high….

levels are high enough that toxic effects begin

83
Q

What is the therapeutic range ?

A

The plasma drug levels falling between the toxic concentration and the MEC

84
Q

Which drug is safer: one with a wider therapeutic range or one with a narrower therapeutic range?

A

The drug with the wider therapeutic range

85
Q

A drug with a narrow therapeutic range must be administered …………………..

A

carefully. There is little room for error between the MEC and the toxic concentration

86
Q

What is the objective of drug dosing ?

A

To administer drug doses within the therapeutic range

87
Q

Patients taking drugs with a _________________ therapeutic range are the most likely to require intervention for drug-related concentrations.

A

Narrow

88
Q

Drug responses cannot occur until ………………..

A

The drug has reached the MEC within the plasma

89
Q

Drugs with a short half life leave the body ______________.

Drugs with a long half life leave the body ______________.

A

quickly; slowly

90
Q

Morphine has a half life of 3 hours - how many mg of morphine will be present in the body after 3 hours ? After another 3 hours ?

A

25 mg after 3 hours

An additional 3 hours would result in 12.5 mg

91
Q

What determines the dosing interval (how much time separates each dose)?

A

The half life of a drug

92
Q

What is the dose response relationship ?

A

The relationship between the dose of the drug and the intensity of the effect it will produce…

93
Q

What does it mean to say the the dose-response relationship is the “graded” ?

A

The greater the dose amount, the more intense the effect will be.
Because the dose-response relationship is graded, we can adjust dosage levels accordingly to achieve the desired therapeutic effect.

94
Q

What is maximal efficacy and relative potency ?

A

The largest effect that a drug can produce

and the amount of drug that we must give to elicit that effect.

95
Q

Potency refers to the fact of a drug ………………

A

producing its effect at low doses.

96
Q

The dose response relationship determines ………….

A

the minimum amount of drug we can use
the maximum response a drug can elicit
How much we need to increase the dosage in order to produce the desired increase in response.

97
Q

What are receptors as it pertains to

drug interactions ?

A

Special chemicals in the body that most drugs interact with to produce effects

98
Q

What are the four primary receptor families ?

A

4 Primary Receptor Families

1. Cell Membrane-Embedded Enzymes
2. Ligand-Gate Ion Channels
3. G Protien-Coupled Receptor Systems
4. Transcriptions
99
Q

Difference between agonist and antagonist

A

Mimic the body’s own regulatory molecules
Activate receptors
Affinity allows the agonist to bind to receptors
Intrinsic activity allows the bound agonist to activate receptor function

Antagonists
Block actions of regulators
Produce their effects by preventing receptor activation

100
Q

Do agonists or antagonists treat overdoses?

A

Antagonists

101
Q

Opioid overdose produces ________________.

what should one do?

A

respiratory depression.

Block the receptor sites by giving an opioid antagonist (Narcan) and engage in competitive antagonism

102
Q

True or false …. some drugs do not act through receptors

A

True …. some drugs act through simple physical or chemical interactions with other small molecules

103
Q

Examples of “receptorless” drugs

A

Antacids, antiseptics, saline laxatives and chelating agents

104
Q

Receptors are dynamic components of ________________. What can happen when there is continuous stimulation of receptors by agonists or continuous exposure to antagonists.

A

The number of receptors on the cell surface can change as can their sensitivity to agonist molecules.

When the receptors of a cell are continually exposed
to an agonist, the cell usually becomes less responsive….. think of insulin resistance
Continuous exposure to antagonists has the opposite effect, causing the cell to become hypersensitive.

105
Q

The nurse who appreciates the reality of ______________ _____________ will be better prepared to anticipate, evaluate and respond appropriately to each patients ______________

A

interpatient variability; therapeutic needs

106
Q

What does a high therapeutic index indicate ?

A

That a drug is relatively safe

107
Q

What does a low therapeutic index indicate ?

A

That a drug is relatively unsafe