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ADT Module 1-4 > Archangelo Chapter 2 - Pharmacology Basis of Therapeutics & Pharmacodymamic Principles > Flashcards

Archangelo Chapter 2 - Pharmacology Basis of Therapeutics & Pharmacodymamic Principles Flashcards

1
Q

What is the term for “how the body affects the drug”?

A

Pharmacokinetics

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2
Q

What is the term for “how the drug affects the body”?

A

Pharmacodynamics

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3
Q

What term defines the range of drug concentration in the blood between a minimally effective level and a toxic level?

A

Therapeutic window

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4
Q

What are the two commonly recognized methods of absorption?

A

1) Enteral (oral or rectal)

2) Parenteral (IM, SubQ, topical)

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5
Q

What is the term for the extent to which the drug reaches the systemic circulation?

A

Bioavailability

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6
Q

Bioavailability is expressed as a ___________

A

Fraction or percentage

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7
Q

What method of drug administration is 100% bioavailable?

A

Intravenous

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8
Q

Cell membranes are made up of what two components forming a bilayer?

A

1) Lipids

2) Proteins

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9
Q

What are the two types of movement across cell membranes?

A

1) Passive diffusion

2) Active transport

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10
Q

What is the term for the process in which molecules move from one side of a barrier to another without expending energy?

A

Passive diffusion

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11
Q

Fick’s law of Diffusion is dependent on what variables?

A

1) The differences in concentrations
2) The strength of the barrier
3) The distance that molecules must travel
4) The size of the molecules

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12
Q

Drugs diffuse more readily through the lipid bilayer in what neutral form?

A

Non-ionized

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13
Q

Weak bases become _____ in gastric acid and ______ in an alkaline environment

A

Ionized, non-ionized

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14
Q

Weak acids become ______ in gastric acid and ______ in an alkaline environment

A

Non-ionized, ionized

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15
Q

What is the term for the process in which membrane proteins act as carrier molecules to transport substances across cell membranes?

A

Active transport

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16
Q

What is the term for when a cell forms a vesicle surrounding a molecule and invaginates it?

A

Endocytosis

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17
Q

In terms of absorption, if blood flow to an area is limited absorption is likely _______

A

Limited

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18
Q

In terms of absorption, if intestinal motility is slowed, absorption may be _______

A

Increased

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19
Q

In terms of absorption, if intestinal motility is increased, absorption may be _______

A

Decreased

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20
Q

In review, what are four factors that affect absorption?

A

1) Movement across membranes and solubility
2) Preparation of the drug
3) Blood flow
4) GI motility

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21
Q

Are most drugs absorbed actively or passively?

A

Passively

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22
Q

Drugs administered orally must be ______ soluble to cross the GI mucosa

A

Lipid

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23
Q

What type of enteral administration is not subject to a first pass effect?

A

Sublingual or buccal

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24
Q

All routes of drug administration involving the GI tract are called _______

A

Enteral

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25
Q

All routes of drug administration NOT involving the GI tract are called _______

A

Parenteral

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26
Q

How are gaseous or small sprayable particles delivered?

A

Inhalation

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27
Q

What type of drug administration is considered the gold standard with regard to bioavailability?

A

Intravenous

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28
Q

What do parenteral administrations avoid?

A

The first pass effect

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29
Q

An implant with drug-releasing mechanisms under the skin is considered what form of administration?

A

Subcutaneous

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30
Q

What type of topical vehicle typically produces the greater effect?

A

Ointment

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31
Q

What form of drug administration is known for a continuous delivery of medication to achieve a constant blood level?

A

Transdermal

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32
Q

What factors affect distribution?

A

1) Blood flow
2) Solubility
3) Protein binding
4) Obesity

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33
Q

What is considered the standard for determining drug dosage and is often adjusted based on weight?

A

Ideal body weight

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34
Q

What is another term for unbound drug?

A

Free drug

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35
Q

What is the term that refers to the attraction between a drug and receptor?

A

Affinity

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36
Q

Acidic drugs commonly bind to what plasma protein?

A

Albumin

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37
Q

Basic drugs commonly bind to what plasma protein?

A

Alpha-acid glycoprotein (lipoproteins)

38
Q

What is the term for the apparent volume into which a drug distributes in the body at equillibrium?

A

Volume of distribution (Vd)

39
Q

Drugs that are hydrophillic or highly bound to protein have a ____ Vd

A

Low

40
Q

Drugs that are lipophyllic and are not highly protein bound have a _____ Vd

A

High

41
Q

Elimination is a combination of what two principles?

A

1) Metabolism

2) Excretion

42
Q

What is the organ that performs most of the body’s metabolic functions?

A

Liver

43
Q

What is the term for the phenomenon by which a drug first passes through the liver for degradation before distribution to the tissues?

A

First pass effect

44
Q

What is the name of a drug that is transformed from an inactive parent drug into an active metabolite?

A

Prodrug

45
Q

What are some common prodrugs and their active metabolites?

A

1) Allopurinol (oxypurinol)
2) Codeine (morphine)
3) Enalapril (enalaprilat)
4) Prednisone (prednisolone)
5) Sulindac (sulindac sulfide)

46
Q

What are the two broadly classified enzyme actions in metabolization?

A

1) Phase I

2) Phase II

47
Q

In which enzyme action is the drug changed to form a more polar or water-soluble compound?

A

Phase I

48
Q

In which enzyme action is a conjugate added to further increase water-solubility and enhance excretion?

A

Phase II

49
Q

Phase I metabolism is catalyzed by a family of enzymes called?

A

Cytochrome P450 system (CYP)

50
Q

What are the three CYP families?

A

1) CYP 1
2) CYP 2
3) CYP 3

51
Q

What are the five CYP isoforms?

A

1) CYP 1AC
2) CYP 2C
3) CYP 2D6
4) CYP 2E1
5) CYP 3A4

52
Q

What is the term for drugs that stimulate the production of isoforms and increase the amount of enzyme available to metabolize drugs?

A

Inductors

53
Q

What is the term for drugs that decrease the production of isoforms and decrease the amount of enzyme available to metabolize drugs?

A

Inhibitors

54
Q

What are the common excretory organs?

A

1) Kidneys
2) Lower GI tract
3) Lungs
4) Skin

55
Q

What are other structures involved in excretion?

A

1) Sweat glands
2) Salivary glands
3) Mammary glands

56
Q

What is the primary route of excretion?

A

Kidney

57
Q

What is the process by which a drug excreted in the bile flows into the GI tract where it is reabsorbed and returned to the circulation?

A

Enterohepatic recirculation

58
Q

What is the term for the time it takes one-half of the drug to be eliminated from the body?

A

Half-life

59
Q

What is the term that refers to the phenomenon that the amount of a drug that is eliminated is proportional to the concentration of that drug?

A

First-order elimination

60
Q

What is it called when fixed amounts of drugs are eliminated at a constant rate?

A

Zero-order elimination

61
Q

After how many half-lives of first-order kinetics is the drug basically eliminated?

A

Three to five

62
Q

What is the term for a constant mean concentration of drug in the body that represents equillibrium?

A

Steady state

63
Q

What is given when a desired blood concentration of a drug is imperative quickly?

A

Loading dose

64
Q

What is the term that represents the removal of a drug from the plasma or organ and is the final process in elimination?

A

Clearance

65
Q

Clearance is _______ related to the elimination half-life

A

Inversely

66
Q

Through what surrogate substrate is clearance estimated in the kidney?

A

Creatinine

67
Q

Why is creatinine able to be used for this purpose?

A

Because it is neither significantly secreted nor absorbed

68
Q

What does creatinine clearance estimate?

A

GFR

69
Q

What is a normal serum creatinine level?

A

0.8 - 1.2 mg/dL

70
Q

What is the creatinine clearance level below which renal function is significantly impaired?

A

50 mL/min

71
Q

In whom do you calculate the creatinine clearance rate when prescribing drugs?

A

1) Patients over 65

2) Those with a serum creatinine > 1.5 mg/dL

72
Q

What is the component of the cell (or an enzyme) to which an endogenous substance binds, initiating a chain of biochemical events?

A

A receptor

73
Q

What is the term for any chemical, endogenous or exogenous, that interacts with a receptor?

A

A ligand

74
Q

What are the four primary receptor types usually classified by the effect they produce?

A

1) Gated ion channel
2) Transmembranous
3) G-protein - coupled
4) Intracellular

75
Q

The function of this receptor is to open or close channels to allow certain ions to pass through

A

Gated ion channel

76
Q

List some examples of gated ion channels

A

1) Nicotinic acetylcholine receptor

2) Gamma-aminobutyric Acid (GABA)

77
Q

This receptor has its ligand-binding domain on the cell’s surface and an enzymatic portion inside the cell

A

Transmembranous

78
Q

What are the two types of change associated with transmembranous receptors?

A

1) A conformational change in the recptor that triggers a response
2) The complex passes through the membrane and triggers a direct response

79
Q

What is a key feature of the transmembranous receptor response?

A

Down regulation - decreased availability of drug receptors

80
Q

What is the term for increased availability of drug receptors?

A

Up regulation

81
Q

What is the term for an intracellular chemical that interacts with other intracellular components?

A

Second messenger

82
Q

What products use a transmembranous receptor signaling pathway?

A

1) growth factor

2) insulin

83
Q

What type of receptor employs an intracellular protein which results in the activation of an enzyme which opens an ion channel?

A

G-protein coupled receptor

84
Q

What uses this type of receptor pathway (G-protein coupled)?

A

Alpha and beta adrenergic receptors and some hormones

85
Q

What receptors allow for passing of a lipid-soluble drug into the cytoplasm?

A

Intracellular receptors

86
Q

What acts by way of intracellular receptors?

A

Glucocorticoids and sex hormones

87
Q

What is the term for the special configuration or shape of a drug, most of which have two?

A

Chirality

88
Q

What is the term for a mirror-image spatial arrangement of a drug also called an isomer?

A

Enantiomer

89
Q

What is an example of a d-isomer and l-isomer pair?

A

Dextromethorphan (Robitussin DM) d-isomer and levorphanol (Levo-Dromoran) l-isomer

90
Q

What are drugs that display a degree of affinity for a receptor and stimulate a response?

A

Agonists

91
Q

What are drugs that display a degree of affinity for a receptor and DO NOT stimulate a response?

A

Antagonists

92
Q

What variables affect the disposition of a drug in the body and the reaction the body has to the drug?

A

1) Body type
2) Weight
3) Diet
4) Ethnicity
5) Genetic makeup

ADT Module 1-4 (21 decks)

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