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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
All routes of drug administration NOT involving the GI tract are called _______
Parenteral
26
How are gaseous or small sprayable particles delivered?
Inhalation
27
What type of drug administration is considered the gold standard with regard to bioavailability?
Intravenous
28
What do parenteral administrations avoid?
The first pass effect
29
An implant with drug-releasing mechanisms under the skin is considered what form of administration?
Subcutaneous
30
What type of topical vehicle typically produces the greater effect?
Ointment
31
What form of drug administration is known for a continuous delivery of medication to achieve a constant blood level?
Transdermal
32
What factors affect distribution?
1) Blood flow 2) Solubility 3) Protein binding 4) Obesity
33
What is considered the standard for determining drug dosage and is often adjusted based on weight?
Ideal body weight
34
What is another term for unbound drug?
Free drug
35
What is the term that refers to the attraction between a drug and receptor?
Affinity
36
Acidic drugs commonly bind to what plasma protein?
Albumin
37
Basic drugs commonly bind to what plasma protein?
Alpha-acid glycoprotein (lipoproteins)
38
What is the term for the apparent volume into which a drug distributes in the body at equillibrium?
Volume of distribution (Vd)
39
Drugs that are hydrophillic or highly bound to protein have a ____ Vd
Low
40
Drugs that are lipophyllic and are not highly protein bound have a _____ Vd
High
41
Elimination is a combination of what two principles?
1) Metabolism | 2) Excretion
42
What is the organ that performs most of the body's metabolic functions?
Liver
43
What is the term for the phenomenon by which a drug first passes through the liver for degradation before distribution to the tissues?
First pass effect
44
What is the name of a drug that is transformed from an inactive parent drug into an active metabolite?
Prodrug
45
What are some common prodrugs and their active metabolites?
1) Allopurinol (oxypurinol) 2) Codeine (morphine) 3) Enalapril (enalaprilat) 4) Prednisone (prednisolone) 5) Sulindac (sulindac sulfide)
46
What are the two broadly classified enzyme actions in metabolization?
1) Phase I | 2) Phase II
47
In which enzyme action is the drug changed to form a more polar or water-soluble compound?
Phase I
48
In which enzyme action is a conjugate added to further increase water-solubility and enhance excretion?
Phase II
49
Phase I metabolism is catalyzed by a family of enzymes called?
Cytochrome P450 system (CYP)
50
What are the three CYP families?
1) CYP 1 2) CYP 2 3) CYP 3
51
What are the five CYP isoforms?
1) CYP 1AC 2) CYP 2C 3) CYP 2D6 4) CYP 2E1 5) CYP 3A4
52
What is the term for drugs that stimulate the production of isoforms and increase the amount of enzyme available to metabolize drugs?
Inductors
53
What is the term for drugs that decrease the production of isoforms and decrease the amount of enzyme available to metabolize drugs?
Inhibitors
54
What are the common excretory organs?
1) Kidneys 2) Lower GI tract 3) Lungs 4) Skin
55
What are other structures involved in excretion?
1) Sweat glands 2) Salivary glands 3) Mammary glands
56
What is the primary route of excretion?
Kidney
57
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?
Enterohepatic recirculation
58
What is the term for the time it takes one-half of the drug to be eliminated from the body?
Half-life
59
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?
First-order elimination
60
What is it called when fixed amounts of drugs are eliminated at a constant rate?
Zero-order elimination
61
After how many half-lives of first-order kinetics is the drug basically eliminated?
Three to five
62
What is the term for a constant mean concentration of drug in the body that represents equillibrium?
Steady state
63
What is given when a desired blood concentration of a drug is imperative quickly?
Loading dose
64
What is the term that represents the removal of a drug from the plasma or organ and is the final process in elimination?
Clearance
65
Clearance is _______ related to the elimination half-life
Inversely
66
Through what surrogate substrate is clearance estimated in the kidney?
Creatinine
67
Why is creatinine able to be used for this purpose?
Because it is neither significantly secreted nor absorbed
68
What does creatinine clearance estimate?
GFR
69
What is a normal serum creatinine level?
0.8 - 1.2 mg/dL
70
What is the creatinine clearance level below which renal function is significantly impaired?
50 mL/min
71
In whom do you calculate the creatinine clearance rate when prescribing drugs?
1) Patients over 65 | 2) Those with a serum creatinine > 1.5 mg/dL
72
What is the component of the cell (or an enzyme) to which an endogenous substance binds, initiating a chain of biochemical events?
A receptor
73
What is the term for any chemical, endogenous or exogenous, that interacts with a receptor?
A ligand
74
What are the four primary receptor types usually classified by the effect they produce?
1) Gated ion channel 2) Transmembranous 3) G-protein - coupled 4) Intracellular
75
The function of this receptor is to open or close channels to allow certain ions to pass through
Gated ion channel
76
List some examples of gated ion channels
1) Nicotinic acetylcholine receptor | 2) Gamma-aminobutyric Acid (GABA)
77
This receptor has its ligand-binding domain on the cell's surface and an enzymatic portion inside the cell
Transmembranous
78
What are the two types of change associated with transmembranous receptors?
1) A conformational change in the recptor that triggers a response 2) The complex passes through the membrane and triggers a direct response
79
What is a key feature of the transmembranous receptor response?
Down regulation - decreased availability of drug receptors
80
What is the term for increased availability of drug receptors?
Up regulation
81
What is the term for an intracellular chemical that interacts with other intracellular components?
Second messenger
82
What products use a transmembranous receptor signaling pathway?
1) growth factor | 2) insulin
83
What type of receptor employs an intracellular protein which results in the activation of an enzyme which opens an ion channel?
G-protein coupled receptor
84
What uses this type of receptor pathway (G-protein coupled)?
Alpha and beta adrenergic receptors and some hormones
85
What receptors allow for passing of a lipid-soluble drug into the cytoplasm?
Intracellular receptors
86
What acts by way of intracellular receptors?
Glucocorticoids and sex hormones
87
What is the term for the special configuration or shape of a drug, most of which have two?
Chirality
88
What is the term for a mirror-image spatial arrangement of a drug also called an isomer?
Enantiomer
89
What is an example of a d-isomer and l-isomer pair?
Dextromethorphan (Robitussin DM) d-isomer and levorphanol (Levo-Dromoran) l-isomer
90
What are drugs that display a degree of affinity for a receptor and stimulate a response?
Agonists
91
What are drugs that display a degree of affinity for a receptor and DO NOT stimulate a response?
Antagonists
92
What variables affect the disposition of a drug in the body and the reaction the body has to the drug?
1) Body type 2) Weight 3) Diet 4) Ethnicity 5) Genetic makeup

ADT Module 1-4 (21 decks)

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