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Pharmacology I > Introduction to Pharmacology > Flashcards

Introduction to Pharmacology Flashcards

1
Q

[…] is what the BODY does to the drug

A

pharmacokinetics

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2
Q

[…] is what the DRUG does to the body

A

pharmacodynamics

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3
Q

What are the 4 parts of pharmacokinetics?

A

Absorption, distribution, metabolism, elimination

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4
Q

What are the 2 parts of pharmacodynamics?

A

Efficacy and Toxicity

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5
Q

[…] is the process by which a drug moves from site of administration to bloodstream

A

absorption

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6
Q

Absorption depends on physical characteristics of the drug such as what?

A

solubility, pKA, binders, formulation

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7
Q

[…] is the relative amount of drug that reaches systemic circulation

A

bioavailability

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8
Q

What is the bioavailability value for IV medications? Why

A

1, bypasses liver upon administration

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9
Q

What are examples of ways drugs can be administered?

A

Oral, sublingual, rectal, transdermal, subcutaneous, IM, IV, Intrathecal, Epidural, Inhalational

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10
Q

The route a drug is administered affects its […]

A

absorption

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11
Q

[…] is a phenomenon of drug metabolism whereby concentration of the drug is greatly reduced before it reaches systemic circulation

A

first-pass metabolism

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12
Q

First-pass metabolism can be attributed to the […] and […] clearance

A

liver , gut wall

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13
Q

Which route of administration can bypass the LIVER on the first pass?

A

IV

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14
Q

Which drug is more readily absorbed: non-ionized or ionized?

A

Non-ionized since they are uncharged

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15
Q

What type of drugs will acidic environment favor during absorption? Example?

A

Acidic drugs, Stomach

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16
Q

What type of drugs will alkaline environments favor during absorption? Example?

A

Basic drugs, intestines

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17
Q

Where are most oral drugs absorbed? Why?

A

Intestine, surface area and prolonged transit duration

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18
Q

Why would drugs absorbed from the stomach or intestine be reduced?

A

Venous drainage goes to liver first (first-pass)

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19
Q

Why are sublingual and buccal administration unique?

A

Bypass 1st pass metabolism

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20
Q

What does parenteral mean? Examples?

A

Outside of intestine (SQ, IM, IV)

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21
Q

[…] administration bypasses process of absorption

A

IV

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22
Q

[…] occurs after absorption when the circulation moves the drug throughout the body

A

Distribution

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23
Q

[…] defines the group of highly perfused organs

A

Vessel Rich Group (VRG)

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24
Q

What organs are in the Vessel Rich Group? (5)

A

Brain, Heart, Kidneys, Liver, Endocrine Glands

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25
Q

What percentage of cardiac output do vessel rich groups receive?

A

75%

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26
Q

What type of drugs will quickly equilibrate into CNS tissue?

A

Lipophilic

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27
Q

[…] will reach equilibrium quicker than other less perfused tissues

A

Vessel Rich Groups (VRG)

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28
Q

Fat & Skin can absorb […] drugs which results in […] reservoir of drug following long infusions

A

lipophilic, larger

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29
Q

What is the mass action law?

A

When plasma concentration exceeds tissue concentration, drug moves from plasma into tissue

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30
Q

What is redistribution?

A

Drug moves back due to plasma concentraiton being less than tissue concentration

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31
Q

What does drug concentration in an organ depend on?

A

Blood flow to organ, Solubility in organ vs solubility in blood

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32
Q

What can molecules in the blood be bound to when they aren’t free?

A

Plasma proteins and lipids

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33
Q

What are 2 examples of plasma binding proteins? What can cause these to be diminished?

A

Albumin and Alpha Acid Glycoprotein (AAG); Kidney disease, Liver disease, CHF

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34
Q

Which induction agent is in lipid emulsion and acts as its own binding molecule?

A

Propofol

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35
Q

What molecules readily cross between blood and organs?

A

Lipophilic

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36
Q

What molecules can pass in SMALL quantities?

A

Charged

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37
Q

Blood Brain Barrier has limited penetration by […] drugs due to pericapillary glial cells and endothelial cell tight junctions

A

ionized

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38
Q

Drugs that are able to cross BBB are readily taken up by what?

A

Body fat

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39
Q

When a drug is highly bound on tissues and unbound in plasma, where is it more likely to transfer to?

A

Tissues

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40
Q

When a drug is unbound in the tissue, it is more likely to transfer to […]

A

plasma

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41
Q

What is albumins capacity and affinity like?

A

High capacity, low affinity

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42
Q

What type of drugs does albumin bind?

A

Weak acids and some bases

43
Q

What is Alpha-1 Acid Glycoprotein capacity and affinity like?

A

High affinity, low capacity

44
Q

What type of drugs are bound to alpha-1 glycoprotein?

A

Weak bases

45
Q

What type of drugs are bound to lipoproteins?

A

Lipophilic drugs

46
Q

When an IV bolus is given what will occur in terms of distribution?

A

Distribution from plasma to tissues (plasma concentration declines) and equilibrium occurs

47
Q

When tissue concentration exceeds plasma concentration what will occur?

A

Redistribution

48
Q

When we give prolonged infusions of a drug, what will be affected when the infusion is discontinued?

A

Redistribution (pro-long drug action)

49
Q

[…] is the time required for a 50% decrease of drug plasma concentration following a steady state infusion

A

context sensitive half-time (context refers to time of infusion)

50
Q

[…] is the apparent volume into which a drug has distrubted

A

Volume of distribution (Vd)

51
Q

Volume of Distribution (Vd) equation:

A

Bolus Dose / [Blood Concentration] at certain time

52
Q

If a drug has a low Vd, what does that mean?

A

Hydrophilic and largely in intravascular space

53
Q

If a drug has a high Vd, what does that mean?

A

Lipophilic and easily cross and distribute throughout tissues

54
Q

Metabolism can also be referred as […]

A

biotransformation

55
Q

[…] is the chemical process by which a drug molecule is altered in the body

A

Metabolism/Biotransformation

56
Q

What organ is a major player in the metabolism process?

A

Liver

57
Q

Where do esters undergo hydrolysis?

A

Plasma or tissue

58
Q

Most products of metabolism are inactive and […] making it easy to be excreted by the […]

A

water soluble ; kidneys

59
Q

How many phases of metabolism are there?

A

2

60
Q

[…] of metabolism is the breakdown of the initial parent compound into more polar metabolites via oxidation, reduction, or hydrolysis

A

Phase 1

61
Q

What enzyme catalyzes most phase 1 metabolism reactions?

A

Cytochrome P-450 (CYP 450)

62
Q

What can cause CYP activity to increase?

A

Constant drug exposure

63
Q

What can inhibit CYP activity?

A

Drugs competing for same CYP subtype

64
Q

[…] metabolism reactions couple or conjugate parent or metabolite with endogenous subtrate to form water soluble product eliminated via stool or urine

A

Phase II

65
Q

Can phase I products be excreted without undergoing phase II reaction?

A

Yes

66
Q

Can phase II reactions occur without a phase I reaction?

A

Yes

67
Q

Give an example of a metabolism polymorphism that exists:

A

pseudocholinesterase deficiency

68
Q

[…] is the volume of blood or plasma cleared of drug per unit of time

A

Hepatic clearance

69
Q

What is the fraction of drug removed by the liver called?

A

Extraction ratio

70
Q

What is the equation for hepatic clearnace?

A

Hepatic Clearance = Liver Blood Flow x Extraction Ratio

71
Q

What does a high extraction ratio mean?

A

Depends on CO - “Flow limited”

72
Q

What does a low extraction ratio mean?

A

Capacity limited - can only handle a set amount at a time

73
Q

What organ removes some drugs and many drug metabolites?

A

Kidney

74
Q

[…] is the rate of elimination of a drug from the body by kidney excretion

A

Renal clearance

75
Q

What is the renal clearance equation?

A

Renal Clearance = Renal Blood Flow x Renal Extraction Ratio

76
Q

[…] portion is reabsorbed in the renal tubules and […] portion is excreted in the urine. This is dependent upon […]

A

Nonionized, Ionized, pH

77
Q

Why do patients with decreased renal function need altered drug dosing?

A

Avoid accumulation of parent compounds and metabolite

78
Q

Drugs can sometimes be excreted from liver to intestine via […]

A

biliary system

79
Q

[…] is the process in which metabolites excreted in bile are subsequently reversed and absorbed back into the parent drug

A

Enterohepatic recirculation

80
Q

[…] is when a fixed percentage of an existing drug is removed per unit of time

A

First-order kinetics

81
Q

In first order kinetics, the […] removed depends on serum levels but the […] removed is independent of serum levels

A

amount ; fraction

82
Q

[…] describes a fixed amount of drug removed per unit of time

A

zero-order kinetics

83
Q

[…] is the time required for serum concetration to decrease by 50%

A

half-life

84
Q

Half life formula

A

Half life = ln2/K

85
Q

[…] is the time required for the drug concentration in the body to fall by 50%

A

elimination half-life

86
Q

What does the 2-compartment model consist of?

A

Central compartment (plasma + VRG) and peripheral compartment

87
Q

What is the alpha phase of the two-compartment model?

A

Quick decline - distribution phase

88
Q

What is the beta phase of the two-compartment model?

A

Slower decline - elimination phase

89
Q

What does pharmodynaics involve concepts of?

A

Potency, efficacy, therpaeutic window

90
Q

Exposure response relationships shows that as the body is exosed to increasing amount of drug the response to the drug can […] up to a maximum value

A

increase

91
Q

[…] dose required to produce a specific effect in 50% of the population

A

ED50 (effective dose)

92
Q

[…] dose required to cause death or toxicity in 50% of the population

A

LD50 (lethal dose)

93
Q

[…] is a safety measure or how much wiggle room you have before your desired outcome starts becoming harmful to the patient

A

Therapeutic index

94
Q

Therapeutic index equation

A

LD50/ED50

95
Q

[…] is the amount of drug needed to produce a given effect

A

potency

96
Q

[…] refers to the relative ability of a drug-receptor complex to produce a maximum fuctional response

A

efficacy

97
Q

[…] bind to a receptor and produce an effect

A

agonists

98
Q

[…] binds to receptor but produces a lower maximal effect than a full agonist

A

partial agonist

99
Q

[…] is diminished response to a drug due to chronic exposure

A

tolerance

100
Q

[…] is an acute tolerance after only a few doses

A

tachyphylaxis

101
Q

[…] bind to receptor without producing an effect

A

antagonists

102
Q

[…] bind reversibly to the same binding site as the agonist

A

competitive antagonists

103
Q

[…] bind irreversibly or at a separate site on the same receptor

A

noncompetitive antagonists

Pharmacology I (3 decks)

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