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Pharm 1 > Lecture 2 > Flashcards

Lecture 2 Flashcards

0
Q

Formula for determining bioavailability

A

Concentration after gastric absorption
—————————————————
Total dose

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1
Q

The fraction of an administered drug that reaches the systemic circulation is ______.

A

Bioavailability

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2
Q

Drugs given IV have ___% bioavailability.

A

100

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3
Q

First pass hepatic elimination occurs via the _______.

A

Portal circulation

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4
Q

The liver can metabolize or excrete drugs via _____ and thus limiting their bioavailability.

A

Bile

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5
Q

Drugs with a high first-pass metabolism must be given in _____ doses parenterally.

A

Higher

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6
Q

Drugs that are too _____ may be poorly absorbed.

A

Lipophilic

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7
Q

Drugs that are too _____ have difficulty passing through the cell membranes.

A

Hydrophilic

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8
Q

The most commonly administered drugs are either weakly alkaline or weakly acidic due to the ______ characteristics of the drug.

A

Solubility

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9
Q

Why is insulin using given SQ and not PO?

A

It is chemically unstable in the GI tract

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10
Q

What 3 factors affect bioavailability?

A

Solubility characteristics of the drug
Chemical stability in the GI tract
Drug formulation

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11
Q

Rectal has a ____ first past effect than oral.

A

Smaller

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12
Q

Transdermal route usually has very ____ absorption, but it is used due to _____.

A

Slow

Lack of first-pass effect

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13
Q

Drugs that are mostly confined to the intravascular space (such as gentamicin or mannitol) have a _____ volume of distribution.

A

Smaller

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14
Q

After absorption, drugs must be ______ throughout the body.

A

Distributed

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15
Q

When there is less _____ in the blood to bind with, there is more free drug in the serum to bind to the receptor and become active.

A

Protein

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16
Q

Drugs that have an ______ appear to have a large volume of distribution.

A

Extensive distribution outside the plasma

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17
Q

Distribution is usually accomplished through _______.

A

Circulation via the blood stream.

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18
Q

What 3 things are distribution mostly dependent on?

A

Blood flow
Fat/water solubility
Protein binding

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19
Q

90 percent of steady state drug concentration is achieved in _____t1/2.

A

3.3

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20
Q

_____ occurs when a portion of the drug is bound to the proteins in the blood and therefore is not able to be free to bind to an active site and produce an effect.

A

Protein binding

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21
Q

Protein binding occurs when a portion of the drug is bound to the proteins in the blood and therefore is not able to _______________.

A

Be free to bind to an active site and produce an effect.

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22
Q

50 percent of steady state drug concentration is achieved in _____t1/2.

A

1

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23
Q

Only the _______ is available to bind with the receptor site.

A

Free drug not bound to the protein

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24
Q

Drugs that have extensive distribution outside the plasma (such as digoxin, diltiazem, labetalol, meperidine, or nortriptyline) appear to have a _____ volume of distribution.

A

Large

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25
Q

Low protein in plasma = _______ free drug

A

Greater

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26
Q

What happens if a second Drug B were in the blood stream in addition to protein-bound Drug A?

A

Drug B would compete and displace Drug A causing an increase in availability and effect of Drug A

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27
Q

The major determinant of hemp filtration is typically the amount of ______.

A

Protein binding

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28
Q

_______ are not well correlated with molecular weight.

A

Sieving coefficients

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29
Q

What are the 5 main ways your patients will eliminate drugs?

A 
Urine
Bile
Hepatic metabolism
Lung/oxygenator expiration 
Artificial filtration
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30
Q

______ is the time required for the concentration or amount of drug in the body to be reduced by one-half.

A

Half-life

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31
Q

_____ percent of steady state drug concentration is achieved in t1/2.

A

50

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32
Q

______ can be thought of as the volume of fluid that is required to contain an entire drug in the body at the same concentration measured in a given compartment.

A

Volume of distribution

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33
Q

Loading doses are particularly important with drugs that have _____.

A

Long half-lives

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34
Q

The half-life assumption assumes _______.

A

First order kinetics

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35
Q

First Order Kinetics means a ______ of the drug is metabolized per unit time.

A

Constant proportion

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36
Q

_____ percent of steady state drug concentration is achieved in 3.3t1/2.

A

90

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37
Q

How do you calculate clearance?

A

Clearance = (.693 x Vd) / (T1/2)

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38
Q

Some drugs are administered in such high doasages that they are eliminated by a constant amount over time because they’ve overwhelmed clearance mechanisms are called ______.

A

Zero-order kinetics

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39
Q

Repeated dosing of a drug won’t allow for the drug to accumulate in the body unless the dosing interval is ________.

A

Less than 4T1/2

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40
Q

________ of drugs into more polar molecules makes them less protein-bound at physiological pH and thus more readily filtered.

A

Biotransformation

41
Q

Accumulation of a drug is necessary in order for the drug to reach a _____ in the plasma.

A

Steady state

42
Q

Induced P450 enzymes metabolize drugs ______.

A

Faster

43
Q

What directions do half-lives work?

A

Reaching a steady state

Elimination

44
Q

What factors affect clearance?

A

Volume distribution
Half life
Kidney and liver function

45
Q

Drugs that are mostly ________ space have a smaller volume of distribution.

A

Confined to intravascular space

46
Q

What factors affect accumulation?

A

Method and frequency of dosing

Bioavailability

47
Q

____ is the drug concentration that will produce the desired therapeutic effect?

A

Target concentration

48
Q

Inhibited P450 enzymes metabolize drugs _____.

A

Slower

49
Q

The liver(and the GI tract to a much lesser degree) extensively by a transform struggle through its _____. complexes

A

Cytochrome P450

50
Q

Loading dose calculation

A

(Vd X target plasma concentration) / bioavailability

51
Q

What can be done if there is not enough time to wait for multiple half-lived to pass to approach a steady-steady of drug accumulation?

A

You can give a bigger loading dose

52
Q

______ P450 enzymes metabolize drugs slower.

A

Inhibited

53
Q

_________ can turn non-biologically active drugs into active drugs or convert drugs into even more active forms.

A

Biotransformation

54
Q

Formula for volume of distribution (Vd)

A

D/C^0

                Amount of drug in body (dose) —————————————————————————— Concentration of drug in given compartment at time zero
55
Q

Cytochrome P450 Complexes are a large family of _____ with the enormous genetic variation.

A

Heme-containing enzymes

56
Q

______ are generally the same doses given at regular intervals.

A

Maintenance doses

57
Q

Maintenance dose formulas

Dosing rate X dosing interval

A

(Clearance X target plasma concentration) / bioavailability

58
Q

_____ is the rate of drug metabolism and elimination is directly proportional to the concentration of free drug.

A

First order kinetics

59
Q

______ P450 enzymes metabolize drugs faster.

A

Induced

60
Q

________ administration of a drug results in oscillations in plasma concentrations that are influenced by both by both the rate of drug absorption and elimination.

A

Repeated fixed dose

61
Q

Phase ___ Biotransformation conjugates the drug with another chemical.

A

2

62
Q

A _____ dose given orally results in a single peak in plasma concentration followed by a continuous decline in drug level.

A

Single fixed dose

63
Q

The plasma concentrations during oral therapy fluctuate around the steady-state levels attained with ______.

A

Intravenous therapy

64
Q

When dosages are doubled, halved, are stopped during steady-state administration, the time required to achieve a new steady-state level is ____________________.

A

Independent of the route administration

65
Q

Where does the majority of biotransformation occur?

A

Liver

66
Q

Some drugs/chemicals make the Cytochrome P450 system more active by increasing the rate of synthesis are decreasing the rate of the degradation, which is called ______.

A

Induction

67
Q

______ are a large family of heme-containing enzymes with the enormous genetic variation.

A

Cytochrome P450 Complexes

68
Q

Noncompetitive antagonist reduce agonist _____.

A

Efficacy (decrease Emax)

69
Q

________ can shorten the drugs biological half-life.

A

Biotransformation

70
Q

Phase ____ Biotransformation metabolizes the drug into a more polar form.

A

1

71
Q

What effect does biotransformation of a drug into a polar molecule?

A

Can greatly decrease activity and half-life

72
Q

Many lipophilic drugs are tightly bound to protein and thus unavailable for excretion by the _______.

A

Kidneys

73
Q

The drug receptor complex initiate alterations in biochemical and or molecular activity of a cell by a process called _____.

A

Signal transduction

74
Q

The phenomenon of desensitizing is called _______.

A

Tachyphylaxis

75
Q

During the recovery phase, unresponsive receptors are said to be ____.

A

Refactory

76
Q

____ of receptors can make the cells more sensitive to agonist and/or more resistant to the effect of the antagonist.

A

Up-regulation

77
Q

______ is a measure of the amount of drug necessary to produce an effect of a given magnitude.

A

Potency

78
Q

______ is the magnitude of response I drug causes when it interacts with the receptor.

A

Efficacy

79
Q

What does efficacy depend on?

A

The number of drug-receptor complexes formed

Intrinsic activity of the drug

80
Q

______ antagonist reduce agonist efficacy (____ Emax).

A

Noncompetitive

Decrease

81
Q

_______ is the drugs ability to activate the receptor and cause a cellular response.

A

Intrinsic activity

82
Q

What does maximum efficacy assume?

A

That all receptors are occupied by the drug, and no increase in response is observed if a higher concentration of drug is obtained.

83
Q

The ______ of a drug determines its ability to fully or partially activate the receptors.

A

Intrinsic activity

84
Q

And agonist binds to a receptor it and produces a _____ based on the concentration of the agonist and the fraction activated receptors.

A

Biological response

85
Q

What is the value of the intrinsic activity for partial agonist?

A

Greater than zero but less than one

86
Q

This type of at antagonist binds to a site other than the agonist binding site and prevents the receptor for being activated by its agonist.

A

Allosteric

87
Q

_____ have an intrinsic activity less than zero, reverse the activity of receptors, and exert the opposite pharmacological effect of agonists.

A

Inverse agonist

88
Q

Competitive antagonist reduce agonist ______.

A

Potency (increase EC50)

89
Q

Which antagonist are considered non-competitive?

A

Irreversible

Allosteric

90
Q

_____ bind to a receptor with high affinity but possess zero intrinsic activity.

A

Antagonist

91
Q

An antagonist has no affect in the absence of an _____.

A

Agonist

92
Q

If both the antagonist in the agonist bind to the same site of the receptor in a reversible manner, they are said to be _____.

A

Competitive

93
Q

What does a competitive antagonist do?

A

Prevents the agonist from binding to its receptor which leaves the receptor in its in active state.

94
Q

_____ antagonist bind covalently to the active site of the receptor, thereby reducing the number of receptors available to the agonist.

A

Irreversible

95
Q

And Allosteric antagonist causes _____ shift of the Emax, with _____ shift of the EC50 values of agonist.

A

Downward

No

96
Q

______ antagonist reduce agonist potency (____ EC50).

A

Competitive

Increase

97
Q

An Irreversible antagonist causes _____ shift of the Emax, with _____ shift of the EC50 values (unless spare receptors are present).

A

Downward

No

98
Q

This antagonist acts at a completely separate receptor, initiating effects that are functionally opposite those of the agonist

A

Functional antagonist

99
Q

What does the larger therapeutic index mean?

A

There is a wide margin between doses that are effective in doses that are toxic.

100
Q

Agents with low therapeutic index, which the dose is critically important, are those drugs for which ____ critically alters the therapeutic effects.

A

Bioavailability

Pharm 1 (6 decks)

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