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Pharmacology > 9 Block > Flashcards

9 Block Flashcards

1
Q

Pharmacodynamics is

A

The actions of a drug on the body

Looks at receptor interactions

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2
Q

Pharmacokinetics is

A

The action the body has on a drug

Looks at absorption, distribution, metabolism, excretion

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3
Q

Therapeutic Index formula

A

TD50/ED50

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4
Q

Which is safest a high or low Therapeutic Index (TI)

A

High

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5
Q

What are the categories for the “old” pregnancy categories

A 
A
B
C
D
X
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6
Q

Pregnancy category A is

A

Safe for pregancy

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7
Q

Pregnancy category B is

A

Safe (there a lot in this category)

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8
Q

Pregnancy Category C is

A

There isn’t data on the effects in pregnancy

“Unknown”

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9
Q

Pregnancy category D is

A

Shouldn’t use unless necessary and the benefits outweigh the risk

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10
Q

Pregancy category X

A

Do not take

Can kill baby

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11
Q

An agonist is

A

Drug that binds to the same site as the ligand and makes same signal

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12
Q

An allosteric agonist is

A

Ligand that binds to a DIFFERENT site with no effect itself

Enhances the response

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13
Q

Partial agonist is

A

A drug that binds to same receptor and produces a lower response
Inhibit agonist binding

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14
Q

An antagonist is

A

Drug that binds to same receptor and inhibits the action of agonist
Has no effect itself

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15
Q

A competitive antagonist is

A

A drug that binds to same receptor and inhibits action of agonist
Can be overcome by increasing agonist concentration

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16
Q

A non-competitive antagonist is

A

A drug that binds to the same or different receptor and prevents agonist from binding at any concentration

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17
Q

As dose increases what happens to the repsonse?

A

It increases proportionally UNTIL the max response is achieved

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18
Q

Potency is

A

The concentration required to produce 50% of that drugs max repsonse (EC50)

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19
Q

Efficacy is

A

The upper limit of the dose-response relation

Max effect

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20
Q

Do we care more about efficacy or potency?

A

Efficacy, we care about the effect a drug has

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21
Q

What is the pharmacological mechanism of antagonism

A

2 drugs

1 receptor

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22
Q

What is chemical antagonism

A

2 drugs

0 receptor

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23
Q

Physiological antagonism is

A

2 drugs
2 receptors
2 receptor oppose each other

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24
Q

Absorption is

A

Movement of drug from site of administration to blood

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25
Q

Distribution is

A

The movement of drug from blood to rest of body

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26
Q

Metabolism of a drug is

A

Drug is converted to a form tat is easily eliminated

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27
Q

Elimination is

A

Removal of drug from body

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28
Q

What is the most common route of administration

A

Oral

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29
Q 
Oral route of administration 
Speed: 
Safety:
Cost:
Absorption:
A

Speed: slow
Safety: safest
Cost: cheap
Absorption: in intestines

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30
Q

Parenteral route does what

A

Bypasses the GI tract

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31
Q

Buccal route of admin

A

Between cheek and gums

Direct absorption

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32
Q

Sublingual RofA

A 
Under the tongue 
Very fast (mouth is very vascular)
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33
Q

Rectal R of A

A

Large amounts of drug can be given

Good if pt can’t keep food/liquids down

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34
Q

IM R of A

A

Faster absorption

Large volume

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35
Q

SubQ R of A

A

Slower absorption

Large doses

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36
Q

IV R of A

A

Does not involve absorption
Goes directly to blood
Most dangerous

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37
Q

Inhalation R of A

A

Fast

Rapid absorption

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38
Q

What is the fastest drug form for absorption

A

Inhalation

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39
Q

Topical drugs are applied to the skin and effect ______

A

Locally

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40
Q

Transdermal drugs are applied to the skin and have a ____ effect

A

Systemic

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41
Q

What is passive diffusion

A

Most common
H>L
No carrier (cannot be saturated)
No energy

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42
Q

Facilitated diffusion

A

Driven by gradient
Carrier proteins (can be saturated)
No energy

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43
Q

Active transport

A

Against gradient
Carrier protein
Saturable
Needs ATP

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44
Q

Most drugs are one of these 2 things

A

A weak acid or base

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45
Q

T/F drugs pass more readily through membranes if they are uncharged?

A

T

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46
Q

You have HA <>H+ + A- and BH+<>B + H+
Which will easily pass through a membrane
Which will not?

A

HA and B

A- and BH+

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47
Q

Henderson- Hasselbalch equation

A

PH-pKa

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48
Q

If Henderson-Hasselbalch is - then

A

PH is lower than pKa, acidic

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49
Q

If Henderson-Hasselbalch is + then

A

PH is higher than pKa

Basic environment

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50
Q

Is the nonionized or ionized form of a drug water soluble?

A

Ionized form

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51
Q

Is the non-ionized or ionized form of a drug lipid soluble?

A

Non-ionized

52
Q

Page 18

A

Hella lot of notes

53
Q

If you take a weak acid drug orally where will it be better absorbed?

A

In the stomach because there is a lower pH

54
Q

If you take a weak base orally it is better absorbed where?

A

Small intestines

Because there is a higher pH

55
Q

If you put a drug in a like environment (acid in acid) (base in base) it will ____

A

Stay

56
Q

If you put a drug its opposite environment (acid in base) it will ____

A

Go out

57
Q

T/F the charged form of a drug is more easily removed from the body

A

True

58
Q

T/F you can change the pH of urine to help keep or eliminate a drug from the body

A

True

59
Q

If you want to get rid of a weak acid what should you do the urine

A

Make it basic

60
Q

If you want to get rid of a weak base what should you do to the urine

A

Make it more acidic

61
Q

If you have a weak acid overdose what should you do

A

Give them bicarb, makes urine more basic

62
Q

What should you do in a weak base overdose

A

Give Nh4CL, makes urine more acidic

63
Q

What are some factors that affect drug absorption

A

Blood flow to the absorption site
Surface area for absorption
Contact time at absorption site

64
Q

Bioavailability is

A

The fraction of the administered dose that makes it to the blood

65
Q

What are some factors that affect bioavailability

A

First pass metabolism
Solubility
Chemical stability

66
Q

What is lag time

A

Time from administration to appearance in blood

67
Q

What is the onset of activity

A

Time from administration to reaching the minimum effective concentration

68
Q

What is the duration of action

A

The amount of time drug concentration stays above MEC

69
Q

Why do most drugs bind to plasma proteins

A

They need a carrier protein

70
Q

What is the volume of distribution?

A

Volume of drug that the drug is disseminated in

71
Q

If you have a low Volume of distribution where is the drug?

A

In the blood

72
Q

If you have a high volume of distribution where is the drug?

A

In the tissues

73
Q

What does a large Vd tell you?

A

Most of the drug is in the extraplasmic space and it is not being delivered to the organs of elimination

74
Q

There are drug reservoirs

A

Know this

75
Q

T/F the placenta is a barrier to drugs

A

False

76
Q

Look at bottom of page 24.

A

The different metabolisms of drugs. I dont feel like typing it all out

77
Q

What are Phase 1 metabolisms

A

Accomplished by enzymes in the Smooth ER

78
Q

What are phase 2 metabolisms

A

Conjugate reactions that use transferase enzyme

They increase the size of the drug

79
Q

What metabolism phase is missing in neonates

A

Phase 2

80
Q

What is the most important site of metabolism

A

The liver

81
Q

Where do phase 1 metabolisms occur

A

Smooth ER

82
Q

Where do phase 2 metabolisms occur

A

Cytoplasm

83
Q

What are the most active drug metabolism cytokines

A

CYP2C
CYP2D
CYP3A

84
Q

What cytokine does metabolism of 50% of all drugs

A

CYP3A

85
Q

What are the phase 1 reactions

A

Oxidations (CYP dependent and independent)

Reduction
Hydrolysis

86
Q

What are CYP inducers

A

They increase the expression of CYP450 enzymes

Which reduces teh plasma level and effectiveness of the drug

87
Q

What are some examples of CYP inducers

A

Benzopyrenes in cigaretter smoke

Chronic ethanol

Barbiturates
Carbamazepine

88
Q

What are CYP inhibitors

A

Decrease the expression of p450 enzymes
Increase the plasma level
Increase risk of toxicity

89
Q

What are some examples of CYP inhibitors

A

Cimetidine
Erythromycin
Grapefruit juice

90
Q

T/F CYP inducers and inhibitors work after 1 exposure

A

False

You need to have regular daily exposure for an extended period of time

91
Q

What are the most important Phase 2 reactions

A
  1. Glucuronidation
  2. Sulfation
  3. Acetylation
92
Q

What is the most common Phase 2 reaction

A

Glucuronidation

93
Q

What enzyme is used in glucuronidation

A

Glucuronosyl transferase

94
Q

What enzyme is used in sulfation

A

Sulfotransferase

95
Q

What enzyme is used in acetylation

A

Acetyltransferase

96
Q

What happens in slow acetylators

A

They are slow metabolizers
Long half life
Can get Lupus

97
Q

What happens in fast acetylators

A

Fast metabolism
Have a lot of drug
Short half life

98
Q

T/F elimination and excretion are the same thing

A

FALSE

99
Q

What occurs in glomerular filtration

A

Only free unbound drug is filtered

100
Q

What occurs in the PCT

A

Secretion
OAT and OBTs
There is competition between drugs for carriers

101
Q

What happens in DCT

A

Reabsorption

102
Q

Weak acid overdose, give:

A

Bicarbonate

103
Q

Weak base OD, give:

A

Ammonium chloride

104
Q

There are many modes of excretion

A

Know this

105
Q

First order kinetics

A

Constant fraction
Half life is constant
Non saturating kinetics

106
Q

Zero order kinetics

A

Constant amount
Half life is not constant
Saturating kinetics

107
Q

What are the zero order drugs

A

High doses of aspirin
Ethanol
Phenytoin

108
Q

How is half life determined

A

Volume of distribution and CLearance

109
Q

Maintenance dose is used for what conditions

A

Chronic

110
Q

Loading doses are used for what conditions

A

Acute

111
Q

How do you pick a drug dose

A
  1. Pick target plasma level
  2. Compute dose
  3. Measure plasma level
  4. Adjust dose
112
Q

What does a maintenance dose do

A

Maintain the steady state or target concentration of a drug

113
Q

What is a loading dose

A

Given in one or a series of doses to achieve a target concentration rapidly

114
Q

What is the loading dose equation?

A

LD: CSS x d/F

115
Q

If the time to reach steady state is long, should you use a LD or a MD?

A

LD

116
Q

What is a steady state?

A

The goal concentration you want to reach with a drug.

117
Q

The time that it takes to reach steady state for a drug eliminated by first order kinetics is a function that drugs what?

A

Half life

118
Q

What is the clinical steady state

A

4-5 half lives

119
Q

What is the mathematical steady state

A

10 half lives

120
Q

T/F the half life of a drug is unaffected by the amount of drug given either by constant infusion, single injections, or orally, as long as the drug is eliminate by 1st order kinetics

A

True

121
Q

Are there oscillations around steady state with continuous infusion?

A

No

122
Q

Are there oscillations around steady state with single or multiple doses

A

Yes

123
Q

The peaks of a half life diagram should always be above or below what?

A

Below Minimum toxic concentration

124
Q

What should troughs of half life diagram always be above or below

A

Above MEC

125
Q

What makes up the therapeutic window?

A

The MTC and MEC

126
Q

What is the normal creatinine clearance

A

100 mL/min

127
Q

What is the renal CL equation

A

CD: average dose x (patients Cre CL/100 mL/min)

Pharmacology (4 decks)

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