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Flashcards in 9 Block Deck (127):
1

Pharmacodynamics is

The actions of a drug on the body
Looks at receptor interactions

2

Pharmacokinetics is

The action the body has on a drug

Looks at absorption, distribution, metabolism, excretion

3

Therapeutic Index formula

TD50/ED50

4

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

High

5

What are the categories for the "old" pregnancy categories

A
B
C
D
X

6

Pregnancy category A is

Safe for pregancy

7

Pregnancy category B is

Safe (there a lot in this category)

8

Pregnancy Category C is

There isn't data on the effects in pregnancy
"Unknown"

9

Pregnancy category D is

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

10

Pregancy category X

Do not take
Can kill baby

11

An agonist is

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

12

An allosteric agonist is

Ligand that binds to a DIFFERENT site with no effect itself
Enhances the response

13

Partial agonist is

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

14

An antagonist is

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

15

A competitive antagonist is

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

16

A non-competitive antagonist is

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

17

As dose increases what happens to the repsonse?

It increases proportionally UNTIL the max response is achieved

18

Potency is

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

19

Efficacy is

The upper limit of the dose-response relation
(Max effect)

20

Do we care more about efficacy or potency?

Efficacy, we care about the effect a drug has

21

What is the pharmacological mechanism of antagonism

2 drugs
1 receptor

22

What is chemical antagonism

2 drugs
0 receptor

23

Physiological antagonism is

2 drugs
2 receptors
2 receptor oppose each other

24

Absorption is

Movement of drug from site of administration to blood

25

Distribution is

The movement of drug from blood to rest of body

26

Metabolism of a drug is

Drug is converted to a form tat is easily eliminated

27

Elimination is

Removal of drug from body

28

What is the most common route of administration

Oral

29

Oral route of administration
Speed:
Safety:
Cost:
Absorption:

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

30

Parenteral route does what

Bypasses the GI tract

31

Buccal route of admin

Between cheek and gums
Direct absorption

32

Sublingual RofA

Under the tongue
Very fast (mouth is very vascular)

33

Rectal R of A

Large amounts of drug can be given
Good if pt can't keep food/liquids down

34

IM R of A

Faster absorption
Large volume

35

SubQ R of A

Slower absorption
Large doses

36

IV R of A

Does not involve absorption
Goes directly to blood
Most dangerous

37

Inhalation R of A

Fast
Rapid absorption

38

What is the fastest drug form for absorption

Inhalation

39

Topical drugs are applied to the skin and effect ______

Locally

40

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

Systemic

41

What is passive diffusion

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

42

Facilitated diffusion

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

43

Active transport

Against gradient
Carrier protein
Saturable
Needs ATP

44

Most drugs are one of these 2 things

A weak acid or base

45

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

T

46

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

HA and B

A- and BH+

47

Henderson- Hasselbalch equation

PH-pKa

48

If Henderson-Hasselbalch is - then

PH is lower than pKa, acidic

49

If Henderson-Hasselbalch is + then

PH is higher than pKa
Basic environment

50

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

Ionized form

51

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

Non-ionized

52

Page 18

Hella lot of notes

53

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

In the stomach because there is a lower pH

54

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

Small intestines
Because there is a higher pH

55

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

Stay

56

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

Go out

57

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

True

58

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

True

59

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

Make it basic

60

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

Make it more acidic

61

If you have a weak acid overdose what should you do

Give them bicarb, makes urine more basic

62

What should you do in a weak base overdose

Give Nh4CL, makes urine more acidic

63

What are some factors that affect drug absorption

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

64

Bioavailability is

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

65

What are some factors that affect bioavailability

First pass metabolism
Solubility
Chemical stability

66

What is lag time

Time from administration to appearance in blood

67

What is the onset of activity

Time from administration to reaching the minimum effective concentration

68

What is the duration of action

The amount of time drug concentration stays above MEC

69

Why do most drugs bind to plasma proteins

They need a carrier protein

70

What is the volume of distribution?

Volume of drug that the drug is disseminated in

71

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

In the blood

72

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

In the tissues

73

What does a large Vd tell you?

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

74

There are drug reservoirs

Know this

75

T/F the placenta is a barrier to drugs

False

76

Look at bottom of page 24.

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

77

What are Phase 1 metabolisms

Accomplished by enzymes in the Smooth ER

78

What are phase 2 metabolisms

Conjugate reactions that use transferase enzyme
They increase the size of the drug

79

What metabolism phase is missing in neonates

Phase 2

80

What is the most important site of metabolism

The liver

81

Where do phase 1 metabolisms occur

Smooth ER

82

Where do phase 2 metabolisms occur

Cytoplasm

83

What are the most active drug metabolism cytokines

CYP2C
CYP2D
CYP3A

84

What cytokine does metabolism of 50% of all drugs

CYP3A

85

What are the phase 1 reactions

Oxidations (CYP dependent and independent)

Reduction
Hydrolysis

86

What are CYP inducers

They increase the expression of CYP450 enzymes
Which reduces teh plasma level and effectiveness of the drug

87

What are some examples of CYP inducers

Benzopyrenes in cigaretter smoke

Chronic ethanol

Barbiturates
Carbamazepine

88

What are CYP inhibitors

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

89

What are some examples of CYP inhibitors

Cimetidine
Erythromycin
Grapefruit juice

90

T/F CYP inducers and inhibitors work after 1 exposure

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

91

What are the most important Phase 2 reactions

1. Glucuronidation
2. Sulfation
3. Acetylation

92

What is the most common Phase 2 reaction

Glucuronidation

93

What enzyme is used in glucuronidation

Glucuronosyl transferase

94

What enzyme is used in sulfation

Sulfotransferase

95

What enzyme is used in acetylation

Acetyltransferase

96

What happens in slow acetylators

They are slow metabolizers
Long half life
Can get Lupus

97

What happens in fast acetylators

Fast metabolism
Have a lot of drug
Short half life

98

T/F elimination and excretion are the same thing

FALSE

99

What occurs in glomerular filtration

Only free unbound drug is filtered

100

What occurs in the PCT

Secretion
OAT and OBTs
There is competition between drugs for carriers

101

What happens in DCT

Reabsorption

102

Weak acid overdose, give:

Bicarbonate

103

Weak base OD, give:

Ammonium chloride

104

There are many modes of excretion

Know this

105

First order kinetics

Constant fraction
Half life is constant
Non saturating kinetics

106

Zero order kinetics

Constant amount
Half life is not constant
Saturating kinetics

107

What are the zero order drugs

High doses of aspirin
Ethanol
Phenytoin

108

How is half life determined

Volume of distribution and CLearance

109

Maintenance dose is used for what conditions

Chronic

110

Loading doses are used for what conditions

Acute

111

How do you pick a drug dose

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

112

What does a maintenance dose do

Maintain the steady state or target concentration of a drug

113

What is a loading dose

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

114

What is the loading dose equation?

LD: CSS x d/F

115

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

LD

116

What is a steady state?

The goal concentration you want to reach with a drug.

117

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

Half life

118

What is the clinical steady state

4-5 half lives

119

What is the mathematical steady state

10 half lives

120

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

True

121

Are there oscillations around steady state with continuous infusion?

No

122

Are there oscillations around steady state with single or multiple doses

Yes

123

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

Below Minimum toxic concentration

124

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

Above MEC

125

What makes up the therapeutic window?

The MTC and MEC

126

What is the normal creatinine clearance

100 mL/min

127

What is the renal CL equation

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