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Fundamentals of Medicine: Exam II > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

Pharmacodynamics is _______
Pharmacokinetics is _____

A

What the drug does to the body

What the body does to the drug (absorption, distribution, metabolism, elimination ADME)

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2
Q

If a drug is bound to ______ protein it can’t move across membranes and be distributed to other tissues

A

Plasma

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3
Q

_____ is helpful to determine the best route of administration and the best choice of dosing

A

Pharmacokinetics (PK)

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4
Q

The first thing a drug encounters to gain excess to cells is the _____ _____. If a drug is ______ it will not cross the membrane as well. _____ drugs will cross the membrane easier

A

Plasma membrane

Hydrophilic
Hydrophobic

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5
Q

____ ____ ____ is the factor that calculates how likely a drug will hangout in octanol phase versus the aqueous phase. Drugs with _____ LPC prefer the octanol phase. Drugs with ____ LPC typically cross the membrane more efficiently.

A

Lipid partition coefficient
Higher
Higher

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6
Q

Free ____ won’t readily cross a lipid membrane. But the _____ form of a drug has solubility with the lipid membrane

A

Ions
Neutral

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7
Q

A ____ ____ is a proton donor, these are lots of drugs. They exist in the plasma as protonated (neutral) and anion forms in equilibrium. ____ does not cross the membrane but _____ does, especially in the stomach were there is a low ____ .

A

Weak acid
Anions
HA
pH

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8
Q

A ___ ___ is a proton acceptor. It exists in plasma as neutral and cation forms in equilibrium. Bases are ____ in their nonprotonated form and ____ when protonated. ____ does not cross the membrane in a low ____ environment. They are not readily absorbed in the stomach. Bases are readily absorbed in ____ environments.

A

Weak base
Neutral
Charges
Cation
pH
Basic

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9
Q

Many drugs are weak ___ and not weak ___. We can increase the ____ of the stomach.

A

Weak acids
Weak bases
pH

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10
Q

____ ___ is the ability to trap compounds on one side of the membrane or another if there is a pH gradient. Ex: weak acid drug with calcium carbonate like Tums would trap the weak acid in the form that we want it

A

Ion trapping

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11
Q

Weak acids are trapped in ___ environments. Weak bases are trapped I. ____ environments.

A

Basic
Acidic

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12
Q
A
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13
Q

____ ____ is a drug that is not bound by proteins. Only this drug has pharmacokinetic activity and can cross a membrane

A

Free

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14
Q

_____ ____ is a drug passively moving down their concentration gradient across a lipid bilayer

A

Simple diffusion

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15
Q

_____ ____ is when molecules move down their concentration gradient but with the help of channel protein or carrier protein

A

Passive transport

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16
Q

____ ____ moves molecules against the concentration gradient and needs energy

A

Active

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17
Q

Summary of transport mechanisms :

A
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18
Q

A lot of transport proteins are _____ meaning they are expressed on one side of the cell or the other

A

Polarized

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19
Q

______ ______ are slight differences, such as a single nucleotide variant, that changes how a protein transporter works

A

Interindividual variability

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20
Q

______ is the study of how genes affect the response to medications

A

Pharmacogenomics (PGx)

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21
Q

We can use a patients _____ to optimize drug dosing. This is called _____ medicine.

A

Genetics
Precision

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22
Q

Active _____ transport is keeping drug molecules out of a compartment. Active _____ transport is maintaining a higher concentration of drug inside a compartment

A

Efflux
Influx

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23
Q
A
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24
Q

Routes of administration:
Enteral/oral: absorbed ____ the intestines
Parenteral: absorbed ____ the intestines

A

Inside
Outside

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25
Q

Absorption efficiency:
_____ is the fastest, then _____, then ____, and the slowest is____

A

Intravenous
IM
Subcutaneous
Oral

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26
Q

_____ describes how efficient or inefficiently a drug is absorbed based on different routes

A

Bioavailability

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27
Q

The most common route is ____.

A

Orally

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28
Q

Oral drugs have to pass through the GI tract and make it into the target area. ____ ____ ____ metabolism.

A

First pass hepatic

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29
Q

Bioavailability (f) is how much drug makes it into the circulating ____. This is oral absorption. It is expressed as a fraction. 100% bioavailable = _____ administration. _____ refers to the area under the curve.

A

Plasma
IV
AUC

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30
Q

_____ avoids the first pass metabolism because it is absorbed directly into the blood stream through the mouth. ____ also avoids the first pass metabolism.

A

Sublingual
Rectal

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31
Q

The ____ is usually the most important contributor to first pass metabolism

A

Liver

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32
Q

After the drug has made it into plasma circulation it needs to be ____. This process is effected by tissue perfusion rates, plasma protein binding, and partitioning between plasma and tissue

A

Distributed
(Kidney and liver have high perfusion)
(Plasma protein binding inhibits distribution)
(Where does the drug like to partition)

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33
Q

Free drug and drug bound to protein is circulating in the plasma, only ____ ___ will be able to make it to the site of action, to other reservoirs, and to a site where it can be metabolized

A

Free drug

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34
Q

____ ___ is how much blood flow is given to a specific tissue. Kidneys lung liver and brain all have high perfusion. The drug will be distributed there ____.

A

Perfusion rate
Faster

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35
Q

Bound drugs are ____ ____. Best known plasma proteins are ____ and _____. They both bind to many weak acids

A

Pharmacologically inert
Albumin
Alpha 1 acid glycoprotein (AGP)

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36
Q

____ ____ refers to the concentration of a drug between plasma and tissue is often not equal. Sometimes drugs prefer to bind to tissue rather than plasma

A

Plasma partitioning

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37
Q

The ____ ____ ____ is a very “tight”endothelium in the capillary bed and glial cells. Only certain drugs can make it passed.

A

Blood brain Barrier

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38
Q

The volume of distribution: simple container model

A
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39
Q

Highly ____ ____ drugs distribute far more widely into tissue and have a large VD

A

Lipid soluble

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40
Q

____ determines the distribution of drugs between the blood and the rest of the body.

A

Vd

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41
Q

This is a low Vd

A
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42
Q

This is a very high Vd

A
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43
Q

Drugs with a high Vd have a ____ initial concentration in the blood. Drugs with a low Vd have a ____ initial concentration in the blood.

A

Low
High

44
Q

A ______ drug will have a smaller Vd and maybe only distribute into the plasma or ECF

A

Hydrophilic

45
Q

______ volume of distribution is the total amount in the body divided by the total concentration in a measured reference compartment

A

Apparent

46
Q

Example

A

500L is not a real volume, plasma is only 42 liters

47
Q

Vd reflect the relative affinity of a drug for the whole ____ and ____. It essentially represents the body as a big bag of plasma into which drugs are diluted. The Vd is the volume of ____ that would be required to contain all of the drug in the body given the measured concentration in only the plasma

A

Body
Plasma
Plasma

48
Q

The Vd is often normalized to ___ ___ as the ratio of different tissue types can vary from individual to individual

A

Body weight

49
Q
A
50
Q

True or false:
If a drug is bound to the plasma proteins, then the drug will have a large Vd

A

False

51
Q

____ of drug action is accomplished by metabolism (bio transformation) and excretion/elimination

A

Termination

52
Q

____ is the chemical modification of compounds to make them more polar, more readily eliminated

A

Biotransformation

53
Q

Bio transformation usually changes the shape of the drug, making them either ____ or ____. A ___ drug is a drug that is designed to be metabolized and transformed into their active form. Ex: Codeine

A

Active
Inactive
Pro

54
Q

The ____ is the main site of metabolism. Optimized space and surface area using a hexagon structure

A

Liver

55
Q

Bio transformation phase 1 and phase 2 both add _____ groups to make drugs more dissolvable, therefore more polar

A

Functional

56
Q

Phase 1 bio transformation usually introduces the ____ group making the drug functional. Phase 2 typically _____ the functional group added in phase 1

A

Functional
Attacks

57
Q

Not all drugs undergo phase ___ of biotransformation

A

1

58
Q
A
59
Q

____ is the most common type of reaction in phase 1. Metabolites are often ____ chemically reactive after phase 1

A

Oxidation
More

60
Q

____ is the most common type of reaction in phase 1. Metabolites are often ____ chemically reactive after phase 1

A

Oxidation
More

61
Q

______ enzyme family is by far the biggest contributors to phase 1 metabolism. About 75% of known drugs are metabolized by these enzymes. They are localized to the ____ _____ ___ in the cell

A

Cytochrome P450
Smooth Endoplasmic reticulum

62
Q

CYP450s are easily ____, meaning the cell has the ability to make more of this enzyme. Ex: St. John’s wart is an herb that upregulates cyp450 in the body which has effects on other drugs

A

Induced

63
Q

_____ is also a big inducer of CYP2E1 which effects the metabolism of acetaminophen to go down a route that has a toxic byproduct

A

Ethanol (alcohol)

64
Q

_____ induces CYP1A2, which effects the metabolism of antidepressants and antipsychotics

A

Smoking

65
Q

Grapefruit juice ____ cytochrome P450 enzymes. Ex: statins, it takes a lot more time to metabolism

A

Inhibits

66
Q

It is also very common to have ___ ___ interactions, prescriptions must be managed carefully

A

Drug-drug

67
Q

An enzyme inducer will increase the clearance by providing more enzyme, drug concentration in the body will ____. An enzyme inhibitor will decrease the amount of enzyme, drug concentration will ____.

A

Decrease
Increase

68
Q

______ has caused a lot of different outcomes due to genetic variability

A

CYP2D6

69
Q

Very different outcomes in ____ cancer treatment depending on if people are extensive metabolizers of CYP2D6 or poor metabolizers

A

Breast

70
Q

Phase 2 are usually _____ reactions such as acetylation, sulfate conjugation, methylation, glutathione conjugation. The result is usually _____

A

Conjugation
Inactivation

71
Q

Phase II drug metabolism enzymes:

A
72
Q

Phase 1 and phase II metabolism summary:

A
73
Q
A
74
Q

The ____ is the major site of drug excretion. Primary function is to remove excess water-soluble molecules from the ____ and return water to the central system

A

Kidney
Blood

75
Q

Three modes of excretion in kidney:
1. _____ - portion of blood flow to the kidneys is filtered through glomerular capillaries to remove compounds
2. ____ - create concentration gradient in collecting tubule and compound diffuses back out
3. _____ - active transporters along the tubule selectively pull compounds from plasma and dump into the urine

A

Filtration
Reabsorption
Secretion

76
Q

____ ____ is the volume of plasma that is cleared of a drug by the kidney per minute. It is based on glomerular filtration rate of kidneys. This goes down as you age

A

Renal clearance (CIR)

77
Q

When a solute is freely filtered (not reabsorbed or decreased) then glomerular filtration rate equals the ____ ____

A

Renal clearance

78
Q

Excretion of drug equation:

A
79
Q

If only _____ is occurring in the kidney, CIR = GFR.

A

Filtration

80
Q

_____ measures the health of the kidney

A

Creatinine

81
Q

If kidneys are filtering and reabsorbing the drug back into the blood stream, CIR is ____ than GFR. This is the case of Mandy drugs

A

Less

82
Q

If the drug is filtered and secreted by the kidney, the CIR is ____ than the GFR. An example of this is p-aminohippurate (PAH)

A

Greater

83
Q

Review:

A
84
Q

Plasma concentration = _____ / _____.

As clearance increases, the plasma concentration ____ because the drug is more readily metabolized and excreted

A

Dose rate
Clearance
Decreases

85
Q
A
86
Q

Y axis: ____ ___
X axis: ____
MTC: ____ ____ ____
MEC: ____ ____ ___
The ____ ____ is between the above two things

A

Drug concentration
Time
Minimum toxic concentration
Minimum effective concentration
Therapeutic range

87
Q

____ ___: when the patient first reaches the beginning of the therapeutic range

A

Onset time

88
Q

Tmax is the time at which the maximum drug _____ is reached

A

Concentration

89
Q

Cmax is the max ____ of the drug

A

Concentration

90
Q

____ = plasma concentration x Vd

A

Dose

91
Q

The units of dose should be ___

A

mg

92
Q

____ = total drug dose / plasma concentration

A

Vd

93
Q

___ is the elimination rate constant

A

k

94
Q

k = ____ / ____
Units for k: ___

A

Clearance / Vd

1/hr

95
Q

t half life = _____ / ____
t half life = _____ ____ / ____

A

0.693 / k

(0.693)(Vd) / clearance

96
Q

If the Vd increases, the half life ____

A

Increases

97
Q

If clearance increases than half life ____

A

Decreases

98
Q

First order kinetics is ____ kinetics and most easily visualized on a semi-log plot

A

Linear

99
Q

C0 is the concentration of the drug as soon as it is ___

A

Administered

100
Q

Log plot of first order kinetics drugs:

A
101
Q

Zero order kinetics

A
102
Q

___ ___ kinetics is when the elimination rate changes proportionally to the does

A

First order

103
Q

___ ___ is when the elimination rate remains constant independently of the dose

A

Zero order

104
Q

Maintenance dose = (_____) ( ____) / ____

A

(IV dosing rate) (desired oral dose interval) / F

105
Q

Equations to memorize:

A

Fundamentals of Medicine: Exam II (19 decks)

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