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SRNAPharmacology I > Basic of Pharmacology: Pharmacokinetics Part II > Flashcards

Basic of Pharmacology: Pharmacokinetics Part II Flashcards

2nd part of PP

1
Q

What is the other name of Cytochrome P-450 system

A

Mixed Function oxidase (MFO) Enzyme system.

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2
Q

CYP 450 enzymes definition? They are responsible for ________and _________ Phase _____metabolic reaction of drug.

A

Group of membrane bound microsomal enzymes responsible for OXIDATION and REDUCTION phase I metabolic reaction of drug

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3
Q

What is the primary membrane bound organelle where CYP 450 is located? the membrane organelle of which specific organ _______; Other organ too.. Yes or NO?

A

Smooth ER in the LIVER; Yes

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4
Q

CYP 450 system has more than ______individual CYP 450 Enzymes

A

50

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5
Q

What is the most abundant CYP expressed in the liver?

A

CYP3A4 (most amount of drug metabolism)

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6
Q

CYP 450 enzyme system, they have enzyme_______ or _________

A

Induction

Inhibition

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7
Q

Enzyme induction means: (Enzyme induced)

A

Enzyme activity increased

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8
Q

Enzyme inhibition means: (Enzyme reduced)

A

Enzyme activity decreased

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9
Q

1 way to major source of drug-drug interactions

A

Enzymes Induction and inhibition

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10
Q

All enzymes cannot be

A

induced or reduced.

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11
Q

CYP 450 inducers are drugs

A

have to ability to stimulate/induce the activity of CYP450 microsomal enzymes

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12
Q

CYP 450 inducers are drugs

A

have to ability to stimulate/induce the activity of CYP450 microsomal enzymes

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13
Q

Classic examples of CYP 450 inducers (RPP-CSC)

A 
Rifampin
Phenobarbital
Phenytoin
Carbamazepine
St John's Wort
Cigarette smoking
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14
Q

IMPORTANT: If you give a patient rifampin (inducer) and you give patient drug B what will happen to drug B

A

DECREASED level of Drug B SYSTEMICALLY because the rifampin induces CYP450 (more enzymes available) Drugs B will go under extensive metabolism, so systemic levels will decrease

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15
Q

IMPORTANT: CYP 450 inhibitor are drugs

Know the reducers drug

A

Inhibit activity of CYP450 microsomal enzymes

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16
Q

Non-MICROSOMAL ENZYMES responsible primarily for phase ____reactions : such as ______ and ______ and some ______ and _____

A

II ; conjugation, hydrolysis; oxidation and reduction

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17
Q

Are non-microsomal enzymes CYP 450 enzymes

A

no

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18
Q

NON-SPECIFIC ESTERASES enzymes responsible for

ANY ester bonds drugs and any ester local anesthetics

A

Hydrolysis of drugs;

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19
Q

Non-microsomal enzymes such as ______ _____ _and ________ enzymes (Do/DO NOT) undergo enzyme induction

A

Plasma cholinesterase and acetylating enzymes

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20
Q

Factors affecting metabolism (DAGPIE) : Which is the most important?

A 
DAGPIE
Disease state
Age
Gender
PHARMACOGENETIC factors 
Induction or inhibition of enzyme
Environmental factors
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21
Q

What is EXCRETION

A

The irreversible removal of drug form the body

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22
Q

What is the main organ responsible for the removal of drugs and drug metabolites

A

Kidney

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23
Q

IMPORTANT: Primary excretory organ

A

Kidney

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24
Q

What are the 2 major pathway of renal excretion?

A

Glomerular filtration

Tubular secretion

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25
Q

How does Biliary excretion occurs :

A

directly into the bile from the liver cells.

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26
Q

Where are gaseous and volatile anesthetics excreted_______

A

Excreted via the lungs

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27
Q

What is clearance (drug elimination other term)

A

the irreversible removal of drugs from the body FROM ALL ROUTES OF ELIMINATION

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28
Q

Drug elimination : clearance (Cl) combined with these two PHARMK…c phases

A

Metabolism and Excretion

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29
Q

IMPORTANT: Why do we care about clearance?

A

body elimination dose of a drug
***MAINTENANCE DOSE OF A DRUG requires to OBTAIN A GIVEN STEADY STATE SERUM CONCENTRATION
How much to give
potential drug-to-drug

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30
Q

Clearance (PHARMACOKINETICS definition)

A

The volume of plasma cleared of drugs from the body per unit of time (Volume of plasma drug -free /unit of time )

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31
Q

Formula of TOTAL CLEARANCE IN THE BODY; clearance

A

Cl total = Cl renal X Cl hepatic x Cl other (lungs)

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32
Q

MEMORIZE THIS (IMPORTANT) Body clearance ? VD is ______ __ _______ and K (el) _____________

A

Cl = Vd + K(el); Volume of distribution; Elimination rate constant K (el)

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33
Q

Clearance made up of 2 processes

A

Metabolism

Excretion

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34
Q

Organ for clearance : primary route of drug metabolism ___________and _______ ______system is the primary system responsible for drug metabolism

A

Liver; CYP 450

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35
Q

a) If the drug infusion matches the clearance rate then the drug concentration _________(elevated, decreased, constant)
b) If the clearance rate exceeds the infusion rate then the drug concentration ________

A

a) will be constant

b) Will fall

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36
Q

The most important to determine clearance of REGULAR DRUGS

A

Drug elimination half life

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37
Q

Hepatic Clearance

A

VOlume of blood that perfuses the liver that is cleared of drug per unit of time

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38
Q

Determinants of HEPATIC CLEARANCE

A 
Liver blood flow (Q) 
Extraction Ration (ER)
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39
Q

Hepatic clearance formula

A

Hepatic blood flow (Q) x Hepatic extraction rate

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40
Q

HWat does Extraction rate takes into consideration

A

Drug intrinsic clearance and protein binding

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41
Q

High hepatic Extraction Ratio (ER >0.7)

A

That particular drug is going to be cleared through the LIVER dependent SOLELY on HEPATIC BLOOD FLOW

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42
Q

Changes in liver enzyme activity have (lot/minimal ) ________influence on hepatic clearance. JUST ______

A

minimal; ______Hepatic

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43
Q

3 drugs with HIGH EXTRACTION RATIO and HEAVILY HEPATICALLY CLEARED

A

Lidocaine, propofol, and propanolol

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44
Q

If patient is on propanolol should __________

A

Take up until ready for surgery

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45
Q

LOW hepatic Extraction Ratio (ER <0.3); Hepatic clearance will/will not dependent on hepatic blood flow

A

Hepatic clearance will NOT depended on hepatic blood flow

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46
Q

Hepatic clearance is affected by _______ _____binding and _______ activity

A

Protein and enzyme binding

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47
Q

Protein binding ________ in binding will _______ hepatic clearance

A

Decreased: increased

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48
Q

Enzyme activity _________ in activity will ______hepatic clearance

A

increased ; increased

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49
Q

CLASSIC example of low hepatic Extraction ration drug

A

Alfentanil

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50
Q

Renal Clearance: 3 Processeses

A

Glomerular filtration
Active tubular secretion
Passive tubular reabsorption

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51
Q

Glomerular filtration what happens:

A

Free fraction of unbound drug filtered via the glomerulus

Bromanc Capsule

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52
Q

Does highly protein bound readily filtered at the glomerulus?

A

No

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53
Q

What is GFR?

A

is the amount of glomerular filtration formed each minute by all nephrons.

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54
Q

The higher the number the ______ the clearance

A

Better

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55
Q

Active tubular secretion requires _______ and_____transport

A

active transport, requires energy

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56
Q

ACtive tubular secretion does what?

A

Move drug from the blood into tubular

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57
Q

The majority of drug tubular secretion takes place where

A

In the PROXIMAL TUBULE

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58
Q

**IMPORTANT the kidneys eliminate drug from plasma by both

A

Glomerular filtration

Active Tubular secretion

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59
Q

***Able to give lasix to some patient because they may use

A

active tubular secretion although GFR may be not working

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60
Q

Passive tubular reabsorption definition

A

is the process by which solutes and water are removed from the tubular fluid and brought back to blood

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61
Q

What form is readily reabsorbed? where does it occur ?

A

NON-IONIZED; DISTAL TUBULE OF the NEPHRON

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62
Q

Example of a drug OCCURS primarily with highly lipid soluble compound

A

Sodium Thiopental

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63
Q

Factors affecting rate of reabsorption

A

pH

pKa

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64
Q

*****IMPORTANT CONCEPT ANSWER THIS : A more acidic urine will do what to a basic drug and what to an acidic drug?

A

excrete faster

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65
Q

Cockcroft-Gault Equation (no need to know formula) : FDA approved

A

Calculate creatinine clearance, how well the kidney is doing the process of glomerular filtration

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66
Q

**IMPORTANT CONCEPT ANSWER THIS: A basic urine will do what to a basic drug and what to an acidic drug?

A

excrete faster

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67
Q

Biliary excretion definition

A

the transfer of drug or metabolites form the PLASMA to the BILE through hepatocytes

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68
Q

This transport is due to ______ secretion of drugs into the ______ by means of Transport protein systems

A

active’ bile

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69
Q

_________ _______May prolong the pharmacological effect of certain drugs

A

ENTEROHEPATIC CIRCULATION

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70
Q

ENTEROHEPATIC CIRCULATION

A

A drug or metabolite secreted into bile will eventually into the duodenum via the gallbladder

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71
Q

Examples of drugs of enterohepatic circulation?

A

morphine

Diazepam

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72
Q

ENTEROHEPATIC CIRCULATION.

A

The cycle in which the drug is absorbed, excreted into the bile and reabsorbed

73
Q

Pharmacokinetic Models

A

Hypothetical structures used to describe the fate of a drug in the body following its administration.

74
Q

The distribution of drugs in the body can be described by :_______, ______ or _________

A

one, two or three compartment models.

75
Q

One COMPARTMENT MODEL means:

EX

A

Entire body as single compartment, evenly distributed; Single volume and clearance;
Example is : SINGLE BOLUS of a drug

76
Q

Assumption of the one compartment model

A

Drug distribution and equilibration to all tissues and fluids occurs instantly (not really true)

77
Q

Elimination occurs via (1 compartmnt) in ______ order kinetics.

A

FIRST ORDER KINETICS

78
Q

Once equilibration is reached in 1 compartment

A

the drug concentration at the site of action is approximately the same as in plasma

79
Q

IMPORTANT : If we know the concentration we want to achievee and know the _____ _________ then we can calculation using the dose required to achieve that concentration. State formula: substitute variables as needed

A

Volume of distribution
Vd= Dose/Concentration
CONCENTRATION= Dose/ Vd

80
Q

Plasma concentration vs. Time curves for drugs

A

A graphical way to show what is happening to the drug concentration overtime after you give an IV bolus.

81
Q

Time is on the ____ axis

Plasma is on the ___axis

A

x axis

y axis

82
Q

NOT IMPORTANT : THE STRAIGHTER CURVE

A

BETTER AT PREDICTING

83
Q

MOST ANESTHETICS undergo________Model

A

Multicompartment

84
Q

Two-compartment model pharmacokinetics design

A

CENTRAL

PERIPHERAL compartments

85
Q

What happens during 2 compartment model ; List 5 organs.

A

Drugs is introducedDistribuated rapidly and UNIFORMY inthe bloodsteram and the highly perfused ORGANS (Heart, lung, kidney, liver, Brain)

86
Q

What is the central compartment

A

lungs, brain, liver, kidney and heart

87
Q

During the 2 compartment model has defined

A

Distribution and Elimination phase

88
Q

Distribution phase is ________During the distribution, changes in the concentration of the drug______What happens?

A

Rapid movement of drugs from the plasma to the rapidly equilibration tissues. Reflect the concentration of drug in the plasma reflect primarily movement of drusg within, rathe than loss from the body. NOT INSTANTANEOUS

89
Q

Explain the elimination phase as it relates to drug in plasma and volume of distribution? What happens when the drug has reached equilibration in plasma and tissue?

A

The relative proportion of drug in the plasma and peripheral volumes of distribution remains constant. Once the drug in the plasma and tissues has
reached equilibrium, the decline of plasma concentration is driven by elimination of the drug from the body from the central compartment be metabolism OR excretion

90
Q

Peripheral compartment”

A

Fat , muscle, skin, CSF

91
Q

*****ANESTHETIC DRUGS distribute extensive into ________ -____

A

peripheral tissues

92
Q

Does drugs elimination occur from peripheral Tissues? They have to go back to the blood stream?

A

NO

93
Q

Some anesthetics should be tailored from patient who are

A

morbidly obese.

94
Q

INTERCOMPARMENTAL CLEARANCE is

A

the movement of the drug from the central to the periperal compartment .

95
Q

Peripheral compartment decline wih

A

Aging.

96
Q

Any residual drug present in the peripheral compartment at the time of repeat IV dosing may result in (increased/diminished)________ effect of distributive process on the reduction of the plasma concentration and lead to exaggerated effects
The degree of cumulative effect can be predicted by several factors such as dosing interval and knowledge of the elimination half-life

A

diminished

97
Q

As you increase time, concentration ________

A

Decreases

98
Q

Vd should be drawn in what phase

A

elimination phase

99
Q

Distribution half life; calculated in ____

Tells you the plasma concentration is declining because moving from PLASMA to the tisses

A

Distribution phase

100
Q

Shorter half life, the faster the plasma

A

decreasing.

101
Q

MOST ANESTHETICS follow a ______compartments model

A

3

102
Q

Such as propofol

A

1 central , 2 peripheral compartments.

103
Q

Drugs like propofol uses : 3 compartments

A

1 central , 2 peripheral compartments.

104
Q

VERY IMPORTANT IN ANESTHESIA: Following the administration of an IV anesthetic drug, the immediate distribution phase causes a brisk decrease in plasma levels as the drug is transported to the rapidly equilibrating vessel-rich group of tissues where the drug can cause their effect

A

From brain to other peripheral compartments.

105
Q

MOST SITE OF ACTION FOR ANESTHESIA meds

A

BRAIN

106
Q

Redistribution is _____________

A

Drug effect is terminated when the drug leaves the vessel-rich group and redistributes to other less well perfused tissues such as muscle and fat

107
Q

Describe redistribution pathway once you give an IV medication …

A

Give IV—> Majority in blood _–> Brain–> Blood concentration decreases –> Brain concentration increased- –> once brain concentration decreased–> tissues and fat concentration increases.

108
Q

Pt wakes up after anethesia

A

Because of redistribution

109
Q

Determinant of tissue uptake of drugs

A

Blood flow
Concentration gradient
BBB
Physiochemical properties of drug (solubility, ionization and protein binding

110
Q

Determinants of the capacity of tissue to store drugs (KEEP IT )

A

lipid solubiltiy (the greater > the more able to keep)
tissue mass
Binding to macromolecules
pH of the tissue.

111
Q

VERY IMPORTANT for non-anesthetics drugs

A

Elimination half life

112
Q

MEMORIZE This DEFINITION

A

Time necessary for the serum (plasma) concentration to decrease by 50% AFTER absorption and distribution phase

113
Q

Half life is directly proportional to ____ ___ _____

as half life increases, _____increases

A

Volume of distribution

114
Q

Half life is _______ _________ to CLEARANCE
AS clearance decreases the half life __________
As clearance increases the half life

A

INVERSELY PROPORTIONAL As clearance decreases, the elmination half-life increases; decreases

115
Q

Elimination half life useful for

A

Estimating the time needed to reach steady state
Dosing interval
Time required for drug removal from the body after the drug is no longer being administered.

116
Q

Elimination half life useful for

A
  • Estimating the time needed to reach steady state
  • Dosing interval
  • Time required for drug removal from the body after the drug is no longer being administered.
117
Q

KNOW THIS FORMULA: ELimination

A

t 1/2 = 0.693 / K (el)
OR
t1/2 = 0.693 * Vd / Cl

118
Q

As you decrease CL, half life ________

A

increases

119
Q

Know The GRAPHS and SCALES

A

know if values are in log or non-log

120
Q

How many half times in takes to remove the drugs

A

4-5 half lives

121
Q

What is Steady state

A

when the rate of drug administration = rate of drug elimination /clearance, so that the serum concentration and amount of drug in the body are constant.

122
Q

Steady-State is achieved at approximately ___________from the time the dosage regimen was initiated for first-order kinetic drugs

A

4 to 5 t1/2

123
Q

MEMORIZED: IMPORTANT FOR ANESTHETIC DRUGS: CONTECT SENSITIVE HALF TIME

A

Time necessary for the plasma drug concentration to decrease by 50% after discontinuing a CONTINUOUS infusion of a specific duration

124
Q

In “context sensitive half life” Context describes the combined effects of

A

DISTRIBUTION , METABOLISM and the DURATION OF THE IV CONTINUOUS RATE

125
Q

Drugs can have (one/multiple) context sensitive half tiem

A

MULTIPLE

126
Q

Primary factors affecting CONTEXT SENSITIVE HALF TIME

A

INFUSION time.

127
Q

Depending on the lipid solubility and the efficiency of the
drugs clearance mechanisms, the context-sensitive half-time (decreases/Increases)__________ in parallel with the duration of the continuous IV infusion, because
it takes longer for the concentrations to fall if the drug has accumulated in peripheral tissues. An exception to this rule is ____________

A

Increases; Remifentanil

128
Q

Is the context-sensitive half life related to Half time

A

NO

129
Q

What is the definition of zero-order kinetics?

A

Refers to the elimination (removal) of a constant AMOUNT OF DRUG PER UNIT OF TIME (i.e.: 2 mg/min), regardless of the amount of drug or drug concentration in the body

130
Q

IMPORTANT Short definition of zero order kinetics? ______ is independent

A

Elimination is INDEPENDENT OF TIME OR DRUG concentration

131
Q

For drugs that undergo ZERO -ORDER KINETICS (think Z-A) small increases in drug dose produces ________ _____ in drug concentration

A

DRASTIC INCREASE in plasma concentration (disproportionate)

132
Q

How does the process of zero order kinetics

A

Enzymes or transporters responsbile for metabolizing the drug become SATURATED

133
Q

Term interchangeable: zero-order kinetics or ________

A

non-linear pharmacokinetics

134
Q

Classic EXAMPLES of ZERO order kinetics DRUGS (PEA)

A

Phenytoin
Ethanol
Aspirin

135
Q

First ORDER KINETICS, what is it?

A

Refers to the elimination of a constant FRACTION or PERCENTAGE of DRUG PER UNIT OF TIME

136
Q

In first order kinetics, the rate of drug elimination is directly proportion to the drug concentration and are ________ on the concentration

A

DEPENDENT

137
Q

ZERO ORDER KINETICS is half life helpful

A

half life is useless, because removal in nonlinear

138
Q

TRUE or FALSE In first order kinetics, serum concentration either increase or decrease proportionally with the dose

A

True

139
Q

In first order kinetic, if you increase the dose of the drug

concentration will increase.

A

concentration will increase

140
Q

FYI: FIRST ORDER kinetic drug, can go into _____ ______when there is a severe __________

A

Zero order kinetic; overdose

141
Q

With a first order reaction, if the y-axis is in linear units, the process will be ____.

A

exponential

142
Q

With first order reactions, if the y-axis is in log form, the process will be ___.

A

linear

143
Q

In context sensitive half time, the “context” represent the

A

Duration of the drug infusion.

144
Q

Why does the context sensitive half time increase with longer infusion duration ?

A

because it takes longer with for the concentrations to fall if drug has accumulated in PERIPHERAL TISSUES>

145
Q

When an CYP450 inducing agent is prescribed with another medication What will happen ? What should be done to the dosage of the other medication?

A

The rate of metabolism is increased; may need to be adjusted and the effect of the medication reduced.

146
Q

When a drug that (reduces CYP 450) Inhibiter/reducer, if a medication is taken with an agent that inhibits its metabolism?

A

then the drug level can rise and possibly result in a harmful or adverse effect.

147
Q

Classic example of drug A (warfarin) given with an enzyme CYP 450 inducer Drug B (Rifampin), what will happen to drug A?

A

If warfarin is given with an enzyme inducer, Such as rifampin, the metabolism activity of CYP450 will increased, so warfarin metabolism increased, and SYSTEMICALLY warfarin is decreased because it is metabolism extensively

148
Q

Inhibitors _______Drug substrate level systemically

A

INCREASE drug B systemically

149
Q

Inducers _________Drugs substrate level systemically

A

INCREASE drug B systemically

150
Q

Classic example of drug A (warfarin) given with an enzyme CYP 450 INHIBITOR Drug B (AMIODARONE), what will happen to drug A?

A

INR will increase and patient will be at risk for bleeding because the enzyme to metabolize the warfarin is inhibited.

151
Q

What is the formula for rate of elimination

A

Cl * Concentration

152
Q

Unit for RofE

A

Mass/ time

153
Q

The faster the rate of clearance

A

The shorter the half life

154
Q

The half-life of any drugs is _________ _______ to its rate of clearance

A

Inversely proportional

155
Q

After 1 half-life, you will have reached ____ of steady state. After 2 half-lives, you will have reached _____ of steady state, and after 3 half-lives you will have reached ______of steady state. The rule of thumb is that steady state will be achieved __________ half lives.

A

50%; 75%; 87.5% ; that steady state will be achieved after 5 half-lives (97% of steady state achieved)

156
Q

Does P450 enzyme induction has an effect on volume of distribution?

A

P450 enzyme induction has no effect on volume of distribution.

157
Q

Hepatic extraction, the first-pass effect, and clearance for CYP3A4 substrates will be _______(inc/dec) by inducers

A

increased

158
Q

If the extraction rate of verapamil is already equal to the hepatic blood flow, Does a further increase in metabolism increase clearance?

A

so further increase in metabolism will not increase clearance of this drug.

159
Q

Graded dose-response curves used to determine

A

The maximal efficacy of the drug

160
Q

______ used to determine potency between 2 drugs

A

ED 50;

161
Q

______ used to determine potency between 2 drugs; the less of it the ______ (more/less) potent; The more of it the _____(more/less) potent

A

ED 50; more; less

162
Q

For decreased or increased ph when using the Henderson Hasselbach equation, ______at 1 pH unit more alkaline than the pKa and_____ at 2 pH units more alkaline.

A

1/10 ______; 1/100

163
Q

Well-documented Cyp450 Innhibitor is

A

AMIODARONE

164
Q

What is called when the drug is excreted in the bile and reabsorbed in the intestine

A

Enterohepatic Circulation

165
Q

What is enterohepatic circulation?

A

when the drugs is excreted into bile and reabsorbed in the small intestine.

166
Q

2 drugs that undergo ESTER HYDROLYSIS

A

SUCCYNYLCHOLINE

MIVACURIUM

167
Q

The majority of drug tubular REABSORPTION takes place where

A

DISTAL TUBULE

168
Q

Example, _____ ______ is a highly lipid soluble agent and is completely reabsorbed from the nephron MINIMALLY CHANGED

A

SODIUM THIOPENTAL.

169
Q

Log from Vd is a ______Line

A

straight

170
Q

Anesthetics drugs are best described by

A

MULTICOMPARTMENT

171
Q

2 compartment model : Drugs distributes into 2 compartments________ and ________ . distributes first to ________ organs and then SLOWLY to _______. drugs moves _____ and _____between these 2 compartments to maintain equillibrium and then returns to_____ when _______occurs

A

central and peripheral; vessel rich group/; peripheral. Back and forth; CENTRAL; ELIMINATION

172
Q

In the 2 compartment, changes in the concentration of drug in the plasma reflect

A

movement of drug within, rather than lost out of the body.

173
Q

In adults, highly perfused make up ___% of body mass but receive ___ of cardiac output

A

10%; 75%

174
Q

Distribute extensively into the PERIPHERAL TISSUES

A

Anesthetics

175
Q

If K (el) is 0.25

A

25% of the amount of drug will be eliminated at any given moment in time.

176
Q

What does K(el) means

A

elimination rate constant is the fractional rate of drug administration from the body.

177
Q

What is morphine ? Wa or wb

Lipid soluble? How does it travel to CNS?

A

Weak base; low ; slowly

178
Q

At higher pH for weak bases, comparing two drugs , the one with higher pH has ________ actions

A

Higher

SRNAPharmacology I (29 decks)

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