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NUR 622: Adv. Pharmacology Lectures > Exam 1A: Dr. Owens > Flashcards

Exam 1A: Dr. Owens Flashcards

1
Q

Parenteral route literally means “other than enteral”, but generally reserved to describe routes when drug is administered by _____.

A

hypodermic injection. (parenteral routes avoid epithelial barriers)

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1
Q

Passive diffusion is quantified by ____.

A

Fick’s First Law of Diffusion

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1
Q

This means that molecules can come apart.

A

Ionization. Note: Some drugs can ionize into charged particles.

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1
Q

Value of f which means the drug is highly bound.

A

f < 0.1 (e.g. 90%)

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1
Q

PK media collection: Biological samples are generally stored in freezers at ____ (temperature)

A

-20C or -80C

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2
Q

Drug tolerance develops to the action of many CNS drugs like (3)

A
  1. Opioids 2. Antipsychotics 3. Antidepressants
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3
Q

Elimination of a constant quantity per time unit of the drug quantity present in the organism.”

A

Zero order elimination. (Linear graph)

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4
Q

Refers to as what the body does the drug does to the drug.

A

Pkinetics

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5
Q

This is referred to drug loss sue to large amount of blood flow that goes through the liver from the GIT.

A

First pass

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6
Q

2 Parameters needed to determine therapeutic window

A
  1. efficacy 2. safety
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7
Q

FYI: Protein Binding is described as a FRACTION.

A

:P

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8
Q

The ________ model frequently accounts for PD effects and describes that the effect may be saturated.

A

Emax

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9
Q

Gives information about rate of absorption

A

Cmax = maximum concentration

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9
Q

This is the negative of the slope.

A

k value. It tells you the half life of the drug.

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9
Q

T/F: PK models are built to describe a system mathematically and depend upon assumptions made about the system. Any lack of adherence of the real system to the assumptions will lead to loss of accuracy in predictions of the model

A

T

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10
Q

These are used to quantify the time-course of drug concentrations in the body.

A

PK models

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10
Q

In Mammillary models, elimination occurs from the ________, reflecting that the kidneys and liver are highly perfused tissues.

A

central compartment

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11
Q

This is the elimination rate constant, gives information about the elimination rate.

A

k

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11
Q

Orally absorbed drug passes through the gut wall, passes through the liver before entering the systemic circulation thereby subject to a grater fractional loss of drug.

A

First-pass metabolism

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12
Q

This is the proportionality between concentration and amount.

A

Volume distribution (Vd)

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12
Q

PD response to a drug may be (2)

A
  1. Rapid: (Neurotransmitters, Neuromuscular blockade, drug effects on electrical signals) 2. Delayed: ( Hormone effects, mRNA effects, protein or enzyme changes, antibiotic effect, wt. loss, bone density, smoking cessation) or response may be inhibitory or stimulatory
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13
Q

This enzyme show 50% of Whites are extensive metabolizers.

A

CYP - 2D6

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14
Q

It describes the sum of elimination from all routes (e.g. renal and hepatic)

A

Total body clearance (ClT)

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15
Q

It is the hypothetical volume of body fluid from which a drug is completely removed per unit time.

A

Clearance

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16
Q

The route of administration influences the _________ of drug in the body.

A

concentration-time profile

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17
Q

Disposition is composed of (3)

A

DME 1. Distribution 2. Metabolism 3. Excretion

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18
Q

Nonsystemic (local route): Drugs merely has to stay at the site of action, or travel a short distance by ______ or ______ to reach its site of action.

A
  1. diffusion 2. absorption through tissue
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18
Q

This is a product of the formulation and the regimen administered.

A

Exposure

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19
Q

Practical considerations in Polymorphism in PK (3)

A
  1. Dose Adjustments 2. Dose Amount 3. Dosing Interval
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20
Q

In Local routes, high concentrations can be achieved. Systemic concentrations may occur, but they are ______. Systemic concentrations resulting from local administration may be a source of _______.

A

coincidental…….. unintended adverse effects.

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21
Q

Administering a bolus and an infusion in order to achieve the steady state.

A

Loading Dose

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23
Q

This refers to the rate of decline (elimination) depends on how much drug is present at that time. The IV Bolus concentration falls in this type of process.

A

First order elimination

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24
Q

The ability of the drug to go in solution is affected by the

A

surface area.

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24
Q

In Mammillary models, other compartments represent collections of other tissues with slower distributional characteristics - e.g. (3)

A
  1. Bone 2. Brain 3. Adipose
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25
Q

Tis is the simplest PK model.

A

One Compartment Model with IV Bolus Admin

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25
Q

This is an example of a high Volume distribution.

A

Digoxin

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25
Q

This reflects how strongly drugs bind to plasma proteins.

A

Affinity (Kd)

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25
Q

Practical considerations in PD (2)

A
  1. Diagnostics for treatment selection 2. Treatment algorithms
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26
Q

PK properties do not change with changes in concentration; aka “dose proportional PK”, “proportionality to kinetics”

A

Linearity

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27
Q

Variables in Cockcroft and Gault method (3)

A
  1. Age 2. weight (kg) 3. Serum cratinine
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28
Q

How well a drug product mixes, or goes into solution, depends in part on whether it is a(an) _____.

A

electrolyte

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30
Q

Route of Administration: Administered drug reaches and travels through the general circulation in order to gain access to its target site of action.

A

Systemic Distribution

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32
Q

Refers to as what the drug does to the body.

A

Pdynamics

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33
Q

Example of a drug that has nonlinear PK.

A

Dilantin. (If you double the dose, you get much proportional levels; can lead to toxicity) AUC increases supra-proportionally with dose

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34
Q

This PK models have a central compartment, and all other compartments connect directly to the central compartment, with REVERSIBLE flow between compartments.

A

Mammillary model

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36
Q

FYI: ER tabs may be seen in stools.

A

:)

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36
Q

GIVE 5 examples of organs of excretion.

A

Kidneys, gall bladder sweat glands, mammary glands lungs

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36
Q

It gives information about the total extent of absorption

A

AUC = Area Under the Concentration-time curve

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37
Q

pH of urine which favors treatment of methamphetamine toxicity.

A

Acidic (Low pH). Increases excretion and shortens 1/2 life

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38
Q

3 Mechanisms for Genetic Factos of Drug Response.

A

Polymorphisms in 1. Drug Receptors 2. Drug Transporters (e.g. MDR1) 3. Drug Metabolizing Enzymes (e.g. CYP 2D6)

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39
Q

This is the ratio of CSF to unbound drug in plasma

A

Equilibration of drug in the CSF

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40
Q

Mechanism of transport at the tubular level (secretion and reabsorption)

A

Active/ Facilitated processes

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41
Q

Polymorphisms in drug receptors alter ____

A

drug binding and action

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42
Q

Part of nephron where drug secretion occurs

A

Proximal convoluted tubule.

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42
Q

This can alter absorption, distribution, or even efficacy and safety when transporters keep the drug away from the site of action or metabolism.

A

Polymorphism in Drug Transporters

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42
Q

This is the first observed polymorphism in drug metabolizing enzymes.

A

CYP 2D6

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44
Q

This route gives the provider the most control or manage the drug.

A

Continuous IV infusion

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45
Q

Clearance units are expressed in ___

A

volume per time (e.g. L/ Hr)

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45
Q

Major routes of drug elimination - % (8)

A
  1. CYP 3A4: 28% (Phase 1) 2. Renal: 25% 3. UDPG: 10% (Phase 2 Glucurunidation) 4. CYP 2D6: 10% 5. Other Metabolism: 10% 6. CYP 2C9: 7% 7. Hepatobiliary: 6% 8. Other CYPs: 4%
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46
Q

This treats the body as one homogeneous volume in which mixing is instantaneous. Input and output are from this one volume. Drug goes in and concentration is uniformed all through out.

A

One Compartment model

46
Q

Letter that symbolizes bioavailability.

A

F

47
Q

Drugs recycled and excreted from bile are metabolized during phase II, like ____ .

A

glucuronidation

49
Q

“open” compartmental models have ______ from the system.

A

elimination

50
Q

This happens when drug is not highly bound.

A

Dissociation

51
Q

Metabolism and excretion is collectively called ___.

A

Elimination

52
Q

Clearance is the product of

A

V (volume distribution) and K (rate of elimination)

53
Q

Pharmacogenetic factors have highest impact on these drugs (3)

A
  1. Psychoactive drugs 2. CV drugs 3. Cancer drugs
54
Q

Mechanism of transport: Filtration at the glomerular capillary

A

Passive transport

56
Q

What is the concentration-time profile for intermittent IV infusion?

A

Saw-tooth pattern.

57
Q

True or False: Absorption still must occur for SC, IM, and intraperitoneal administration.

A

true

58
Q

When effect is plotted against concentration, different responses are seen at the same concentration; graph shows a loop.

A

Hysteresis

59
Q

Other name for “open” compartmental model

A

Multicompartmental model

60
Q

Enzymes that are important in Phase 1 (3)

A

2C9 2C19 2D6

62
Q

T/F: Charged molecules typically can’t cross the lipid bilayer.

A

true

63
Q

Drugs can be eliminated before absorbed by the body by __ (3)

A

HCG 1. Hepatic Metabolism/ 1st pass 2. Chemical degradation 3. GI metabolism

64
Q

Noncompartmental Analysis (NCA) Parameters (4)

A

Cmax, Tmax, k, AUC

65
Q

These (2) define relationship between concentration and effect of most drugs.

A
  1. Emax (Max effect) 2. C50: Concentration achieving 50% maximal drug effect
66
Q

Initial passage of drugs through the liver

A

First Pass metabolism

67
Q

Oral drugs absorbed through the gut wall flows into the ___.

A

portal vein to the liver.

68
Q

This PK models are similar to mammillary compartmental models, but one to more compartments do not connect directly to the central compartment.

A

Catenary Models

69
Q

What happens when you take simvastatin with grapefruit juice?

A

It blocks3A4 and PGP therefore it increases AUC and decreases clearance.

70
Q

PK/ PD models can “______”, when they appropriately describe the mechanism or time-course of the hysteresis.

A

collapse the hysteresis

71
Q

PK medium where cellular fraction is used. The use of anticoagulant like heparin or EDTA is used to prevent clotting.

A

Plasma

73
Q

Bioavailability is described in terms of (2)

A

Rate and Extent of Absorption

73
Q

Examples of Dosage Regimen Designs (2)

A
  1. Therapeutic Range 2. Therapeutic Window
75
Q

Enterohepatic recycling can occur. The highest concentration of reabsorption occurs in the _____, where there is increased villi surface area.

A

duodenum.

76
Q

In intermittent IV infusion profile, the peaks refer to the ____

A

end of infusion.

78
Q

This is the ability of a drug to get into the systemic circulation from the site of administration.

A

Bioavailability

79
Q

This is termed for induction or inhibition of PD responses. It results in a change of PK/PD relationships overtime.

A

Functional Adaptation

79
Q

This is the study of individual variations in drug response due to genetic variations.

A

Pharmacogenomics

81
Q

Processes (or phases) of pharmacokinetics (4).

A

ADME 1. Absorption 2. Distribution 3. Metabolism 4. Excretion

83
Q

In continuous infusions, this refer to the balance between drug going in and drug going out. This leads to constant plasma concentration level.

A

steady state.

84
Q

PK Media Collection (4)

A
  1. Whole Blood 2. Serum 3. Plasma 4. Urine
86
Q

T/F: Parenteral route has either local or systemic effects.

A

True

87
Q

Elements of a Regimen (3). These are the things we control in a regimen.

A
  1. Route 2. Dose 3. Frequency
88
Q

This model refer to time zero drug is evenly distributed in the body.

A

Well-stirred Model

88
Q

PK medium where in the clotting facts and cellular components are removed.

A

Serum

89
Q

Parameters (3) used in Hill Equation (Drug Effect Calculation)

A
  1. Emax (Max effect) 2. C50: Concentration achieving 50% maximal drug effect 3. C: Unbound drug concentration
90
Q

Part of nephron where drug reabsorption occurs.

A

Distal convoluted tuble

91
Q

PK Sources of Drug tolerance

A

Increase or decrease in metabolic activity

92
Q

This can cause non-linearity

A

Saturation of drug metabolizing enzymes

94
Q

These transporters cause INTESTINAL EFFLUX. It takes out the drug molecule out of the blood stream and throw it back to the GIT. (2)

A
  1. MDR1 or PGP (P-glycoprotein) 2. BCRP
95
Q

Causes of Functional Adaptation (3)

A
  1. Desensitization of receptors 2. Up/ down regulation (feedback) 3. Precursor pool depletion
97
Q

T/ F: The magnitude of the apparent Vd does NOT always have a true anatomical or physiological interpretation because of the interactions that may occur in the body.

A

True

98
Q

The site of action and pathways of response could be immediate or prolonged due to ____

A

pharmacodynamic events or time-delays

100
Q

2 Assumptions of One Compartment Model

A
  1. Rapid equilibration of drug throughout the body (“well-stirred”) 2. First order elimination
100
Q

Refers to the functional adaptation of the effect. (Does the kinetic/ dynamic system change overtime?)

A

Stationarity

102
Q

Down side of Continuous IV infusion.

A

Titrate the drug and its effects

103
Q

This term refers to drugs metabolized or changed into another compound by the liver. It can be an active compound (could have adverse effect or toxicity) and can be further metabolized by the liver, or excreted.

A

Metabolites

104
Q

These (2) may drive the time-course and extent of DRUG EFFECTS.

A
  1. Total exposure 2. time-course of drug concentrations
106
Q

Drugs must cross membranes in order to reach their sites of action. The most common process is by ____.

A

passive diffusion

107
Q

This is the amount of time for the drug concentration fall by half.

A

half-life

108
Q

The elimination of drug is proportional to the drug concentration.

A

First order elimination

108
Q

This PK Medium contains cells and clotting factors. They are more difficult to work with.

A

Whole Blood

109
Q

The behavior of the drug in the body depends on (4)

A
  1. chemistry of the drug molecule 2. chemistry of the local environment 3. Physical properties of the local environment 4. Anatomy and physiology of the local environment.
110
Q

Route of Administration: Drug is administered at or near the site of its intended action. (there are chances of systemic distribution though)

A

Nonsystemic (Local) Use

112
Q

This refers to the time course of drug concentrations in the body.

A

Pharmacokinetics

113
Q

What happens when PGP or MDR-1 is active?

A

It moves drug from the blood stream back to the GIT. Therefore there is less exposure to the drug.

114
Q

This PK modesl view the body as a collection of compartments that have drug transfer between compartments.

A

Compartment model

115
Q

Co (initial concentration), can be seen that the fraction of the original concentration that remains is described by:

A

e, to the - kt

116
Q

This reflects that drugs may not get into every tissue to the same extent.

A

tissue permeability limitations

117
Q

This states that BOUND DRUG is generally not available for distribution, metabolism, or for exerting an effect in the body.

A

Free Drug Hypothesis

118
Q

The release of drugs happen at different intervals. There is continuous absorption of drugs.

A

Extended-release formulation.

119
Q

PD sources of Drug Tolerance

A

Increase or decrease in number of receptors

121
Q

Drug elimination can alternatively be described in the context of _____.

A

clearance

123
Q

Example of autoinducer drug.

A

Modafinil

124
Q

T/F: Many drugs are weak electrolytes. Weak acids or bases. Very few are strong electrolytes.

A

True

125
Q

Symbol for initial concentration.

A

Co

126
Q

Multiplier used in calculating Creatinine clearance in females.

A

.85

127
Q

Metabolism of drugs most occur in the

A

liver

128
Q

Passive diffusion depends on appropriate _____ in the membrane barrier components.

A

solubility

129
Q

What is the goal of pharmacogenomics?

A

to individualize therapy

130
Q

Type of drug release for oral sustained-release drugs.

A

Zero-order release or Infusion-like release

132
Q

For a drug substance to be available for absorption, it generally must be ____.

A

in solution at the site of absorption

133
Q

This is the estimate of kidney function.

A

Estimated creatinine clearance

134
Q

Drug excretion occurs in what organs in the body? (2)

A
  1. Kidneys (renal) 2. Gallbladder (biliary)
135
Q

The amount eliminated per unit time is dependent upon the amount present at that time.

A

First order elimination

137
Q

FYI: Protein Binding 1. Can be become saturated for some drugs 2. There can be multiple binding sites per protein molecule for some drugs.

A

:D

138
Q

Gives information about the time of the peak concentration.

A

Tmax

139
Q

Oral drugs can be absorbed at the gut wall and be metabolized due to high concentration of which enzyme?

A

Cytochrome P 450 - 3A4

140
Q

The peak concentration of IV Bolus occurs ____

A

right after administration of drug.

141
Q

In Mammillary models, the central compartment represents the (2)

A
  1. Vascular spaces 2. Any highly perfused, rapidly equilibrating tissues.
143
Q

Method used to measure estimated renal clearance

A

Cockcroft and Gault Method

144
Q

Drugs doses can enter the blood through (2)

A
  1. Extravascular dose (orally, transdermal, rectal, etc..) 2. IV dose
145
Q

Tolerance to Nitroglycerine develops within ___.

A

a day. Reminder: Have off periods during the day

146
Q

Polymorphisms in drug metabolizing enzymes may lead to different population who are ___ (3)

A
  1. Poor metabolizers 2. Extensive metabolizers 3. Ultrarapid metabolizers
147
Q

Name of the formal in calculating Drug Effect (E)

A

Hill Equation

148
Q

These are predictors of PK. This is how we individualized doses.

A

Covariates

149
Q

Referred to as unwanted safety risks.

A

Adverse effects

NUR 622: Adv. Pharmacology Lectures (7 decks)

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