Week 1 (Cont) Flashcards

PHARMACOKINETICS

1
Q

The study of the bodily processes that affect the movement of a drug in the body.

A

pharmacokinetics

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2
Q

What are the four fundamental pathways of drug movement in the body?

A

Absorption, distribution, metabolism, and excretion.

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3
Q

What must a drug reach to cause a therapeutic response?

A

Adequate concentrations in the blood.

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4
Q

What is the peak serum concentration?

A

The highest amount of drug in the blood after administration.

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5
Q

What is the half-life of elimination (t1/2)?

A

The time it takes for the serum concentration of a drug to fall by one half.

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6
Q

The transfer of a drug from its site of administration to the bloodstream.

A

absorption

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7
Q

What factors affect drug absorption?

A
  • Route of administration
  • Formulation and chemical properties of the drug
  • Physiologic factors
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8
Q

The relationship between the drug dose and the amount ultimately delivered to the bloodstream, expressed as a percentage?

A

bioavailability

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9
Q

The significant metabolism of a drug during its first passage through the liver after oral administration?

A

first-pass effect

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10
Q

What is the primary site of drug absorption after oral administration?

A

The small intestine.

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11
Q

What can significantly impair drug absorption?

A

Removal of sections of the small intestine.

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12
Q

How does blood flow affect drug distribution?

A

Higher blood flow to vital organs results in greater drug delivery to those organs.

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13
Q

A significant barrier that protects brain tissue from many drugs, requiring drugs to be small and lipid-soluble to penetrate.

A

blood-brain barrier

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14
Q

What is the role of albumin in drug distribution?

A

Albumin binds to drugs in the bloodstream, affecting their distribution into tissues.

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15
Q

Fill in the blank: The time it takes for the serum concentration of a drug to fall by one half is called the _______.

A

half-life.

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16
Q

True or False: Liquid formulations of drugs require dissolution before absorption.

17
Q

What are factors that can reduce drug bioavailability after oral administration?

A
  • Acid environment in the stomach
  • Presence of food
  • Metabolism in the liver
18
Q

What affects drug distribution into tissues?

A

Binding to plasma proteins

Only unbound drug can penetrate tissues and exert activity.

19
Q

What role does albumin play in drug administration?

A

Acts as a reservoir of an administered drug

Albumin helps maintain a balance between free and bound drug.

20
Q

What happens when albumin levels are low in patients using highly protein bound drugs?

A

May lead to toxicity due to increased free drug

Fewer binding sites result in more unbound drug available.

21
Q

How do two highly protein bound drugs interact?

A

They compete for binding sites on albumin

The drug with greater affinity binds first, affecting the availability of the second drug.

22
Q

What factors can affect the apparent volume of distribution (Vd) of a drug?

A

Body composition, cardiac decompensation, age

These factors influence the appropriate drug dosage.

23
Q

What is the formula for calculating the volume of distribution?

A

Vd = Dose / Cp

Where Cp is the serum concentration.

24
Q

What are the three compartments of total body water?

A
  • Intracellular fluid
  • Extracellular fluid
  • Plasma volume

Total body water is about 60% of body weight.

25
Why do small, highly lipophilic drugs have a large apparent volume of distribution?
They tend to distribute widely in body tissues ## Footnote In contrast, hydrophilic drugs remain in the circulatory system.
26
Why is dosing in infants and children different from adults?
Children have different body composition and organ maturity ## Footnote They have higher water content and lower muscle and fat.
27
The process of chemical changes for easier excretion?
biotransformation ## Footnote This is also known as metabolism.
28
What is the major site for drug metabolism?
The liver ## Footnote Other tissues may also contribute to drug biotransformation.
29
What happens to highly fat-soluble drugs in the kidneys?
They are reabsorbed instead of being excreted ## Footnote These drugs must be metabolized to water-soluble forms first.
30
What are the two types of metabolic processes drugs undergo in the liver?
* Oxidation-reduction reactions * Conjugation reactions ## Footnote Most drugs undergo one or both types of reactions.
31
A common conjugation reaction making drugs more water-soluble
glucuronidation ## Footnote It aids in excretion by the kidneys.
32
An inactive compound converted to an active form by metabolism?
prodrug ## Footnote Example: Fosphenytoin is a prodrug of phenytoin.
33
How does age affect drug metabolism?
Organ function declines with age ## Footnote Elderly may poorly tolerate drugs requiring metabolism.
34
What is steady state in drug dosing?
The point where drug intake equals drug elimination ## Footnote Drug levels remain constant unless changes occur.
35
What factors affect drug excretion?
* Liver function * Kidney function * Age ## Footnote Reduced function can require dosage adjustments.
36
Why is it important to monitor steady state serum drug levels?
To ensure appropriate drug response ## Footnote Adjustments may be needed based on therapeutic effects.
37
What complications arise from reduced kidney or liver function?
Drugs may accumulate in the body ## Footnote This can lead to toxicity and requires careful dose selection.
38
What is the role of the kidneys in drug elimination?
Filter blood and create urine for waste removal ## Footnote Non-bound drug molecules are filtered out into the glomerular filtrate.