Pharmacokinetics - Quiz 1 Flashcards

Quiz 1

1
Q

Absorption

A

Bioavailability (F): % of medication that reaches systemic circulation

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2
Q

What is the bioavailability of IV/IM/SQ meds?

A

F=1 or 100%

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3
Q

If bioavailability for oral Synthroid is 50%, and the dose is 100 mcg, what would your IV dose be?

A

Bioavailability F=.5
100X.5

50 mcg

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4
Q

What does an increase in surface area do to absorption?

A

the more surface area, the more likely it will be absorbed into the body

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5
Q

Where does meds given via SL/buccal drain?

A

Vena Cava

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6
Q

For meds to pass through membrane under tongue, they MUST be

A

highly lipid soluble and potent

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7
Q

When a drug is absorbed across the GI membranes, it enters the hepatic portal system which carries molecules directly to the

A

Liver

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8
Q

Anything given topically needs to be _________ because it needs to cross the skin barrier

A

lipophilic

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9
Q

Temperature does what to absorption?

A

Increases absorption

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10
Q

Why does inhalation cause a rapid effect?

A
  • D/T the large surface area
  • Avoids first pass
  • Local site of action
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11
Q

IV injections have what effect?

A

Potentially immediate

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12
Q

IV/IM/SQ is absorbed through which type of diffusion?

A

Simple diffusion

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13
Q

What is volume of distribution?

A

Size of compartment necessary to account for the total amount of drug in the body if it were present throughout the body at the same concentration found in the plasma

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14
Q

Average adult plasma is how many liters?

A

about 3

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15
Q

What is compartment 1?

A

systemic system

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16
Q

What is compartment 2?

A

highly vascular organs

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17
Q

What is compartment 3?

A

fatty compartment

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18
Q

What do you need to be in order to reach compartment 3?

A

Highly lipophilic

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19
Q

If albumin has bound up your medication molecule, what does that mean?

A

You will see less of an effect

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20
Q

Low albumin levels will cause what in terms of distribution?

A

It will cause more med floating around, hight potential for toxicity. (albumin is a binder for medication)

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21
Q

Fat tissue binds to

A

lipid soluble drugs

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22
Q

Bones bind to

A

tetracyclines

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23
Q

Heart muscle binds to

A

Digoxin

24
Q

In order to cross the blood brain barrier, you need to be

A

lipophilic

25
Q

What meds is a fetus exposed to?

A

nearly all medications a mother takes

26
Q

What are P-glycoproteins?

A

a giant class of transport proteins all over body that requires ATP

27
Q

What is passive diffusion?

A

Moves through lipid bilayer with ease, no transport or energy needed.

28
Q

What is facilitated diffusion?

A

Goes from high concentration to low concentration using carrier protein to get through lipid bilayer. No energy needed.

29
Q

What is aqueous channels?

A

Where water and electrolytes can move through. No energy or carrier needed.

30
Q

What is active transport?

A

Move against concentration gradient via a carrier and ATP

31
Q

What is Metabolism

A

Breakdown for ease of elimination

32
Q

Metabolism may make a drug become a ________?

A

Prodrug

33
Q

What is a prodrug?

A

A drug not administered in active form, needs to be metabolized before works. (e.g. propofol)

34
Q

What is phase 1 metabolism?

A

Induce or expose a functional group on the parent compound.
Generally lose activity, rare instances of preserved.
Readily eliminated.

35
Q

What is phase 2 metabolism?

A

Conjugation reactions.

Links parent compound OR phase I metabolite with a functional group via covalent linkage.

36
Q

Most reactions are driven by what?

A

enzymes

37
Q

CYPs reaction occurs in which phase of metabolism?

A

Phase 1 metabolism

38
Q

What does inhibition of an enzyme do?

A

Will keep the enzyme from working properly.
Ability to increase amount of parent compound.
Leads to toxicity.

39
Q

What does inductions of an enzyme do?

A

Will enhance the capability of the enzyme.
Ability to quickly metabolize the parent compound.
Levels dropping faster.

40
Q

Name some CYP inhibitors

A

amiodarone, Fluconazole, Ketoconazole, SSRIs, methadone

41
Q

Name some CYP inducers

A

Rifampin, smoking, alcohol

42
Q

What factors affect metabolism?

A

Genetics -
Environmental - diet
Disease Factors
Age and sex - As we get older, CYP enzymes begin to fail
Do not have full set of CYP enzymes until 25

43
Q

In which forms can a medication be eliminated?

A

Unchanged (parent molecule, metabolite or mixed

44
Q

Is it easier to eliminate polar/hydrophillic compounds or lipophillic compounds

A

polar/hydrophilic compounds

45
Q

What is the primary excretory organ in the body

A

the kidneys

46
Q

Glomerular filtrations eliminates

A

unbound medication

47
Q

Active tubular secretion eliminates

A

P-gp and other transport proteins

48
Q

Passive tubular reabsorption processes

A

Weak acids and bases via concentration gradients

49
Q

What is first order kinetics?

A

As the concentration of the drug in the plasma decreases, less drug is available at the site of metabolism or excretion, and thus as the concentration decreases, the amount being eliminated is also decreasing. Same percentage % always being excreted.

50
Q

What is zero order kinetics?

A

Seen when the metabolism or excretion processes become saturated. A constant amount or number of drug molecules are eliminated per unit time

51
Q

What is elimination rate?

A

Fraction or % of the total amount of drug in the body removed per unit of time. This equation can only be done if elimination rate is by first order process.

52
Q

What can cause an increased half life for a med that is eliminated primarily through the liver?

A

hepatic disorders: cirrhosis, liver failure

53
Q

What is pharmacokinetics?

A

how drug molecules are handles in the body

54
Q

What are the properties of pharmacokinetics?

A

Absorption
Distribution
Metabolism
Excretion

55
Q

What factors can effect absorption?

A
  • Dissolution and absorption characteristics
  • Route
  • Stability in GI
  • Metabolism prior to blood stream