Pharmacokinetics Flashcards

1
Q

ADME concept (4)

A

Absorption, Distribution, Metabolism, Excretion

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2
Q

This term describes what the body does to the drug.

A

Pharmacokinetics

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3
Q

What are the main steps of pharmacokinetics?

A

1.) absorption 2.) Distribution 3.) Elimination

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4
Q

This term describes when the drug is acting on the body

A

pharmacodynamics

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5
Q

What are the ways to administer drugs? (6)

A
  1. ) oral or rectal
  2. ) percutaneous
  3. ) intravenous
  4. ) intramuscular
  5. ) intrathecal
  6. ) Inhalation
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6
Q

How are drugs eliminated in the body? (5)

A
  1. ) urine
  2. ) feces
  3. ) milk, sweat
  4. ) expired air
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7
Q

What factors affect oral absorption? (4)

A
  1. ) Disintegration
  2. ) Drug in small particles
  3. ) Dissolution
  4. ) Drug in solution
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8
Q

What part of the body are drugs maximally absorbed?

A

small intestine

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9
Q

what makes the small intestine the best place for maximal absorption?

A

large surface area allows more blood to flow

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10
Q

What factors affect gastric emptying? (6)

A
  1. ) volume of meal
  2. )meal composition
  3. )viscosity,
  4. )osmotic pressure,
  5. ) position
  6. ) drugs
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11
Q

What factors slow gastric emptying?

A

high meal fat content, increased viscosity, increased osmotic pressure, opioids, anticholinergics, ethanol, bile salts and acidification

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12
Q

What factors influence drug absorption? (8)

A
  1. ) Molecular weight
  2. ) Blood flow
  3. ) solubility
  4. ) concentration
  5. ) Disintegration and dissolution
  6. ) partition coefficient
  7. ) transporters
  8. ) pH partition theory
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13
Q

What are the non-oral routes of drug administration? (6)

A
  1. ) sublingual (under the tongue)
  2. ) rectal
  3. ) pulmonary
  4. ) subcutaneous
  5. ) intramuscular
  6. ) intravenous
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14
Q

What types of non-oral routes of drug administration are perfusion- rate limited?

A

subcutaneous and intramuscular

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15
Q

phenomenon of drug metabolism when the drug concentration is greatly reduced before entering systemic circulation

A

First pass effect

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16
Q

the fraction of lost drug during the process of absorption related to liver and gut wall clearance

A

first pass

17
Q

How do you recognize a drug with a first pass clearance?

A

Look at the F value

18
Q

If F=1 what is its first pass clearance?

A

there is NO first pass clearance

19
Q

True/False: If a drug has a much larger oral dose than intravenously, there is a first pass clearance.

A

TRUE

20
Q

How can you describe drug absorption? (2)

A
  1. ) the EXTENT or total amount of drug entering systemic circulation
  2. ) the RATE or how quickly the drug enters the systemic circulation
21
Q

Rate and extent to which the active ingredient or active moiety is absorbed from a drug product and which becomes systemically available

A

Bioavailability

22
Q

How would you determine rate if given a graph?

A

Tmax and Cpmax values

23
Q

How would you determine extent if given a graph?

A

AUC (area under the curve)

24
Q

A higher peak on a graph of generic vs. brand would indicate ____.

A

a higher/faster rate of absorption

25
Q

True/False: A higher AUC yields a higher extent or total amount of drug absorbed.

A

TRUE

26
Q

Fraction of drug administered which becomes systemically available. Comparing an oral dose to and intravenous dose of a drug.

A

Absolute Bioavailability

27
Q

If a drug is not absorbed at all, what would the absolute bioavailability be?

A

0

28
Q

If a drug has a F= <1 value what has to happen?

A

a larger oral dose has to be given compared to the intravenous dose

29
Q

used to determine bioequivalence or when 2 orally administered drugs are being compared

A

relative bioavailability

30
Q

represents how extensively the drug distributes in the body

A

volume of distribution (Vd)

31
Q

What would a drug with a large volume of distribution indicate?

A

they are bound, and stored somewhere and lipid soluble. They do NOT stay in the blood.

32
Q

What are the factors that affect drug distribution between body compartments? (5)

A
  1. ) tissue differences contribute to differences in blood perfusion
  2. ) presence of disease states
  3. ) degree of drug lipid solubility
  4. ) extent of drug protein binding
  5. ) regional differences in pH
33
Q

What determines the size of the loading dose?

A

concentration and volume of distribution

34
Q

allows you to rapidly achieve the therapeutic concentration of a drug

A

loading dose

35
Q

If a drug with a F= 0.5 value is given, what effect would this have on the loading dose?

A

the loading dose would be TWICE as much than an IV.

36
Q

True/False: Loading dose is dependent on clearance.

A

FALSE; not dependent on clearance