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Test 4 MCM Leesy > B2.070 - Pharmacokinetics > Flashcards

B2.070 - Pharmacokinetics Flashcards

1
Q

What is acetaminophen

A

Analgesic

Antipyretic (anti fever)

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2
Q

How many hospitalizations and deaths each year due to Tylenol

A

80,000 hospitalizations

500 deaths

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3
Q

What is the therapeutic index

A

The difference in amount it takes to achieve therapeutic effect and the amount it takes to kill you

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4
Q

Types of effects and intensity of effects are proportional to what

A

Active drug concentration at its sites of action

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5
Q

How do drugs get to the site of action? (4 steps)

A 
ADME
A- Absorption
D - Distribution
M- Metabolism
E - Excretion
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6
Q

What are the types of absorption

A

Passive diffusion
Carrier mediated transport
Facilitated diffusion
Active transport

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7
Q

What is passive diffusion

A

Direct passage through lipid bilayers of cell membrane driven by a concentration gradient
Dependent on size and chemical properties

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8
Q

What is the most common form of drug absorption

A

Passive diffusion

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9
Q

How does carrier mediated transport work

A

Transporters facilitate movement of molecules into tissues

Influx or efflux

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10
Q

Characteristics of all carrier mediated transport

A

Structural selectivity
Competition by similar molecules
Saturable

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11
Q

What is facilitated diffusion

A

A type of carrier mediated transport
Facilitates passage of polar or charged molecules
Does not require ATP
Involves movement of a drug down a concentration gradient

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12
Q

What is active transport

A

Energy dependent carrier mediated transport

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13
Q

What is the difference between primary and secondary active transport

A

Primary - transport coupled to ATP hydrolysis

Secondary - cotransport substrate down a gradient

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14
Q

What is the most rapid mode of membrane permeation

A

Active transport

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15
Q

What are important sites of active transport

A 
Enterocytes
Hepatocytes
Neuronal membranes
Renal tubular cells
Blood brain barrier
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16
Q

What is most absorption of acetominophen

A

Passive diffusion

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17
Q

How long does it take to get maximum plasma concentrations of acetominophen

A

T max = .5-1 hr

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18
Q

What is the bioavailability of acetominophen

A

.7-.9 = F

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19
Q

What is bioavailability

A

Difference between amount of drug administered and how much actually gets into the blood stream

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20
Q

What is distribution

A

Process of getting out of the blood stream and into the organs

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21
Q

What types of drugs stay in blood

A

Very large molecules (proteins), high charged molecules (heparin)

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22
Q

What types of drugs stay in extracellular water

A

Larger, very polar, water soluble (mannitol)

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23
Q

What types of drugs stay in total body water

A

Smaller, water soluble (ethanol, acetominophen)

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24
Q

What types of drugs go to adipose tissue

A

Lipid soluble (diazepam)

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25
Q

What types of drugs go to bone and teeth

A

Ions, chelates

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26
Q

What is the apparent volume of distribution (Vd)

A

Compartment where a drug appears to distribute

27
Q

What is the extrapolated concentration of a drug in plasma at time 0 after equilibration (Co)

A

Co=amount of drug / Vd

28
Q

What is the equation for Vd

A

Vd=amount of drug/Co

29
Q

What compartment has the smallest Vd

A

Plasma water

30
Q

What compartments have the highest Vd

A

Tissues

31
Q

How can Vd exceed the actual volume of total body water?

A

If the concentration in any compartment/tissue is higher than Cp then the V*C production will be higher

32
Q

What is Vd really a measure of

A

The relative distribution between plasma and the rest of the body

33
Q

What is the importance of Vd qualitatively

A

Indicates ratio of plasma concentration to concentrations in tissues

34
Q

Which is more useful a qualitative use of Vd or quantitative

A

Quantitative

35
Q

What are the quantitative uses for Vd

A

Half life determination

Supports determination of dose required to achieve target drug concentration

36
Q

How do you calculate how much drug is left in a patient

A

Plasma concentration X Vd

37
Q

Clearance and Vd are inherent properties of a drug what do they represent

A

CL - primary parameter for elimination

Vd - primary parameter for distribution

38
Q

What are the secondary parameters derived from the primary parameters

A 
KeI = CL/Vd = elimination rate constant
T1/2 = .693xVd/CL = Half life
39
Q

How do you calculate the amount of drug in the body at any given time

A

Plasma concentration x Vd

40
Q

Where does acetaminophen distributes to

A

Total body water

41
Q

Efficient excretion of drugs requires what

A

Water solubility

42
Q

What is phase 1 of drug metabolism

A

Introduce or unmask a functional group
Relatively few atoms involved (usually 1-3)
Three major reaction classes (oxidation, reduction, hydrolysis)

43
Q

What is phase 2 drug metabolism

A

Synthetic (conjugation) reaction
Addition of molecules
Require specific functional groups

44
Q

what contribute to first pass affect

A

High activities in enterocytes

45
Q

What’s an example of an adverse reaction due to metabolizing of a drug

A

Acetaminophen induced hepatotoxicity

46
Q

What are the metabolic pathways of acetominophen

A
  1. Glucuronidation (non toxic)
  2. NAPQI - toxic if not GSH involved
  3. Sulfation (non toxic)
47
Q

Intestinal enterocytes transporters modulate

A

Absorption

48
Q

What role does ATP driven transport have in metabolism of acetominophen

A

Secretion of glucuronide and sulfate conjugated from hepatocyte into bile or blood

49
Q

Amount excreted by any process per unit time is proportional to

A

Rate of elimination for that process and concentration of drug in plasma

50
Q

Drug concentration in the plasma is inversely proportional to the volume of distribution so drugs with…

A

Larger volumes of distribution are eliminated slower

Lower volumes of distribution will be eliminated faster

51
Q

What are the major pathways of excretion

A

Renal

Hepatic, biliary

52
Q

How is acetominophen excreted

A

In the ruin

53
Q

How is acetominophen excreted in the urine

A

Glutathione conjugate is further metabolized and excreted in urine as cysteine conjugate and mercapturic acid

54
Q

How do you irreversibly eliminate a drug from systemic circulation

A

Metabolism

Excretion

55
Q

What’s the equation for elimination rate

A

Elimination rate = CL x Concentration

56
Q

What’s the unit of measurement for elimination rate

A

Mg/hr

57
Q

What’s the equation for elimination rate constant

A

Kei = CL/Vd

58
Q

What is the equation for half life

A

T1/2 = .693 x Vd/CL

59
Q

What is the equation for clearance

A

CL = rate of elimination from the body/plasma concentration

60
Q

Total body clearance is what

A

The sum of hepatic clearance and renal clearance

61
Q

Most drugs follow what

A

First order kinetics

62
Q

Zero order elimination rate =

A

K

63
Q

First order elimination rate =

A

K[drug]

64
Q

In first order kinetics what is rate limiting

A

Concentration

Test 4 MCM Leesy (6 decks)

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