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Abbey MSII Unit 1 pt 2 > Pharm 4. > Flashcards

Pharm 4. Flashcards

1
Q

What is the most important route of elimination of drug or metabolites?

A

renal excretion

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2
Q

Amount drug excreted = ?

A

(amount entering tubule) - (amount reabsorbed) OR (glomerular filtration + active tubular secretion) - (passive reabsorption + active reabsorption)

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3
Q

How do drugs enter the nephron?

A

glomerular filtration (only free drug molecules filtered), and active tubular secretion

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4
Q

When does saturation for active tubular secretion happen?

A

at therapeutic doses or with over doses

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5
Q

How doe saturation change the process?

A

from a 1st order to a zero order process

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6
Q

What is the equation for a first order secretion?

A

V = Vmax [D] / Km + [D]

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7
Q

What is the equation for a zero order secretion?

A

V = Vmax

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8
Q

How are drugs reabsorbed?

A

passive reabsorption (esp lipid soluble) and active reabsorption

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9
Q

What type of drug is most easily eliminated?

A

water soluble drugs

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10
Q

What do lipid soluble drugs need to be excreted?

A

phase I and sometimes phase II transformations

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11
Q

How can renal excretion be enhanced?

A

forced diuresis or manipulate the pH of the ruin to trap ionized drug in urine (higher pH will trap ionize a lipid soluble drug)

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12
Q

What is commonly used to alkalinize the urine?

A

sodium bicarbonate

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13
Q

What are other routes of drug elimination?

A

bile, lung, sweat, saliva, tears, breast milk

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14
Q

What are the methods of elimination of drugs from site of action?

A

redistribution, biotransformation, excretion

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15
Q

Total clearance = ?

A

clearance metabolic + clearance renal

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16
Q

How is total clearance affected in hepatic disease?

A

reduced, esp metabolic (reduced in renal as well)

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17
Q

What determines the elimination rate constant (ke) for a drug?

A

rate limiting step

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18
Q

What are 6 factors influencing clearance?

A
  1. body surface area 2. protein binding 3. cardiac output 4. renal function 5. hepatic function 6. blood flow to systemic organs
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19
Q

inulin

A

used to estimate glomerular filtration rate (all is filtered, none reabsorbed or excreted)

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20
Q

glucose

A

all should be reabsorbed - effectiveness of reabsorption

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21
Q

PAH

A

approximates renal blood flow - all is filtered and secreted

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22
Q

What can be determined using the volume of distribution and clearance?

A

how often to dose a drug, what size dose to give, how long to expect a dose to last, when to re-dose a drug to sustain effect

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23
Q

On the logCp/time graph, what is alpha and beta respectively?

A

alpha: distribution (leaving volume initial); beta: elimination (liver/kidney/both)

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24
Q

ka

A

absorption rate constant

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25
Q

ke

A

elimination rate constant

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26
Q

How is ke determined?

A

by the rate limiting step in clearance (either metabolic or renal)

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27
Q

What is happening at max intensity?

A

absorption and elimination of drug are equal

28
Q

How are zero order drugs related to absorption rates?

A

carrier mediated with saturated carrier protein at Vmax - not sensitive to drug concentration

29
Q

How are first order drugs related to absorption rates?

A

absorption is sensitive to drug concentration

30
Q

What do absorption kinetics tell us?

A

how much dose to give

31
Q

What equation describes zero order rate? What is the slope?

A

Ct = k’a t (an amount absorbed per unit time) slope = ka (straight line)

32
Q

What equation describes first order rate? what is the slope?

A

Ct = M/Vd X (1 - e ^-Ka t) (a proportion of unit time) slope = log slope

33
Q

zero order elimination

A

an amount per unit time - is saturated (at Vmax)

34
Q

What is the danger with zero order elimination?

A

have to be careful with toxicity - small changes can make a drug toxic

35
Q

What is an example of a drug with zero order elimination?

A

alcohol - .02 eliminated an hour

36
Q

When Ct

A

first order rate

37
Q

When Ct&raquo_space; Km

A

zero order rate

38
Q

Half life applies to……

A

first order elimination kinetics

39
Q

T1/2 equation

A

t1/2 = 0.693 / ke —> A CONSTANT NUMBER THAT CAN BE LOOKED UP IN A BOOK!

40
Q

If clearance of a drug is large then the half life is….

A

small

41
Q

Steady state

A

drug enters a compartment at a constant rate and is eliminated in a manner proportional to the concentration in the Vd. when the elimination increases to equal the rate of entry = steady state

42
Q

How many half lives does it normally take to reach steady state?

A

4

43
Q

Single doses casues what?

A

no steady state - dose interval is much greater than t 1/2

44
Q

Repeated administrations causes what?

A

steady state (plateau) level - dose interval is less than or equal to t 1/2

45
Q

Does route of administration affect Css average?

A

NO - you still need 4 half lives to get to steady state

46
Q

Does dose affect time to achieve steady state?

A

NO SHUT UP

47
Q

Fast elimination rate = ?

A

fast to steady state (slow elimination rate = slow to steady state)

48
Q

How does achievement of steady state compare to elimination?

A

mirror image (takes 4 half lives to eliminate from steady state

49
Q

What is the loading dose?

A

rapid attainment of therapeutic plasma level (not steady state) - need maintenance doses to keep at steady state

50
Q

Iatrogenic

A

predictable adverse drug reaction - may be dose dependent

51
Q

Spontaneous

A

not predictable - not dose dependent. includes allergies (once they occur once though they become predictable) and idiosyncratic

52
Q

tolerance

A

decreased response to continued administration due to receptors and/or metabolism

53
Q

cumulation

A

drug administered faster than it can be eliminated

54
Q

ED50

A

effective dose in 50% of the population

55
Q

TD50

A

toxic dose in 50% of the population

56
Q

LD50

A

lethal dose in 50% of the population

57
Q

Margin of safety

A

TD50 - ED50

58
Q

Therapeutic Index

A

TI = TD50 / ED50

59
Q

What is the ideal clinical for therapeutic index?

A

TD 1 / ED 99

60
Q

What is a good therapeutic index?

A

larger the number the better - more doses between therapeutic window and toxicity

61
Q

What will changing the pH or other electrolytes do?

A

alter excretion or protein binding

62
Q

How is excretion changed?

A

active transport inhibitors or simple competition for a transporter

63
Q

How is metabolism changed?

A

induction or inhibition

64
Q

What does protein binding and displacement have the potential of causing?

A

toxicity

65
Q

How is absorption changed/

A

charcoal binds drug molecules - decreases absorption

66
Q

What are examples of direct molecular drug interactions?

A

antibiotics and calcium

Abbey MSII Unit 1 pt 2 (21 decks)

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