pharmacokinetics Flashcards

1
Q

renal excretion terminates actions of what drugs?

A

small hydrophilic
fully/nearly fully ionized at physiological ph
not protein bound

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2
Q

most pharmacologically active drugs are..

A

lipophilic
unionized / partially ionized
bound to plasma proteins

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3
Q

what is the primary determinant of duration and intensity of drug action?

A

rate of drug metabolism

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4
Q

drug metabolism mainly occurs where?

A

liver in er

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5
Q

what other organs can also metabolize substances?

A
gi mucosa = lower bowel 
kidneys 
lungs 
nasal mucosa 
skin
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6
Q

first pass effect

A

drugs are extensively metabolized during initial pass though the liver

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7
Q

what enzymes are involved in phase I ?

A

CYP450

oxidases

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8
Q

what is the most common phase ii rxn?

A

glucuronidation

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9
Q

conjugation using what?

A

glucorunic acid
sulphate
glutathione

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10
Q

what are examples of phase ii rxns?

A

glucuronidation

methylation

sulfation

n-acetylation

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11
Q

codeine, a prodrug, is demethylated to produce

A

morphine

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12
Q

inducers of metabolism

A

increase synthesis of p450 and reduce degradation

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13
Q

inhibitors of metabolism

A

bind to cytochrome oxidase and inhibit metabolism of other drugs

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14
Q

CYP2D6 affects

A

beta blockers –> alter effect

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15
Q

CYP2C9

A

warfarin –> change dose

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16
Q

CYP2C19

A

omeprazole –> variable response in peptic ulcers

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17
Q

what are the most imp routes of drug elimination?

A

urine and feces

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18
Q

what drugs follow zero order kinetics?

A

ethanol and aspirin

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19
Q

ethanol is excreted in …

A

sweat

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20
Q

what’s penicillin?

A

an acidic antibiotic

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21
Q

how are penicillin and aspirin excreted?

A

via proximal tubular secretion (renal excretion)

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22
Q

what is used in the excretion of penicillin and aspirin?

A

anion transport system

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23
Q

what may prolong effects of penicillin?

A

competition for secretion with probenecid

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24
Q

what is aspirin?

A

acidic salicylate

25
Q

what is given to prevent gout?

A

aspirin is given to compete with uric acid during distal tubular active reabsorption

26
Q

drug clearance

A

apparent volume of blood that is cleared of drug per time period

27
Q

clearance equation

A

U x V / P

28
Q

clearance equation what everything stands for

A
U = urine drug concentration
V = rate of urine flow
P = plasma drug concentration
29
Q

lamda equation

A

drug in lung blood / drug in lung air

30
Q

what does low / small lambda mean?

A

short DOA

rapid elimination

31
Q

what does high/large lambda mean?

A

long DOA

slow elimination

32
Q

rate of elimination equation

A

plasma drug concentration x clearance

33
Q

general rate equation

A
rate = k x C ^n
k = rate constant 
n = order if zero = 0 if first = 1
34
Q

one compartment model

A

body is a single compartment
drug is rapidly distributed
elimination = first order

35
Q

Vd equation

A

Vd = dose / Co

36
Q

Clearance equation

A

CL = Vd x ke

37
Q

t 1/2 equation

A

0.0693 / ke

38
Q

ka aka

A

absorption

39
Q

ke aka

A

elimination

40
Q

graph of log plasma drug concentration vs time in one compartment model when drug given via IV dose looks like ?

A

its linear and negative slope

41
Q

graph of log plasma drug concentration vs time in one compartment model when drug given via oral dose looks like ?

A

first it rapidly increases ( bc being absorbed) then its linear with a negative slope

42
Q

true or false. t 1/2 depends of dose

A

false it doesn’t depend on dose

43
Q

in 2 compartment model what are the two phases and what do they rep?

A

S phase = elimination rate constant

F phase = distribution rate constant

44
Q

at steady state what’s true about about dosing rate?

A

dosing rate = elimination rate

45
Q

dosing rate equation

A

dosing rate = clearance x Css ( steady state concentration)

46
Q

for drugs with first order elimination what does the time to reach Css depend on?

A

half life of elimination

47
Q

Css is a function of what?

A

dose
dosing interval
clearance

48
Q

how many half lives to reach Css 94-97%?

A

4-5

49
Q

infusion rate equation

A

CL x Css ( unit = mg/min)

50
Q

dosing rate equation ( maintenance dose)

A

clearance x desired plasma concentration

51
Q

kinetics for multiple iv ( iv bolus)

A

dose / T = CL x Css

52
Q

kinetics after multiple oral administration

A

dose x f ( bioavailability) / T = CL x Css

53
Q

maintenance dose equation

A

CL x Css x T

54
Q

loading dose equation

A

loading dose = vd x Css

55
Q

non compartmental clearance eq

A

cl = dose / auc or cl = Vd x kel

56
Q

non compartmental t1/2 eq

A

0.693 / k el

57
Q

non compartmental Vd eq

A

2

(1) dose / Co
(2) CL / kel

58
Q

non compartmental bioavailablity eq

A

auc oral / auc IV x 100