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PBL PY2 Fall > HTN PK > Flashcards

HTN PK Flashcards

1
Q

which CCB has the longest half-life?

A

amlodipine (33hrs)

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2
Q

which CCB has the highest F?

A

amlodipine (64%)

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3
Q

what is the issue with short-acting nifedipine?

A

cause major fluctuations in BP due to quick inset and offset and this can lead to things like MI and stroke

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4
Q

most CCBs are metabolized by what enzymes?

A

CYP3A4 and CYP3A5

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5
Q

t/f most CCBs show stereoselective PK

A

t

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6
Q

which CCBs have active metabolites?

A

diltiazem and verapamil

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7
Q

why does nifedipine not show stereoselective PK?

A

it is achiral

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8
Q

what is stereoselective metabolism?

A

preference of drug metabolizing enzymes for one enantiomer over the other

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9
Q

stereoselectivity influences the degree of ___

A

hepatic first pass F and rate of metabolism

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10
Q

for most CCBs, which enantiomer is greater?

A

R

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11
Q

verapamil and diltiazem and its metabolites are potent inhibitors of ___ and ___

A

CYP3A4 and PGP

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12
Q

formula for clearance

A

dose/AUC

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13
Q

which antibiotics do CCBs have a tendency to interact with?

A

macrolides (erythromycin and clarithromycin, not so much azithromycin)

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14
Q

most ACE-I have ____(high/low) protein binding

A

low

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15
Q

most ACE-I have low Vd, except ___

A

linsinopril

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16
Q

the fraction unbound (Fu) is expressed as the ration of _____

A

concentration of unbound drug to the concentration of total drug

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17
Q

give 2 examples of things that can influence the Fu

A

drugs and disease state

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18
Q

list 7 things that can affect drug distribution and protein binding

A
  1. physiochemical properties of drug (lipid solubility, ionization, pka)
  2. pH differences of biological fluids (affects permeability)
  3. blood flow through organs
  4. drug transporters and efflux pumps
  5. extent of protein binding
  6. amount of drug-binding proteins which can be affected by liver dx
  7. Binding inhibitors and drugs (may displace or alter conformation)
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19
Q

what is Vd?

A

a hypothetical volume with no physiological or anatomical meaning. It is a characteristic PK parameter of a drug indicating distribution between plasma and other binding sites where drug is distributed

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20
Q

how is Vd calculated?

A

Dose/plasma drug concentration (free and unbound)

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21
Q

how is Vd calculated for an IV drug?

A

amount of drug in body / plasma drug concentration

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22
Q

if a drug distributes well to tissues, it will have a ___(large/small) Vd?

A

large

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23
Q

if a drug is bound to plasma proteins but not to tissue proteins, the Vd will be ____ (small/large)

A

small

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24
Q

if a drug is highly bound to tissue proteins, the Vd will be ____ (small/large)

A

large

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25
Q

what are 3 applications of Vd in practice?

A
  1. knowing where drug is in the body
  2. calculation of dose and amount in body
  3. dose adjustment
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26
Q

how is the amount fo drug in the body (dose) calculated?

A

concentration x Vd

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27
Q

most ACE-I are prodrugs except ___ and ___

A

captopril and linsinopril

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28
Q

what type of prodrugs are ACE-I, how are they activated?

A

ester-prodrugs; converted by esterases like CES1/2 in the liver

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29
Q

most active metabolites of ACE-I are inactivated by ____

A

UGTs in the kidneys, the CYPs are not involved

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30
Q

is linsinopril metabolized?

A

no, it is excreted unchanged in the urine

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31
Q

what is the effect of ACE-I in patients with renal dx?

A

have a large, unpredictable increases in AUC and since ACE-I also get excreted by the liver, the amount excreted in the feces will increase

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32
Q

what did the FDA recommend for the trough to peak ratio?

A

the placebo corrected trough effect should be at least one-half of the placebo corrected peak effect (T:P more than 50%)

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33
Q

which 3 ACE-I exhibit T:P>50%?

A

fosinopril, ramipril, trandolapril

34
Q

which ARBs are prodrugs?

A

losartan and olmesartan

35
Q

how is losartan turned into its active EXP3174 form?

A

metabolized by CYP2C9 through an oxidative reaction that converts OH group to an acid group

36
Q

do ARBs show stereoselective pk?

A

no, they dont have a chiral center

37
Q

most ARBs are metabolized by which enzyme?

A

CYP2C9

38
Q

most ARBs have a high ___

A

hepatic peak extraction ratio

39
Q

out of ACE-I and ARBs, which have a higher protein binding?

A

ARBs

40
Q

out of ACE-I and ARBs, which has fewer ADRs in end-stage renal disease?

A

ARBs (bc they are more hepatically cleared?)

41
Q

which 2 ARBs have the least renal excretion?

A

irbesartan and telmisartan

42
Q

the ocurrence and extent of CNS effects of B blockers depends on the ___ of the B blocke

A

lipophilicity

43
Q

which B blocker has the highest lipophilicity?

A

propranolol

44
Q

beta blockers are metabolized by what enzymes?

A

various CYP enzymes

45
Q

do B blockers have stereselective metabolism?

A

yes

46
Q

most beta blockers have ___(high/low) hepatic extraction ratio

A

high

47
Q

why are only a fraction of diuretics filtred by the glomerulus?

A

they are highly protein bound to plasma proteins

48
Q

do OAT transport acids or bases

A

acids

49
Q

loop diuretic and thiazides are secreted in the ___

A

tubules

50
Q

thiazide and thiazide diuretics other than chlorothiazide have ___ (high/low) oral F

A

high

51
Q

how are thiazide and like diuretics excreted?

A

mostly unchanged in the urine

52
Q

high concentrations of thiazides is attained in the ___ fluid

A

luminal

53
Q

most thiazides are weak __ (acids/bases)

A

acids

54
Q

glomerular filtration is a passive process that depends on what 3 things?

A
  1. protein binding (unbound drugs only)
  2. molecular size (filtered when MW <500)
  3. number of functional nephrons
55
Q

lipophillic drugs are absorbed ____(actively/passively) in the tubules

A

passively

56
Q

for weak acid drugs, what is the effect of pH on their tubule reabsorption>

A

higher pH increases the ionized component and increases drug excretion

57
Q

for weak bases, what is the effect of pH on their tubule reabsorption?

A

as pH increases, the ionization decreases and the drug excretion decreases

58
Q

active secretion in the renal tubules deoends on what 3 factors?

A
  1. affinity of drug for transport protein
  2. rate of delivery of drug to the secretory site
  3. rate of transfer of drug across tubular membrane
59
Q

what proteins are involved in active tubule secretion?

A

OAT, OCT, PGP, MrP, MATE

60
Q

what is total drug clearance?

A

volume of blood/plasma/body fluid cleared of drug per unit time. The sum of cl by all routes of elimination (liver, kidney, lung etc.)

61
Q

how is total clearance calculated?

A

(F x dose) / AUC

62
Q

does total drug clearance indicate the amount of drug elimination?

A

no

63
Q

how is extraction ratio (ER) calculated?

A

Concentration into liver-concentration leaving liver / concentration going into liver

64
Q

if drug is completely eliminated in ONE passage through the liver, the EHR is equal to ___

A

1

65
Q

if drug is not eliminated, the EHR is equal to __

A

0

66
Q

low ER

A

<0.3

67
Q

mild ER

A

0.3-0.7

68
Q

high ER

A

0.7-1.0

69
Q

what is hepatic clearance?

A

volume of blood from which a drug will be cleared by the liver per unit time

70
Q

the hepatic clearance is a ratio of ___

A

hepatic elimination rate to plasma drug concentration

71
Q

how to calculate hepatic clearance

A

Q x ER

72
Q

for drugs with high hepatic ER, what is the rate limiting step?

A

flow

73
Q

for drugs with low ER and low protein binding (<75-80%) what is the rate limiting step? Does it depend on proetin binding?

A

metabolism capacity; no

74
Q

for drugs with low ER and high protein binding (>75-80%), what is the rate limiting step? Does it depend on protein binding?

A

metabolism capacity; yes

75
Q

give 2 examples of drugs with high renal ER

A

penicillin G and glucuronides

76
Q

for high renal ER drugs, the CLr is dependent on ____ and ___ is involved

A

blood flow; active secretion

77
Q

give 2 examples of low renal ER drugs

A

gentamicin, tetracycline

78
Q

for low renal ER drugs, the CLr is limited by ____

A

glomerular filtration rate

79
Q

give examples of drugs that are enzyme inducers

A

phenytoin, carbemazepine, phenobarbital, rifampicin

80
Q

give examples of drugs that induce CYP3A4

A

rifampicin/rifampin, carbemazepine and phenytoin

81
Q

give examples of CYP2B6induceer

A

phenobarbital

82
Q

what are the PK consequences of induction on the parent drug?

A

decreased plasma drug concentration, decreased AUC, decreased elimination half-life

PBL PY2 Fall (21 decks)

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