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N926 Pharmacology > Pharmacokinetics lecture > Flashcards

Pharmacokinetics lecture Flashcards

1
Q

What is the most common CYP450 enzyme

A

CYP3A4

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2
Q

What CYP450 enzyme converts codeine to active opioid (morphine)

A

CYP2D6

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3
Q

What does grape juice do to liver enzyme and what impact does it have on drug’s plasma concentration?

A

it inhibits liver enzyme, thus increases plasma drug concentration

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4
Q

Clearance formula

A

Clearance=Q (liver blood flow) X E (extraction ratio)

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5
Q

What does high extraction ratio mean to clearnace?

A

The more blood flow I have, the more drug will be taken out of the system

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6
Q

Extraction ratio of perfusion dependent elimination

A

E>=0.7

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7
Q

Examples of high-clearance drugs

A

verapamil, morphine and lidocaine

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8
Q

Total volume of fluid in body

A

42L

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9
Q

volume of ISF

A

10L

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10
Q

volume of intracellular

A

28L

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11
Q

volume of plasma

A

5L

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12
Q

normal Vd

A

0.6L/kg (42L/70kg)

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13
Q

what are the 2 types of hepatic clearance?

A

perfusion dependent elimination & capacity dependent elimination

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14
Q

Extraction ratio of capacity dependent elimination

A

E<0.3

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15
Q

what does capacity dependent elimination depend on?

A

Protein binding and hepatic enzymes

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16
Q

examples of capacity dependent elimination drugs

A

diazepam and theophylline

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17
Q

how many half-lives does it take for a drug to be considered eliminated from the body

A

4-5 half-lives

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18
Q

drugs actively excreted by kidneys

A

furosemide, morphine, meperidine(demerol), penicillin, quaternary ammonium compounds

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19
Q

drugs excreted during passive glomerular filtration

A

amino glycoside antibiotics

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20
Q

drugs excreted by active secretion in proximal loop

A

penicillin

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21
Q

drugs reabsorbed in distal loop

A

propofol (lipophilic)

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22
Q

What factors does age affect drug PK?

A

liver fxn, renal fxn, increased fat, increased Vd

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23
Q

Women specific response to anesthetics

A

quicker emergence; sensitive to paralytics, adverse effects of opioids

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24
Q

Men specific response to anesthetics

A

more sensitive to propofol

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25
Q

common membrane transporters

A

P-gp, MDR1, ABCB1

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26
Q

what type of drug is dapagliflozin?

A

SGLT2 inhibitor

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27
Q

what adverse effect does SGLT2 have?

A

hypotension, dehydration

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28
Q

2 types of membrane transporters

A

Uptake and efflux

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29
Q

examples of uptake transporters

A

OATP family, OAT family (SLC22A), OCT family(SLC22A), glucose transporters (organic anion-transporter, transporters are more uptakers )

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30
Q

examples of efflux transporters

A

P-GP, MRP, BSEP, BCRP (the last P stands for pump, pumps are more effluxers)

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31
Q

what is efflux transporter also called

A

reverse transporter

32
Q

factors influence PK activity

A

ionization and lipid solubility; ion trapping; protein binding; molecular size; drug transporters.

33
Q

important compartments in the body are:

A

BBB; GI; placenta

34
Q

what plays important role in ionization?

A

hepatocytes and renal absorptive membrane

35
Q

locations ion trapping commonly happens

A

brain and placenta

36
Q

ph of CSF

A

7.4

37
Q

ph of stomach, small intestine and ileum + large intestine

A

1-3, 5-6, 7-8

38
Q

max size of molecular to pass lipid barriers

A

100-200 amu

39
Q

which patients have reduction in proteins?

A

Liver or kidney disease; malnutrition, pregnant woman

40
Q

albumin likes to bind with what?

A

acids

41
Q

alpha1-acid protein likes to bind with what

A

bases

42
Q

rank the force of chemical bonds between molecules (intermolecule)

A

covalent>ionic>hydrogen>van der waals

43
Q

what forces are intramolecular

A

covalent> ionic

44
Q

what forces are intermolecular

A

hydrogen>dipole>van der waal

45
Q

SLT, OST main site of action includes

A

BBB, GI tract, renal tubules, biliary tract, placenta

46
Q

PGP aka

A

MDR1 (multidrug resistance protein 1), ABCB1 (ATP binding cassettes sub family b1)

47
Q

PGP characteristics

A

membrane embedded protein; efflux transporter; non-selective; protective fxn (fetus, brain)

48
Q

differentiate 1st order, zero order, 1st pass effect, phase 1 and phase 2. Perfusion dependent vs capacity dependent clearance.

A

1st order, zero order, phase 1, phase 2 describe metabolism. 1st pass effect is absorption, perfusion dependency vs capacity dependency are about clearance

49
Q

IM bioavailability

A

75-100%

50
Q

transdermal

A

80-100%

51
Q

inhalation

A

5-100%

52
Q

is liver the only organ having first pass effect?

A

lungs also have first pass effect

53
Q

large Vd

A

>0.6L/kg

54
Q

small Vd

A

<0.4L/kg

55
Q

blood brain barrier characteristics

A

tight junction; P-GP, lipophilic, small molecules

56
Q

metabolism aka

A

biotransformation

57
Q

Other than liver, what other organs metabolize?

A

Lungs, plasma, GI, skin, kidneys, heart, brain

58
Q

what happens during phase 1

A

oxidation, reduction and hydrolysis

59
Q

what happens during phase 2. List one substance involved

A

conjugation.
Glucuronic

60
Q

In which phase of metabolism is CYP450 involved?

A

phase I

61
Q

where are CYP450 located?

A

smooth ER

62
Q

CYP aka

A

mixed-function oxidase system

63
Q

example of enzyme induction and effect

A

alcohol, reduced half life, subtherapeutic

64
Q

example of enzyme inhibition and effect

A

grape fruit juice, overdose

65
Q

example of enzyme inhibition and effect

A

grape fruit juice, overdose

66
Q

example of zero order kinetics

A

alcohol

67
Q

perfusion dependent elimination extraction ratio

A

>0.7

68
Q

capacity dependent elimination extraction ratio

A

<0.3

69
Q

perfusion dependent elimination drugs aka and examples

A

high clearance drugs; verapamil, lidocaine, morphine

70
Q

what does capacity dependent elimination depend on

A

hepatic enzyme and protein binding

71
Q

examples of capacity dependent elimination

A

diazepam and theophylline

72
Q

examples of drugs actively secreted by liver

A

morphine, meperidine, quaternary ammonium, furosemide, penicillin

73
Q

drug that is eliminated during glomerular filteration

A

aminoglycoside antibodies

74
Q

drug eliminated during active secretion

A

penicillin

75
Q

drug going through reabsorption

A

propofol

76
Q

gender factors with drugs

A

female emerge quicker, more sensitive to paralytics, more PONV; Male sensitive to propofol

77
Q

is sux affected by liver? why?

A

no, sux effect is at NMJ, does not get metabolized, just in vascular.

N926 Pharmacology (16 decks)

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