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N926 Pharmacology > Pharmacokinetics lecture > Flashcards

Pharmacokinetics lecture Flashcards

(77 cards)

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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
common membrane transporters
P-gp, MDR1, ABCB1
26
what type of drug is dapagliflozin?
SGLT2 inhibitor
27
what adverse effect does SGLT2 have?
hypotension, dehydration
28
2 types of membrane transporters
Uptake and efflux
29
examples of uptake transporters
OATP family, OAT family (SLC22A), OCT family(SLC22A), glucose transporters (organic anion-transporter, transporters are more uptakers )
30
examples of efflux transporters
P-GP, MRP, BSEP, BCRP (the last P stands for pump, pumps are more effluxers)
31
what is efflux transporter also called
reverse transporter
32
factors influence PK activity
ionization and lipid solubility; ion trapping; protein binding; molecular size; drug transporters.
33
important compartments in the body are:
BBB; GI; placenta
34
what plays important role in ionization?
hepatocytes and renal absorptive membrane
35
locations ion trapping commonly happens
brain and placenta
36
ph of CSF
7.4
37
ph of stomach, small intestine and ileum + large intestine
1-3, 5-6, 7-8
38
max size of molecular to pass lipid barriers
100-200 amu
39
which patients have reduction in proteins?
Liver or kidney disease; malnutrition, pregnant woman
40
albumin likes to bind with what?
acids
41
alpha1-acid protein likes to bind with what
bases
42
rank the force of chemical bonds between molecules (intermolecule)
covalent\>ionic\>hydrogen\>van der waals
43
what forces are intramolecular
covalent\> ionic
44
what forces are intermolecular
hydrogen\>dipole\>van der waal
45
SLT, OST main site of action includes
BBB, GI tract, renal tubules, biliary tract, placenta
46
PGP aka
MDR1 (multidrug resistance protein 1), ABCB1 (ATP binding cassettes sub family b1)
47
PGP characteristics
membrane embedded protein; efflux transporter; non-selective; protective fxn (fetus, brain)
48
differentiate 1st order, zero order, 1st pass effect, phase 1 and phase 2. Perfusion dependent vs capacity dependent clearance.
1st order, zero order, phase 1, phase 2 describe metabolism. 1st pass effect is absorption, perfusion dependency vs capacity dependency are about clearance
49
IM bioavailability
75-100%
50
transdermal
80-100%
51
inhalation
5-100%
52
is liver the only organ having first pass effect?
lungs also have first pass effect
53
large Vd
\>0.6L/kg
54
small Vd
\<0.4L/kg
55
blood brain barrier characteristics
tight junction; P-GP, lipophilic, small molecules
56
metabolism aka
biotransformation
57
Other than liver, what other organs metabolize?
Lungs, plasma, GI, skin, kidneys, heart, brain
58
what happens during phase 1
oxidation, reduction and hydrolysis
59
what happens during phase 2. List one substance involved
conjugation. Glucuronic
60
In which phase of metabolism is CYP450 involved?
phase I
61
where are CYP450 located?
smooth ER
62
CYP aka
mixed-function oxidase system
63
example of enzyme induction and effect
alcohol, reduced half life, subtherapeutic
64
example of enzyme inhibition and effect
grape fruit juice, overdose
65
example of enzyme inhibition and effect
grape fruit juice, overdose
66
example of zero order kinetics
alcohol
67
perfusion dependent elimination extraction ratio
\>0.7
68
capacity dependent elimination extraction ratio
\<0.3
69
perfusion dependent elimination drugs aka and examples
high clearance drugs; verapamil, lidocaine, morphine
70
what does capacity dependent elimination depend on
hepatic enzyme and protein binding
71
examples of capacity dependent elimination
diazepam and theophylline
72
examples of drugs actively secreted by liver
morphine, meperidine, quaternary ammonium, furosemide, penicillin
73
drug that is eliminated during glomerular filteration
aminoglycoside antibodies
74
drug eliminated during active secretion
penicillin
75
drug going through reabsorption
propofol
76
gender factors with drugs
female emerge quicker, more sensitive to paralytics, more PONV; Male sensitive to propofol
77
is sux affected by liver? why?
no, sux effect is at NMJ, does not get metabolized, just in vascular.

N926 Pharmacology (16 decks)

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