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Pharmacodynamics > Lecture 3- ADME > Flashcards

Lecture 3- ADME Flashcards

(67 cards)

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1
Q

permeation

A

movement of drug through barriers

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2
Q

aqueous/passive

A

no energy required: high to low conc

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3
Q

ficks law

A

“helps determine how well drugs can cross membranes” involves aqueous diffusion and passive diffusion of molecules down a conc. gradient

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4
Q

faster diffusion/absorption occurs when (ficks)

A

larger conc. gradients,
large area,
thin membrane

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5
Q

c1 (ficks law)

A

higher conc.

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6
Q

c2 (ficks law)

A

lower conc.

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7
Q

area (ficks law)

A

that diffusion is occurring

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8
Q

permeability coefficient (ficks)

A

measure of the mobility of drug mol. in the medium of diffusion path

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9
Q

thickness (ficks)

A

length of the diffusion path

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10
Q

the bigger the area, the thinner the membrane the ____ diffusion

A

faster diffusion

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11
Q

charged drugs are lipid ___ and water ____

A

insoluble, soluble

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12
Q

uncharged drugs are lipid ___ and water ___

A

soluble, insoluble

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13
Q

pKa

A

acid dissociation constant

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14
Q

HA

A

protonated acid, uncharged

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15
Q

A

A

unprotonated acid, charged

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16
Q

BH+

A

protonated base, charged

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17
Q

B

A

unprotonated base, uncharged

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18
Q

if pH equals pKa

A

50% protonated 50% unrpotonated

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19
Q

in order to cross membrane weak acids need to be _____ and weak bases need to be____; thus both are ____

A

protonated (acids)
unprotonated (bases)
both are uncharged

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20
Q

endocytosis

A

cell engulf

-occurs when substance is too large or insoluble or impemeant to cell by pinching it off

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21
Q

exocytosis

A

cell directs the contents of secretory vesicles out of the cell membrane, releasing a substance from the cell

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22
Q

volume distribution

A

how far the drug distributes out into body tissue; either bloodstream (SMALL) or out into tissues (HIGH vd)

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23
Q

Vd (L) equation

A

(D)amt of drug in body/conc. in plasma (C0)

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24
Q

a high VD indicates

A

out into tissues = lipophilic (fat lovin)

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25
how can vd be decreased
plasma protein binding, dehydration
26
how can vd be increased
renal failure or liver failure
27
metabolism
mechanism that terminates/alters the biologic activity of a substance
28
prodrug
an inactive substance that must be converted by metabolism (liver) before it has biologic activity
29
sites of metabolism
liver*** | lungs, GI, skin, kidney
30
what is the goal of metabolism
to convert xenobiotics into more water-soluble (polar) components for excretion
31
phase 1 rxn
makes more water soluble (polar) either for the kidneys or for a phase 2 rxn
32
major classes of phase 1 rxns
oxidation, reduction, hydrolysis
33
phase 2 rxn
add/alter molecule to increase water sol. | -conjugation, glucuronidation, sulfation
34
define CYP2D6
CYP- cytochrome P450 2- family D- subfamily 6- individual enzyme
35
cyp 3A4
most drug interactions
36
gut flora
vitamin K absorption
37
what can impair hepatic drug metabolism
``` -liver dz: alcoholics, cirrhosis, hepatitis, Renal dz- fluid backup affecting liver -cardiac dz -endocrine -genetic -diet -age gender -any dz that lower blood flow ```
38
whats the most important enzyme system in liver
Cytochrome P-450 system
39
what organ does elimination mainly occur?
kidneys
40
where are weak acids excreted in?
alkaline urine
41
where do weak bases excrete faster in?
acidic urine
42
if weak acids are charged
less reabsorption occurs
43
where does "trapping" occur
stomach, SI, breast milk, aqueous humar, vaginal/prostatic secretions
44
clearance
volume of blood cleared of drug per unit time
45
what happens to cr Clearance if age goes up
it declines
46
what happens to crCl when wight increases
it goes up
47
what happens when Serum clearance increases
crCl goes down
48
half life (t1/2)
time it takes for the body to get rid half of the drug out of the system
49
steady state
amount of drug coming in during a period of time is equal to the amount leaving the body at that same time frame
50
first order elimination
elimination percentage-proportional to concentration | -most drugs follow
51
zero-order (cap limited)
elimination of constant AMOUNT | -independent of conc.
52
what is Ke
elimination constant = cl/Vd =(peak/trough)/changeintime
53
what happens to Ke when Cl increases
cl/vd | ke increases
54
what happens to Ke when vd increases
cl/vd | ke decreases
55
formula for t1/2 and ke
``` t1/2= 0.693/ke ke= cl/vd ``` .. t1/2=0.693*vd/cl
56
a larger vd has what effect on half life
increase
57
a smaller cl will have what effect on half life?
increase
58
what constant makes the avg steady state plasma drug level equal to the rate of drug admin?
clearance
59
equation for avg conc. (steady state)
Css= Dose/( Cl*dosing interval)
60
what effect does dose have on the Css
proportional, increase =increase
61
what effect does increasing the dose interval have on Css?
inverse -- decrease css
62
how long is time to steady state
4-5 half-lives
63
loading dose
gets pt to steady state immediately | -skipping 4-5 half lives by big dose, then intermittent
64
amidirone
takes a year for elimination or something like that lol
65
maintenance dose
administrating drug in such a way to maintain a steady state of a drug in body (given after load dose)
66
what is the best cure to toxicity, why?
tincture of time-gives body time to metabolize | provides good supportive care
67
graph of zero order vs first order
zero order- straight line down (CONSTANT amount) | first order- curve line down (percent of drug)

Pharmacodynamics (6 decks)

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