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Neuro 2 Exam 1 > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

Four main processes that drugs use

A

ADME: Absorption, Distribution, Metabolism, Elimination

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2
Q

Passive absorption (AKA simple): -Types (x2) -what are they determined by?

A

-filtration through pores or channels is determined by osmotic/hydrostatic pressure differential -diffusion through cell membranes determined by concentration gradient and is MOST COMMONLY utilized by drugs *passive processes dont require energy and cant proceed against gradients

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3
Q

what generic endings indicate a weak base drug

A

chloride, hydrochloride, sulfate, acetate

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4
Q

what generic endings indicate a weak acid

A

sodium, potassium

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5
Q

passive absorption also depends on what coefficient/status?

A

lipid-to-water partition coefficient and ionization status

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6
Q

States a drug can be in when inside the body

A

ionized (charged/polar) and unionized add to 100%

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7
Q

ionized compounds: -lipid solubility -water solubility

A

lower lipid solubility and higher water solubility. dont pass through lipid bilayers easily

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8
Q

unionized compounds -lipid and water solubility

A

higher lipid solubility, lower water solubility

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9
Q

ionization status depends on what 2 factors

A

pKa of medication (propensity of a compound to donate [acids] or accept [bases] a proton) pH of membrane-gradient/milieu

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10
Q

When pKa=pH??

A

there is a 50/50 ratio of ionized:unionized

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11
Q

What happens to highly ionized drugs in the gi tract/ renal tubules?

A

Highly ionized drugs do not readily get absorbed in GI tract OR re-absorbed from the renal tubules back into the systemic circulation. Therefore, drugs are ELIMINATRED

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12
Q

what happens to highly unionized drugs in the gi tract, renal tubules?

A

they do get readily absorbed in the gi tract or reabsorbed from the renal tubules back into the systemic circulation. NOT ELIMINATED

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13
Q

Active absorption: -energy needs? -gradients? -saturation kinetics?

A

energy requiring, saturable, movement against gradients both electrochemical and concentration

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14
Q

active absorption: -facilitated diffusion

A

does not require energy, does not proceed against gradients.

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15
Q

what elements are important during the Distribution phase?

A

active/passive transporting, ionization status, lipid-to-water partition coefficient, and PROTEIN BINDING

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16
Q

states of drugs in the blood stream

A

bound and unbound

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17
Q

unbound: -what value represents the unbound fraction -small value vs large value -value is opposite what?

A

alpha represents the unbound fraction small alpha (.1;10%) vs large alpha (.8;80%) -alpha is OPPOSITE OF % protein bound

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18
Q

drugs that have low protein binding are less effected by what? example

A

drug-drug interactions that are protein competitive. codeine (alpha of 93)

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19
Q

drugs that have high protein binding are more effected by what? example?

A

drug-drug interactions that are protein competitive ex. warfarin-97% protein bound, alpha of 3

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20
Q

impact of inducers/inhibitors cyt450 on prodrugs in terms of onset of action

A

-inducers are going to make the onset sooner, active prodrug in presence of inducer will have shorter duration of action (more enzyme activity) -inhibitors do opposite

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21
Q

First order kinetics -rate of elimination is proportional to what? -amount of drug removed per unit of time varies how? -percentage of the total amount of change in the Cp remains?

A

-rate of elimination is proportional to Cp, OR -amount of drug removed per unit of time will vary proportionately with Cp -the percentage (fraction) of the total amount of change in the Cp remains constant over time

22
Q

Zero order kinetics -rate of elimination? pwhat stays the same over time? -is percentage of total amount Cp constant?

A

-saturable -rate of elimination is not proportional to Cp,OR -amount of drug removed per unit of time stays the same over time. -the percentage of the total amount of change in the Cp is not constant over time

23
Q

what is cmax

A

maximum drug concentration

24
Q

therapeutic range is between what two values?

A

MTC (maximum therapeutic Conc.) and MEC (minimum effective conc.)

25
Q

duration of action

A

from when MEC is first reached till where it is reached again as Cp declines

26
Q

Bioavailability -what abbreviation -represents what? -describes what about the absorption? -what is it considered for IV route?

A

-F -Represents Fraction (F) of a dose that enters circulation -describes extent of absorption, not the rate -always considered 100% (F=1) for IV route

27
Q

Salt Factor: -sign -define

A

-S -think of it as an equivalency factor derived from potency, and represents percentage of a dose that equals the primary serum-assessed drug

28
Q

3 items determining amount of drug absorbed

A

Dose, F, S

29
Q

Bioavailability equation

A

(AUCoral/AUCiv)x100

30
Q

Volume of distribution -symbol -represents what? -is it a physiological number? -what does it numerically represent (bigger vs smaller value)

A

Vd, represents implied volume of compartment necessary to account for total amount of drug in body and drug-concentration in plasma. - not a physiological value -numerically represents extent of drug distribution… bigger value represents a larger body distribution “metaphorically the amount of water you would need to give you the drug concentration based on the dose you gave”

31
Q

how is the Vd reported?

A

L/Kg so multiply by body weight to eliminate Kg

32
Q

Ideal Body Weight female vs male

A

Female 45kg+((2.3kg x (height (in)-60 (in)) Male 50kg+((2.3kg x (height inches-60 inches))

33
Q

Adjusted dosing body weight used when? how to calculate?

A

for ABW>40% higher than IBW Adj body weight=(0.4 x (ABW-IBW)) + IBW

34
Q

Clearance: units, what does it represent

A

L/hr represents the volume of blood per unit of time. must get rid of the Kg first by multiplying by the patient’s weight

35
Q

Tau: units? what does it represent? -continuous infusion what do you use?

A

elimination term units=hr represents dosing interval q8h, tau would be 8. if its q.d. then tau is 24 hours *continuous infustion administration q1h tau would be 1 hour.*

36
Q

Elimination Rate Constant: -units? -represents?

A

Kel units X^-hours represents a rate of drug eliminates described as a percentage (fraction) of drug removed per unit of time

37
Q

Half-life: -units? -represents?

A

t1/2 units=hr -represents time required for 50% of drug to be eliminated

38
Q

Steady State: -units -represents? what=what? -related to?

A

-Cpss units =w/v #’s -represents an equilibrium between drug administration and body clearance where rate in=rate out -related to dose, Cl, Kel, and t1/2

39
Q

Amount of drug absorbed equation -units

A

Amount=(S)(F)(Dose) units are weight

40
Q

Changing Dosage Forms equation -units

A

Dose of alternative formulation=amount of drug absorbed from current form divided by (S)(F) of new dosage form -weight is units

41
Q

how many half lives to steady state

A

4-5

42
Q
A
43
Q

Concentration in plasma equation

A
44
Q

Loading dose equation

A
45
Q

Supplemental loading dose equation

A
46
Q

Clearance equation

A
47
Q

Maintenance Dose equation

A
48
Q

Elimination rate constant equation

A
49
Q

Elimination rate constant 2

A
50
Q

Half Life equation

A
51
Q

Creatinine Clearance equation

-male vs female

A

Neuro 2 Exam 1 (7 decks)

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