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Psychopharmacology > Lecture 4: Pharmacokinetics > Flashcards

Lecture 4: Pharmacokinetics Flashcards

1
Q

pharmacokinetics

A

how drugs are handled by the body

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2
Q

goal of pharmacokinetics

A

predicting time course of active drug in blood that is available at receptor sites

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3
Q

the time course of a drug’s action allows a determine of ___

A

the intensity of the drug effect as a function of time

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4
Q

ADME

A

absorption
distribution
metabolism
elimination

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5
Q

absorption

A

movement of drug from site of administration to the blood

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6
Q

distribution

A

movement of drug from blood to rest of body

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7
Q

metabolism

A

breakdown of drug

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8
Q

elimination

A

removal of drug’s metabolic waste products from the body

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9
Q

therapeutic index (TI)

A

in animals: ratio of the dose that causes death in 50% of the population (LD50) to dose that is effective in 50% of population
TI = (LD50)/(ED50)

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10
Q

therapeutic ratio (TR)

A

in humans: ratio of dose that causes toxicity in 50% of population (TD50) to dose that is effective in 50% of the population (ED50)
TR = (TD50)/(ED50)

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11
Q

Cmax

A

max concentration of drug

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12
Q

Tmax

A

time at which Cmax is reached

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13
Q

T1/2

A

half life

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14
Q

AUC

A

area under the curve; total exposure to drug

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15
Q

half life

A

time it takes to remove half of current concentration of drug from the body

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16
Q

enteral routes

A

oral, rectal

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17
Q

drugs enter the capillaries and blood through ____

A

passive diffusion down concentration gradients

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18
Q

4 disadvantages of oral admin

A
  1. stomach distress
  2. hard to know how much will be absorbed
  3. stomach acid
  4. slow onset
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19
Q

path to brain for inhaled drugs

A

rapid absorption into blood through lungs, pulmonary capillaries carry drug to left side of heart and into arteries

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20
Q

benefits of transdermal administration

A

continuous absorption over hours or days

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21
Q

2 types of IM injections

A
  1. rapid onset/short duration (aqueous solution

2. slow onset/prolonged duration (oily solution)

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22
Q

2 types of IM injections

A
  1. rapid onset/short duration (aqueous solution

2. slow onset/prolonged duration (oily solution)

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23
Q

pulmonary circulation

A

circulation of blood from heart to lungs for oxygenation and back to heart (artery = from heart, vein = to heart)

24
Q

systemic circulation

A

between heart and all other body tissues

25
Q

function of right side of heart

A

veins flow to it; blood flows from it to brain

26
Q

function of left side of heart

A

oxygenated blood goes from there to rest of body; oxygenated blood goes from there to brain

27
Q

blood returning to the heart from the ____ enters the ___ and flows to the ___ ventricle

A
  1. systemic venous system
  2. right atrium
  3. right ventricle
28
Q

with contraction of the heart, blood is pumped into the ___, leading to the ___. once in pulmonary capillaries, ___ is lost and replaced with ____

A
  1. pulmonary arteries
  2. lungs
  3. CO2 is lost and replaced with O2
29
Q

oxygenated blood returns to the heart in the ___ veins, which empty into the ___. with heart contraction, blood is pumped from ____ into ___ and is carried to ___

A
  1. pulmonary
  2. left atrium
  3. left ventricle
  4. aorta
  5. body tissues and brain
30
Q

3 places drug molecules can be found in blood

A
  1. plasma (free; water-soluble drugs)
  2. attached to proteins like albumin (bound)
  3. platelets (lipid soluble drugs)
31
Q

4 membranes that affect drug distribution

A
  1. cell membranes
  2. capillary walls
  3. BBB
  4. placental barrier
32
Q

cell membranes are made of a ____ and therefore only permeable to ___

A
  1. phospholipid bilayer

2. small lipid-soluble molecules

33
Q

experimental methods allow small therapeutic agents to pass thru BBB by turning off ___

A

P-glycoprotein

34
Q

drugs cross placenta by ___

A

passive diffusion

35
Q

5 compartments

A
  1. blood
  2. fat
  3. extracellular fluid
  4. intracellular fluid
  5. other
36
Q

when drugs move into a new compartment…

A

some of that drug is sequestered by binding to proteins within that compartment

37
Q

Kc

A

equilibrium constant; number showing whether balance is in forward or backward direction

38
Q

Kc is dep on (3)

A
  1. permeability of barriers
  2. pH of compartments
  3. binding capacity
39
Q

Vd

A

volume of distribution: total amt of drug in the body/conc of drug in plasma

40
Q

synonym for metabolism

A

biotransformation

41
Q

____ drugs are hard for kidneys to hold on to, so they ___ before excretion

A
  1. lipid soluble

2. cross back into circulation

42
Q

the kidneys change molecules from ____ to ____

A

highly lipid soluble

less lipid soluble; can also change to another lipid soluble molecule, active metabolite

43
Q

main category of enzymes

A

cytochrome P450

44
Q

location of enzymes

A

hepatocytes (liver cells)

45
Q

two enzymes that metabolize over 50% of drugs

A

CYP2D6

CYP3A

46
Q

two enzymes that metabolize over 50% of drugs

A

CYP2D6

CYP3A4

47
Q

4 potential results of metabolism

A
  1. active drug to inactive metabolite
  2. active drug to active metabolite
  3. inactive prodrug to active metabolite
  4. active drug to toxic metabolite
48
Q

grapefruit juice inhibits ___

A

CYP3A4

49
Q

enzyme induction

A

liver “learns” and creates more enzymes for a specific drug

50
Q

graphs for 0, first, and second order kinetics

A

page 53

51
Q

plasma concentration is plotted as ___

A

log concentration

52
Q

what kind of function describes terminal decay?

A

exponential decay

53
Q

a quantity is subject to exponential decay if it decreases at a rate proportional to its…

A

current value

54
Q

in how many half lives is elimination achieved?

A

6

55
Q

4 routes through which drugs can leave the body

A
  1. kidneys
  2. lungs
  3. bile
  4. skin
56
Q

diagram of kidney

A

page 61

57
Q

three types of tolerance

A
  1. metabolic
  2. cellular-adaptive or pharmacodynamic response
  3. behavioral conditioning (conditional stimuli elicit compensatory conditional response)

Psychopharmacology (22 decks)

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