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Pharmacology > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

name the two general types of transport

A
  • transcellular transport

- intercellular transport

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2
Q

name ways of transversing a cell membrane

A
  • diffusion
  • filtration
  • facilitated diffusion
  • active transport
  • pinocytosis
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3
Q

whats the most common and important mode of transversing biological mambranes

A

diffusion

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4
Q

in which direction does diffusion go

A

down the cc gradient

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5
Q

what significantly influences diffusion

A
  • lipid-water partition of drug

- thiccness of the cell membrane

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6
Q

how does the pk value influence drug transport

A

-different pk values will diffuse differently

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7
Q

the cc gradient affects the rate of filtration t/f

A

t

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8
Q

does facilitated diffusion requ. E ?

A

no

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9
Q

is facilitated diffusion saturable

A

yes

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10
Q

describe active transport

A
  • requ. energy
  • against cc gradient
  • occurs only in one direction
  • is saturable
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11
Q

describe the phases of absorption

A

1 - administration
2 -has to be taken up into bloodstream
3 - uptake into target organ

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12
Q

what could reduce compound absorption

A
  • poor solubility
  • chemical instability in stomach
  • ianbility to penetrate int. wall
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13
Q

define bioavailability

A

the fraction of drug that reaches the bloodstream unaltered
-measrement of the extent of a therapeutically active drug that reaches systemic circulation and is available @ site of action

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14
Q

define absolute bioavailability

A

availability of active drug in circulation after non -IV admin.

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15
Q

what is the absolute bioavailability of drug admin. IV

A

1

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16
Q

name factors influencing bioav. (7)

A
  • absorption rate
  • degradation or metabolism of drug prior to hepatic absorption
  • first pass effect
  • food taken with p.o. admin
  • other drugs
  • intest. mot.
  • liver state
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17
Q

is distribution reversible

A

yes

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18
Q

what does distribution depnd on

A
  • permeability between tissues
  • blood flow and perfusion rate
  • ability of drug to bind to plasma proteins and tissues
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19
Q

rank the flow of the organs liver, bone, fat, skin, muscle, kidney, brain

A

brain, liver, kidney>muscle, skin> fat, bone

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20
Q

factors affecting drug distr.

A
  • dose
  • admin.
  • membrane permeabilty
  • blood perfusion
  • lipid solubility
  • ph-pka
  • plasma protein binding
  • intracellular binding
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21
Q

how do drugs travel in plasma

A

free or bound to plasma proteins

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22
Q

the drug plasma protein binding is always at least 10%

A

f

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23
Q

name the main points of plasma protein binding

A
  • generally reversible
  • only the free drugs diffuse through capillary walls
  • extensive binding may prolong duration of action
  • some plasma proteins bind many different drugs some just one
  • changes in PPB can lead to change in drug effect
24
Q

what is the volume of distr.

A

VD= volume of total body fluid in which the drug appears to be distributing

25
Q

how would you calculate the vd

A

amount of drug administered/initial plasma cc

26
Q

for the majority of the drugs the vd is an accurate representation of their actual distribution t/f

A

f

27
Q

the lower the VD of a drug the more it spreads through the body t/f

A

f

28
Q

What does a low VD indicate in regards to PPB

A

extensive plasma protein binding

29
Q

A very high VD may indicate extensive tissue binding t/F

A

t

30
Q

what ends the pharmacological acion of a parent drug

A

biotransformation

31
Q

what could biotransformation lead to

A

Metabolites that are:

  • inert and deactivate administered dose as well as reduce effect on body
  • similar or different in action to parent drug
  • toxic
  • even more active than parent drug ( pro-drug)
32
Q

define Xenobiotics

A

-compoundswith no metabolic function that can cause harm if accumulated

33
Q

Where is the majority of small molecule drug metabolism carried out

A

liver

34
Q

By what are the majority of small molecule drug metoblism reaction carried out

A

CYP450

35
Q

what factors may influence biotransformation

A
  • prior administration?
  • diet
  • hormonal status
  • hydrolysis reaction
  • genetics
  • diseases
  • age
  • liver function
36
Q

Name the phases of biotransformation

A

1 nonsynthetic reaction

2 synthetic reaction

37
Q

describe the nonsynthetic phase of biotransformation

A
  • enzyme catalyzed biotrasn. without conjugation

- oxidations, reductions, hydrolysis

38
Q

describe the synthetic phase of biotransformation

A
  • enzyme catalyzed combination of drug with an endogenous substance
  • a functional group acts as the active centre of conjugation
39
Q

which enzymes are inducible by drugs

A

those of the endoplasmatic reticulum

40
Q

How many Cytochrome families

A

18

41
Q

In which biotrans. stage is CYP most commonly involved in?

A

stage 1

42
Q

Which subfamily is responsible for a large amount of reactions in liver

A

CYP3A

43
Q

CYP3A is accountable for 10% of clinically imp. drugs metabolism t/F

A

f - 50%

44
Q

name tissues other than the liver where cyp is found abundantly

A
  • adrenals
  • ovaries or testes
  • tissues inolved in stereogenesis
  • or steroid metabolism
45
Q

describe inhibtion

A
  • competitive or non competitive
  • reduced metabolism of other drugs or endogenous substrates
  • major source of drug-drug interactions
46
Q

Which group of enzymes are commonly involved in phase 2 reactions

A

glucoronyl transferase

47
Q

name possible routes of excretion

A
  • urine
  • faeces
  • saliva
  • sweat
  • tears
  • milk
  • lungs
  • bile
48
Q

Which organ is central in excretion of drugs

A

kidney

49
Q

What factors into the renal excretion of a drug

A
  • drug filtered glomerulus
  • plus amount secreted by active transport mechanisms in the kidney
  • minus amount of drug passively reabsorbed throughout the tubule
50
Q

what’s the glomerular filtration rate

A

30-40%

51
Q

name the 2 ways of reabsorption

A
  • active reabsorption - endogenous compound such as glucose

- simple passive diffusion - un-ionized drugs

52
Q

does the urinary ph influence reabsorption

A

yes

53
Q

define renal clearance

A

-volume of plasma cleared of drug per unit time

54
Q

how would you calculate clearance

A

CL=U*V/P

  • U:cc of drug in urine
  • V: vol. urine
  • P: cc of drug in plasma
55
Q

if drug is excreted by filtration alone, what does that tell you regarding to clearance and glomerular filtration

A

Cl=GFR

56
Q

describe the first pass effect

A

orally taken drugs penetrate int. membrane and enter the portal vein and liver before entering circulation

Pharmacology (9 decks)

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