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Pharm. Final > Intro to pharmacology/pharmokinetics/pharmodynamics > Flashcards

Intro to pharmacology/pharmokinetics/pharmodynamics Flashcards

1
Q

Dose

A

amount of drug administered in a given formulation

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2
Q

response is proportional to?

A

of receptors occupied by the drug, but not always a linear relationship

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3
Q

response affected by?

A

affinity and receptor signal transmission

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4
Q

curves represent what?

A

dosage over which the drug is effective and peak effect/response that can be expected.

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5
Q

shape of curve and plateau indicate what?

A

info regarding binding of drug to cellular receptors

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6
Q

threshold dose

A

where response begins and increases in magnitude until a response plateau is reached

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7
Q

ceiling effect ( maximal efficacy)

A

point at which there is no further response (even if dosage continues to be increased)

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8
Q

potency

A

threshold dose that produces a given response

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9
Q

what does higher potency mean?

A

less of the compound is required to produce given response

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10
Q

efficacy

A

dose ranges over which the drug has desired effect

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11
Q

what happens to magnitude of response?

A

increases as dosage increases

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12
Q

First Pass Effect

A

…

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13
Q

What is first pass effect?

A

metabolism/destruction of drug molecule in liver before reaching its site of action

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14
Q

What medications endure first pass effect?

A

Enteral/oral meds

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15
Q

What meds. bypass first pass?

A

Para-enternal meds. bypass GI system and take a more direct route to target site

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16
Q

Bioavailability

A

…

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17
Q

what is bioavailability?

A

% of drug administered that reaches the bloodstream

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18
Q

What does bioavailability depend on?

A

route of administration and drugs ability to cross membrane barriers

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19
Q

Volume of distribution

A

…

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20
Q

What is volume of distribution?

A

amount of drug administered divided by concentration of drug in plasma

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21
Q

Vd = total body H20

A

uniform body distribution

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22
Q

Vd> total body H20

A

drug is being concentrated in tissues

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23
Q

Vd

A

drug is being retained in bloodstream

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24
Q

Distribution?

A

moving the drug throughout the body

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25
Q

What does distribution depend on? -4

A
  1. tissue permeability
  2. blood flow
  3. plasma protein binding
  4. sub cellular protein binding
26
Q

Tissue permeability

A

highly lipid soluble molecules cross membranes more easliy

27
Q

blood flow

A

bloodstream carries drugs to highly perfused organs, can be affected by disease

28
Q

what does negative venule pressure due?

A

pulls drug from tissues back into blood

29
Q

what does positive arteriole pressure do?

A

draws drug via blood into tissue spaces

30
Q

what is plasma protein binding?

A

reversible bonds

-bound portion of drug doesn’t have a therapeutic effect and is not eliminated

31
Q

what is an inactive drug?

A

bound in plasma protein and cannot leave blood to distribute into tissues

32
Q

what is active?

A

unbound and can distribute to tissues

33
Q

what is sub cellular protein binding?

A

drug gets trapped within the cell (lysosome)

ex. Anti depressants

34
Q

How are drugs metabolized and eliminated?

35
Q

metabolism

A
  1. primarily in liver

2. also in lungs, kidneys, Gi, skin

36
Q

factors affecting metabolism?

A

tissue/organ damage, metabolic inhibitors, enzyme induction

37
Q

competitive inhibition?

A

inhibition of enzyme that metabolizes drub B by drug A

- decreases metabolism of drug B

38
Q

irreversible inhibition of metabolism?

A

Inhibition of the enzyme that metabolizes drug B by drug A

  • decreases metabolism of drug B
  • covalent bonding of inhibitor
39
Q

induction of metabolism

A

induction of the enzyme that metabolizes drub B by drug A

-increases the metabolism of drug B by increasing the enzyme quantity

40
Q

Elimination

41
Q

What is biotransformation (metabolism)?

A

Chemical altering of a drug to metabolite via enzymes to deactivate that drug

42
Q

oxidation

A

usual method via endoplasmic smooth reticulum via enzymes O & H
Phase I reaction

43
Q

Reduction

A

happens in cell via cytoplasm

phase I reaction

44
Q

Hydrolysis

A

original compound is broken into separate parts via enzymes

phase I

45
Q

Conjugation

A

drug or metabolite bi product of one or other mechanisms

46
Q

Excretion

A

eliminating active form of drug

47
Q

where does it occur?

48
Q

factors affecting excretion?

A

reabsorption
polarity of metabolite
polar (ionized) drugs tend to be excreted
non polar tend to be reabsorbed

49
Q

what is clearance?

A

ability of organs to clear drug

dependent on perfusion

50
Q

factors that affect clearance?

A

blood flow to organ
extraction ratio - fraction of drug removed from plasma as it passes through organ
concentration

51
Q

half life

A

duration of activity of the compound in body

amount of time required for 50% of the drug remaining in body to be eliminated

52
Q

what is half life a function of?

A

clearance and Vd

volume of distribution

53
Q

Drug administration - oral vs. transdermal

54
Q

oral

A 
enteral
easiest to self administer 
absorbed by small intestine
-must have high lipid solubility
-undergoes first pass effect
55
Q

disadvantages of oral?

A

limited or erratic absorption of some drugs

56
Q

transdermal?

A

bypasses GI system and first pass effect.
takes more direct route to target site
more predictable quantity

57
Q

disadvantage of transdermal?

A

drug must be able to pass through intact dermal layers

ex. injection, IV, Sub-q

58
Q

continuous administration

A

matching the rate of administration with the rate of drug elimination once desired plasma concentration is achieved

59
Q

interval administration

A

dosage is adjusted to provide an average plasma concentration over the dosing period

60
Q

what does dosing interval (time in hours) do ?

A

affects size of dosage needed to maintain same relative plasma concentration

Pharm. Final (16 decks)

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