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PHARMACO PRELIMS > I. PPT > Flashcards

I. PPT Flashcards

1
Q

Determines the fraction of drug molecules charged (ionized) vs uncharged (non-ionized)

A

pH

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2
Q

a neutral molecule that can reversibly dissociate into an anion and a proton

A

weak acid

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3
Q

a neutral molecule that can form a cation by combining with a proton

A

weak bases

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4
Q

(weak acids)

unprotonated form is more ____

A

water soluble

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5
Q

(weak acids)

protonated is more ___

A

lipid soluble

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6
Q

(weak acids)

better clearance

protonated/unprotonated

A

unprotonated

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7
Q

(weak acids)

cross biological membrane easily

protonated/unprotonated

A

protonated

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8
Q

(weak bases)

more lipid soluble, cross biological membrane easily

protonated/unprotonated

A

unprotonated

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9
Q

(weak bases)

more water soluble, better clearance

protonated/unprotonated

A

protonated

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10
Q

excretion of weak acid is accelerated by ___

A

alkalinizing the urine

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11
Q

excretion of weak base is accelerated by ____

A

acidifying the urine

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12
Q

the component of a cell or organism that interacts with a drug and initiates the chain of events leading to the drug’s observed effects

A

receptor

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13
Q

responsible for selectivity of drug action

A

receptors

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14
Q

largely determine the quantitative relations between dose or concentration of drug and pharmacologic effects

A

receptors

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15
Q

mediate the actions of both pharmacologic agonists and antagonists

A

receptors

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16
Q

receptors (3)

A

enzymes
transport proteins
structural proteins

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17
Q

responses to low doses of a drug usually increase in ___ to dose

A

direct proportion

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18
Q

as doses increase, the response increment __

A

diminishes

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19
Q

the transduction process that links drug occupancy of receptors and pharmacologic response

A

coupling

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20
Q

it is possible to elicit a maximal biologic response at a concentration of agonist that does not result in occupancy of all of the available receptors

A

spare receptors

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21
Q

may be demonstrated by using irreversible antagonists to prevent binding of agonist to a proportion of available receptors and showing that high concentrations of agonist can still
produce an undiminished maximal response

A

spare receptors

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22
Q

bind to receptors but do not activate them

A

antagonist

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23
Q

prevents agonists from activating receptors

A

antagonist

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24
Q

antagonists 2 types

A

competitive (reversible)
non-competitive (irreversible)

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25
Q

___ agonist binds to receptors in a reversibleway

A

competetive

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26
Q

the presence of antagonist increases the agonist concentration required for a given degree of response, and so the agonist concentration-effect curve is shifted to the ___

A

right

27
Q

the degree of inhibition produced by a competitive antagonist depends on the ____

A

concentration of antagonist

28
Q

cause downward shift of DRC

A

non competitive antagonist

29
Q

agonists 2 types

A

full a.
partial a.

30
Q

capable of fully activating the effector system

A

full agonist

31
Q

high affinity for the activated receptor conformation

A

full agonist

32
Q

produce less than the full effect, even when it has saturated the receptors

A

partial agonist

33
Q

in the presence of an agonist, it acts as an inhibitor

A

partial agonist

34
Q

Interact directly with the drug being antagonized to remove it or to prevent it from reaching its target

A

Chemical antagonist

35
Q

Does not depend on the interaction with the agonist’s receptor

A

Chemical antagonist

36
Q

Binds to a different receptor, producing an effect opposite to that produced by the drug it is antagonizing

A

Physiologic Antagonist

37
Q

Response of a particular receptor-effector system measured against increasing drug concentration

A

dose-response curve

Emax, EC50

38
Q

Maximal effect an agonist can produce

A

Efficacy

39
Q

Determined mainly by the nature of the receptor and its associated effector system

A

Efficacy

40
Q

refers to the concentration (EC50) or dose (ED50) of a drug required to produce 50% of that drug’s maximal effect

A

Potency

41
Q

Determined mainly by the affinity (Kd) of the receptor to the drug

A

Potency

42
Q

Minimum dose required to produce a specified response is determined in each member of a population

A

QUANTAL DOSE-EFFECT CURVES

43
Q

the measure of the ability of the body to eliminate the durg

A

clearance

44
Q

the factor that predicts the rate of elimination in relation to the drug concentration

A

clearance

45
Q

two major sites of drug elimination:

A

kidneys and liver

46
Q

clearance will vary depending on the concentration of drug that is achieved

A

capacity-limited elimination

47
Q

also known as saturable, dose- or concentration-dependent, nonlinear, and Michaelis-menten elimination

A

capacity-limited elimination

48
Q

drugs are cleared very readily by the organ of elimination, so that at any clinically realistic concentration of the drug, most of the drug in the blood perfusing the organ is eliminated on the first pass of the drug through it

A

flow-dependent elimination

49
Q

the elimination of these drugs will depend primarily on the rate of drug delivery to the organ of elimination

A

flow-dependent elimination

50
Q

is the time required to change the amount of drug in the body by one-half during elimination/ during constant infusion

A

half life

51
Q

indicates the time required to attain 50% of steady state

A

half time

52
Q

defined as the fraction of unchanged drug reaching the systemic circulation following administration by any route

A

bioavailability

53
Q

for a drug administered orally, bioavailability may be less than 100% for 2 reasons:

A
  1. incomplete extent of absorption
  2. first-pass elimination
54
Q

different routes of administration

A

IV
IM
SC
PO
Rectal
Inhalation
Transdermal

55
Q

following absorption across the gut wall, the portal blood delivers the drug to the liver prior to entry into the systemic circulation

A

first-pass elimination

56
Q

____ plays a pivotal role in terminating the biologic activity of some drugs

A

renal excretion

57
Q

converts the parent drug to a more polar or more reactive product by unmasking or inserting a polar functional group

A

PHASE 1

58
Q

phase 1 reactions examples

A

oxidation
reduction
deamination
hydrolysis

59
Q

also called mixed-function oxidases

A

cytochrome P450

60
Q

Cytochrome P450 is found in the

A

SER of liver

61
Q

reactions that makes the drug more polar and less lipid-soluble

A

Phase II reactions

62
Q

Phase II reactions examples

A

glucoronidation
acetylation
glutathione conjugation
glycine conjugation
sulfation
methylation

63
Q

metabolized to products that irreversibly inhibit the metabolizing enzymes

A

suicide inhibitors

PHARMACO PRELIMS (5 decks)

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