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Pharmacology > Basic Principles > Flashcards

Basic Principles Flashcards

1
Q

____ actions of a drug on the body

A

Pharmacodynamics

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2
Q

___ actions of the body on the drug

A

Pharmacokinetics

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3
Q

Arrange to according to decreasing strength

Covalent, Hydrophobic, Electrostatic bonds

A
  1. Covalent
  2. Electrostatic
  3. Hydrophobic bonding
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4
Q

[Type of diffusion]

passive movement of non-protein bound drugs

A

Aqueous diffusion

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5
Q

[Type of diffusion]

affected by the drug concentration and charge

A

Aqueous diffusion

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6
Q

[Type of diffusion]

governed by Fick’s Law of Diffusion

A

Aqueous diffusion, Lipid Diffusion

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7
Q

[Type of diffusion]

movement of drugs through lipid membranes from ECF to the ICF

A

lipid diffusion

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8
Q

[Type of diffusion]

most important limiting factor for permeation

A

Lipid diffusion

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9
Q

[Type of diffusion]

important for the diffusion of weak acids and weak bases

A

Lipid diffusion

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10
Q

[Type of diffusion]

for drugs that do not readily cross through membranes; transported across barriers by mechanisms that carry similar endogenous substances

A

transport by special carriers

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11
Q

[Type of diffusion]

not governed by Fick’s law of diffusion is capacity-limited

A

transport by special carriers

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12
Q

[Type of diffusion]

vitamin B12 bound to intrinsic factor is a type of _____

A

endocytosis

pinocytosis

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13
Q

[Type of diffusion]

iron bound to transferrin

A

endocytosis and pinocytosis

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14
Q

[Water/Lipid Solubility of Drugs]

____ is directly proportional to electrostatic charge

A

directly proportiona

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15
Q

[Water/Lipid Solubility of Drugs]

ionized and polar drugs _____ (water/lipid soluble)

A

water soluble

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16
Q

[Water/Lipid Solubility of Drugs]

this is associated with an increased clearance

A

water soluble

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17
Q

[Water/Lipid Solubility of Drugs]

inversely proportional to electrostatic charge

A

inversely proportional

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18
Q

What are the 3 dependent factors for permeation?

A
  1. Solubility
  2. Concentration gradient
  3. Surface area and vascularity
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19
Q

[Water/Lipid Solubility of Drugs]

unprotonated weak acid

A

more water-soluble, better clearance

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20
Q

[Water/Lipid Solubility of Drugs]

protonated weak acid

A

more lipid soluble, more likely to cross biological membranes

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21
Q

[Water/Lipid Solubility of Drugs]

unprotonated weak base

A

more lipid soluble, cross biological membrane

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22
Q

[Water/Lipid Solubility of Drugs]

protonated weak base

A

more water soluble, better clearance

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23
Q

[Absorption/Excretion]

if a compound is placed in a solution above its pKa

this favors? (Absorption/excretion)

A

favors absorption

Above its pKa, unprotonated form predominates, which favors absorption

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24
Q

[Absorption/Excretion]

if a compound is s placed in a solution below its pKa

this favors? (Absorption/excretion)

A

favors excretion

Below its pKa, protonated form predominates, which favors absorption

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25
Q

[Absorption/Excretion]

if a weak base is placed in an acidic environment?

this favors? (Absorption/excretion)

A

favors excretion

Again, basic drugs are excreted in an acidic environment

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26
Q

[Absorption/Excretion]

if an acidic compound is placed in an alkalitic environment

this favors? (Absorption/excretion)

A

favors excretion

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27
Q

What are the 3 major factors that affect drug absorption>

A
  1. Route of administration
  2. Blood flow
  3. Concentration
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28
Q

[Route of drug administration]

highest first pass effect?

A

oral route

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29
Q

[Route of drug administration]

potentially more dangerous

A

IV route

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30
Q

[Route of drug administration]

bypasses first pass effect

A

IV
IM
SQ
Buccal/Sublingual

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31
Q

[Route of drug administration]

anticoagulants cant be given by this route

A

IM

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32
Q

[Route of drug administration]

IM injection to buttocks is safest at

A

superolateral

33
Q

[Route of drug administration]

inferomedial buttock IM injection can result to this complication

A

sciatica

34
Q

[Route of drug administration]

superomedial buttock IM injection is associated with this gait

A

gluteus medius gait

35
Q

[Route of drug administration]

Offers direct absoprtion to systemic venous circulation, bypasses the FPE

A

Buccal/Sublingual

36
Q

[Route of drug administration]

trace the route of the drug via the sublingual route before reaching the heart

A

lingual, IJV, Brachiocephalic, SVC, RA

37
Q

[Route of drug administration]

partial avoidance of the FPE, used for large amounts of drugs with unpleasant tase

A

Racta

38
Q

[Route of drug administration]

offers delivery closes to target

A

inhalational

39
Q

[Drug distribution]

What are the factors that affect drug distribution?

A
  1. Size of the organ
  2. Blood flow
  3. Solubility
  4. Protein binding
40
Q

[Drug distribution]

Basic drugs are bound to these proteins ____

A

orosomucoid and alpha 1 acid glycoprotein

41
Q

[Drug distribution]

acidic drugs are bound to this protein

A

albumin

42
Q

Drug with the lowest molecular weight, can cross BBB

A

lithium

43
Q

Drug that is water soluble, but can cross the BBB because it has a low molecular weight

A

ethanol

44
Q

the duration of drug action is determined by?

A
  1. dose administered

2. rate of elimination following last dose

45
Q

[Drug elimination]

rate of elimination is proportionate to the concentration

A

first order

46
Q

[Drug elimination]

rate of elimination is constant regardless of concentration

A

Zero-order

47
Q

What drugs display zero order elimination kinetics?

A
  1. Warfarin
  2. Heparin
  3. Aspirin
  4. Tolbutamide
  5. Phenytoid
  6. Ethanol
  7. Theophylline
48
Q

What are the characteristics of a receptor?

A
  1. Selective in their ligand-binding
  2. modifiable
  3. most are proteins
49
Q

[Graded dose-response relationship]

___ concentration required to bind 50% of the receptors

A

Kd

50
Q

[Graded dose-response relationship]

A ____ kd is associated with greater affinity for its receptor

A

smaller Kd

51
Q

[Graded dose-response relationship]

____ is the maximal effect achievable with increasing concentration of a drug

A

Emax

52
Q

[Graded dose-response relationship]

____ concentration of drug wherein half of the maximal effect is achieved

A

EC50

53
Q

[Graded dose-response relationship]

___ maximum percentage of receptors with increasing concentration of a drug/maximal number of receptors boudn

A

Bmax

54
Q

[Type of dose response curve]

response of a particular receptor-effector mechanism measured against increasing drug concentration

A

dose response

55
Q

[Type of dose response curve]

fraction of the population that response at each dose against the log of the dose administered

A

quantal dose-reponse curve

56
Q

[Type of dose response curve]

Efficacy and potency are derived from this curve

A

graded dose-response curve

57
Q

[Type of dose response curve]

Median effective, median toxic, median lethal doses are derived from this curve

A

quantal dose-response curve

58
Q

What is the formula to determine the therapeutic index?

A

TI = TD50/ED50

59
Q

___ refers to the dose range between the most effective dose and the most toxic dose

A

Therapeutic index

60
Q

___ refers to the amount of drug needed to produce a given effect

A

potency

61
Q

___ is determined by the affinity of the receptor for the drug (efficacy/potency)

A

potency

62
Q

Noncompetitive antagonist causes ____ shift of the DRC

A

downward

63
Q

competitive antagonist causes _____ shift of DRC

A

right shift

64
Q

_____ continuous activation may lead to depletion of essential substrates

A

tolerance

65
Q

____ responsiveness diminishes rapidly after administration of a drug; frequent or continuous exposure to agonist results in short-term diminution of the receptor

A

tachyplaxis

66
Q

[Volume of distribution]

a low Vd distributes in?

A

blood

67
Q

[Volume of distribution]

a high Vd distributes in?

A

tissues

68
Q

___ most important pharmacokinetic parameter to be considered in defining rational steady state during dosage regimen

A

clearance1

69
Q

Steady state is achieved after how many half-lives?

A

4-5

70
Q

___ are also called mixed function enzyme

A

Cyt P450

71
Q

____ is a standard in vitro test for mutagenicity

A

Ames test

72
Q

____ is an in vivo mutagenicity test carried out in mice

A

dominant lethal test

73
Q

[Clinical trial]

____ preclinical data collected up to time ofsubmission

A

investigation

74
Q

[Clinical trial]

____ request for approval of general marketing of the agent for prescription use

A

new drug application

75
Q

[Clinical trial]

evaluation of the dose-response relationship and pharmakokinetics among normal human volunteers (20-100 volunteers)

A

Phase 1 Trial

76
Q

[Clinical trial]

in phase 1 trial of a cancer drug, how many volunteer patients are needed

A

20-50

77
Q

[Clinical trial]

100-200 patients with target disease, done in hospital ward

A

phase 2

78
Q

[Clinical trial]

1000-5000 patients; double-blind crossover design

A

phase 3

79
Q

[Clinical trial]

post marketing surveillance

A

phase 4

Pharmacology (35 decks)

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