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Flashcards in I - Basic Principles Deck (86)
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1
Q

Any substance that brings about a change in biologic function through its chemical actions

A

drugs

2
Q

Actions of a drug on the body

A

Pharmacodynamics

3
Q

Actions of the body on a drug

A

Pharmacokinetics

4
Q

Molecular Weight of most drugs

A

100-1000

5
Q

MW of Lithium

A

7

6
Q

MW of Altepase

A

50,000

7
Q

MW: rarely selective in their actions

A

< 100

8
Q

MW: poorly absorbed and poorly distributed

A

> 1000

9
Q

Bonds According to Strength

A

covalent > electrostatic > hydrophobic

10
Q

Movement of drug molecules into and within biologic environments

A

Permeation

11
Q

Passive movement of non-protein-bound drugs between the blood and extravascular space through small water-filled pores

A

Aqueous Diffusion

12
Q

Aqueous Diffusion happens in all organs except

A

brain, testes, eye, placenta

13
Q

Aqueus Diffusion is governed by

A

Fick’s Law of Diffusion

14
Q

Movement of drugs through lipid membranes separating body compartments and the ECF from the ICF

A

Lipid Diffusion

15
Q

Most important limiting factor for permeation

A

Lipid Diffusion

16
Q

Lipid Diffusion is governed by

A

Fick’s Law of Diffusion

17
Q

Lipid Diffusion is very important for the diffusion of

A

weak acids and weak bases

18
Q

Drugs that do not readily cross through membranes may be transported across barriers by mechanisms that carry

A

similar endogenous substances

19
Q

Transport by special carriers is _____ by Fick’s Law of Diffusion and is _____-limited

A

not governed by Fick’s Law of Diffusion, capacity-limited

20
Q

For large drugs to be endocytosed, they have to

A

bind with receptors

21
Q

Large drugs are internalized and released after

A

vesicle breakdown

22
Q

Small polar drugs combine with _____ to form _____ which undergo endocytosis.

A

special proteins, complexes

23
Q

Predicts the rate of movement of molecules across a barrier

A

Fick’s Law of Diffusion

24
Q

Rate = (C1-C2) x (permeability coefficient/thickness) x area

A

Fick’s Law of Diffusion

25
Q

Absorption is faster in organs with _____ surface area and _____ membranes.

A

larger surface area, thinner membranes

26
Q

Aqueous solubility is _____ proportional to electrostatic charge.

A

directly

27
Q

Lipid solubility is _____ proportional to electrostatic charge.

A

inversely

28
Q

Many drugs are _____ acids and bases.

A

weak

29
Q

Unprotonated acids are more _____-soluble and undergoes _____ clearance.

A

water-soluble, better clearance

30
Q

Protonated acids are more _____-soluble and are _____ to cross biological membranes.

A

lipid-soluble, more likely to cross biological membranes

31
Q

Unprotonated bases are more _____-soluble and are _____ to cross biological membranes.

A

lipid-soluble, more likely to cross biological membranes

32
Q

Protonated bases are more _____-soluble and undergoes _____ clearance.

A

water-soluble, better clearance

33
Q

pH below pKa: protonated __ unprotonated

A

>

34
Q

pH at pKa: protonated __ unprotonated

A

=

35
Q

pH above pKa: protonated __ unprotonated

A

<

36
Q

Excretion of a weak acid may be accelerated by _____ the urine with _____.

A

alkalinizing urine, bicarbonate (HCO3-)

37
Q

Excretion of a weak base may be accelerated by _____ the urine with _____.

A

acidifying urine, ammonium chloride (NH4Cl)

38
Q

Transfer of a drug from its site of administration to the bloodstream

A

Absorption

39
Q

Absorption is affected by

A

route of administration, blood flow, concentration

40
Q

Route of Administration: offers maximum convenience

A

oral

41
Q

Route of Administration: most common

A

oral

42
Q

For the oral route, absorption is

A

slow, less complete

43
Q

A significant amount of the drug is metabolized in the gut wall, portal circulation and liver before it reaches the systemic circulation

A

First-Pass Effect

44
Q

Route of Administration: instantaneous, complete absorption, bypasses first-pass effect

A

intravenous

45
Q

IV route is _____ dangerous than oral.

A

more dangerous

46
Q

Route of Administration: faster absorption, more complete absorption than oral, large volume, less irritation

A

intramuscular

47
Q

Anticoagulants cannot by given intramuscularly because they can cause

A

hematomas

48
Q

IM Injections to Buttocks: superolateral

A

safe

49
Q

IM Injections to Buttocks: superomedial

A

gluteus medius gait

50
Q

IM Injections to Buttocks: inferomedial

A

sciatica

51
Q

Route of Administration: slower absorption than IM, bypasses first pass effect

A

subcutaneous

52
Q

Route of Administration: direct absorption into the systemic venous circulation, bypasses the first-pass effect

A

buccal, sublingual, IV

53
Q

Route of Sublingual Administration

A

lingual vein → internal jugular vein → brachiocephalic vein → superior vena cava → right atrium

54
Q

Route of Administration: partial avoidance of the first-pass effect, large amounts, drugs w/ unpleasant taste, vomiting patient

A

rectal (suppository)

55
Q

Route of Rectal Administration: Superior Rectal Vein

A

IMV → PV (first-pass)

56
Q

Route of Rectal Administration: Middle Rectal Vein

A

IIV → IVC

57
Q

Route of Rectal Administration: Inferior Rectal Vein

A

IPV → IIV → IVC

58
Q

Route of Administration: delivery closest to the target in respiratory diseases, rapid absorption with minimal systemic effects, gases at room temperature, easily volatilized

A

inhalational

59
Q

Route of Administration: local effect, slowest

A

topical

60
Q

Topical Drugs: Most to Least Evaporation

A

tinctures > wet dressings > lotions > gels > aerosols > powders > pastes > creams > foams > ointments

61
Q

Topical Drugs: Acute Inflammation

A

drying agents: tinctures, wet dressings, lotions

62
Q

Topical Drugs: Chronic Inflammation

A

lubricating agents: creams, ointments

63
Q

Route of Administration: skin, systemic effect, slow, bypasses first-pass effect

A

transdermal

64
Q

Drug reversibly leaves the bloodstream and enters the target organ

A

Distribution

65
Q

Distribution is affected by

A

size of organ, blood flow, solubility, binding

66
Q

Distribution: determines concentration gradient between blood and the organ

A

size of organ

67
Q

Distribution: important determinant of the rate of drug uptake

A

blood flow

68
Q

Distribution: influences the concentration of the drug in the extracellular fluid surrounding blood vessels

A

Solubility

69
Q

Most barriers are _____ barriers.

A

lipid

70
Q

Distribution: increases the drug’s concentration in the compartment with macromolecules

A

Binding

71
Q

Acidic drugs are bound to

A

albumin

72
Q

Basic drugs are bound to

A

orosomucoid

73
Q

Chemical alteration of a drug in the body

A

Metabolism

74
Q

Metabolic Fates of Drugs

A

termination of drug action, drug activation, elimination without metabolism

75
Q

Termination of a drug action

A

Elimination

76
Q

Release of a drug and its metabolites

A

Excretion

77
Q

Duration of drug action is determined by

A

dose, rate of elimination

78
Q

Mode of elimination of drugs that are not metabolized

A

Excretion

79
Q

Elimination: concentration decreases exponentially over time

A

First-Order

80
Q

Elimination: concentration decreases by 50% for every half-life

A

First-Order

81
Q

Elimination: most common

A

First-Order

82
Q

Elimination: rate is proportionate to the concentration

A

First-Order

83
Q

Elimination: rate is constant

A

Zero-Order

84
Q

Elimination: concentration decreases linearly over time

A

Zero-Order

85
Q

Elimination: occurs when drugs have saturated their elimination

A

Zero-Order

86
Q

Drugs that follow Zero-Order Kinetics

A

warfarin, heparin, aspirin, tolbutamide, phenytoin, ethanol, theophylline