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chapter 1 pharmacology Flashcards

1
Q

Body of knowledge concerned with the action
of chemicals on biologic systems, especially by
binding to regulatory molecules (receptors) and
activating or inhibiting normal body processe

A

pharmacology

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2
Q

Area of pharmacology concerned with the
use of chemicals in the prevention, diagnosis,
and treatment of disease, especially in humans

A

MEDICAL PHARMACOLOGY

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3
Q

Area of pharmacology concerned with the
undesirable effects of chemicals on
biologic systems

A

TOXICOLOGY

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4
Q

Identifies the exact mechanism of action
of one particular drug
Identifies the receptors

A

MOLECULAR BIOLOGY

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5
Q

Any substance that brings about a change

in biologic function through chemical actions

A

DRUG

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6
Q

Specific molecule in the biologic system that

plays a regulatory role

A

receptor

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7
Q

Drugs are given at a site ___________ from the

intended site of action

A

distant

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8
Q

general range of drug size

A

100 - 1000

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9
Q

MW For selective binding

A

100

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10
Q

MW For traversing to different barriers of the body

A

1000

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11
Q

MW
 Cannot move within the body
 Given directly at the site of action

A

> 1000

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12
Q 
 Chemical forces or bonds through
which the drug interacts with the
receptors
 Weaker bonds are more selective
bonds
A

DRUG RECEPTOR BONDS

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13
Q

DRUG RECEPTOR BONDS
 Strongest
 Irreversible

A

COVALENT

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14
Q

DRUG RECEPTOR BONDS
 More common
 Weaker
 Eg, between cation and an anion

A

ELECTROSTATIC BONDS

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15
Q

DRUG RECEPTOR BONDS
 Weakest
 Highly lipid soluble drug

A

HYDROPHOBIC BONDS

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16
Q 
To reach its receptors and bring about biologic
effect
 A drug molecule (eg, sedative) must
travel from the site of \_\_\_\_\_\_\_\_\_\_
(eg, gastrointestinal tract) to the site
of \_\_\_\_\_\_\_\_ (eg, brain)
A

administration- action

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17
Q

 Movement of drug molecules into and within

the biologic environment

A

PERMEATION

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18
Q

 Movement of molecules through the watery

extracellular and intracellular spaces

A

AQUEOUS DIFFUSION

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19
Q

aqueous diffusion is a passive or active process?

A

passive

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20
Q

AQUEOUS DIFFUSION is governed by

A

Governed by Fick’s law

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21
Q

where does aqueous diffusion take place? (membranes of ….)

A

Membranes of capillaries with small waterfilled pores

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22
Q

Movement of molecules through membranes

and other lipid structures

A

lipid diffusion

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23
Q

type of diffusion

Most important factor for drug permeation

A

lipid diffusion

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24
Q

LIPID DIFFUSION is governed by

A

Governed by Fick’s law

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25
Q

LIPID diffusion is a passive or active process?

A

PASSIVE

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26
Q 
TYPE OF PERMEATION
Drugs transported across barriers by
mechanisms that carry similar endogenous
substances
Capacity limited
A

TRANSPORT BY SPECIAL CARRIERS

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27
Q

IS TRANSPORT BY SPECIAL CARRIERS GOVERNED BY FICK’S LAW

A

NO

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28
Q

TRANSPORT BY SPECIAL CARRIERS

TYPES OF TRANSPORT

A

ACTIVE TRANSPORT

FACILITATED DIFFUSION

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29
Q

No energy required

 Downhill

A

FACILITATED DIFFUSION

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30
Q

Needs energy

 Against a concentration gradient

A

ACTIVE TRANSPORT

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31
Q

type of permeation
Binding to specialized components
(receptors) on cell membranes
 Internalization by infolding of the area of
the membrane and contents of the vesicle
are subsequently released into the cytoplasm

A

endocytosis

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32
Q

type of permeation
Permits very large or very lipid-insoluble
chemicals to enter the cell
 Eg, B12 with intrinsic factor and iron with
transferrin

A

endocytosis

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33
Q

 Reverse process
 Expulsion of membrane-encapsulated
material from the cell

A

EXOCYTOSIS

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34
Q

 Predicts the movement of molecules across

a barrier

A

FICK’S LAW OF DIFFUSION

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35
Q

Drug absorption is faster in organs with
______ (eg, small intestine)
than from organs with ______________ (eg, stomach)

A

larger surface areas
smaller absorbing
areas

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36
Q

Drug absorption is faster from organs with
(eg, lungs) than
those with (eg, skin)

A

thin membrane barriers

thick barriers

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37
Q

fick’s law
measure of the mobility
of the drug in medium of the diffusion path

A

Permeability coefficient

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38
Q

fick’s law

length of the diffusion path

A

Thickness

39
Q

a function of the electrostatic charge (degree of ionization,
polarity) of the molecule

A

Aqueous solubility

40
Q

Water molecules are attracted to —— forming an aqueous shell
around them

A

charged

drug molecules

41
Q

——- solubility of a molecule is inversely proportional to its charge

A

lipid

42
Q

lipid solubility of a molecule is —— proportional to its charge

A

inversely

43
Q

Many drugs are —- bases or —- acids

A

weak

44
Q

determines the fraction of molecules charged (ionized) versus uncharged
(nonionized

A

pH of the medium

45
Q

Fraction of molecules in the ionized state can

be predicted by means of the

A

H-H equation

46
Q

Neutral molecule that can form a cation
(+ charged) by combining with a proton
(hydrogen ion)

A

WEAK BASE

47
Q

Ionized, —– polar, —- water soluble

when they are protonated

A

more

48
Q 
 Neutral molecule that can reversibly
dissociate into an anion (- charged) and
a proton ( hydrogen ion)
 Not ionized, less polar, less water soluble
when they are protonated
A

WEAK ACID

49
Q

base
charged,
more water-soluble

A

protonated weak base

50
Q

base
uncharged,
more lipid soluble

A

unprotonated weak base

51
Q

acid
uncharged,
more lipid soluble

A

protonated weak acid

52
Q

acid
charged,
more water-soluble

A

unprotonated weak acid

53
Q

Clinically important when it is necessary
to estimate or alter the partition of drugs
between compartments of different pH

A

Henderson-Hasselbach Equation

54
Q

When a patient takes an overdose of a weak

acid drug, excretion maybe accelerated by

A

alkalinizing the urine

55
Q

Weak acids dissociate to its
in alkaline urine and cannot readily diffuse back
from the renal tubule back to the blood

A

charged, polar form

56
Q

amount absorbed into the systemic circulation /

amount of drug administered

A

BIOAVAILABILITY

57
Q

ROUTES OF ADMINISTRATION

 Maximum convenience
 Absorption maybe slower, and less complete

A
  1. ORAL (swallowed)
58
Q

 Some drugs have low bioavailability when

given

A

orally

59
Q

Subject to first-pass effect

A

oral administration

60
Q

(significant amount
of the agent is metabolized in the gut wall,
portal circulation, and liver before it reaches
the systemic circulation)

A

first pass effect

61
Q

ROUTES OF ADMINISTRATION

 Instantaneous and complete absorption
 Bioavailability by definition is 100%
 Potentially more dangerous, high blood
levels reached if administration is too rapid

A
  1. INTRAVENOUS (IV)/PARENTERAL
62
Q

ROUTES OF ADMINISTRATION

 Absorption is often faster and more complete
(higher bioavailability) than oral
 Large volumes (>5 ml into each buttock) if the
drug is not irritating

A
  1. INTRAMUSCULAR (IM)
63
Q

 First-pass effect is avoided
 Heparin cannot be given by this route,
causes bleeding in the —

A

INTRAMUSCULAR (IM)

64
Q

ROUTES OF ADMINISTRATION

 Slower absorption than IM route
 First-pass effect is avoided
 Heparin can be given by this route, does
not cause hematoma

A
  1. SUBCUTANEOUS
65
Q

(in the pouch between gums
and cheeks or under the tongue)
 Permits absorption direct into the systemic
circulation, bypassing hepatic portal circuit
and first-pass metabolism

A

BUCCAL AND SUBLINGUAL

66
Q

ROUTES OF ADMINISTRATION
Slow or fast depending on formulation of
the product

A

BUCCAL AND SUBLINGUAL

67
Q

ROUTES OF ADMINISTRATION

 Partial avoidance of first-pass effect
(not completely as the sublingual route)
 Suppositories tend to migrate upward in
the rectum where absorption is partially
into the portal circulation
A
  1. RECTAL (suppository)
68
Q

ROUTES OF ADMINISTRATION
Larger amounts of unpleasant drugs
are better administered —–
 May cause significant irritation

A
  1. RECTAL (suppository)
69
Q

ROUTES OF ADMINISTRATION

 For respiratory diseases
 Delivery closest to the target tissue
 Results into rapid absorption because of
the rapid and thin alveolar surface area

A
  1. INHALATION
70
Q

Drugs that are gases at room temperature
(eg, nitrous oxide), or easily volatilized
(anesthetics)
Drugs that are gases at room temperature
(eg, nitrous oxide), or easily volatilized
(anesthetics)

A
  1. INHALATION
71
Q

ROUTES OF ADMINISTRATION

 Application to the skin or mucous membrane
of the eye, nose, throat, airway, or vagina
for local effect

A
  1. TOPICAL
72
Q

ROUTES OF ADMINISTRATION

 Rate of absorption varies with the area
of application and drug’s formulation
 Absorption is slower compared to other
routes

A
  1. TOPICAL
73
Q

ROUTES OF ADMINISTRATION

 Application to the skin for systemic effect
 Rate of absorption occurs very slowly
 First-pass effect is avoided

A
  1. TRANSDERMAL
74
Q

 Influences absorption from IM, subcutaneous,

and in shock

A

BLOOD FLOW

75
Q

 High blood flow maintains a — drug depotto-blood concentration gradient
 Maximizes absorption

A

high

76
Q

Concentration gradient
 Major determinant of the rate of absorption
(Fick’s law)

A

concentration

77
Q

DETERMINANTS OF DISTRIBUTION

 determines the concentration
gradient between blood and the organ
 Eg, skeletal muscle and brain

A
  1. Size of the organ
78
Q

DETERMINANTS OF DISTRIBUTION

 Important determinant of the rate of uptake

A
  1. Blood flow
79
Q

Well-perfused organs

A

 Brain
 Heart, kidneys
 Splanchnic organs

80
Q

If the drug is ____ in cells, the
concentration in the perivascular space
will be ______ and diffusion from the vessel
into the extravascular tissue will be facilitated

A

very soluble

lower

81
Q

DETERMINANTS OF DISTRIBUTION
—- of drugs to macromolecules in
the blood or tissue compartment will tend
to increase the drug’s concentration in that
compartment

A

Binding

 Binding

82
Q

Amount of drug in the body to the

concentration in the plasma

A

APPARENT VOLUME OF DISTRIBUTION

83
Q

METABOLISM OF DRUGS
Action of many drugs is terminated before they
are excreted
 Metabolized to biologically inactive derivatives
 Conversion to a metabolite is a form of
elimination

A

AS MECHANISM OF TERMINATION OF

DRUG ACTION

84
Q

METABOLISM OF DRUGS

 Inactive as administered and must be
metabolized in the body to become active
 Eg, levodopa, minoxidil
 Many drugs are active as administered
and have active metabolites as well
 Some benzodiazepines
A

AS MECHANISM OF DRUG ACTIVATION

PRODRUGS

85
Q

METABOLISM OF DRUGS

 Drugs not modified by the body
 Continue to act until they are excreted
 Eg, lithium

A

DRUG ELIMINATION WITHOUT

METABOLISM

86
Q

Determinants of the duration of action for most

drugs

A

 Dosage
 Rate of elimination following the last dose
 Disappearance of the active molecules
from the bloodstream

87
Q

Are Drug elimination and drug excretion similar

A

NO.
A drug maybe eliminated by metabolism
long before the modified molecules are
excreted from the body

88
Q

For most drugs, excretion is by way of the ——

(except ——-)

A

kidneys

anesthetic gases-lungs

89
Q

For drugs with active metabolites
(eg, diazepam), elimination of the parent
molecule by metabolism is not synonymous
with

A

termination of action

90
Q

For drugs that are not metabolized,—-

is the mode of elimination

A

EXCRETION

91
Q

 Rate of elimination is proportionate to the
concentration (ie, the higher the concentration,
the greater the amount eliminated per unit
time)
 Drug’s concentration in plasma decreases
exponentially with time

A

A. FIRST ORDER ELIMINATION

92
Q

 Half-life of elimination is constant regardless
of amount of drug in the body
 Concentration of such drug in the blood will
decrease by 50% for every half-life
 Most common process
 Followed by most drugs

A

FIRST ORDER ELIMINATION

93
Q

 Rate of elimination is constant regardless
of concentration
 Occurs with drugs that saturate their
elimination of mechanism at concentrations
of clinical interest

A

ZERO ORDER ELIMINATION

94
Q

Concentration of such drugs in plasma
decrease in linear fashion over time
 With higher doses, there will be bigger
chances of toxic effect because the patient
may not be able to eliminate it
 Eg, alcohol, phenytoin, aspirin

A

ZERO ORDER ELIMINATION

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