I.A. Introduction: The Nature of Drugs & Drug Development & Regulation Flashcards

1
Q

can be defined as the study of substances that
interact with living systems through chemical processes

A

Pharmacology

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2
Q

defined as the science of substances used to prevent, diagnose, and
treat disease

A

medical pharmacology

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3
Q

the branch of pharmacology that deals with the undesirable effects of chemicals on living systems, from individual cells to humans to complex ecosystems

A

Toxicology

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4
Q

aimed at understanding the actions of drugs as chemicals on individualorganisms, especially humans and domestic animals

A

medical pharmacology and toxicology

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5
Q

deals with the absorption, distribution, and elimination of drugs

A

Pharmacokinetics

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6
Q

concerns the actions of the chemical on the organism

A

Pharmacodynamics

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7
Q

concerned with the effects of chemicals on all organisms and their survival in groups and as species

A

environmental toxicology

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8
Q

the science of drug preparation and the medical uses of drugs

A

materia medica

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9
Q

the relation of the individual’s genetic makeup to his or her response to specific drugs

A

Pharmacogenomics

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10
Q

T/F

the chemicals in botanicals (herbs and plant extracts,
“nutraceuticals”) are no different from chemicals in manufactured drugs except for the much greater proportion of impurities in botanicals

A

true

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11
Q

defined as any substance that brings about a change in biologic function through its chemical actions

A

drug

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12
Q

the drug molecule interacts as an ___ or ___ with a specific target molecule that plays a regulatory role in the biologic system.

A

agonist (activator) or antagonist (inhibitor)

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13
Q

target molecule is called a ___

A

receptor

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14
Q

are drugs that have almost exclusively harmful effects

A

Poisons

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15
Q

defined as poisons of biologic origin

A

Toxins

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16
Q

most drugs have molecular weights between ___

A

100 and 1000

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17
Q

Drugs interact with receptors by means of ___

A

chemical forces or bond

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18
Q

3 major types of bonds

A

covalent
electrostatic
hydrophobic

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19
Q

___ bonds are very strong and in many cases
not reversible under biologic conditions.

A

Covalent

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20
Q

___ is much more common than covalent
bonding in drug-receptor interactions

A

Electrostatic bonding

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21
Q

are usually quite weak and are probably important in the interactions of highly lipid-soluble drugs with
the lipids of cell membranes and perhaps in the interaction of drugs with the internal walls of receptor “pockets.”

A

Hydrophobic bonds

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22
Q

drugs that bind through weak bonds to their receptors are generally more ___ than drugs that bind by means of very strong bonds

A

selective

[because weak bonds require a very precise fit of the drug to its receptor
if an interaction is to occur]

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23
Q

a drug that interacts with adrenoceptors

A

carvedilol

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24
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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25
Q

Area of pharmacology concerned with the
undesirable effects of chemicals, whether it is a
drug or poison, on biologic systems

A

TOXICOLOGY

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26
Q

the relation of the individual’s genetic makeup to his or her response to specific drugs

A

PHARMACOGENOMICS

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27
Q

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

A

DRUG

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28
Q

Hydrophobic bonds are usually quite ___

A

weak

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29
Q

___ MW For selective binding

A

100

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30
Q

___ MW For traversing to different barriers
of the body

A

1000

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31
Q

Cannot move within the body
because of impediments

____ MW

A

> 1000

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32
Q

Aspirin binds to the ___

A

platelets

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33
Q

The tendency of a drug that binds to a
receptor via a covalent bond is to have a
___ bond

A

permanent

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34
Q

a process to prevent and stop
bleeding in the body.

A

Hemostasis

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35
Q

Activates receptor-effector system
to the maximum extent (Ra-D
pool){activated form}

A

Full agonist

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36
Q

Binds to the same receptors and
activate them in the same way but
do not evoke as great a response

A

Partial agonist

37
Q

Binds to a site on the receptor molecule
separate from the agonist binding site

A

Allosteric modulators

38
Q

Enzymes are a class of ___

A

receptors

39
Q

they could bind together with the agonist

A

allosteric modulators

40
Q

Results in effects that are opposite of the
effects produced by conventional agonists

A

Inverse agonist

41
Q

Binds to a receptor, compete with and
prevent binding by other molecules

A

Antagonist

42
Q

They need to be activated by passing
through the liver

A

Prodrug

43
Q

types of permeation

A

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

44
Q

movement of molecules through the watery
extracellular and intracellular spaces

A

AQUEOUS DIFFUSION

45
Q

AQUEOUS DIFFUSION occurs within…

A

LARGER aqueous compartments
of the body (eg: interstitial space, cytosol, etc.) and
across epithelial membrane tight junctions and
the endothelial lining of blood vessels

46
Q

Movement of molecules through membranes and
other lipid structures

A

LIPID DIFFUSION

47
Q

LIPID DIFFUSION is governed by ___

A

Fick’s law

48
Q

TRANSPORT BY SPECIAL CARRIERS 2 TYPES

A
  1. Active transport
  2. Facilitated diffusion
49
Q

NET (norepinephrine transporter)

  1. Physiologic Function
  2. Pharmacologic Significance
A
  1. Norepinephrine reuptake from synapse
  2. Target of cocaine and some tricyclic antidepressants
50
Q

SERT (serotonin reuptake transporter)

  1. Physiologic Function
  2. Pharmacologic Significance
A
  1. Serotonin reuptake from synapse
  2. Target of selective serotonin reuptake inhibitors and some tricyclic antidepressants
51
Q

VMAT (vesicular monoamine transporter)

  1. Physiologic Function
  2. Pharmacologic Significance
A
  1. Transport of dopamine and norepinephrine into adrenergic vesicles in nerve endings
  2. Target of reserpine and tetrabenazine
52
Q

MDR1 (multidrug resistance protein - 1)

  1. Physiologic Function
  2. Pharmacologic Significance
A
  1. Transport of many xenobiotics out of cells
  2. Increased expression confers resistance to
    certain anticancer drugs; inhibition increases blood levels of digoxin
53
Q

MRP1 (multidrug resistance-associated protein -1)

  1. Physiologic Function
  2. Pharmacologic Significance
A
  1. Leukotriene secretion
  2. Confers resistance to certain anticancer
    and antifungal drugs
54
Q

the process by which the substance is bound at a cell-surface receptor, engulfed by the cell
membrane, and carried into the cell by pinching off of the newly formed vesicle inside the membrane

A

ENDOCYTOSIS

55
Q

Expulsion (or secretion) of
membrane-encapsulated material from the cell

A

EXOCYTOSIS

56
Q

Predicts the movement of molecules across a
barrier

A

FICK’S LAW OF DIFFUSION

57
Q

Drug absorption is faster in organs with larger
___

A

surface areas

58
Q

Drug absorption is faster from organs with ___ membrane barriers

A

thin

59
Q

The passive flux of molecules down a concentration gradient is governed by ___

A

Fick’s law

60
Q

Water soluble drugs are (polar/nonpolar)

A

polar

(they follow the water diffusion)

61
Q

Lipid soluble drugs are (polar/nonpolar)

A

nonpolar

62
Q

Aqueous solubility of a drug is a function of the ___ (degree of ionization, polarity) of the molecule

A

electrostatic charge

63
Q

Lipid solubility of a molecule is ___
proportional to its charge

A

inversely

64
Q

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

A

THE HENDERSON-HASSELBACH EQUATION

65
Q

amount absorbed into the systemic circulation

A

BIOAVAILABILITY

66
Q

When the drug passes through the ___, it is
metabolized and when the drug goes to the blood circulation, it will be less than 100% of what you administered

A

liver

67
Q

Instantaneous and complete absorption

A

INTRAVENOUS (IV) / PARENTERAL ABSORPTION

68
Q

Absorption maybe slower, and less complete

A

ORAL (swallowed)

69
Q

Absorption is often faster and more complete
(higher bioavailability) than oral

A

INTRAMUSCULAR (IM) ABSORPTION

70
Q

___ cannot be given by IM, causes
bleeding in the muscle

A

heparin

71
Q

Most vaccines are administered through
___

A

intramuscular injection

72
Q

___ are injected subcutaneously to avoid being
recycled by the liver

A

Insulin

73
Q

Slower absorption than IM route

A

SUBCUTANEOUS ABSORPTION

74
Q

____ drugs are pressed under
the tongue and the buccal

A

Nitroglycerin antianginal

75
Q

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

A

TOPICAL

76
Q

Application to the skin for systemic effect

A

TRANSDERMAL

77
Q

ABSORPTION OF DRUGS

ROUTES OF ADMINISTRATION (9)

A
  1. ORAL (swallowed)
  2. INTRAVENOUS (IV) / PARENTERAL
  3. INTRAMUSCULAR (IM)
    4.. SUBCUTANEOUS
  4. BUCCAL AND SUBLINGUAL
  5. RECTAL (suppository)
  6. INHALATION
  7. TOPICAL
  8. TRANSDERMAL
78
Q

(high/low) blood flow maintains a high drug
depot-to-blood concentration gradient

A

high

79
Q

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

A

CONCENTRATION

80
Q

DETERMINANTS OF DISTRIBUTION

A

SIZE OF THE ORGAN
BLOOD FLOW
SOLUBILITY
BINDING

81
Q

determines the concentration
gradient between blood and the organ

A

Size of the organ

82
Q

Important determinant of the rate of uptake

A

BLOOD FLOW

83
Q

If the drug is very soluble in cells, the concentration in the perivascular space will be ___ and diffusion from the vessel into the extravascular tissue will be ___

A

lower

facilitated

84
Q

Binding of drugs to macromolecules in the blood or tissue compartment will tend to ___ the drug’s concentration in that compartment

A

increase

85
Q

Amount of drug in the body to the concentration in
the plasma

A

Vd

86
Q

Drug elimination is the same as drug excretion

(T/F)

A

FALSE

*A drug maybe eliminated by metabolism long before the modified molecules are excreted from the body

87
Q

For most drugs, excretion is by way of the ___

A

kidneys

88
Q

Rate of elimination is proportionate to the
concentration

A

FIRST ORDER ELIMINATION

89
Q

Drug’s concentration in plasma ___
exponentially with time

A

decreases