[2] Chapter 1 Introduction Flashcards
1
Q
Can be defined as the study of substances that interact with living systems through chemical processes
A
Pharmacology
2
Q
[Pharmacology] These interactions usually occur by _______ of the substance to regulatory molecules and ________ or _______ normal body processes.
A
binding
activating or inhibiting
3
Q
These substances may be chemicals administered to achieve a _______ _________effect on some process within the patient or for their _____ effects on regulatory processes in parasites infecting the patient.
A
beneficial therapeutic
toxic
4
Q
Often defined as the science of substances used to prevent, diagnose, and treat disease.
A
Medical Pharmacology
5
Q
Medical Pharmacology often defined as the science of substances used to _______, _______, and __________.
A
prevent, diagnose, and treat disease.
6
Q
Such deliberate therapeutic applications may be considered the proper role of _____________.
A
medical pharmacology
7
Q
Such deliberate ______ may be considered the proper role of medical pharmacology
A
therapeutic applications
8
Q
_____ is 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
9
Q
2 Large Domain
A
- medical pharmacology and toxicology
- environmental toxicology
10
Q
What domain?
aimed at understanding the actions of drugs as chemicals on individual organisms, especially humans and domestic animals.
A
medical pharmacology and toxicology
11
Q
What domain?
Both beneficial and toxic effects are included
A
medical pharmacology and toxicology
12
Q
Pharmacokinetics and Pharmacodynamics are in which domain?
A
medical pharmacology and toxicology
13
Q
Deals with the absorption, distribution, and elimination of drugs
- Pharmacokinetics
- Pharmacodynamics
A
Pharmacokinetics
14
Q
concerns the actions of the chemical on the organism.
- Pharmacokinetics
- Pharmacodynamics
A
Pharmacodynamics
15
Q
WHat is the 2nd domain?
A
Environment Toxicology
16
Q
Domain in which concerned with the effects of chemicals on all organisms and their survival in groups and as species
A
2nd domain: Environmental Toxicology
17
Q
3 reason why there are new drugs added every year
A
(1) increasing resistance by bacteria and other parasites
(2) discovery of new target processes in diseases that have not been adequately treated
(3) recognition of new diseases.
18
Q
Furthermore, a dramatic increase has occurred in the number of _______________(especially antibodies) approved during the last two decades. The development of new drugs and their regulation by government agencies are discussed in part II.
A
large molecule drugs
19
Q
THE HISTORY OF PHARMACOLOGYTHE HISTORY OF PHARMACOLOGY
who undoubtedly recognized the beneficial or toxic effects of many plant and animal materials.
A
Prehistoric people
20
Q
THE HISTORY OF PHARMACOLOGY
Beginning about ______years ago, sporadic attempts were made to introduce rational methods into medicine, but none was successful owing to the dominance of systems of thought (“schools”) that purported to explain all of biology and disease without the need for experimentation and observation.
A
1500 years ago
21
Q
THE HISTORY OF PHARMACOLOGY
It is when concepts based on observation and experimentation began to replace theorizing in physiology and clinical medicine.
A
Around the end of the 17th century
22
Q
THE HISTORY OF PHARMACOLOGY
As the value of these methods in the study of disease became clear, physicians in ______ and on_______ began to apply them systematically to the effects of traditional drugs used in their own practices.
A
Great Britain and on the Continent
23
Q
THE HISTORY OF PHARMACOLOGY
thus, ____ _____ the science of drug preparation and the medical uses of drugs—began to develop as the precursor to pharmacology.
A
materia medica
24
Q
THE HISTORY OF PHARMACOLOGY
materia medica is the drug ______ and the _____ uses of drugs—began to develop as the precursor to pharmacology.
A
preparation and the medical
25
# THE HISTORY OF PHARMACOLOGY
However, any real understanding of the mechanisms of action of drugs was prevented by the _________ of methods for purifying active agents from the crude materials that were available and—even more—by the _________for testing hypotheses about the nature of drug actions.
absence
lack of methods
26
# THE HISTORY OF PHARMACOLOGY
François Magendie and his student Claude Bernard began to develop the methods of what?
experimental physiology and pharmacology
27
# THE HISTORY OF PHARMACOLOGY
real advances in basic pharmacology during this time were accompanied by an outburst of unscientific claims by manufacturers and marketers of worthless "___________________"
“patent medicines.”
28
# THE HISTORY OF PHARMACOLOGY
It is when advances in chemistry and the further development of physiology laid the foundation needed for understanding how drugs work at the organ and cellular levels.
18th, 19th, and early 20th centuries
29
# THE HISTORY OF PHARMACOLOGY
It is when **François Magendie and his student Claude Bernard*** began to develop the methods of *experimental physiology and pharmacology.*
Late 18th century and early 19th century
30
# THE HISTORY OF PHARMACOLOGY
As new concepts and new techniques were introduced, information accumulated about drug action and the biologic substrate of that action, the_______
drug receptor
31
# THE HISTORY OF PHARMACOLOGY
Not until the concepts of rational therapeutics, especially that of the ________, were reintroduced into medicine—only about 60 years ago—did it become possible to adequately evaluate therapeutic claims.
**controlled clinical trial**
32
# THE HISTORY OF PHARMACOLOGY
In the late 18th and early 19th centuries, who began to develop the methods of experimental physiology and pharmacology?
Francois Magendie and his student Claude Bernard
33
# THE HISTORY OF PHARMACOLOGY
When was controlled clinical trial reintroduced into medicine?
(It is the concepts of rational therapeutics and did it become possible to adequately evaluate therapeutic claims
60 years ago
34
# THE HISTORY OF PHARMACOLOGY
It is when a major expansion of research efforts in all areas of biology began.
(2) years
Around the 1940s and 1950s
35
# THE HISTORY OF PHARMACOLOGY
It is the concepts of rational therapeutics and did it become possible to adequately evaluate therapeutic claims which was reintroduced into medicine about 60 years ago
Controlled Clinical Trial
36
# THE HISTORY OF PHARMACOLOGY
The molecular mechanisms of action of many drugs have now been identified, and numerous receptors have been isolated, structurally characterized, and cloned.
In fact, the use of receptor identification methods (described in Chapter 2) has led to the discovery of many _______—receptors for which no ligand has been discovered and whose function can only be guessed.
orphan receptors
37
# THE HISTORY OF PHARMACOLOGY
receptors for which no ligand has been discovered and whose function can only be guessed.
orphan receptors
38
# THE HISTORY OF PHARMACOLOGY
Studies of the local molecular environment of receptors have shown that receptors and effectors do not function in ________; they are strongly influenced by other receptors and by companion ________(what proteins.)
isolation;
regulatory protein
39
# THE HISTORY OF PHARMACOLOGY
THE HISTORY OF PHARMACOLOGY
Does receptors and effectors (function or not) in isolation based on studies of local molecular environment of receptors?
Do not function
40
# THE HISTORY OF PHARMACOLOGY
Most recently, it has become clear that ______________, __________, and other aspects of space *outside* the Earth’s environment require the development of ________ (what).
gravitational change
radiation
development of *space medicine*
41
# THE HISTORY OF PHARMACOLOGY
...One result of these discoveries is the confirmation that pharmacology represents an area where ________, ________,
_________, _______, _______, _______, and the ________ meet. (6)
anatomy
physiology
biochemistry
genetics
pathology
clinical medicine
environment
42
# THE HISTORY OF PHARMACOLOGY
Many problems that the health practitioner confronts can now be corrected or mitigated using ________________.
pharmacologic tools.
43
# THE HISTORY OF PHARMACOLOGY
the relation of the individual’s **genetic makeup** to his or her response to specific drugs—is becoming an important part of therapeutics
Pharmacogenomics
44
# THE HISTORY OF PHARMACOLOGY
This has led to the recognition of **unsuspected relationships** between receptor families and the ways that receptor proteins have evolved.
Decoding of the genomes of many species—from bacteria to humans
45
# THE HISTORY OF PHARMACOLOGY
This has led to open a *new area of possible manipulation* of the genes—epigenetics—that control pharmacologic responses.
discovery of ***regulatory functions*** exerted by the
**neighbors of chromosomes** and the noncoding regions of DNA on the expression of exons
46
# THE HISTORY OF PHARMACOLOGY
This has led to investigation of small interfering RNAs (siRNAs) and micro-RNAs (miRNAs) as therapeutic agents.
The discovery that small segments of RNA can interfere with protein synthesis with extreme selectivity
47
# THE HISTORY OF PHARMACOLOGY
Similarly, short nucleotide chains called _________(ANOs), synthesized to be complementary to natural RNA or DNA, can interfere with the readout of genes and the transcription of RNA.
antisense oligonucleotides
48
# THE HISTORY OF PHARMACOLOGY
Finally, new, efficient methods of DNA editing have made possible the modification of genes that encode proteins that are critical to immunologic functions, including ______ receptors on _____ cells. ----- These developments have led to a dramatic increase in large molecule therapeutics in the last 20 years
anticancer receptors on T-cells
49
# THE HISTORY OF PHARMACOLOGY
Unfortunately, the _________ is still exposed to vast amounts of inaccurate or unscientific information regarding the pharmacologic effects of chemicals.
## Footnote
This results in the irrational use of innumerable *expensive, ineffective, and sometimes harmful remedies* and *the growth of a huge “alternative health care” industry.*
medication-consuming public
50
# THE HISTORY OF PHARMACOLOGY
Manipulation of the legislative process in the United States has allowed many substances promoted for health—but not promoted specifically as “drugs”—to avoid meeting the Food and Drug Administration (FDA) standards described in the second part of this chapter.
| ---- n/a
51
# THE HISTORY OF PHARMACOLOGY
**lack of understanding of basic scientific principles in ______ and _______** and the *absence of _________ about public health issues* **have led to rejection of medical science, including vaccines**, by a segment of the public and to a *common tendency to assume that all adverse drug effects are the result of malpractice.*
biology and statistics
critical thinking
52
# THE HISTORY OF PHARMACOLOGY
3 General principles that the student should remember are
1 - that ***all substances*** can under certain circumstances be ______.
2 - that the chemicals in botanicals (herbs and plant extracts, “nutraceuticals”) are no different from chemicals in ________except for the much greater proportion of impurities in botanicals;
(3) that all dietary supplements and all therapies promoted as health-enhancing *should meet the same standards* of _____ and _____ as *conventional drugs and medical therapies. *
(1) that *all substances *can under certain circumstances be ***toxic***;
(2) that 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;
(3) that all dietary supplements and all therapies promoted as health-enhancing *should meet the same standards* of ***efficacy and safety*** as *conventional drugs and medical therapies. *
53
# THE HISTORY OF PHARMACOLOGY
...That is, there should be no artificial separation between________ and "________" or "________" medicine.
scientific medicine
“alternative” or “complementary” medicine
54
# THE HISTORY OF PHARMACOLOGY
Ideally, all nutritional and botanical substances should be tested by the same types of _____________(RCTs) as synthetic compounds.
randomized controlled trials
55
# THE HISTORY OF PHARMACOLOGY
Ideally, all ________ and ________ substances should be tested by the same types of randomized controlled trials (RCTs) as synthetic compounds.
nutritional and botanical
56
# THE HISTORY OF PHARMACOLOGY
Ideally, all nutritional and botanical substances should be tested by the same types of randomized controlled trials (RCTs) as _______ compound (what type of compoun?
Synthetic compound
57
# GENERAL PRINCIPLES OF PHARMACOLOGY
it describes the **effects of the body on drugs** (eg, absorption, excretion, etc.)
Pharmacokinetics
58
# GENERAL PRINCIPLES OF PHARMACOLOGY
deals with the ***absorption, distribution, metabolism, and elimination of drugs.*** Elimination of a drug may be achieved
by metabolism or by excretion.
| - Pharmacokinetics
- Pharmacodynamics
Pharmacokinetics
59
# GENERAL PRINCIPLES OF PHARMACOLOGY
Under Pharmacokinetics, it is a term sometimes used to describe the **processes of metabolism and excretion**
Biodisposition
60
# GENERAL PRINCIPLES OF PHARMACOLOGY
denotes the **actions of the drug on the body**, such as *mechanism of action* and *therapeutic and toxic effect*
| - Pharmacokinetics
- Pharmacodynamics
Pharmacodynamics
60
# GENERAL PRINCIPLES OF PHARMACOLOGY
Elimination of drug may be achieved by _____ and _____
metabolism or excretion
61
# GENERAL PRINCIPLES OF PHARMACOLOGY
concerns the *actions of the chemical on the organism*
- Pharmacodynamics
| - Pharmacokinetics
Pharmacodynamics
62
# GENERAL PRINCIPLES OF PHARMACOLOGY
effect on other organisms other than humans
Environment
63
# GENERAL PRINCIPLES OF PHARMACOLOGY
area of pharmacology concerned with
the use of chemicals in the prevention, diagnosis, and treatment of disease, especially in humans; science of substances used to
prevent, diagnose, and treat disease
Medical Pharmacology
64
# GENERAL PRINCIPLES OF PHARMACOLOGY
finds the exact mechanism of action of
drugs; Identifies the receptors
Pharmacogenomics
65
# GENERAL PRINCIPLES OF PHARMACOLOGY
any substance that brings about a change in biologic function through chemical actions
Drug
66
# GENERAL PRINCIPLES OF PHARMACOLOGY
substances that act on biologic systems at the chemical (molecular) level and alter their functions
Drug
67
# GENERAL PRINCIPLES OF PHARMACOLOGY
specific molecules in the biologic system that **plays a regulatory role**
Receptors
68
# GENERAL PRINCIPLES OF PHARMACOLOGY
molecular components of the body with which **drugs interact to bring about their effects**
Receptors
69
# THE NATURE OF DRUGS
the drug molecule interacts as an ______ (activator) or ________ (inhibitor) with a specific target molecule that plays a regulatory role in the
biologic system.
agonist (activator)
antagonist (inhibitor)
70
Agonist is ?
Activator
71
Antagonist is ?
Inhibitor
72
# THE NATURE OF DRUGS
Drugs that may interact directly with other drugs
Chemical antagonists
73
# THE NATURE OF DRUGS
Few drugs that interact almost **exclusively with water molecules**
Osmotic agents
74
# THE NATURE OF DRUGS
Drugs
may be synthesized within the body like what example?
Hormones
75
# THE NATURE OF DRUGS
Drugs may be chemicals not synthesized in the patient’s body that is?
xenobiotics
75
# THE NATURE OF DRUGS
drugs
that have **almost exclusively harmful effects. **
Poisons
75
# THE NATURE OF DRUGS
Who said that "the dose makes the poison" meaning that any substance can be hamtful if taken the wrong dosage
Paracelsus
75
# THE NATURE OF DRUGS
Theses are usually defined as poisons of biologic origin, ie, synthesized by plants or animals, in contrast to inorganic poisons such as lead and arsenic.
Toxins
75
# The Physical Nature of Drugs
To interact chemically with its receptor, a drug molecule must have the _______, _________,_________, _________ (4)
appropriate size
electrical charge
shape
atomic composition
75
# The Physical Nature of Drugs
a practical drug should be
_____ or excreted from the body at a reasonable rate so that its actions will be of appropriate duration
inactivated
75
# The Physical Nature of Drugs
Drugs that may be solid at room temp are eg.?
Aspirin, Atropine
76
# The Physical Nature of Drugs
Drugs that may be liquid eg. are?
Nicotine and Ethanol
76
# The Physical Nature of Drugs
Drugs that may be gaseous eg. are?
Nitrous Oxide
Isoflurane
Xenon
76
# The Physical Nature of Drugs
What various classes of organic compounds are presented in pharmacology?
Carbohydrates
Proteins
Lipids
Smaller Molecules
76
# The Physical Nature of Drugs
Examples of Inorganic elements that are both useful an dangerous drugs
Fluoride
Lithium
Iron
Heavy Metals
77
# The Physical Nature of Drugs
Many organic drugs are weak acidsm or bases.
## Footnote
T or F
True
## Footnote
This fact has important implications for the way they are handled by the body, because pH differences in the various compartments of the body may alter the degree of ionization of weak acids and bases
77
# Drug Size
78
# Drug Size
78
# Drug Size
The molecular size of drugs varies from very small to very large.
(lithium ion, molecular weight [MW] 7) < (eg, alteplase [tPA], a protein of MW 59,050).
78
Many antibodies are even larger;
| What is an example
erenumab
## Footnote
an antibody used in the management of migraine, has a MW of more than 145,000
78
However, most
drugs have molecular weights between ____ and _____
100 and 1000
78
To have a good “fit” to only one type of receptor, a drug molecule must be sufficiently unique in _____, ______, and other properties to prevent its binding to other receptors.
shape, charge
78
To achieve such selective binding, it appears that a molecule should in most cases be at least ______MW units in size
100 MW
78
The (lower/upper) limit of this narrow range is probably set by the requirements for specificity of action
lower limmit
78
The (lower/upper) limit in molecular weight is determined primarily by the requirement that drugs must be able to move within the body (e.g. from the site of administration to the site of action).
Upper
78
Drugs much larger than MW 1000 do not diffuse readily between compartments of the body
| T/F
True
78
Very (large/small) drugs (usually proteins) must **often be administered directly into the compartment where they have
their effect.**
Large
## Footnote
For **alteplase**, a clot-dissolving enzyme, the drug is
administered directly into the vascular compartment by
intravenous or intra-arterial infusion.
78
# DRUG SHAPE
Shape of a drug molecule must be such as to permit binding to its receptor site via the
receptor bonds
78
# DRUG SHAPE
Optimally, the drug’s shape is complementary to that of the __________ in the same way that a key is complementary to a _______.
## Footnote
shape = ?
key = ?
shape = receptor site;
ket = lock.
79
they contain one or more
*asymmetric centers* and *can exist as enantiomers*
| What type of molecule and drug? (2)
## Footnote
such enantiomers may be metabolized at different rates in the body, with important clinical consequences
endogenous molecules;
exogenous drugs
| which are optically active
79
Drugs with two asymmetric centers have how many diasterreomers?
| e.g., ephedrine, a sympathomimetic drug.
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