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leonee, pharm class > Chapter one pharmacology -leonee > Flashcards

Chapter one pharmacology -leonee Flashcards

1
Q

what is materia medica

A
  • first medical textbook dealing with Western medicine
  • a collection of works throughout history
  • body of knowledge on botany and medicinal substances
  • discusses its preparation and use
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2
Q

what was developed as the precursor to pharmacology

A

material medica

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3
Q

What is the study of chemicals inside the body

A

physiology

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4
Q

what is exogenous

A

chemicals outside the body

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5
Q

what is pharmacology

A

the study of chemical interactions with living systems- exogenous

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6
Q

Ayurvedic

A

From the Indian subcontinent

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7
Q

what is Toxicology

A

-poisons and toxins and how they affect the body.
-undesirable effects of chemicals on living systems

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8
Q

what symbol is used to represent medicine and caregivers

A

the rod of Asclepius

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8
Q

The first recorded physician

A

Imhotep, ancient Egypt
3000 BCE

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8
Q

Ancient Greek god of medicine

A

Asclepius

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9
Q

who is Hippocrates

A

the father of Western medicine

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10
Q

what is caduceus

A

is the rod of Hermes, represents trade or commerce

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11
Q

who is materia medica attributed to

A

dioscorides (c40 BCE)

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12
Q

paracelsus

A

the father of toxicology, 1493-1541

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13
Q

who said all things are poison, and nothing is without poison; only the dose permits something not to be poisonous and what does it mean

or “the dose makes the poison”

A

Paracelsus and it means depending on the dose if you give anything in large quantity it can be posionous

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14
Q

what does regulations have to do with?

A

adherence to scientific principles and clinical testing (controlled drug trial)
(the idea that we have to show that the drug is working)

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15
Q

Describe prehistoric early medicine

A

shamanism, animism, spiritualism, divination

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16
Q

what does having drug regulations do

A

evaluates therapeutic claims
controls worthless patent medicine
makes sure that a controlled drug trial is done

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17
Q

How many drug groups are there

A

70 groups

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18
Q

what are the branches of pharmacology

A

pharmacodynamics, pharmacokinetics, pharmacogenomics,
toxicology

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19
Q

what is pharmacodynamics

A

what the drug does to the body
(dose-response will change depending on how much of the drug you give)

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20
Q

what is pharmacogenomics

A

genetic profile determines how you respond to the drug.

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21
Q

what is pharmacokinetics

A

what the body does to the drug (has to do with what the half-life is, how the half-life is determined, how does it cross barriers)

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22
Q

what is an example of pharmacogenomics

A

if you are her2 positive you have a growth factor receptor on the surface of the tumor cell that will respond to a particular drug called her Herceptin

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23
Q

what is agonist

A

a drug that elicits a response from the receptor when it binds to that receptor

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24
Q

what is an example of an agonist

A

norepinephrine drug given will bind to the same receptors and will elicit the same response as epinephrine that’s already in the body

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25
Q

what is an antagonist

A

it blocks the endogenous ligand from binding to the receptor

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26
Q

what is an example of an antagonist

A

propranolol is given to slow the heart rate and epinephrine speeds it up by binding to the beta 1 receptor. propranolol blocks the effects of epinephrine by binding to the same receptor making it an antagonist

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27
Q

what are poisons, give examples

A

things that are nonbiologic
ex: arsenic, cadmium, lead

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28
Q

what are toxins, give examples

A

biological substances
ex: pufferfish, certain mushrooms

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29
Q

what are the physical nature of drugs

A

solid, liquid, gas

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30
Q

what are organic compounds

A

compounds that have carbohydrate, lipid, protein, nucleic acid as part of their makeup

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31
Q

what is an inorganic compound

A

compounds that have lithium, iron (Fe) as part of their makeup

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32
Q

what are the characteristics of drug size

A

expressed in molecular weight
most drugs are 100-1000 MW (usually in daltons)
>1000 MW: can not diffuse readily

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33
Q

what happens if a drug has a high molecular weight

A

it might not be able to bypass barriers so we might have to give into the bloodstream

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34
Q

receptor reactions need what to elicit the right reaction

A

appropriate size
electrical charge
shape
atomic composition

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35
Q

what are the types of bonds

A

covalent
electrostatic
hydrophobic

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36
Q

what are the characteristics of covalent bonds

A

strongest when they share electrons

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37
Q

what are examples of electrostatic bonds

A

charged molecules, hydrogen bonds
Van der Waals forces

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38
Q

what are the characteristics of electrostatic bonds

A

they attract because opposites attract, like ionic bonds

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39
Q

what are hydrophobic bonds

A

lipid-soluble drugs that form between a drug that has no charge and an active site of a receptor with no charge
-weak

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40
Q

what does specificity have to do with

A

how specific the drug have to fit perfectly into the site to elicit a response

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41
Q

how specific do covalent bonds have to be

A

covalent bond doesn’t have to be specific because of how strong the bonds are

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42
Q

how specific do hydrophobic bonds have to be

A

they have to be very specific and perfect to have a real response

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43
Q

what are isomers

A

different structures with the same chemical equation but different shapes

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44
Q

what are optimal isomers

A

mirror images of each other with the same molecules but it will not work the same in the body

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45
Q

what are racemic mixtures

A

a mixture of several different optical isomers

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46
Q

where do orthosteric drugs bind

A

binds inside the active site

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47
Q

where do allosteric drugs bind

A

binds outside the active site

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48
Q

what is nonspecific binding

A

drugs bind somewhere else

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49
Q

what are the characteristics of pharmacokinetic

A

ADME
Absorption
Distribution
Metabolism
Excretion

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50
Q

what is a native ligand

A

compound that’s in the body already

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51
Q

Describe drug-receptor interactions of agonist

A

drugs bind to receptors and activate response
the effect may be greater or lesser than the native ligand

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52
Q

describe the drug-receptor interaction of the antagonist

A

bind to receptor- prevent binding of the native ligand
does not activate the response

53
Q

what is EC50

A

where we see 50% of drug effect

54
Q

what is Kd

A

where we see 50% of receptors bound

55
Q

what is Bmax

A

maximum binding to receptor, can change depending on the amount of drug given

56
Q

what does Kd, not equal EC50

A

because you don’t have to have 100% of your receptors bound or 50%, sometimes there’s only 10% and you still receive the maximal effect

57
Q

what does an allosteric activator do when given with an agonist?

A

increases the maximal effect of drug

58
Q

what does the allosteric inhibitor do when given with an agonist

A

you see lesser effect because you cannot outcompete it

59
Q

characteristics of competitive antagonist drugs

A

bind and inhibit agonist response
can be countered by giving increased amounts of the agonist- it is surmountable

60
Q

characteristics of noncompetitive antagonists

A

you can never overcome the allosteric binding since it binds outside of the active site or if it is orthosteric forms a covalent bond that is unbreakable

61
Q

what is an example of an orthosteric competitive antagonist

A

propranolol

62
Q

compared to full agonists partial agonists have antagonist interaction

A

produce a lower response at full receptor occupancy
blocks full agonist binding

63
Q

what is an inverse agonist

A

when drugs favor the inactive form of a receptor leading to greater shutting down of downstream receptors worse than an antagonist

64
Q

Give an example of the administration of the opposite charge to inhibit the effect of a drug

A

giving protamine (+) to inhibit the effect of heparin (-)

65
Q

give an example of physiologic antagonism

A

drugs act at different receptors to squelch effect of other drugs

epinephrine binds to beta one to increase heart rate and acetylcholine binds to muscarinic receptors to decrease heart rate

66
Q

what are the pharmacodynamics of partial agonist

A

-the effect is much weaker than full agonist
in the absence of a full agonist, it acts as an agonist
in the presence of a full agonist, it acts as an antagonist because it is competing for the site

67
Q

example of direct agonists

A

epinephrine, norepinephrine

68
Q

example of indirect agonists (mimic) and how does it work

A

amphetamine, cocaine
they bind to the beta one receptor, increasing the transporter’s activity that transports epinephrine out of the cell. makes more epinephrine present at any given time

69
Q

what downstream effects can occur after a drug binds to a receptor

A

phosphorylation of other proteins, activation of different proteins and the downstream effectors

70
Q

what happens to the downstream effectors when a drug is bound to the receptor

A

the downstream effectors are all used up and they stop signaling

71
Q

what are signs of a good receptor

A

it has to be selective
it has to be altered once it binds to a drug for a downstream effect to occur

72
Q

what are the signs of a bad receptor or inert receptors

A

things that will bind to the drug but wont have any change in function.

73
Q

what is the most import drug carrier

A

albumin

74
Q

what happens when a plasma protein is bound to a drug

A

the drug cannot cross barriers

75
Q

what is another term for the unbound form of a drug

A

freeform

76
Q

why is albumin a bad receptor

A

albumin is not able to cross barriers due it being a protein and being large

77
Q

why is a decreased level of albumin important

A

it affects the dose we have to give. ex: if we give a patient who’s malnourished a drug with high protein affinity, it will have a higher effect because there is not a lot of albumin available to bind to the drug

78
Q

what other drug carriers are available

A

alpha one acid glycoprotein, proteins, cortisol, binding globulin

79
Q

what kind of drugs does albumin mostly bind to

A

acidic drugs

80
Q

what kind of drugs do alpha one acid glycoprotein bind to

A

basic drugs

81
Q

what kind of drugs does lipoproteins bind to

A

neutral drugs

82
Q

what is potency

A

concentration in the plasma or the dose you gave the patient. it tells us how much is in the bloodstream

83
Q

what is efficacy

A

the maximal response that a drug can deliver

84
Q

what does the therapeutic index do

A

it establishes the margin of safety for drugs, ED50 VS TD50

85
Q

What can lead to variations in drug responsiveness

A
  1. Alteration in concentration of drug that actually reaches the receptor
  2. Variation in concentration of endogenous receptor ligand
  3. Alteration in number or function of receptors
  4. Changes in components of response distal (downstream) to receptor
86
Q

tolerance

A

response of a drug changes over time

87
Q

what is tachyphylaxis

A

quick tolerance to a drug

88
Q

for drugs to cross the barrier what do they need to be

A

they need to be uncharged, no positive or negative charge because the barrier they have to cross is uncharged

89
Q

most barrier are provided by what and what do they have

A

cell membrane and they are made up of phospholipids

90
Q

what affects the charge of a drug

A

pKa- dissociation constant
ph of the environment the drug is in

91
Q

what is a weak acid

A

something that releases hydrogen ions in solution

92
Q

what is a weak base

A

takes up hydrogen ions from solutions

93
Q

if the ph of a drug is less than pKa what does it favor

A

it favors the protanted form, the form that has hydrogen ion attached to it

94
Q

if the ph of a drug is greater than pKa

A

it favors the unprotonated form that does not have hydrogen attached to it

95
Q

what does the henderson hasselbach equation do

A

it relates pKa to ph

96
Q

what does proteinated mean

A

if the drug has a hydrogen attached or not

97
Q

concentration in the renal tubule is what

A

ph dependent

98
Q

weak acids excrete faster in

A

alkaline urine

99
Q

what are drugs created by living organisms

A

biologics

100
Q

weak bases excrete faster in

A

acidic urine

101
Q

examples of drugs extracted from living systems

A

antibiotics, blood, transplants, microbata

102
Q

examples of drugs produced by recombinant dna

A

insulin, growth hormone, interferons, monoclonal antibodies and fusion proteins

103
Q

what are monoclonal antibodies produced from

A

produced by clones of a single-parent cell

103
Q

what are the two functions of antibodies

A

recognize and bind antigen
induce immune responses after binding

104
Q

how do monoclonal antibodies decrease adverse effects

A

because they only bind to very specific sites. they have an area called the antigen binding site that only binds to one particular antigen or one particular target

105
Q

what tells us a drug is a monoclonal antibody

A

it has an mab at the end of it

106
Q

what does the fda do

A

oversees development process in the us
grants approval for marketing
must be safe and effective
reviews all claims, makes a recommendation
places drugs in categories: otc, herbal supplements

107
Q

Describe prescription drugs

A

only available by recommendation of health professional
drug misuse has higher potential for harm
regulated by fda

108
Q

Describe nonprescription drugs

A

freely available to general public
low risk for harm/abuse
does not equate to safe

109
Q

describe thalidomide and why did fda refuse it

A

introduced in the 1950s for morning sickness
teratogen
FDA refused due to safety testing not being thorough enough
currently being used for multiple myeloma
was causing phocomelia in children born to pregnant mothers who took this drug

110
Q

who was instrumental in blocking this drug from going to the market

A

dr. oldham cook kelsey

111
Q

what occurs in phase 1 of clinical testing

A

safety, dosing, ADME (pharmacokinetic properties),

112
Q

what occurs in phase 2 of clinical testing

A

double-blind, efficacy, looking at patients who actually have the disease now

113
Q

what. is phase 3 of clinical testing

A

market formjulation, route

114
Q

what does NDA in clinical testing do

A

gives us the ability to market and put the drug on the market. usually when the company makes its money back

115
Q

what does IND in clinical testing mean

A

we can start testing in human

116
Q

drug patent expires when

A

20 years

117
Q

what is phase 4

A

looking at side effects reported to fda

118
Q

how long can nda approval process take

A

about one year

119
Q

what are some factors in receptor concept

A

receptor affinity determines dose
receptor selectivity varies per drug
receptor can be activated or blocked

120
Q

what can receptors be

A

receptors are proteins that can be regulatory proteins, enzymes, transport proteins, structural proteins

121
Q

what are orphan receptors

A

receptors identified in the body that we are not sure what they bind to

122
Q

give the receptor categorization by molecular structure

A

seven transmembrane receptors
ligand gated channels
ion channels
catalytic receptors
nuclear receptors
transporters
enzymes

123
Q

the first messenger that send up the signal is what

A

the signaling molecule, drug, endogenous ligand

124
Q

the second messager might have what

A

might have a cyclic amp, inositol 3 phosphate,
diacylglycerol

125
Q

what are the steps of cell signaling

A

signaling molecule
receptor
signal transduction proteins
second messengers
effector proteins

126
Q

what is a lag period

A

when receptors take a while to see a response

127
Q

persistence

A

the drug is given once and might last a longer period of time

128
Q

what is a kinase

A

any enzyme that attaches a phosphate group to another protein

129
Q

what three amino acids strains come together to form g protein

A

alpha, beta and gamma

129
Q
A
130
Q
A

leonee, pharm class (2 decks)

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