Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharmacology I > Intro to Pharmacology > Flashcards

Intro to Pharmacology Flashcards

1
Q

what is pharmacology

A

the study of the effects of drugs on the function of living systems

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

what is a drug

A

a chemical substance of known structure, other than a nutrient or an essential dietary ingredient, which when administered to a living organism produces a biological effect

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

what was the first textbook of pharmacology

A

de materia medica

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

who wrote de materia medica

A

pedanius dioscorides

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

what did paul ehrlich do

A
  • modern chemotherapy
  • german physician scientist
  • determined how to differentiate healthy tissue from invading pathogen by gram staining
  • made salvasan (arsphenamine) to tx syphilis
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

what did alexander flemming do

A
  • st marys in london
  • staphylococcus cultrues contaminated with mold
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

when was FDA created

A

1938

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

what are the divisions of pharmacology

A

basic and clinical pharmacology and organ system pharmacology

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

what makes up basic and clinical pharmacology

A

pharmacokinetics and pharmacodynamics (PKPD)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

what are the sub disciplines of pharmacology

A
  • pharmacology
  • pharmacogenetics
  • pharmacogenomics
  • pharmacoepidemiology
  • pharmacoeconomics
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

what is involved in pharmacokinetics

A

-absorption
- distribution
- metabolism
- excretion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

what is involved in pharmacodynamics

A
  • drug-receptor interactions
  • signal transduction
  • drug effects
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

what is pharmacoepidemiology

A

the study of drug effects at the population level
- concerned with variability of drug effects between individuals in a population and between populations
- made possible with big data sets

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

what is pharmacoeconoics

A

the study of cost and benefits/detriments of drugs used clinically
- made possible with big data sets

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

what is the difference between pharmacology and toxicology

A

pharmacology is the beneficial effects of drugs and toxicology is the adverse effects of drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

what does the FDA do

A

adminsitrative body that oversees drug evaluation process

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

FDA grants approval for marketing ______

A

new drug products

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

to get FDA approval for marketing what evidence is needed

A

safety and efficacy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

safe does not mean complete absence of _____

A

risk

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

FDA shares responsibility with _____ for food safety

A

USDA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

what did the dietary supplement health and education act of 1994 do

A
  • prohibited full FDA review of supplements and botanicals as drugs
  • established labeling requirements for dietary supplements
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

the burden of safety and efficacy is on the _____ for supplements

A

manufacturer not the FDA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

what is the definition of drug by the FDA

A

a substance other than food recognized by an official pharmacopoeia or formulary intended:
- for use in the diagnosis, cure, mitigation, treatment or prevention of disease
- to affect the structure or any function of the body
- for use as a component of a medicine but not a device or a component, part or accessory of a device

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

what is a generic drug defined by the FDA as

A

the same as a brand name drug in dosage, safety, strength, how it is taken , quality, performance, and intended use

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

before approving a generic drug product what does the FDA base evaluations off of

A

substitutability or therapeutic equivalence of generic drugs based on scientific evaluations

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

what is the drug development process

A
  • chemical synthesis and in vitro screening
  • preclinical testing
  • phase I
  • phase II
  • phase III
  • phase IV
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

when are healthy subjects tested in the drug development process

A

phase I

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

when are disease subjects tested in drug development process

A

phase II

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

when is broad testing done done in the drug development process

A

phase III

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

when is marketing and post marketing surveillance done

A

phase IV

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

who said “a drug will not work unless it is bound”

A

paul ehrlich

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

what are the protein targets for drug binding

A
  • receptors
  • enzymes
  • carrier molecules
  • ion channels
  • specific circulation plasma proteins
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

what are the “other” targets for drugs

A

ion chelators

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

what are the nucleic acid targets for drug binding

A
  • RNA and DNA
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

what are receptors

A

protein molecules which function to recognize and respond to endogenous chemical signals
- may also bind xenobiotics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

what are xenobiotics

A

foreign chemicals that does not exist in the body otherwise

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

what are receptors classified based on

A

ligands

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

what are the receptors in the autonomic nervous system

A
  • adrenergic receptors
  • cholinergic
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

what are the adrenergic receptors

A

-alpha1
- alpha 2
- beta 1
- beta 2
- beta 3

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
39
Q

what are the cholinergic receptors

A

muscarinic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
40
Q

what are the vascular system receptors

A
  • angiotensin II receptors (AT1 and At2)
  • endothelin receptors (ETa and ETb)
  • prostaglandin receptors (DP, EP, FP, IP, TP)
  • histamine receptors (H1, H2, H3)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
41
Q

what are the steroid receptors

A
  • estrogen receptors (ER alpha, ER beta)
  • androgen receptor
  • glucocorticoid receptor (cortisol)
  • mineralocorticoid receptor (aldosterone)
  • retinoid X receptor (RXR)
  • constitutive androstane receptor (CAR_
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
42
Q

for a drug to be useful

A
  • must act selectively on particular cells and tissues
  • must show a high degree of binding site specificity
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
43
Q

for a protein to function as a receptor

A
  • generally shows a high degree of ligand specificity
  • bind only molecules of certain physicochemical properties such as size, shape, charge, lipophilicty
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
44
Q

what does angiotensin II do

A

selectively activates angiotensin II receptors in vascular smooth muscle to cause contractiona

45
Q

angiotensin II does not affect smooth muscle in:

A

the GI tract, genitourinary tract or uterus

46
Q

angiotensin II receptors selectively bind:

A

angiotensin II

47
Q

angiotensin II does not bind:

A

angiotensinogen or angiotensin IV

48
Q

describe electrostatic bonds

A
  • weaker: hydrogen bonding and van der waals forces (dipoles)
  • stronger: ionic bonding
  • most common bonds
49
Q

describe hydrophobic bonds

A
  • less common
  • weak associations of hydrophobic compounds with hydrophobic domains of receptors
50
Q

describe covalent bonds

A
  • relatively rare
  • permanent, lasting bonding
  • aspirin and cyclooxygenase
  • omeprazole and proton pump
51
Q

describe lipophilic properties of drugs

A
  • more soluble in fat than blood
  • steroids
  • readily diffuse across membranes
  • more likely to be metabolized by gut and liver
52
Q

describe hydrophilic properties of drugs

A
  • more soluble in blood than fat
  • small molecules, weak acids/bases
  • ionized at physiologic pH (7.4)
  • not as easy to diffuse across plasma membranes
  • more likely to be excreted unchanged by kidney
53
Q

what is pKa

A

the pH at which the concentrations of ionized and unionized species are equal

54
Q

what is the example of a weak acid and what would the pKa be

A

aspirin
- 3.5

55
Q

what is an example of a weak bases and the pKa

A

epinephrine
-8.7

56
Q

what are enantiomers

A

1 pair for each chiral carbon

57
Q

what is carvedilol

A

alpha 1, beta 1, and beta 2 adrenergic receptor antagonist used to treat heart failure

58
Q

what does R (+) carvedilol do

A

blocks alpha adrenergic receptors

59
Q

what does S (-) carvedilol do

A

blocks beta adrenergic receptors

60
Q

what does R,S (+/-) carvedilol do

A

blocks alpha, Beta adrenergic receptors

61
Q

what is affinity

A

tendency of a drug to bind the receptor

62
Q

what is the dissociation constant (Kd)

A

concentration required for 50% saturation of available receptors

63
Q

higher the Kd, _____ the affinity

A

lower

64
Q

what is efficacy

A

tendency of a drug to activate the receptor once bound

65
Q

efficacy is generally expressed as:

A

dose-response curves or concentration effect curves

66
Q

highly effective drugs generally have ___ affinity

A

high

67
Q

an agonist possesses _____

A

significant efficacy

68
Q

full agonist = elicits ___ response

A

maximal

69
Q

partial agonist = elicits _____, even when ______

A

partial response, 100% of receptors are occupied

70
Q

antagonist possesses ____ efficacy

A

zero

71
Q

what do allosteric agonists and antagonists do

A
  • bind to the same receptor but do not prevent binding of the agonist
  • may enhance or inhibit the action of agonists
72
Q

what does the addition of an antagonist to an agonist do to the dose response curve

A

shifts it to the right

73
Q

where do competitive agonists and antagonists bind on the receptor

A

at the same site

74
Q

where do allosteric agonists and antagonists bind on the receptor

A

different sites

75
Q

what does an allosteric activator do

A

increase response to a drug

76
Q

what does an allosteric inhibitor do

A

decreases efficacy

77
Q

most receptors are in an ___ state

A

inactive

78
Q

agonists have high affinity for _____ state and ______

A

activated; stabilizes it

79
Q

what does a full agonist do to receptor action

A
  • high affinity for Ra and stabilize Ra on binding
  • shift nearly entire pool of receptors from Ri to Ra
  • maximal effect is produced
80
Q

what does a partial agonist do to receptor actions

A
  • do not stabilize Ra as effectively
  • significant fraction stays in Ri pool
  • only partially effective no matter how high concentration
  • some can act as agonist or antagonist
81
Q

when would a partial agonist act as an agonist? antagonist?

A
  • act as agonist if no full agonist is present
  • act as antagonist if full agonist is present
82
Q

what is an example of a partial agonist and describe it

A

-pindolol, beta adrenergic receptor antagonist when epinephrine is present, agonist when absent

83
Q

what does an antagonist do as receptor actions

A
  • Ra and Ri stay in same relative amounts as in the absence of any drug
  • no change in effect measured
  • block effects of agonist
84
Q

what does inverse agonist do to receptor actions

A
  • higher affinity for Ri than for Ra
  • stabilize Ri on binding
  • reduces any constitutive activity of receptor thus producing opposite effects as a conventional agonist
85
Q

what is an example of an inverse agonist and describe it

A
  • gamma- aminobutyric acid (GABA) receptors; diazepam agonist, flumazenil antagonist
86
Q

what is the formula for drug- receptor binding

A

B = Bmax x C/ C + Kd

87
Q

what is B in the drug receptor binding equation

A

drug bound to receptors at given concentration (C)

88
Q

as dose increases:

A

binding increment diminishes

89
Q

what is Bmax in the drug receptor binding equation

A

point at which all receptors are bound

90
Q

what is the equation for concentration-effect (dose-response)

A

E = Emax X C / C + EC50

91
Q

what does E stand for in the concentration effect equation

A

effect observed at given concentration

92
Q

what is Emax in the concentration effect equation

A

point at which no further effect is achieved as dose increases further

93
Q

what does EC50 stand for in the concentration- effect equation

A

concentration of drug that produced 50% of maximal effect/response

94
Q

what does a competitive antagonist do

A
  • bind to same site on receptor as agonist
  • compete with agonist for binding
  • with fixed agonist concentration, progressive increases in antagonist will decrease effect up to completely stopping it
95
Q

what can overcome competitive antagonist

A

increasing agonist concentration

96
Q

describe noncompetitive antagonists

A
  • often bind covalently and irreversibly
  • often allosteric inhibition but can be same binding site as agonist
97
Q

will increasing agonist concentration overcome noncompetitive antagonist

A

not always

98
Q

what does the addition of a noncompetitive antagonist to an agonist do to concnetration- effect curve

A

reduced max effect

99
Q

what is an example of a chemical antagonist

A

ionic interaction between positively charged protamine and negatively charged heparin
- protamine antagonizes heparin

100
Q

what is an example of a physiologic antagonist

A

different regulatory pathways mediated by different receptors resulting in opposing actions
- anticholinergic atropine can physiologically antagonize effects of beta blockers on heart rate

101
Q

what does atropine do

A

increase heart rate

102
Q

what do beta blockers do

A

decrease herat rate

103
Q

what do pharmacokinetic antagonists do and give example

A
  • one drug increases the metabolism of another
  • rifampin increases metabolism of many drugs
104
Q

what ways can drug- receptor actions be terminated

A
  • dissociation of drug from receptor
  • dissociation of drug from receptor but effects continue for some time
  • covalently bound drugs require destruction of the drug- receptor complex and synthesis of new receptors
  • desensitization
105
Q

why do effects continue for some time after dissociation of drug from receptor

A

downstream activation of effects by kinase phosphorylation of downstream proteins

106
Q

how do activated effectors be deactivated

A

phosphatase dephosphorylation of downstream proteins

107
Q

what is another word for desensitization

A

tachyphylaxis

108
Q

what are the mechanisms of desensitization

A
  • change in receptors: phosphorylation of receptors
  • translocation of receptors: beta- adrenergic receptor internalization
  • exhaustion of mediators: NT depletion
  • increased drug metabolism
  • physiologic adaptation: BP lowering from a diuretic
  • active extrusion of drug from cell: multi-drug resistnace (P-glycoprotein)
109
Q

how long do rapid responses to drug effects take and what are examples

A
  • seconds to minutes
  • beta- adrenergic receptor activation
  • nicotinic-acetylcholine receptor activation in nerve synapse
110
Q

how long do intermediate responses to drug effects take and give example

A

minutes to hours
- receptor desensitization

111
Q

how long do delayed responses to drug effects take and give example

A
  • hours to days
  • steroid induced increase in gene expression

Pharmacology I (12 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions