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House Pharmacology > Pharmarcodymamic > Flashcards

Pharmarcodymamic Flashcards

1
Q

Pharmacodynamics describes the effect of _____

A

the drug on the body

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2
Q

The components of pharmacodynamics includes
*Drug ____(___)
*Drug ____(_____)

A

Action; invisible

Effect; visible

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3
Q

DRUG ACTION
-Drug action refers to the mechanism by which _______

A

the drug produces desirable or undesirable effects in the body

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4
Q

TYPES OF DRUG ACTION
-list 5

A

Stimulation
-Depression
-Irritation
-Replacement
-Cytotoxic

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5
Q

Stimulation
Involves ________
E.g. ___ in Cardiac arrest

A

the selective enhancement of specific activity done by a specialized cell

Adrenaline

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6
Q

Depression
Involves the ______
E.g. _____ for Hypertension

A

selective diminution of specific activity done by a specialized cell

Lisinopril

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7
Q

Irritation
Involves producing ______
E.g. ——- for Joint and Muscle pain

A

non selective noxious effect on non-specialized cells

Methylsalycylate

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8
Q

Replacement
Involves _______
E.g ______ in Diabetes Mellitus

A

replacement of deficient endogenous substances

Insulin

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9
Q

Cytotoxic action
Involves the _______, usually ———- or _____, without significantly affecting other cells
E.g. ———- for cancer

A

selective destruction of cells

neoplasm or microbes

Cyclophosphamide

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10
Q

MECHANISM OF THE DRUG ACTION

_____
_____
____

A

Physical
Chemical
Biochemical

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11
Q

Physical mechanism
-Drug neither produces a _____ or _____
-Effect are purely _____
-E.g.
*______ for Constipation
*______ binds with Poisons
*_____ as an Osmotic diuretic

A

chemical reaction or change in the cells of the body

physiological

Laxatives

Activated charcoal

Mannitol

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12
Q

Chemical mechanism
-Drugs act by producing ______
-E.g.
*_____ for dyspepsia
*______ as chelating agents.
*_____ as a choline esterase reactivator.
*Cholestyramine for sequestration of bile acids and cholesterol in the gut

A

a chemical reaction in the body

Antacids

Deferoxamine

Pralidoxime

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13
Q

Biochemical mechanism ( _____ )
List them

A

RICE

Receptors

Ion channels

Carrier

Enzymes

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14
Q

Receptors
______ for Asthma
Ion channels
______ for Local anesthesia
Carrier
______ for Peptic Ulcer Disease
Enzymes
______ for Hypertension

A

Albuterol

Lidocaine

Omeprazole

Captopril

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15
Q

RECEPTORS

Ligand gated channel receptors
-Location: ____
-Effectors:____
-Coupling: ____
-Examples: GABA Type __
-Drugs: ——
-Structure: Oligometric assembly of subunits surrounding central pore

A

Membrane

Ion channel

Direct

A

Benzodiazepines

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16
Q

G-protein coupled receptors
-Location:_____
-Effectors: _____
-Coupling:______
-Examples:_____
-Drugs: _____
-Structure: Monomeric or Dimeric structure comprising seven transmembrane helices.

A

Membrane

Channel or Enzymes

G-protein

Muscarinic receptors

Atropine

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17
Q

Enzyme linked receptors
-Location: ____
-Effectors: _____
-Coupling: ____
-Examples:______
-Drugs:_____
-Structure: Single Transmembrane Helix linking extracellular receptor domain to intracellular kinase domain.

A

Membrane

Enzyme
Direct

Insulin receptors

Insulin

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18
Q

Intracellular receptors
-Location:_____
-Effectors:______
-Coupling:_____
-Examples:______
-Drugs:_____
-Structure: Monomeric structure with separate receptor and DNA binding domains.

A

Intracellular

Gene transcription

via DNA

Steroid receptors

Steroid

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19
Q

DRUG RECEPTOR RELATIONSHIP

____
_____

A

Affinity
Intrinsic activity

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20
Q

Affinity (A):
________

A

Propensity of a drug to bind with a given receptor

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21
Q

Intrinsic activity (I.A):
Capacity of a drug to ________

A

induce functional change in a given receptor in a way that produces a biological response

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22
Q

all drugs have intrinsic activity

T/F

A

F

Not all

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23
Q

if a drug is using a receptor, there must be ____ and ____

A

affinity and a bond

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24
Q

DRUG RECEPTOR OUTCOME

List 4

A

Full agonist
Partial agonist
Inverse agonist
Antagonist

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25
Q

Full agonist
Drug that _______
Full Agonist = A + I.A =___

A

stimulates a given receptor to produce a maximal biological response

1

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26
Q

Partial agonist
Drug that ________
Partial Agonist = A + I.A = ___

A

stimulates a given receptor to produce a sub-maximal biological response

> 0 but < 1

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27
Q

Inverse agonist
Drug that _____
Inverse Agonist = A+ I.A = ____

A

interacts with a given receptor to produce a negative biological response

< 0 but > -1

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28
Q

Antagonist
Drug that _____
Antagonist = A + I.A =__

A

interacts with a given receptor but does not produce any response

0

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29
Q

DRUG RECEPTOR REGULATION

Up-regulation
Increase in the _____ leads to
Increase _____

Down-regulation
Decrease in the ______ leads to
Decrease ______

A

number of receptors

sensitivity of the receptor

number of receptors

sensitivity of the receptors

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30
Q

What are:

Spare receptors
Silent receptors

A

Ise, know it!!!!

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31
Q

A receptor may exist in two interchangeable states, ______ and ______ which are in equilibrium.

A

active (Ra) & inactive (Ri)

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32
Q

______- any molecule which attaches selectively to particular receptors.

A

Ligand

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33
Q

Affinity -The ______ of the (reversible or irreversible?) interaction between ______ and ______, as measured by the ______, is defined as the affinity of one for the other.

A

strength; reversible

a drug and its receptor

dissociation constant

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34
Q

Intrinsic activity – capacity to induce a ______ in the ______.

A

functional change

receptor

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35
Q

Specificity - A drug that interacts with a single type of receptor that is expressed on only a limited number of differentiated cells will exhibit (Low or high?) specificity.

A

High

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36
Q

Agonists are ___ that bind to physiological receptors and mimic the ________ of the endogenous signaling compounds

A

Drugs

regulatory effects

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37
Q

If the drug binds to the same recognition site as the endogenous agonist the drug is said to be a _______

A

primary agonist.

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38
Q

endogenous agonist’s attachment site is the ______ or ________ site on the receptor

A

primary or orthosteric

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39
Q

Allosteric agonists bind to a (same or different?) region on the receptor referred to as ________ site.

A

Different
An allosteric

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40
Q

Antagonists are Drugs that (aid or block?) or (increase or reduce?) the action of an agonist

A

Block
Reduce

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41
Q

Antagonism most commonly results from competition with an agonist for the same or overlapping site on the receptor (a ______ interaction)

A

syntopic

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42
Q

Physical antagonist binds to the drug and prevents ________ like _____ binds to ______ and prevents _______.

A

its absorption

charcoal; alkaloids

Their absorption

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43
Q

Chemical antagonist combines with a substance _____ally like _______ binds with the metals.

A

chemic

chelating agents

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44
Q

Physiological antagonist produces an action (similar or opposite?) to a substance but by binding to the (same or different?) receptors

e.g. adrenaline is a physiological antagonist of _____ because adrenaline causes broncho_____ by binding to ____ receptors, which is opposite to broncho________ caused by _____ through ____ receptors.

A

Opposite
Different

histamine

dilatation; β2
constriction; histamine ; H1

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45
Q

Partial agonists -Agents that are ________ regardless of the concentration employed.

A

only partly as effective as agonists

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46
Q

Inverse agonists -Many receptors exhibit some _______ in the absence of a _____; drugs that _____ such receptors in an ______ conformation are termed inverse agonists (produce effect opposite to that of agonist).

A

constitutive activity

regulatory ligand

stabilize

inactive

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47
Q

Efficacy of an agonist is A ________ an agonist can produce.

It can be measured with a _________ only.

A

maximal effect (Emax)

graded dose-response curve

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48
Q

Potency is The _______________

A

amount of the drug needed to produce a given effect.

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49
Q

potency is not determined by the affinity of the receptor for the drug.
T/F

A

F

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50
Q

The dose causing 50% potency from the maximal effect (ED50) can be obtained from ________.

A

graded dose-response curve

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51
Q

In ______________ curve, ED50, TD50 and LD50 are potency variables.

A

quantal dose response

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52
Q

Repeated administration of a drug results in diminished effect “ _______ ”.

A

Tolerance

53
Q

List the types of tolerance

A

Tachyphylaxis
Desensitization

54
Q

Tachyphylaxis: is a type of tolerance which ______

A

occurs very rapidly.

55
Q

Desensitization: ___eased response to the agonist after its _______ in (small or large?) doses.

A

Decr ; repeated injection; small

56
Q

Desensitization
May be due to
1- ______ or ______ of the receptors.
2- Loss of receptors (_____)- due to _____ or ______
3- Exhaustion of _________ (depletion of catecholamine).

A

Masking or internalization

down regulation

decreased synthesis or increased destruction.

mediators

57
Q

Answer with competitive or non competitive antagonist

Antagonist binds with the same receptor as agonist
Antagonist chemically resembles the agonist

A

Competitive
Competitive

58
Q

Effect of competitive antagonist on agonist Drug response curve?

A

Parallel rightward shift of agonist DRC

59
Q

Effect of non competitive antagonist on agonist Drug response curve?

A

Flattening of agonist DRC

60
Q

With non competitive antagonism, the antagonist appears to have inactivated a number of receptors
T/F

A

T

61
Q

In ______ antagonism, the intensity of response depends on the conc of both agonist and antagonist

A

Competitive

62
Q

In ______ antagonism, the intensity of response depends on the conc of only the antagonist

A

Non competitive

63
Q

Examples of competitive antagonism

Ach -
Morphin-

A

Atropine
Naloxone

64
Q

Examples of non competitive antagonist

Diazepam-

A

Bicuculline

65
Q

Drug synergism is When ______________________________ they are said to be synergistic.

A

the action of one drug is facilitated or increased by the other,

66
Q

In a synergistic pair, both the drugs can’t have action in the same direction
T/F

A

F
They can

67
Q

In a synergistic pair, given alone one may be ____ but still ______ the action of the other when given together.

A

inactive

enhance

68
Q

Additive

The effect of the two drugs is in (the same or different?) direction and simply adds up:

A

The same

69
Q

In an additive drug pair,

effect of drugs A + B = ______________

A

effect of drug A + effect of drug B

70
Q

In a Supraadditive (aka _____ ) drug pair, The effect of combination is (lesser or greater than or equal to?) the individual effects of the components

A

potentiation

Greater than

71
Q

In a supradditive drug pair,

effect of drug A+ B __ effect of drug A+ effect of drug B

A

>

72
Q

Physiological receptors

List 6

A

GPCR
Ion channels
Transmembrane enzymes
Transmembrane, non-enzymes
Nuclear receptors
Intracellular enzymes

73
Q

Physiological receptors have at least two major functions, ______ and ________

A

ligand binding and message propagation

74
Q

Two functional domains within the receptor:
-________ domain and
-________ domain.

A

ligand-binding

effector

75
Q

The regulatory actions of a receptor may be exerted directly on its ______, on ________, or may be conveyed by intermediary cellular signaling molecules called ______.

A

cellular target(s)

effector protein(s)

transducers

76
Q

In Ligand gated ion channels, there is little intervention of G-protein or second messenger.
T/F

A

F
None

77
Q

For ligand gated ion channels, Response is (slowest or fastest?) (in _______).

A

fastest

milliseconds

78
Q

GPCRs a family of ______ GTP-binding regulatory proteins termed _______

A

heterotrimeric; G proteins

79
Q

G proteins are _______ that convey the information that agonist is bound to the receptor from the ______ to one or more ________

A

signal transducers

receptor

effector proteins.

80
Q

The G protein heterotrimer is composed of a ____ nucleotide-binding ___ subunit, which confers specific recognition to _____ and _____, and an associated dimer of _____ and _____.

A

guanine

α

both receptors and effectors

β and ϒ subunits

81
Q

G–protein-regulated effectors include enzymes such as
-________,
-_______,
-___________ (PDE6),
-membrane ion channels selective for _______

A

adenylyl cyclase

phospholipase C

cyclic GMP phosphodiesterase

Ca2+ and K+.

82
Q

GPCRs span the plasma membrane as a bundle of __________.

A

seven alfa-helices

83
Q

GPCRs serve as (Intra or Extra?) cellular binding site for ligand and ______ binding site for transducer G-protein.

A

Extra

Cytosolic

84
Q

Active alpha-GTP returns to basal state by ____ proteins

A

RGS

85
Q

G-proteins :

The subunits fall into four families (_____,_____,____, and _____).

A

Gs, Gi, Gq, and G12/13

86
Q

The Gs α-subunit uniformly (activates or inhibits?) _________

the Gi α-subunit can (activate or inhibit?) certain isoforms of _____;

the Gq α-subunit (activates or inhibits?) all forms of ________

the G12/13 α-subunits couple to _________(GEFs), such as p115RhoGEF for the small GTP-binding proteins ___ and _____

A

Activates ; adenylyl cyclase

Inhibit; adenylyl cyclase

Activates; phospholipase C

guanine nucleotide exchange factors ; Rho and Rac.

87
Q

RESENSITIZATION AND DOWN-REGULATION OF RECEPTOR

1)
Agonist binding to receptors initiates signaling by promoting receptor interaction with G proteins (Gs) located in the cytoplasm.

Agonist-activated receptors are phosphorylated by a _________, preventing receptor interaction with ___ and promoting binding of a different protein, - ______, to the receptor.

A

G protein-coupled receptor kinase (GRK)

Gs

β arrestin (β-Arr)

88
Q

RESENSITIZATION AND DOWN-REGULATION OF RECEPTOR

2)

The receptor- β arrestin complex binds to ____, promoting ______

________________ reduces - β Arr binding affinity, allowing _______ of receptors by ______.

A

coated pits; receptor internalization.

Dissociation of agonist from internalized receptors

dephosphorylation; phosphatase

89
Q

RESENSITIZATION AND DOWN-REGULATION OF RECEPTOR

3)

Return of receptors to the ______ result in the efficient resensitization of cellular responsiveness.

Repeated or prolonged exposure of cells to _____ favors the delivery of internalized receptors to _____ , promoting receptor ______ rather than _______

A

plasma membrane

agonist

lysosomes

down-regulation

resensitization

90
Q

Enzyme linked receptors

Either
1) With ___________.

or

2)Without _________(but bind a ______ on activation

A

intrinsic enzymatic activity

intrinsic enzymatic activity ; JAK-STAT kinase

91
Q

JAKs- STATS PATHWAY

Binding of the cytokine causes _____ of the receptor and recruits the _____ to the cytoplasmic _____ of the receptor.

JAKs __________ and lead to the phosphorylation of the _______.

The phosphorylated STATS translocate to the _____ and __________

A

dimerization; Janus Kinases (JAKs); tails

trans-phosphorylate; signal transducers and activators of transcription (STATs)

nucleus; regulate transcription

92
Q

There are proteins termed __________ that inhibit the JAK-STAT pathway

A

suppressors of cytokine signaling (SOCS)

93
Q

Therapeutic index = —— Or ——-
——— ————
—— ——

A

TD50/ED50

LD50/ED50

94
Q

TD = ________
LD= ________

A

Toxic dose
Lethal dose

95
Q

The higher the therapeutic index, the more dangerous a drug is

T/F

A

F
The safer it is

96
Q

List 4 common drugs with very low TI

A

Theophylline
Digoxin
Warfarin
Lithium

97
Q

Response to steroid receptors

(Slower or faster?) in onset; (shorter or longer ?) in duration

A

Slower

Longer

98
Q

All beta receptors use ____ Gprotein

Who uses Gi

A

Gs

M2,A2,D2

99
Q

Most 1s and M3 use ____Gprotein

A

Gq

100
Q

_____ is a specific TK inhibitor
_______ is a non specific TK inhibitor

A

Imatinib
Sorafenib

101
Q

MLCK-

A

Myosin light chain kinase

102
Q

stimulation of the nicotinic
receptor by acetylcholine results in _______ and _________

A

sodium influx and potassium
outflux

103
Q

agonist stimulation of the
γ-aminobutyric acid (GABA) receptor increases ________
and hyperpolarization of neurons.

A

chloride influx

104
Q

Up-regulation of receptors can make the cells more resistant to the effect of
the antagonist.
T/F

A

T

105
Q

Which is more clinically useful

Efficacy or drug potency?

A

Efficacy is a more clinically useful characteristic than is drug potency,

106
Q

Full agonists have intrinsic activity of ____

Partial agonists have intrinsic activity of ____

inverse agonists have an intrinsic activity of ___

A

One

greater than zero but less
than one

less than zero

107
Q

RGS ?

A

Regulator of G-protein signaling

108
Q

Lorazepam works on _____ receptors to ____

A

GABA
Reduce seizures

109
Q

TYPES OF DRUG EFFECT
_____ Effect
_____ Effect
______ Effect

A

Desired

Side

Adverse

110
Q

Desired Effect
Refers to physiological changes that are _____ and _____

A

expected and desired

111
Q

Side Effect
Refers to physiological changes that are __________ but ______

A

expected but undesired

112
Q

Side effect Occurs at the normal therapeutic dose of the drug

T/F

A

T

113
Q

Desired effect Occurs at the normal therapeutic dose of the drug

T/F

A

T

114
Q

Side effect of aspirin is ??

A

Increased bleeding

115
Q

Adverse Effect

Refers to physiological changes that are _______ and _____

A

unexpected and undesired

116
Q

Adverse effects Occurs at a specific dose
T/F

A

F

At any dose

117
Q

Adverse effects can be life threatening

T/F

A

T

118
Q

About ____ to ____% of the sigmoid curve is a straight line for statistical analysis

A

20

80

119
Q

Potency = EC50

T/F

A

T

120
Q

Margin of safety is a term used in _______ curve

A

Dose response Quantal curve

121
Q

Margin of Safety (M.S)
Refers to the ratio of the _____ dose for __% of the population(___) divided by the effective dose for ___% of the population (____)

A

lethal

1; LD1

99; ED99

122
Q

MS= ___/___

A

LD1

ED99

123
Q

Examples of potentiation

Levodopa + ______
Amoxicillin + _______

A

Carbidopa

Clavulanic acid

124
Q

Example of synergism

Penicillin + _______
Prednisolone + _____

A

Aminoglycoside

NSAIDs

125
Q

Example of antagonism

Propranolol + ______
Pilocarpine + ______

A

Salbutamol

Atropine

126
Q

Combination of Deferoxamine and _____ metal is an example of a _____ antagonism

A

Iron

Chemical

127
Q

List the 3 competitive inhibition in the slide

A

Ace inhibitor- captopril
Reversibile AchE - neostigmine
Allopurinol- inhibits xanthine oxidase

128
Q

List the non competitive inhibition in the slide

A

Irreversible anti ACHE
Aspirin
Monoamine oxidase inhibitor
Proton pump inhibitor

House Pharmacology (50 decks)

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