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Pharmacodynamics Flashcards

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1
Q

Pharmacodynamics is the study of — and —- effects of drugs and it’s — of —-

A

Biochemical, physiological, mechanism of action

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2
Q

Simplified, pharmacodynamics refers to ——

A

Effects of a drug on the body

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3
Q

A receptor exists in two in uninterchangeable state. T/F

A

False. Interchangeable

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4
Q

What are the two states of the receptor

A

Active and inactive(Ra and Ri)

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5
Q

Binding of a drug to a receptor shifts the equilibrium in one direction alone

A

False. It’s in either direction depending on where it binds

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6
Q

Intrinsic activity is the capacity to ——-

A

Induce a functional change in the receptor

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7
Q

Affinity is the strength of irreversible interaction between a drug and its receptor

A

False. Reversible

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8
Q

Affinity is measured by?

A

Dissociation constant

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9
Q

A drug that interacts with only a single type of receptor that is expressed on only a limited number of differentiated cells will exhibit———

A

High specificity

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10
Q

What is an agonist?

A

It is a drug/substance that binds to a receptor inside a cell or on the surface of a cell and causes the same action as the substance that normally binds to the receptor

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11
Q

Drugs that bind to physiological receptors and mimic regulatory effects of the endogenous signaling compounds are termed?

A

Agonist

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12
Q

If the drug binds to the same recognition site as the endogenous agonist it is said to be?

A

A Primary agonist

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13
Q

Allosteric agonists bind to a different region. T/F and it’s referred to as?

A

True. Allosteric site

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14
Q

What is the binding site for the natural(endogenous) agonist called?

A

Primary or orthosteric site

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15
Q

Drugs that block or reduce the action of an agonist are termed?

A

Antagonist

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16
Q

Antagonism most commonly results from competition with an agonist or overlapping site on the receptor. T/F

A

True

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17
Q

Physical anatagonist binds to the drug and prevents it’s ——— like———

A

Absorption like charcoal binds to alkaloid and prevents their absorption

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18
Q

Chemical antagonist combines with a substance chemically like——

A

Chelating agents bind with the metals

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19
Q

A physiological antagonist binds to a different receptor molecule producing an effect ——- to that produced by the drug it ——-

A

Opposite, Antagonizes

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20
Q

Adrenaline causes ——— by binding to ———

A

Bronchodilation, B2 receptors

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21
Q

Histamine causes —— through——- receptors

A

Bronchoconstriction, H1

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22
Q

Agents that are only partly as effective as agonists regardless of concern employed are called?

A

Partial agonist

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23
Q

A ligand that binds to a receptor and produces the opposite pharmacological effect that would be produced by an agonist is called?

A

Inverse agonist

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24
Q

Inverse agonist produce effects opposite that of the agonist. T/F

A

True

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25
What is efficacy?
The maximal effect an agonist can produce
26
How is efficacy measured?
Graded Dose-response curve
27
What is potency?
The amount of drug needed to produce a given effect!
28
How is potency determined?
The affinity of the receptor for the drug
29
The measure of the potency of a substance in inhibiting a specific biological or biochemical function is known as?
Half maximal inhibitory concentration
30
The dose required for an individual to experience 50% of the maximum effect
EC50
31
What is ED50
The dose for 50% of the population to obtain the therapeutic effect
32
Repeated administration of a drug results in?
Diminished effect “Tolerance”
33
A type of tolerance which occurs very rapidly is called?
Tachyphylaxis
34
Decreased response to agonist after it’s repeated injections in small doses is called?
Desensitization
35
Desensitization can occur due to
Internalization of receptors(endocytosis) Loss of receptors (due to lack of synthesis or increased destruction) Exhaustion of mediators(depletion of catecholamine)
36
DRC of a competitive antagonist has a parallel right shift. T/F
True
37
Is non-competitive antagonist surmountable?
No. It isn’t
38
Competitive anatagonists inactivates a certain number of receptors. T/F
False! It’s the agonist molecules. This is for uncompetitive
39
Intensity of responds depends on only antagonist in competitive antagonist interactions
False! It depends on both agonist and antagonist
40
Examples of competitive antagonist interaction
Ach———Atropine Morphine——-Naloxone
41
Examples of non competitive
Diazepam——-Bicuculline
42
When the action of one drug is facilitated or increased by another it is said to be?
Synergistic!
43
In synergistic pair, only one drug can have action in a direction. T/F
False! Both of them can have
44
In synergistic pair one may be inactive but still enhance the action of the other. T/F
True
45
Physiological receptors include?
GPCR Ion channels Transmembrane enzymes Transmembrane non-enzymes Nuclear receptors Intercellular enzymes
46
What are the two major functions of physiological receptors?
Ligand binding Message propagation(signaling)
47
Functional domains within the receptor
Ligand binding Effector
48
The regulatory actions of a receptor may be exerted directly on its ——, on —— or may be conveyed by intermediary cellular signaling molecules called ——
Cellular target, effector proteins, transducers
49
What are the functional families of ion channels?
Ligand gated and voltage gated
50
Physiological ligands of ligand-gated ion channels?
Ach, GABA, 5-HT
51
Physiological ligands of voltage ion channels
None because they are activated by membrane depolarization
52
Effectors and transducers of ligand gated and voltage gated channels?
Na, Ca, K, Cl for ligand gated and same for voltage gated with exception of chloride
53
Examples of drugs that act on ligand gated channels?
Nicotine Gabapentin
54
Examples of drugs that act on voltage gated channels
Lidocaine Verapamil
55
What kind of receptors are the fastest
Receptors with intrinsic ion channels
56
Examples of receptors with intrinsic ion channels
Ligand gated ion channels
57
Classify these voltage sensitive calcium channels according in relation to these properties. L, T, N, PQR 1)Activation threshold 2)inactivation rate 3)location 4)Function 5)Blockers
Blockers L-Verapamil and dihydropyridine group of CCBs and Cd2+ T-Ethosuxinide Flunarizine Ni+ N-Cd+ Gabapentin PQR Toxin from funnel web spider
58
Q channels have properties similar to P channels. T/F
True
59
The neuronal pharmacology of CNS is modulated by what channels?
N, P, Q, R
60
What channel has weak effects on CNS functions?
L channel
61
Functional families of GCPR includes?
Beta adrenergic receptors Muscarinic receptors Eicosanoid receptors
62
What are the physiological ligands of Adrenergic receptors, muscarinic and eicosanoid receptors?
A-NE, Epi, DA M-Ach E-prostaglandins Leukotrienes Thromboxanes
63
What are the effectors and transducers and examples of drugs for Adrenergic, muscarinic and eicosanoid receptors?
Adrenergic-Gs, AC… Eg is Dobutamine Muscarinic-Gi, Gq, AC, ion channels, PLC. Eg Atropine Eicosanoid-Gi, Gq, Gs.. Eg mistroprostol, montelukast
64
GCPRs is a family of —— GTP binding regulatory proteins called ——
Heterotrimeric, G-proteins
65
The G-protein heterotrimer is composed of a —— and an —-
Guanine nucleotide-binding alpha subunit , associated dimer beta and gamma subunits
66
G-protein regulated effectors include enzymes such as?
Phospholipase C Adenylyl Cyclase cyclic GMP phosphodiesterase(PDE6) Membrane ion channels selective for Ca and K
67
GCPRs span the PM as a bundle of —- alpha helices
7
68
GCPR is a cystolic binding site for —— and extracellular binding site for ——
G-proteins and ligands
69
Function of Gi subunits?
Inhibit certain isoforms of adenylyl cyclase
70
Gs alpha subunit function
Stimulate/activate adenylyl cyclase
71
Gq subunit function
Activates all forms of phospholipase C
72
What GPCR subunit is coupled to guanine nucleotide exchange factors(GEFs) such as p115RhoGEF for the small GTP-binding proteins Rho and Rac
G12/13
73
Phosphorylation can cause?
SM relaxation Heart contraction Glycogenolysis Lipolysis

Pharmacology (7 decks)

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