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Pharmacology > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

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
Q

What is efficacy?

A

The maximal effect an agonist can produce

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26
Q

How is efficacy measured?

A

Graded Dose-response curve

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27
Q

What is potency?

A

The amount of drug needed to produce a given effect!

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28
Q

How is potency determined?

A

The affinity of the receptor for the drug

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29
Q

The measure of the potency of a substance in inhibiting a specific biological or biochemical function is known as?

A

Half maximal inhibitory concentration

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30
Q

The dose required for an individual to experience 50% of the maximum effect

A

EC50

31
Q

What is ED50

A

The dose for 50% of the population to obtain the therapeutic effect

32
Q

Repeated administration of a drug results in?

A

Diminished effect “Tolerance”

33
Q

A type of tolerance which occurs very rapidly is called?

A

Tachyphylaxis

34
Q

Decreased response to agonist after it’s repeated injections in small doses is called?

A

Desensitization

35
Q

Desensitization can occur due to

A

Internalization of receptors(endocytosis)
Loss of receptors (due to lack of synthesis or increased destruction)
Exhaustion of mediators(depletion of catecholamine)

36
Q

DRC of a competitive antagonist has a parallel right shift. T/F

A

True

37
Q

Is non-competitive antagonist surmountable?

A

No. It isn’t

38
Q

Competitive anatagonists inactivates a certain number of receptors. T/F

A

False! It’s the agonist molecules. This is for uncompetitive

39
Q

Intensity of responds depends on only antagonist in competitive antagonist interactions

A

False! It depends on both agonist and antagonist

40
Q

Examples of competitive antagonist interaction

A

Ach———Atropine
Morphine——-Naloxone

41
Q

Examples of non competitive

A

Diazepam——-Bicuculline

42
Q

When the action of one drug is facilitated or increased by another it is said to be?

A

Synergistic!

43
Q

In synergistic pair, only one drug can have action in a direction. T/F

A

False! Both of them can have

44
Q

In synergistic pair one may be inactive but still enhance the action of the other. T/F

A

True

45
Q

Physiological receptors include?

A

GPCR
Ion channels
Transmembrane enzymes
Transmembrane non-enzymes
Nuclear receptors
Intercellular enzymes

46
Q

What are the two major functions of physiological receptors?

A

Ligand binding
Message propagation(signaling)

47
Q

Functional domains within the receptor

A

Ligand binding
Effector

48
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, effector proteins, transducers

49
Q

What are the functional families of ion channels?

A

Ligand gated and voltage gated

50
Q

Physiological ligands of ligand-gated ion channels?

A

Ach, GABA, 5-HT

51
Q

Physiological ligands of voltage ion channels

A

None because they are activated by membrane depolarization

52
Q

Effectors and transducers of ligand gated and voltage gated channels?

A

Na, Ca, K, Cl for ligand gated and same for voltage gated with exception of chloride

53
Q

Examples of drugs that act on ligand gated channels?

A

Nicotine
Gabapentin

54
Q

Examples of drugs that act on voltage gated channels

A

Lidocaine
Verapamil

55
Q

What kind of receptors are the fastest

A

Receptors with intrinsic ion channels

56
Q

Examples of receptors with intrinsic ion channels

A

Ligand gated ion channels

57
Q

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

A

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

Q channels have properties similar to P channels. T/F

A

True

59
Q

The neuronal pharmacology of CNS is modulated by what channels?

A

N, P, Q, R

60
Q

What channel has weak effects on CNS functions?

A

L channel

61
Q

Functional families of GCPR includes?

A

Beta adrenergic receptors
Muscarinic receptors
Eicosanoid receptors

62
Q

What are the physiological ligands of Adrenergic receptors, muscarinic and eicosanoid receptors?

A

A-NE, Epi, DA
M-Ach
E-prostaglandins
Leukotrienes
Thromboxanes

63
Q

What are the effectors and transducers and examples of drugs for Adrenergic, muscarinic and eicosanoid receptors?

A

Adrenergic-Gs, AC… Eg is Dobutamine
Muscarinic-Gi, Gq, AC, ion channels, PLC. Eg Atropine
Eicosanoid-Gi, Gq, Gs.. Eg mistroprostol, montelukast

64
Q

GCPRs is a family of —— GTP binding regulatory proteins called ——

A

Heterotrimeric, G-proteins

65
Q

The G-protein heterotrimer is composed of a —— and an —-

A

Guanine nucleotide-binding alpha subunit , associated dimer beta and gamma subunits

66
Q

G-protein regulated effectors include enzymes such as?

A

Phospholipase C
Adenylyl Cyclase
cyclic GMP phosphodiesterase(PDE6)
Membrane ion channels selective for Ca and K

67
Q

GCPRs span the PM as a bundle of —- alpha helices

A

7

68
Q

GCPR is a cystolic binding site for —— and extracellular binding site for ——

A

G-proteins and ligands

69
Q

Function of Gi subunits?

A

Inhibit certain isoforms of adenylyl cyclase

70
Q

Gs alpha subunit function

A

Stimulate/activate adenylyl cyclase

71
Q

Gq subunit function

A

Activates all forms of phospholipase C

72
Q

What GPCR subunit is coupled to guanine nucleotide exchange factors(GEFs) such as p115RhoGEF for the small GTP-binding proteins Rho and Rac

A

G12/13

73
Q

Phosphorylation can cause?

A

SM relaxation
Heart contraction
Glycogenolysis
Lipolysis

Pharmacology (7 decks)

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