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Pharmacology > Unit 1- Pharmacodynamics > Flashcards

Unit 1- Pharmacodynamics Flashcards

1
Q

Pharmacodynamics

A

Relationship between drug concentration and intensity of action at the receptor level

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2
Q

Types of Drug Targets

A

Enzyme, carrier, ion channel, receptor

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3
Q

Receptor Usage

A

When the interaction triggers a cascade of events for signal transmission

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4
Q

Binding Site

A

Drug molecule must bind with target and result in a response

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5
Q

Drug

A

Molecule that interacts with molecular components of an organism to produce biochemical and physiological changes, exogenous ligands

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6
Q

Enzymes

A

Enzymes as targets are inhibited

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7
Q

Cyclooxygenase Enzymes

A

Targeted by NSAIDs to suppress proinflammatory prostaglandins

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8
Q

Acetylcholinesterase Enzyme

A

Cholinesterase inhibitors prevent metabolism of acetylcholine

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9
Q

Antibiotics

A

May inhibit enzymes in cell wall biosynthesis, nucleic acid metabolism and repair, or protein synthesis

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10
Q

Carriers

A

Membrane transport proteins targeted by drugs

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11
Q

Na+/K+/2Cl- Carrier

A

Targeted by diuretics in the nephron

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12
Q

Sodium Pump Carriers

A

Targeted by digitalis

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13
Q

K+/H+ Carrier

A

Targeted by proton pump inhibitors in the gastric parietal cells

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14
Q

Ion Channels

A

Voltage gated calcium channels targeted by calcium channel blockers

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15
Q

Receptors

A

Regulatory proteins that play a roll in cell communication

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16
Q

GPCRs

A

Largest family of receptors involved in almost all physiological processes, most drugs act on GPCRs

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17
Q

Beta 2 Adrenergic Receptor

A

Albuterol binding activates adenylate cyclase forming cAMP and causing smooth muscle cell relaxation in the airways

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18
Q

Ligands

A

The exogenous compounds that bind receptors

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19
Q

Endogenous Ligands

A

Endogenous transmitters

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20
Q

Occupancy Theory

A

Drug response is a linear function of drug occupancy at the receptor level, drug has to occupy all receptors to achieve a maximal effect

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21
Q

Unliganded Receptor in Occupancy Theory

A

Is silent with no basal activity

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22
Q

Concept of Efficacy

A

The more receptors occupied by a drug the greater the response

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23
Q

Antagonist in Occupancy Theory

A

A drug with null efficacy but that blocks access of the receptor to other ligands

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24
Q

Two-State Model

A

Receptor exists in active and inactive form in dynamic equilibrium, ligand binding can shift equilibrium

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25
Q

Agonist in Two-State Model

A

A drug with a higher affinity for the active state will drive equilibrium to active and activate the receptor

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26
Q

Full Agonist in Two-State Model

A

A drug that highly favors the active state and drives the receptor all the way to active to get a maximal response

27
Q

Partial Agonist in Two-State Model

A

A drug only has moderately higher affinity for the active state and has lower effect than a full agonist

28
Q

Inverse Agonist in Two-State Model

A

A drug has higher affinity for the inactive state and drives equilibrium to inactive

29
Q

Neutral Agonist in Two-State Model

A

Antagonist, binds the active and inactive states in equal affinity and will not alter equilibrium, but acts as a competitive antagonist

30
Q

Antagonist vs Neutral Agonist

A

Antagonist has no intrinsic activity, a neutral agonist binds equally to both states of receptors

31
Q

Primary Agonist

A

Binds to the same site as endogenous ligands

32
Q

Allosteric Agonist

A

Drug that binds to a different region of the receptor than endogenous ligands

33
Q

Receptor Antagonists

A

Prevent the action of natural agonists

34
Q

Drug Affinity

A

The ability of a drug to bind to a receptor

35
Q

Constant of Affinity

A

Numerical representation of drug affinity

36
Q

Drug Receptor Complexes

A

Binding of drugs to receptors that is responsible for drug action

37
Q

Drug Efficacy

A

Drug ability to initiate changes that lead to the production of responses

38
Q

Level of Maximal Response

A

Highest response an agonist can achieve, characterized by efficacy

39
Q

Drug Potency

A

Concentration of a drug required to achieve a given effect, expressed by EC50

40
Q

EC50

A

Concentration of agonist that produces 50% of its maximal response

41
Q

Potency and EC50

A

Potency varies inversely with EC50, higher potency requires lower EC50

42
Q

Requiring Potent Drugs

A

Spot on treatments, eyedrops, and intra-articular administration

43
Q

Potency of Antagonist

A

Effect of inhibition, determined by IC50

44
Q

IC50

A

Concentration of antagonist that reduces agonist response by 50%

45
Q

Competitive Antagonism

A

Antagonists act on the same receptor as the agonist

46
Q

Reversible Competitive Antagonism

A

Antagonism can be reversed when agonist concentration is increased

47
Q

Irreversible Competitive Antagonism

A

Displacement of antagonist from its binding site cannot be achieved by increasing agonist concentration

48
Q

How to investigate receptor function?

A

Use irreversible competitive antagonists as experimental probes

49
Q

Dose Response Curve and Competitive Antagonism

A

Agonist curve is shifted to the right: potency decreases because it depends on dosage but efficacy remains the same

50
Q

Noncompetitive Antagonism

A

The drug blocks the agonist response at a downstream point in the cascade of events

51
Q

Dose Response Curve and Noncompetitive Antagonism

A

Maximal efficacy of the agonist is reduced

52
Q

Drug Specificity

A

Most drugs can be agonist or antagonist and do not have specificity to one type of receptor

53
Q

Submaximal Drug Response

A

Increase dose of the drug to increase therapeutic effect

54
Q

Clinical Efficacy

A

Therapeutic effectiveness of a drug in patients

55
Q

Intrinsic Efficacy

A

Capacity of agonists to activate a receptor

56
Q

Antagonist Efficacy

A

No intrinsic efficacy (no receptor activation) but clinical efficacy (therapeutic effect)

57
Q

Quantal Dose Response Relationships

A

Relationship between dose of a drug and proportion of a population of patients that respond to it, used to determine the dose at which most of the population responds

58
Q

ED50

A

Median effective dose, dose at which 50% of subjects exhibit a therapeutic response to a drug

59
Q

TD50

A

Median toxic dose, dose at which 50% of subjects experience a toxic effect

60
Q

LD50

A

Median lethal dose, dose at which 50% of subjects die

61
Q

Therapeutic Index

A

Ratio of TD50 to ED50, used as a measure of drug safety

62
Q

Certain Safety Factor

A

CSF should be >1, a dose effective in 99% of the population is less than what would be lethal in 1% of the population

63
Q

Therapeutic Window

A

Range of drug doses that provides therapeutic efficacy with minimal toxicity, range between ED50 and the start of the toxicity curve

Pharmacology (32 decks)

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