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SBL Week 1 > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

What is pharmocodynamics?

A

The effects of the drug on the body

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2
Q

When you plot drug dose arithmetically on the x-axis vs drug effect on the y-axis you typically get what type of curve?

A

Hyperbolic curve

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3
Q

When you graph the logarithm of the drug dose vs the response what what type of curve do you get?

A

Sigmoidal curve

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4
Q

What is the Emax of a drug?

A

The maximal effect that can be produced by the drug

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5
Q

What is the ED50 of a drug?

A

The effective dose 50 is the dose of drug that produces 50% of its maximal effect

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6
Q

Which Dose-Response Curve deals with the magnitude of a response varying continuously?

A

Graded Dose-Response curve

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7
Q

What does the Graded Dose-Response curve typically represent?

A

The mean value within a population or a single subject

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8
Q

Which Dose-Response Curve answers whether the response occurs or does not occur along with how many responses there are?

A

Quantal Dose-Response curve

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9
Q

What is the Quantal Dose-Response curve used for?

A

Relates dose of a drug to the frequency of a response within a population

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10
Q

What is a non-cumulative quantal dose response curve?

A

The number or % of individuals responding at a dose of a drug and only at that dose

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11
Q

What is a cumulative quantal dose response curve?

A

Number or % of individuals responding at a dose of a drug and at all doses lower than that dose

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12
Q

What shape does a quantal dose-response curve create?

A

Sigmoidal

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13
Q

What is TD50?

A

The median toxic dose

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14
Q

How do you calculate the Therapeutic Index?

What does it mean if the number is high?

A

1) TD50 / ED50

2) The higher the TI the safer the drug

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15
Q

In regards to a therapeutic window which drugs are considered more dangerous?

A

More narrow therapeutic window

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16
Q

What is drug potency?

A

The amount of drug required to produce a specific pharmacological effect

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17
Q

What is drug potency represented by?

What describes a more potent drug?

A

1) ED50

2) Lower ED50

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18
Q

What is drug efficacy?

A

The maximal pharmacological effect that a drug can produce

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19
Q

What is drug efficacy represented by?

What describes a more efficacious drug?

A

1) Emax

2) Greater Emax

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20
Q

Between drug potency vs drug efficacy which is related to the total number of receptors available to bind a drug?

A

Drug Efficacy

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21
Q

Which bonds are irreversible?

A

Covalent bonds

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22
Q

What is required for drug removal/receptor re-activation for covalent bonds?

A

Re-synthesis of the receptor or enzymatic removal of the drug

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23
Q

Most drugs bind to receptors via what bonds?

A

Non-covalent bonds

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24
Q

The affinity of a drug for a receptor describes?

A

How readily and tightly that drug binds to its receptor

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25
Q

How much drug is needed to produce a response when it has a high affinity for its receptor?

A

Less drug

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26
Q

What is the Kd (equilibrium dissociation constant)?

A

The drug concentration at which 50% of the drug receptor binding sites are occupied by the drug

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27
Q

A drug with a higher affinity for a receptor will have what Kd?

A

Lower

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28
Q

What is drug selectivity?

A

A property of a drug determined by its affinities at various binding sites

29
Q

What is the Kd ratio?

A

Kd ratio = Kd, off-target / Kd, target

30
Q

How do more selective drugs compare to less selective drugs?

A

1) Higher Kd ratio

2) Fewer adverse effects

31
Q

Intrinsic activity describes what ability of a drug?

A

To change a receptors function and produce a physiological response upon binding to a receptor

32
Q

Between agonists and antagonists which does not have intrinsic activity?

A

Antagonists

33
Q

What effect does a full agonist have?

A

Produces a max pharmacological effect when all receptors are occupied

34
Q

What effect does an inverse agonist have?

A

Produces an effect opposite to a full or partial agonist by decreasing receptor signaling

35
Q

Partial agonists and full agonists at the same receptor will differ in what way?

A

The Emax of the partial will be lower

36
Q

What is pharmacologic antagonism?

A

Action at the same receptor as endogenous ligands or agonist drugs

37
Q

What is chemical antagonism?

A

When chemical antagonist makes the other drug unavailable

38
Q

What is physiological antagonism?

A

Occurs between endogenous pathways regulated by different receptors

39
Q

What do competitive antagonists compete with?

A

Endogenous chemicals or agonist drugs for the same receptor

40
Q

Which non-competitive antagonist binds to and occludes the agonist site on the receptor by forming covalent bonds?

A

Irreversible antagonists

41
Q

Which non-competitive antagonist binds to a site other than the agonist site to prevent or reduce agonist binding of the receptor?

A

Allosteric antagonists

42
Q

Which pharmacologic antagonist can be displaced from the receptor by other drugs (effects are surmountable)?

A

Competitive antagonists

43
Q

What effect does a competitive antagonist have on a dose-response curve?

A

Agonist EC50 increases and the Emax does not change

44
Q

What effect does a noncompetitive antagonist have on a dose-response curve?

A

Agonist Emax decreases and the EC50 does not change

45
Q

When an agonist activates a GPCR this promotes Gα protein to release?

This allows the entry of what?

A

1) GDP

2) GTP

46
Q

In what state does the G protein regulate the activity of an effector enzyme or ion channel?

How is the signal terminated?

A

1) In the GTP-bound state (Gα-GTP)

2) Hydrolysis of GTP by α subunit

47
Q

What is the target and action of Gs proteins?

A

1) Adenylyl cyclase

2) Activation

48
Q

What is the target and action of Gi proteins?

A

1) Adenylyl cyclase

2) Inhibition

49
Q

What is the target and action of Gq proteins?

A

1) PLC

2) Activation

50
Q

What is the target and action of G12/13 proteins?

A

1) Rho GTPases

2) Cytoskeletal rearrangements

51
Q

The repeated or prolonged exposure of cells to agonists favors the delivery of internalized receptors to?

This promotes?

A

1) Lysosomes

2) Receptor down-regulation rather than resensitization

52
Q

What is the role of phosphodiesterase?

A

It degrades cAMP

53
Q

When JAKs are activated what do they do?

A

Phosphorylate STAT molecules so that STAT dimers travel to nucleus and regulate transcription

54
Q

What effect does EGF molecules have upon binding to receptor tyrosine kinases (RTKs)?

A

Activates it

55
Q

How does the RAS GTPase become activated?

A

1) Adaptor protein binds to phosphorylated tyrosine in cytoplasmic side of RTK
2) Ras activating protein binds to adaptor protein to activate Ras GTPase

56
Q

What mutation is found in 90% of pancreatic adenocarcinomas?

What mutation is found in 70% of melanomas?

A

1) Point mutation in Ras

2) Point mutation in Raf

57
Q

What type of drugs inhibit upregulated GF signaling?

Examples?

A

1) Targeted anticancer drugs

2) Monoclonal Abs to GF receptors and multikinase inhibitors

58
Q

What are ligand-activated transcription factors that modulate gene expression?

The ligands are what type of molecules?

A

1) Nuclear receptors

2) Lipophilic

59
Q

During glucocorticoid action, what protein binds to the receptor in the absence of the hormone and presents folding into the active conformation of the receptor?

A

hsp90

60
Q

What ion channel is a target of verapamil?

A

L-Type Calcium channel

61
Q

What does verapamil act on in a patient with atrial and supraventricular arrhythmias?

What effect does it have?

A

1) SA node and AV node

2) Decreases HR in SA node and decreases AV conductivity

62
Q

What does verapamil act on in a patient with Angina pectoris?

What effect does it have?

A

1) Cardiomyocyte

2) Decreased contractility and O2 demand

63
Q

What does verapamil act on in a patient with Hypertension?

What effect does it have?

A

1) Vascular smooth muscle

2) Relaxation

64
Q

The receptors for growth factors are often?

A

Receptor tyrosine kinases

65
Q

Inhibition of phosphodiesterase would have what effect on protein kinase A?

A

Increase its activity

66
Q

When do nuclear receptor ligands produce their effects?

A

After a lag period of several hours or days

67
Q

What is activated as a result of binding of interferon, interleukins, leptins, and erythropoietin to a cognate receptor?

A

Cytosolic protein kinases

68
Q

What reduces the level of PIP2?

A

Gαq

SBL Week 1 (7 decks)

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