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CPR II Exam #1 > Intro to Pharmacodynamics > Flashcards

Intro to Pharmacodynamics Flashcards

1
Q

What is pharmacokinetics?

A

Effects of the body on drugs: absorption, distribution, metabolism, elimination.

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2
Q

What is pharmacodynamics?

A

Effects of drugs on body: drug receptors, dose response curves, mechanisms of drug actions.

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3
Q

Inert binding site

A

A component of the system that a drug binds and does not change the function.

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4
Q

Covalent bonds in drug interactions are:

A

They are irreversible.

Drug removal/receptor re-activation requires re-synthesis of the receptor or enzymatic removal of the drug.

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5
Q

Non-covalent bons in drug interactions are:

A

Reversible.

Most drugs bind to receptors this way.

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6
Q

Strongest to weakest non-covalent bonds (3)

A

Ionic bond > hydrogen bond > hydrophobic interactions

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7
Q

3 parameters describing the interaction of a drug w/ a receptor

A

Affinity
Selectivity
Intrinsic activity

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8
Q

Affinity

A

How readily and tightly the drug binds to its receptor.

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9
Q

What is Kd?

What is the unit for Kd?

What does a low/high Kd mean?

A

Equilibrium dissociation constant (describes affinity).
Drug conc. at which 50% of drug receptor binding sites are occupied w/ the drug.

Kd is expressed in molar conc. (micromoles, nanomoles, etc.).

Low -> higher affinity
High -> low affinity

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10
Q

How do you find Kd mathematically?

L + R -> LR

A

Kd = ([L][R])/[LR]

Reactants over products

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11
Q

How is selectivity measured?

A

By comparing affinities of a drug to different receptors.

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12
Q

What is a drug’s intrinsic activity?

A

The ability of a drug to change a receptor function and produce a physiological response upon binding to a receptor.

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13
Q

Do agonists have intrinsic activity?

A

Yes.

They bind to a receptor and stabilize it in a particular conformation and produce a response.

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14
Q

Do antagonists have intrinsic activity?

A

No.

They bind to the receptor but do NOT change its function. They prevent activation of the receptor in the presence of an agonist. There is no pharmacological effect in the absence of an agonist.

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15
Q

What are inverse agonists?

A

They produce an effect opposite to a full or partial agonist.

  • decrease receptor signaling
  • decrease response at receptors
  • intrinsic activity is present and related to the inhibition of receptor function
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16
Q

Competitive antagonists

A

Compete w/ endogenous chemicals or agonist drugs for binding the receptor.

Can be outcompeted.

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17
Q

Irreversible antagonists

A

Irreversibly bind to and occlude the agonist site by forming covalent bonds.

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18
Q

Allosteric antagonists

A

Bind to a site other than the agonist site to prevent or reduce agonist binding.

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19
Q

What happens to EC50 and Emax in competitive antagonism?

A

EC50 increases

Emax does not change

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20
Q

What happens to EC50 and Emax in noncompetitive antagonism?

A

EC50 does not change

Emax decreases

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21
Q

Nonreceptor antagonists include:

A

Chemical and physiologic antagonists

22
Q

Arithmetically, the dose-response curve is:

More commonly, the dose response curve is:

A

Hyperbolic curve

Sigmoidal curve (take the log)

23
Q

What is a graded response?

A

Answers “how much?”
Magnitude of a response varies continuously.
Usually represents the mean value within a pop. or a single subject.

24
Q

What is a quantal response?

A

All or none, yes or no, etc. Answers “does the response occur at all?”
Requires a pre-defined response (death, falling asleep, etc.)
Used to examine the freq. of a response within a large group.

25
Q

Quantal dose-response curve

A

Relates dose of a drug to the freq. of a response.

Bell-curve looking.

26
Q

Non-cumulative quantal dose response curve

A

Number or percent of individuals responding at a dose of a drug and only at that dose.

27
Q

Cumulative quantal dose response curve

A

Numer or percent of individuals responding at a dose of a drug and at all doses lower than that dose.

28
Q

ED50

TD50

LD50

A

Median effective dose

Median toxic dose

Median lethal dose

29
Q

Therapeautic index =

A

TD50/ED50

The higher the TI the safer the drug

30
Q

Drugs with what kind of affinity tend to be more potent?

What is it represented by?

What does a low ED50 mean?

What does it determine?

A

High affinity (low Kd)

ED50

The more potent the drug

Determines the drug dose that will be used clinically

31
Q

What is potency?

A

The amt. of a drug required to produce a specific pharmacological effect.

32
Q

What is efficacy?

A

The maximal pharmacological effect that a drug can produce.

33
Q

What represents efficacy?

What is efficacy related to?

What does it determine?

A

Emax (the greater the Emax, the more efficacious the drug.

Related to the amt. of receptors available.

Determines the magnitude of clinical effect.

34
Q

5 major classes of drug targets

A 
Membrane receptors
Nuclear receptors
Ion channels
Transport proteins
Enzymes
35
Q

How do protein kinases work?

Examples (2)

A

Modify protein by covalently attaching PO4- to an AA residue.

Ser-Thr kinases, Tyr kinases

36
Q

Gs second messenger and effect

A

Adenylyl cyclases -> AC activation

37
Q

Gi second messenger and effect

A

Adenylyl cyclases -> AC inhibition

38
Q

Gq second messenger and effect

A

Phospholipase C -> PLC activation

39
Q

G12/13 second messenger and effect

A

Rho GTPases -> cytoskeletal rearrangements

40
Q

Gs effects:

A

Activates all isoforms of AC and Src try kinase

41
Q

Gi effects:

A

Inhibits AC 13, 5, 6.

Activates Src tyr kinase.

42
Q

Gq effects:

A

Activates phospholipase C-beta

43
Q

G12/13 effects:

A

Rho GTPases

44
Q

GRK and beta-arr

A

GRK improves beta-arr binding and stops the signaling cascade

45
Q

Receptors w/ intrinsic tyrosine kinase activity (RTKs) (6)

A 
IGF-1
Insulin
VEGF - vascular endothelial
EGF - epidermal
NGF - nerve
PDGF - platelet-derived
46
Q

What are JAKs?

What are 5 examples of hormones/cytokines that effect it?

A

A family of cytosolic tyr kinases.

GH (somatotropin)
Erythropoietin
Leptin
Interferons
ILs 2-10, 15
47
Q

When do nuclear receptors produce their effects?

What is unique about them?

A

After a lag period.

The effects can persist after the agonist conc. has been reduced to 0.

48
Q

What is the MOA of a glucocorticoid?

A

Hsp 90 binds the 3 domained receptor in the absence of the hormone and blocks folding into active conformation. When the hormone binds, hsp90 dissociates and permits conversion to the active configuration.

49
Q

Full agonists (3)

A

Fully activate R
Produce max. effect when all Rs occupied
Max. intrinsic activity

50
Q

Partial agonists (3)

A

Partially activate the R upon binding
Produce sub-max effect when all Rs are occupied
Intrinsic activity varies depending on drug, but always sub-max.

CPR II Exam #1 (30 decks)

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