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II. Pharmacology > Drug Receptors and Pharmacodynamics (M1) > Flashcards

Drug Receptors and Pharmacodynamics (M1) Flashcards

1
Q

As the dose of a drug increases, what does the response increment do?

A

diminishes

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2
Q

What is the concentration-effect curve equation?

A

E = (Emax*C)/(C+EC50) where EC50 is concentration of drug that produces 50% of maximal effect

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3
Q

What is the ability of a drug to initiate a cellular effect?

A

efficacy (or intrinsic activity)

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4
Q

What are drugs that have both receptor affinity and efficacy?

A

agonist

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5
Q

What are drugs that bind to receptors (affinity) but do not activate them?

A

antagonist

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6
Q

What is the affect of an irreversible antagonist (noncompetitive)? 1. What kind of bonds do they generally form? 2

A
  1. reduces maximal effect the agonist can achieve and may not affect EC50
  2. covalent bonds
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7
Q

What bind to separate sites on the receptor protein and alter receptor function without blocking the receptor?

A

allosteric modulators

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8
Q

What are the enzyme effector systems with transduction though G-proteins?

A
  1. adenylyl (adenylate) cyclase
  2. guanylyl cyclase
  3. phospholipase C
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9
Q

What are the second messengers for transduction though G-proteins?

A
  1. cAMP
  2. cGMP
  3. IP3
  4. DAG
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10
Q

What are the protein kinases for transduction though G-proteins?

A
  1. cAMP-
  2. cGMP-
  3. calmodulin-dependent protein kinase C
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11
Q

What is the result of antagonists upregulating the number of receptors?

A

supersensitivity

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12
Q

What are examples of ion-channel- coupled ligand receptors?

A
  1. serotonin
  2. GABA
  3. glutamate
  4. acetylcholine
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13
Q

What mediate the signaling in enzyme-coupled receptors?

A
  1. EGF
  2. PDGF
  3. ANP
  4. TGF-Beta
  5. other tropic hormones
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14
Q

What make up the polypeptides in enzyme-coupled receptors?

A
  1. extracellular hormone-binding domain
  2. cytoplasmic enzyme domain
  3. hydrophobic connecting segment
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15
Q

What happens, upon the binding of the ligand to the extracellular domain in enzyme-coupled receptors?

A

receptor molecules bind together (dimerization) and become active and phosphorylate each other

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16
Q

What are tyrosine kinase inhibitors useful for?

A

neoplastic disorders

17
Q

For graded dose-response relationships, what is on the x-axis? 1. y-axis? 2

A
  1. log dose of drug

2. percentage of the maximal response

18
Q

What does the potency depend on?

A
  1. affinity

2. efficiency drug-receptor interaction coupled response

19
Q

What is the effect of competitive antagonists on the dose-response curve?

A
  1. shift curve to right

2. does not reduce maximal response

20
Q

What is the effect of non-competitive antagonists on the dose-response curve?

A
  1. shift curve to right
  2. reduces response (maximal response)
  3. cannot be overcome with more agonist
21
Q

In what is the response elicited with each dose of drug described in terms of the cumulative percentage of subjects exhibiting a defined all-or-none effect, plotted against the log dose of the drug?

A

Quantal Dose-Effect Curves

22
Q

What is the ED50? 1. The TD50? 2. The LD50? 3

A
  1. median effective dose, 50% of subjects get observed effect
  2. median toxic dose, 50% of animals get particular toxic effect
  3. median lethal dose, 50% of animals die
23
Q

What is the ratio of the median lethal dose (LD50) and the ED50?

A

TI

24
Q

What is the ratio between the dose that is lethal in 1% of the subjects (LD1) and the dose that produces a therapeutic effect in 99% of subjects (ED99)?

A

CSF

25
Q

What is a drug response that is infrequently observed in most patients due to differences in metabolism or allergies?

A

Idiosyncratic drug response

26
Q

What is it called when the effect of a given dose diminished?

A

Hyporeaction

27
Q

What is it called when the effect of a given dose increased compared with the effect seen in most individuals?

A

hyperreactive

28
Q

What is it called when drug responsiveness decreases with continued drug administration?

A

tolerance

29
Q

What is it called when drug responsiveness diminishes rapidly?

A

tachyphylaxis

30
Q

What is a description of molecular events initiated with the ligand binding and ending with a physiologic effect called?

A

signal transduction pathway

31
Q

What do G-protein-coupled receptors that activate an inhibitory Galpha subunit alter activity of adenylyl cyclase to?

A

decrease production of cAMP

32
Q

What determines the drug potency on a log dose-response plot?

A

position of the curve along the log-dose axis

II. Pharmacology (43 decks)

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