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Pharmacology > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

What is pharmacodynamics?

A

biochemical and physiological effect of drugs and their mechanism

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2
Q

What is the mechanism of action?

A

initial interactions between drug and cellular macromolecules

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3
Q

Most drug receptors have what type of ligand?

A

endogenous

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4
Q

What are the non-receptor mediated drug actions?

A
  • gastric antacid
  • mannitol (osmotic diuretic)
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5
Q

Most drugs have what types of reversible forces?

A
  • ionic
  • hydrogen
  • hydrophobic
  • van der waals
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6
Q

What is the 2 state model?

A
  • agonists bind and stabilizes in the active configuration
  • population shifts to the right when agonists are present
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7
Q

When does basal activity occur?

A

when more receptors are active

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8
Q

An inverse agonist favors which side?

A

left side

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9
Q

What are the mechanisms needed for signal transduction?

A
  • ion channels
  • receptor coupled G-proteins
  • receptors with intrinsic enzyme activity
  • receptors that are internalized to deliver receptor complexes to intracellular targets
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10
Q

What are the characteristics of nicotinic Ach receptors?

A
  • made of 5 subunits
  • every subunit goes through the membrane 4 times
  • subunits are higly homologous
  • binding of receptor allow Na+ and K+ to flow across membrane
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11
Q

What type of receptor is a partial agonist?

A

GABA

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12
Q

Binding to a GABA receptor results in what?

A

pore opening and allowing Cl- ions across the membrane to cause hyperpolarization

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13
Q

What are the drugs that modulate GABA receptors?

A

barbituates and benzodiazepine

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14
Q

Glycine and glutamate are what type of ligand channels?

A

glycine: inhibitory
glutamate: excitatory

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15
Q

A transient change in the voltage across membrane can trigger what?

A

opening of gate allowing Na+ ions across membrane

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16
Q

Where do local anesthetics bind?

A

to the intracellular domain of voltage-gated Na channel

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17
Q

What is the purpose of receptor coupled G-proteins?

A

regulate generation of intracellular second messengers

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18
Q

What are the 3 types of G-proteins?

A

alpha, gamma, beta

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19
Q

What are the enzymes coupled to G-proteins?

A
  • adenylyl
  • cyclase
  • phospholipase C
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20
Q

What are the channels coupled to G-proteins?

A

Ca++ and K+

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21
Q

What 2 things can regulate the activity of other enzymes?

A

cAMP and Ca++

22
Q

What is a ligand regulated transmembrane enzyme?

A

tyrosine kinase receptor

23
Q

What is an intracellular receptor and where does it bind?

A

steroids; bind inside the membrane

24
Q

When a durg is more potent, where is it located on the graph?

A

furthest to the left

25
Q

Partial agonists have a lower what compared to fulla agonists?

A

lower efficacy

26
Q

What is the EC50?

A
  • the conc. that produces 1/2 the max effect
  • measures potency
27
Q

If the drug needs less conc. for same EC50 then?

A

increase potency

28
Q

What is an agonist?

A

drug or ligand that binds to the same site as endogenous ligand and produces a signal

29
Q

What does a full agonist have affinity for?

A

ONLY for active state

30
Q

What does a partial agonist have affinity for?

A

higher affinity only for active than inactive state

31
Q

What is efficacy/intrinsic activity?

A

properties of durgs that bind to the same receptor site but DO NOT produce equal maximum effects

32
Q

What is the most efficacious agonist?

A

drug that produces greatest maximum effect

33
Q

What is an antagonist?

A

drug that binds to the site used by endogenous ligand and blocks the signal produced by the endogenous ligand

34
Q

What is the difference between agonists and antagonists when it comes to the binding states?

A

agonists change the equil. to active while antagonists DO NOT

35
Q

What are the characteristics of competitive antagonists?

A
  • reversible
  • inhibition overcome by increasing the conc. of an agonist
36
Q

What are the characteristics of noncompetitive antagonists?

A
  • irreversible
  • prevents agonist, at any conc., from producing a maximum effect on a given receptor
37
Q

When looking at a graph, what is the movement of competitive antagonists?

A

shift from left to right

38
Q

When looking at a graph, what is the movement of noncompetitive antagonists?

A

has a decrease, line gets closer to 0

39
Q

What is an inverse agonist?

A

reduce constituitive activity of a receptor

40
Q

An inverse agonist has affinity for what?

A

ONLY for inactive state (shifts the equil.)

41
Q

On a graph how would you differenciate between the types of antagonists and agonists?

A
  • full agonist: at the very top
  • patial agonist: halfway between 0 and full agonist
  • antagonis: at 0
  • inverse agonist: below 0
42
Q

What is receptor desensitization?

A

when continued exposure ot the same conc. of the drug diminishes the effect as a function of time of exposure to the agonist

43
Q

Continuous exposure to an agonist can what?

A

decrease the number of receptors

44
Q

Continuous exposure to an antagonist can what?

A

increase the number of receptors

45
Q

What is responsible for pharmacodynamic tolerance?

A

receptor desensitization and down regulation

46
Q

What is required to produce a given magnitude of effect and what is it known as?

A

increasing doses of drugs; tachyphylaxis

47
Q

What are spare receptors?

A

when the max effect is reached with a small fraction of the receptors

48
Q

What gives the terapeutic index?

A

ED50

49
Q

What is ED50?

A

median effective does that causes 50% of individuals to have an effect

50
Q

What is LD50?

A

median lethal does that kills 50% of tested animals

51
Q

What is TD50?

A

dose that produces toxic effect in 50% of individuals

52
Q

For a drug to be safe, what is the ratio we need?

A

a high TD50 and a low ED50

Pharmacology (5 decks)

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