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Pharmacology > pharmacodynamics > Flashcards

pharmacodynamics Flashcards

1
Q

agonist

A

causes active change of target (excitation or inhibition)

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2
Q

antagonist

A

occupies site and prevents agonist from binding

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3
Q

specific binding

A

binding to receptor

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4
Q

non-specific binding

A

binding to cell membrane

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5
Q

competitive binding

A

binding at active site

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6
Q

non-competitive binding

A

binding at allosteric site

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7
Q

benzodiazepines and barbiturates are examples of

A

allosteric agonists

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8
Q

pumps function at what type of enzyme kinetics

A

saturable (zero order)

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9
Q

MDR transporters and Na+/K+ ATPase pumps are an example of what type of transporter

A

pump

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10
Q

lidocaine

A

voltage-gated Na+ channel blocker

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11
Q

dihydropiridine

A

L-type Ca+2 channel blocker (allosteric modulator)

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12
Q

fluoxetine blocks the serotonin selective reuptake, an example of what type of target

A

symport transporter

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13
Q

furosemide block what

A

Na+/K+/Cl-2 symport transporter

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14
Q

digoxin blocks

A

Na+/Ca+2 exchanger (antiport transporter)

Na+/K+ ATPase

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15
Q

CYP2C9 inhibitors

A

penecillin and azoles

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16
Q

CYP2C9 inducers

A

phenytoin, alcohol, ginseng

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17
Q

if you induce enzyme activity, drug level ___

A

decrease

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18
Q

if you inhibit enzyme activity, drug level ___

A

increases

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19
Q

4 types of receptor interactions

A
  1. ion channels
  2. GPCR
  3. enzyme-linked receptor
  4. diffuse through membrane
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20
Q

ion channels have how many transmembrane domains

A

5

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21
Q

how many transmembrane domains does a GPCR have

A

7

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22
Q

G proteins have how many subunits

A

3 (a, b, g)

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23
Q

competitive antagonist

A

binds to active site and blocks agonist from binding, so nothing happens

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24
Q

non-competitive antagonist

A

binds to allosteric site and decreases the effect of the agonist

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25
Q

non-competitive agonist

A

binds to allosteric site and increases the effect of the agonist

26
Q

ligand-gated channels or ROC: # of binding sites

A

2

27
Q

what is the subunit where the ligand binds on an ROC

A

alpha

28
Q

ROCs or ligand-gated channels have how many subunits

A

5

29
Q

nicotinic Ach receptor is a type of

A

ROC

30
Q

nicotinic Ach receptor: location of ligand-binding site

A

outside of cell near amino terminal

31
Q

GABA-A receptor is a type of

A

ROC

32
Q

how many transmembrane proteins does GPCR have

A

7

33
Q

where is the ligand-recognition site for GPCR

A

hidden within the cell membrane between 2nd and 3rd domain

34
Q

where is the g protein-coupling domain in GPCR

A

at the 3rd intracellular loop

35
Q

4 steps for g protein pathway

A
  1. ligand binds to GPCR
  2. g protein activates adenylyl cyclase
  3. adenylyl cyclase: ATP -> cAMP
  4. protein kinase A uses cAMP to phosphorylate
36
Q

steps for g protein activation

A
  1. agonist binds
  2. GTP-GDP exchange (g-protein binds to GTP)
  3. g protein is activated
37
Q

steps after g protein is activated

A
  1. alpha-GTP binds to effector (adenylyl cyclase)
  2. effector is activated
  3. agonist unbinds
  4. GTP hydrolyzed
  5. g protein formed again
38
Q

2 main effector proteins in the GPCR pathway

A
  • adenylyl cyclase

- phospholipase C (PLC)

39
Q

phospholipase C converts what to what

A

PIP2 -> IP3 + DAG

40
Q

what does IP3 do

A

stimulates vesicles to release Ca+2

41
Q

what does DAG do

A

activates PKC

42
Q

what do these G proteins do?: Gi, Gs, G12, Gq

A

Gi inhibits

Gs, G12, and Gq activate

43
Q

which G proteins activate adenylyl cyclase

A

Gi and Gs

44
Q

which G proteins activate phospholipase C

A

G12 and Gq

45
Q

for a proteinase-activated receptor (PAR), cleavage at the amino terminal will cause

A

activation of the PAR

46
Q

can PARs be activated again?

A

no, because cleavage cannot be reversed

47
Q

location of ligand-recognition site for enzyme-linked receptor

A

outside of cell near amino terminal

48
Q

steps when ligand binds to enzyme-linked receptor

A
  1. ligand binds
  2. dimerization
  3. autophosphorylation
  4. Grb2 binds and gets phosphorylated
  5. Activation of Ras/Raf/MAP kinase pathway
49
Q

example of enzyme-linked receptors

A

receptor tyrosine kinase (for growth factors and insulin)

50
Q

cytokine receptors follow the ___ pathway

A

Jak/Stat

51
Q

what is unique about the Jak/Stat pathway

A
  • no catalytic domains
  • Stat dimer has 2 NLS
  • moves into nucleus to bind to genes
52
Q

ANP and Nitric Oxide (NO) receptors are part of what pathway

A

guanylyl recptor cyclases

53
Q

Class I receptors location

A

cytoplasm

54
Q

Class II receptors location

A

nucleus

55
Q

function of chaperones

A

bound to receptor to prevent accidental translocation to nucleus

56
Q

how are the DNA and ligand binding sites ordered

A

N-DNA -Ligand - C

57
Q

examples of class 1 receptors

A

estrogen, progesteron, and androgen receptors, corticosteroid receptors

58
Q

steps of agonist binding to LBD on class 1 receptor

A
  • ligand binds
  • AF2 binds to LBD
  • co-activator protein binds to LBD
59
Q

what happens when the antagonist binds to LBD on class 1 receptor

A
  • antagonist prevents AF2 from binding to LBD

- co-activator protein cannot bind also

60
Q

examples of class 2 receptor

A
  • vitamin d3 receptor

- thyroid hormone receptor

61
Q

inflammatory response is mediated by what type of receptors

A

class 2 receptors

Pharmacology (17 decks)

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