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FM 1 > Drug Action > Flashcards

Drug Action Flashcards

1
Q

Physiological variables affecting drug responses

A
  • body weight and size (surface area)
  • age (eg infants and elderly-different renal fxn)
  • gender differences in lean/fat mass
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2
Q

Pathologic variables affecting drug responses

A
  • renal insufficiency
  • hepatic disease
  • acid/base imbalance (changes charged species)
  • altered electrolyte status
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3
Q

Genetic variables affecting drug responses

A

variations in :

  • biotransformation
  • functional proteins and enzymes
  • receptor proteins
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4
Q

Nonspecific drug action

A

drugs that act by physicochemical processes

  • laxatives (surfactants, inorganic ions)
  • metal chelators (EDTA)
  • osmotic diuretics (urea, mannitol)
  • acids, bases (antacids)
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5
Q

Specific drug action

A

-Drugs that act on receptors, enzymes, transporters, or other identified components of the cell

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6
Q

Domains of nuclear drug receptor

A
  • transcription activating domain-interacts w/ DNA->gene expression
  • DNA binding domain-blocked by heat shock protein when no ligand bound
  • Ligand binding domain-ligand binding causes conformational change, HSP dissociates, receptor translates into nucleus and binds
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7
Q

desensitization

A

response diminishes over seconds/mins, even in continued presence of agonist

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8
Q

Gs

A
  • stimulatory
  • B-adrenergic amines, glucagon, histamine, serotonin, hormones
  • activates adenylyl cyclase-> increase cAMP
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9
Q

Gi 1, 2, and 3

A
  • inhibitory
  • a2-adrenergic amines, acetylcholine (muscarinic), opiods, serotonin
  • inhibits adenylyl cyclase->decrease cAMP
  • activates cardiac K+ channels->hyperpolarize->decrease HR
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10
Q

Gq

A

-Activates phospholipase C->increase IP3, DAG, intracellular Ca

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11
Q

Kd

A

equilibrium dissociation constant
k2/k1
50% of binding sites are occupied if [D]=Kd
low Kd=tight binding=high affinity

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12
Q

EC50

A

Effective [ ] for 50% response

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13
Q

ED50

A

effective dose for 50% response

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14
Q

Spare receptors

A

fractional occupation of total receptor population can generate full response
with spare receptors, EC50

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15
Q

Potency

A
  • dose required to produce a specified response

- different drugs may require different doses to produce the same response

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16
Q

Agonist

A

activates receptor to initiate a sequence of events leading to a biological response (stabilize active form)
has intrinsic efficacy
full agonist elicits maximal response

17
Q

Partial Agonist

A
  • agent which is less effective at activating receptor
  • elicits a response that is less than the maximal response produced by a full agonist
  • has less efficacy than a full agonist
  • appears to be antagonist in presence of full agonist due to occupation of agonist receptor sites
  • sometimes may be useful-blunting response
18
Q

Antagonist

A
  • Agent which does not activate receptor upon binding
  • has no intrinsic efficacy
  • blunts effect of agonists
  • have zero efficacy, but not necessarily zero effect
19
Q

Competitive antagonism

A

antagonist competes for agonist binding site on receptor

surmountable

20
Q

Noncompetitive antagonism

A

-antagonist produces nonfunctional complex or has post-receptor site of action
-insurmountable
-antagonist binds allosteric receptor site, change affinity of receptor for agonist OR blocks step beyond receptor activation OR two agonists produce opposite pharmacodynamic response
eg NE and histamine
-ED50 remains unchanged (but % response of changes compared to without antagonist)

21
Q

Irreversible antagonism

A
  • form of noncompetitive antagonism

- drug forms covalent antagonist-receptor complex; antagonism cannot be washed out

22
Q

Physiological antagonism

A
  • drugs produce opposing responses by acting on different systems
  • each drug has intrinsic activity
  • eg phenylephrine and nitroglycerin
23
Q

Chemical antagonism

A
  • antagonist acts directly on agonist to chemically alter it

- protamine and heparin

24
Q

Allosteric modulators

A
  • regulate activity of agonist, can either enhance or inhibit
  • no effect in absence of receptor activation by agonist
  • eg benzodiazepines enhance action of GABA on GABAa receptor
  • B-carbolines decrease action of GABA on GABAa receptor
25
Q

Inverse agonist

A

-inhibit agonist-dependent and agonist-independent receptor activity (stabilize inactive form)

FM 1 (9 decks)

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