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Pharmacyology 3 > Aspirin > Flashcards

Aspirin Flashcards

1
Q

Prostaglandins are major mediators of

A

pain
fever
inflammation

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2
Q

COX leads to…

A
  • Prostaglandins
  • thromboxane
  • prostacyclin
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3
Q

RLS in PG synthesis

A

COX

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4
Q

COX-1 is _____ expressed

A

constitutively

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5
Q

Where does COX1 work?

A
  • CNS: fever/pain
  • peripheral: pain
  • stomach: protect mucosal lining
  • platelets: increase platelet aggregation and blood clotting
  • regulate kidney function
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6
Q

Prototype COX-1 inhibitor

A

aspirin

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7
Q

COX2 is ____ expressed ____

A

constitutively expressed isozyme

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8
Q

Where does COX2 work?

A
  • CNS: pain
  • stomach: protect mucosal lining
  • endothelial cells: decrease platelet aggregation
  • wound healing, bone repair
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9
Q

COX1 work in platelets or endothelial cells?

A

Platelets: increase platelet aggregation

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10
Q

COX2 work in platelets or endothelial cells?

A

endothelial cells: decreases platelet aggregation

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11
Q

COX2 has a ____ isozyme that is critical for inflammation

A

inducible

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12
Q

COX1 or COX2 key target for NSAID anti-inflammatory effects?

A

COX2

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13
Q

Prototype COX2 inhibitor

A

Celecoxib

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14
Q

Most NSAIDs inhibit both COX1 and COX2, usually stronger on ______. This makes them useful for treating what?

A

COX1

  • pain (1 and constitutive 2)
  • fever (1)
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15
Q

COX1 and COX2 suppression of inflammation

A

require high doses

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16
Q

COX 2 inhibitor drugs used for

A
  • inflammation
  • sometimes pain
  • fewer unwanted COX1 adverse effects
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17
Q

Prototype of all NSAIDs and non-opioid analgesics

A

Aspirin

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18
Q

Aspirin is ____ ___

A

acetyl-salicylic acid

- rapidly hydrolyzed (de-acetylated) to salicylic acid

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19
Q

The anti-inflammatory and analgesic effects of aspirin are mediated by its ______ metabolite

A

salicylate

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20
Q

Salicylate are what type of inhibitors?

A

reversible

competitive

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21
Q

T/F salicylates are distributed throughout body

A

True

- including CNS for fever/pain

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22
Q

Aspirin is ____% protein bound in plasma

A

80%

  • slow accumulation of free drug
  • drug interactions from displacing warfarin, methotrexate, sulfonamides
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23
Q

At low to moderate doses, salicylate is metabolized where? what kinetics?

A
  • liver by conjugation
  • first order
  • saturable
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24
Q

At higher doses, salicylate is metabolized where? what kinetics?

A
  • unmetabolized by kidneys
  • zero order
  • OATs
  • half-life increases with increasing dose
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25
Q

Lower doses of aspirin effects

A

analgesic
anti-pyretic
COX1 response

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26
Q

Higher doses of aspirin effects

A
  • anti-inflammatory

- COX2 response

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27
Q

Low doses of aspirin how is it excreted?

A

glycine salts

glucuronide salts

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28
Q

Higher doses of aspirin how is it excreted?

A

free salicylate excretion

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29
Q

Aspirin amount for analgesia, anti=pyresis

A

2 tablets

650mg

30
Q

Aspirin amount for anti inflammation

A

5 tablets

31
Q

Aspirin t1/2 for low dose

A

2 hour

32
Q

Aspirin t1/2 for moderate dose

A

10-12 hour

33
Q

Aspirin t1/2 for high dose

A

15-30 hour

34
Q

Is aspirin good for pain of inflammation?

A

yes!

inhibit pain and underlying inflammation

35
Q

Unique use of aspirin

A

prevent thrombus formation (blood clotting)

prolong bleeding time

36
Q

Aspirin can _____ inactivate COXs in some tissues by _____ acetylating enzyme

A

irreversible

covalently

37
Q

____ near the site of GI absorption are the main cells exposed to acetyl-salicylic acid and covalent acetylation of COXs

A

platelets

38
Q

Major current use of aspirin

A

prevent MI and stroke

39
Q

lifetime of platelets

A

7 days

40
Q

Why is MI and stroke a unique feature of aspirin?

A
  • covalent acetylation of COX
  • irreversible and prolonged action
  • acetyl effect! not salicylate!
41
Q

Side effects of aspirin

A
  • bleeding (even at low doses)
42
Q

CI aspirin

A

clotting deficiency

43
Q

To ensure adequate clotting during and after surgery aspirin is stopped ____ days prior to surgery

A

7-10 days

44
Q

Other possible uses of Aspirin

A

reduce GI cancer risk

AD

45
Q

Platelets use ___ to make thromboxanes

A

COX1

- increase clotting and thrombosis risk

46
Q

Endothelial cells use ____ to make prostacyclins

A

COX2

- decrease clotting and thrombosis risk

47
Q

Low aspirin dose and thrombosis

A
  • anti-thrombosis PGIs formation from endothelial cells
48
Q

Prolonged inhibition of platelet COX1 causes _______

A

sustained reduction in Txs

49
Q

Current aspirin recommendation for thrombosis prevention

A

75-81 mg

- if benefit outweighs risk of GI hemorrhage

50
Q

Enteric coating to reduce ____

A

GI distress

51
Q

Cautions of aspirin

A
  • premature closure of ductus arterioles
  • avoid 3rd trimester
  • renal and hepatic toxicities (long term use, elderly)
52
Q

Salicylism

A

mild toxicity

  • from excess chronic use in older adults
  • tinnitus, dizzy, HA, confusion, deafness
  • drowsy, thirst, N/V
53
Q

low dose aspirin toxicity

A
  • increase O2 consumption, CO2 production
  • stimulates respiration
  • exces CO2 inhaled
54
Q

high dose aspirin toxicity

A
  • respiratory alkalosis
55
Q

Adverse effects of aspirin

A
  • GI irritation
  • GI bleeding
  • peptic ulcers
  • CV effects
  • induce asthma attacks
56
Q

____ is responsible for 15,000 aspirin related deaths

A

GI hemorrhage

57
Q

Reyes syndrome

A
  • aspirin

- do not use <16

58
Q

overdose aspirin

A
  • children ingest large dose: >150 lethal
  • GI disturbance
  • CNS disturbance
  • fever, dehydration, sweating
  • skin eruptions
  • metabolic acidosis, hypokalemia
  • decrease blood flow
59
Q

______ is eventual cause of death in aspirin OD

A
  • respiratory failure

- respiratory depression: respiratory acidosis

60
Q

Low dose aspirin acid base effect

A
  • increased CO2

- acidosis

61
Q

Low dose aspirin respiratory effect

A

compensation for acidosis by respiration

62
Q

low dose aspirin serum pH

A

normal

63
Q

higher dose aspirin acid base effect

A
  • compensation for alkalosis by HCO3 excretion
64
Q

higher dose aspirin respiratory effect

A

direct stimulation leads to alkalosis

65
Q

higher dose aspirin serum pH

A

normal

66
Q

toxic dose aspirin acid base effect

A

metabolic acidosis

renal + respiratory

67
Q

toxic dose aspirin respiratory effect

A

central depression produces acidosis

68
Q

toxic dose aspirin serum pH

A

acidic with organ failure

69
Q

treating OD in aspirin

A
  • hospitalize and maintain vital signs
  • whole bowel irrigation
  • activated charcoal
  • hasten elimination
70
Q

How to hasten elimination of aspirin

A
  • volume repletion
  • alkalization of urine with sodium bicarb
  • ion trapping

Pharmacyology 3 (12 decks)

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