NSAIDs Flashcards

1
Q

Name 3 chemical mediators of inflammation.

A

1) kinins
2) histamine
3) neuropeptides

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2
Q

Give an example of a kinin.

A

bradykinin

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3
Q

Give an example of a neuropeptide.

A

substance P

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4
Q

Tissue destruction leads to release of _____ and synthesis of _____.

A

chemical mediators; eicosanoid mediators

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5
Q

Where do eicosanoid mediators derive from?

A

arachadonic acid

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6
Q

What is the target of an NSAID?

A

COX-1 and COX-2

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7
Q

By inhibiting COX1 and 2, production of ____ and ____ will decrease.

A

inflammatory prostaglandins; thromboxanes

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8
Q

COX is the major synthetic enzyme for ___ and ____.

A

prostaglandins (PGs); thromboxane A2 (TXA2)

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9
Q

What are the 4 therapeutic uses of an NSAID?

A

1) analgesia
2) antipyretic
3) anti-inflammatory
4) antithrombogenesis

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10
Q

How is analgesia achieved by an NSAID?

A

inhibition of inducible COX-2 at sites of tissue injury

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11
Q

How is an antipyretic affect achieved by an NSAID?

A

inhibition of inducible COX-2 in the hypothalamus

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12
Q

How is an anti-inflammatory affect achieved by an NSAID?

A

inhibition of inducible COX-2 at sites of inflammation

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13
Q

How is an antithrobogenesis affect achieved by an NSAID?

A

inhibition of constituitive COX-1 in platelets

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14
Q

Name 5 common side affects of NSAIDs.

A

1) GI ulcers, bleeding, nausea
2) increased bleeding problems
3) renal failure and nephritis
4) interference with uterine contractions
5) increased thrombotic events

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15
Q

Aspirin group

A

irreversible inhibition of COX-1 AND COX-2

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16
Q

traditional NSAIDs group

A

reversible inhibition of COX-1 and COX-2

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17
Q

acetaminophen group

A

inhibits COX-2 in CNS ONLY

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18
Q

cox-2 selective inhibitors group

A

selective reversible inhibition of COX-2 ONLY

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19
Q

Name the 5 chemical classes of traditional NSAIDs.

A

1) salicylates
2) pyrazolone derivatives
3) acetic/carboxylic acids
4) oxicam derivatives
5) propionic acid derivatives

20
Q

What are salicylates used for?

A

analgesic, antipyretic, anti-inflammatory

21
Q

What are pyrazolone derivatives used for?

A

analgesic, antipyretic, anti-inflammatory

22
Q

What are acetic/carboxylic acids used for?

A

analgesic, antipyretic, anti-inflammatory

23
Q

What are oxicam derivatives used for?

A

analgesic, antipyretic, anti-inflammatory

24
Q

What are propionic acid used for?

A

analgesic, antipyretic, anti-inflammatory

25
Q

What is aspirin used for?

A

analgesic, antipyretic, anti-inflammatory, antithrombotic

26
Q

Name 2 Pyrazolone derivatives.

A

1) phenylbutazone

2) oxyphenbutazone

27
Q

Name 4 acetic/carboxylic acids.

A

1) Indomethacin
2) Sulindac
3) Ketorolac
4) Nabumetone

28
Q

Name 2 oxicam derivatives.

A

1) piroxicam

2) meloxicam

29
Q

Name 5 proprionic acid derivatives.

A

1) ibuprofen
2) naproxen
3) ketoprofen
4) flurbiprofen
5) oxaprozin

30
Q

Name one positive and one negative to pyrazolone derivative use.

A

positive: more potent and longer lasting
negative: serious toxicities with chronic use or misuse

31
Q

Name one positive and one negative to pyrazolone acetic/carboxylic acid use.

A

positive: fewer toxic rxns than pyrazolones
negative: more total adverse rxns; limited to arthritis

32
Q

Name one positive and one negative to oxicam derivative use.

A

positive: Potent, extremely long half-lives (15-50 hrs)
negative: Potent, extremely long half-lives (15-50 hrs)

33
Q

Name one positive and one negative to proprionic acid derivative use.

A

positive: better tolerated than other NSAIDs
negative: general NSAID risks

34
Q

What is acetaminophen used for?

A

Analgesic; antipyretic

35
Q

What is a positive to acetaminiophen use?

A

less GI side effects

36
Q

What is celecoxib (Celebrex) used for?

A

Analgesic, antipyretic, anti-inflammatory

37
Q

What is a positive to celecoxib (Celebrex) use?

A

less GI side effects

38
Q

Treatment of ____ pain usually requires opiod analgesics.

A

visceral

39
Q

Treatment of visceral pain usually requires _____.

A

opiod analgesics

40
Q

What is visceral pain caused by?

A

direct stimulation of sensory nerves (Aδ)

41
Q

What is the dose for anti-inflammatory NSAID affects?

A

> 4g/day

42
Q

What is the mechanism of action for the anti-platelet affect seen with NSAIDs?

A

inhibition of platelet aggregation

43
Q

Why is platelet clumping prevented for the life of the platelet?

A

platelets cannot synthesize new COX-1

44
Q

Where is the largest concentration of acetylsalicylic acid?

A

in the portal vein

45
Q

_____ is rapidly hydrolyzed to salicylate by esterases in blood.

A

Acetylsalicylic acid

46
Q

Acetylsalicylic acid is rapidly hydrolyzed to _____ by _____ in blood.

A

salicylate; esterases