Pharmacology - Inflammation Flashcards Preview

MS 2 - Unit 2 > Pharmacology - Inflammation > Flashcards

Flashcards in Pharmacology - Inflammation Deck (45):
1

The major cytokines involved in inflammation are:

IL-1 - endogenous pyrogen
IL-8 - chemotacttic agent
TNF - regulates the production of other cytokines and induces fibrosis and tissue catabolism

2

What are the two cyclooxygenases involved in the inflammatory response?

COX-1 and COX-2
COX-1 - made constitutively throughout the body, makes TXA2
COX-2 induced during inflammation, makes prostaglandins
Both COXs are inhibited by NSAIDs

3

Histamine is released from:

mast celle and basophils

functions to dilate capillaries, increase venule permeability and involved in sensitization

4

Kinins are released from:

kinin system

same effects as histamine, but more chronic

5

Cytokines are released from:

primarily lymphoid cells

functions in immunoregulation, inflammation, fever, chemotaxis, tissue catabolism, induction of COX-2 etc.

6

Eicosanoids are released from:

lymphoid and non-lymphoid cells

functions same as histamine, plus contraction/relaxation

7

MOA: acetylsalicylic acid

irreversibly blocks the synthesis of eicosanoids bby acetylating COX-1 and COX-2

8

Class: acetylsalicylic acid

Salicylate

9

What is the primary site of ASA transformation?

Liver

10

Therapeutic uses: ASA

1. Anti-inflammatory
2. Analgesic effects
3. Antipyretic effects (blocks PGE2)
4. Platelet effects - increases bleeding time by inhibiting TXA2 synthesis (and thus, platelet aggregation)

11

T/F: ASA is not effective at relieving visceral pain.

True

12

Side effects: ASA

GI irritation and bleeding (loss of protective effect of PGE2 and PGI2);
Anemia;
Hepatotoxicity
Hypersensitivity rxns
Salicylate toxicity
Nephrotoxocity

13

Class: Diflunisal

Salicylate

14

MOA: Diflunisal

Competitive inhibitor of COX-1 and COX-2
Better half life than ASA

15

Uses: Diflunisal

Best for sprains and strains;
Dental pain;
Postepisiotomy pain;
Osteoarthritis
Cancer pain with bone mets

16

Side effects: Diflunisal

Fewer GI side effects and platelet effects than ASA

17

Class: Acetominophen

Para-amino phenol

18

MOA: Acetominophen

Reversibly inhibits COX-1 and COX-2

19

Uses: Acetominophen

NOT anti-inflammatory
for pain and fever

20

Side effects: Acetominophen

Fulminant liver failure possible w/ overdose;
renal tubular necrosis - rare and with chronic use

21

What is the toxic intermediate formed by the metabolism of acetaminophen, that gets removed by glutathione in moderate and low doses?

N-acetyl-benzoquinoneimine

22

What is given to reverse acetaminophen overdose?

Acetylcysteine (Mucomyst)
restores glutathione levels

23

Class:
Indomethacin
Sulindac

Indole

24

MOA:
Indomethacin
Sulindac

Reversible inhibits COX-1 and COX-2;
favors COX-1

25

Uses:
Indomethacin
Sulindac

RA
Ankylosing spondylitis
Osteoarthritis
Gout

26

What is the difference between indomethacin and sulindac?

Sulindac is half as potent as indomethacin
No renal toxicity

27

What is the therapeutic difference between ASA and indomethacin?

Indomethacin is 10x more potent than ASA

28

Side effects:
Indomethacin
Sulindac

Thrombocytopenia
Aplastic Anemia
Severe frontal headaches

29

What is the ONLY indication for indomethacin in children?

closure of ductus arteriosis

30

Class:
Ibuprofen
Flurbiprofen
Naproxen
Oxaprozin

Proprionic acid derivative

31

MOA:
Ibuprofen
Flurbiprofen
Naproxen
Oxaprozin

Reversibly inhibits COX-1 and COX-2
favors COX-1

32

Uses:
Ibuprofen
Flurbiprofen
Naproxen
Oxaprozin

RA;
osteoarthritis;
Ankylosing spondylitis;
Acute gout attacks

33

What prioprionic acid derivative has the longest half life?

Naproxen (13 hours) and Oxaprozin (50 hours)

34

Class: Piroxicam

Enolic Acid

35

Uses: Piroxicam

RA
Osteoarthritis
recommended bc of its long half life (45 hours)

36

Side Effects: Piroxicam

Same as ASA

GI irritation and bleeding (loss of protective effect of PGE2 and PGI2);
Anemia;
Hepatotoxicity
Hypersensitivity rxns
Salicylate toxicity
Nephrotoxocity

37

MOA: Piroxicam

Reversibly inhibits COX-1 and COX-2
favors COX-1

38

Class:
Keterolac
Diclofenac

Heteroaryl acetic acids

39

MOA:
Keterolac
Diclofenac

Reversibly inhibits COX-1 and COX-2
favors COX-1

40

What NSAID is injectable (intramuscular)?

Keterolac
Potent analgesic - use for postoperative pain

41

Side Effects: Keterolac

Same as ASA

GI irritation and bleeding (loss of protective effect of PGE2 and PGI2);
Anemia;
Hepatotoxicity
Hypersensitivity rxns
Salicylate toxicity
Nephrotoxocity

42

Class:
Celecoxib
Etoricoxib

COX-2 inhibitor

43

MOA:
Celecoxib
Etoricoxib

selectively inhibits COX-2

44

Selective COX-2 inhibitors are contraindicated in what patient populations?

Pregnant patients
Patients with heart problems

45

Do NSAIDS inhibit leukotriene synthesis?

No
They inhibit prostaglandin, prostacycline and thromboxane synthesis