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MS 2 - Unit 2 > Pharmacology - Inflammation > Flashcards

Pharmacology - Inflammation Flashcards

1
Q

The major cytokines involved in inflammation are:

A

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

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2
Q

What are the two cyclooxygenases involved in the inflammatory response?

A

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

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3
Q

Histamine is released from:

A

mast celle and basophils

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

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4
Q

Kinins are released from:

A

kinin system

same effects as histamine, but more chronic

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5
Q

Cytokines are released from:

A

primarily lymphoid cells

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

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6
Q

Eicosanoids are released from:

A

lymphoid and non-lymphoid cells

functions same as histamine, plus contraction/relaxation

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7
Q

MOA: acetylsalicylic acid

A

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

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8
Q

Class: acetylsalicylic acid

A

Salicylate

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9
Q

What is the primary site of ASA transformation?

A

Liver

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10
Q

Therapeutic uses: ASA

A
  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)
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11
Q

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

A

True

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12
Q

Side effects: ASA

A 
GI irritation and bleeding (loss of protective effect of PGE2 and PGI2);
Anemia;
Hepatotoxicity
Hypersensitivity rxns
Salicylate toxicity
Nephrotoxocity
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13
Q

Class: Diflunisal

A

Salicylate

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14
Q

MOA: Diflunisal

A

Competitive inhibitor of COX-1 and COX-2

Better half life than ASA

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15
Q

Uses: Diflunisal

A 
Best for sprains and strains;
Dental pain;
Postepisiotomy pain;
Osteoarthritis
Cancer pain with bone mets
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16
Q

Side effects: Diflunisal

A

Fewer GI side effects and platelet effects than ASA

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17
Q

Class: Acetominophen

A

Para-amino phenol

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18
Q

MOA: Acetominophen

A

Reversibly inhibits COX-1 and COX-2

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19
Q

Uses: Acetominophen

A

NOT anti-inflammatory

for pain and fever

20
Q

Side effects: Acetominophen

A

Fulminant liver failure possible w/ overdose;

renal tubular necrosis - rare and with chronic use

21
Q

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

A

N-acetyl-benzoquinoneimine

22
Q

What is given to reverse acetaminophen overdose?

A

Acetylcysteine (Mucomyst)

restores glutathione levels

23
Q

Class:
Indomethacin
Sulindac

A

Indole

24
Q

MOA:
Indomethacin
Sulindac

A

Reversible inhibits COX-1 and COX-2;

favors COX-1

25
Q

Uses:
Indomethacin
Sulindac

A

RA
Ankylosing spondylitis
Osteoarthritis
Gout

26
Q

What is the difference between indomethacin and sulindac?

A

Sulindac is half as potent as indomethacin

No renal toxicity

27
Q

What is the therapeutic difference between ASA and indomethacin?

A

Indomethacin is 10x more potent than ASA

28
Q

Side effects:
Indomethacin
Sulindac

A

Thrombocytopenia
Aplastic Anemia
Severe frontal headaches

29
Q

What is the ONLY indication for indomethacin in children?

A

closure of ductus arteriosis

30
Q 
Class:
Ibuprofen
Flurbiprofen
Naproxen
Oxaprozin
A

Proprionic acid derivative

31
Q 
MOA:
Ibuprofen
Flurbiprofen
Naproxen
Oxaprozin
A

Reversibly inhibits COX-1 and COX-2

favors COX-1

32
Q 
Uses: 
Ibuprofen
Flurbiprofen
Naproxen
Oxaprozin
A

RA;
osteoarthritis;
Ankylosing spondylitis;
Acute gout attacks

33
Q

What prioprionic acid derivative has the longest half life?

A

Naproxen (13 hours) and Oxaprozin (50 hours)

34
Q

Class: Piroxicam

A

Enolic Acid

35
Q

Uses: Piroxicam

A

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

36
Q

Side Effects: Piroxicam

A

Same as ASA

GI irritation and bleeding (loss of protective effect of PGE2 and PGI2);
Anemia;
Hepatotoxicity
Hypersensitivity rxns
Salicylate toxicity
Nephrotoxocity
37
Q

MOA: Piroxicam

A

Reversibly inhibits COX-1 and COX-2

favors COX-1

38
Q

Class:
Keterolac
Diclofenac

A

Heteroaryl acetic acids

39
Q

MOA:
Keterolac
Diclofenac

A

Reversibly inhibits COX-1 and COX-2

favors COX-1

40
Q

What NSAID is injectable (intramuscular)?

A

Keterolac

Potent analgesic - use for postoperative pain

41
Q

Side Effects: Keterolac

A

Same as ASA

GI irritation and bleeding (loss of protective effect of PGE2 and PGI2);
Anemia;
Hepatotoxicity
Hypersensitivity rxns
Salicylate toxicity
Nephrotoxocity
42
Q

Class:
Celecoxib
Etoricoxib

A

COX-2 inhibitor

43
Q

MOA:
Celecoxib
Etoricoxib

A

selectively inhibits COX-2

44
Q

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

A

Pregnant patients

Patients with heart problems

45
Q

Do NSAIDS inhibit leukotriene synthesis?

A

No

They inhibit prostaglandin, prostacycline and thromboxane synthesis

MS 2 - Unit 2 (26 decks)

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