Pharm 42 - Eicosanoids Flashcards Preview

PBL Pharm Block 3 > Pharm 42 - Eicosanoids > Flashcards

Flashcards in Pharm 42 - Eicosanoids Deck (69)
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1

Aspirin MOA

Irreversible inhibits COX-1 and COX-2 by acetylating the active site serine residue

2

Aspirin clinical applications

Mild-to-moderate pain, HA, myalgia, arthralgia, prophylaxis of stroke and MI (@ low doses -> antiplatelet effect)

3

Aspirin adverse effects

GI ulcer/bleeding, Reye's syndrome, asthma exacerbation, bronchospasm, angioedema; also tinnitus

4

Aspirin contraindications

Hypersensitivity; aspirin-triggered asthma; chickenpox/flu in children/teens (risk of Reye's syndrome)

5

Aspirin therapeutic considerations

Increases plasma concentration of acetazolamide -> CNS toxicity; Ibuprofen may inhibit antiplatelet effect; may enhance methotrexate toxicity; increased risk of bleeding in anti coagulated pts

6

NSAID MOA and classes

Inhibit COX-1 and COX-2, decreasing synthesis of eicosanoids and limiting inflammatory response
Includes Proprionic acids, acetic acids, Oxicams, Fenamates, Ketones

7

Priopionic Acids (4)

Ibuprofen, Naproxen, Ketoprofen, Flurbiprofen

8

Acetic Acids (5)

Indomethacin, Sulindac, Etodolac, Diclofenac, Keterolac

9

Oxicams (1)

Prioxicam (duh)

10

Fenamates (2)

Mefenamate, Meclofenamate

11

Ketones (1)

Nabumetone

12

NSAID clinical applications

Mild-to-moderate pain, F, OA, RA, dysmenorrhea, gout, PDA closure (indomethacin)

13

NSAID adverse effects

GI hemorrhage/ulceration/perforation, nephrotoxicity, Stevens-Johnson syndrome, pseudoporphyria (naproxen); also tinnitus

14

NSAID contraindications

GI/intracranial bleeding; coagulation defects; asthma, urticaria, or allergic rxn to NSAIDs including ASA (b/c of risk of fatal anaphylaxis); renal insufficiency

15

NSAID therapeutic considerations

1) Naproxen has longer T1/2, more potency, and fewer GI effects than ASA
2) Keterolac is used for 3-5 days post-surgery
3) Piroxicam has long T1/2 - dose once daily
4) Nabumetone has greatest COX-2 selectivity
5) Fenamate is less useful than ASA

16

Acetominophen MOA

COX-3 inhibitor in CNS

17

Acetominophen clinical applications

F, mild-to-moderate pain

18

Acetominophen adverse effects

Hepatotoxicity, nephrotoxicity; also rash and hypothermia

19

Acetominophen contraindications

Hypersensitivity

20

Acetominophen therapeutic considerations

Insignificant anti-inflammatory effects b/c of weak inhibition of peripheral COX; overdose is LEADING CAUSE OF HEPATIC FAILURE (b/c of modification by CYP40 to reactive metabolite that requires detoxification by glutathione) -> antidote is N-ACETYLCYSTEINE

21

Celecoxib MOA

Selective inhibition of COX-2

22

Celecoxib clinical applications

OA, RA in adults, ankylosing spondylitis, primary dysmenorrhea, acute pain in adults, familial adenomatous polyposis (b/c of some interaction w/ PPAR-delta)

23

Celecoxib adverse effects

MI, ischemic stroke, heart failure, GI bleeding/ulceration/perforation, renal papillary necrosis, exacerbation of asthma; also peripheral edema

24

Celecoxib contraindications

Hypersensitivity to sulfonomides or celecoxib; asthma, urticaria, or allergic rxn to NSAIDs (b/c of risk of fatal anaphylaxis); pain with CABG

25

Celecoxib therapeutic considerations

Decreased efficacy of ACE inhibitors

26

Glucocorticoid MOA and names (4)

Induces lipocortins -> inhibit COX-2 action and prostaglandin biosynthesis
Prednison, Prednisolone, Methylprednisolone, Dexaethasone

27

Glucocorticoid clinical applications

Inflammatory conditions; autoimmune diseases

28

Glucocorticoid adverse effects

Immunosuppression, cataracts, hyperglycemia, hypercortisolism, depression, euphoria, osteoporosis, growth retardation in children, muscle atrophy; topical may cause skin atrophy

29

Glucocorticoid contraindications

Systemic fungal infection

30

Zileuton MOA

Inhibits 5-lipoxygenase -> decreases leukotriene synthesis