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POD > Eicosanoids and NSAID > Flashcards

Eicosanoids and NSAID Flashcards

1
Q

Prostacyclin (PGI2)

A 
Inhibit platelet aggregation
Powerful bronchodialator
Inhibits gastric acid secretion/promotes mucus
Increase Renal GFR
Relax uterine muscle
Induces pain
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2
Q

Prostaglandin (PGE2)

A

Vasodialator
Low conc enhances/high conc inhibits platelet agg.
Bronchodialator
Inhibit gastric acid secretion/ promote mucus
Increase GFR
Contracts uterine sooth muscle (low conc.)
Induces Pain and Fever

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3
Q

Thromboxane (TXA2)

A 
potent vasoconstrictor
enhance platelet aggregation
product of platelet COX-1
Bronchoconstrictor
decreased renal function (vasoconstriction) 
Uterine muscle contraction
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4
Q

Prostaglandin F2a (PGF2a)

A

Vasoconstrictor
Bronchoconstrictor
Contracts uterine smooth muscle
Decreases intra-ocular pressure

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5
Q

Misoprostol

A

PGE1 analog
Inhibits gastric acid secretion
Adjunct to NSAID therapy (reduce ulcer)
Contraindicated in pregnancy (uterine contraction)

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6
Q

Alprostadil

A

PGE1
maintains patent ductus arteriosus
vasodialator (increases lung perfusion = inc. O2)

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7
Q

Latanoprost

A

PGF2a analog

used to treat open angle glaucoma

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8
Q

LTB4

A

Chemotactic for PMN leukocytes/eosinophils/monocyte
hyperalgesia
Elevated in IBD

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9
Q

Cysteinyl Luekotrienes (LTC4, LTD4, LTE4)

A

Chemotactic for eosinophils
Bronchoconstrictors
Increase vascular permeability
Components of slow acting substance of anaphylaxis

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10
Q

Leukotriene Receptors

A

BLT1 - LTB4 - none - some suppression of inflammation
BLT2- LTB4 - HPETE - ?
CysLT1 -LTD4 - C4,E4 - Pulm inflam. and fibrosis respon.
CysLT2 -LTD4,C4 - E4- Pulm inflam and fibrosis respon.

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11
Q

Zafirlukast

A

Competitive, reversible LTD4 receptor antagonist
decrease airway constriction & vascular perm.
Uses: prophylactic for asthma, allergic rhinitis
Adverse: headache, pharyngitis, increase LFTs (rare)
Drug interax: inhibits CYP3A4 and 2C9

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12
Q

Montelukast

A

Competitive, reversible LTD4 receptor antagonist
decrease airway constriction & vascular perm.
Uses: prophylactic for asthma, allergic rhinitis, aspirin sensitivity induced asthma
Adverse: headache

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13
Q

Zileuton

A

Inhibitor of 5-lipoxygenase
Uses: Asthma prophylaxis
Adverse: 4-5% elevated hepatic transaminase must monitor hepatic function, Contraindicated with liver disease and ergot alkaloids
Drug interax: Decreased clearance of Theophylline, Warfarin, and Propranolol

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14
Q

Aspirin

A

Irreversible inhibitor of cyclooxygenase
Uses: Antipyretic, antiinflammitory, analgesic (limited to brain/no effect on opioid receptor)
Low dose aspirin for MI, thrombosis, transient ischeic attacks, ect. Preecclampsia
Adverse: GI pain/bleeding/ulcers, Reye’s syndrome, salycylism - characterized by tinnitis

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15
Q

Aspirin Dosing

A

Antipyretic/analgesic - 350-625mg
Anti-inflammatory - 4-6g
Lethal - 10-30g

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16
Q

Aspirin - Platelets

A

Irreversibly inhibit platelet COX
Low doses inhibit platelet TXA2 production
Prolonged bleeding time (stop 2 weeks before surgery)

17
Q

Ibuprofen

A

Competitive, reversible COX-1 & 2 inhibitor
Use: mild to moderate pain, antipyretic, symptoms of rheumatoid and osteoarthritis, dysmenorrhea, acute migraines
Drug Interax: decrease effectiveness of ACE inhibitors

18
Q

Naproxen

A

Competitive, reversible COX-1 & 2 Inhibitor
Better anti-inflammatory than Ibuprofen
Use: mild to moderate pain, antipyretic, symptoms of rheumatoid and osteoarthritis, dysmenorrhea, ankylosing spondylitis, acute gout
Adverse: Increased risk of stroke/MI with extended use
Drug interax: decrease effectiveness of ACE inhibitors, antacids and sucralfate (divalent cations) decrease naproxen absorption

19
Q

Ketorolac (Topical)

A

Opthalmic prep.

Allergic conjunctivitis or recovery from cataract surgery

20
Q

Ketorolac

A

Analgesic (comparable to morphine)
Use: Post operative pain (Moderate to severe)
IM, IV, and Oral admin. options
Inhibits platelet aggregation
Adverse: GI bleeding, Gen. bleeding, Hepatic,
Lower dose in elderly or

21
Q

Diclofenac

A

Analgesic
Use: rheumatoid/osteoarthritis, ankylosing spondylitis, primary dymenorrhea
Opthalmic prep for post cataract surgery
Arthrotec: Diclofenac+Misoprostol - used when risk of ulcers; contraindicated in pregnancy
Zorvolex: low dose diclofenac (mild to moderate acute pain);
Adverse: elevation of AST (monitor transaminases first 8 weeks)
Metabolized by CYP2C9

22
Q

Indomethacin

A

Oral: Acute gouty/rhematoid/osteo-arthritis, tendonitis, ankylosing spondylitis,
IV: nonsurgical closure PDA (limited by renal toxicity)
Adverse: GI pain (take w/ food), displace bilirubin from albumin, decreased urine output
Contraindicated: hyperbilirubinemia, renal failure

23
Q

Celecoxib

A

Selective COX-2 inhibitor
Rheumatoid and osteoarthritis
Adverse: Low incidence GI pain, increased risk stroke/MI
Drug interax: metabolized by CYP2C9, watch dose w/ 2C9 inhibitors (Fluconazole)

24
Q

Selecting NSAID

A

Same mechanism, different potency
Aspirin sensitivity cross to other NSAIDs
GI ulcers
Pregnancy - bleeding, premature closure ductus arteriosus, inhibit uterine motility
DO NOT COMBINE NSAIDs
Renal function

25
Q

prostaglandins & kidney

A

PGE & PGI effects: increase renin release; vasodialation increases GFR; decrease effect of ADH
Loop Diuretics increase COX activity to increase sodium and water excretion (NSAIDs reduce this)
Hyperkalemia in patients w/ reduced renal function, worse in combo w/ certain drugs (propranolol, potassium sparing diuretics, ACE inhibitors

26
Q

Acetaminophen

A

Alternative for aspirin sensitivity (not NSAID)
Antipyretic, analgesic, weak anti-inflammatory
Does not alter platelet function, less GI issue
Mx: COX-1 & 2 inhibitor; COX-3 inhibitor?; activate cannabinoid receptor?
Adverse: Hepatic and renal toxic
#1 cause acute hepatic failure in US
Drug interax: Alcohol

27
Q

Auranofin

A

Gold based drug
Mx: Inhibition of function and maturation of T cells, less rheumatoid factor, inhibit phagocytosis by macrophages
Use: rheumatoid arthritis not responding to NSAIDs
Adverse: lesions of the mucus membranes, Chrysiasis, protienuria, glomerulonephritis

28
Q

Gold Sodium Thiomalate

A

Mx: Inhibition of function and maturation of T cells, less rheumatoid factor, inhibit phagocytosis by macrophages
Use: rheumatoid arthritis not responding to NSAIDs
Adverse: lesions of the mucus membranes, Chrysiasis, protienuria, glomerulonephritis, thrombocytopenia, anemia, anaphylaxis
Contraindicated in renal disease, lupus, gold sensitivity

POD (7 decks)

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