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POD III > Antipyretics, NSAIDs > Flashcards

Antipyretics, NSAIDs Flashcards

1
Q

Eicosanoids consist of what 3 things?

A
  1. Prostaglandins
  2. Thromboxanes
  3. Leukotrienes
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2
Q

Whats the most abundant eiconsanoids fatty acids?

A

Arachidonic acid

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3
Q

What is the name of the enzyme complex that converts arachidonic acid to prostaglandin?

A

Prostaglandin G/H synthetase

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4
Q

What is the mechanism of action of prostaglandins?

A
  1. Act locally - paracrine/autocrine
  2. Interact with GPCRs
  3. Increase/decrease adenylate cyclase
  4. Major effects on smooth muscle, other effects on platelets, kidney, CNS, endocrine organs and eye
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5
Q

What are the physiological actions of prostacyclin (PGI2)?

A
  • Circulation: Vasodilator and inhibits platelet aggregation
  • Airways: bronchodilator
  • GI: inhibits gastric acid secretion; increase mucus secretion
  • Renal: enhances renal excretion of sodium and water
  • Reproductive: relaxes uterine muscle
  • Pain: induces pain by lowering the threshold of nociceptors
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6
Q

What are the physiological actions of prostaglandin (PGE2)?

A
  • Circulation: Vasodilator; low conc. enhances and high conc. inhibits aggregation
  • Airways: bronchodilator
  • GI: inhibits gastric acid secretion; increase mucus secretion
  • Renal: enhances renal excretion of sodium and water
  • Reproductive: uterine smooth muscle contraction
  • Fever and inflammation: direct pyrogen in hypothalamus
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7
Q

What are the physiological actions of Thromboxane (TXA2)?

A
  • Vascular: vasoconstriction

- Stimulates platelet aggregation (major product of platelet COX1)

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8
Q

What are the physiological actions of PGF2alpha?

A
  • Vascular: Vasoconstrictor
  • Airway: contracts smooth muscle
  • Reproductive: contracts smooth muscle
  • Eye: decreases intraocular pressure.
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9
Q

Misoprostol (cytotec)

A
  • PGE1 analogue
  • Inhibits gastric acid secretion, reduces risk of peptic ulcer in pts taking NSAID
  • Contra: Pregnancy
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10
Q

Latanoprost (Xalatan)

A
  • PGF2alpha analogue
  • Tx: open angle glaucoma
  • Increases uveoscleral outflow which lowers intraocular pressure.
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11
Q

Alprostadil (Prostin) PGE1

A
  • Used to maintaing patency of ductus arteriosus during sx.
  • Vasodilator
  • Erectile disfunction
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12
Q

What is required to convert LTA4 to LTC4?

A

Glutathione

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13
Q

5-HETE

LTB4

A

-Chemotactic agents

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14
Q

LTC4
LTD4
LTE4

A
  • Bronchoconstrictor
  • Increase vascular permeability
  • Components of slow reacting substance of anaphylaxis (SRS-A)
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15
Q

Zafirlukast (Accolate)

Montelukast (Singulair)

A
  • Competitive LTD4 receptor antagonist
  • Prophylactic tx of asthma in adults
  • Allergic rhinitis
  • Aspirin sensitivity induced asthma (montelukast)
  • S/Es: Headache, pharyngitis
  • Inhibits Cyp 2C9, Cyp 3A4 (warfarin)
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16
Q

Zileuton (Zyflo)

A
  • Inhibitor of 5-lipoxygenase (all leukotriens)
  • Porphylaxis for asthma in adults (12 yr and older)
  • Elevated liver enzymes, must monitor ALT
  • Contra: liver disease, combination with ergot alkaloids
17
Q

What is the mechanism of action for NSAIDs?

A

Inhibition of cyclo-oxygenase

18
Q

Aspirin

A
  • Irreversible cyclo-oxygenase inhibitor
  • Analgesic, antipyretic, anti-inflammatory
  • Rheumatoid and osteoarthritis
  • Contra: Viral infection due to risk of Reyes syndrome in children
19
Q

Ibuprofen

A
  • Reversible inhibition of Cox 1 and 2
  • Antipyretic, can be used in children
  • Primary dysmenorrhea, migraine, rheumatoid/osteoarthritis
20
Q

Naproxen

A
  • Reversible inhibition of Cox 1 and 2
  • Antipyretic, can be used in children
  • Primary dysmenorrhea, migraine, rheumatoid/osteoarthritis
  • Acute gout
21
Q

Ketorolac

A
  • Ophthalmic: allergy, cataract removal
  • IV, IM, PO
  • Greater analgesic activity than anti-inflammatory
  • S/Es: Bleeding, Hepatic
  • Must stop prior to surgery
22
Q

Diclofenac

A
  • Rheumatoid, osteoarthritis, ankylosing spondylitis
  • Ophthalmic: pain, cataract sx
  • Primary dysmenorrhea
  • Arthotec contra during pregnancy
23
Q

Indomethacin

A
  • Oral: Rheumatoid/osteoarthritis, ankylosing spondylitis, gout, tendinitis
  • IV: Closure of patent ductus arteriosus
  • Take w/ food
  • Must monitor urinary output
24
Q

Celecoxib

A
  • Selective COX-2 competitive reversible inhibitor

- Increased risk of cardiovasular and stroke event with high dose for prolonged time.

25
Q

Acetaminophen

A
  • Antipyretic and analgesic
  • Hepatotoxicity, renal toxicity w/ chronic use
  • COX-3 inhibition

POD III (12 decks)

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