07- NSAIDS Flashcards

1
Q

analgesic

A

is any member of the group of drugs used to achieve analgesia, or relief from pain (painkiller)
-accomplished by NSAIDs through reduction of PGE2 and PGI2 induced hyperalgesia and general reduced inflammation (not effective against non-inflammatory pain

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2
Q

anti-platelet

A

drugs that decrease platelet aggregation and inhibit thrombus formation
-NSAIDs inhibit platelet COX-1 (no COX-2)

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3
Q

antipyretic

A

are substances that reduce fever

-antipyretics cause the hypothalamus to override an PGE2-induced increase in temperature

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4
Q

gastric effects

A

histamine activation of H2 receptors in mucosal lining of stomach leads to increased acid production, pepsin, and intrinsic factor
-leads to mucosal erosion and ulceration

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5
Q

arachidonic acid

A

the substrate for production of lipid mediators of inflammation (prostaglandins produced by cyclooxygenase, or leukotrienes produced by lipoxygenase)

  • cyclooxygenase inhibited by NSAIDS
  • lipoxygenase inhibited by Zileuton (Zyflo)
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6
Q

cyclooxygenase (COX)

A

produces prostaglandins which are lipid mediators of inflammation
-inhibited by NSAIDS

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7
Q

dyspepsia

A

indigestion, upper abdominal pain, bloating, nausea

-common symptom of chronic NSAID use

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8
Q

eicosanoids

A

prostanoid and leukotriene derivatives of C-20 fatty acids

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9
Q

Fc Domain

A

area of an antibody protein that does not change

-this area does not bind to antigen (variable region is specific for and binds antigens)

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10
Q

humanized antibody

A

also know as chimeric antibody

  • graft ligand binding domain from animals onto backbone of fully human antibody
  • has same function as a fully human antibody with out resistance produced from animal antibodies
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11
Q

leukocytes

A

cell that circulates in the blood and body fluids and is involved in counteracting foreign substances and disease; a white (blood) cell
-several types including lymphocytes, granulocytes, monocytes, and macrophage

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12
Q

mast cells

A

a cell filled with basophil granules, found in numbers in connective tissue and releasing histamine and other substances during inflammatory and allergic reactions
-most dense in tissue with higher chance of injury such as mouth, nose, hands/feet, blood vessels, GI mucosa

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13
Q

motion sickness

A

triggered by histamine activation of H1 receptors in the emetic center of the CNS

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14
Q

phospholipase A2 (PLA2)

A

hydrolyzes phosphatidylcholine in plasma membrane to release free arachidonic acid (AA)

  • eventually leads to production of lipid mediators by AA
  • activity inhibited by annexins (aka lipocortins) (annexin expression increased by glucocorticosteroids)
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15
Q

phospholipase C (PLC)

A

activates signaling pathways that increase Ca+2 mobilization and promote fusion of cytoplasmic vesicles with the plasma membrane and extracellular release of their contents (degranulation)

  • stored mediators (e.g., histamine) are released in response to PLC activation
  • inhibited by agents such as cromolyn (Intal) and nedocromil (Tilade)
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16
Q

prostaglandin

A

lipid compounds that play a major role in initiation and mediation of inflammatory response
-formed by cyclooxygenase and can be inhibited by NSAIDs and glucocorticosteroids

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17
Q

prostanoid

A

synthesized by cyclooxygenase

  • short half-lives and lack of stored products make activity synthesis dependent
  • membrane permeable and passively released from other cells
  • have autocrine and paracrine activity
  • can effect blood vessels, smooth muscles, platelet aggregation, pain response, and body temperature
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18
Q

Reye’s syndrome

A

associated with the use of ASA and other salicylates in children who have viral illness

  • acute encephalopathy, fatty liver degeneration
  • also associated with viral vaccines
19
Q

salicylism

A

hypersensitivity to ASA

-symptoms include: hyperventilation, tinnitus, vertigo, emesis, sweating

20
Q

triple response

A

response seen in the skin caused by histamine release

    1. WHEAL = edema (and reddening from dilation of small vessels)
    1. FLARE = axon reflex: histamine stimulation of sensory nerve terminals cause release of vasodilators at other branches
    1. ITCHING
21
Q

urticaria

A

hives which caused raised, itchy, and red skin

-triggered by histamine activation of H1 receptors on sensory nerves

22
Q

Anti-Inflammatory action of NSAIDs

A

block production of all prostanoids by inhibition of cyclooxygenase
-COX-2 primarily responsible for prostanoid production during inflammation

23
Q

Infliximab

A

anti- TNF alpha, human antibody

  • Rheumatoid arthritis
  • Crohn’s disease
    complications: increased frequency of infection (respiratory and urinary)
24
Q

Adalimumab

A

anti-TNF alpha, human antibody

  • Rheumatoid Arthritis
  • Crohn’s disease
    complications: increased frequency of infection
25
Q

Etanercept

A

anti-TNF alpha, fusion protein

  • Rheumatoid Arthritis
  • Crohn’s disease
    complications: increased frequency of infections
26
Q

Anakinra

A

competitive IL-1 receptor antagonist
- Rheumatoid Arthritis
short half-life, daily injections
complications: increased susceptibility to infections

27
Q

Tofacitinib

A

Jak Inhibitor
-Rheumatoid Arthritis (for those who fail methotrexate)
-inhibits activities for many inflammatory cytokines
small dose (5mg)
adverse effects: anemia, neutropenia, myelosuppression
increased risk of infection (herpes zoster)

28
Q

Prednisone

A

GLUCOCORTICOSTEROID
-inhibits PLA2
-inhibits production of chemotactic factors
decreased production of prostaglandsin, leukotrienes
-induces annexins (inhibits PLA2)

29
Q

Cyclizine

A

H1 Receptor Antagonist (1st generation)
Uses: allergic rhinitis and urticaria, motions sickness/emesis
adverse effects: sedation, anticholinergic effects (dry mouth, urinary retention, tachycardia)

30
Q

dimenhydrinate

A

H1 receptor antagonist (1st generation)
uses: motion sickness/ emesis
adverse effects: sedation,
anticholinergic effects (dry mouth, urinary retention, tachycardia)

31
Q

diphenhydramine

A

H1 receptor antagonist (1st generation)
uses: allergic rhinitis and urticaria, motion sickness/emesis
adverse effects: sedation, anticholinergic effects (dry mouth, urinary retention, tachycardia) blocks Na channels

32
Q

promethazine

A

H1 receptor antagonist (1st generation)
uses: antiemetic
adverse effects: sedation, anticholinergic effects (dry mouth, urinary retention, tachycardia) blocks Na channels

33
Q

loratadine

A

H1 receptor antagonist (2nd generation)
Uses:
poor CNS penetration
few anticholinergic effects

34
Q

cetirizine

A

H1 receptor antagonist (2nd generation)
uses:
poor CNS penetration
few anticholinergic effects

35
Q

fexofendadine

A

H1 receptor antagonist (2nd generation)
uses:
poor CNS penetration
few anticholinergic effects

36
Q

aspirin

A

mixed COX-1 and COX-2 inhibitor
rapidly converted to salicylic acid (reversible inhibitor)
(ASA irreversible inhibitor)
all metabolites excreted in urine
elimination saturates beyound 600 mg and 1/2 life increases to 12-16 hours
uses: fever, analgesia, muscle pain, tendonitis, bursitis (inflammation)
rheumatoid and osteoarthritis
Cardiovascular prophylaxis– reduced platelet aggregation (75-80 mg/daily)

37
Q

ketorolac

A

mixed COX-1 and COX-2 inhibitor

uses: post-surgical analgesic

38
Q

indomethacin

A

mixed COX-1 and COX-2 inhibitor
uses: Rx- arthritis/anti-inflammatory
high frequency of intolerance

39
Q

naproxen

A

mixed COX-1 and COX-2 inhibitor

Rx- anti-inflammatory

40
Q

ibuprofen

A

mixed COX-1 and COX-2 inhibitor

OTC: analgesic/antipyretic

41
Q

diclofenac

A

mixed COX-1 and COX-2 inhibitor

Rx- arthritis/anti-inflammatory

42
Q

acetaminophen

A

non-selective COX inhibitor
uses: analgesic and antipyretic
hepatotoxicity with overdose

43
Q

celecoxib

A

selective COX-2 inhibitor (10-20 times more selective for COX-2 than COX-1)
anti-inflammatory effects, antipyretic, analgesic effects, renal toxicity
mainly used for osteoarthritis and rheumatoid arthritis
expensive