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NSAID Drugs Flashcards

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1
Q

Irreversible* inhibitor of COX 1 and 2

A

Acetylsalicylic acid/Aspirin

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2
Q

Aspirin/Acetylsalicylic acid effect on:
Platelets
Endothelial Cells

A

Lifetime inhibition of COX in platelets

Endothelial cells can re-synthesize new COX enZ

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3
Q

What group on COX does aspirin/acetylsalicyclic acid act on?

A

Aceylates the serine group on COX.

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4
Q

In LOW doses of aspirin, what unique effect do we see?

A

uric acid secretion (low doses = incr in serum uric acid [decr. excretion]

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5
Q

In HIGH doses of aspirin what unique effect do we see?

A

high doses = decr. serum uric acid [an URICOSURIC agent])

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6
Q

Aspirin does/does not cross the BBB

A

Does cross the BBB

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7
Q

Aspirin use;
Low dose for:
Intermediate dose for:
High dose:

A 
Low dose: CV disease.  
Intermediate dose (typical OTC): low intensity pain/fever.   
High dose: chronic inflammatory disease, rheumatoid arthritis
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8
Q

What side effects do we see with aspirin?

A

CNS (high doses): stimulation followed by depression, tinnitus, high-tone deafness, confusion, dizziness, delirium, psychosis, coma, nausea, vomiting

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9
Q

Aspirin (acetylsalicyclic acid) has a ______ half life (15 mins) and is hydrolyzed to ________.

A

short

salicyclic acid

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10
Q

Salicyclic acid is a ________ COX inhibitor (half life 2-3 hrs)

A

weak/reverisble

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11
Q

Ibuprofen acts on what?

A

reversible COX 1 and 2 inhibitor

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12
Q

Ibuprofen is used to tx which 2 diseases states?

A

Inflammatory disease and rheumatoid disorders including juvenile rheumatoid arthrisits, mild-to-moderate pain;

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13
Q

Why is ibuprofen used in premature infmants?

A

Injection to induce closure of a clinically-significant patent ductus arteriosus in premature infants

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14
Q

4 side effects of ibuprofen

A

GI discomfort, increased risk of bleeding, hypersensitivity/allergic response, possible renal effects

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15
Q

What is the 1/2 life of ibuprofen

A

2 hours

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16
Q

This drug is used in premature infmants to induce closure of clinically significant patent ductus arteriosus

A

Ibuprofen

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17
Q

Management of ankylosing spondylitis, osteoarthritis, and rheumatoid disorders (including juvenile rheumatoid arthritis); acute gout; mild-to-moderate pain; tendonitis, bursitis; dysmenorrhea; fever

A

Naproxen

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18
Q

Naproxen is used to tx which disorders…

which type of pain…

A

manage ankylosing spondylitis, osteoarthritis, RA (including juvenile RA) and acute gout
mild-to-moderate pain, tendonitis, bursitis, dysmenorrhea, fever

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19
Q

Side effects of Naproxen

A

GI discomfort, increased risk of bleeding, hypersensitivity/allergic response, possible renal effects

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20
Q

1/2 life of Naproxen

A

14 hours

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21
Q

Indomethacin works on which enZs

A

Reversible inhibitor of COX 1 and 2

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22
Q

Indomethacin

A

Acute gouty arthritis, acute bursitis/tendonitis, moderate-to-severe osteoarthritis, rheumatoid arthritis, ankylosing spondylitis; I.V. form used as alternative to surgery for closure of patent ductus arteriosus in neonates. Not routinely used to treat pain and fever

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23
Q

I.V. form used as alternative to surgery for closure of patent ductus arteriosus in neonates. Not routinely used to treat pain and fever

24
Q

NSAID Not routinely used to treat pain and fever

25
Side effects of Indomethacin
GI discomfort, increased risk of bleeding, hypersensitivity/allergic response, possible renal effects. + Severe frontal headache
26
Half life of indomethacin
3 hours
27
Uses of Ketorolac
Short-term (less than or equal to 5 days) management of moderate-to-severe acute pain requiring analgesia at the opioid level
28
Side effects of Ketorolac
GI discomfort, increased risk of bleeding, hypersensitivity/allergic response, possible renal effects.
29
Which NSAID has less of an anti-inflammatory effect and is used at an opiod levle
Ketorolac
30
Mode of delivery for ketorolac
injection or IV
31
Which NSAID is used for osteoarthristic and RA which less side effects
Nabumetobe
32
Uses of Nabumetone
well tolerated NSAID for osteoarthritis and RA | -reversible COX 1 and 2 inhibitor
33
This reversible COX1 and COX2 NSAID is a PRODRUG and has a long 1/2 life
Nabumetone
34
Uses of Piroxicam
Symptomatic treatment of acute and chronic rheumatoid arthritis and osteoarthritis; may offer advantage in treatment of osteoarthritis because of long half-life
35
This NSAID has a 1/2 life of 50 hours
Piroxicam
36
Side effects of Piroxicam
GI toxicitiy
37
This NSAID is great for symptomatic tx of acute or chronic RA and osteroarthrisis... may even be better for osteoarthritis d/t its long half life
Piroxicam
38
Uses of Sulfasalazine
Mild or moderately active ulcerative colitis; rheumatoid arthritis and ankylosing spondylitis
39
Method of Sulfasalazine
unknown~ not a COX 1 or 2 inhibitor
40
Side effects of Sulfasalazine
headache, nausea, fatigue, decreased sperm motility, inhibits folate absorption
41
This NSAID has side effects including: decreased sperm motility, inhibits folate absorption, headache, nausea, fatigue,
Sulfasalazine
42
NSAID used to treat ulcerative colitis, RA and ankylosing spondylitis
Sulfasalazine
43
Effect of Sulfasalazine
Local effect in GI: inhibit inflammatory response
44
Sulfasalazine is contraindicated in patients with
a sulfa allergy
45
This NSAID is a reversible inhibitor of COX 2 only
Celecoxib
46
Uses of Celecoxib
Signs/symptoms of rheumatoid arthritis and osteoarthritis; treatment of primary dysmenorrheal; management of acute pain; to reduce number of intestinal polyps in familial adenomatous polyposis
47
NSAID used to reduce number of intestinal polyps in familial adenomatous polyposis
Celecoxib
48
Side effects of Celecoxib
GI discomfort, increased risk of bleeding, hypersensitivity/allergic response, possible renal effects
49
Contraindications of Celecoxib
Sulfa allergy, prior NSAID hypersensitivity, CV disease, GI bleeding, after coronary artery surgery, deficient CYP2C9
50
If you have deficiency of CYP2C9 you should not use
Celecoxib
51
NSAID that contains a sulfonamide side chain (causes allergic reactions). Metabolized by CYP2C9.
Celecoxib
52
Administration of Celecoxib and peak activity
oral | after 3 hours = peak activity
53
Uses of Acetominophen
Acute pain, fever (NO anti-inflammatory effects)
54
This NSAID has no anti- inflammatory properties
acetominophen
55
What toxicity issues do we run into with Acetominophen
Hepatic toxicity: CYP2E1 -> NAPQI. (very little GI issues)
56
What is the mode of delivery and peak time for acetominophen
30-60 mins and oral delivery
57
What do we use for tx for acetominophen overdose
N-acetylcysteine replenishes glutathione stores (Tment for overdose)

Block 2 Drugs (10 decks)

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