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Block 2 Drugs > NSAID Drugs > Flashcards

NSAID Drugs Flashcards

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

A

Indomethacin

24
Q

NSAID Not routinely used to treat pain and fever

A

Indomethacin

25
Q

Side effects of Indomethacin

A

GI discomfort, increased risk of bleeding, hypersensitivity/allergic response, possible renal effects. + Severe frontal headache

26
Q

Half life of indomethacin

A

3 hours

27
Q

Uses of Ketorolac

A

Short-term (less than or equal to 5 days) management of moderate-to-severe acute pain requiring analgesia at the opioid level

28
Q

Side effects of Ketorolac

A

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

29
Q

Which NSAID has less of an anti-inflammatory effect and is used at an opiod levle

A

Ketorolac

30
Q

Mode of delivery for ketorolac

A

injection or IV

31
Q

Which NSAID is used for osteoarthristic and RA which less side effects

A

Nabumetobe

32
Q

Uses of Nabumetone

A

well tolerated NSAID for osteoarthritis and RA

-reversible COX 1 and 2 inhibitor

33
Q

This reversible COX1 and COX2 NSAID is a PRODRUG and has a long 1/2 life

A

Nabumetone

34
Q

Uses of Piroxicam

A

Symptomatic treatment of acute and chronic rheumatoid arthritis and osteoarthritis; may offer advantage in treatment of osteoarthritis because of long half-life

35
Q

This NSAID has a 1/2 life of 50 hours

A

Piroxicam

36
Q

Side effects of Piroxicam

A

GI toxicitiy

37
Q

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

A

Piroxicam

38
Q

Uses of Sulfasalazine

A

Mild or moderately active ulcerative colitis; rheumatoid arthritis and ankylosing spondylitis

39
Q

Method of Sulfasalazine

A

unknown~ not a COX 1 or 2 inhibitor

40
Q

Side effects of Sulfasalazine

A

headache, nausea, fatigue, decreased sperm motility, inhibits folate absorption

41
Q

This NSAID has side effects including: decreased sperm motility, inhibits folate absorption, headache, nausea, fatigue,

A

Sulfasalazine

42
Q

NSAID used to treat ulcerative colitis, RA and ankylosing spondylitis

A

Sulfasalazine

43
Q

Effect of Sulfasalazine

A

Local effect in GI: inhibit inflammatory response

44
Q

Sulfasalazine is contraindicated in patients with

A

a sulfa allergy

45
Q

This NSAID is a reversible inhibitor of COX 2 only

A

Celecoxib

46
Q

Uses of Celecoxib

A

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
Q

NSAID used to reduce number of intestinal polyps in familial adenomatous polyposis

A

Celecoxib

48
Q

Side effects of Celecoxib

A

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

49
Q

Contraindications of Celecoxib

A

Sulfa allergy, prior NSAID hypersensitivity, CV disease, GI bleeding, after coronary artery surgery, deficient CYP2C9

50
Q

If you have deficiency of CYP2C9 you should not use

A

Celecoxib

51
Q

NSAID that contains a sulfonamide side chain (causes allergic reactions). Metabolized by CYP2C9.

A

Celecoxib

52
Q

Administration of Celecoxib and peak activity

A

oral

after 3 hours = peak activity

53
Q

Uses of Acetominophen

A

Acute pain, fever (NO anti-inflammatory effects)

54
Q

This NSAID has no anti- inflammatory properties

A

acetominophen

55
Q

What toxicity issues do we run into with Acetominophen

A

Hepatic toxicity: CYP2E1 -> NAPQI. (very little GI issues)

56
Q

What is the mode of delivery and peak time for acetominophen

A

30-60 mins and oral delivery

57
Q

What do we use for tx for acetominophen overdose

A

N-acetylcysteine replenishes glutathione stores (Tment for overdose)

Block 2 Drugs (10 decks)

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