2- NSAIDS Flashcards

1
Q

Which mediators of acute inflammation have the greatest vasodilatory effects?

A

Bradykinin, prostaglandins

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2
Q

Which mediators of acute inflammation have the greatest vascular permeability effects?

A

Histamine, leukotrienes

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3
Q

Which mediators of acute inflammation have the greatest chemotaxis effects?

A

Prostaglandins, leukotrienes

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4
Q

Which mediator of acute inflammation has the greatest pain effects?

A

Bradykinin

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5
Q

The following is the MOA for what drug?

Nonselective, irreversible inhibitor of COX-1 and COX-2

A

Aspirin

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6
Q

How does aspirin cross the placental barrier and blood-brain barrier?

A

Readily crosses placental barrier

Slowly crosses BBB

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7
Q

What drug competes with thyroxin T3, PenG, thiopental, bilirubin, phenytoin, sulfinpyrazone, and naproxen for protein plasma binding sites, causing drug interactions?

A

Aspirin

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8
Q

How is aspirin metabolized at low and high doses?

A

Low- 1st order kinetics

High- zero order kinetics

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9
Q

How is aspirin excreted?

A

Renally (alkalinization of the urine)

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10
Q

What are the uses for acetylsalicylic acid?

A

Analgetic, antipyretic, antiinflammatory, antiplatelet

ONLY irreversible (used for long-term effects, prevention of MI/ stroke)

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11
Q

What are the uses of NSAIDs?

A

Analgetic, antipyretic, antiinflammatory

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12
Q

What are the uses of acetaminophen?

A

Analgetic, antipyretic

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13
Q

Adverse effects of aspirin?

A

Respiratory alkalosis, GI effects, aspirin asthma (lungs), kidney damage

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14
Q

A single dose of 650mg of aspirin has what effect on bleeding time?

A

Doubles it

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15
Q

Pt with hypothrombinemia, vit K def, hemophilia, gastric ulcer or severe hepatic damage should avoid taking what drug?

A

Aspirin

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16
Q

In what circumstances should aspirin be avoided?

A

Prior to labor (3 mos), 1 week before elective surgery

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17
Q

What drug competes for excretion of uric acid (at low doses) and in what population should it be avoided?

A

Aspirin, pts with gout

(high doses enhances excretion but poorly tolerated- GI effects)

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18
Q

What is the DOC for analgesic and antipyretic effects in children?

A

Acetaminophen

(lower risk of Reye’s syndrome)

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19
Q

What is the fatal dose for aspirin or methyl salicylate (oil of Wintergreen)?

A

Aspirin ~ 20g

Methyl salicylate (oil of Wintergreen) ~ 4-5mL (children)

20
Q

Magnesium choline salicylate, sodium salicylate, and salicyl salicylate are all what drug class?

A

Nonacetylated salicylates

Anti-inflammatory drugs, NO irreversible COX inhibition

21
Q

What drugs are used for removal of warts, corns, fungal infections and eczematous dermatitis and have analgesic, antipyretic, and anti-inflammatory effects?

A

Nonacetylated salicylates

(magnesium choline salicylate, sodium salicylate, and salicyl salicylate)

22
Q

What drug is a salicylic acid derivative but NOT metabolized to salicylic acid (not a pro-drug) and does not have significant antipyretic effects (poor CNS penetration)?

A

Diflunisal

23
Q

What drug is a selective, reversible COX-2 inhibitor and has the potential to cause less gastropathy and risk of GI bleeding (due to no inhibitory effect on platelet aggregation)?

A

Celecoxib

(Valdecoxib, Rofecoxib)

24
Q

Aside from GI effects, what is the adverse effect a/w Celecoxib?

A

Increased risk of CV disease

25
Q

What are the contraindications for Celecoxib?

(selective, reversible COX-2 inhibitor)

A

GI disease, asthma, breast feeding/ pregnancy, renal failure

26
Q

What is the first choice NSAID that is a nonspecific reversible inhibitor of COX-1 and COX-2 and is used in combo with ASA to decrease the effect on platelet aggregation?

A

Ibuprofen (fewest SEs)

27
Q

What are the most potent NSAIDs that are nonspecific reversible inhibitors of COX-1 and COX-2?

A

Indomethacin, phenylbutazone

(serious SEs- GI, BM)

28
Q

What AI AR agent is used to tx patent ductus arteriosus and reduce PMN migration via inhibition of phospholipase A?

(AI AR = anti-inflammatory, anti-rheumatic)

A

Indomethacin

29
Q

What potent COX inhibitor is used in combination with misoprostol to decrease GI side effects?

A

Diclofenac

30
Q

What drug should be used as an analgesic in postsurgical pain and may be combined with opiates?

A

Ketorolac

(> 5 days of use = GI effects)

31
Q

How is ibuprofen excreted?

A

Renally

(overall toxicity is low, GI effects)

32
Q

What NSAID should be used for once a day dosing due to half life ~ 13 hours?

A

Naproxen

33
Q

What NSAID is largely excreted in the urine, is c/i’d in pregnancy and causes adverse drug reactions with oral anticoagulants and hypoglycemic agents?

A

Naproxen

(toxicity = GERD-like, mild GI bleed)

34
Q

What NSAIDS inhibit PMN migration and lymphocyte function, decrease oxygen radical production, and have a long half life with high incidence of GI SEs?

A

Piroxicam, Meloxicam

35
Q

Acetaminophen overdose (dose dependent, ~25g) can lead to what fatal SE?

A

Fatal hepatic necrosis

(encephalopathy/ coma > death)

36
Q

What drug is preferred over aspirin due to absence of SEs such as PUD, inhibition of clotting, acid-base imbalance, and auditory toxicity?

A

Acetaminophen

37
Q

What drug has dose dependent free radical production with antipyretic and analgesic action but NO anti-inflammatory action and NO platelet effects?

A

Acetaminophen

38
Q

What NSAID can be combined with codeine, sedatives, cough suppressants, tramadol, diphenhydramine, and caffeine?

A

Ibuprofen

39
Q

Ibuprofen has the potential to cause cross-sensitivity with what drugs?

A

Salicylates

40
Q

What drug toxicity is a result of circulating toxic metabolites exceeding the available reduced glutathione in the body (no longer able to neutralize) and what increases this toxicity?

A

Acetaminophen

Chronic alcohol consumption increases toxicity

41
Q

Pt presents with acetaminophen intoxication should be tx with what?

A

N-acetylcysteine (specific antidote, administered parenterally asap, w/i 10-12 hrs after intoxication)

42
Q

If pt has NO hx of PUD, are there any restictions with type of NSAID given?

A

No

43
Q

Pt has hx of PUD but it is NOT currently active. What is the tx?

A

Celecoxib +/- antacids

(some NSAIDs w/ misoprostol or “prazols”)

44
Q

Pt with active PUD should be given what analgesic?

A

Acetaminophen and/ or opioids (codeine) only

45
Q

How do antacids affect aspirin absorption?

A

Decrease absorption