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Year 2 > NSAIDs and Related Drugs > Flashcards

NSAIDs and Related Drugs Flashcards

1
Q

What is the mechanism of action of aspirin?

A

Acetylation of cyclooxygenase.

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2
Q

What is the ceiling dose for aspirin?

A

650mg

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3
Q

What is overdose of aspirin called and what are its effects?

A

Salicyism. Effects are tinnitus, decreased hearing, headache, and vertigo.

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4
Q

What is the therapy for overdose of aspirin?

A

Sodium bicarbonate infusion and gastric lavage.

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5
Q

What are the side effects of aspirin?

A

Irritates gastric mucosa; inhibits platelet aggregation; hypersensitive reactions.

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6
Q

What is a contraindication of aspirin?

A

Allergy; Hemophilia; Children with Influenza (Reye’s Syndrome)

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7
Q

Why does aspirin irritate gastric mucosa?

A

It inhibits PG synthesis and removes protective PGs.

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8
Q

How can aspirin reduce gastric intolerance?

A

By buffering to increase stomach pH.

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9
Q

What is the use of enteric coated aspirin (Ecotrin)?

A

Used in patients in whom buffering fails to control gastritis.

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10
Q

What are examples of non-acetylacted salicylates?

A

Methyl salicylate (Oil of Wintergreen); Diflunisal; Magnesium Choline Salicylate; Sodium Salicylate; Salicylsalicylate.

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11
Q

When are non-acetyl salicylates preferred?

A

When cyclooxygenase inhibition is undesirable. As in patients with asthma, bleeding tendencies, and renal dysfunction.

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12
Q

What is the preferred drug for patients allergic to aspirin?

A

Acetaminophen.

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13
Q

True or false: Acetaminophen is a strong prostaglandin inhibitor in peripheral tissues.

A

False. It is a WEAK PG inhibitor.

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14
Q

What is the mechanism of action of acetominophen?

A

Unknown!

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15
Q

What are the therapeutic actions of acetaminophen?

A

It is an analgesic and antipyretic.

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16
Q

Is acetaminophen an anti-inflammatory?

A

No. It also does not have anti platelet activity.

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17
Q

What is the ceiling dose of acetaminophen?

A

650 to 1000mg.

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18
Q

What can 6 grams of acetaminophen do to the liver?

A

Damage the liver due to formation of N-acetyl-p-benzoquinone metabolite.

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19
Q

What is the antidote to acetaminophen toxicity?

A

Gastric lavage and N-acetylcysteine.

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20
Q

What are the side effects of acetaminophen?

A

Increase in hepatic enzymes; skin rash/ allergic reaction.

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21
Q

Ingestion of 15g of acetaminophen will case what?

A

Can be fatal. Severe hepatoxicity with centrilobular necrosis; acute renal tubular necrosis.

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22
Q

Why are NSAIDs inflammatory?

A

The decrease concentration PG (PGE2, PGI2). PGs are vasodilators, thus their absence causes decreased edema.

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23
Q

Is the accumulation of inflammatory cells significantly reduced by NSAIDs?

A

No.

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24
Q

Why are NSAIDs analgesic?

A

Decreased PG results in less sensitization of nociceptive nerve endings to mediators, such as bradykinin and 5-HT.

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25
Q

Why are NSAIDs antipyretic?

A

Centrally mediated; Partly the result of a decrease in PG response to cytokines (IL-1).

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26
Q

Why are NSAIDs anti platelet?

A

They induce reversible inhibition of thromboxane. Except for aspirin which is irreversible.

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27
Q

What are the side effects of NSAIDs?

A

GI ulceration and renal injury. GI ulceration possibly due to inhibition of CO.

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28
Q

Indomethacin (NSAID)

A

Used in gout. More toxic than aspirin.

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29
Q

Ibuprofen (NSAID)

A

Fewer side effects than aspirin.

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30
Q

Naproxen (NSAID)

A

Half life of 13 hours.

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31
Q

Piroxicam (NSAID)

A

Long acting; half life of 45 hours.

32
Q

Diclofenac (NSAID)

A

Well tolerated; enteric coated.

33
Q

Flurbiprofen (NSAID)

A

Ocular use.

34
Q

Ketorolac (NSAID)

A

Not used in most cases. Reserved for patients, postoperatively, who cannot take opioids.

35
Q

Which 2 NSAIDs are used in acute attacks of flare-ups?

A

Sulindac and Phenylbutaxone.

36
Q

Sulindac

A

500x more potent than indomethacin. It is a prodrug sulfoxide. Enterohepatic cycling occur.

37
Q

Phenylbutoxone

A

For RA. Side effects include agranulocytosis and aplastic anemia.

38
Q

What are the two COX-2 inhibitors?

A

Celecoxib and Rofecoxib.

39
Q

Celecoxib

A

Highly selective COX-2 inhibitor; Treatment of RA

40
Q

True or false: Celecoxib has been shown to cause fewer endoscopic ulcers than most other NSAIDs.

A

True.

41
Q

What are the effects of Celecoxib on platelet aggregation?

A

None.

42
Q

Rofecoxib

A

Potent, highly selective COX-2 inhibitor.

43
Q

What is Rofecoxib approved for?

A

Osteoarthritis and RA; Acute pain in adults; treatment of primary dysmenorrhea

44
Q

What are the effects of Rofecoxib on platelet aggregation?

A

None

45
Q

What are the effects of Rofecoxib on gastric mucosal prostaglandins?

A

Appears to have little affect on gastric mucosal prostaglandins.

46
Q

What are DMARDs?

A

Disease Modifying Antirheumatic Drugs. Can alter the course of rheumatic disorders.

47
Q

Aurothiomalate

A

A gold salt used in chrysotherapy; possibly suppresses the immune system; used for active RA.

48
Q

How is aurothiomalate administered?

A

IM as a water soluble gold salt (50% gold).

49
Q

Auranofin

A

A gold salt used in chrysotherapy; possibly suppresses the immune system; used for active RA.

50
Q

How is auranofin administered?

A

As a substituted gold thioglucose derivative (29% gold). Administered P.O.

51
Q

What are the contraindication of gold salts?

A

History of previous toxicity to gold, pregnancy, impaired living or renal function, blood dyscrasias.

52
Q

What is hydroxychloroquine?

A

An antimalarial.

53
Q

When should hydroxychloroquine be used and how long does it take to get maximal effects?

A

Used when other measures have failed. More popular than Chloroquine. Takes several weeks of treatment for maximal effects.

54
Q

What are antimalarials usually taken alongside with?

A

NSAIDs

55
Q

What is a major toxicity of Hydroxychloroquine?

A

Ocular toxicity. Deposition of the drug in the cornea causing blurring of vision. Can be irreversible.

56
Q

In what case can Hydroxychloroquine make the rheumatoid state worse?

A

In the presence of psoriasis. Can cause Psoriatic Rheumatoid Syndrome and exacerbate the psoriasis.

57
Q

What is used in the treatment of heave metal poisoning?

A

Penicillamine

58
Q

What are the toxic effects of penicillamine?

A

Skin changes (mild); decrease in B6 after prolonged use; bone marrow depression; proteinuria; autoimmune syndromes.

59
Q

How long must Penicillamine be used to obtain maximum effect?

A

14-16 weeks.

60
Q

Which patients should penicillamine be reserved for?

A

Those not responding to gold.

61
Q

What is the use of glucocorticoids?

A

Short term use to inhibit COX-2 induction? It is a relatively non-specific inhibitor of protein synthesis.

62
Q

Methotrexate, Azathioprine, and cyclophosphamide are what kind of drugs?

A

Immunosuppressives.

63
Q

How does methotrexate work?

A

It is an inhibitor of dehydrofolate reductase. It is a potent immunosuppressive drug.

64
Q

What is the maximum weekly dose of methotrexate?

A

7.5 mg

65
Q

What percentage of patients exhibitor hepatotoxicity from taking methotrexate?

A

40%

66
Q

What is the use for azathioprine?

A

Used in renal transplants; some cases of RA; as a chemotherapeutic agent. Results in severe myelosuppression and GI intolerance. Acts to inhibit DNA synthesis.

67
Q

Does allopurinol enhance or decrease the effects of azathioprine, and why?

A

Enhance, because azathioprine is metabolized by xanthine oxidase.

68
Q

What type of agent is Cyclophosphamide?

A

An alkylating agent.

69
Q

What is the use for Cyclophosphamide?

A

It destroys proliferating lymphoid cells. Used in severe, unresponsive RA.

70
Q

What percentage of patients exhibit side effects from Cyclophosphamide, and what are they?

A

90%. GI and bone marrow toxicity.

71
Q

What kind of drugs are Infliximab and Etanercept?

A

Anti-TNF alpha.

72
Q

How does Infliximab work?

A

It is an antibody that binds with high affinity and specificity to human TNF alpha.

73
Q

Infliximab has been approved for use only in conjunction with another drug. Which one?

A

Methotrexate.

74
Q

What are the side effects of Infliximab?

A

Upper respiratory tract infection; Nausea, headaches, sinusitis, rash, cough.

75
Q

How does Etanercept work?

A

It is a protein that binds to two TNF alpha molecules.

76
Q

Can Etanercept be used alone/

A

Yes. It is the first TNF inhibitor that can be used alone.

77
Q

What are the side effects of Etanercept?

A

Erythema, local pain, swelling, itching at the site of injection.

Year 2 (9 decks)

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