NSAIDS and DMARDS Flashcards

1
Q

What are Eicosanoids produced by?

A

The actions of Phospholipase A2 on cell membranes

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2
Q

What is the clinical use of Epoprostenol?

A

Pulmonary hypertension and hemodialysis to harvest platelets

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3
Q

What is Dinoprostone used for?

A

Medical abortion and relaxing the cervix for inducing labor

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4
Q

What are the clinical uses of Misoprostol?

A

Treating peptic ulcers and medical abortion

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5
Q

What are the clinical uses of Alprostadil?

A

Opening ductus arteriosus in neonates and treating erectile dysfunction

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6
Q

What is the clinical use of Carboprost?

A

Labor induction

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7
Q

What is Latanoprost used to treat?

A

Glaucoma

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8
Q

What are the three main effects of NSAIDs?

A

Analgesic (pain-relieving), antipyretic (fever-reducing), and anti-inflammatory effects

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9
Q

What enzymes do NSAIDs inhibit?

A

Cyclooxygenase (COX) enzymes, COX-1 and COX-2

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10
Q

What are the three main categories of NSAID side effects?

A

Gastrointestinal, renal, and cardiovascular

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11
Q

What is the primary function of DMARDs in treating inflammatory arthritis?

A

Slowing down disease progression

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12
Q

What are four common side effects of DMARDs?

A

Bone marrow suppression, liver toxicity, gastrointestinal issues, and increased risk of infections

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13
Q

What is unique about Aspirin’s mechanism of action compared to other NSAIDs?

A

It irreversibly inhibits COX-1 and COX-2

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14
Q

What syndrome can Aspirin cause in children?

A

Reye’s syndrome

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15
Q

What are three examples of Propionic Acid Derivative NSAIDs?

A

Ibuprofen, naproxen, and ketoprofen

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16
Q

What type of arthritis are Oxicam Derivatives primarily used for?

A

Chronic arthritis

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17
Q

What are two examples of Indole Derivative NSAIDs?

A

Indomethacin and sulindac

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18
Q

What receptors do Fenmate NSAIDs block in addition to COX inhibition?

A

Prostaglandin receptors

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19
Q

What is an example of a Benzopyrrole NSAID?

A

Tolmetin

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20
Q

What two mechanisms are involved in the action of Phenylacetic Acid NSAIDs?

A

COX inhibition and blocking the release of Arachidonic acids

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21
Q

What is the main advantage of Selective COX-2 Inhibitors over traditional NSAIDs?

A

Lower risk of gastrointestinal side effects

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22
Q

What makes Nimesulide useful for certain patients?

A

It can be used in patients allergic to aspirin and other NSAIDs

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23
Q

How does Ketorolac compare to Indomethacin in potency?

A

It is 40 times more potent

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24
Q

What type of drug is Nabumetone?

A

A prodrug converted to its active form by the liver

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25
Q

What enzyme does Zileuton inhibit?

A

LOX (lipoxygenase)

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26
Q

What does Etancercept inhibit?

A

TNF-α receptor

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27
Q

What enzyme does Methotrexate inhibit?

A

Dihydrofolate reductase

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28
Q

What two conditions is Sulfasalazine commonly used to treat?

A

Rheumatoid arthritis and inflammatory bowel disease

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29
Q

What cellular process does Hydroxychloroquine interfere with?

A

Lysosomal activity and antigen presentation

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30
Q

What does Leflunomide inhibit to reduce lymphocyte proliferation?

A

Pyrimidine synthesis

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31
Q

What cellular process do Calcineurin inhibitors affect?

A

Dephosphorylation of NF-AT cells, regulating cytokine release

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32
Q

How do DMARDs differ from NSAIDs in their effect on rheumatoid arthritis?

A

DMARDs target the underlying disease processes, while NSAIDs provide symptomatic relief

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33
Q

What is a major long-term risk of DMARD use?

A

Increased risk of infections due to immunosuppression

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34
Q

What is the main trade-off when using selective COX-2 inhibitors instead of traditional NSAIDs?

A

Lower gastrointestinal risk but potentially higher cardiovascular risk

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35
Q

What is Epoprostenol and what is it an analogue of?

A

Epoprostenol is an analogue of PGI2

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36
Q

What are the two main indications for Epoprostenol?

A
  1. Pulmonary hypertension
  2. Hemodialysis to harvest platelets
37
Q

What is Dinoprostone and what is it an analogue of?

A

Dinoprostone is an analogue of PGE2

38
Q

What are the two main clinical uses of Dinoprostone?

A
  1. Medical abortion
  2. Relaxing the cervix for inducing labor
39
Q

What is Misoprostol and what is it an analogue of?

A

Misoprostol is an analogue of PGE1

40
Q

What are the two main clinical uses of Misoprostol?

A
  1. Treating peptic ulcers
  2. Medical abortion
41
Q

What is Alprostadil and what is it an analogue of?

A

Alprostadil is an analogue of PGE1

42
Q

What are the two main clinical uses of Alprostadil?

A
  1. Opening ductus arteriosus in neonates
  2. Treating erectile dysfunction
43
Q

What is Carboprost and what is it an analogue of?

A

Carboprost is an analogue of PGF2α

44
Q

What is the main clinical use of Carboprost?

A

Labor induction

45
Q

What is Latanoprost and what is it an analogue of?

A

Latanoprost is an analogue of PGF2α

46
Q

What is the main clinical use of Latanoprost?

A

Treating glaucoma

47
Q

What is the mechanism of action of Aspirin?

A

Aspirin irreversibly inhibits COX-1 and COX-2 enzymes

48
Q

What are four indications for Aspirin use?

A
  1. Pain relief
  2. Fever reduction
  3. Anti-inflammatory effects
  4. Cardiovascular protection (low dose)
49
Q

What is a unique side effect of Aspirin in children?

A

Reye’s syndrome

50
Q

Name three examples of Propionic Acid Derivative NSAIDs

A

Ibuprofen, naproxen, and ketoprofen

51
Q

What is the mechanism of action of Propionic Acid Derivatives?

A

They reversibly inhibit COX-1 and COX-2 enzymes

52
Q

What are the main indications for Propionic Acid Derivatives?

A

Pain, fever, and inflammation

53
Q

Name two examples of Oxicam Derivative NSAIDs

A

Piroxicam and meloxicam

54
Q

What type of COX selectivity does meloxicam have?

A

Meloxicam is more COX-2 selective

55
Q

What is the main indication for Oxicam Derivatives?

A

Chronic arthritis

56
Q

Name two examples of Indole Derivative NSAIDs

A

Indomethacin and sulindac

57
Q

What are two indications for Indole Derivative NSAIDs?

A
  1. Rheumatoid arthritis
  2. Ankylosing spondylitis
58
Q

What is a severe side effect associated with Indole Derivatives?

A

Aplastic anemia

59
Q

Name two examples of Fenmate NSAIDs

A

Mefenamic acid and Meclofenamate

60
Q

What is a unique feature of Fenmate NSAIDs besides COX inhibition?

A

They block Prostaglandin receptors

61
Q

What is a characteristic of Fenmates related to protein binding?

A

They have high plasma protein binding

62
Q

What is an example of a Benzopyrrole NSAID?

A

Tolmetin

63
Q

What are three side effects of Benzopyrrole NSAIDs?

A
  1. GI irritation
  2. CNS effects
  3. Tinnitus
64
Q

What is a unique feature of Benzopyrroles regarding anticoagulation?

A

They have high plasma protein binding but do not increase clotting time when given with warfarin

65
Q

Name two examples of Phenylacetic Acid NSAIDs

A

Diclofenac and Aceclofenac

66
Q

What are two mechanisms of action for Phenylacetic Acid NSAIDs?

A
  1. COX inhibition
  2. Blocking the release of Arachidonic acids
67
Q

What are three indications for Phenylacetic Acid NSAIDs?

A
  1. Rheumatoid arthritis
  2. Osteoarthritis
  3. Ankylosing spondylitis
68
Q

What is an example of a Selective COX-2 Inhibitor?

A

Celecoxib

69
Q

What is the main advantage of Selective COX-2 Inhibitors?

A

Lower risk of gastrointestinal side effects

70
Q

What is the main disadvantage of Selective COX-2 Inhibitors?

A

Higher cardiovascular risk

71
Q

What is unique about Nimesulide’s effect on Prostaglandin synthase?

A

It’s a weak inhibitor of Prostaglandin synthase

72
Q

What makes Nimesulide useful for certain patients?

A

It can be used in patients allergic to aspirin and other NSAIDs

73
Q

How does Ketorolac compare to Indomethacin in terms of potency?

A

Ketorolac is 40 times more potent than Indomethacin

74
Q

What type of drug is Nabumetone?

A

Nabumetone is a prodrug

75
Q

What are two characteristics of Nabumetone?

A
  1. It’s a selective COX-2 inhibitor
  2. It’s converted to its active form by the liver
76
Q

What enzyme does Zileuton inhibit?

A

Zileuton inhibits LOX (lipoxygenase)

77
Q

What are three indications for Zileuton?

A
  1. Ulcerative colitis
  2. Asthma
  3. Allergic rhinitis
78
Q

What does Etancercept inhibit?

A

Etancercept inhibits the TNF-α receptor

79
Q

What is the mechanism of action of Methotrexate?

A

Methotrexate inhibits dihydrofolate reductase, affecting DNA synthesis

80
Q

What are two indications for Methotrexate?

A
  1. Rheumatoid arthritis
  2. Psoriasis
81
Q

What is the mechanism of action of Sulfasalazine?

A

Sulfasalazine has unknown mechanism but shows anti-inflammatory and immunomodulatory effects

82
Q

What are two indications for Sulfasalazine?

A
  1. Rheumatoid arthritis
  2. Inflammatory bowel disease
83
Q

What is the mechanism of action of Hydroxychloroquine?

A

Hydroxychloroquine interferes with lysosomal activity and antigen presentation

84
Q

What are two indications for Hydroxychloroquine?

A
  1. Rheumatoid arthritis
  2. Lupus
85
Q

What is the mechanism of action of Leflunomide?

A

Leflunomide inhibits pyrimidine synthesis, reducing lymphocyte proliferation

86
Q

What is the main indication for Leflunomide?

A

Rheumatoid arthritis

87
Q

What is the mechanism of action of Calcineurin inhibitors?

A

Calcineurin inhibitors dephosphorylate NF-AT cells, regulating the release of cytokines

88
Q

Name two examples of Calcineurin inhibitors and their binding targets

A
  1. Cyclosporin - binds to cytosolic cyclophilin
  2. Tacrolimus (FK 506) - binds to FKB12