Rheumatology, NSAIDs, Acetaminophen Flashcards

1
Q

Rapidly converted to mycophenolic acid which inhibits inosine monophosphate dehydrogenase (an enzyme in the de novo pathway of guanosine triphosphate synthesis GTP)

Supresses both B and T lymphocyte activation

A

Mycophenolate mofetil

Ind: SLE, Transplants

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2
Q

Mycophenolate toxicity

A

GI

Myelosupression (neutropenia)

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3
Q

Alkylating agents

A

Cyclophosphamide

Cisplatin

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4
Q

Antimetabolites

A

5-FU
Methotrexate
Gemcitabine
6-mercaptopurine

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5
Q

Antitumor antibiotics

A

Bleomycin
Doxorubicin
Mitomycin

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6
Q

Natural product

A

Etoposide
Paclitaxel
Vincristine

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7
Q

Alklyating agents form reactive molecular species that alkylate

A

nucleophilic groups on DNA bases particulary N-7 position of guanine

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8
Q

Nitrogen mustard alkylating agent that alkylates nucleophilic groups ob DNA bases particularly the N-7 position of guanine

Cross-linking of bases, abnormal base pairing, and DNA strand breakage

Used in SLE, leukemia, non-Hodgkin’s, breast, ovarian cancer and neuroblastoma

A

Cyclophosphamide

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9
Q

Breakdown product of cyclophosphamide by CYP450

Needed for antitumor activity

A

Acrolein

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10
Q

Cyclophosphamide toxicity

A

GI distress
Myelosupression
Alopecia

Hemorrhagic cystitis
Cardiac dysfunction
Pulmo toxicity
SIADH

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11
Q

Adverse effect of cyclophosphamide from acrolein formation

Decreased by vigorous hydration and by use of mercaptoethane sulfonate (MESNA)

A

Hemorrhagic cystitis

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12
Q

First ever targeted biological treatment for SLE

Fully humanized IgG1 gamma monoclonal antibody against soluble B lymphocyte stimulator

A

Belimumab

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13
Q

Enter the cell and bind to cytosolic receptors that transport it into the nucleus

This complex alters genes expression by binding to GRE (response elements) and tissue specific responses are made possible by protein regulators

A

Glucocorticoids

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14
Q

Glucocorticoid organ and tissue effect on metabolism

A
Stimulates gluconeogenesis
Blood glucose rise
Muscle protein catabolism
Increased insulin secretion
Lipolysis and lipogenesis stimulation with fat deposition
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15
Q

Glucocorticoid catabolic effect

A

Muscle protein catabolism
Lymphoid tissue connective tissue fat and skin wasting
Osteoporosis

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16
Q

Glucocorticoid immunosupressive effect

A

Inhibit cell mediated immunologic functions especially those dependent on lymphocytes

17
Q

Glucocorticoid anti-inflammatory effect

A

Supressant on inflammatory process
Increase neutrophil
Decrease lymphocyte, eosinophil, basophil, monocyte
Inhibition of leukocyte migration

Induced synthesis of inhibitor of phospholipase A2
Decreased mRNA for COX2
Decreased IL-2 and IL-3
Decreased platelet activating factor

18
Q

Other glucocorticoid effects

A

Normal renal excretion of water
CNS behavioral change
Stimulate gastric acid secretion
Decreased resistance to ulcer formation

19
Q

DMARDs that interfere with activity of T lymphocytes

Immunosupressant used for rheumatoid arthritis

A

DMARDs
Hydroxychloroquine
Chloroquine

20
Q

DMARD toxicity

A
Retinal toxicity
Rash
GI distress
Myopathy
Neuropathy
21
Q

Inhibitot of dihydroorotate dehydrogenase an enzyme involved in de novo pyrimidine synthesis

Used in RA

A

Leflunomide

22
Q

Cytotoxic to rapidly dividing immune cells due to inhibition of dihydrofolate reductase

Anticancer, rheumatoid disorders

A

Methotrexate

23
Q

Methotrexate toxicity

A
Nausea
Mucosal ulcera
Hematoxicity
Hepatotoxicity
Teratogenecity
24
Q

Inhibition of microtubule assembly decreases macrophage migration and phagocytosis

Chronic and acute gout
Familial Mediterranean Fever

A

Colchicine

25
Q

Colchicine toxicity

A

Diarrhea

Severe liver and kidney damage in overdose

26
Q

Aminosalicylate
Contains 5-aminosalicylic acid (5-ASA generic Mesalamine) used as topical therapy for IBD and RA

Inhibiting synthesis of prostaglandin and inflammatory leukotrienes, and interfering with the production of inflammatory cytokines

5 ASA + sulfapyridine

A

Sulfasalazine

27
Q

Sulfasalazine adverse effect

A

Sulfonamide toxicity due to absorption of sulfapyridine moiety

28
Q

Cytotoxic drug

Prodrug of anticancer drug mercaptopurine, which interferes with purine nucleic acid metabolism used for rheumatic diseases and organ transplantation

A

Azathioprine

29
Q

Acetylation of COX-1 and COX-2 results in decreased prostaglandin synthesis
Irreversible COX inhibition

Analgesia
Antipyretic
Anti-inflammatory
Anti-thrombotic

Prevents colon cancer

A

Aspirin

Salicylate

30
Q

Reversible inhibition of COX-1 and COX-2 results in decreased prostaglandin synthesis

Analgesia
Antipyretic
Anti-inflammatory

Closure of Patent Ductus Arteriosus

Interferes with aspirin’s antithrombotic action

A

Ibuprofen

Nonselective NSAIDs

31
Q

Selective, reversible inhibition of COX-2 results in decreased prostaglandin synthesis

Analgesia
Antipyretic
Anti-inflammatory

Hepatic metabolism
Less risk of GI toxicity
Greater risk of thrombosis

A

Celecoxib

COX-2

32
Q

Mechanism unknown
Weak COX inhibitor

Analgesia
Antipyretic
NOT ANTI-INFLAMMATORY

Hepatic conjugation

Hepatotoxicity in overdose more likely in chronic alcohol consumltion which induces CYP450

A

Acetaminophen

33
Q

Inhibition of renal reuptake of uric acid

Chronic gout, prolongation of antimicrobial drug action

Exacerbation of acute gout
Inhibits renal tubular secretion of weak acids such as methotrexate

A

Probenecid

Sulfinpyrazone

34
Q

Active metabolite irreversibly inhibits xanthine oxidase and lowers production of uric acid

Chronic gout, adjunct to cancer chemotherapy

Activated by xanthine oxidase

A

Allopurinol

35
Q

Reversible inhibitor of xanthine oxidase

A

Febuxostat

36
Q

Biologic agents that inhibit the action of tumor necrosis factor - alpha

Decreases formation of interleukins and adhesion molecules involved in leukocyte activation

Used in RA, IBD, Ankylosing spondylitis,

A

Infliximab
Adalimumab
Etanercept

37
Q

Recombinant human interleukin-1 receptor antagonist

A

Anakinra