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
Colchicine toxicity
Diarrhea | Severe liver and kidney damage in overdose
26
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
Sulfasalazine
27
Sulfasalazine adverse effect
Sulfonamide toxicity due to absorption of sulfapyridine moiety
28
Cytotoxic drug Prodrug of anticancer drug mercaptopurine, which interferes with purine nucleic acid metabolism used for rheumatic diseases and organ transplantation
Azathioprine
29
Acetylation of COX-1 and COX-2 results in decreased prostaglandin synthesis Irreversible COX inhibition Analgesia Antipyretic Anti-inflammatory Anti-thrombotic Prevents colon cancer
Aspirin | Salicylate
30
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
Ibuprofen | Nonselective NSAIDs
31
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
Celecoxib | COX-2
32
Mechanism unknown Weak COX inhibitor Analgesia Antipyretic NOT ANTI-INFLAMMATORY Hepatic conjugation Hepatotoxicity in overdose more likely in chronic alcohol consumltion which induces CYP450
Acetaminophen
33
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
Probenecid | Sulfinpyrazone
34
Active metabolite irreversibly inhibits xanthine oxidase and lowers production of uric acid Chronic gout, adjunct to cancer chemotherapy Activated by xanthine oxidase
Allopurinol
35
Reversible inhibitor of xanthine oxidase
Febuxostat
36
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,
Infliximab Adalimumab Etanercept
37
Recombinant human interleukin-1 receptor antagonist
Anakinra