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Pharmacology > DMARDs, Immunomodulators, Immunosuppressors > Flashcards

DMARDs, Immunomodulators, Immunosuppressors Flashcards

1
Q

DMARDs - Clinical use

A

Rheumatoid arthritis – limited use (resistance to drug within 5 years, adverse effects)

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2
Q

Gold salts

A

Auranofin
Gold sodium thiomalate
Aurothioglucose

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3
Q

Gold salts - MoA

A

Suggested antimitochondrial activity and cell apoptosis

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4
Q

Gold salts - Adverse effects

A

Hematologic, dermatologic, GI, renal effects.
Flushing, hypotension, tachycardia
Skin rash & stomatitis

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5
Q

Glucocorticoid

A

Prednisone

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6
Q

Prednisone - MoA

A

Induce formation of lipocortin which inhibits phospholipase A2, This inhibits release of arachidonic acid.

Also inhibit production of cytokines (ILs, TNF)

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7
Q

Prednisone - Clinical use

A

RA to induce remission while waiting for slower-acting DMARD to work.
Short courses during flare-ups.
Continuous low-dose background therapy

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8
Q

Methotrexate - Classification

A

Antineoplastic and immunomodulating drug

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9
Q

Methotrexate - MoA

A

Inhibition of human folate reductase which decreases thymidylate and DNA synthesis.

Inhibition of lymphocyte proliferation and production of cytokines and rheumatoid factor.

Interferes with polymorphonuclear leukocyte chemotaxis, which reduces cytotoxins and free radicals

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10
Q

Methotrexate - Clinical use

A

DMARD of choice in most patients with RA

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11
Q

Methotrexate - Contraindications

A

Pregnancy and in combination with leflunomide because of hepatotoxicity

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12
Q

Methotrexate - Adverse effects

A

GI, hematologic, hepatic, pulmonary reactions.

Elevated liver enzymes.

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13
Q

Leflunomide - Classification

A

Immunosuppressive drug

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14
Q

Leflunomide - MoA

A

Inhibits leukocyte and T-cell proliferation by inhibiting pyrimidine synthesis (DNA replication, RNA synthesis, protein synthesis) in immune cells

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15
Q

Leflunomide - Clinical use

A

Alternative to methotrexate for RA

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16
Q

Leflunomide - Contraindications

A

Pregnancy and in combination with methotrexate because of hepatotoxicity

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17
Q

Leflunomide - Adverse effects

A

Diarrhea
Reversible alopecia (baldness)
Increased serum hepatic enzymes
Teratogenic

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18
Q

Leflunomide - Interactions

A

Inhibition of CYP2C9: increases serum levels of many drugs (ibuprofen)

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19
Q

Hydroxychloroquine - Classification

A

Antimalarial drug

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20
Q

Hydroxychloroquine - MoA

A

Reduces chemotaxis and phagocytosis of PMNs, reduced superoxides from these cells

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21
Q

Hydroxychloroquine - Adverse effects

A

GI disturbances

Blurred vision, scotomas, night blindness

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22
Q

Anti TNF-α agents

A 
Etanercept
Infliximab
Adalimumab
Cetrolizumab
Golimumab
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23
Q

Anti TNF-α agents - MoA

A

Binds to and inactivates TNF-α. Newer agents prevents interleukin binding and T-cell activation.

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24
Q

Anti TNF-α agents - Adverse effects

A

Serious infections and sepsis
Tuberculosis and invasive opportunistic fungal infections
Lymphoma

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25
Q

Etanercept - MoA

A

Dimer of human TNF receptor fused to IgG constant region

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26
Q

Etanercept - Clinical use

A

RA resistant to other DMARDs

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27
Q

Etanercept can be combined with

A

Methotrexate

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28
Q

Etanercept - Adverse effects

A

Injection site reactions

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29
Q

Infliximab - MoA

A

MAb binds to TNF-α and prevents it from activating TNF-α receptor

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30
Q

Infliximab - Clinical use

A

Crohn’s disease and rheumatoid arthritis

ankylosing spondylitis, psoriatic arthritis*

*=Katzung

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31
Q

Infliximab can be combined with

A

Methotrexate

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32
Q

Infliximab - Adverse effects

A

Hypersensitivity reactions
Infection
Malignancy
Reactivation of latent TB

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33
Q

Adalimumab - MoA

A

Human IgG1 MAb similar to daclizumab, specific for human TNF α

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34
Q

Cetrolizumab - MoA

A

Pegylated Mab directed against TNF α.

35
Q

Cetrolizumab - Interactions

A

By combining the active molecule with PEG, the resulting product remains in the body longer.

36
Q

Golimumab - MoA

A

Human Mab that binds to both the soluble and transmembrane forms of human TNFα. This interaction prevents the binding of TNFα to its receptor, thereby inhibiting the biologic activity of TNFα.

37
Q

Cytokine inhibitors

A

Anakinra
Canakinumab
Rilonacept

38
Q

Anakinra - MoA

A

Recombinant form of the human interleukin- 1 receptor antagonist (IL-1Ra).
Blocks the biologic activity of IL-1 by competitively inhibiting IL-1 binding to the interleukin-1 type I receptor (IL-1RI).

39
Q

Anakinra - Clinical use

40
Q

Canakinumab - MoA

A

Recombinant human anti-IL-1β monoclonal antibody. It binds to human IL-1β and prevents it from binding to IL-1 receptors.

41
Q

Rilonacept - MoA

A

Dimeric fusion protein consisting of the ligand-binding domains of the extracellular portions of the human interleukin-1 receptor component (IL-1RI) and IL-1 receptor accessory protein (IL-1RAcP) fused to the Fc portion of human IgG1.

42
Q

Abatacept - MoA

A

Selective costimulation modulator, inhibits T-cell activation by binding to cell surface markers (proteins) in leukocytes.

43
Q

Abatacept - Clinical use

44
Q

Tocilizumab - MoA

A

Humanized anti-IL-6 receptor Mab. Binds selectively to IL-6 receptors and blocks IL-6 acitivity.

45
Q

Tocilizumab - Clinical use

A

RA

Active systemic juvenile idiopathic arthritis in patients 2 y and older

46
Q

Sulfasalazine - Clinical use

47
Q

Sulfasalazine - Contraindication

A

Sulfa-allergy

48
Q

D-Penicillamine - MoA

A

Reduces blood levels of inflammation cytokines

49
Q

D-Penicillamine - Clinical use

A

RA

Less used, better alternatives today.
Copper chelating agent in Willsons disease

50
Q

Apremilast - MoA

A

Inhibitor of phosphodiesterase type 4 (PDE4) –> increases cAMP levels, which decreases expression of TNFα and other proinflammatory cytokines.

51
Q

Which cytokine inhibitor has the same adverse effects as the TNFα blockers?

52
Q

Aldesleukin - MoA

A

Recombinant interleukin-2

53
Q

Aldesleukin - Clinical use

A

Adjunctive treatment of renal cell carcinoma and malignant melanoma.

54
Q

Daclizumab - MoA

A

Highly specific MAb that binds to the alpha subunit of the IL-2 receptor displayed on the surface of T cells and prevents activation by IL-2

55
Q

Daclizumab - Clinical use

A

Prevent renal transplant rejection.

In comb with other immunosuppressants

56
Q

Interferon–α-2a - MoA

A

Inhibits cell proliferation

57
Q

Interferon–α-2a - Clinical use

A

Hairy cell leukemia, chronic myelogenous leukemia, malignant melanoma, Kaposi’s sarcoma, Hepatitis B and C.

58
Q

Interferon-b-1b - Clinical use

A

Relapsing multiple sclerosis

59
Q

Interferon-g-1b - MoA

A

Greater immune-enhancing actions. Act by increasing the synthesis of TNF.

60
Q

Interferon-g-1b - Clinical use

A

Recombinant form: decrease the incidence and severity of infections in patient with chronic granulomatous disease

61
Q

Immunosuppressants

A

Corticosteroids
Calcineurin and mTOR inhibitors
Mycocephenolate Mofetil
Thalidomide and derivatives

62
Q

Immunosuppressants - Clinical use

A

Prevent rejection of transplanted organs

Treat RA and other autoimmune disorders

63
Q

Glucocorticoids - MoA

A

Biochemical level:, their actions on gene expression decrease the synthesis of prostaglandins, leukotrienes, cytokines, and other signaling molecules that participate in immune responses (eg, platelet activating factor).

Cellular level: the glucocorticoids inhibit the proliferation of T lymphocytes and are cytotoxic to certain subsets of T cells

Humoral immunity is also dampened –> continuous therapy lowers IgG levels by increasing the catabolic rate.

64
Q

Glucocorticoids - Clinical use

A

Medical conditions that have an underlying undesirable immunologic basis.
Suppress immunologic reaction in patients undergoing organ-transplant.
Treat hematologic cancers

65
Q

Glucocorticoids - Adverse effects

A 
Adrenal suppression
Growth inhibition
Muscle wasting
Osteoporosis
Salt retention
Glucose intolerance
Behavioral changes
66
Q

Calcineurin and mTOR inhibitors - MoA

A

Interfere with T-cell function by binding to immunophilins

Prevent the increased production of cytokines that normally occurs in response to T-cell receptor activation.

67
Q

Calcineurin and mTOR inhibitors - Clinical use

A

Solid organ transplantation.

Prevent and treat graft-versus-host (GVH) disease (allogeneic stem cell transplantation)

68
Q

Cyclosporine - MoA

A

Binds to cyclophilin –> completely inhibits calcineurine

69
Q

Cyclosporine, Tacrolimus - Clinical use

A

Some autoimmune diseases:

RA, uveitis, psoriasis, asthma, DIA1

70
Q

Cyclosporine, Tacrolimus - Adverse effects

A

Most common:
Renal dysfunction
Hypertension
Neurotoxicity

Also:
Hyperglycemia
Hyperlipidemia
Cholelithiasis.

71
Q

Cyclosporine - Interactions

A

Slow hepatic metabolism by CYT P-450

72
Q

Tacrolimus - MoA

A

Binds to FK-binding protein (FKBP) –> completely inhibits calcineurine

73
Q

Sirolimus analogs

A

Everolimus

Temsirolimus)

74
Q

Sirolimus - MoA

A

Binds to FKBP 12. Inhibit the kinase activity of mammalian target of rapamycin (mTOR). By inhibiting the mTOR pathway, inhibits T-cell proliferation response to IL.2

75
Q

Sirolimus and analogs - Clinical use

A

Prevent restenosis after coronary angioplasty.

Everolimus: immunosuppressant
Everolimus and temsirolimus: cancers

76
Q

Sirolimus and analogs - Adverse effects

A

Myelosuppression.
Hypertriglyceridemia
Hepatotoxicity
Diarrhea

77
Q

Mycocephenolate Mofetil - MoA

A

Rapidly converted into mycophenolic acid, which inhibits inosine monophosphate dehydrogenase (involved in GTP synthesis pathway) –> suppression of B and T-lymphocyte activation.

78
Q

Mycocephenolate Mofetil - Clinical use

A

Sole agent in kidney, liver and heart transplantations

79
Q

Mycocephenolate Mofetil in renal transplantation

A

Renal transplantation: use with low-dose cyclosporine to reduce the cyclosporine-induced nephrotoxicity

80
Q

Mycocephenolate Mofetil - Adverse effects

A

GI distrubances
Myelosuppression
Neutropenia

81
Q

Thalidomide - MoA

A

Suppression of TNF-α production, increased IL-10, reduced neutrophil phagocytosis, altered adhesion molecule expression, and enhanced cell-mediated immunity.

82
Q

Thalidomide - Clinical use

A 
Leprosy
Immunologic diseases (systemic lupus)
Anticancer 
Aphthous ulcers
Wasting syndrome in AIDS patients.
83
Q

Thalidomide derivatives

A

Lenalidomine and Pomalidomide

84
Q

Thalidomide derivatives - Clinical use

A

Multiple myeloma

Pharmacology (55 decks)

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