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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
Etanercept - MoA
Dimer of human TNF receptor fused to IgG constant region
26
Etanercept - Clinical use
RA resistant to other DMARDs
27
Etanercept can be combined with
Methotrexate
28
Etanercept - Adverse effects
Injection site reactions
29
Infliximab - MoA
MAb binds to TNF-α and prevents it from activating TNF-α receptor
30
Infliximab - Clinical use
Crohn's disease and rheumatoid arthritis ankylosing spondylitis, psoriatic arthritis* *=Katzung
31
Infliximab can be combined with
Methotrexate
32
Infliximab - Adverse effects
Hypersensitivity reactions Infection Malignancy Reactivation of latent TB
33
Adalimumab - MoA
Human IgG1 MAb similar to daclizumab, specific for human TNF α
34
Cetrolizumab - MoA
Pegylated Mab directed against TNF α.
35
Cetrolizumab - Interactions
By combining the active molecule with PEG, the resulting product remains in the body longer.
36
Golimumab - MoA
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
Cytokine inhibitors
Anakinra Canakinumab Rilonacept
38
Anakinra - MoA
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
Anakinra - Clinical use
RA
40
Canakinumab - MoA
Recombinant human anti-IL-1β monoclonal antibody. It binds to human IL-1β and prevents it from binding to IL-1 receptors.
41
Rilonacept - MoA
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
Abatacept - MoA
Selective costimulation modulator, inhibits T-cell activation by binding to cell surface markers (proteins) in leukocytes.
43
Abatacept - Clinical use
RA
44
Tocilizumab - MoA
Humanized anti-IL-6 receptor Mab. Binds selectively to IL-6 receptors and blocks IL-6 acitivity.
45
Tocilizumab - Clinical use
RA Active systemic juvenile idiopathic arthritis in patients 2 y and older
46
Sulfasalazine - Clinical use
RA
47
Sulfasalazine - Contraindication
Sulfa-allergy
48
D-Penicillamine - MoA
Reduces blood levels of inflammation cytokines
49
D-Penicillamine - Clinical use
RA Less used, better alternatives today. Copper chelating agent in Willsons disease
50
Apremilast - MoA
Inhibitor of phosphodiesterase type 4 (PDE4) --> increases cAMP levels, which decreases expression of TNFα and other proinflammatory cytokines.
51
Which cytokine inhibitor has the same adverse effects as the TNFα blockers?
Anakinra
52
Aldesleukin - MoA
Recombinant interleukin-2
53
Aldesleukin - Clinical use
Adjunctive treatment of renal cell carcinoma and malignant melanoma.
54
Daclizumab - MoA
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
Daclizumab - Clinical use
Prevent renal transplant rejection. | In comb with other immunosuppressants
56
Interferon–α-2a - MoA
Inhibits cell proliferation
57
Interferon–α-2a - Clinical use
Hairy cell leukemia, chronic myelogenous leukemia, malignant melanoma, Kaposi’s sarcoma, Hepatitis B and C.
58
Interferon-b-1b - Clinical use
Relapsing multiple sclerosis
59
Interferon-g-1b - MoA
Greater immune-enhancing actions. Act by increasing the synthesis of TNF.
60
Interferon-g-1b - Clinical use
Recombinant form: decrease the incidence and severity of infections in patient with chronic granulomatous disease
61
Immunosuppressants
Corticosteroids Calcineurin and mTOR inhibitors Mycocephenolate Mofetil Thalidomide and derivatives
62
Immunosuppressants - Clinical use
Prevent rejection of transplanted organs | Treat RA and other autoimmune disorders
63
Glucocorticoids - MoA
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
Glucocorticoids - Clinical use
Medical conditions that have an underlying undesirable immunologic basis. Suppress immunologic reaction in patients undergoing organ-transplant. Treat hematologic cancers
65
Glucocorticoids - Adverse effects
``` Adrenal suppression Growth inhibition Muscle wasting Osteoporosis Salt retention Glucose intolerance Behavioral changes ```
66
Calcineurin and mTOR inhibitors - MoA
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
Calcineurin and mTOR inhibitors - Clinical use
Solid organ transplantation. | Prevent and treat graft-versus-host (GVH) disease (allogeneic stem cell transplantation)
68
Cyclosporine - MoA
Binds to cyclophilin --> completely inhibits calcineurine
69
Cyclosporine, Tacrolimus - Clinical use
Some autoimmune diseases: | RA, uveitis, psoriasis, asthma, DIA1
70
Cyclosporine, Tacrolimus - Adverse effects
Most common: Renal dysfunction Hypertension Neurotoxicity Also: Hyperglycemia Hyperlipidemia Cholelithiasis.
71
Cyclosporine - Interactions
Slow hepatic metabolism by CYT P-450
72
Tacrolimus - MoA
Binds to FK-binding protein (FKBP) --> completely inhibits calcineurine
73
Sirolimus analogs
Everolimus | Temsirolimus)
74
Sirolimus - MoA
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
Sirolimus and analogs - Clinical use
Prevent restenosis after coronary angioplasty. Everolimus: immunosuppressant Everolimus and temsirolimus: cancers
76
Sirolimus and analogs - Adverse effects
Myelosuppression. Hypertriglyceridemia Hepatotoxicity Diarrhea
77
Mycocephenolate Mofetil - MoA
Rapidly converted into mycophenolic acid, which inhibits inosine monophosphate dehydrogenase (involved in GTP synthesis pathway) --> suppression of B and T-lymphocyte activation.
78
Mycocephenolate Mofetil - Clinical use
Sole agent in kidney, liver and heart transplantations
79
Mycocephenolate Mofetil in renal transplantation
Renal transplantation: use with low-dose cyclosporine to reduce the cyclosporine-induced nephrotoxicity
80
Mycocephenolate Mofetil - Adverse effects
GI distrubances Myelosuppression Neutropenia
81
Thalidomide - MoA
Suppression of TNF-α production, increased IL-10, reduced neutrophil phagocytosis, altered adhesion molecule expression, and enhanced cell-mediated immunity.
82
Thalidomide - Clinical use
``` Leprosy Immunologic diseases (systemic lupus) Anticancer Aphthous ulcers Wasting syndrome in AIDS patients. ```
83
Thalidomide derivatives
Lenalidomine and Pomalidomide
84
Thalidomide derivatives - Clinical use
Multiple myeloma

Pharmacology (55 decks)

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