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IC Part II > Immune Drugs > Flashcards

Immune Drugs Flashcards

1
Q

_______ cells already committed to a given cell lineage are most sensitive to cytotoxic drugs such as anticancer drugs b/c they are large cycling cells

A

progenitor

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2
Q

prednisone and methylprednisolone inhibit ______ and ______ synthesis via upregulation of lipocortin, inhibits PLA2

A

prostaglandin, leukotriene

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3
Q
  • suppress both cell and humoral immunity
  • inhibit leukocyte infiltration at site of inflammation
  • adverse: predispose to infection, adrenal gland suppression
  • not toxic to myeloid and erythrocyte progenitor cells
  • use for organ transplants, autoimmune diseases, bronchial asthma
A

corticosteroids (prednisone, methylprednisolone)

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4
Q

azathiorpine converted to _______ by glutathione S transferases than to 6-thiouric acid by xanthine oxidase

  • reduce dose in patients with TPMT deficiency
  • bioactivated by purine salvage path
A

6-mercaptopurine

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5
Q
  • interferes with nucleic acid metabolism and synthesis, inhibiting cell proliferation
  • toxic to proliferating lymphocytes following antigen exposure
  • adverse: bone marrow suppression, skin rash, fever, nausea, vomiitng, diarrhea
  • occasional liver dysfunction
  • adverse increased by kidney disease and allopurinol
  • used in kidney/organ transplant, autoimmune disease
A

azathioprine

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6
Q
  • DNA alkylating agent
  • nitrogen mustard compound
  • most potent immunosuppressive, destroys proliferating lymphoid cells
  • organ transplants, autoimmune disease
A

cyclophosphamide

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7
Q
  • folate antagonist
  • low dose in rheumatic diseases
  • inhibits thymidylate synthase
  • high dose inhibits DHFR, blocks cell proliferation
  • cytotoxic to proliferating lymphocytes
  • prophylaxis for GVHD, rheumatoid arthritis, psoriasis
A

methotrexate

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8
Q
  • inhibit IMP
  • prodrug for MPA
  • inhibits de novo purine path
  • in conjunction w/ cyclosporine and steroids for prevention of rejection in patients with renal allograft
A

mycophenolate mofetil

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9
Q
  • polypeptide antibiotic produced by certain fungi that has immunosuppressive activity
  • inhibits calcineurin, blocks production of cytokines (IL-2, 3, IFNalpha)
  • does not affect suppressor T cells or T cell independent antibody mediated immunity
  • actions of helper T lymhocytes are impaired
A

cyclosporine

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10
Q
  • high first pass metabolism
  • metabolized by CYP3A4, active metabolites
  • drugs that decrease clearance increase nephrotoxicity and seizures
  • increase clearance may lead to graft rejection (naficillin, omeprazole, rifampin)
A

cyclosporine

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11
Q
  • nephrotoxicity (clonidine minimizes, decreases ischemia)
  • additive nephrotoxicity
  • seizures
  • to prevent allogradt rejection, autoimmune
  • blood level too low - graft rejection, blood level too high nephrotoxic or seizures
A

cyclosporine

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12
Q
  • macrolide derived from fungus with similar PK to cyclosporine
  • effective in acute rejection, more potent immunosuppressant
  • kidney toxicity less
  • for liver transplants, w/ azathioprine or mycophenolate for kidney and heart transplant
A

tacrolimus

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13
Q

-omab

A

murine

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14
Q

-ximab

A

chimeric

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15
Q

-zumab

A

humanized

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16
Q
  • parenteral monoclonal antibody for murine origin that targets CD3/TCR receptor complex
  • treatment of acute allograft rejection in patients who have undergone kidney, heart, liver transplant
  • stimulates inflammatory cytokine release due to intact Fc region
  • teplizumab substitutions prevent cytokine release, ala ala - make it invisible to Fc receptors on immune cells
A

muromonab-CD3

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17
Q
  • humanized monoclonal antibody
  • binds CD52 antigen on normal and malignant B lymphocytes
  • CD52 antigen also found on T lymphocytes, NK cells, macrophages, platelets
  • approved for CLL
  • profound leukopenia, 6 months to get normal counts back
A

alemtuzumab

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18
Q
  • chimeric (murine/human) monoclonal antibodies produced by recombinant DNA technology
  • block binding of IL-2 to its receptors
  • used prophylactically in combo with cyclosporine patients undergoing renal transplantation
A

daclizumab, basiliximab

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19
Q
  • antibody to surface protein for RSV

- used to prevent RSV

A

palivizumab

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20
Q

used to treat serious RSV infections

A

ribavirin

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21
Q
  • binds CD20 antigen on B cells
  • used in non Hodgkins lymphoma
  • in combo w/ methotrexate to reduce signs and symptoms of rheumatoid arthritis in adults who had inadequate responses to one or more TNF antagonist therapies
A

rituximab

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22
Q

targets CD20 antigen found on preB and mature B lymphocytes, used for CD20 positive follicular non Hodgkins lymphoma whose disease is refractory to rituximab and has relapsed following chemo

A

tositumomab

23
Q
  • Ab directed towards the IgE high affinity Fc receptor on mast cells
  • given SC every 2-4 weeks for prophylaxis of asthma and to control symptoms of moderate to severe asthma not controlled by inhaled steroids
A

omalizumab

24
Q
  • IL-5 antagonists
  • IL-5 responsible for growth and differentiation, recruitment, activation, and survival of eosinophils
  • cell type assoc’d with inflammation and an important component of the pathogenesis of asthma
A

mepolizumab, reslizumab

25
Q
  • binds Her2 protein on surface of tumor cells

- used for metastatic breast tumors that over express Her2 protein

A

trastuzumab

26
Q
  • antagonist of GP2b3a receptor of platelets
  • used post angioplasty in acute coronary syndromes
  • stents coated with this drug
A

abciximab

27
Q
  • monoclonal antibody that targets integrin molecules blocking the attachment on inflammatory cells to inflamed tissues
  • treats Crohn disease and MS
A

natalizumab

28
Q
  • monoclonal antibody that targets integrin molecules blocking migration of memory T lymphocytes across the endothelium into inflamed GI parenchymal tissue
  • treats Crohn disease, ulcerative colitis
A

vedolizumab

29
Q
  • treatment of bladder carcinoma and a prophylactic agent against TB
  • instilled into bladder
  • causes local inflammatory rxn with histiocytic and leukocytic infiltration in urinary bladder
  • adverse: dysuria, urinary frequency, hematuria, cystitis, urinary urgency …..
A

bacillus calmette guerin, live intravesical

30
Q
  • infamous drug assoc’d with phocomelia in offspring of mothers who took it during pregnancy
  • used in treament of leprosy
  • orphan drug status for several conditions
  • most heavily regulated drug in US
A

thalidomide

31
Q
  • restricted use for MDS, mantle cell lymphoma, multiple myeloma
  • concerns about increased risk of secondary malignancies
A

lenalidomide, pomalidomide

32
Q
  • endogenous are secreted by cells in response to viral infection or biological inducers
  • approved for hairy cell leukemia, AIDS related Kaposis sarcoma, condyloma acuminata, chronic hep B and C
  • antiviral and antitumor activity
A

interferon alpha

33
Q
  • produced by fibroblasts and epithelial cells
  • endogenous interferon gamma triggers autoimmune reaction leading to MS
  • decrease number and severity of multiple sclerosis attacks
A

interferon beta

34
Q
  • derived from genetically engineered EColi
  • used in treatment of chronic granulomatous disease, an inherited disorder of phagocytic oxidative metabolism
  • potent phagocyte activating properties that result from enhancement of oxidative metabolism in tissue macrophages
  • enhancement of antibody dependent cellular cytotoxicity and NK cell activity
  • flu like symptoms
A

interferon gamma

35
Q
  • non glycosylated biosynthetic IL-2 (T cell growth factor)
  • for metastatic renal cell carcinoma
  • for AML, non hodgkin, HIV, leprosy
  • induces proliferation and differentiation of B and T cells, monocytes, macrophages, and cytotoxic lymphocytes
  • high dose IV bolus assoc’d with adverse rxn
A

aldesleukin

36
Q
  • recombinant version of human IL-11

- SC once a day to prevent severe chemo induced thrombocytopenia

A

oprelvekin

37
Q
  • symptomatic relief for RA but do not prevent erosions or alter disease progression
  • not appropriate for monotherapy and should only be used in conjunction with DMARDS
A

NSAIDS

38
Q
  • cause dramatic improvement in RA
  • do not arrest disease process itself
  • adverse effects limit long term use
A

corticosteroids

39
Q
  • widely used to treat RA
  • low doses, inhibition of AICAR transformylase and thymidylate synthase
  • inhibits DHFR, blocks folate reactions in biosynthesis of nucleotides needed for cell proliferation
A

DMARDS: methotrexate

40
Q
  • antimalarial, reduce oxidative stress?
  • contraindicated in psoriatic arthritis b/c of possible development of exfoliated dermatitis
  • can cause irreversible retinal damage
A

hydroxychloroquine/chloroquine

41
Q
  • don’t give with penicillamine b/c it chelates
  • contraindications: pregnancy, liver or kidney impairment, aplastic anemia
  • adjunctive treatment of early active cases of adult and juvenile RA, given IM, cutaneous rxns may occur
A

aurothioglucose

42
Q
  • only gold compound available for oral admin

- treats early active cases of both adult and juvenile types of RA

A

auranofin

43
Q
  • oral chelating agent

- treat Wilsons, cystinuria, resistant cases of RA

A

penicillamine

44
Q
  • used for RA, ankylosing spondylitis, ulcerative colitis

- suppess IL1, TNF alpha, apoptosis of inflammatory cells

A

sulfasalazine

45
Q
  • converted to active metabolite that inhibits dihydroorotic acid dehydrogenase, involved in pyrmidine ribonucleotide synthesis
  • translocation of p53 to nucleus, stimulated cells arrest in G1
  • inhibits autoimmune T cell proliferation, production of autoAb by B cells
  • first agent for RA indicated by symptomatic improvement and retardation of structural joint damage
  • cause alopecia, rash, diarrhea
A

leflunodime

46
Q
  • IL-1 receptor antagonist
  • slows progression of structural damage of RA in patients who failed one or more DMARDS
  • given SQ once a day
  • treat and prevent gout
A

anakinra, canakinumab, rilonacept

47
Q
  • dimeric fusion protein produced by recombinant DNA technology that binds TNF
  • soluble TNF receptor
  • given by injection
  • RA, works by decreasing TNF alpha effects
A

etanercept

48
Q
  • chimeric monoclonal anitbody that binds TNFalpha
  • IV infusion with methotrexate for RA
  • Crohn’s when conventional therapy fails
A

infliximab

49
Q

all _____ drugs increase opportunistic infections and the risk of lymphomas

A

anti-TNF

50
Q

IL-6 antagonist, may increase CYP450 activity (increase warfarin and cyclosporine metabolism), for RA with inadequate response to TNF antagonists, increase opportunistic

A

tocilizumab

51
Q
  • recombinant fusion protein composed of extracellular domain of cytotoxic T lymphocyte associated antigen (CTLA4) fused to human IgG
  • immune checkpoint receptor found on T cells that binds to CD80 and CD86 on antigen presenting cells, inhibits T cell activation
  • blocks activation of T cells by binding CD80 or 86 so CD28 on T cells cannot bind and stimulate the T cell and lead to cytokine release
  • severe RA who have failed other DMARDS
  • should not take other antiTNF or IL1 or IL6 antagonists at same time
A

abatacept

52
Q
  • inhibits JAK enzymes
  • disrupts cell enzymes involved in stimulating hematopoeiesis and immune cell via signaling path
  • 2X day
  • metab’d by CYP3A4
  • RA in adults intolerant of methotrexate
  • increases risk for opportunistic infections
A

tofacitinib

53
Q
  • oral drug for psoriasis and psoriatic arthritis
  • inhibits PDE4, increasing cAMP
  • decreases iNOS, decrease TNFalpha, IL-23
  • increase IL-10 antiinflammatory
  • opportunistic infections
  • reports of neuropsych and weight loss
A

apremilast

IC Part II (29 decks)

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