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
2
Q
prednisone and methylprednisolone inhibit ______ and ______ synthesis via upregulation of lipocortin, inhibits PLA2
A
prostaglandin, leukotriene
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)
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
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
6
Q
- DNA alkylating agent
- nitrogen mustard compound
- most potent immunosuppressive, destroys proliferating lymphoid cells
- organ transplants, autoimmune disease
A
cyclophosphamide
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
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
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
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
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
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
13
Q
-omab
A
murine
14
Q
-ximab
A
chimeric
15
Q
-zumab
A
humanized
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
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
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
19
Q
- antibody to surface protein for RSV
- used to prevent RSV
A
palivizumab
20
Q
used to treat serious RSV infections
A
ribavirin
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
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
