Immunomodulators Flashcards
(78 cards)
1
Q
Purine metabolism metabolism inhibitors or antimetabolites examples
A
Methotrexate, Azathioprine, Mycophenolic acid mofetil
2
Q
TNF alpha inhibitors
A
Infliximab, Adalimumab
3
Q
Calcineurin inhibitors
A
Cyclosporine, Tacrolimus
4
Q
Anti integrins
A
Natalizumab
5
Q
Tyrosine kinase inhibitors
A
Tofacitinib, Upadacitinib
6
Q
Alkalyting agents
A
Cyclophosphamide
7
Q
Antibodies against Antigen CD20
A
Rituximab
8
Q
Interferon receptor agonist (IFNAR)
A
Peginterferon beta
9
Q
DMARDS full form
A
Disease Modifying anti rheumatic drugs
10
Q
3 types of DMARDS
A
Synthetic, biological and Janus kinase s tirosine kinase inhibitor
11
Q
Synthetic DMARDS example
A
Methotrexate
12
Q
Biological DMARDs example
A
Infliximab, Adalimumab
13
Q
Janus kinase s tirosine kinase inhibitors example
A
Tofacitinib
14
Q
Alternative synthetic DMARDS example
A
Leflunomide, sulfasalazine, hydroxychloroquine
15
Q
As the onset of action of S- DMARDS are slow, patient doesn’t gets benefits during
A
First 2 to 12 hrs
16
Q
Until the full effect of S- DMARDS therapy is achieved,——- is added to therapy at the beginning
A
Glucocorticoid
17
Q
The full effect of methotrexate therapy is achieved within ( —duration—–)
A
3 to 6 months
18
Q
Calcineurin
A
Calcium dependent cytoplasmic phosphatase required for T lymphocyte activation and IL 2 production
19
Q
Prodrug of Mycophenolic acid
A
Mycophenolate Mofetil
20
Q
Inhibition of denovo purine synthesis is done by
A
Methotrexate, Azathioprine, Mycophenolate Mofetil
21
Q
Inhibition of denovo pyramiding synthesis is done by
A
Leflunomide
22
Q
Inhibition of IL-2R signalling done by
A
Sirolimus
23
Q
Cytokine blockade done by
A
Infliximab, Etanercept, Adalimumab
24
Q
Inhibition of IL 2 expression done by
A
Ciclosporin and Tacrolimus
25
Inhibition of TNF alpha and other cytokines done by
Sulfasalazine and hydroxychloroquine
26
Cytotoxicity via DNA damage is done by
Cyclophosphamide
27
Purine antimetabolite ( Methotrexate) action
An antineoplastic agent,is a dihydrofolate or folic acid analogue which increases extracellular adenosine concentration and it inhibits dihydrofolate reductase ( Dihydrofolate is not converted to tetrahydrofolate ( active form)- DNA synthesis inhibition),inhibit T lymphocyte proliferation,inhibit IL 2 secretion......so Immunosuppressive and Antiproliferative effect
28
Adenosine is a
Endogenous inflammatory inhibitor
29
Methotrexate clinical use
Active rheumatoid arthritis, chronic lupus erythematosus, vasculitis, juvenile arthritis, psoriasis, psoriatic arthritis, supportive therapy for Acute lymphocytic leukemia, Crohn's disease
30
SE of methotrexate
Myelosuppression, pulmonary toxicity, hepatotoxicity,nephrotoxicity, stomatitis
31
Methotrexate (MTX) shouldn't be co-administered with
Co trimoxazole, salicylates etc
32
Typical clinical manifestations of methotrexate toxicity
Mucositis, necrotic skin lesions, pancytopenia
33
MTX toxicity after oral. Overdose are seen as
Hematopoietic and GIT system issues
34
Most common symptoms of methotrexate toxicity
Leukocytopenia, thrombocytopenia anaemia, pancytopenia ,bone marrow suppression,ulcerative stomatitis, nausea, vomiting, gastrointestinal ulceration and haemorrhage
35
Cause of death related to MTX toxicity is
Multi organ failure
36
Methotrexate toxicology treatment
For nausea and vomiting - anti emetics like ondansetron, metoclopramide
For fluid deficit - crystalloid solution IV
Calcium folinate IV against toxicity
Glucarpidase - an enzyme that hydrolyze MTX
Corticosteroids administration and urinary alkalization also recommended
37
Calcium folinate is
Derivative of tetrahydrofolic acid( active form of folic acid).It is not affected by dihydrofolate reductase inhibitor..used as folic acid rescue therapy in patients prescribed medium or high dose MTX
38
Calcium folinate other name
Leucovorin
39
Purine antimetabolite Azathioprine action
A prodrug metabolized in Vivo to mercaptopurine,it inhibits T and B lymphocyte proliferation,has Immunosuppressive and Antiproliferative effect
40
Clinical use of Azathioprine ( purine antimetabolite)
Chronic lupus erythematosus,severe ulcerative colitis or chrons disease
41
SE of azathioprine ( purine antimetabolite)
Mutagenicity and carcinogenicity
42
Purine antimetabolite ( Mycophenolate Mofetil action
Selective inhibition of inosine monophosphate dehydrogenase,inhibits T and B lymphocyte proliferation, immunosuppressive and Antiproliferative effects
43
Clinical use of Mycophenolate Mofetil ( purine antimetabolite)
Transplantology ( prevention of graft rejection),Chronic lupus erythematosus
44
Cyclosporine and Tacrolimus ( calcineurin inhibitors) action
Inhibits T and B lymphocyte proliferation, inhibition of IL2 secretion, Immunosuppressive and Antiproliferative effect
45
Clinical use of calcineurin inhibitors ( cyclosporine and Tacrolimus)
Transplantology, Atopic dermatitis (Tacrolimus in Topical therapy), Chronic lupus erythematosus ( cyclosporine
46
SE of cyclosporine and Tacrolimus (Calcineurin inhibitors)
Nephrotoxicity
47
TNF alpha action
Stimulate macrophage activity and has cytotoxic effect
48
Activated macrophages and lymphocyte are most prominent sources of pro inflammatory cytokines like
Il 2,1,6 and TNF alpha
49
Chronic lupus erythematosus treatment options
Cyclosporine ( CI), Mycophenolate Mofetil, Azathioprine, Methotrexate
50
Transplantology ( graft rejection) prevention
Mycophenolate Mofetil and cyclosporine and Tacrolimus
51
Multiple sclerosis
Autoimmunity demyelinating disease of brain and spinal cord, inflammatory reaction with T lymphocyte, diagnosed in young people aged 20 to 40,most common non traumatic disability in young people,most common form is relapsing remitting form of MS
52
Integrins are expressed in leukocytes ensures
Leukocyte adhesion and subsequent transmigration,it is a heterodimeric receptor with alpha and beta subunit
53
Infliximab is chimaeric meaning
75 % human and 25%mouse
54
TNF alpha inhibitors are
Infliximab and Adalimumab
55
TNF alpha inhibitors ( infliximab and Adalimumab) action
Inactive all TNF receptors-inhibit all responses and release of pro-inflammatory cytokines, affect lymphocyte and leukocyte migration,induce apoptosis of TNF producing cells,inhibit NF
Immunosuppressive effect
56
57
Clinical use of infliximab and Adalimumab ( TNF alpha inhibitors)
Rheumatoid arthritis, autoimmune disease like psoriasis, Crohn's disease, ulcerative colitis
58
Immunosuppressive caused by S-DMARD and B-DMARD increase risk of
Active and or latent infections
59
Anti integrins ( Natalizumab) action
Is a humanised monoclonal antibody against cell adhesion molecule alpha 4 integrin- inhibits transmigration of immune cells across BBB
Immunosuppressive effect
60
Natalizumab ( anti integrins) use
Relapsing remitting multiple sclerosis
61
Tyrosine kinase action
Cell growth and differentiation
62
TK inhibitors are small molecules that
Pass through cell membrane and act on target intracellularly
63
JAK ( Janus Kinase ) inhibitor
Blocks cytokine mediated signalling and transcription
64
Tofacitinib (TK inhibitor) action
Inhibition of JAK 1 or 3
65
Upadacitinib action ( TKi)
Selective inhibition of JAK 1
66
Inhibition of JAK supress
IL 2,4 and 6- Antiproliferative effect
67
Tyrosine kinase inhibitors ( Tofacitinib and Upadacitinib) use
Rheumatoid arthritis, Psoriatic arthritis, ulcerative colitis
68
SE of TK I ( Tofacitinib and Upadacitinib)
Severe infection due to immune aupression, opportunistic infection,risk of high dose venous thromboembolism
69
Contraindications for TK I (Tofacitinib and Upadacitinib)
Active or latent infection with M.tuberculosis
70
Peginterferon beta ( interferon receptor agonist) action
Activation of antiinflammatory cytokines IL 4 and 10, deactivate pro inflammatory cytokines ( IL 2,IFN gamma, TNF alpha), Inhibition of activated T lymphocyte migration
Immunosuppressive and Antiproliferative effect
71
Peginterferon is produced through
Recombinant DNA technology
72
Clinical use of peginterferon beta
Relapsing remitting multiple sclerosis
73
SE of of peginterferon beta
Influenza like symptoms upon initiation of treatment, hepatotoxicity, depression
74
Relapsing remitting multiple sclerosis treatment options
Peginterferon beta , Natalizumab
75
76
Ulcerative colitis treatment
Tofacitinib, Upadacitinib infliximab and Adalimumab, Azathioprine
77
Psoriatic arthritis treatment
Tofacitinib and Upadacitinib, methotrexate
78
Chrons disease treatment option
Methotrexate, Azathioprine, infliximab and Adalimumab
