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Pharmacology > Immunosuppressants + > Flashcards

Immunosuppressants + Flashcards

1
Q

bDMARDs

A 
Anti TNF alpha:
Etanercept
Infliximab
Adalimumab
Golimumab
Immunomodulating:
Anakinra
Belimumab
Abatacept
Tocilizimab

Immunosuppressive
Rituximab

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2
Q

csDMARDs

A 
Methotrexate 
Leflunomide 
Hydroxychloroquine
Azathioprine
Sulfasalazine
Cyclosporine 
Cyclophosphamide
Mycocephenolate Mofetil
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3
Q

tsDMARD

A

Tofacitinib

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4
Q

Immunosuppressives

A 
Leflunomide
Teriflunomide
Corticosteorids: Glucocorticoids
Calcineurin and mTOR inh: Cyclosporine, Tacrolimus, Sirolimus, Everolimus, Temsirolimus
Tofecitinib
Azathioprine 
Mycocephenolate Mofetil
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5
Q

Teriflunomide - MoA

A

Same as Leflunomide. Inhibits leukocyte & T-cell proliferation by inhibiting pyrimidine synthesis (DNA replication, RNA synthesis, protein synthesis) in immune cells.

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6
Q

Teriflunomide - Clinical use

A

Relapsing-remitting multiple sclerosis.

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7
Q

Teriflunomide - Contraindication

A

Pregnancy and patients with severe liver disease.

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8
Q

Teriflunomide - Adverse effects

A

Same as Leflunomide

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9
Q

Glucocorticoids - MoA

A

Biochemical level:, their actions on gene expression decrease the synthesis of prostaglandins, leukotrienes, cytokines, and other signaling molecules that paricipate 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.

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10
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

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11
Q

Glucocorticoids - Adverse effects

A 
Adrenal suppression
Growth inhibition
Muscle wasting
Osteoporosis
Salt retention
Glucose intolerance
Behavioral changes
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12
Q

Calcineurin and mTOR inhibitors - MoA

A

Interfere with T-cell function by binding to immunophilins.

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13
Q

Calcineurin and mTOR inhibitors - Clinical use

A

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

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

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14
Q

Cyclosporine - MoA

A

Binds to cyclophilin –> completely inhibits calcineurine

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15
Q

Cyclosporine and Tacrolimus - Clinical use

A

Some autoimmune diseases:

RA, uveitis, psoriasis, asthma, DIA1

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16
Q

Cyclosporine and Tacrolimus - Adverse effects

A 
Most common:
Renal dysfunction, hypertension,
neurotoxicity 
Also:
Hyperglycemia, hyperlipidemia, cholelithiasis.
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17
Q

Cyclosporine - Interaction

A

slow hepatic metabolism by CYT P-450

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18
Q

Tacrolimus - MoA

A

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

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19
Q

Cyclophosphamide - MoA

A

Cross-links DNA to prevent cell replication. It suppresses T- cell and B-cell.

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20
Q

Cyclophosphamide - Clinical use and Adverse effects

A

SLE, vasculitis, Wegener’s granulomatosis.

Adverse effects: Large doses: risk of pancytopenia.
May cause hemorrhagic cystitis which can be treated or prevented with mesna.

21
Q

Sirolimus and analogs - 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

22
Q

Sirolimus and analogs - Clinical use

A

Prevent restenosis after coronary angioplasty.

Everolimus: immunosuppressant
Everolimus and temsirolimus: cancers

23
Q

Sirolimus and analogs - Adverse effects and Contraindication

A

Hypertriglyceridemia
Hepatotoxicity
Diarrhea
Myelosuppression.

Pregnancy

24
Q

Tofecitinib (Xeljanz) - MoA

A

Selectively inhibits all members of the Janus kinase family.

25
Q

Tofecitinib (Xeljanz) - Clinical use

A

Adults with moderate to severe RA.
Prevent solid organ allograft rejection.
Inflammatory bowel disease

26
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.

27
Q

Mycocephenolate Mofetil - Clinical use

A

Sole agent in kidney, liver and heart transplantations

28
Q

Mycocephenolate Mofetil - Special consideration

A

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

29
Q

Mycocephenolate Mofetil - Adverse effects

A

GI distrubances
Myelosuppression
Neutropenia

30
Q

Thalidomide - MoA

A

Suppression of TNF-α production, increased IL-10, reduced neutrophil phagocytosis, altered adhesion molecule expression, and enhanced cell-mediated immunity.
Inh il-2, angiogenesis, tnf alpha

31
Q

Thalidomide - Clinical use

A 
Leprosy
Immunologic diseases (systemic lupus)
Anticancer 
Aphthous ulcers
Wasting syndrome in AIDS patients.
32
Q

Thalidomide derivatives and their clinical use

A

Lenalidomide and Pomalidomide

Multiple myeloma

33
Q

Ustekinumab- MoA

A

IgG monoclonal antibody. Prevents binding of the p40 subunit of both IL-12 and IL-21

34
Q

Ustekinumab - Clinical use

A

IV for Crohn

Adult with PsA

Plaque psoriasis and Crohn`s disease.

35
Q

Ustekinumab - Adverse effects

A

Upper respiratory tract infection.

Reversible posterior leukoencephalopathy syndrome.

36
Q

Secukinumab - MoA

A

IgG1 monoclonal antibody. Selectively binds to and inhibits IL-17A

37
Q

Secukinumab - Clinical use

A

Moderate to severe plaque psoriasis.

Psoriatic arthritis.

Ankylosing spondylosis

38
Q

Secukinumab - Adverse effects

A

Infection is a common side effect.

Nasopharyngitis

It may exacerbate Crohn`s disease.

39
Q

Tofecitinib - Adverse effects and interactions

A

Metabolized by CYP-450 in the liver. Should be screened for latent or active tuberculosis- Not given to patients with severe hepatic disease.

Increase risk of infection.
Upper respiratory tract infection and urinary tract infection.

40
Q

Belimumab - MoA

A

Inhibits B-lymphocyte stimulator (BLyS)

41
Q

Belimumab - Clinical use

A

Approved only for the treatment of adult patients with active, seropositive SLE who are receiving standard treatment.

42
Q

Belimumab - Contraindication

A

Should not be used in patients with active renal or neurological manifestations of SLE.

43
Q

Belimumab - Adverse effects

A

Nausea, diarrhea, and respiratory tract infections.

Increased risk of infections.

Cases of depression and suicide have been reported in patients receiving belimumab, although these patients may have had neurologic SLE.

Anaphylaxis.

44
Q

Azathioprine - MoA

A

Acts through its metabolite 6-thioguanine, which suppresses inosinic acid synthesis, B- cell and T-cell function, Ig production, and IL-2 secretion.

45
Q

Azathioprine - Clinical use

A

RA
Prevention of kidney transplant rejection in combo with other immune suppressants.

PA, reactive arthritis, polymyositis, SLE, maintenance of remission in vasculitis, and Behcet`s disease.
Scleroderma

46
Q

Azathioprine - Adverse effects

A

Bone marrow suppression (low TPMT).

  • Increased risk of infection.
  • lymphoma risk.
  • rarely, fever, rash and hepatotoxicity signal acute allergic reactions.
47
Q

Rituximab - MoA

A

Monoclonal antibody that binds to protein CD20 and cause apoptosis. Found on the surface of B cells.

48
Q

Rituximab - Clinical use

A

Moderate- severe RA in combo w methotrexate in patients with an inadequate response to one or more TNF-alpha antagonist.

Granulomatosis with polyangiitis (Wegener’s granulomatosis) and microscopic polyangiitis.

Lymphomas and leukemia.

49
Q

Rituximab - Adverse effects

A

30% develop rash.
IgG and IgM may decrease.

Serious, and sometimes fatal, bacterial, fungal, and viral infections are reported 1y of last dose.

Associated with reactivation of HBV infection.

Fatal mucocutaneous reactions.

Different cytopenia`s.

Pharmacology (55 decks)

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