Immunopharm Flashcards

1
Q

Dexamethasone

A

Glucocorticoid

Induce annexin I (inhibit Phospholipase A2)
Repress COX-2 (via NF-kB inhibition)
Induce MAPK phosphatase I (inhibits MAPKs –> antiinflammatory effects)

Treat cancer-related pain.

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2
Q

Prednisone & Methylprednisone

A

Glucocorticoid

Induce annexin I (inhibit Phospholipase A2)
Repress COX-2 (via NF-kB inhibition)
Induce MAPK phosphatase I (inhibits MAPKs –> antiinflammatory effects)

Treat & Prevent Transplant Rejection

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3
Q

Prednisolone

A

Glucocorticoid

Induce annexin I (inhibit Phospholipase A2)
Repress COX-2 (via NF-kB inhibition)
Induce MAPK phosphatase I (inhibits MAPKs –> antiinflammatory effects)

Treat autoimmune disorders

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4
Q

Cyclosporine

A

Calcineurin Inhibitor

Forms complex with cyclophilin which inhibits calcineurin. Inhibits cytokine transcription. Metbolized by CYP3A4. Nephrotoxicity.

Used in organ transplantation, uveitits, RA, psoriasis.

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5
Q

Tacrolimus

A

Calcineurin Inhibitor

Forms complex with FK-binding protein which inhibits calcineurin. Inhibits cytokine transcription. Nephrotoxicity.

Used in organ transplantation. Topical formulation used for atopic dermatitis & psoriasis.

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6
Q

Sirolimus

A

T-Cell proliferation inhibitor

Structurally similar to Tacrolimus. Binds FKBP. Complex inhibits mTOR which is needed for IL-2 driven T-Cell proliferation.
Less nephrotoxic than Calcineurin inhibitors.

Used in renal transplantation & coronary stents.

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7
Q

Thalidomide

A

Unclear mechanism of action.

Inhibits TNF-a synthesis & angiogenesis.

AE: Teratogen, peripheral neuropathy, inc risk of DVT

Treat erythema nodosum leprosum & multiple myeloma.

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8
Q

Azathioprine

A

Antimetabolite

Pro-drug of 6-mercaptopurine. Inhiits de-novo purine synthesis. Suppresses B & T Cell function.

Inactivated by Xanthine Oxidase –> Adverse interaction with Allopurinol.

Prevent organ transplant rejection & treat severe RA.

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9
Q

Methotrexate

A

Antimetabolite

Inhibits AICAR transformylase. AICAR accumulates & inhibits AMP deaminase. Leads to accumulation of AMP –> adenosine –> anti-inflammatory.

AE: Nausea, ulcers, leukopenia, anemia, dose-related hepatotoxicity, pneumonitis, stomatitis. AE worse in pt with renal dysfunction.

Treat: DOC for RA, psoriasis, ankylosing spondilitis, lupus, graft vs host disease.

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10
Q

Leucovorin

A

Helps reduce methotrexate toxicity in RA treatment.

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11
Q

Mycophenolate Mofetil

A

Antimetabolite

Prodrug of Mycophenolic Acid. Inhibits IMP dehydrogenase –> inhibit GTP synthesis –> suppresses B & T cell activation.

AE: Nausea, vomiting, diarrhea, abd pain, htn, headache, myelosuppression.

Used as prophylaxis of transplant rejection.

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12
Q

Leflunomide

A

Antimetabolite

Prodrug of teriflunomide. Inhibits dihydroorate dehydrogenase, decreases levels of UMP, inhibits pyrimidine synthesis.

AE: Diarrhea, alopecia, rash, myelosuppression, carcinogenic, teratogenic.

Only approved use is RA. Efficacy seen in Lupus & myasthenia gravis.

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13
Q

Cyclophosphamide

A

Alkylating Agent

Alkylates DNA molecules, destroys proliferating lymphoid cells.

AE: Dose-limiting infertility, bone marrow suppression, hemorrhagic cystitis, bladder carcinoma. Long term use inc risk of infection & malignancy.
Acrolein is a metabolite, responsible for urinary toxicity.

Treats lupus & other autoimmune diseases.

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14
Q

Tofacitinib

A

JAK inhibitor

Inhibits JAK thus inhibits hematopoesis & immune cell function in response to cytokines & growth factors.

Treats moderate-severa RA. Similar effect to anti-TNF-a inhibitors.

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15
Q

Hydroxychloroquine

A

Unclear mechanism of action.

AE: Hemolysis in pt with G6PD def, retinal damage.

Treat mild RA & lupus.

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16
Q

Sulfasalazine

A

Metabolized to Sulfapyridine & 5-aminosalicylic (5-ASA). Sulfapridine is active metabolite for RA. 5-ASA active for ulcerative colitis.

AE: Nausea, vomiting, headache, rash, neutropenia, thrombocytopenia, lupus, hemolysis in pt with G6PD def.

Used to treat ulcerative colitis, RA, crohn’s, ankylosing spondylitis.

17
Q

Rho(D) globulin (Rhogam)

A

Human IgG

Ab against Rho (D) RBC antigen.

Given to R- women with R+ fetus in pregnancy to prevent hemolytic disease of the newborn.

18
Q

Adalimumab

A

Human IgG1

Ab against TNF-a.

AE: Cytopenia, inc risk of inection, inc risk of malignancies, ulcers, anti drug abs, exacerbate heart failure. No live vaccines, check for ongoing infection before administering.

Treats RA, psoriatic arthritis, ankylosing spondylitis, Crohn’s, ulcerative colitis

19
Q

Infliximab

A

Chimeric monoclonal Ab

Ab against TNF-a

AE: Cytopenia, inc risk of inection, inc risk of malignancies, ulcers, anti drug abs, exacerbate heart failure. No live vaccines, check for ongoing infection before administering.

Treats RA, psoriatic arthritis, ankylosing spondylitis, Crohn’s, ulcerative colitis

20
Q

Etanercept

A

Not a true Monoclonal Ab

Ligand binding portion of TNF-a receptor + Fc portion of human IgG1.

AE: Cytopenia, inc risk of inection, inc risk of malignancies, ulcers, anti drug abs, exacerbate heart failure. No live vaccines, check for ongoing infection before administering.

Treats RA, psoriatic arthritis, ankylosing spondylitis, plaque psoriasis.

21
Q

Omalizumab

A

Anti IgE antibody

Used in patients >12 for asthma & chronic utricaria.

22
Q

Rituximab

A

Anti CD20 antibody

Depletes circulating B Cells

Used to treat non-Hodgkin’s Lymphoma and Chronic Lymphocytic Leukemia.
Also treat RA in combination with methotrexate.

23
Q

Tocilizumab

A

Anti IL6 receptor antibody.

Prevents IL6 action.

AE: elevated liver funct tests, hyperlipidemia, neutropenia, htn, infusion related injection site reactions.

Treat RA, giant cell arteritis, juvenile idiopathic arthritis, cytokine release syndrome.

24
Q

Sarilumab

A

Anti IL6 receptor antibody.

Prevents IL6 action.

AE: elevated liver funct tests, hyperlipidemia, neutropenia, htn, infusion related injection site reactions.

Treat RA

25
Q

Abtacept

A

Fusion protein that interferes with T-cell activation

Treat moderate to severe RA, polyarticular juvenile idiopathic arthritis.

26
Q

Aldesleukin

A

Immunostimulant

Recombinant IL-2. Activates NK cells, promotes production of CTLs.

Adjunctive treatment of renal cell carcinoma & malignant melanoma.

27
Q

Interferons

A

Interferon-a in leukemias, melanoma, sarcoma, Hep B & C

Interferon-b in relapsing MS

Interferon-y in chronic granulomatous disease

28
Q

BCG

A

Live culture of Bacillus Calmette & Guerin strains of mycobacterium.

Active against tumors due to unclear mechanism.

Treatment & prophylaxis of urinary bladder carcinoma.