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Pharm (M2) > Immunopharmacology > Flashcards

Immunopharmacology Flashcards

1
Q

What are the 4 classes of immunopharm drugs?

A
  1. calcineurin inhibitor
  2. mTOR inhibitor
  3. cytotoxic agent
  4. immunosuppressant antibodies
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2
Q

Name the drugs under each class.

A
  1. cyclosporine A, tacrolimus
  2. Sirolimus (rapamycin)
  3. azathioprine, MMF & MPS, Fingolimod
  4. polyclonal - lymphocyte & thymocyte antibodies
    monoclonal
    - Anti IL2R alpha
    - CTLF4 Ig Fusion protein
    - Anti BAFF mAb
    - Anti TNF alpha
    - Anti IL5
    - Anti IL4 alpha
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3
Q

MOA

A
  1. binds to cyclophilin
    - chaperone in immunosuppression// PPIase (peptidyl-prolyl cistrans isomerase)
  2. CsA-cyclophilin complex inhibits calcineurin, a Ca2+-calmodulin Ser/Thr phosphatase
  3. prevent desphosp + translocation of NF-AT
  4. inhibits cytokine prdn (IL-2,TNFa,IFNgamma)
  5. inhibits T/B/CTL cells proliferation but primarily T cells
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4
Q

Use

A

oral/IV/ **ophthalamic

  1. transplants: kidney, liver, pancreas, heart
  2. uveitis, RA, psoarisis
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5
Q

Adverse effects

A
  1. hypertension, hyperlipidemia, hyperglycemia
  2. gum hyperplasia
  3. nephrotoxicity, neurotoxicity
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6
Q

MOA

A
  1. binds to immunophilin FKBP-12

- FKBP: chaperone in immunosuppr + PPIase

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7
Q

Use

A

oral/IV/**topical macrolide

  1. more potent than CsA
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8
Q

Adverse effects

A
  1. hypertension, hyperlipidemia, hyperglycemia

2. nephrotoxicity, neurotoxicity

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9
Q

MOA

A
  1. sirolimus:FKBP immunophilin complex
  2. binds & inhibits mTOR (ser/thr kinase)
  3. inhibiting 70kDa S6 kinase
  4. growth arrest from G1 to S phase
  5. maintain repressor activity of 4E-BP1
  6. inhibits cytokine-mediated proliferation of T & B cells
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10
Q

MOA

A

against receptors in immune system

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11
Q

Adverse effects

A
  1. hypertension, hyperlipidemia, hyperglycemia

2. nephrotoxicity, neurotoxicity

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12
Q

Use

A
  1. anti proliferative & anti angiogenic activities
  2. sirolimus-eluting coronary stents to prevent arterial restenosis
  3. gd combo: sirolimus + cyclosporine A but renal impairment
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13
Q

Adverse effects

A
  1. hypertension, hyperlipidemia, hyperglycemia

2. thrombocytopenia

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14
Q

*Azathioprine

A

other 2 include cyclophosphamide (alkylating) + methotrexate (DHFR inhib)

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15
Q

MOA

A
  1. prodrug–> converted to 6MP –> 6TG

2. 6TG impedes DNA synthesis, de novo purine synthesis –> decrease proliferation of lymphocytes

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16
Q

Use

A
  1. renal transplant &

2. other autoimmune disorders using triple therapy (calcineurin inhibitor + steroid + cytotoxic agent azathioprine)

17
Q

Adverse effects

A
  1. bone marrow suppression: leukopenia, thrombocytopenia, anaemia
  2. bleeding
  3. GI toxicity
  4. lymphoma & neoplasia
18
Q

MOA

A
  1. converted to mycophenolic acid
  2. inhibit preferentially type II (inducible) IMPDH
  3. inhibit de novo guanosine synthesis
19
Q

Use

A
  1. less bone marrow suppression & GI toxicity than aza
  2. more selective T/B antiproliferative effects
  3. suppress antibody prdn
  4. inhibit leukocyte recruitment to graft site
20
Q

Adverse effects

A
  1. diarrhoea
  2. neutropenia
  3. anemia
  4. hypertension
21
Q

MOA

A
  1. prodrug phosph to FTY720P
  2. S1PR agonist
  3. activates S1P (1,3,4,5)
  4. S1P1 & 4 promotes chemokine mediated lymphocyte homing + decrease circulating lymphocyte
22
Q

Use

A

multiple sclerosis

23
Q

Adverse effects

A
  1. first dose negative cardiac chronotropic effect due to activation of S1P1,3 in SA nodal cells
24
Q

*Polyclonal antibodies (non selective IgG)

A

lymphocyte antibody- atgam

thymocyte antibody- thymoglobulin

25
Q

MOA

A
  1. opsonisation
  2. complement-dependent cytotoxicity
  3. ADCC
  4. depletion of t cells
  5. cross link TCR– anergy
26
Q

Use

A

-

27
Q

Adverse effects

A
  1. first dose effect cytokine release syndrome (fever, chills. hypotension)
  2. serum sickness/ thromobcytopenia/ leukopenia
  3. dev anti foreign IgG antibodies
  4. histiocytic lymphoma at site injection

Pharm (M2) (13 decks)

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