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MNI (immuno pharm) > L41- Immunopharmacology > Flashcards

L41- Immunopharmacology Flashcards

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1
Q

list the immunosuppressive agents

A
  • glucocorticoids
  • calcineurin inhibitors
  • proliferation signal inhibitors
  • angiogenesis inhibitors
  • cytotoxic agents
  • other agents
  • immunosuppressive Antibodies
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2
Q

immunosupressive agents are used for the following clinical situations….

A

(dampen immune response)

  • organ transplantation
  • auto-immune disease
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3
Q

Glucocorticoids:

  • (1) general immune effects
  • (2) MOA in terms of immune system
A

1- anti-inflammatory, immunosuppressive effects

2:
-binds cytosolic glucocorticoid receptor
-receptor complex translocates to nucleus
-binds GREs (glucocorticoid response elements) in promoter region of genes
-down-regulation of many inflammatory mediators
+
-dec PG synthesis

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4
Q

______ is the preferred glucocorticoid for immunosuppression, explain

A

dexamethasone- long half-life, low mineralocorticoid effects

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5
Q

list the immune uses of glucocorticoids

A
  • prevent/treat transplant rejection
  • autoimmune disorders: RA, SLE, psoriasis, asthma, IBD
  • neuropathic and bone pain
  • palliative care: alleviate pain, nausea, fatigue
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6
Q

Glucocorticoids AEs:

  • (1) short term use AEs
  • (2) long term use AEs
A

1- HTN, hyperglycemia, immunosuppression, psychotic reactions, cognitive impairment

2- myopathy, Cushing’s syndrome, osteoporosis

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7
Q

Cyclosporin uses

A

(calcineurin inhibitor)

  • organ transplants
  • uveitis
  • RA
  • psoriasis
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8
Q

list the many AEs for Cyclosporin

A

(calcineurin inhibitor)

  • **nephrotoxicity (most common reason to stop drug –> RAAS activation + endothelin release)
  • tremor
  • HTN
  • hyperglycemia, hyperlipidemia
  • osteoporosis
  • hirsutism
  • gum hyperplasia

-CYP3A4 metabolism –> drug interactions

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9
Q

list the calcineurin inhibitors

A
  • cyclosporin

- tacrolimus

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10
Q

Calcineurin is a (1) type enzyme, which functions to activate (2) that is required for induction of (3).

A

1- phosphatase (dephosphorylation)

2- NFAT (T-cell specific transcription factor)

3- CK gene upregulation (IL-2 gene)

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11
Q

Cyclosporin MOA

A
  • forms complex with cyclophilin (an immunophilin)
  • complex inhibits calcineurin
  • prevents dephosphorylation of NFAT
  • no CK (IL-2) production
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12
Q

Tacrolimus uses

A

(calcineurin inhibitor)

  • transplant rejection: kidney, liver, heart
  • topical: psoriasis, atopic dermatitis
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13
Q

Tacrolimus AEs

A

(calcineurin inhibitor, less AE severity than cyclosporin)

  • nephrotoxicity, neurotoxicity
  • HTN, hyperkalemia, hyperglycemia
  • GI issues
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14
Q

Tacrolimus MOA

A

(calcineurin inhibitor)

  • forms complex with FKBP (FK-binding protein, an immunophilin)
  • complex inhibits calcineurin
  • prevents dephosphorylation of NFAT
  • no CK (IL-2) production
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15
Q

______ is the main proliferation signal inhibitor

A

Sirolimus

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16
Q

Sirolimus uses

A

(proliferation signal inhibitor)
-renal transplant

-Coronary Stents: sirolimus released –> inhibits restenosis of BV via reduction in cell proliferation

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17
Q

Sirolimus AEs

A

(proliferation signal inhibitor)

  • myelosuppression
  • hepatotoxicity
  • hypertriglyceridemia
  • pneumonitis
  • diarrhea
  • HA
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18
Q

Sirolimus MOA

A

(proliferation signal inhibitor- note it has similar structure to Tacrolimus a calcineurin inhibitor)

  • binds FKBP (FK binding protein, an immunophilin) [–> no calcineurin inhibitor]
  • inhibits serine-threonine kinase mTOR
  • blocks IL-2 driven T-cell proliferation
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19
Q

______ is the main angiogenesis inhibitor

A

Thalidomide

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20
Q

Thalidomide uses

A

(angiogenesis inhibitor)
erythema nodosum leprosum
multiple myeloma

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21
Q

Thalidomide MOA

A

(angiogenesis inhibitor)
mostly unclear:
-inhibits TNF-α synthesis
-inhibits angiogenesis

technically an immunomodulatory drug

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22
Q

list the Cytotoxic agents

A

antimetabolites:

  • azathioprine
  • methtrexate (MTX)
  • mycophenolate mofetil
  • leflunomide

alkylating agents:
-cyclophosphamide

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23
Q

Azathioprine:

  • (purine/pyrimidine) anti-metabolite
  • prodrug of (2) which functions to suppress (3)
A

1- purine

2- 6-MP (6-mercaptopurine)

3- B and T cell function, Ig production, IL-2 secretion

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24
Q

Azathioprine uses

A
  • organ transplant

- severe RA

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25
Azathioprine: - (1) AEs - (2) drug interactions
1- BM suppression, GI issues, inc infections and malignancies 2- allopurinol --> give lower dose as inactivation requires xanthine oxidase
26
MTX uses
- RA - psoriasis, psoriatic arthritis - ankylosing spondylitis - SLE
27
MTX MOA
(low doses) Rheumatic Diseases: -inhibition of aminoimidazolecarboxamide ribonucleotide (AICAR) transformylase -AMP accumulation -converted to adenosine extracellularly -adenosine is potent inhibitor inflammation
28
MTX AEs + contraindication
- nausea, GI ulcerations - mucosal ulcers - leukopenia, anemia - hepatotoxicity, (rarely cirrhosis) - hypersensitivity pneumonitis Contraindicated in pregnancy
29
MTX toxicity can be reduced with co-administration of....
- folic acid | - leucovorin
30
Mycophenolate MOA
- converted to mycophenolic aid - inhibits ionosine monophosphate dehydrogenase - dec Guanosine synthesis -suppresses B, T cell activation -- particularly susceptible to inhibition b/c lacking enzymes in salvage pathway
31
Mycophenolate uses
- prophylaxis transplant rejection | - SLE
32
Mycophenolate AEs
- n/v/d, abdominal pain - HTN, HA - reversible myelosuppression
33
______ is the simple reason why anti-metabolites are effective as immunosuppressants
B/T-lymphocytes are particularly susceptible to inhibition b/c they lack the necessary enzymes for the salvage pathway
34
Leflunomide MOA
- prodrug of turiflunomide - turiflunomide inhibits dihyrdrooroate dehydrogenase - dec UMP levels
35
Leflunomide uses
- RA - SLE - myasthenia gravis
36
Leflunomide AEs
- diarrhea - rash, reversible alopecia - myelosuppression - inc aminotransferase activity - cardiogenic / teratogenic in animals - contraindicated in pregnancy
37
Cyclophosphamide MOA (briefly / generally)
- destroys proliferating lymphoid cells | - alkylates DNA / other molecules in resting cells
38
Cyclophosphamide uses
SLE + others
39
Cyclophosphamide AEs
- infertility - BM suppression - hemorrhagic cystitis via acrolein - bladder cancer (rare) -- general inc of infection and malignancy with long-term use
40
list the 'other' agents of immunosuppression
- hydroxychloroquine | - sulfasalazine
41
Hydroxychloroquine MOA
unclear anti-inflammatory mechanism
42
Hydroxychloroquine uses
- RA (moderate effect, well-tolerated) - SLE note- often in combination with MTX, sulfasalaxine and may require 3-6 mos to show clinical benefit
43
Hydroxychloroquine AEs
(serious and rare) - hemolysis in G6PD deficiency - retinal damage (monitor vision)
44
Sulfasalazine: - (1) structure - (2) metabolism allows for (3) function
Sulfasalazine = sulfapyridine + 5-aminosalicylic acid (5-ASA) - connected via diazo bond - Sulfasalazine is metabolized into moieties by bacteria in colon Sulfapyridine ---> RA Tx 5-ASA --> ulcerative colitis Tx
45
Sulfasalazine uses
- UC, CD - RA - ankylosing spondylitis
46
Sulfasalazine AEs
- n/v - HA - rash - neutropenia, hemolysis in G6PD def. Rare: thyrombocytopenia, drug-induced lupus
47
list the immunosuppressive POLYclonal Abs and their uses
ALG, ATG (antilymphocyte and antithymocyte globulin): - stem cell transplant - solid organ transplant Rho(D) immune globulin: an IgG against Rho(D) Ag on RBCs -prevents Rh hemolytic disease in newborns
48
list the TNF-α inhibitor monoclonal antibodies
- adalimumab - infliximab - etanercept
49
list the 'other' immunosuppressuve monoclonal antibodies
- omalizumab - basiliximab - rituximab
50
list some of functions TNF-α signalling
-inc inflammation (macrophages) - inc cell infiltration (endothelium) - inc angiogenesis (endothelium) - inc CRP (hepatocytes) - cartilage degradation via MMPs (synoviocytes)
51
match the Ab structure with the TNF-α monoclonal antibody: - (1) contains ligand-binding portion of human TNF-α receptor fused to Fc portion of human IgG - (2) chimeric monoclonal Ab - (3) fully human IgG1 anti-TNF monoclonal Ab
1- etanercept (not true mab) 2- infliximab 3- adalimumab
52
list the uses for monoclonal anti-TNF antibodies
All: - RA - psoriatic arthritis - ankylosing spondylitis Infliximab, Adalimumab: -CD, UC
53
monoclonal Anti-TNF antibodies: - screen for (1) before starting therapy - monitor for (2) during therapy - never give (3) to people on these Abs - most AEs result from (4) activity
1- Tb, HBV infections 2- CBC for cytopenias 3- live vaccinations + Pts w/ infections 4- TNF inhibition: inc infections, don't give to infected Pts
54
list the AEs of TNF inhibitors
- inc risk of malignancies and GI ulcers - anti-drug Ab complexes formation --> interferes with efficacy + correlates w/ infusion site reaction - exacerbate HF
55
Omalizumab: - (1) MOA - (2) uses
1- anti-IgE recombinant humanized monoclonal Ab --> prevents IgE from binding/activating mast cells and basophils --> prevents release of inflammatory mediators after allergen exposure 2: - asthma with allergy sensitization - chronic urticaria
56
Basiliximab: - (1) structure - (2) MOA - (3) uses
1- chimeric human-mouse IgG 2- IL-2 receptor antagonist -- binds and blocks IL-2 receptor 3- prevent transplant rejection
57
Ritusimab: - (1) structure - (2) MOA - (3) uses
1- chimeric murine-human monoclonal Ab 2- binds CD20 on B cells --> depletion of circulationg B cells 3: - non-Hodgkin's lymphoma - chronic lymphocytic leukemia - note: approved for RA
58
Anakinra: - (1) structure - (2) MOA - (3) uses
1- recombinant human IL-1RA 2- IL-1 receptor antagonist --> prevents IL-1 binding its receptor 3- moderate to severe RA
59
Abatacept: - (1) MOA - (2) uses
1- fusion protein --> interferes with T cell activation 2: - moderate to severe RA - polyarticular juvenile idiopathic arthritis
60
list the immunostimulants
Aldesleukin IFN-α, β, γ BCG- bacillus calmette-guerin
61
Aldesleukin: - (1) structure / MOA - (2) uses
1- recombinant IL-2 2- renal cell carcinoma, malignant melanoma
62
list the functions for each IFN
IFN-α: HBV/HCV infections, hairy cell leukemia, CML, malignant melanoma, Kaposi's sarcoma IFN-β: relapsing MS IFN-γ: chronic granulomatous disease
63
BCG: - (1) structure - (2) MOA - (3) uses - (4) AEs
(Bacillus Calmette-Guerin) 1- attenuated live culture of Mycobacterium bovis 2- unknown --> active against tumors 3- Tx/prophylaxis urinary bladder carcinoma 4: - fever, chills, malaise - hypersensitivity, immune complex disease, shock

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