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IMMUNOPHARMACOLOGY Flashcards

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1
Q

Cytotoxic Agents

A

Antimetabolites

Alkylating agents

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2
Q

Azathioprine
MOA
Drug interactions

A

Purine antimetabolite
Prodrug of 6-mercaptopurine converted to 6-MP
- 6-MP is converted to metabolites that inhibit de novo puine nucleotide synthesis–> suppression of B and T cell function of immunoglobulin production and of IL-2 secretion.

DI: Inactivation of drugs has to do with Xanthine oxidase

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3
Q

Glucocorticoids anti-inflammatory MOA

A

Inhibition of PLA2

Reduction of transcription of COX-2 (inflammatory cancer)

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4
Q

Glucocorticoids AE

A 
Short term use: HTN 
hyperglycemia 
immunosuppresion
psychotic reactions 
cognitive impairment

Long term use:
Myopathy
Cushing’s syndrome
osteoporosis

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5
Q

Glucocorticoids uses:

A 
Prevent treat transplant rejection
Treat autoimmune disorders such 
- RA
- SLE
- Psoriasis
- Asthma 
- IBD
In palliative care glucocorticoids arae used to alleviate pain; nausea and fatigue
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6
Q

Calcineurin inhibitors

MOA?

A 
Cyclosporine
- primarily metabolized by CYP 3A4
- forms a complex w/ cyclophilin (immunophilin).
- complex inhibits calcineurin
Tacrolimus
- Binds to FK-binding protein (FKBP)
- FKBP is an immunophilin
- Tacrolimus -FKBP complex inhibits calcineurin
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7
Q

Calcineurin

A

Phosphatase used to activat T- Cell specific Transcription factor (NFAT)

NFAT is required for induction of cytokine genes

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8
Q

Cyclosporine adverse effects

A 
Nephrotoxicity*: limiting and occurs in majority of patients
tremor
HTN
Hyperglycemia
Hyperlipidemia
Osteoporosis
Hirsutism*
Gum Hyperplasia*
- Very little bone marrow toxicity
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9
Q

Cyclosporine USES?

A

Organ transplant
Uveitis
Rheumatoid Arthritis
Psoriasis

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10
Q

Tacrolimus Adverse Effects

A 
Nephrotoxicity
Neurotoxicity*
Hyperglycemia
HTN
Hyperkalemia
GI complaints
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11
Q

Tacromlimus uses

A
  • transplant rejection prevention of kidneys liver and heart

- topical formulation is used for topical dermatitis and psoriasis

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12
Q

MOA of sirolimus a Proliferation signal inhibitor:

A

Sirolimus

  • structurel similar to tacrolimus
  • also binds to FKBP but does not inhibit calcineurin
  • inhibits Serine-threonine kinase mTOR*–>blocks IL-2-driven T- cell proliferation.
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13
Q

Sirolimus Adverse Effects?

A 
Myelosuppresion*
Hepatotoxicity
Diarrhea
Hypertriglyceridemia
Pneumonitis
Headache
  • Nephrotoxicity is less common than w/ calcineruin inhibitors!!!
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14
Q

Sirolimus uses

A

Renal transplantation
Sirolimus-eluting stents are used to inhibit restenosis of the blood vessels in patients with severe CAD by reducing cell proliferation.

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15
Q

Inhibitors of Angiogenesis MOA?

A

Thalidomide

  • MOA unclear
  • inhibits synthesis of TNF-a
  • now called an immunomodulatory drug
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16
Q

Thalidomide indications

A

“MEL”
Erythema nodosum
Leprosum
multiple myeloma

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17
Q

Cytotoxic agents

A

Antimetabolites:

  • Azathioprine
  • Methotrexate
  • Mycophenolat mofetil
  • Leflunomide

Alkylating agents:
Cyclophosphamide

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18
Q

Azathioprine AE:

A

AE:

  • Bone marrow suppression
  • GI disturbances
  • increase in infections and malignancies
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19
Q

Azathioprine inactivation depends on the action of what enzyme?
What drug interaction should be avoided when taking AZA?

A

Xanthine oxidase

Allopurinol: used for control of hyperuricemia. Patients receiving allopurinol should have the dose of azathioprine reduced.

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20
Q

AZAthioprine uses

A

Prevention of organ transplant rejection

severe RA

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21
Q

Methotrexate MOA

A

At low doses is used in Rheumatic diseases to inhibit Aminoimidazolecarboxamide ribonucleotide (AICAR) transformylase.
- accumulation of AMP–> increased adenosine–> immunosuppressive (potent inhibition of inflammation by adenosine).

AICAR tranformylase catalyzes the penultimate and final step in de novo purine biosynthesis which lead to synthesis of IMP.

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22
Q

Methotrexate AE

A 
Mucosal ulceration
Hypersensitivity pneumonitis
GI ulcerations
Nausea
Leukopenia
Anemia
cirrhosis is rare
Hepatotoxicity
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23
Q

Methotrexate toxicity can be reduced with?

A

Leucovorin

Folic acid

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24
Q

Methotrexate CIs

25
Methotrexate uses
``` "RAPPS" RA Psoriasis Psoriasis arthritis Ankylosing spondylitis SLE ```
26
Mycophenolate Mofetil | MOA?
converted to mycophenolic acid mycophenolic acid inhibits inosine monophosphate DH an enzyme in the de novo pathway of guanosinentriphosphate (GTP) synthesis. This suppresses both B and T lymphocyte activation. - lymphocytes lack enzymes necessary for the salvage pathway so they are susceptible to inhibitors of the de novo pathway
27
Mycophenolate Mofetil AE
``` Nausea vomiting diarrrhea abdominal pain headache HTN Reversible myelosuppression ```
28
Mycophenlate mofetil uses
Prophylaxis of transplant rejection | SLE
29
Leflunomide MOA
Pro drug of teriflunomide Teriflunomide inhibits dihydroorotate DH decreases levels of UMP UMP is essential for the synthesis of pyrimidines
30
Leflunomide AE
``` Diarrhea Reversible alopecia Rash Myelosupression Increases in aminotranferases activity CBC and liver function tests should be monitored Carcinogenic and teratogenic in animals Contraindicated in pregnancy ```
31
Leflunomide USES
"RaMS" RA SLE Myasthenia Gravis
32
Alkylating agents
Cyclophosphamide - one of the most effective immunosuppressive drugs available - destroys proliferating lymphoid cells - alkylates DNA and other molecules in resting cells
33
Cyclophosphamide AE
Infertiltiy Bone marrow suppression Hemorrhagic cystitis Rarely bladder carcinoma Acrolein a metabolite is responsible for urinary toxicities Long term use increases risk of infection and malignancy
34
Cyclophosphamide USEs
treat SLE and other autoimmune diseases. | may take 3-6 months to show benefit.
35
Hydrochloroquine AE
Hemolysis in patients w/ G6PD defeciency | Retinal damage: vision should be monitored
36
Sulfasalazine structure
consists of sulfapyridine and 5-aminosalicylic (5-ASA) connected by diazo bond.
37
Sulfasalazine MOA
Metabolized by bacteria in the colon to constituent moieties: - sulfapyridine is probably the active moiety in the tx. of rheumatoid arthritis. - 5-ASA moiety important in ulcerative colitis.
38
Sulfasalazine AE
``` Nausea vomiting Headache rash Neutropenia Thrombocytopenia is very rare Drug induced lupus is rare Hemolysis in patients with G6PD def. ```
39
Sulfasalazine uses
Ulcerative colitis Rheumatoid arthritis Crohn's disease Ankylosing spondylitis
40
Immunosuppressive Antibodies
Polyclonal antibodies: - Antilymphocyte (ALG) and Antithymocyte (ATG) Antibodies - Rho(D) Immune Globulin Monoclonal antibodies
41
Antilymphocytic globobulin (ALG) and Antithymocyte Globulin (ATG) uses
- Used before stem cell transplantation to prevent graft-versus-host reaction. - Also use for solid organ transplantation
42
Monclonal antibodies
TNF-a inhibitors - Infliximab - Adalimumab - Etanercept
43
Anti-TNF-a drugs adverse effects
- Cytopenias can occur: CBC should be monitored regularly - Serious infections are the most important potential adverse effects of TNF inhibition - Drugs should not be given to patients with an active infection - *Patients should be screened for latent TB infection before and during tx. w/ a TNF inhibitor. - Patients may be at risk for malignancies
44
Infliximab
- Chimeric monoclonal antibody - Binds with high affinity and specficity to humna TNF-a - Used in the tx. of rheumatoid arthritis; psoriatic arthirtis; ankylosing spondylitis; Crohn's disease; and ulcerative colitis.
45
Adalimumab
Fully humna IgG1 anti-TNF monoclonal antibody - Binds soluble TNF-a and prevents its interation with TNF receptors. - Used in the tx. of rheumatoid arthritis; psoriatic arthritis; ankylosing spondylitis; Crohn;s disease and ulcerative colitis.
46
Etanercept
Not a true Mab - Ligand-binding portion of a human TNF-a receptor fused to the Fc portion of human IgG1. - Binds to TNF-a and prevents it from interacting w/ its receptors.
47
Etanercept uses
``` RA Ankylosing spondylitis Plaque psoriasis polyarticular juvenile idiopathic arthritis psoriatic arthritis ```
48
Omalizumab MOA? USE?
- Anti-IgE recombinant humanized monoclonal antibody - Binds to IgE and prevents IgE from binding to mast cells and basophils thereby preventing release of inflammatory mediators after allergen expopsure - Used in asthma refractory to inhaled corticoids and evidence of allergic sensitization - also approved for chronic urticaria
49
Basiliximab
- IL-2 receptor antagonist - Chimeric human-mouse IgG - Binds to the IL-2 receptor - Used in combination w/ ther immunosuppressants to prevent transplant rejection.
50
Rituximab
- Chimeric murine-human monoclonal antibody that binds to the CD20 molecule on B lymphocytes. - Causes depletion of circulating B cells - Used for tx. of non-hodgkins lymphoma and chronic lymphocytic leukemia - Also approved for rheumatoid arthritis.
51
Anakinra MOA USE
- IL-1 receptor antagonist - Recombinant version of the naturally occurring human IL-1RA that prevents IL-1 from binding to its receptor. - Approved for moderate to severe rheumatoid arthritis
52
Abatacept MOA? USE?
- Fusion protein that interferes w/ T-cell activation - Used for moderate to severe rheumatoid arthritis - Used for moderate to severe polyarticular juvenile idiopathic arthritis.
53
Immunostimulants
Aldesleukin Interferons Bacillus Calmette-Guerin (BCG)
54
Aldesleukin MOA? USE?
- Recombinant interleukin-2 (IL-2) - IL-2 is lymphokine that promotes the production of cytotoxic T lymphocytes and activates NK cells. - Aldesleukin is indicated for the adjunctive treatment of renal cell carcinoma and malignant melanoma
55
Interferons | USE?
``` Hairy cell leukemia chronic myelogenous leukemia malignant melanoma Kaposi sarcoma hep B and C infections ```
56
Bacillus Calmette-Guerin (BCG)
attenuated live culture of Mycibacterium bovis - active against tumors MOA unknown - indicated for tx. and prophylaxis of carcinoma of the urinary bladder. ``` AE: hypersensitivity shock chills fever malaise immune complex disease ```
57
Drugs used to stop transplant rejection:
``` Glucocorticoids - prevent and treat Tacrolimus - prevention of rejection for HLK (heartLiverKidney) Azathioprine Mycophenolate - prophylaxis Basiliximab - renal transplant ```
58
Drugs used for rheumatoid arthritis
``` Glucocorticoids Cyclosporine Azathioprine (SEVERE) Methotrexate Leflunomide hydroxychloroquine (MILD) sulfasalzine Infliximab adalimumab Etanercept Rituximab Anakinra (moderate-->severe) Abatacept (moderate to severe) ```
59
Renal transplant drugs
Sirolimus | Basiliximab

Pharmacology (27 decks)

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