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Introduction to Pharmacology > Immunosuppressants > Flashcards

Immunosuppressants Flashcards

1
Q

How do cytotoxic drugs, lymphocyte drugs, and glucocorticoids work as immunosuppressants?

A

CYTOTOXIC = cause cell necrosis and apoptosis, or impair proliferation

LYMPHOCYTE = suppress the immune system by inhibiting function of lymphocytes and production of cytokines

GLUCOCORTICOIDS = affect innate and adaptive immunity

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2
Q

What are the main 3 classifications of immunosuppressants? What other 2 immunomodulators can be used?

A
  1. ANTIMETABOLITES - purine synthesis inhibitors (Azathioprine, Mycophenolic acid), pyrimidine synthesis inhibitors (Leflunomide)
  2. MATRIx METALLOPROTINASE INHIBITORS - tetracycline
  3. CYTOKINE INHIBITORS - IL-2 (cyclosporine, tacrolimus), TNFα (pentoxifylline)
  • gold therapy: auranofin, gold sodium thiomalate
  • niacinamide
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3
Q

What is Azathioprine (Imuran)? What is its 2 mechanisms of action?

A

purine synthesis inhibitor that inhibits the cellular synthesis of nucleic acids required for RNA and DNA synthesis resulting in cellular proliferation and function arrest

  • inhibits DNA synthesis in B- and T-lymphocytes
  • blocks CD28 signaling on T-cells, resulting in impaired RNA synthesis
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4
Q

How is Azathioprine (Imuran) most commonly used?

A

in conjunction with steroids to treat immune-mediated diseases, like:
- immune-mediated hemolytic anemia and thrombocytopenia
- colitis and skin disease
- myasthenia gravis
- IBD
- immune-mediated inflammatory conditions and perianal fistulas in dogs
- autoimmune skin diseases in horses

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5
Q

What is important to note about Azathioprine pharmacokinetics? Is it given to cats?

A

its a prodrug that is well absorbed in the gut

NO - causes toxicity

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6
Q

What are 4 possible adverse effects associated with Azathiprine (Imuran)?

A
  1. bone marrow suppression, leadint to an increased risk for infection
  2. fatal leukopenia and thrombocytopenia
  3. hepatotoxicity and acute pancreatitis
  4. mutagenic, teratogenic, carcinogen
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7
Q

What is Leflunomide? What is its mechanisms of action?

A

pyrimidine synthesis inhibitor

inhibits mitochondrial enzyme necessary for de novo pyrimidine synthesis, particularly affecting B- and T-lymphocyte synthesis

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8
Q

What is Leflunomide most commonly used to treat? What are 3 other possible uses?

A

immune-mediated polymyositis

  1. immune-mediated hemolytic anemia and thrombocytopenia
  2. multifocal nonsuppurative encephalitis/meningomyelitis
  3. Evan’s syndrome
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9
Q

Are adverse effects common in dogs with use of Leflunomide?

A

no, but can cause Gi disturbances and anemia

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10
Q

What is polymyositis? What are the 3 main causes?

A

relatively common inflammatory disease in dogs that causes muscle weakness and fatigue

  1. infectious agents: bacteria, viruses, protozoa, parasites
  2. immune-mediated: autoimmune
  3. paraneoplastic: tumor invading muscles
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11
Q

What are the 5 signs of polymyositis in dogs?

A
  1. generalized weakness that worsens with exercise
  2. muscle swelling and pain
  3. anorexia
  4. exercise intolerance
  5. muscle wasting
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12
Q

What are the 4 most common treatments of polymyositis?

A
  1. Azathioprine
  2. Leflunomide
  3. Cyclosporine
  4. Prednisone
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13
Q

What is cyclosporine? How does it work?

A

IL-2 inhibitor

binds to CsA, which blocks calcineurin, making it unable to dephosphorylate NF-ATc to block IL-2 production

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14
Q

What are the main pharmacological effects cyclosporine has on T-lymphocytes and mast cells?

A

T-CELLS: decreases the production of IL-2, 3, 4, G-CSF, and TNFα, and decreases the proliferation of CD4+ and CD8+ lymphocytes, increases TGFβ (inhibits IL-2)

MAST CELLS: decreases histamine release in canine mast cells

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15
Q

What are the 3 main uses of cyclosporine?

A
  1. keratoconjunctivitis sicca
  2. perianal fistulas
  3. IMHA in conjunction with glucocorticoids
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16
Q

What are 4 possible adverse effects of cyclosporine?

A
  1. GI disturbances
  2. gingival hyperplasia
  3. papillomatosis in dogs
  4. viral infections in cats
17
Q

What is tacrolimus (FK-506)? How does it work?

A

IL-2 inhibitor

binds to FKBP12 and blocks calcineurin, making it unable to dephosphorylate NF-ATc to block IL-2 production

18
Q

What are the main 2 therapeutic uses of tacrolimus? What is the most common adverse effect?

A
  1. keratoconjunctivitis sicca
  2. localized topical treatment of immune-mediated dermatological diseases

local irritation due to topical application

19
Q

What is pentoxifylline (PTX)? How does it work?

A

TNFα inhibitor

downregulates the release of production of profibrotic TNF, suppresses the production of platelet-activating factor, and inhibits action on neutrophils

20
Q

What are the most common uses of pentoxifylline (PTX) in dogs and horses?

A

canine skin diseases, like vasculitis, dermatomyositis, contact allergy, atopic dermatitis, and vaccine-induced ischemic dermatitis

systemic inflammatory response syndrome, caudal heal syndrome

21
Q

How are tetracyclines used as immunosuppressors? What are the 2 types?

A

inhibits matrix metalloproteinase, which is responsible for cell proliferation, differentiation, and migration, angiogenesis, and host defense

  1. SHORT-ACTING: tetracycline, oxytetracycline
  2. LONG-ACTING: doxycycline, minocycline
22
Q

What 2 drugs are used in gold therapy (chrysotherapy)? What is thought to be their mechanism of action?

A
  1. Auranofin*
  2. gold sodium thiomalate

inhibits phagocytes (macrophages) and T-cells

23
Q

What are the main uses of gold therapy in dogs, cats, and horses?

A

DOGS: idiopathic polyarthritis, rheumatoid arthrisi, pemphigus foliaceous

CATS: pemphigus foliaceous, chronic gingivitis/stomatitis

HORSES: pemphigus foliaceous

24
Q

What is niacinamide? How is it thought to work as an immunosuppressant?

A

vitamin B2, common nutritional supplement with other medications

blocks mast cell degranulation and inhibits protease release for leukocytes

25
Q

What are the main 4 uses of niacinamide as an immunosuppressant?

A
  1. discoid lupus erythematosus
  2. pemphigus erythematosus
  3. pemphigus foliaceous
  4. autoimmune disease
26
Q

What causes autoimmune disorders? What 3 things happen? What are the 2 major causes?

A

disorders where the immune system attacks healthy cells in the body by mistake

  1. body has lost its ability to differentiate between antigens and its own cells
  2. antibodies attack self-antigens
  3. inflammation leading to tissue damage

genetic, environmental

Introduction to Pharmacology (39 decks)

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