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4 Clinical Pharmacology and Intro to Prescribing > 19 Immunosuppressants > Flashcards

19 Immunosuppressants Flashcards

1
Q

How do corticosteroids eg prednisolone work?

A
  • Decrease prostanoids production
    • reduced expression of COX-2
  • Decrease cytokine generation
  • Decrease nitric oxide generation
  • Decrease mediator release from basophils and mast cells eg histamine
  • Decrease IgG production
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2
Q

What are the long term side effects that are caused by taking corticosteroids?

A

Think CUSHINGS (proteolysis)

  • Weight gain
  • Thin skin
  • High blood sugar
  • Proximal muscle weakness

Osteoporosis

Immunosuppression

Glaucoma

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3
Q

Name 4 (systemic) corticosteroids (not inhaled).

A
  1. Prednisolone
  2. Betamethasone
  3. Dexamethasone
  4. Hydrocortisone

Inhaled:

  1. Beclomethasone
  2. Budesonide
  3. Fluticasone
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4
Q

What are DMARDs?

A

Disease modifying anti-rheumatic drugs

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5
Q

Give some examples of DMARDs: (disease modifying anti-rhuematic drugs)

A

Azathioprine

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6
Q

How does azathioprine work? (DMARD)

A

= an antimetabolite

Azathioprine–> 6-mercaptopurine

-purine synthesis inhibitor

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7
Q

What are the indiications for azathioprine?

A
  1. Organ transplant eg renal
  2. IBD
  3. Rheumatoid arthritis
  4. SLE
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8
Q

What are the 2 main adverse effects of the drug azathioprine?

A

Adverse effects=

  • Bone marrow suppression
  • Thrombocytopenia
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9
Q

What are the indications for the drugs:

  • Cyclosporin
  • Tacrolimus
A
  • Organ transplants
  • Dermatomyositis
  • Crohn’s disease
  • Rheumatoid artiritis
  • Psoriasis
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10
Q

How do the following drugs work?:

  • Cyclosporin
  • Tacrolimus
A
  • Active against T-cells
  • Inhibit calcineurin- prevent production of IL-2
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11
Q

What are some of the adverse effects of ciclosporin?

A
  • Eye discomfort
  • Nephrotoxicity
  • Hepatitis
  • Gingival hyperplasia (gums)
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12
Q

What are the indications for cyclophosphamide? (2)

A

SLE nephritis

Systemic vasculitis

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13
Q

Why do you need to test for TPMT (thiopurine methyltransferase) activity before prescribing azathioprine?

A

6-mercaptopurine (active metabolite of azthioprine)= metabolised by TPMT

TPMT= highly polymorphic

Low/absent TPMT- risk myelosuppression if given azathioprine

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14
Q

What is the main active metabolite of cyclophosphamide?

A

Main active metabolite= 4-hydroxycyclophosphamide

Other metabolites=

  • Phosphoramide mustard
  • Acrolein
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15
Q

Why do we sometimes give Mesna (drug) with cyclophosphamide?

A

Acrolein (metabolite of cyclophosphamide) = toxic to bladder

Can cause haemorrhagic cystitis

To prevent this:

  • Give mesna
  • Aggressive hydration
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16
Q

Useful diagram for chemotherapy toxicities:

A
17
Q

How does methotrexate work?

A

Competitively and reversibly

Inhibits DHFR (dihydrofolate reductase) - required to make nucleotides

18
Q

What are the indications for methotrexate? (= immunosuppressant and chemotherapy) (4)

A
  1. Rhuematoid arthritis
  2. Ectopic if it hasn’t ruptured (+ abortions)
  3. Crohn’s disease
  4. Psoriatic arthritis
  5. Cancer: breast cancer, leukemia, lung cancer, lymphoma, and osteosarcoma

(Should only be given weekly)

19
Q

Give 3 adverse effects of methotrexate:

A
  1. Inflammation of membranes
    1. Pneumonitis
    2. Stomatitis (sore or inflammation inside of the mouth)
  2. Hepatitis
20
Q

How does mycophenolate mofetil work?

A

Inhibits inosine monophosphate dehydrogenase

Stops DNA synthesis essentially

(= Antiproliferative immunosupressant)

21
Q

What are the indications for mycophenolate mofetil?

A

Primary organ transplantation

SLE nephritis

22
Q

What are some of the adversr effects of mycophenolate mofetil?

A

Increase risk of skin malignancy

Nausea, vomiting, diarrhoea

Myelosuppression

23
Q

Sulfasalazine is a DMARD. What are some of its indications?

(5—aminosalicylic acid donor in RA as a DMARD)

A
  1. Rheumatoid arthritis
  2. Ankylosing spondylitis
  3. IBD
24
Q

Give some of the adverse effects of sulphasalazine.

A
  • Nausea +/- vomiting
  • Leucopenia
  • Dizzyness
  • Arthralgia
25
Q

How do each of the following work as immunosuppressants?

  • infliximab
  • adalinumab
  • rituximab
  • tocilizumab
A
26
Q

When should we consider using disease modifying antirheumatic drugs in combination?

A

In severe rheumatoid disease

4 Clinical Pharmacology and Intro to Prescribing (27 decks)

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