anti metabolites Flashcards

1
Q

what is the mechanism of action of anti metabolites?

A

interfere with DNA synthesis

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2
Q

Name two anti metabolites?

A
  1. Azathioprine

2. Methotrexate

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3
Q

What is the mechanism of action of Azathioprine?

A
  1. Azathiprine is converted to 6-mercaptopurine
  2. in turn acts as an immunosupressant
  3. TPMT enzyme is responsible to break down the active metabolite
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4
Q

What should be tested prior to commencing to Azathioprine?

A
  1. TPMT testing
  2. TPMT deficiency is an autosomal recessive condition
  3. ## Patients with low TPMT activity - very high levels of Azathioprine
  4. risk of excessive bone marrow supression and hepatotoxicity
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5
Q

What is Azathioprine used for?

A
  1. Crohn’s disease
  2. Ulcerative colitis
  3. Rheumatoid arthritis
  4. SLE
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6
Q

What are the 2 side effects of methotrexate?

A
  1. bone marrow depression

2. increased risk of infection

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7
Q

What is the mechanism of action of methotrexate

A
  1. folate antagonist

2. inhibits DNA synthesis

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8
Q

Name some conditions methotrexate is used for?

A
  1. Crohn’s

2. Rheumatoid arthritis

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9
Q

What are the main side effects of methotrexate?

A
  1. teratogenic - must be on contraception

2. Given with folic acid to reduce GI side effects

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