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Immunsupressive Drugs (Glucocorticoids (Standard in treatment regime
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Immunsupressive Drugs
Glucocorticoids
Standard in treatment regime
Usually combined
Serious long-term side effects (diabetes, cataract peptic ulcers)
Cortisone
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-Double bond increases glucocorticoid activity over mineralocorticoid activity.
-Methyl group increases lipophilicity (better absorption)
- C11 hydroxy group required for glucocorticoid activity.
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Cytostatic's
Inhibit or suppress cellular growth and multiplication.
Usually at smaller doses than for malignancy.
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Mercaptopurine (purine analogue)
Inhibits DNA synthesis.
Problem: Converted quickly to inactive and eliminated.
Azathioprine (prodrug of 6-mercaptopurine)
Slow release (not enzymatic) in the liver.
To control transplant rejection
Leflunomide
Inhibits dihydroorotate dehydrogenase, and pyrimidine synthesis.
Treatment for RA
Serious side effects inc. birth defects. up to a year after treatment.
Mycophenolate
Inhibitor of inosine monophosphate, and purine synthesis.
Used in renal transplants.
Mycophenolate mofetil
Prodrug of mycophenolate - undergoes rapid hydrolysis.
Improved oral bioavailability
Inhibits T and B cell proliferation.
Used when azathioprine cannot be.
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