Immunosuppressants

Question 1

Indications

Answer 1

1. Autoimmune disease - lupus, immune hemolytic anemia, KCS
2. Hypersensitivity disease: atopic dermatitis , asthma , inflammatory bowl disease
3. Transplantation

Question 2

Drug list

Answer 2

1.Purine analogues - azathioprine , mycophenolate-mofetil (safer)
Pyrimidine- analogues (leflunomide),
Folic acid antagonist (methotrexate)
2.glucocorticoids
3. alkylating agent - cyclophosphamide
4. Cytokine gene expression inhibitor - Calcineurine- inhibotor : CYCLOSPORINE , tarcolimus , pimercolimus
Toxic , used locally

Question 3

Antimetabolites

Answer 3

*Purine+ pyrimidine analogue: inhibition / DNA damage
Effect cell division
1.azathioperine:(purine) prodrug (don’t use in liver failure), given in autoimmune diseases, never in cats. SE: bone marrow supression , GI symptoms . Causes anemia , diarrhea , vomiting. OP/IV
2. mycophenolate-mofetil: (purine)prodrug, IMP DH inhibitor, T,B cells, safer, autoimmune glomerulonephritis.
3. Methotrexate : ,(folic acid) inhibits cell division, dihydrofolate reductase inhibitor , anticancer, kills T cells

Question 4

Alkylating agent

Answer 4

Cyclophosphamide: B+T equally , GI,BM SE , antineoplastic, autoimmune, hemorragic cystitis (furosemide+ MENSA for urine dilution)

Question 5

Calcineurine inhibitors

Answer 5

Dephosphorylate NFAT- IL-2 expression, only T cells, mastocyte inhibition

• Cyclosporine - T cells, autoimmune diseases (KCS, atopic dermatitis , IBD) ,+ Little food. SE: Vomiting, diarrhea , gingival hyperplesia (bacteria) - give with food
• Tarcolimus , pimecrolimus: 500x more active, toxic, topical, T cells . Used for atopic dermatitis