Immunopharmacology

Question 1

Prednisone

Answer 1

Decreases macrophage, cytotoxic T cell, and NK response to IL2; Modify helper T cells by inhibiting expression of IL’s, decrease T-Cell proliferation
USE: Short-term post transplant or long-term for autoimmune dz
SE: CUSHING’S

Question 2

Cyclosporine

Answer 2

inhibits T-cell activation without marrow suppression- inhibits CALCINEURIN by binding cyclophilin to decrease IL1/2
Not commonly used anymore (narrow therapeutic range)
SE: GINGIVAL HYPERPLASIA, HTN, HLD
Drug interactions common! No grapefruit juice!

Question 3

Tacrolimus

Answer 3

inhibits T-cell activation through FK506 protein binding– inhibit calcineurin. Decreases IL2/4
DOC for REJECTION PREVENTION! Rescue during acute rejection
SE: Better tolerated than cyclosporine
NEPHROTOX, HTN, HYPERGLYCEMIA, INCREASED RISK OF INFECTIONS
Interactions: NO GRAPEFRUIT JUICE, take on empty stomach

Question 4

Pimecrolimus

Answer 4

Similar to tacrolimus

Cream used for atopic dermatitis

Question 5

Sirolimus

Answer 5

Blocks T cell respons to IL2, inhibits B Cell proliferation
Starting to replace Tacro and Cyclo
SE: Increases cholesterol, triglycerides

Question 6

Mycophenolate

Answer 6

Inhibits inosine monophosphate DH for DE NOVO SYNTHESIS OF T AND B CELLS (purines)– Very selective!
Combo with cyclo and tacro for rejection prevention; refractory rejection
SE: Increase infection/sepsis, SKIN RASH (discontinue)
Usually well tolerated

Question 7

Azathioprine (Inuran)

Answer 7

Prodrug of 6-MP to inhibit de novo purine synthesis
Use: Acute glomerulonephritis, RENAL SLE, SEVERE RA
SE: Increase infection risk, TERATOGEN
REDUCE DOSE IF GIVING WITH ALLOPURINOL FOR HYPERURICEMIA

Question 8

Cyclophosphamide

Answer 8

Alkylating agent- direct effect on T/B cells, INHIBITS ESTABLISHED IMMUNE RESPONSE
Use: Antineoplastic, organ/marrow rescue
SE: Hemorrhagic cystitis (MESNA), bladder fibrosis

Question 9

Methotrexate

Answer 9

inhibits dihydrofolate reductase, blocks folate metabolism in purine synthesis
Uses: Post transplant, Psoriasis, RA
SE: HEPATOTOXICITY, FETAL DEATH

Question 10

Thalidomide

Answer 10

Suppresses TNF-alpha, shifts T-cell response with increase in IL4/5
Use: Prevents graft vs host, TERATOGEN CAT XXXXX!

Question 11

Muromonab-CD3

Answer 11

MOUSE Monoclonal Antibody for CD3 on T cells to block cytotoxic T-cells and prevents new cytotoxic cells
RARELY USED, highly toxic
SE: Cytokine release syndrome (flu, shock)
Pulm edema
(Muro-Mouse)

Question 12

Daclizumab or basiliximab

Answer 12

HUMAN monoclonal AB binds to IL2 receptor on activated T-cells to decrease T-cell
PRIOR TO TRANSPLANT, then combine with cyclosporine after transplant
SE: rare

Question 13

Efalizumab

Answer 13

Anti-CD11 monoclonal AB prevents binding to prevent T-cell activation without destroying T-cells
IM (IV?)
Use: Psoriasis and skin grafts

Question 14

Interferon a-2b

Answer 14

induce antiviral proteins to inhibit virus directed translation
Use: Hairy cell leukemia, Kaposi’s sarcoma, condylomata, Hep C
SE: DEPRESSION! Increase LFTs, triglycerides

Question 15

Interferon b-1b

Answer 15

induce antiviral proteins to inhibit virus directed translation; DECREASE CLASS 1 mHC presentation for MS TREATMENT

Question 16

Interleukin-2

Answer 16

Stimulates T-cell productivity and increases B-cells, stimulates macrophages and NK cells
Uses: METASTATIC RENAL CELL CARCINOMA AND MALIGNANT MELANOMA, IV ONLY!!! SEVERE SE!!!!

Question 17

Interleukin-2 SE

Answer 17

SEVERE HYPOTENSION, REDUCED ORGAN PERFUSION, pulmonary congestion, anemia, TCP, constitutional, AMS, DEPRESSION, INCREASED RISK OF INFECTION

Question 18

Oprelvekin rh-IL11

Answer 18

recombinant IL-11
SQ FOR SEVERE CHEMO-INDUCED TCP
SE: Fluid retention, decreased hemoglobin

Question 19

G-CSF

Answer 19

Human recombinant C-CSF

Tx for SEVERE NEUTROPENIA

Question 20

Erythropoietin

Answer 20

Acts on erythropoietin receptors to reverse anemia
SQ for anemia (Zidovudine, interferon)
SE: HTN, blood clots