Immunosuppressant Drugs

Question 1

2 main applications of immunosuppressants

Answer 1

1) prevent organ rejection

2) tretment of autoimmune disorders

Question 2

2 big toxicities of immunosuppressants

Answer 2

Increased risk of infection, increased risk of neoplasm development

Question 3

Cyclosporine/tacrolimus/pimecrolimus mech of action

Answer 3

Inhibit calcineurin, blocking IL2 for T cell proliferation

Question 4

Cyclosporine ADRs (3)

Answer 4

• nephrotoxicity
• Increased risk of infection, hypertension, hirsutism, tremor
• Increased risk of lymphoma

Question 5

DOC for preventing organ rejection after allogenic transplant

Answer 5

Cyclosporine

Question 6

Cyclosporine differs from other immunosuppressants in that…

Answer 6

Prevent rejection of allogenic organ without suppressing bone marrow

Question 7

3 most effective immunosuppressants and their class

Answer 7

cyclosporine
tacrolimus
pimecrolimus

Calcineurin inhibitors

Question 8

mTOR inhibitors mech of action

Answer 8

Inhibit enzyme known as target of rampamycin, a protein kinase in cell proliferation and survival, acts on B and T cells by acting on IL2 but not thru calcineurin

Question 9

Cytotoxic drugs mech of action

Answer 9

Suppress immune cells by killing B and T cell lymphocytes undergoing proliferation, are toxic to all proliferating cells

Question 10

Cytotoxic drugs ADRS (4)

Answer 10

• less safe agent than cyclosporine and glucocorticoids
• bone marrow suppression
• GI disturbances
• alopecia

Question 11

Cyclophosphamide (cytoxan) mech of action and what drug class is it?

Answer 11

Prodrug converted into active form in liver, decreases number of B and T lymphocytes by cross linking DNA, toxic to all cells

Cytotoxic drugs

Question 12

Cyclophosphamide (cytoxan) ADRs (3)

Answer 12

• neutropenia
• hemorrhagic cystitis
• sterility

Question 13

Mycophenolate mofentil mech of action, what class of drugs does it belong to?

Answer 13

Prophylaxis of organ rejection, converted to active form after absorption and acts on B and T lymphocytes to inhibit an enzyme needed for synthesis of purines

Cytotoxic drugs

Question 14

Basiliximab (simulect) mech of action and what drug class does it belong to?

Answer 14

blocks activity of T lymphocytes blocking proliferation of T cells by IL 2 binding

Antibodies

Question 15

Cyclosporine indications

Answer 15

Prevention of rejection of allogenic organ transplants, as well as RA and psoriasis

Question 16

Cyclosporine drug interactions

Answer 16

Aminoglycosides, grapefruit juice, and amphoterecin B

Question 17

Because of serious adverse effects, cytotoxic drugs are reserved for….

Answer 17

…patients not responding to safer agents (cyclosporine and glucocorticoids)

Question 18

Methotrexate summary, what class of drugs does it belong to?

Answer 18

Anticancer drug also used for immunosuppression

Cytotoxic

Question 19

Mycophenolate mofentil unique characteristic among cytotoxic drugs

Answer 19

It only inhibits B and T lymphocytes because of the purine synthesis pathway it targets