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Flashcards in Immunopharmacology Deck (37):
1

overall effect of glucocorticoid administration

anti inflammatory and immunosuppressive

2

mechanism of glucocorticoids in term of anti inflammatory actions

inhibit prostaglandin synthesis by

1. induction of annex I --> inhibits phospholipase A2α
2. induction of MAPK phosphatase I
3. inhibition of NF-kB -> reducing expression of COX-2

3

uses of glucocorticoids

-prevent and treat transplant rejection
-treat autoimmune disorders
-alleviate pain, nausea, fatigue, anorexia, malaise, and improve quality of life

4

name some glucocorticoids

Dexamethasone
Prednisone
Prednisolone
Methylprednisolone

5

adverse effects of glucocorticoids

-short term: hypertension, hyperglycemia, immunosuppression, psychotic reactions, cognitive impairment

-long term: osteoporosis, weight gain, poor wound healing, increased risk of infections, adrenal suprresion

6

what are the immunosuppressive agents

glucocorticoids
calcineurin inhibitors
proliferation signal inhibitors
angiogenesis inhibitors
cytotoxic drugs
other agents

7

what are the calcineurin inhibitors

Cyclosporine
Tacrolimus

8

mechanism of cyclosporine

binds to cyclophilin and forms a complex that inhibits cytoplasmic phosphatase, calcineurin which is needed for activation of T cell transcription factors --> IL-2, IL-3, TNFα etc

9

uses of cyclosporine

organ transplantation
uveitis
RA
psoriasis

10

adverse effects of cyclosporine

Nephrotoxicity
Osteoporosis
Hirsutism
Gum Hyperplasia

11

mechanism of tacrolimus

binds to FK binding protein and then the complex inhibits calcineurin needed for T cell transcription factor

12

uses of tacrolimus

- prevention of rejection of kidneys, liver, or heart
- atopic dermatitis and psoriasis (topical use)

13

adverse effects of tacrolimus

similar to cyclosporine

Nephrotoxicity
Neurotoxicity
Hyperglycemia
Hypertension
Hyperkalemia
GI symptoms

14

what is the proliferation signal inhibitor

Sirolimus

15

mechanism of Sirolimus

binds to FK binding protein then the complex binds and inhibits serine threonine kinase mTOR --> leading to blockage of IL-2 driven T cell proliferation

16

uses of Sirolimus

renal transplantation

inhibition of re-stenosis of BV in CAD

17

adverse effects of Sirolimus

Myelosuppression
Hepatotoxicity
Hypertriglyceridemia
Pneumonitis

18

inhibitor of angiogenesis and its mechanism

Thalidomide

inhibits synthesis of TNFα and inhibits angiogenesis

19

uses of thalidomide

Erythema nodosum leprosum
Multiple Myeloma

20

adverse effects of thalidomide

Teratogenesis
Increased risk of DVT
Peripheral Neuropathy, constipation, rash, fatigue, hypothyroidism

21

what are the cytotoxic drugs

CLAMM

Cyclophosphamide
Leflunomide
Azathioprine
Methotrexate
Mycophenolate Mofetil

22

mechanism of azathioprine

converted to 6-mercaptopurine --> inhibits de novo purine synthesis --> suppression of B and T cells function, immunoglobin production, IL-2 secretion

23

uses and drug interaction of azathioprine

-used for organ transplant rejection and RA
-with allopurinol, should be reduced dose of azathioprine (since its effect relies on interaction with xanthine oxidase) to prevent excessive toxicity

24

mechanism of methotrexate

inhibits AICAR transformylase --> increased AICAR --> inhibits AMP deaminase --> increased AMP --> converted to adenosine --> suppresses NF-kB and inhibits inflammation

25

uses of methotrexate

RA
psoriasis
Lupus
Wegeners
Graft vs. host disease

26

contraindications and adverse effects of methotrexate

contraindication - pregnancy

adverse:
Nausea and mucosal ulcers
increased creatinine in those with renal insufficiency
Hepatotoxicity

27

mechanism of mycophenolate mofetil

inhibits inosine monophosphate dehydrogenase --> inhibition of GTP synthesis --> suppression of B and T lymphocyte activation

28

uses of mycophenolate mofetil

prophylaxis for transplant rejection
off label in SLE

29

adverse effects of mycophenolate mofetil

-reversible myelosuppression
-nausea, vomiting, diarrhea, abdominal pain

30

mechanism of leflunomide

inhibits dihydroorate dehydrogenase --> reduced UMP needed for pyrimidine synthesis

31

adverse effects of leflunomide and contraindication

Reversible alopecia
myelosuppression
increased aminotransferase activity

contraindicated in pregnancy

32

mechanism of cyclophosphamide

destroys proliferating lymphoid cells and alkylates DNA

33

adverse effects of cyclophosphamide

-infertility in men and women
-hemorrhagic cystitis
-bladder carcinoma
-urinary toxicities from its metabolite acrolein

34

what are the OTHER immunosuppressant agent

hydroxychloroquine
sulfasalazine

35

adverse effects of hydroxychloroquine

hemolysis in G6PD deficiency
retinal damage

36

uses of sulfasalazine

RA
IBD
Ankylosing Spondylitis

37

adverse effects of sulfasalazine

Neutropenia
Hemolysis in G6PD deficiency

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