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Pharmacology > Immunopharmacology > Flashcards

Immunopharmacology Flashcards

1
Q

overall effect of glucocorticoid administration

A

anti inflammatory and immunosuppressive

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2
Q

mechanism of glucocorticoids in term of anti inflammatory actions

A

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
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3
Q

uses of glucocorticoids

A
  • prevent and treat transplant rejection
  • treat autoimmune disorders
  • alleviate pain, nausea, fatigue, anorexia, malaise, and improve quality of life
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4
Q

name some glucocorticoids

A

Dexamethasone
Prednisone
Prednisolone
Methylprednisolone

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5
Q

adverse effects of glucocorticoids

A
  • short term: hypertension, hyperglycemia, immunosuppression, psychotic reactions, cognitive impairment
  • long term: osteoporosis, weight gain, poor wound healing, increased risk of infections, adrenal suprresion
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6
Q

what are the immunosuppressive agents

A 
glucocorticoids
calcineurin inhibitors
proliferation signal inhibitors
angiogenesis inhibitors
cytotoxic drugs
other agents
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7
Q

what are the calcineurin inhibitors

A

Cyclosporine

Tacrolimus

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8
Q

mechanism of cyclosporine

A

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

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9
Q

uses of cyclosporine

A

organ transplantation
uveitis
RA
psoriasis

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10
Q

adverse effects of cyclosporine

A

Nephrotoxicity
Osteoporosis
Hirsutism
Gum Hyperplasia

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11
Q

mechanism of tacrolimus

A

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

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12
Q

uses of tacrolimus

A
  • prevention of rejection of kidneys, liver, or heart

- atopic dermatitis and psoriasis (topical use)

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13
Q

adverse effects of tacrolimus

A

similar to cyclosporine

Nephrotoxicity
Neurotoxicity
Hyperglycemia
Hypertension
Hyperkalemia
GI symptoms
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14
Q

what is the proliferation signal inhibitor

A

Sirolimus

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15
Q

mechanism of Sirolimus

A

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

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16
Q

uses of Sirolimus

A

renal transplantation

inhibition of re-stenosis of BV in CAD

17
Q

adverse effects of Sirolimus

A

Myelosuppression
Hepatotoxicity
Hypertriglyceridemia
Pneumonitis

18
Q

inhibitor of angiogenesis and its mechanism

A

Thalidomide

inhibits synthesis of TNFα and inhibits angiogenesis

19
Q

uses of thalidomide

A

Erythema nodosum leprosum

Multiple Myeloma

20
Q

adverse effects of thalidomide

A

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

21
Q

what are the cytotoxic drugs

A

CLAMM

Cyclophosphamide
Leflunomide
Azathioprine
Methotrexate
Mycophenolate Mofetil
22
Q

mechanism of azathioprine

A

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

23
Q

uses and drug interaction of azathioprine

A
  • 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
Q

mechanism of methotrexate

A

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

25
Q

uses of methotrexate

A 
RA
psoriasis
Lupus
Wegeners
Graft vs. host disease
26
Q

contraindications and adverse effects of methotrexate

A

contraindication - pregnancy

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

27
Q

mechanism of mycophenolate mofetil

A

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

28
Q

uses of mycophenolate mofetil

A

prophylaxis for transplant rejection

off label in SLE

29
Q

adverse effects of mycophenolate mofetil

A
  • reversible myelosuppression

- nausea, vomiting, diarrhea, abdominal pain

30
Q

mechanism of leflunomide

A

inhibits dihydroorate dehydrogenase –> reduced UMP needed for pyrimidine synthesis

31
Q

adverse effects of leflunomide and contraindication

A

Reversible alopecia
myelosuppression
increased aminotransferase activity

contraindicated in pregnancy

32
Q

mechanism of cyclophosphamide

A

destroys proliferating lymphoid cells and alkylates DNA

33
Q

adverse effects of cyclophosphamide

A
  • infertility in men and women
  • hemorrhagic cystitis
  • bladder carcinoma
  • urinary toxicities from its metabolite acrolein
34
Q

what are the OTHER immunosuppressant agent

A

hydroxychloroquine

sulfasalazine

35
Q

adverse effects of hydroxychloroquine

A

hemolysis in G6PD deficiency

retinal damage

36
Q

uses of sulfasalazine

A

RA
IBD
Ankylosing Spondylitis

37
Q

adverse effects of sulfasalazine

A

Neutropenia

Hemolysis in G6PD deficiency

Pharmacology (79 decks)

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