Immunosuppressants Flashcards

1
Q

Immunosuppressants

A
Cyclosporine
Tacrolimus (FK-506)
Sirolimus (rapamycin)
Azathioprine
Muromonab-CD3 (OKT3)
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2
Q

Cyclosporine

A
  1. Post-transplant immunosuppression; select autoimmune disorders
  2. Binds to cyclophilins. Complex blocks differentiation and activation of Tcells–> inhibiting calcineurin–> preventing production of IL-2 and its receptor
  3. Nephrotoxicity, hypertension, hyperlipidemia, hyperglycemia, tremor, gingival hyperplasia, hirsutism
  4. Think old man with diabetes who wants to look good for his date so he put in dentures and got hair plugs: old (renal failure, HTN, cholesterol), diabetes (hyperglycemia), dentures (gum hyperplasia), hair plugs (hirsutism, and he is taking the drug because of his hair transplant)
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3
Q

Tacrolimus (FK-506)

A
  1. Post- organ transplant immunosuppression; POTENT
  2. Binds to FK protein->inhibiting calcineurin->preventing IL-2
  3. Nephrotoxicity, hypertension, hyperlipidemia, hyperglycemia, tremor
  4. Think old with diabetes who is nervous because he is super sick: old (renal failure, HTN, cholesterol), diabetes (hyperglycemia), nervous (tremor), super sick (strong immunosuppressant)
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4
Q

Sirolimus (rapamycin)

A
  1. Immunosuppression post-KIDNEY transplant (Give with cyclosporine); used with drug-eluting stents
  2. Inhibits mTOR. Decreased cell proliferation in response to IL-2
  3. Hyperlipidemia, thrombocytopenia, leukopenia
  4. SIROlimus= SERIOUS complications: immunosuppression
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5
Q

Azathioprine

A
  1. Immunosuppression post-KIDNEY transplant; autoimmune disorders (including glomerulonephritis and hemolytic anemia)
  2. Antimetabolite. Blocks 6-mercaptopurine synth-> decreased synthesis of nucleic acids. Toxic to proliferating lymphocytes.
  3. Bone marrow suppression.
  4. Active metabolite (mercaptopurine) is metabolized by xanthine oxidase so more toxic when given with allopurinol
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6
Q

Muromonab-CD3 (OKT3)

A
  1. Immunosuppression post-KIDNEY transplant
  2. Monoclonal antibody to CD3 on T-cells. Blocks interaction with CD3 responsible for T-cell signal transduction
  3. Cytokine release syndrome, hypersensitivity reaction
  4. Antibodies= hypersensitivity, hypersensitivity= cytokine release
    - nab= monocolonal antibody therapy (usually)
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8
Q

Recombinant Cytokines

A
Aldesleukin (interleukin-2)
Epoetin alfa (erythropoietin)
Filgrastim (CSF-G)
Sargramostim (CSF-GM)
Alpha-Interferon
Beta-Interferon
Gamma-Interferon
Oprelvekin (interleukin-11)
Thrombopoietin
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9
Q

Aldesleukin

A
  1. Renal cell carcinoma
    Metastatic Melanoma
  2. Cytokine: Interleukin-2
    MOA: increases helper, cytotoxic, and regulatory T cells
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10
Q

Epoetin alfa

A
  1. Anemias (esp in renal failure)
  2. Cytokine: Erythropoietin
    MOA: Stimulates Erythrocyte replication
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11
Q

Filgrastim

A
  1. Recovery of bone marrow

2. GM-CSF (Granulocyte Colony Stimulating Factor)

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12
Q

Sargramostim (CSF-GM)

A
  1. Recovery of bone marrow

2. GM-CSF (Granulocyte-Macrophage Colony Stimulating Factor)

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13
Q

Alpha-Interferon

A
1. Hepatitis B and C
Kaposi's Sarcoma
Leukemia
Malignant Melanoma
2. Inhibit viral protein synthesis and activates NK cells to kill virally infected cells
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14
Q

Beta-Interferon

A

Multiple Sclerosis

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15
Q

Gamma-Interferon

A
  1. Chronic Granulomatous disease
  2. Activates macrophages and Th1 cells
    Suppresses Th2 cells.
  3. (G)amma = (G)ranulomatous
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16
Q

Oprelvekin

A
  1. Thrombocytopenia

2. IL-11

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17
Q

Thrombopoietin

A

Thrombocytopenia

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19
Q

Theraputic Antibodies

A
Muromonab-CD3 (OKT3
Digoxin Immune Fab
Infliximab
Adalimumab
Abciximab
Trastuzumab (Herceptin)
Rituximab
Omalizumab
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20
Q

Muromonab-CD3 (OKT3)

A
  1. Immunosuppression post-KIDNEY transplant
  2. Monoclonal antibody to CD3 on T-cells. Blocks interaction with CD3 responsible for T-cell signal transduction
  3. Cytokine release syndrome, hypersensitivity reaction
  4. Antibodies= hypersensitivity, hypersensitivity= cytokine release
    - nab= monocolonal antibody therapy (usually)
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21
Q

Digoxin Immune Fab

A

Target: Digoxin
Use: Antidote for Digoxin toxicity

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22
Q

Infliximab

A

Target: TNF-alpha
Use: Crohn’s Disease, Rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis

23
Q

Adalimumab

A

Target: TNF-alpha
Use: Crohn’s Disease, Rheumatoid arthritis, psoriatic arthritis

24
Q

Abciximab

A

Target: Glycoprotien IIb/IIIa
Use: Prevent cardiac ischemia in unstable angina and patients treated with percutaneous coronary intervention
MOA: Prevents platelet aggregation by inhibiting the platelet-GIIb/IIIa-fibrinogen bonds

25
Q

Trastuzumab (Herceptin)

A

Target: HER2
Use: HER2 overexpressing breast cancer

26
Q

Rituximab

A

Target: CD20
Use: B-cell non-Hodgkin’s lymphoma

27
Q

Omalizumab

A

Target: IgE
Use: Additional treatment for severe asthma

30
Q

-azole

A

Antifungal

Ex: Ketoconazole

31
Q

-cillin

A

Penicillin

Ex: Methicillin

32
Q

-cycline

A

Antibiotic, protein synthesis inhibitor

Ex: Tetracycline

33
Q

-navir

A

Antibiotic, protease inhibitor

Ex: Saqyubavir

35
Q

-triptan

A

5-HT 1B/1D agonists (for migranes)

Ex: Sumatriptan

36
Q

-ane

A

Inhalational general anesthetic

Ex: Halothane

37
Q

-caine

A

Local anesthetic

Ex: Lidocaine

38
Q

-operidol

A

Butyrophenone (neuroleptic)

Ex: Haloperidol

39
Q

-azine

A

Phenothiazine (neuroleptic, antiemetic)

Ex: Chlorpromazine, compazine

40
Q

-barbital

A

Barbituate

Ex: Phenobarbital

41
Q

-zolam

A

Benzodiazepine

Ex: Alprazolam

42
Q

-azepam

A

Benzodiazepine

Ex: Diazepam

43
Q

-etine

A

SSRI

Ex: Fluoxetine

44
Q

-ipramine

A

TCA

Ex: Imipramine

45
Q

-triptyline

A

TCA

Ex: Amitriptyline

47
Q

-olol

A

B-antagonist

Ex: Propranolol

48
Q

-terol

A

B2-agonist

Ex: Albuterol

49
Q

-zosin

A

Alpha1-antagonist

Ex: Prazosin

51
Q

-oxin

A
Cardiac glycoside (inotropic agent)
Ex: Digoxin
52
Q

-pril

A

ACE inhibitor

Ex: Captopril

53
Q

-afil

A

Erectile Dysfunction

Ex: Sildenafil

55
Q

-tropin

A

Pituitary hormone

Ex: Somatotropin

56
Q

-tidine

A

H2 antagonist

Ex: Cimetidine