Immunosuppr Rx

Question 1

Immunosuppressants

Answer 1

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

Question 2

Cyclosporine

Answer 2

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)

Question 3

Tacrolimus (FK-506)

Answer 3

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)

Question 4

Sirolimus (rapamycin)

Answer 4

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

Question 5

Azathioprine

Answer 5

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

Question 6

Muromonab-CD3 (OKT3)

Answer 6

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)

Question 8

Recombinant Cytokines

Answer 8

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

Question 9

Aldesleukin

Answer 9

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

Question 10

Epoetin alfa

Answer 10

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

Question 11

Filgrastim

Answer 11

1. Recovery of bone marrow 2. GM-CSF (Granulocyte Colony Stimulating Factor)

Question 12

Sargramostim (CSF-GM)

Answer 12

1. Recovery of bone marrow 2. GM-CSF (Granulocyte-Macrophage Colony Stimulating Factor)

Question 13

Alpha-Interferon

Answer 13

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

Question 14

Beta-Interferon

Answer 14

Multiple Sclerosis

Question 15

Gamma-Interferon

Answer 15

1. Chronic Granulomatous disease 2. Activates macrophages and Th1 cells Suppresses Th2 cells. 4. (G)amma = (G)ranulomatous

Question 16

Oprelvekin

Answer 16

1. Thrombocytopenia 2. IL-11

Question 17

Thrombopoietin

Answer 17

Thrombocytopenia

Question 19

Theraputic Antibodies

Answer 19

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

Question 20

Muromonab-CD3 (OKT3)

Answer 20

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)

Question 21

Digoxin Immune Fab

Answer 21

Target: Digoxin Use: Antidote for Digoxin toxicity

Question 22

Infliximab

Answer 22

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

Question 23

Adalimumab

Answer 23

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

Question 24

Abciximab

Answer 24

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

Question 25

Trastuzumab (Herceptin)

Answer 25

Target: HER2 Use: HER2 overexpressing breast cancer

Question 26

Rituximab

Answer 26

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

Question 27

Omalizumab

Answer 27

Target: IgE Use: Additional treatment for severe asthma

Question 30

-azole

Answer 30

Antifungal Ex: Ketoconazole

Question 31

-cillin

Answer 31

Penicillin Ex: Methicillin

Question 32

-cycline

Answer 32

Antibiotic, protein synthesis inhibitor Ex: Tetracycline

Question 33

-navir

Answer 33

Antibiotic, protease inhibitor Ex: Saqyubavir

Question 35

-triptan

Answer 35

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

Question 36

-ane

Answer 36

Inhalational general anesthetic Ex: Halothane

Question 37

-caine

Answer 37

Local anesthetic Ex: Lidocaine

Question 38

-operidol

Answer 38

Butyrophenone (neuroleptic) Ex: Haloperidol

Question 39

-azine

Answer 39

Phenothiazine (neuroleptic, antiemetic) Ex: Chlorpromazine, compazine

Question 40

-barbital

Answer 40

Barbituate Ex: Phenobarbital

Question 41

-zolam

Answer 41

Benzodiazepine Ex: Alprazolam

Question 42

-azepam

Answer 42

Benzodiazepine Ex: Diazepam

Question 43

-etine

Answer 43

SSRI Ex: Fluoxetine

Question 44

-ipramine

Answer 44

TCA Ex: Imipramine

Question 45

-triptyline

Answer 45

TCA Ex: Amitriptyline

Question 47

-olol

Answer 47

B-antagonist Ex: Propranolol

Question 48

-terol

Answer 48

B2-agonist Ex: Albuterol

Question 49

-zosin

Answer 49

Alpha1-antagonist Ex: Prazosin

Question 51

-oxin

Answer 51

Cardiac glycoside (inotropic agent) Ex: Digoxin

Question 52

-pril

Answer 52

ACE inhibitor Ex: Captopril

Question 53

-afil

Answer 53

Erectile Dysfunction Ex: Sildenafil

Question 55

-tropin

Answer 55

Pituitary hormone Ex: Somatotropin

Question 56

-tidine

Answer 56

H2 antagonist Ex: Cimetidine