Immunosuppr Rx Flashcards
Immunosuppressants
Cyclosporine Tacrolimus (FK-506) Sirolimus (rapamycin) Azathioprine Muromonab-CD3 (OKT3)
Cyclosporine
- 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)
Tacrolimus (FK-506)
- 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)
Sirolimus (rapamycin)
- 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
Azathioprine
- 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
Muromonab-CD3 (OKT3)
- 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)
Recombinant Cytokines
Aldesleukin (interleukin-2) Epoetin alfa (erythropoietin) Filgrastim (CSF-G) Sargramostim (CSF-GM) Alpha-Interferon Beta-Interferon Gamma-Interferon Oprelvekin (interleukin-11) Thrombopoietin
Aldesleukin
- Renal cell carcinoma Metastatic Melanoma 2. Cytokine: Interleukin-2 MOA: increases helper, cytotoxic, and regulatory T cells
Epoetin alfa
- Anemias (esp in renal failure) 2. Cytokine: Erythropoietin MOA: Stimulates Erythrocyte replication
Filgrastim
- Recovery of bone marrow 2. GM-CSF (Granulocyte Colony Stimulating Factor)
Sargramostim (CSF-GM)
- Recovery of bone marrow 2. GM-CSF (Granulocyte-Macrophage Colony Stimulating Factor)
Alpha-Interferon
- Hepatitis B and C Kaposi’s Sarcoma Leukemia Malignant Melanoma 2. Inhibit viral protein synthesis and activates NK cells to kill virally infected cells
Beta-Interferon
Multiple Sclerosis
Gamma-Interferon
- Chronic Granulomatous disease 2. Activates macrophages and Th1 cells Suppresses Th2 cells. 4. (G)amma = (G)ranulomatous
Oprelvekin
- Thrombocytopenia 2. IL-11
Thrombopoietin
Thrombocytopenia
Theraputic Antibodies
Muromonab-CD3 (OKT3 Digoxin Immune Fab Infliximab Adalimumab Abciximab Trastuzumab (Herceptin) Rituximab Omalizumab
Muromonab-CD3 (OKT3)
- 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)
Digoxin Immune Fab
Target: Digoxin Use: Antidote for Digoxin toxicity
Infliximab
Target: TNF-alpha Use: Crohn’s Disease, Rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis
Adalimumab
Target: TNF-alpha Use: Crohn’s Disease, Rheumatoid arthritis, psoriatic arthritis
Abciximab
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
Trastuzumab (Herceptin)
Target: HER2 Use: HER2 overexpressing breast cancer
Rituximab
Target: CD20 Use: B-cell non-Hodgkin’s lymphoma
Omalizumab
Target: IgE Use: Additional treatment for severe asthma
-azole
Antifungal Ex: Ketoconazole
-cillin
Penicillin Ex: Methicillin
-cycline
Antibiotic, protein synthesis inhibitor Ex: Tetracycline
-navir
Antibiotic, protease inhibitor Ex: Saqyubavir
-triptan
5-HT 1B/1D agonists (for migranes) Ex: Sumatriptan
-ane
Inhalational general anesthetic Ex: Halothane
-caine
Local anesthetic Ex: Lidocaine
-operidol
Butyrophenone (neuroleptic) Ex: Haloperidol
-azine
Phenothiazine (neuroleptic, antiemetic) Ex: Chlorpromazine, compazine
-barbital
Barbituate Ex: Phenobarbital
-zolam
Benzodiazepine Ex: Alprazolam
-azepam
Benzodiazepine Ex: Diazepam
-etine
SSRI Ex: Fluoxetine
-ipramine
TCA Ex: Imipramine
-triptyline
TCA Ex: Amitriptyline
-olol
B-antagonist Ex: Propranolol
-terol
B2-agonist Ex: Albuterol
-zosin
Alpha1-antagonist Ex: Prazosin
-oxin
Cardiac glycoside (inotropic agent) Ex: Digoxin
-pril
ACE inhibitor Ex: Captopril
-afil
Erectile Dysfunction Ex: Sildenafil
-tropin
Pituitary hormone Ex: Somatotropin
-tidine
H2 antagonist Ex: Cimetidine