Immunosuppressants Flashcards
Immunosuppressants
Cyclosporine Tacrolimus (FK-506) Sirolimus (rapamycin) Azathioprine Muromonab-CD3 (OKT3)
Cyclosporine
- Post-transplant immunosuppression; select autoimmune disorders
- Binds to cyclophilins. Complex blocks differentiation and activation of Tcells–> inhibiting calcineurin–> preventing production of IL-2 and its receptor
- Nephrotoxicity, hypertension, hyperlipidemia, hyperglycemia, tremor, gingival hyperplasia, hirsutism
- 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
- Binds to FK protein->inhibiting calcineurin->preventing IL-2
- Nephrotoxicity, hypertension, hyperlipidemia, hyperglycemia, tremor
- 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
- Inhibits mTOR. Decreased cell proliferation in response to IL-2
- Hyperlipidemia, thrombocytopenia, leukopenia
- SIROlimus= SERIOUS complications: immunosuppression
Azathioprine
- Immunosuppression post-KIDNEY transplant; autoimmune disorders (including glomerulonephritis and hemolytic anemia)
- Antimetabolite. Blocks 6-mercaptopurine synth-> decreased synthesis of nucleic acids. Toxic to proliferating lymphocytes.
- Bone marrow suppression.
- Active metabolite (mercaptopurine) is metabolized by xanthine oxidase so more toxic when given with allopurinol
Muromonab-CD3 (OKT3)
- Immunosuppression post-KIDNEY transplant
- Monoclonal antibody to CD3 on T-cells. Blocks interaction with CD3 responsible for T-cell signal transduction
- Cytokine release syndrome, hypersensitivity reaction
- 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 - Cytokine: Interleukin-2
MOA: increases helper, cytotoxic, and regulatory T cells
Epoetin alfa
- Anemias (esp in renal failure)
- 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
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
Beta-Interferon
Multiple Sclerosis
Gamma-Interferon
- Chronic Granulomatous disease
- Activates macrophages and Th1 cells
Suppresses Th2 cells. - (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
- Monoclonal antibody to CD3 on T-cells. Blocks interaction with CD3 responsible for T-cell signal transduction
- Cytokine release syndrome, hypersensitivity reaction
- 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
