Pharm: Immunomodulating Drugs Flashcards
(58 cards)
What class of drugs regulates gene expression (BY INHBITING SYNTHESIS OF EICOSANOIDS) and interferes with cellular immunity?
Corticosteroids
Prednisone, Dexamethasone, and FLUDROCORTISONE (as well as Cortisone, Triamcinolone and Betamethasone) belong to what class of immune-modulating drugs?
Corticosteroids
What drugs are used as FIRST LINE immunosuppression for solid organ transplant and hematopoietic stem cell transplant?
Corticosteroids
What effect does corticosteroids have on glucose?
Causes hyperglycemia –> STEROID DIABETES
What are two major side effects of corticosteroids associated with long term use?
Osteoporosis and Glaucoma
What 2 drugs belong to the “Calcineurin inhibitor” Class?
Cyclosporine, Tacrolimus
What drug binds to cyclophilin?
Cyclosporine
What happens after cyclosporine binds to cyclophilin?
Inhibits T-cell activation –> Decreases IL-2, IL-3, IFN-gamma
Inhibits Calcineurin
What organ transplants is Cyclosporine used for?
Cadaveric –> Kidneys, Liver, Pancreas, Cardiac
What is the role of Cyclosprine in Graft-vs-Host disease?
Tx of G-vs-H disease AFTER hematopoietic stem cell transplant. Combined with methotrexate.
STANDARD PROPHYLAXIS TO PREVENT G-VS-H DISEASE AFTER ALLOGENIC STEM CELL TRANSPLANT
What 4 Autoimmune disorders is cyclosporine indicated for? (one bolded)
UVEITIS, RA, psoriasis, asthma
What should you know about the metabolism of cyclosporine?
Metabolized by the P450 3A enzyme in the liver –> resultant multidrug interactions.
What is the role of inducers on the P450 system?
Inducers DECREASE the half-life and blood levels of the drug.
What are the most important (bolded) toxicities of cyclosporine? (4)
Induces TGF-Beta;
Promotes tumor invasion and metastasis;
Increases incidence of lymphomas;
Kaposi’s Sarcoma
Tacrolimus belongs to what drug class?
Calcineurin inhibitor
What is the MOA for Tacrolimus?
Binds to immunophilin FK-binding protein (FKBP)
Clinical indications, metabolism, and toxicity of tacrolimus are similar to what other drug? What is the difference between the 2 drugs?
Cyclosporine –> Tacrolimus is more potent than cyclosporine
Sirolimus belongs to what drug class?
Proliferation signal inhibitors
What is the MOA of sirolimus?
- Binds to Immunophilin (FKBP-12) but does NOT inhibit calcineurine.
- BLOCKS mTOR (mammalian target of rapamycin) –> BLOCKS THE RESPONSE OF T CELL TO CYTOKINES
- A potent inhibitor of B-cell proliferation and immunoglobulin production
What is the most important toxicity associated with Sirolimus?
PROFOUND MYELOSUPPRESSION, especially thrombocytopenia
RH0 Immune Globulin Micro-Dose is used in the prevention of what disease?
Hemolytic disease of newborns
What are the indications for Hyperimmune Immunoglobulins?
Respiratory syncytial virus; CMV; Varicella zoster, Human Herpes virus-3; Hep B; Rabies; Tetanus; Digoxin overdose
What drugs classification does Alemtuzumab, Bevacizumab, Cetuximab, Gemtuzumab, Rituximab, and Trastuzumab fit into?
Monoclonal Antibodes - which are Immunosuppressive antibodies
MOA of Alemtuzumab?
Humanized IgG1 that binds to CD52 on normal and malignant B and T lymphocytes, NK cells, monocytes, and macrophages