Immunopharmacology Flashcards
What is MoA of Glucocorticoids?
Bind to cytosolic receptors
Cytotoxic T lymphocytes and macrophages inhibited
Antigen-presenting cells inhibited
What is MoA of Cyclosporine?
Calcineurin inhibitor
Cyclosporine forms a complex with cyclophilin
The complex inhibits calcineurin phosphatase activity
Prevents NFAT dephosphorylation
T lymphocyte fails to respond to antigenic stimulation
What is the use of Cyclosporine?
Organ transplantation
Rheumatoid arthritis
Psoriasis
What are the ADR of Cyclosporine?
Renal dysfunction Hypertension Hyperlipidemia Hyperglycemia Gum hyperplasia
What drugs increase cyclosporine levels? What drugs decrease?
Increase- Ca2+ channel blockers (verapamil) because they reverse efflux pump and P450 inhibitors.
Decrease- P450 inducers. Never give along with tacrolimus because enhances renal toxicity
What is MoA of Tacrolimus?
Calcineurin inhibitor
Tacrolimus forms a complex with immunophilin then follows same mechanism as cyclosporine.
What is the use of Tacrolimus?
Prophylaxis of solid-organ allograft rejection
What are the ADR of Tacrolimus?
Hyperglycemia more than cyclosporine
Nephrotoxicity
Hypertension
Neurotoxicity
What is MoA of Sirolimus?
mTOR inhibitor
Binds to FKBP-12- inhibits T-lymphocyte activation and proliferation downstream of the IL-2
What is the use of Sirolimus?
Prophylaxis of organ transplant rejection
What are the ADR of Sirolimus?
BM depression
Increase in serum cholesterol and triglycerides
Hyperglycemia
Because no renal toxicity, is the first line drug to prevent renal transplant rejection
What is MoA of Mycophenolate Mofetil?
IMP dehydrogenase inhibitor
Prevents B and T cell proliferation
What is the use and ADR of Mycophenolate Mofetil?
Use- for prophylaxis of transplant rejection
ADR- Reversible BM depression
What is MoA and use of Levamisole?
Restores depressed immune function of B & T cells
Adjuvant therapy with 5-fluorouracil after surgical resection in patients with colon cancer
What is the use of Thalidomide?
Erythema nodosum leprosum and in multiple myeloma