Immuner modulating drugs Flashcards
Cyclosporin/ Sandimmune
Class
MOA
SE
Immunosupp ressant drug derived from a soil fungus
- Target Calcineurin, Inhibit production of interleukinn 1,2,3,4 and IF-y, thus stoping activated T- Lymphocytes from reproducing
N/V, diarrhea, loss of appetite, High blood pressure, kidney damage, tremors, HA, seizures, excessive hair grown, excessive gum growth, confusion, coma, and gout……. Cleared by P450- 3A4
Cyclosporin/ Sandimmune
Indication
Prevent rejection of Kidney, liver and heart transplants as well as for treatment of RA and other autoimmune diseases. Also used in Severe dermatitis
Cyclosporin/ Sandimmune
Interactions
Phenobarbit one, Phenytoin and Rifampin enhance clearance.
Erythromycin or Ketoconazol e, grapefruit juice decrease clearance
Methotrexate
MOa
Prevent clonal expansion of both B and T lymphocytes - Methotrexate - Is a purine analog of Folate B-9 that gets polyglutamat ed and will slow/alter growth of cells using B-9. Slows formation of GMP and AMP, making DNA unstable.
- As Abortifacient , Low hCG, Low progesteron e, are used to ascertain if Methotrexate is working
Methotrexate dosege considerations
Polyglutamat e can be measured in the blood to gauge doseage, Polyglutamat ed Methotrexate is the active form. Taken Weekly, not daily
Methotrexate SE
Hepatic Toxicity, Nephro Toxicity,Gen etic malformation s in the MHTFR, N/ V, oral ulcerations, Hepatitis, blood dycrasias and immunosupp ression. -Causes Pulmonary Fibrosis and is treatment for pulmonary Fibrosis
Methotrexate class
Anti- metabolite, anti-folate immunosupp ressant and chemotherap eutic
Methotrexate indications
Cancer, AI, Abortifacient
Azathioprine/ Imuran
MOA
Metabolic breakdown products of Azathiprine act to inhibit purine synthesis which will block protein synthesis, particularly in cells that experience rapid turn over—— gets conve
Azathioprine/ Imuran
Dose
SE
Class
INd
3-5 mg/kg/ day
Bone marrow depression - Takes 12 months or longer to take effect
Purine anti- metabolite immunosupp ressant
Prevention of transplant rejection, inflammatory bowel disease, SLE and rheumatoid arthritis
Tacrolimus/ Program
MOA
T-Cell inhibition similar to that of Cyclosporine .Tacrolimus is approximatel y 100x more potent in its immunosupp ressive effects then an equal volume of cyclosporine
Tacrolimus/ Program SE
N/V diarrhea, loss of appetite, high blood pressure, kidney damage and increased risk for infection
Tacrolimus/ Program
Class
Immunosupp rressant drug related to the macrolide class of antibiotics extracted from soil microorganis m.
Tacrolimus/ Program
Char
Protection against rejection of organ transplantati on. Topical treatment for severe eczema
Metabolized by the P450… avoid grape juice
Etanercept/ Enbrel
MOA
Mimics the inhibitory effects of naturally occurring soluble anti- TNF receptors, however it has double the half life of biologic form