Term
Cyclosporine
Use
mechanism
Adv. Effects
Contra
Interactions
Metabolism |
|
Definition
Prevent Trans rejection/GVHD
Autoimmune/Inflammatory disorders
Bind to cyclophilin
Inhibit calcineurin
Stop NF-AT from entering nucleus
Stop cytokine production
Nephrotoxicity (does limiting - via renal vasoconstriciton)
Neurotoxicity (tremor)
Hypertension
Hyperlipidemia
Hyperuricemia
Hyperkalemia
Hirsutism
Gingival hyperplasia
Breastfeeding
Hypersensitivity
Statins via CYP3A4
CYP3A4/PGP inhibitor |
|
|
Term
Tacrolimus
Use
mechanism
Adv. Effects
Contra
Metabolism |
|
Definition
Prevent & Treat Trans. rejection/GVHD
Bind to FKBP
Inhibit calcineurin
Stop NF-AT from entering nucleus
Stop cytokine production
Nephrotoxicity (dose limit - via renal vasoconstriciton)
Neurotoxicity (tremor +)
Hypertension
Hyperkalemia
Hyperglycemia
Liver enzymes up
GI upset
Breastfeeding
Hypersensitivity
CYP3A4/PGP metabolism
High protein binding |
|
|
Term
Sirolimus
Use
mechanism
Adv. Effects
Contra
Metabolism |
|
Definition
Prevent Trans Rejection
Bind FKBP
inhibit mTOR in IL-2 pathway
Stop G1->S phase
Stops proliferation
Hypertension
Hyperlipidemia
Lymphocele risk up (renal transplant)
Poor wound healing
Clotting disorders
Anemia/neutropenia
No contra
Synergism w/ cyclosporin
CsA - up [sirolimus]
increase nephrotoxicity
CYP3A4/PGP |
|
|
Term
Mycophenolate
Class
Use
mechanism
Adv. Effects
Interactions
Metabolism |
|
Definition
Anti-metabolite
Prevent/Treat Trans rejection/GVHD
Autoimmune diseases
noncompetitive IMPDH inhib.
stop de novo purine synthesis
Stop DNA/RNA synthesis
GI upset
Renal tubular necrosis 10-20%
Myelosuppression
CsA inhibits secretion into bile
Glucuronide conjug.
Excreted via kindey and bile (enterohepatic recycling)
High protein bound
No Cyp/PGP |
|
|
Term
Methotrexate
Class
Use
mechanism
Adv. Effects
Contra
Interactions
Metabolism |
|
Definition
Anti-metabolite
Prevent GVHD (rare
cancer chemo
Inflammatory/autoimmune disease
RA
Psoriasis
Folate antimetabolite
AICAR build up
Adenosine up
Inhibit NF-kB
Inhibit purine.pyrimadine synthesis
Hepatotoxicity
GI
Hyperhomocysteinuria
Myelosuppression
Renal toxicity (precip in tubules)
Teratogenesis
Pregnancy/Breastfeeding
Myelosuppression/AIDS
Salicylates/NASIDs compete prot binding
Penicillin inhib MTX elimination
Folate supplement - stop adverse effects.
Polyglutamated in cell - retention
High protein binding
No CYP/PGP |
|
|
Term
Azathioprine
Class
Use
mechanism
Adv. Effects
Contra
Interactions
Metabolism |
|
Definition
Anti-metabolite
Prevent Trans rejection
Autoimm/Inflamm diseases
->6-MP->6-TGN
6TGN stops DNA synthesis (dideoxy)
6MP inhibit de novo purine synthesis
GI upset
Myelosuppression
Hepatotoxicity
Pregnancy/Breastfeeding
Xanthine oxidase destroys 6MP
Allopurinol (gout) inhibits xan oxid.
No CYP/PGP (Xan oxidase) |
|
|
Term
Antithymocyte Globulin
Class
Use
mechanism
Adv. Effects
Contra |
|
Definition
Antibody
Prevent/Treat Trans rejec/GVHD
Anti-T-cell Ab
Opsonize T cells
Serum sickness
Thrombocytopenia/neutropenia (cross rxn)
Hypersensitivity to rabbit/horse |
|
|
Term
Muromonab
Class
Use
mechanism
Adv. Effects
Contra |
|
Definition
Antibody
Treat Trans rejection
Anti-CD3
Internalization of TCR
Cytokine release syndrome
Severe pulmonary edema
Hypervolemia
Heart Failure
Hypersensitivity to mouse |
|
|
Term
Daclizumab
Class
Use
mechanism
Adv. Effects
Contra |
|
Definition
Antibody
Prevent Trans rejection
Anti IL2R AB
inhibit IL-2 and activ. of T cells
Serum sickenss
use in combo - no added ADR
Hypersensitivity |
|
|
Term
Basiliximab
Class
Use
mechanism
Adv. Effects
Contra |
|
Definition
Antibody
Prevent Trans rejection
Anti IL2R AB
inhibit IL-2 and activ. of T cells
Serum sickenss
use in combo - no added ADR
Hypersensitivity |
|
|
Term
Cyclophosphamide
Use
Mechanism |
|
Definition
Lupus nephritis
Prevent/treat trans rejection
Cancer chemo
Alkylating agent - DNA cross links |
|
|
Term
Glucocorticoids
Use
Mechanism
Adverse Effects |
|
Definition
Prevent/Treat Trans rejection
Autoimm/Inflamm dis
RA - for flare ups (last resort)
SLE
Bind to receptor
Reverse NF-kB actions
Deacetylation of histones
Turn off HAT/NF-kB
Bind ot DNa promoters
CNS stimulation
Appetite stimulation OR NV
Adrenal crisis
Infection risk up
Osteoporosis
Diabetes
Glaucoma |
|
|
