Study your flashcards anywhere!

Download the official Cram app for free >

  • Shuffle
    Toggle On
    Toggle Off
  • Alphabetize
    Toggle On
    Toggle Off
  • Front First
    Toggle On
    Toggle Off
  • Both Sides
    Toggle On
    Toggle Off
  • Read
    Toggle On
    Toggle Off
Reading...
Front

How to study your flashcards.

Right/Left arrow keys: Navigate between flashcards.right arrow keyleft arrow key

Up/Down arrow keys: Flip the card between the front and back.down keyup key

H key: Show hint (3rd side).h key

A key: Read text to speech.a key

image

Play button

image

Play button

image

Progress

1/20

Click to flip

20 Cards in this Set

  • Front
  • Back
IMMUNOSUPPRESSANTS:
Calcineurin inhibitors:
- Cyclosporine
- Tacrolimus
Metabolite of the fungus B. Nivea
Cyclosporine (SANDIMMUNE, NEORAL)
MOA of Cyclosporine:
Inhibits antigen-triggered signal transduction in T-lymphocytes.
CYCLOPHILIN:
Cytoplasmic receptor protein
Indication for cyclosporin
1. organ transplant
2. RA
3. PSORIASIS
Cyclosporin used in combo with:
1. glucocorticoids
2. AZA
3. Mycophenolate mofetil
4. sirolimus
MOST COMMON SIDE EFFECT OF CYCLOSPORIN:
1. Nephrotoxicity
2. HTN - 50% of renal transplant and almost all cardiac transplant
Drugs that DECREASE cyclo.
1. Rifampin
2. Phenobarbital
3. Phenytoin.
Increase cyclo:
1. Verapamil, nicardipine
2. Fluconazole, Keto
3. Erythromycin
4. Indinavir
5. Grape fruit juice
Cyclo reduces CL
1. digoxin
2. lovastatin
3. prednisolone
TACROLIMUS same pathway except binds to:
FKBP-12 an immunophilin structually related to cyclophilin.
Therapeutic Dosage
Prophylaxis of solid organ rejection.
Toxicity of Tacrolimus:
if switching b/w cyclo wait for 24 hrs.
Nephrotoxicity
Neurotoxicity
GI complaint
Hypertension
Hyperkalemia
Hyperglycemia
Nephrotoxicity of Tacrolimus:
Negative effect of pancreatic islet beta cells:
1. glucose intolerance
2. diabetes mellitus
3. increased risk of secondary tumors and opportunistic infections.
RAPAMUNE (Sirolimus/Rapamycin)
Macrocyclic lactone produced by STREPTOMYCES HYGROSCOPICUS
RAPAMUNE
inhibits the mammalian kinase, target of rapamycin (mTOR)
rapamune used in conjunction with:
calcineurin inhibitor and glucocorticoids for PROPHYLAXIS of organ transplant rejection
Use of Sirolimus:
dose-dependent increase in serum cholesterol and TG that may require tx.
Mycophenolate Mofetil (cellcept)
- ester prodrug
- mycophenolic drug (active drug)
INHIBITS INOSINE MONOPHOSPHATE DEHYDROGENASE
CELLCEPT is decreased absorption when:
CO-ADM with Al/Mg hydroxide
cholestyramine