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Calcineurin Inhibitor

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Calcineurin Inhibitor, Cyclosporine, Sandimmune, Tacrolimus, Prograf, Voclosporin

  • See Also
  1. Pimecrolimus (Elidel)
  • Indications
  1. Solid Organ Transplant Immunosuppression (maintenance prevention of rejection)
  • Preparations
  1. Cyclosporine (Sandimmune)
  2. Tacrolimus (Prograf)
  3. Voclosporin
  • Adverse Effects
  1. Cardiovascular adverse effects
    1. Hypertension
    2. Hyperlipidemia (Cyclosporine)
  2. Neurologic adverse effects
    1. Headaches
    2. Tremor
    3. Neuropathy
    4. Seizures
  3. Miscellaneous adverse effects
    1. Nephrotoxicity
    2. Hyperkalemia
    3. Gingival Hyperplasia (Cyclosporine)
    4. Diabetes Mellitus (Tacrolimus)
  • Drug Interactions
  • Agents that increase Calcineurin Inhibitor concentrations
  1. See Cytochrome P-450 3A4
  2. Antibiotics
    1. Aminoglycosides
    2. Ofloxacin (other Fluoroquinolones such as Ciprofloxacin and Levofloxacin may be used with caution)
    3. Erythromycin (and Clarithromycin to a lesser extent)
    4. Metronidazole (Flagyl)
  3. Antifungal agents
    1. Amphoteracin B
    2. Fluconazole
    3. Itraconazole
    4. Ketoconazole
  4. Cardiovascular agents
    1. Amiodarone
    2. Spironolactone (Hyperkalemia risk)
    3. Nondihydropyridine Calcium Channel Blockers (Diltiazem, Verapamil)
  5. Foods
    1. Grapefruit (and juice)
    2. Pineapple, papaya (affect Cyclosporine)
    3. Pomegantes (and juice)
  6. Misellaneous agents
    1. Ethinyl Estradiol (Oral Contraceptives)
    2. Warfarin (Coumadin)
    3. NSAIDS (Nephrotoxicity Risk)
  • Drug Interactions
  • Agents that decrease Calcineurin Inhbitor concentrations
  1. See Cytochrome P-450 3A4
  2. Antibiotics
    1. Nafcillin
    2. Rifampin
  3. Seizure medications
    1. Carbamazepine (Tegretol)
    2. Phenytoin (Dilantin)
    3. Valproic Acid
  4. Supplements
    1. Echinacea (risk of Transplant Rejection)
    2. St. John's Wort
  5. Gastrointestinal agents
    1. Antacids
    2. Loperamide (Imodium)
  6. Miscellaneous agents
    1. Cholestyramine
  • References
  1. Cimino (2016) Am Fam Physician 93(3): 203-10 [PubMed]
  2. Costanzo (2010) J Heart Lung Transplant 29(8): 914-56 [PubMed]