Calcineurin Inhibitor

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

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II. Indications

  1. Solid Organ Transplant Immunosuppression (maintenance prevention of rejection)

III. Preparations

  1. Cyclosporine (Sandimmune)
  2. Tacrolimus (Prograf)
  3. Voclosporin

IV. 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)

V. 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)

VI. 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

VII. References

  1. Cimino (2016) Am Fam Physician 93(3): 203-10 [PubMed]
  2. Costanzo (2010) J Heart Lung Transplant 29(8): 914-56 [PubMed]

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Related Studies

Cost: Medications

cyclosporine (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
CYCLOSPORINE 0.05% EYE EMULSION Generic $3.93 each
CYCLOSPORINE 100 MG CAPSULE Generic $6.70 each
CYCLOSPORINE 25 MG CAPSULE Generic $2.30 each
CYCLOSPORINE MODIFIED 100 MG Generic $1.44 each
CYCLOSPORINE MODIFIED 25 MG Generic $0.43 each
CYCLOSPORINE MODIFIED 50 MG Generic $1.16 each
tacrolimus (on 11/2/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
TACROLIMUS 0.03% OINTMENT Generic $0.73 per gram
TACROLIMUS 0.1% OINTMENT Generic $1.91 per gram
TACROLIMUS 0.5 MG CAPSULE (IMMEDIATE RELEASE) Generic $0.19 each
TACROLIMUS 1 MG CAPSULE (IMMEDIATE RELEASE) Generic $0.28 each
TACROLIMUS 5 MG CAPSULE (IMMEDIATE RELEASE) Generic $1.55 each
prograf (on 1/12/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
PROGRAF 0.5 MG CAPSULE Generic $0.19 each
PROGRAF 1 MG CAPSULE Generic $0.28 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information. GoodRx is another tool for finding lower drug prices.

Related Topics in Pharmacology

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