Nephrology Question 37 Instructor

List 4 classes of drugs that decrease cyclosporine levels and 4 classes of drugs that increase cyclosporine levels.

Cyclosporine is metabolized by the hepatic cytochrome P450 family of enzymes and excreted into the bile. As a result of this, a variety of important drug interactions with drugs that either effect or are metabolized by these enzymes can occur.

Drugs that induce CYP3A4 may decrease the levels of cyclosporine. Examples of these include:

  • Carbamazepine
  • Nafcillin
  • Nevirapine
  • Phenobarbital
  • Phenytoin

Drugs that inhibit CYP3A4 may increase the levels of cyclosporine. Examples of these include:

  • Azole antifungals
  • Clarithromycin
  • Diclofenac
  • Doxycycline
  • Erythromycin
  • Isoniazid
  • Nicardipine
  • Propofol
  • Protease inhibitors
  • Quinidine
  • verapamil

Cyclosporine may increase the levels of CVP3A4 substrates. Examples of substrates include:

  • Benzodiazepines
  • Calcium channel blockers
  • Mirtazapine
  • Sildenafil
  • Tacrolimus
  • Venlafaxine

Selected benzodiazepines (midazolam and triazolam) and selected HMG-CoA reductase inhibitors (lovastatin and simvastatin) are generally contraindicated with strong CYP3A4 inhibitors.

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