III. Mechanism

  1. Purine Nucleoside antimetabolite analog
  2. Cladribine is metabolized intracellularly to 2-CdATP (Cladribine triphosphate, an active metabolite)
  3. 2-CdATP incorporates into DNA
    1. Results in DNA single strand breaks
  4. Also depletes energy molecules
    1. Nicotinamide Adenine Dinucleotide (NAD)
    2. Adenosine Triphosphate (ATP)
  5. Selectively more toxic to cancerous Lymphocytes and Monocytes
    1. Cladribine is resistant to Adenosine deaminase (therefore selective for Lymphocytes and Monocytes)
    2. Noncancerous Lymphocytes and Monocytes are less responsive to Cladribine

IV. Medications

  1. IV Solution: 10 mg per 10 ml vials

V. Dosing

  1. See other references for disease specific dosing protocols

VI. Adverse Effects

  1. Alopecia
  2. Fever
  3. Headache
  4. Impaired future fertility
  5. Myelosuppression (with prolonged drop in CD4 Count)
  6. Nephrotoxicity
  7. Neurotoxic
  8. Rash

VII. Safety

  1. Avoid in Pregnancy (any trimester)
    1. Use reliable Contraception
  2. Avoid in Lactation
  3. Monitoring
    1. Complete Blood Count
    2. Renal Function tests

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