Bleomycin

CLINICAL USE


Antineoplastic agent

DOSE IN NORMAL RENAL FUNCTION

Squamous cell carcinoma and testicular teratoma:

  • range 45–60 × 10 3 IU per week IM/IV (total cumulative dose up to 500 × 103 IU)
  • OR, continuous IV infusion 15 × 10 3 IU/24 hours for up to 10 days
  • OR, 30 × 10 3 IU/24 hours for up to 5 days
  • Malignant lymphomas:15–30 × 10 3 IU/week IM to total dose of 225 × 103 IU Lower doses required in combination chemotherapy
  • Malignant effusions:60 × 10 3 IU in 100 mL sodium chloride 0.9% intrapleurally (total cumulative dose of 500 × 103 IU)

    PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Approximately 1500
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :<1
  • %Excreted unchanged in urine &nbsp &nbsp : 60–70

  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :0.3

  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :4 (bolus), 9 (continuous infusion)/20

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50 &nbsp &nbsp : Dose as in normal renal function
  • 10 to 20 &nbsp &nbsp : 75% of normal dose (100% for malignant effusions)
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : 50% of normal dose (100% for malignant effusions)

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Not dialysed. Dose as in GFR <10 mL/min

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Not dialysed. Dose as in GFR <10 mL/min
  • HDF/high flux &nbsp :Unknown dialysability. Dose as in GFR <10 mL/min
  • CAV/VVHD &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in GFR 10 to 20 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs
  • Antipsychotics: avoid concomitant use with clozapine, increased risk of agranulocytosis
  • Cytotoxics: increased pulmonary toxicity with cisplatin; in combination with vinca alkaloids can lead to Raynaud’s syndrome and peripheral ischaemia

    ADMINISTRATION

    Reconstition

  • IM: dissolve required dose in up to 5 mL sodium chloride 0.9% (or 1% solution of lidocaine if pain on injection)
  • IV: dissolve dose in 5–200 mL sodium chloride 0.9%
  • Intracavitary: 60 × 10 3 IU in 100 mL sodium chloride 0.9%
  • Locally: dissolve in sodium chloride 0.9% to make a 1–3 ×103 IU/mL solution

    Route

  • IM, IV, also intra-arterially, intrapleurally, intraperitoneally, locally into tumour

    Rate of Administration

  • Give by slow IV injection, or add to reservoir of a running IV infusion

    Comments

    Avoid direct contact with the skin

    OTHER INFORMATION

  • Lesions of skin and oral mucosa common after full course of bleomycin
  • Pulmonary toxicity: interstitial pneumonia and fibrosis – most serious delayed effectIn patients with moderately severe renal impairment less than 20% of the dose is excreted in the urine
  • Rapid distribution to body tissues (highest concentration is in skin, lungs, peritoneum and lymph)
  • Inactivation takes place primarily in the liver. Approximately 60–70% of drug is excreted unchanged in the urine, probably by glomerular filtration
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