Bleomycin

Bleomycin injection is used as a palliative (disease-managing) cancer treatment, either alone or alongside other chemotherapy drugs. Here are the conditions it is used for:

• Squamous cell carcinoma of the head and neck — including the mouth, tongue, tonsil, nasopharynx, oropharynx, sinuses, palate, lip, buccal mucosa, gums, epiglottis, skin, and larynx; note that response is poorer in patients who have already had radiation to the head and neck
• Squamous cell carcinoma of the penis, cervix, and vulva
• Hodgkin's disease and non-Hodgkin's lymphoma
• Testicular carcinoma — including embryonal cell carcinoma, choriocarcinoma, and teratocarcinoma
• Malignant pleural effusion (fluid buildup around the lungs) — when given as an intrapleural injection, Bleomycin acts as a sclerosing agent to seal off the space and prevent recurrence

Bleomycin's main action is to interfere with a cancer cell's DNA. It causes breaks in the DNA strands — both single and double-strand breaks — which the cell cannot easily repair. This stops the cell from copying itself and triggers a halt in the cell cycle at a stage called G2/mitosis. The result is that cancer cells are unable to divide and multiply. When injected directly into the pleural space (around the lungs), bleomycin works differently: it acts as a sclerosing agent, causing the lining of the lungs and chest wall to stick together so fluid can no longer collect there.

One reason bleomycin is particularly toxic to the lungs and skin is that the enzyme responsible for breaking it down — bleomycin hydrolase — is found in most body tissues except the skin and lungs. That means those two tissues have less protection against the drug's effects.

Bleomycin is given only by injection — never by mouth. The route (into a vein, muscle, under the skin, or into the chest cavity) depends on what it is being used for. For most cancers, it is typically given once or twice a week. For malignant pleural effusion, it is given as a single intrapleural injection directly into the chest cavity.

• Lymphoma patients receive a smaller test dose for the first two treatments to check for a severe reaction before full dosing begins
• Patients with reduced kidney function need lower doses — your care team will adjust based on kidney function tests
• Total cumulative dose is tracked carefully; lung toxicity risk rises sharply above 400 units total

Always follow your prescriber's exact schedule. This medicine is prepared and administered by your healthcare team.

Bleomycin can cause a range of side effects — some common, some serious enough to require stopping treatment.

• Skin and mucous membrane changes (about 50% of patients): rash, redness, darkening, blistering, skin thickening, nail changes, hair loss, itching, and mouth sores
• Fever and chills
• Nausea, loss of appetite, and weight loss (which may persist after treatment ends)
• Pain at the injection or tumor site
• Shortness of breath or cough (early lung warning signs)
• Low blood pressure

If you notice any shortness of breath, new cough, or chest tightness, contact your doctor right away — these can be the earliest signs of serious lung damage. A sudden severe reaction with confusion, low blood pressure, and wheezing — most likely after the first or second dose in lymphoma patients — requires emergency medical attention immediately.

• Lung toxicity (pulmonary fibrosis): This is the most serious risk. About 10% of patients develop lung inflammation (pneumonitis); in about 1%, this progresses to permanent lung scarring (pulmonary fibrosis), which can be fatal. Risk is higher in patients over 70 and those with higher total cumulative doses, but it can occur unpredictably at any age or dose. Regular chest X-rays and lung function monitoring are essential throughout treatment.
• Oxygen sensitivity during surgery: Bleomycin sensitizes lung tissue. Even normal surgical oxygen levels can trigger serious lung damage in people who have received this drug. Always inform your anesthesiologist and surgical team of your bleomycin history.
• Severe idiosyncratic reactions: About 1% of lymphoma patients have a serious reaction — low blood pressure, confusion, fever, chills, wheezing — typically after the first or second dose. Close monitoring after these doses is essential.
• Kidney and liver toxicity: Bleomycin can impair kidney and liver function at any point during therapy. Kidney impairment also slows bleomycin clearance, increasing all other risks.
• Pregnancy: Bleomycin is classified Pregnancy Category D — it can cause serious harm to a developing baby. Women who can become pregnant must avoid pregnancy during treatment.

Because bleomycin is cleared mainly through the kidneys, drugs that affect kidney function can significantly change how much bleomycin stays in your body — and for how long.

• Cisplatin and other kidney-toxic drugs: These can reduce bleomycin's clearance, causing it to build up to dangerous levels. Fatal lung toxicity has been reported when bleomycin was used alongside cisplatin in a patient with unrecognized kidney failure.
• Any nephrotoxic (kidney-harming) drug: Slowing bleomycin's elimination can amplify its toxicity across all organ systems.
• G-CSF (filgrastim) and other cytokines: Some reports have suggested a possible increased risk of lung toxicity when these immune-stimulating drugs are combined with bleomycin, though randomized studies have not confirmed this definitively.

This is not a complete list of interactions. Always talk with your doctor or pharmacist before starting, stopping, or changing any medication.

• Previous reaction to bleomycin: Do not use bleomycin if you have had a prior hypersensitivity or severe idiosyncratic reaction to it — this is a contraindication.
• Kidney problems: Bleomycin is primarily cleared by the kidneys. Reduced kidney function requires careful dose adjustment and close monitoring.
• Lung problems: Pre-existing pulmonary (lung) disease requires extreme caution. Discuss your lung history fully with your prescriber.
• Upcoming surgery: Tell every member of your surgical and anesthesia team that you have received bleomycin. Special precautions around oxygen use are needed.
• Pregnancy: Bleomycin can harm a developing baby. Women of childbearing potential should use effective contraception and inform their doctor immediately if pregnancy occurs during treatment.
• Older adults: Patients over 70 face a higher risk of serious lung toxicity and require especially close monitoring.
• Lymphoma patients: At higher risk for the severe first-dose reaction — the first two doses require close medical observation.
• Children under 3 years: Young children clear bleomycin faster than adults; children over 8 have comparable clearance to adults. Dose adjustments may be needed.

Bleomycin causes breaks in cancer cell DNA — both single-strand and double-strand cuts — which prevents the cell from dividing and triggers cell cycle arrest at the G2 and mitosis stages. In the lungs and skin, bleomycin is more active because these tissues lack the enzyme (bleomycin hydrolase) that normally breaks the drug down, making them particularly vulnerable to its toxic effects. When introduced into the pleural space, bleomycin produces local irritation that causes the lung lining and chest wall to scar together, eliminating the space where fluid accumulates.

Bleomycin is rapidly absorbed after intramuscular, subcutaneous, or intrapleural injection, reaching peak blood levels within 30 to 60 minutes. It is widely distributed throughout the body. The drug is broken down by an enzyme called bleomycin hydrolase found in most tissues, but this process matters mainly when kidney function is severely reduced. The kidneys are the primary route of elimination — about 65% of an intravenous dose leaves the body in urine within 24 hours, with a half-life of about 2 hours in people with normal kidney function. When kidney function is impaired, bleomycin clears much more slowly, and the half-life can increase dramatically — raising the risk of toxicity significantly.

Store refrigerated between 2° and 8°C (36° and 46°F). refrigeration and should not be used after the expiration date is reached.