Bleomycin sulfate
Bleomycin sulfate (Blenoxane)
Bleomycin sulfate
(blee-oh-
MY-sin)
Pregnancy Category: D
Blenoxane (Abbreviation: BLM)
(Rx)
Classification:
Antineoplastic, antibiotic
See Also:
See also
Antineoplastic Agents
[.
]
Action/Kinetics:
Bleomycin is a mixture of cytotoxic glycopeptide antibiotics isolated from
Streptomyces verticillus. The action may be due to binding to DNA, inducing lability of the DNA structure and decreasing synthesis of DNA and to a lesser extent RNA and protein. Most effective in the G
2 and M phases of cell division. Drug currently used is mostly a mixture of bleomycin A
2 and B
2. Relatively low bone marrow depressant activity, localizes in certain tissues, and is an important component of some combination regimens.
Peak plasma levels (after 4-5 days of therapy): 50 ng/mL.
t
1/2, distribution, after IV: 10-20 min.
Peak blood levels, after IM: 30-60 min with levels that are about one-third that of IV.
t
1/2, elimination, C
CR less than 35 mL/min: About 2 hr; half-life increases exponentially as (creatinine clearance) decreases below 35 mL/min. Two-thirds excreted in the urine as active bleomycin.
Uses:
Palliative treatment of cancers listed, either used alone or in combination. Squamous cell carcinoma of the head and neck, including mouth, tongue, tonsil, nasopharynx, oropharynx, sinus, palate, lip, buccal mucosa, gingiva, epiglottis, skin, and larynx. Carcinoma of the skin, penis, cervix, and vulva. Lymphomas, including Hodgkin's, non-Hodgkin's, reticulum cell sarcoma, and lymphosarcoma. Testicular carcinoma, including embryonal cell, choriocarcinoma, and teratocarcinoma. Sclerosing agent to prevent or treat malignant pleural effusions associated with cancer.
Investigational: Soft tissue sarcomas, osteosarcoma, malignant effusions (peritoneal, pleural), ovarian tumors. Also for severe, recalcitrant common warts (verruca vulgaris).
Contraindications:
Lactation. Renal or pulmonary diseases. Pregnancy.
Special Concerns:
Safety and efficacy have not been determined in children. When used in combination with other antineoplastic drugs, pulmonary toxicity may occur at lower doses.
Side Effects:
Pulmonary: Pneumonitis,
pulmonary fibrosis, especially in older clients.
Hypersensitivity: In approximately 1% of lymphoma clients, an idiosyncratic reaction manifested by hypotension, fever, chills, mental confusion, and wheezing has been reported.
Integumentary and mucous membranes: Erythema, rash, striae, vesiculation, hyperpigmentation, skin tenderness, hyperkeratosis, nail changes, alopecia, pruritus, stomatitis, skin toxicity.
GI: Vomiting, anorexia, weight loss.
Miscellaneous: Renal and hepatic toxicity.
Drug Interactions:
-
Digoxin /
Serum digoxin levels
-
Filgrastim /
Risk of pulmonary toxicity
-
Phenytoin /
Serum phenytoin levels
How Supplied:
Powder for injection: 15 U, 30 U
Dosage
?SC, IM, IV
Hodgkin's disease.
Initial: 0.25-0.5 units/kg (10-20 units/m
2 once or twice weekly).
Maintenance: After a 50% response, give 1 unit/day or 5 units/week given IM or IV. Due to pulmonary toxicity, give doses greater than 400 units with great caution.
Squamous cell carcinoma, non-Hodgkin's lymphoma, testicular carcinoma.
0.25-0.5 units/kg (10-20 units/m
2) once or twice a week. Due to the possibility of anaphylaxis, lymphoma clients should receive 2 units or less for the first two doses; if no acute reaction occurs, follow the regular dosage schedule.
?Intrapleural Injection
Malignant pleural effusion.
60 units given as a single bolus dose by a thoracostomy tube following drainage of excess pleural fluid and confirmation of complete lung expansion.
?Intralesional
Warts.
0.2-0.8 unit (depending on the size) one or more times q 2-4 weeks (up to a maximum total dose of 2 units using a solution of 15 units of sterile bleomycin solution in 15 mL 0.9% saline or water for injection). |
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