Indications
Treatment of: Lymphomas, Squamous cell carcinoma,
Testicular embryonal cell carcinoma, Choriocarcinoma,
Teratocarcinoma. Intrapleural administration to
prevent the reaccumulation of malignant effusions.
Action
Inhibits DNA and RNA synthesis. Therapeutic Effects:
Death of rapidly replicating cells, particularly
malignant ones.
Pharmacokinetics
Absorption: Well absorbed from IM and subcut
sites. Absorption follows intrapleural and intraperitoneal
administration.
Distribution: Widely distributed, concentrates in
skin, lungs, peritoneum, kidneys, and lymphatics.
Metabolism and Excretion: 60–70% excreted
unchanged by the kidneys.
Half-life: 2 hr (qin renal impairment).
TIME/ACTION PROFILE (tumor response)
ROUTE ONSET PEAK DURATION
IV, IM, Subcut 2–3 wk unknown unknown
Contraindications/Precautions
Contraindicated in: Hypersensitivity; OB, Lactation:
Potential for fetal, infant harm.
Use Cautiously in: Renal impairment (doseprequired
if CCr 35 mL/min); Pulmonary impairment;
Nonmalignant chronic debilitating illness; Patients with
childbearing potential; Geri:qrisk of pulmonary toxicity
and reduction in renal function.
Adverse Reactions/Side Effects
CNS: aggressive behavior, disorientation, weakness.
Resp: PULMONARY FIBROSIS, pneumonitis. CV: hypotension,
peripheral vasoconstriction. GI: anorexia,
nausea, stomatitis, vomiting. Derm: hyperpigmentation,
mucocutaneous toxicity, alopecia, erythema,
rashes, urticaria, vesiculation. Hemat: anemia, leukopenia,
thrombocytopenia. Local: pain at tumor site,
phlebitis at IV site. Metab: weight loss. Misc: ANAPHYLACTOID
REACTIONS, chills, fever.
Interactions
Drug-Drug: Hematologic toxicityqwith concurrent
use of radiation therapy and other antineoplastics.
Concurrent use with cisplatinpelimination of bleomycin
and mayqtoxicity.qrisk of pulmonary toxicity with
other antineoplastics or thoracic radiation therapy.
General anesthesiaqthe risk of pulmonary toxicity.
qrisk of Raynaud’s phenomenon when used with
vinblastine.
Route/Dosage
Lymphoma patients should receive initial test doses of 2
units or less for the first 2 doses.
IV, IM, Subcut (Adults and Children): 0.25–0.5
unit/kg (10–20 units/m2) weekly or twice weekly initially.
If favorable response, lower maintenance doses
given (1 unit/day or 5 units/wk IM or IV). May also be
given as continuous IV infusion at 0.25 unit/kg or 15
units/m2/day for 4–5 days.
Intrapleural (Adults): 15–20 units instilled for 4 hr,
then removed.
Availability (generic available)
Injection: 15 units/vial, 30 units/vial.
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