[.
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Action/Kinetics:
Believed to interfere with metabolic pathways of amino acids leading from glutamic acid to the citric acid cycle and urea. Also affects cell energy production needed for mitosis (affects growing cells in metaphase) and interferes with nucleic acid synthesis. Rapidly cleared from plasma but poor penetration to the brain. About 75% bound to serum proteins. Almost completely metabolized in the liver after IV administration.
t
1/2, triphasic: initial, 3.7 min; intermediate, 1.6 hr; final, 24.8 hr. Metabolites are excreted in the bile with smaller amounts in the urine. No cross-resistance with vincristine.
Uses:
Palliative treatment of generalized Hodgkin's disease (stages III and IV, Ann Arbor modification of Rye staging system); lymphocytic lymphoma (nodular and diffuse, poorly and well differentiated); histiocytic lymphoma; advanced stages of mycosis fungoides; advanced testicular carcinoma; Kaposi's sarcoma; Letterer-Siwe disease (histiocytosis X).
Less effective for palliative treatment of coriocarcinoma resistant to other chemotherapy; breast cancer unresponsive to endocrine surgery and hormonal therapy.
Usually given in combination therapy. However, it has been used as a single agent to treat Hodgkin's disease and advanced testicular germinal-cell cancers (although combination therapy is more effective).
Contraindications:
Leukopenia, granulocytopenia. Bacterial infections. Lactation.
Additional Side Effects:
Toxicity is dose-related and more pronounced in clients over age 65 or in those suffering from cachexia (profound general ill health) or skin ulceration.
GI: Ileus, rectal bleeding,
hemorrhagic enterocolitis vesiculation of the mouth,
bleeding from a former ulcer.
Dermatologic: Total epilation, skin vesiculation.
Respiratory: Acute SOB,
severe bronchospasm.
Neurologic: Paresthesias, neuritis, mental depression, loss of deep tendon reflexes,
seizures. Extravasation may result in phlebitis and cellulitis with sloughing.
Overdose Management:
Symptoms: Exaggeration of side effects (see the above). Neurotoxicity.
Treatment:
- If ingestion is discovered early enough, oral activated charcoal slurry should be given followed by a cathartic.
- Treat side effects due to inappropriate secretion of ADH.
- Prevent ileus (e.g., enemas, cathartic).
- Administer an anticonvulsant (e.g., phenobarbital), if necessary.
- Monitor the CV system.
- Monitor blood counts daily to determine risk of infection and whether blood transfusions are necessary.
Drug Interactions:
-
Bleomycin sulfate
and cisplatin / Combination of bleomycin, cisplatin, and vinblastine may produce signs of Raynaud's disease in clients with testicular cancer
-
Erythromycin / Severe myalgia, neutropenia, and constipation
-
Glutamic acid / Inhibits effect of vinblastine
-
Mitomycin C / Severe bronchospasm with SOB
-
Phenytoin /
Effect of phenytoin due to
plasma levels
-
Tryptophan / Inhibits effect of vinblastine
How Supplied:
Injection: 1 mg/mL;
Powder for injection: 10 mg
Dosage
?IV
Individualized, using WBC count as guide. Administered once every 7 days.
Adults, initial: 3.7 mg/m
2;
then, after 7 days, graded doses of 5.5, 7.4, 9.25, and 11.1 mg/m
2 at intervals of 7 days (maximum dose should not exceed 18.5 mg/m
2).
Children, initial: 2.5 mg/m
2;
then, after 7 days, graded doses of 3.75, 5.0, 6.25, and 7.5 mg/m
2 at intervals of 7 days (maximum dose should not exceed 12.5 mg/m
2).
Maintenance doses are calculated based on WBC count--at least 4,000/mm
3.