VINBLASTINE SULFATE
Chemistry - Commonly referred to as a vinca alklaoid, vinblastine sulfate is isolated from the plant
Cantharanthus roseus (Vinca rosea Linn) and occurs as a white or slightly yellow, hygroscopic, amorphous or crystalline powder that is freely soluble in water. The commercially availableinjection has a pH of 3-5.5. Vinblastine sulfate may also be known as vincaleukoblastine sulfate orby the initials VLB.
Vinblastine sulfate is reportedly compatible with the following intravenous solutions and drugs:
D5W and bleomycin sulfate. In syringes or at Y-sites with: bleomycin sulfate, cisplatin, cyclophosphamide, droperidol, fluorouracil, leucovorin calcium, methotrexate sodium, metoclopramide HCl, mitomycin, and vincristine sulfate.
Vinblastine sulfate compatibility information conflicts or is dependent on diluent or concentration factors with the following drugs or solutions: doxorubicin HCl, and heparin sodium (insyringes). Compatibility is dependent upon factors such as pH, concentration, temperature anddiluents used. It is suggested to consult specialized references for more specific information (e.g.,
Handbook on Injectable Drugs by Trissel; see bibliography).
Vinblastine sulfate is reportedly incompatible with the following solutions or drugs: furosemide.
Vinblastine is extensively metabolized by the liver and is primarily excreted in the bile/feces.
Lesser amounts are eliminated in the urine.
As vinblastine may be a skin irritant, gloves and protective clothing should be worn whenpreparing or administering the medication. If skin/mucous membrane exposure occurs, thoroughlywash area with soap and water.
Little is known about the effects of vinblastine on developing fetuses, but it is believed that thedrug possesses some teratogenic and embryotoxic properties. It may also cause aspermia in males.
Vinblastine may not possess the degree of peripheral neurotoxic effects seen with vincristine, but athigh doses these effects may also be seen. Additional y, vinblastine may cause constipation, alopecia, stomatitis, ileus, inappropriate ADH secretion, jaw and muscle pain, and loss of deeptendon reflexes.
Extravasation of vinblastine may cause significant tissue irritation and cellulitis. Because of thevessicant action of this drug, it is recommended to use a different needle for injecting the drug thanthe one used to withdraw the drug from the vial. Should symptoms of extravasation be noted, discontinue infusion immediately at that site and apply moderate heat to the area to help disperse thedrug. Injections of hyaluronidase have also been suggested to diffuse the drug.
In humans, treatment of overdoses of vinblastine include supportive care and the attempt to preventthe effects associated with the syndrome of inappropriate antidiuretic hormone (fluid restriction andloop diuretics to maintain serum osmolality), anticonvulsants, prevention of ileus, and cardiovascularand hematologic monitoring.
Drug/Laboratory Interactions - Vinblastine may significantly increase both blood and urineconcentrations of uric acid.
Cantharanthus roseus (Vinca rosea Linn) and occurs as a white or slightly yellow, hygroscopic, amorphous or crystalline powder that is freely soluble in water. The commercially availableinjection has a pH of 3-5.5. Vinblastine sulfate may also be known as vincaleukoblastine sulfate orby the initials VLB.
Storage, Stability, Compatibility
The sterile powder for injection, solution for injection and reconstituted powder for injection should all be protected from light. The powder for injection andinjection should be stored in the refrigerator (2-8°C). The intact powder for injection is stable atroom temperature for at least one month. After reconstituting with bacteriostatic saline, the powderfor injection is stable for 30 days if refrigerated.Vinblastine sulfate is reportedly compatible with the following intravenous solutions and drugs:
D5W and bleomycin sulfate. In syringes or at Y-sites with: bleomycin sulfate, cisplatin, cyclophosphamide, droperidol, fluorouracil, leucovorin calcium, methotrexate sodium, metoclopramide HCl, mitomycin, and vincristine sulfate.
Vinblastine sulfate compatibility information conflicts or is dependent on diluent or concentration factors with the following drugs or solutions: doxorubicin HCl, and heparin sodium (insyringes). Compatibility is dependent upon factors such as pH, concentration, temperature anddiluents used. It is suggested to consult specialized references for more specific information (e.g.,
Handbook on Injectable Drugs by Trissel; see bibliography).
Vinblastine sulfate is reportedly incompatible with the following solutions or drugs: furosemide.
Pharmacology - VINBLASTINE SULFATE
Vinblastine apparently binds to microtubular proteins (tubulin) in the mitoticspindle, thereby preventing cell division during metaphase. It also interferes with amino acidmetabolism by inhibiting glutamic acid utilization and preventing purine synthesis, citric acid cycleand urea formation.Uses, Indications
Vinblastine may be employed in the treatment of lymphomas, carcinomas, mastocytomas and splenic tumors in small animals.Pharmacokinetics - VINBLASTINE SULFATE
Vinblastine is administered IV. After injection it is rapidly distributed totissues. In humans, approximately 75% is bound to tissue proteins and the drug does not appreciably enter the CNS.Vinblastine is extensively metabolized by the liver and is primarily excreted in the bile/feces.
Lesser amounts are eliminated in the urine.
Contraindications, Precautions, Reproductive Safety
Vinblastine is contraindicated in patientswith preexisting leukopenia or granulocytopenia (unless a result of the disease being treated), oractive bacterial infection.As vinblastine may be a skin irritant, gloves and protective clothing should be worn whenpreparing or administering the medication. If skin/mucous membrane exposure occurs, thoroughlywash area with soap and water.
Little is known about the effects of vinblastine on developing fetuses, but it is believed that thedrug possesses some teratogenic and embryotoxic properties. It may also cause aspermia in males.
Adverse Effects, Warnings
Vinblastine can cause gastroenterocolitis (nausea/vomiting) and canbe myelosuppressive at usual dosages (nadir at 4-9 days after treatment; recovery at 7-14 days).Vinblastine may not possess the degree of peripheral neurotoxic effects seen with vincristine, but athigh doses these effects may also be seen. Additional y, vinblastine may cause constipation, alopecia, stomatitis, ileus, inappropriate ADH secretion, jaw and muscle pain, and loss of deeptendon reflexes.
Extravasation of vinblastine may cause significant tissue irritation and cellulitis. Because of thevessicant action of this drug, it is recommended to use a different needle for injecting the drug thanthe one used to withdraw the drug from the vial. Should symptoms of extravasation be noted, discontinue infusion immediately at that site and apply moderate heat to the area to help disperse thedrug. Injections of hyaluronidase have also been suggested to diffuse the drug.
Overdosage, Acute Toxicity
In dogs, the lethal dose for vinblastine has been reported as 0.2mg/kg. Effects of an overdosage of vinblastine are basically exacerbations of the adverse effectsoutlined above. Additionally, neurotoxic effects similar to those associated with vincristine may alsobe noted.In humans, treatment of overdoses of vinblastine include supportive care and the attempt to preventthe effects associated with the syndrome of inappropriate antidiuretic hormone (fluid restriction andloop diuretics to maintain serum osmolality), anticonvulsants, prevention of ileus, and cardiovascularand hematologic monitoring.
Drug Interactions
In humans who have previously or simultaneously received mitomycin-Cwith vinca alkaloids, severe bronchospasm has occurred.Drug/Laboratory Interactions - Vinblastine may significantly increase both blood and urineconcentrations of uric acid.