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Vinblastine

Vinblastine is a chemotherapy medication, typically used with other medications, to treat a number of types of cancer. This includes Hodgkin's lymphoma, non-small cell lung cancer, bladder cancer, brain cancer, melanoma, and testicular cancer. More

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Description

Vinblastine is a chemotherapy medication, typically used with other medications, to treat a number of types of cancer. This includes Hodgkin's lymphoma, non-small cell lung cancer, bladder cancer, brain cancer, melanoma, and testicular cancer.

Generic Name

Vinblastine

Chemical names

Vinblastine; Vincaleukoblastine; Velban; Vincaleucoblastine

Brand names

Cytoblastin, Uniblastin, Vblastin

IUPAC name

methyl (1R,9R,10S,11R,12R,19R)-11-(acetyloxy)-12-ethyl-4-[(13S,15R,17S)-17-ethyl-17-hydroxy-13-(methoxycarbonyl)-1,11-diazatetracyclo[13.3.1.0?,¹².0?,¹?]nonadeca-4(12),5,7,9-tetraen-13-yl]-10-hydroxy-5-methoxy-8-methyl-8,1

Pharmacokinetics

Hepatic metabolism.

Actions

Vinblastine is a vinca alkaloid antineoplastic agent. The vinca alkaloids are structurally similar compounds comprised of 2 multiringed units: vindoline and catharanthine. Vinblastine has some immunosuppressant effect. The vinca alkaloids are considered to be cell cycle phase-specific.

Dosage/Dosage form

The recommended dose is 3.7 mg/m2 as IV, dose may be increased if needed.

Therapeutic uses

For treatment of lymphomas, breast cancer, neuroblastoma, testicular cancer, Hodgkin's and non-Hodgkin's lymphomas, mycosis fungoides, histiocytosis, and Kaposi's sarcoma.

Adverse effects/Side effects

Alopecia, constipation, malaise, stomatitis, GI bleeds, dose-limiting bone marrow suppression (e.g. granulocytopenia, thrombocytopenia, anaemia), hypertension, central and peripheral neurotoxicity, vomiting, 8th cranial nerve damage resulting in vestibular and auditory toxicity, ischaemic cardiac toxicity, breathlessness, bone, tumour or jaw pain, nausea, necrosis.

Interaction

  • Increased toxicity of vinblastine with erythromycin.
  • Increased myelotoxicity and neurotoxicity with azole antifungals e.g. itraconazole and posaconazole.
  • Reduced vinblastine metabolism with miconazole.
  • Possible increase in vinblastine levels with aprepitant.
  • Variable interactions with Phenytoin
  • Reduced immune response with vaccines.
  • Additive myelotoxicity with zidovudine.
  • Increased toxicity when ganciclovir is given with, immediately before or after vinblastine.
  • Concurrent admin of vinblastine with CYP3A inhibitors may cause an earlier onset and/or an increased severity of side effects.
  • Increased risk of severe neutropenia with ritonavir.
  • Increased risk of acute pulmonary toxicity with mitomycin.

Contraindications

  • Severe bone marrow suppression; presence of bacterial infection; maglignant cell infiltration of bone marrow; Injection into extremity with poor circulation; porphyria; granulocytopenia.
  • Elderly with extreme skin ulcerations or cachexia.
  • Pregnancy; lactation.
  •  Intrathecal use may result in death.

Storage

Store at 2-8°C

Information

Molecular weight

810.9741

Molecular formula

C46H58N4O9

CAS number

865-21-4

Precautions

  • If extravasation occurs discontinue immediately, with local injection of hyaluronidase and local heat application to decrease discomfort and risk of cellulitis; remaining injection to be injected into another vein. Routine prophylaxis against constipation recommended especially in high doses.
  • Neurotoxicity; Hepatic impairment; ischemic heart disease; preexisting pulmonary dysfunction; extravasation may cause tissue damage and pain.
  • Nadir in leukocyte count occur 4-10 days after vinblastine admin; recovery observed 7-14 days after treatment.