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Vincristine sulfate or Leurocristine

Vincristine is an antitumor vinca alkaloid isolated from Vinca Rosea. Vincristine is indicated for the treatment of acute leukaemia, malignant lymphoma, Hodgkin's disease, acute erythraemia, and acute panmyelosis. More

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Description

Vincristine is an antitumor vinca alkaloid isolated from Vinca Rosea. Vincristine is indicated for the treatment of acute leukaemia, malignant lymphoma, Hodgkin's disease, acute erythraemia, and acute panmyelosis.

Generic Name

Vincristine sulfate or Leurocristine

Chemical names

Vincristine sulfate; Onkovin; Vincasar PFS; Kyocristine; Vincrisul

Brand names

Alcrist, Biocristin, Cytocristin, Oncocristin-AQ, Unicristin, VCR, Vincristine, Vincryst, Vinlon, Vinstin

IUPAC name

methyl (1R,9R,10S,11R,12R,19R)-11-(acetyloxy)-12-ethyl-4-[(13S,15S,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]-8-formyl-10-hydroxy-5-methoxy-8,1

Pharmacokinetics

Hepatic metabolism

Actions

It is a vinca alkaloid. Indicated as antineoplastic agent used to treat various cancers including Hodgkin's disease, breast cancer, Kaposi's sarcoma, and testicular cancer. The vinca alkaloids are structurally similar compounds comprised of 2 multiringed units, vindoline and catharanthine. This will inhibits the mitosis at metaphase through its interaction with tubulin. 

Dosage/Dosage form

1.4-1.5 mg/m2 once weekly as IV dose.

Therapeutic uses

Treatment of acute lymphocytic leukemia (ALL), Hodgkin lymphoma, non-Hodgkin lymphomas, Wilms' tumor, neuroblastoma, rhabdomyosarcoma. 

Adverse effects/Side effects

Convulsions, myelosuppression, bronchospasm, hyperuricaemia, azospermia, alopoecia, amenorrhoea, leucopenia, abdominal cramps, urinary dysfunction, vomiting, severe constipation, diarrhoea, paralytic ileus, hypertension, orthostatic hypotension, ptosis, hoarseness, optic neuropathies, hallucinations, blindness, neurological deafness, difficulty in walking, syndrome of inappropriate ADH secretion.

Interaction

  • Increased risk of bronchospasm with mitomycin C.
  • Increased etoposide serum levels with vincristine.
  •  Increased toxicity when ganciclovir given with, immediately before or after vincristine.
  • Reduced vincristine metabolism with miconazole.
  • Increased neurotoxicity with isoniazid, itraconazole, voriconazole, posaconazole and nifedipine.
  • Increased risk of ototoxicity with platinum-containing antineoplastic agents.
  • Decreased immune response when used concurrently with vaccines.
  • Increased myelotoxicity with zidovudine.
  • Increased risk of thromboembolic complications with tamoxifen.
  • Possible risk of earlier onset and/or increased severity of adverse effects with macrolides.
  •  Vincristine levels increase with possible aprepitant.
  • Reduced vincristine clearance and increased toxicity with asparaginase, minimise toxicity by giving vincristine 12-24 hours before L-asparaginase admin.

Contraindications

  • Patients with demyelinating form of Charcot-Marie-Tooth syndrome.
  • Pregnancy and lactation.
  • Intrathecal admin (may be fatal).
  • Patients receiving radiation therapy through ports which include liver.

Storage

Store at 2-8°C. 

Information

Molecular weight

824.9576

Molecular formula

C46H56N4O10

CAS number

57-22-7

Precautions

  • Elderly.
  • Preexisting pulmonary dysfunction or neuromuscular disease; leucopenia or a complicating infection; impaired liver function; obstructive jaundice.
  • CBC to be checked before each dose admin.
  • Discontinue in patients who develop progressive dyspnea.
  • Frequent monitoring of uric acid during first 3-4 weeks of treatment and watch out for uric acid nephropathy.