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Vinorelbine

Vinorelbine, sold under the brand name Navelbine among others, is a chemotherapy medication used to treat a number of types of cancer. This includes breast cancer and non-small cell lung cancer. It is given by injection into a vein or by mouth More

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Description

Vinorelbine, sold under the brand name Navelbine among others, is a chemotherapy medication used to treat a number of types of cancer. This includes breast cancer and non-small cell lung cancer. It is given by injection into a vein or by mouth

Generic Name

Vinorelbine

Chemical names

Vinorelbine; Navelbine base; Vinorelbinum [Latin]; Vinorelbina [Spanish]; Navelbine

Brand names

Navelbine, Relbovin, Vinbine, Vinelbine, Vinotec

IUPAC name

methyl (1R,9R,10R,11R,12R,19R)-11-(acetyloxy)-12-ethyl-4-[(12S,14R)-16-ethyl-12-(methoxycarbonyl)-1,10-diazatetracyclo[12.3.1.0³,¹¹.0?,?]octadeca-3(11),4,6,8,15-pentaen-12-yl]-10-hydroxy-5-methoxy-8-methyl-8,16-diazapentac

Pharmacokinetics

NA

Actions

It is one of the types of vinca alkaloid used to treat various types of 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 drug binds to the mitotic spindle of the microtubular proteins, this leads to crystallization of the microtubule and mitotic arrest or cell death. Vinorelbine interferes with calmodulin-dependent Ca2+-transport ATPase activity, amino acid, cyclic AMP, and glutathione metabolism, cellular respiration, and nucleic acid and lipid biosynthesis.

Dosage/Dosage form

For IV use only

Therapeutic uses

For the treatment of non-small-cell lung carcinoma.

Adverse effects/Side effects

Neurotoxicity, peripheral paraesthesia, loss of deep tendon reflexes, abdominal pain, severe constipation, diarrhoea, alopecia, severe local irritation. Dose limiting granulocytopenia, leukopenia and anaemia. Intestinal obstruction, paralytic ileus, nausea, vomitinh, increased in LFT, chest pain, fatigue. Local pain and thrombophlebitis with repeated injection.

Interaction

  • Increased risk of granulocytopenia with cisplatin.
  •  Increased risk of neurotoxicity with paclitaxel, itraconazole, ketoconazole.
  •  Increased radiosensitising effects with prior or concomitant radiation therapy.
  • Increased pulmonary toxicity with mitomycin.
  • Increased myelotoxicity with zidovudine.
  • Earlier onset and/or an increased severity of side effects with CYP3A inhibitors. Possible increase in vincristine levels with aprepitant.
  • Possible infection with live vaccines.

Contraindications

  • Hypersensitivity, thrombocytopenia; neutropenia; severe hepatic impairment.
  •  Intrathecal admin.
  • Pregnancy, lactation.

Storage

Store at 2-8°C.

Information

Molecular weight

778.9323

Molecular formula

C45H54N4O8

CAS number

71486-22-1

Precautions

  • Hepatic impairment.
  • Compromised bone marrow reserve due to prior irradiation or chemotherapy; recovering marrow function from the effects of previous chemotherapy.
  • Complete blood counts with differentials to be monitored prior to administration of subsequent doses.
  • Prior radiation therapy; past history or pre-existing neuropathy.
  • Avoid extravasation.
  • Do not father a child during and up to six months after treatment and females of childbearing potential to use effective method of contraception during treatment and three months thereafter.