SYNONYM(S): VBL; Vincaleukoblastine; VLB
COMMON TRADE NAME(S): Velban® (multiple brands available)
The vinca alkaloids have become clinically useful since the discovery of their antitumour properties in 1959. Initially, extracts of the periwinkle plant (Catharanthus roseus) were investigated because of putative hypoglycemic properties, but were noted to cause marrow suppression in rats and antileukemic effects in vitro. Similar to other vinca alkaloids, vinblastine binds to the microtubular proteins of the mitotic spindle, leading to depolymerization of the microtubule and mitotic arrest at metaphase or cell death. Vinblastine has some immunosuppressant effects. The vinca alkaloids are considered to be cell cycle phase-specific (M and S phases).
Rapid and extensive binding to tissues and to formed elements of peripheral blood. Distributes to the liver.
|Cross blood brain barrier?||poorly|
Extensively metabolized in liver via CYP3A subfamilies, including CYP3A4. Inhibits CYP3A4 and 2D6.
Slowly excreted in urine and feces (via bile).
|Urine||< 1% unchanged|
|Half-life||25 hours (terminal)|
- Frequently responsive:
- Hodgkin's disease
- Lymphocytic lymphoma
- Histolytic lymphoma
- Mycosis fungoides
- Testicular cancer
- Kaposi's sarcoma
- Letterer-Siwe disease (histiocytosis-X)
- Less frequently responsive:
- Choriocarcinoma resistant to other chemotherapy
- Breast cancer (unresponsive to endocrine surgery and hormonal therapy)
- Bladder cancer
- Non-small cell lung cancer
- Desmoid tumour
- CNS cancer
Extravasation Potential: Vesicant
|ORGAN SITE||SIDE EFFECT* (%)||ONSET**|
|Auditory||Hearing impaired (rare)||E|
|ECG changes (transient; rare)||E|
|Hypertension (<10%)||I E|
|Gastrointestinal||Abdominal pain (>10%)||E|
|Nausea, vomiting (>10%)||I|
|Pain (tumour pain)||I|
|Myelosuppression ± infection, bleeding (>10%)||E|
|Injection site||Phlebitis||I E|
|Metabolic / Endocrine||Hyperuricemia (during periods of active cell lysis)||I|
|Musculoskeletal||Musculoskeletal pain (<10%, including jaw pain, may be severe)||E|
|Nervous System||Depression (<10%)||E|
|Reproductive and breast disorders||Infertility||L|
|Respiratory||Bronchospasm (or shortness of breath, especially in combination with mitomycin; <10%)||I|
|Vascular||Peripheral ischemia (<10%)||D|
* "Incidence" may refer to an absolute value or the higher value from a reported range.
"Rare" may refer to events with < 1% incidence, reported in post-marketing, phase 1 studies,
isolated data or anecdotal reports.
Dose-limiting side effects are underlined.
** I = immediate (onset in hours to days) E = early (days to weeks)
D = delayed (weeks to months) L = late (months to years)
Myelosuppression and neurotoxicity are the main dose-limiting effects of vinblastine.
Hyperuricemia during periods of active cell lysis, which is caused by cytotoxic chemotherapy of highly proliferative tumours of massive burden (e.g. some leukemias and lymphomas), can be minimized with allopurinol and hydration. In hospitalized patients the urine may be alkalinized, by addition of sodium bicarbonate to the IV fluids, if tumour lysis is expected.
Neurotoxicity with the vinca alkaloids is qualitatively similar but quantitatively different (vincristine> vinblastine>vinorelbine). Symptoms tend to be worse with prolonged exposure. Neurotoxicity may be manifested as numbness, paresthesia, mental depression, loss of deep tendon reflex, headache, malaise, dizziness, seizures or psychosis. Cranial nerve neuropathy may lead to vocal cord paresis or paralysis, oculomotor nerve dysfunction and bilateral facial nerve palsies.
Cranial nerve toxicities tend to be bilateral and reversible when treatment with vinblastine is discontinued.
Severe jaw pain or parotid gland pain can occur within a few hours of the first dose of vinblastine. This is not an indication to stop or modify the dose; treat with analgesics. Autonomic neuropathy is manifested as constipation, abdominal pain, urinary retention and paralytic ileus. These gastrointestinal symptoms are seen especially when high doses are used (e.g. >20 mg) and are rare with doses <10 mg.
Toxicity and hematologic toxicity may be more severe in patients with severe cachexia, skin ulcers or marrow infiltration.
Refer to protocol by which patient is being treated. Numerous dosing schedules exist and depend on disease, response and concomitant therapy. Guidelines for dosing also include consideration of white blood cell count. Dosage may be reduced and/or delayed in patients with bone marrow depression due to cytotoxic/radiation therapy. Do not re-treat with vinblastine until marrow recovery has occurred.
(range 3.7-18.5 mg/m2; usual weekly dose: 5.5 – 7.4 mg/m2; maximum weekly dose: 18.5 mg/m2)
Dosage with toxicity:
- Modify according to protocol by which patient is being treated; if no guidelines available, refer to Appendix 6 "Dosage Modification for Hematologic and Non-Hematologic Toxicities."
Worst Toxicity / Counts in Previous Cycle (x 109/L)
Dose (% previous dose)*
Febrile neutropenia, grade 4 ANC for ≥ 5-7 days or thrombocytopenic bleeding
Grade 3 related organ / non-hematologic
Hold, then 75%*
Grade 4 related organ / non-hematologic
*Do not retreat until ANC ≥ 1-1.5 x 109L, platelets ≥ 100 x 109L and toxicity ≤ grade 2
|Bilirubin||% Usual dose|
|1 - 2.5 x ULN||50%|
|> 2.5 x ULN||25%|
Refer to protocol being used.
FOR INTRAVENOUS USE ONLY.
Intrathecal administration of other vinca alkaloids has resulted in death. Syringes containing this product should be labelled
“WARNING – FOR INTRAVENOUS USE ONLY. FATAL if given intrathecally.”
- Quick push through sidearm of free flowing IV (5% Dextrose or Normal Saline); Inject over 1 minute. Do not admix with solutions that can change pH (e.g. lactate containing solutions).
- May mix in 50 mL minibag (NS or D5W); infusions over ≥30-60 minutes are not recommended.
- If any signs or symptoms of extravasation occur, the injection or infusion should be immediately terminated and restarted in another vein. Any known or suspected extravasation should be managed promptly.
Vinblastine is contraindicated in patients who have hypersensitivity to vinblastine or its formulation and in patients with severe myelosuppression or infection. Intrathecal vinblastine administration is absolutely contraindicated.
Myelosuppressive effects are more marked in patients with bone marrow infiltration and in elderly/cachectic patients. Use with caution in patients with ischemic heart disease and in combination with neurotoxic drugs. Do not give vinblastine more frequently than once every 7 days.
Standard doses of vinblastine given for prolonged periods (e.g. daily for 7 days) may result in permanent or fatal neurologic toxicity and should not be used.
Vinblastine is teratogenic, embryotoxic, potentially mutagenic and carcinogenic; therefore, it is contraindicated in pregnancy. Adequate contraception should be used by both sexes during vinblastine treatment and for at least 6 months after the last dose. Vinblastine affects fertility in humans, which may be reversible in some cases. Breast feeding is not recommended due to the potential secretion into breast milk.
|Mitomycin||Acute bronchospasm has occurred minutes to hours after administration. Reaction may occur up to 2 weeks after mitomycin.||Unknown||Caution|
|Phenytoin||↓ serum concentration of phenytoin||Possibly ↓ absorption or increased metabolism of phenytoin||Monitor serum levels of phenytoin and adjust dose prn|
|CYP3A4 inhibitors (i.e. ketoconazole, voriconazole, clarithromycin, ritonavir, fruit or juice from grapefruit, Seville oranges, starfruit or pomegranate )||↑ risk of neurotoxicity||inhibits CYP3A4 and interferes with metabolism of vinblastine||Avoid concomitant use|
|CYP3A4 substrates (i.e., aprepitant, tolterodine)||↑ toxicity||↓ metabolism (vinblastine a a potent CYP3A4 inhibitor)||Avoid if possible. If must use, monitor or adjust dose.|
|CYP3A4 inducers (i.e. phenytoin, rifampin, dexamethasone, carbamazepine, phenobarbital, St. John’s Wort, etc)||↓ vinblastine effect||↑ metabolism (CYP3A4)||Caution|
|Bleomycin +/- cisplatin||Raynaud's phenomenon, MI, CVA reported||Unknown||Caution|
|Ototoxic drugs (i.e., cisplatin, aminoglycosides)||↑ ototoxicity (reported with other vinca alkaloids)||Additive||Caution|
Treating physicians may decide to monitor more or less frequently for individual patients but should always consider recommendations from the product monograph.
|Monitor Type||Monitor Frequency|
|CBC||Baseline and regular|
|Liver function tests||Baseline and regular|
Clinical assessment for neurotoxicity, infection, bleeding, local toxicity.
|At each visit|
Grade toxicity using the current NCI-CTCAE (Common Terminology Criteria for Adverse Events) version
CPhA Monograph: Vinblastine. Compendium of Pharmaceuticals and Specialties, March 2009.
Johnson IS, Armstrong JG, Gorman M, et al. The vinca alkaloids: a new class of oncolytic agents. Cancer Research 1963;23:1390-427.
McEvoy GK, editor. AHFS Drug Information 2011. Bethesda: American Society of Health-System Pharmacists, p. 1263-5.
Prescribing information: Vinblastine. Bedford Laboratories (US)., December 2001.
Product Monograph: Vinblastine. Hospira Corporation, June 18, 2007.
Scripture CD, Figg WD. Drug interactions in cancer therapy. Nature Reviews Cancer 2006;6:546-58.
Vinblastine: BC Cancer Agency Cancer Drug Manual. March 2008.
Zidan J, Robenstein W, Abzah A, et al. Treatment of Kaposi's Sarcoma with Vinblastine in Patients with Disseminated Dermal Disease. IMAJ 2001;3:251-3.
October 2017 edited indications
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