Vinblastine
Drug Related WarningVinblastine
- The medication must be taken under the supervision of a medical professional proficient in cancer chemotherapy and in a setting that can detect and manage side effects.
- Before administering this product, the needle must be inserted correctly into the vein.
- When administering an IV, leakage to nearby tissue may irritate the area significantly. Stop the injection immediately, then administer the remaining dose into a different vein. Hyaluronidase can be locally injected to help spread the medication, and moderate heat applied to the leaky area can help reduce discomfort and cellulitis risk.
- Using intrathecal can be made fatal.
Medicine Type :
Allopathy
Allopathy
Prescription Type:
Prescription Required
Prescription Required
Approval :
DCGI (Drugs Controller General of India)
DCGI (Drugs Controller General of India)
Schedule
Schedule H
Schedule H
Pharmacological Class:
Vinca Alkaloids, Therapy Class:
Antineoplastic agent, Approved Countries
India, the United States, Canada, European countries (such as the UK, Germany, France, etc.) and Australia.
Vinblastine is an antineoplastic agent belonging to the pharmacological class of vinca alkaloids.
Vinblastine is FDA-approved to treat various cancers, including Hodgkin's disease, non-Hodgkin lymphoma, testicular cancer, breast cancer, and lung cancer.
Vinblastine, administered intravenously, swiftly enters the bloodstream, distributing widely but not crossing the blood-brain barrier. Primarily metabolized in the liver, it is mainly eliminated through bile and faeces, with minimal unchanged excretion in urine.
The most common side effects of Vinblastine are nausea, vomiting, diarrhea, and decreased appetite.
Vinblastine is available as an injectable solution and powder for injection.
The molecule is available in India, the United States, Canada, European countries (such as the UK, Germany, France, etc.) and Australia.
Vinblastine is an antineoplastic agent belonging to the pharmacological class of vinca alkaloids.
Although its specific mode of action is unknown, it attaches to microtubular proteins. It prevents the mitotic spindle's microtubule formation, which stops dividing cells at the metaphase stage, specifically the M phase. Moreover, it disrupts the metabolism of amino acids by obstructing the cell's ability to use glutamic acid, which inhibits the production of urea, citric acid cycle, and purine synthesis.
Vinblastine exhibits a triphasic half-life of 4 minutes, 1.4 hours, and 24.8 hours. At its peak plasma concentration, it reaches 150 ng/mL, indicative of its varying elimination rates and distribution within the body.
Injectable solutions: To be administered parenterally, as applicable.
As the physician recommends, take the medication with or without food. Dosage and frequency depend on the specific medical condition.
As a palliative measure, vinblastine sulfate has been approved for:
- Cancer of the breast for which alternative therapies have not improved. Adults use it.
- Gestational trophoblastic disease type choriocarcinoma, which has not improved with previous chemotherapy. Adults use it.
- Lymphoma Hodgkin. It is applied to children and adults with severe illnesses.
- Sarcoma Kaposi. Adults use it.
- Mycosis fungoides a form of T-cell lymphoma in the skin. Adults use it.
- Adult cases of non-Hodgkin lymphoma (NHL).
- Germ cell tumours in the testicles. It is applied to children and adults with severe illnesses.
- Non-Hodgkin lymphoma (NHL): Vinblastine Injection inhibits cancer progression by impeding the growth of white blood cell cancers like non-Hodgkin's lymphoma, including mantle-cell lymphoma. It interferes with cancer expansion by blocking essential chemicals aiding growth and spread. To minimize infection risks, avoid crowded places and maintain frequent hand hygiene. Unless advised otherwise by a doctor, staying hydrated is recommended to support health while undergoing this treatment.
- Breast cancer: Vinblastine Injection effectively treats breast cancer, either alone or alongside other therapies like chemotherapy. It alleviates associated symptoms such as breast lumps, nipple discharge, or alterations in breast texture. By stopping cancer cell growth and multiplication, it actively eradicates or suppresses the progression of cancer cells, offering a comprehensive approach to managing and combating breast cancer.
- Kidney cancer: Utilized for kidney cancer, Vinblastine Injection targets associated symptoms like blood in urine, unexplained back pain, weight loss, fatigue, and loss of appetite. By halting cancer growth and impeding cell multiplication, it actively prevents the progression of cancer cells, curbing their spread to unaffected areas and offering a crucial intervention against the advancement of kidney cancer.
- Hodgkin’s disease: Vinblastine Injection combats Hodgkin’s disease, a form of lymphoma originating in the lymphatic system, a vital component of the immune system. It acts by eliminating or arresting the growth of cancer cells and inhibiting their multiplication. By actively impeding cancer cell proliferation, it plays a pivotal role in suppressing the progression of Hodgkin’s disease, supporting the body’s defence mechanisms, and aiding in the removal of waste while enhancing its ability to combat infections.
Vinblastine works well when taken alone, but it has a more significant therapeutic impact when combined with other antitumor medications.
- Hodgkin's disease (Stages III and IV) has been treated with Vinblastine in the treatment of advanced testicular carcinoma (using cisplatin and bleomycin) and in combination therapy [using adriamycin (doxorubicin), bleomycin, and dacarbazine as ABVD].
- Vinblastine has been indicated in the palliative management of Histiocytosis X, Kaposi's sarcoma, advanced stages of Mycosis Fungoides, and lymphocytic lymphoma.
- Vinblastine can be used to treat breast carcinoma that is not responding to appropriate hormone therapy or endocrine surgery, as well as choriocarcinoma that is resistant to other chemotherapy agents.
Parenterally: Vinblastine must be prepared appropriately in an infusion bag and diluted in 25–50 mL of NS, D5W, or LR solutions; do not use more than 100 mL of solution. It is necessary to carefully place the IV needle or catheter for only IVPB administration to prevent fatal complications. It is recommended to complete the infusion in less than a minute to avoid irritating the veins and possible tissue damage. It is essential to act quickly once extravasation occurs, stop the injection, aspirate any excess material, and elevate the affected area four times a day for 15-20 minutes using warm packs to reduce the risk of tissue sloughing. Close monitoring is necessary during the infusion to control any side effects and ensure the safe and efficient administration of Vinblastine.
The dosage and duration of treatment should be as per the treating physician's clinical judgment.
Injectable solutions: 1mg/mL
Powder for injections: 10mg
Vinblastine is available in the form of Injectable solutions and powder for injections.
Dose Adjustment in Adult Patients:
Cancers: Histiocytic lymphoma, mycosis fungoides, squamous cell carcinoma of the head and neck, Hodgkin's disease, and Kaposi's sarcoma; Letterer-Siwe disease (histiocytosis X)
Standard Dosing Ranges
IV every 7–10 days at 3.7–18 mg/m³/day
IV first dose: 3.7 mg/m²/day
boosted by 1.85 mg/m² every week until the WBC reached 3000/mm³.
Range of dosage: 5.5-7.4 mg/m²
Not more than 18.5 mg/m^
Hodgkin's illness
As part of a combination treatment, 6 mg/m² every two weeks
Cancer of the Testicles
6 mg/m³/day x 2 days every 3–4 weeks; a component of combination therapy
Cancer of the Bladder
3 mg/m² q7d x 3 weeks; as a component of a combination therapy
Off-label melanoma
Days 1-4 and 22–25 of the 6-week cycle: 2 mg/m²
Lung Cancer, Nonsmall (Off-label)
Day 1, 8, 15, 22, 29, and day 4 mg/m²/day; as part of a combination treatment
Off-label Use of Ovarian Cancer
As part of a combination treatment, 0.11 mg/kg/day for two days per week
(Off-label) Prostate Cancer
8-week cycle x 6 weeks = 4 mg/m²/week
Individuals with chronic illnesses, including cancer, should consume diets rich in protein, healthy fats, whole grains, and essential vitamins and minerals. Opt for plant-based proteins like nuts, seeds, beans, and legumes during chemotherapy or cancer treatments, as they offer high concentrations of vital nutrients. Maintain a healthy weight through regular exercise and a balanced diet that includes leafy vegetables, citrus fruits, fatty fish, berries, yoghurt, apples, peaches, cauliflower, cabbage, broccoli, beans, and herbs. Prioritize adequate sleep, avoid smoking and alcohol, and steer clear of fast, fried, processed meats, refined carbs, and added sugars.
The dietary restriction should be individualized as per patient requirements.
- Hypersensitivity: Anyone who has previously experienced hypersensitivity to Vinblastine or any of the other components of Vinblastine.
- Active bacterial infection
- Myelosuppression
- Intrathecal administration of Vinblastine.
Bone marrow depression, neuropathy, and neuromuscular disease represent potential adverse effects linked to this medication. Administer neurotoxic and ototoxic agents concurrently with caution. Exercise caution in patients with pulmonary disease, liver impairment, intestinal obstruction, or paralytic ileus. This drug may lead to jaw or parotid pain, hoarseness, and dysphagia due to cranial neuropathy. It's important to note its vesicant nature. Patients who underwent previous radiation treatment or chemotherapy should be closely monitored. It's advisable to avoid pregnancy during treatment due to potential risks. Careful consideration and close monitoring are necessary when using this medication in patients with the conditions above or those previously treated with specific therapies, ensuring the timely identification and management of any adverse reactions.
Alcohol Warning
It is unsafe to consume Vinblastine with alcohol.
Breast Feeding Warning
It is not recommended for use during breastfeeding.
Pregnancy Warning
It is not recommended for use during pregnancy.
Food Warning
Consume an antioxidant-rich diet, and avoid smoking/alcohol.
The adverse reactions related to Vinblastine can be categorized as
•Common Adverse Effects: Bone marrow suppression leads to decreased blood cell counts, nausea, vomiting, and hair loss.
•Less Common Adverse Effects: Neurotoxicity, causing peripheral neuropathy, constipation, mouth sores, weakness, or allergic responses.
•Rare Adverse Effects: Severe allergic reactions, organ-specific issues like liver or kidney toxicity, and skin reactions like rashes might occur.
The clinically relevant drug interactions of Vinblastine are briefly summarized here.
- Drug Interactions: Vinblastine may interact with vaccines (e.g., BCG, Mumps, and Influenza vaccines), cancer medications (e.g., Adalimumab), medications for schizophrenia (e.g., Clozapine), medications for treating moderate to severe plaque psoriasis (e.g., Deucravacitinib), medicines for treating Multiple Sclerosis (e.g., Cladribine), medications for managing and treating autoimmune conditions (e.g., Etanercept), immunomodulating drugs (e.g., Fingolimod), and antirheumatic drugs (e.g., Leflunomide).
- Drug-Food Interactions: Avoid intake of alcoholic drinks.
- Drug-Disease Interactions: Myelosuppression (the insufficient production of blood cells or platelets by the bone marrow), infections, pulmonary impairment, and hepatic dysfunction are diseases that Vinblastine may interact with.
The common side effects of Vinblastine include:
- Injection site reactions
- A drop in the number of blood cells and platelets
- Vomiting
- Decreased appetite
- constipation
- diarrhoea
- abdominal pain
- Feeling sick (nausea)
- Being sick (vomiting)
- Mouth ulcers
- Hair loss
- Pregnancy
Pregnancy Category D (FDA): Use in cases where no safer medication is available and life is in danger. Positive evidence of prenatal risk in humans.
When administering any oncolytic medication during pregnancy, caution must be used. Very little is known about the use of vinblastine sulfate during human pregnancy. Teratogenic effects are possible, according to animal studies, using vinblastine sulfate. When given to a pregnant woman, vinblastine sulfate can harm the fetus. When this drug is administered early in pregnancy, laboratory animals experience conceptus resorption; the surviving fetuses show severe malformations. Pregnant women have not been the subject of sufficient, carefully monitored studies. Patients who take this medication while pregnant or who become pregnant while taking it should be informed of the possible risks to the developing fetus. It is essential to advise potentially fertile women to refrain from getting pregnant.
There are reports of Aspermia in humans. Studies on animals reveal degenerative changes in germ cells and metaphase arrest.
The higher recommended doses of leukopenia (granulocytopenia) may cause dangerously low levels of the condition. It is crucial to adhere to the suggested dosage method for this reason. Even though they are uncommon and transient, stomatitis and neurologic toxicity can be incapacitating.
• Nursing Mothers
Very little information is available regarding the excretion of antineoplastic agents in breast milk. If vinblastine sulfate is eliminated from human milk, it is a matter of uncertainty.
It is not advised to breastfeed an infant while receiving Vinblastine due to potential risks. One should consider the importance of the drug to the mother when deciding whether to stop nursing or the drug altogether due to the possibility of severe adverse reactions in nursing infants.
• Pediatric Use
Established the safety and efficacy of Vinblastine in pediatric use to treat specific cancers. Adhering to pediatric protocols ensures its safety and effectiveness, requiring proper dosage adjustments and vigilant monitoring for conditions like lymphomas or certain childhood cancers.
Dose adjustment in pediatric patients:
Cancers include histiocytic lymphoma, mycosis fungicides, Kaposi's sarcoma, squamous cell carcinoma of the head and neck, testicular cancer, and Letterer-Siwe disease (histiocytosis X).
Standard dosage ranges
Every 7–10 days, 2.5–12.5 mg/m² IV over 1 minute
first dosage 2.5 mg/m³ IV
A rise of 1.25 mg/m^qWeek to reach 3000/mm^ WBC
A maximum of 12.5 mg/m²
Hodgkin's illness
IV: 6 mg/m²/day q 1-2 week x 3–4 week
No more than 12.5 mg/m² per week
Hemotoxiocytosis IV: 0.4 mg/kg every 7–10 days
IV 3 mg/m² for germ cell tumours, not to exceed qweekly
• Geriatric use
The safety and effectiveness of Vinblastine in elderly individuals require cautious monitoring due to age-related changes. Careful dosage adjustments and assessments mitigate risks, ensuring its suitability for treating specific cancers in older individuals, though individual considerations remain crucial.
Dose Adjustment in Renal Impairment Patients:
Renal impairment: No need to adjust dosage
Dose Adjustment in Hepatic Impairment Patients:
Hepatic impairment: AST 60-180 units or bilirubin 1.5-3 mg/dL: 50% of the usual dosage should be administered.
Administer 25% of the usual dosage if the bilirubin level is 3-5 mg/dL.
It is not suggested if the AST is more significant than 180 units or if the bilirubin is greater than 5 mg/dL.
The physician should be vigilant about the knowledge pertaining to identifying and treating overdosage of Vinblastine.
Signs and Symptoms
Granulocytopoeisis, including signs of myelosuppression, may be life-threatening. In addition, neurotoxicity may be observed.
Management
There is no specific antidote; Supportive and symptomatic treatment is essential. Gastrointestinal decontamination methods like gastric lavage or activated charcoal administration might be considered if ingestion occurs recently. In case of an overdose, promptly discontinue Vinblastine, provide appropriate supportive care, and closely monitor the patient's vital signs.
In severe cases where myelosuppression or neurotoxicity occurs, appropriate interventions such as blood transfusions or G-CSF (granulocyte colony-stimulating factor) administration for myelosuppression or supportive care for neurotoxicity may be necessary.
Continuous observation and appropriate, timely medical interventions to address specific symptoms or complications are recommended.
Pharmacodynamics:
The vinca alkaloids comprise two multi-ringed units, vindoline and catharanthine, with similar structural makeup. The vinca alkaloids were found to have antitumor properties in 1959, which led to their clinical utility. Initially studied for their possible hypoglycemic effects, periwinkle plant (Catharanthus roseus) extracts were found to suppress marrow in rats and have antileukemic effects in vitro. There is some immunosuppressive effect of Vinblastine. It is considered that the vinca alkaloids are phase-specific to the cell cycle.
Pharmacokinetics:
- Absorption: Vinblastine is typically administered intravenously and enters the bloodstream directly.
- Distribution: Vinblastine distributes across body tissues and notably accumulates in blood platelets.
- Metabolism: CYP3A isoenzymes extensively metabolize it within the liver into desacetylvinblastine, a more potent form by weight than the original drug.
- Excretion: It occurs predominantly through faeces (10%) and, to a lesser extent, urine (14%).
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Published on: 2 Jan 2024 5:29 PM GMT