Vincristine
Vincristine Uses, Dosage, Side Effects, Food Interaction and all others data.
Vincristine arrests cell division at the metaphase stage by inhibiting microtubule formation in the mitotic spindle.
Vincristine is a vinca alkaloid antineoplastic agent used as a treatment for various cancers including breast cancer, Hodgkin's disease, Kaposi's sarcoma, and testicular cancer. The vinca alkaloids are structurally similar compounds comprised of 2 multiringed units, vindoline and catharanthine. 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. Vincristine binds to the microtubular proteins of the mitotic spindle, leading to crystallization of the microtubule and mitotic arrest or cell death. Vincristine has some immunosuppressant effect. The vinca alkaloids are considered to be cell cycle phase-specific.
| Trade Name | Vincristine |
| Availability | Prescription only |
| Generic | Vincristine |
| Vincristine Other Names | 22-Oxovincaleukoblastin, 22-Oxovincaleukoblastine, Leurocristine, Vincristin, Vincristina, Vincristine, Vincristinum |
| Related Drugs | Venclexta, prednisone, methotrexate, Keytruda, rituximab, carboplatin, pembrolizumab, fluorouracil, Rituxan, doxorubicin |
| Type | |
| Formula | C46H56N4O10 |
| Weight | Average: 824.972 Monoisotopic: 824.399644019 |
| Protein binding | ~75% |
| Groups | Approved, Investigational |
| Therapeutic Class | Cytotoxic Chemotherapy |
| Manufacturer | |
| Available Country | Canada, United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Vincristine sulfate injection is used for acute leukemia. Vincristine sulfate injection has also been shown to be useful in combination with other oncolytic agents in Hodgkin's disease, non-Hodgkin's malignant lymphomas (lymphocytic, mixed cell, histiocytic, undifferentiated, nodular and diffuse types), rhabdomyosarcoma, neuroblastoma, and Wilms' tumor.
Vincristine is also used to associated treatment for these conditions: Acute Lymphoblastic Leukaemia Recurrent, Acute Lymphocytic Leukemia (ALL), Choriocarcinoma, Chronic Lymphocytic Leukaemia (CLL), Ewing's Sarcoma, Gestational Trophoblastic Disease, Hepatoblastomas, Immune Thrombocytopenic Purpura ( ITP ), Kaposi’s sarcoma, Lymphoma, Hodgkins, Multiple Myeloma (MM), Neuroblastomas, Non-Hodgkin's Lymphoma (NHL), Ovarian germ cell tumour, Pheochromocytomas, Retinoblastoma, Rhabdomyosarcomas, Small Cell Lung Cancer (SCLC), Wilms' tumor, Advanced Thymoma
How Vincristine works
The antitumor activity of Vincristine is thought to be due primarily to inhibition of mitosis at metaphase through its interaction with tubulin. Like other vinca alkaloids, Vincristine may also interfere with: 1) amino acid, cyclic AMP, and glutathione metabolism, 2) calmodulin-dependent Ca2+-transport ATPase activity, 3) cellular respiration, and 4) nucleic acid and lipid biosynthesis.
Dosage
Vincristine dosage
Adult (Intravenous): Usual recommended dosage: 1.4-1.5 mg/m2 once wkly. Max: 2 mg wkly. Subsequent doses may be modified based on clinical and haematological responses and tolerance of the patient. May be used in combination with other drugs. Prescribers should consult published protocols for the dosage, method and sequence of admin.
Child (Intravenous): Usual recommended dosage: 1.5-2 mg/m2 once wkly; for patients ≤10 kg: Initiate at 0.05 mg/kg once wkly. Subsequent doses may be modified based on clinical and haematological responses and tolerance of the patient. May be used in combination with other drugs. Prescribers should consult published protocols for the dosage, method and sequence of admin.
Side Effects
Dose limiting neurotoxicity (e.g. motor function impairment, gait abnormalities), hyperuricaemia, bronchospasm, azospermia, amenorrhoea, alopoecia, leucopenia, urinary dysfunction, abdominal cramps, vomiting, diarrhoea, severe constipation, paralytic ileus, convulsions, hypertension, orthostatic hypotension, ptosis, hoarseness, optic neuropathies, hallucinations, blindness, neurological deafness, difficulty in walking, syndrome of inappropriate ADH secretion.
Toxicity
IVN-RAT LD50 1300 mg/kg; IPR-MUS LD50 5.2 mg/kg. Marqibo® must only be administered IV because it is fatal if administered by other routes. Marqibo® also has different dosing than vincristine sulphate injection, so attention is needed to prevent overdoses. The most clinically significant adverse effect of vincristine is neurotoxicity.
Precaution
Elderly. Preexisting pulmonary dysfunction or neuromuscular disease; leucopenia or a complicating infection; impaired liver function; obstructive jaundice. Routine prophylactic laxative needed to ensure regular bowel movement. Discontinue immediately if extravasation occurs, and inj any remaining drug into another vein, followed by local Inj of hyaluronidase and topical heat application to the affected area to aid in drug removal and reduce discomfort. Discontinue in patients who develop progressive dyspnea. CBC to be checked before each dose admin. Frequent monitoring of uric acid during first 3-4 wk of treatment and watch out for uric acid nephropathy.
Interaction
Decreased digoxin (tablets) and verapamil absorption with antineoplastic regimens. 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. Decreased immune response when used concurrently with vaccines. Increased myelotoxicity with zidovudine. Increased risk of thromboembolic complications with tamoxifen. Increased risk of ototoxicity with ototoxic drugs (e.g. platinum-containing antineoplastic agents). Possible risk of earlier onset and/or increased severity of adverse effects with macrolides. Possible increase in vincristine levels with aprepitant. Possible decrease in antiepileptic levels with vincristine, monitor serum antiepileptic levels and effectiveness of chemotherapy.
Food Interaction
- Exercise caution with grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of vincristine.
- Exercise caution with St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce serum levels of vincristine.
Vincristine Drug Interaction
Moderate: pegfilgrastimMinor: doxorubicinUnknown: lorazepam, sulfamethoxazole / trimethoprim, diphenhydramine, sulfamethoxazole / trimethoprim, prochlorperazine, cyclophosphamide, meperidine, arginine, levocarnitine, cysteine, lithium, rituximab, acetaminophen, cyanocobalamin, cholecalciferol, phytonadione, menaquinone, ondansetron
Vincristine Disease Interaction
Major: pulmonary dysfunction, neurologic dysfunctionModerate: constipation, hepatic dysfunction, infections, myelosuppression, renal impairment, SIADH
Volume of Distribution
Within 15 to 30 minutes after injection, over 90% of the drug is distributed from the blood into tissue, where it remains tightly, but not irreversibly, bound.
Half Life
When intravenously injected into cancer patients, a triphasic serum decay patten was observed. The initial, middle, and terminal half-lives are 5 minutes, 2.3 hours, 85 hours respectively. The range of the terminal half-life is humans is 19 - 155 hours.
Elimination Route
The liver is the major excretory organ in humans and animals. 80% of an injected dose of vincristine sulfate is excreted via feces. 10 - 20% is excreted via urine.
Pregnancy & Breastfeeding use
Pregnancy Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Contraindication
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.
Special Warning
Hepatic Impairment: Dose adjustment may be needed. Serum bilirubin >3 mg/100ml: Reduce dose by 50%.
Acute Overdose
Symptoms: mainly extensions of its common adverse effects.
Management: Treatment is supportive and includes prevention of side effects from syndrome of inappropriate antidiuretic hormone secretion (SIADH) (e.g. fluid restriction and admin of loop diuretic); admin of anticonvulsants and use of enemas (to prevent ileus). Closely monitor the CV system and determine the blood counts daily to guide transfusion requirements. Folinic acid 100 mg admin IV every 3 hr for 24 hr and then every 6 hr for at least 48 h may be admin. Haemodialysis unlikely to be useful.
Storage Condition
Store at 2-8° C. Protect from light.
Innovators Monograph
You find simplified version here Vincristine
Vincristine contains Vincristine see full prescribing information from innovator Vincristine Monograph, Vincristine MSDS, Vincristine FDA label
FAQ
What Vincristine is used for?
Vincristine is used to treat leukemia, Hodgkin's disease, non-Hodgkin's lymphoma, rhabdomyosarcoma , neuroblastoma (cancer that forms in nerve tissue), and Wilms' tumor.Vincristine is cancer medication that interferes with the growth of cancer cells and slows their spread in the body.
What are the side effects of Vincristine?
Vincristine may cause side effects include:
- nausea.
- vomiting.
- sores in the mouth and throat.
- loss of appetite or weight.
- stomach pain.
- diarrhea.
- headache.
- hair loss.
Can Vincristine cause liver damage?
Vincristine has been suspected to cause liver damage and to enhance radiation-induced hepatic injury.
Is Vincristine safe during pregnancy?
Vincristine can cause birth defects for the baby if you are already pregnant. Both men and women should not plan on conceiving a child while on Vincristine.
Is Vincristine safe during breastfeeding?
Most sources consider breastfeeding to be contraindicated during maternal antineoplastic drug therapy.It is probably impractical to resume breastfeeding after Vincristine therapy because of the drug’s long half-life. Chemotherapy may adversely affect the normal microbiome and chemical makeup of breastmilk.
Does Vincristine make me tired?
Vincristine may make you dizzy or tired or cause numbness in your hands/feet.
What does Vincristine do to the body?
Numbness and tingling in fingers and toes may become progressively worse with repeated doses of Vincristine.
How long is Vincristine good for?
Stable for 7 days under refrigeration, or 2 days at room temperature. In ambulatory pumps, solution is stable for 7 days at room temperature. After preparation, keep Vincristine in a location away from the separate storage location recommended for intrathecal medications.
Can Vincristine cause eye problems?
Vincristine exposure can potentially lead to transient or permanent blindness by mechanisms including cranial neuropathy, optic nerve atrophy and cortical blindness.
Does Vincristine cause my hair loss?
Vincristine often causes a temporary loss of hair. After treatment with Vincristine has ended, or sometimes even during treatment, normal hair growth should return.
Can Vincristine cause hearing loss?
Sudden hearing loss during Vincristine therapy is a very rare event.
Does Vincristine affect the heart?
Vincristine may causes heart problems, rare events associated with Vincristine include lung damage, stroke, and heart attack.
How does Vincristine work in the body?
Vincristine works by stopping the cancer cells from separating into 2 new cells.
How long does Vincristine jaw pain last?
Onset was usually 3 days after Vincristine administration; mean duration was 2 days.
Can Vincristine cause seizures?
No other cause for the seizures was documented.
Can Vincristine cause abdominal pain?
Vincristine can cause serious constipation, abdominal pain and can even lead to a blockage or stoppage of the bowel (called paralytic ileus) if not treated promptly.
How often do you take Vincristine?
Vincristine may be given by a variety of dosing schedules from weekly to bi-weekly to monthly (every 28 days).
How do you administer Vincristine?
Vincristine should not be given intramuscularly, subcutaneously or intrathecally. The solution may be injected either directly into the vein or into the injection site of a running intravenous infusion.
How often is Vincristine given?
Vincristine is usually given once a week.
Can I drive after taking Vincristine?
You should avoid driving after taking Vincristine.Do not drive, use machinery, or do anything that needs alertness until you can do it safely.
