Vinblastinesulfaat

Vinblastinesulfaat Uses, Dosage, Side Effects, Food Interaction and all others data.

Vinblastinesulfaat is M phase specific. It binds to microtubular proteins and arrests mitosis at the metaphase by disrupting mitotic spindle formation. It blocks glutamic acid utilization, thus inhibiting purine synthesis, the citric acid cycle, and the formation of urea. It may also interfere with nucleic acid and protein synthesis.

Vinblastinesulfaat is a vinca alkaloid antineoplastic agent. 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. Vinblastinesulfaat has some immunosuppressant effect. The vinca alkaloids are considered to be cell cycle phase-specific.

Trade Name Vinblastinesulfaat
Availability Prescription only
Generic Vinblastine
Vinblastine Other Names Vinblastin, Vinblastina, Vinblastine, Vinblastinum, Vincaleukoblastine
Related Drugs prednisone, methotrexate, dexamethasone, Decadron, Keytruda, Arimidex, carboplatin, pembrolizumab, fluorouracil, doxorubicin
Type
Formula C46H58N4O9
Weight Average: 810.9741
Monoisotopic: 810.420379474
Protein binding

98-99%

Groups Approved
Therapeutic Class Cytotoxic Chemotherapy
Manufacturer
Available Country Netherlands
Last Updated: September 19, 2023 at 7:00 am
Vinblastinesulfaat
Vinblastinesulfaat

Uses

Vinblastinesulfaat is effective as a single agent, but its therapeutic effect is enhanced when used in combination with other antineoplastic drugs. Vinblastinesulfaat has been used in the treatment of Hodgkin’s disease (Stages III and IV) in combination therapy (with adriamycin (doxorubicin), bleomycin and dacarbazine as ABVD) and in the treatment of advanced testicular carcinoma (with cisplatin and bleomycin). Vinblastinesulfaat has been used in the palliative treatment of lymphocytic lymphoma, histiocytic lymphoma, advanced stages of mycosis fungoides, Kaposi's sarcoma and Histiocytosis X.

Vinblastinesulfaat may be used in the treatment of choriocarcinoma resistant to other chemotherapeutic agents; carcinoma of the breast, unresponsive to appropriate endocrine surgery and hormonal therapy. One of the most effective single agents for treatment of Hodgkin’s disease is vinblastine. A protocol substituting cyclophosphamide for nitrogen mustard and vinblastine for vincristine in MOPP is an alternative therapy for previously untreated patients with advanced Hodgkin’s disease. Patients suffering relapse have also responded to combination therapy that included vinblastine. Advanced testicular germ-cell cancers are sensitive to vinblastine alone but the administration of vinblastine concomitantly with other antineoplastic agents, produces better clinical results. Bleomycin effectiveness is enhanced when vinblastine is administered 6 to 8 hours prior to bleomycin administration; this schedule permits more cells to be arrested during metaphase, in which bleomycin is active.

Vinblastinesulfaat is also used to associated treatment for these conditions: Advanced Soft Tissue Sarcoma, Autoimmune Hemolytic Anemia, Cancer, Bladder, Immune Thrombocytopenic Purpura ( ITP ), Kaposi’s sarcoma, Letterer-Siwe disease, Lymphoma, Hodgkins, Metastatic Melanoma, Non-Small Cell Lung Carcinoma (NSCLC), Advanced Alibert-Bazin syndrome, Advanced Testicular cancer, Histiocytic lymphoma, Refractory Breast cancer

How Vinblastinesulfaat works

The antitumor activity of vinblastine is thought to be due primarily to inhibition of mitosis at metaphase through its interaction with tubulin. Vinblastinesulfaat binds to the microtubular proteins of the mitotic spindle, leading to crystallization of the microtubule and mitotic arrest or cell death.

Dosage

Vinblastinesulfaat dosage

Adult (Intravenous): Initially, 3.7 mg/m2, increase dose wkly based on WBC counts in increments of about 1.8 mg/m2 until leukocyte count decreases to about 3000/mm3, or max wkly dose of 18.5 mg/m2 reached. Do not increase dose if leukocyte count is reduced to approximately 3000 cells/mm3; administer the max dose that does not cause leucopenia for maintenance. Do not increase subsequent doses if onolytic activity occurs before leucopenic effect. Usual dose: 5.5-7.4 mg/m2 per wk. Do not admin next dose, even though 7 days have lapsed unless the leukocyte count has returned to at least 4000/mm3.

Child (Intravenous): Initial 2.5 mg/m2 of BSA, increased dose at wkly intervals in increments of about 1.25 mg/m2 until leukocyte count decreases to about 3000/ mm3, or max wkly dose of 12.5 mg/m2 reached. Do not increase dose once leukocyte count reaches approximately 3000 cells/mm3, instead, a dose of 1 increment smaller to be admin at wkly intervals for maintenance i.e. patient receives the max dose that does not cause leucopenia. If onolytic activity is encountered before leucopenic effect, then there is no need to increase subsequent doses. Do not admin next dose, even though 7 days have lapsed unless the leukocyte count has returned to at least 4000/mm3. Duration of maintenance therapy depends on disease state and the antineoplastic agent combination.

Side Effects

Alopecia, constipation, malaise, stomatitis, dose-limiting bone marrow suppression (e.g. granulocytopenia, thrombocytopenia, anaemia), hypertension, central and peripheral neurotoxicity, 8th cranial nerve damage resulting in vestibular and auditory toxicity, ischaemic cardiac toxicity, breathlessness, bone, tumour or jaw pain. Nausea, vomiting, GI bleed, syndrome of inappropriate antidiuretic hormone. Necrosis, cellulitis if extravasation occurs.

Toxicity

Oral, mouse: LD50 = 423 mg/kg; Oral, rat: LD50 = 305 mg/kg.

Precaution

Hepatic impairment; neurotoxicity; ischemic heart disease; preexisting pulmonary dysfunction; extravasation may cause tissue damage and pain. Discontinue immediately if extravasation occurs, with local Inj of hyaluronidase and local heat application to decrease discomfort and risk of cellulitis; remaining Inj to be injected into another vein. Routine prophylaxis against constipation recommended especially in high doses. Nadir in leukocyte count occur 4-10 days after vinblastine admin; recovery observed 7-14 days after treatment.

Interaction

Possible increase in vinblastine levels with aprepitant. Reduced vinblastine metabolism with miconazole. Variable interactions with phenytoin, monitor serum phenytoin levels. Reduced immune response with vaccines. Additive myelotoxicity with zidovudine. Concurrent admin of vinblastine with CYP3A inhibitors may cause an earlier onset and/or an increased severity of side effects.

Food Interaction

  • Avoid grapefruit products. Grapefruit inhibits CYP3A metabolism, which may increase the serum concentration of vinblastine.
  • Exercise caution with St. John's Wort. This herb induces CYP3A metabolism, which may reduce serum levels of vinblastine.

Half Life

Triphasic: 35 min, 53 min, and 19 hours

Elimination Route

The major route of excretion may be through the biliary system.

Pregnancy & Breastfeeding use

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

Severe bone marrow suppression; presence of bacterial infection; maglignant cell infiltration of bone marrow; Inj into extremity with poor circulation; porphyria; granulocytopenia. Elderly with cachexia or extreme skin ulcerations. Pregnancy; lactation. Intrathecal use may result in death.

Special Warning

Hepatic Impairment: Serum bilirubin >3 mg/100ml: Reduce dose by 50%.

Acute Overdose

Symptoms: Severe bone marrow suppression and extensions of its usual side effects.

Management: Treatment is supportive. Restrict fluid and use of loop diuretics to counteract the effects of syndrome of inappropriate secretion of antidiuretic hormone. Monitor the patient's CV system and daily blood counts for transfusion requirement.

Storage Condition

Store at 2-8° C.

Innovators Monograph

You find simplified version here Vinblastinesulfaat

Vinblastinesulfaat contains Vinblastine see full prescribing information from innovator Vinblastinesulfaat Monograph, Vinblastinesulfaat MSDS, Vinblastinesulfaat FDA label

FAQ

What is Vinblastinesulfaat used for?

brans is used to treat Hodgkin's disease, certain types of lymphoma, testicular cancer, breast cancer, choriocarcinoma (a type of uterine cancer), Kaposi's sarcoma, and Letterer-Siwe disease.Vinblastinesulfaat is often used in combination with other cancer drugs.

What does Vinblastinesulfaat do to cancer cells?

Vinblastinesulfaat works by stopping the cancer cells from separating into 2 new cells. So it blocks the growth of the cancer.

What are the side effects of Vinblastinesulfaat?

Vinblastinesulfaat may cause side effects include:

  • constipation
  • nausea
  • vomiting
  • loss of appetite or weight
  • stomach pain
  • diarrhea
  • headache
  • dizziness
  • jaw pain, bone pain, and other aches
  • hair loss

How often is Vinblastinesulfaat given?

It is usually given once a week. The length of treatment depends on the types of drugs you are taking, how well your body responds to them, and the type of cancer you have.

How do you give Vinblastinesulfaat?

Vinblastinesulfaat 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. Injection of Vinblastinesulfaat sulfate may be completed in about one minute.

Is Vinblastinesulfaat safe during pregnancy ?

Vinblastinesulfaat may be used if the potential benefits to the mother outweigh the potential risks to the unborn child.Vinblastinesulfaat may harm your unborn baby.

Is Vinblastinesulfaat safe during breastfeeding?

Most sources consider breastfeeding to be contraindicated during maternal antineoplastic drug therapy.It is probably impractical to resume breastfeeding after Vinblastinesulfaat therapy because of the drug's long half-life.

Does Vinblastinesulfaat cause hair loss?

This medicine often causes a temporary loss of hair. After treatment with Vinblastinesulfaat has ended, or sometimes even during treatment, normal hair growth should return.

What class of drug is Vinblastinesulfaat?

Vinblastinesulfaat is in a class of medications called vinca alkaloids. It works by slowing or stopping the growth of cancer cells in your body.

How do you administer Vinblastinesulfaat?

The solution may be injected either directly into the vein or into the injection site of a running intravenous infusion. Injection of Vinblastinesulfaat sulfate may be completed in about one minute.

Can I take Vinblastinesulfaat for a long time?

This medication should not be mixed in a large amount of solution and/or injected over a long time (such as 30 to 60 minutes) unless directed by your doctor.

What happens to cancer cells when given Vinblastinesulfaat?

Vinblastinesulfaat works by stopping the cancer cells from separating into 2 new cells. So it blocks the growth of the cancer.

Vinblastinesulfaat is safe for liver?

It is generally considered as safe and rarely has been reported to cause acute liver failure.

*** Taking medicines without doctor's advice can cause long-term problems.
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