Vinorelbine

Vinorelbine (Vinorelbine) is an antitumor drug from the class of antimetabolites that is often used in chemotherapy to treat a variety of cancers, including breast cancer and lung cancer.

Vinorelbine works by inhibiting the division of cancer cells, which helps stop tumor growth. It is usually given intravenously and can be used in different treatment regimens depending on the type of cancer and the stage of the disease.

Like any other anticancer drug, the drug can cause a variety of side effects, including nausea, vomiting, decreased blood cell counts, fatigue, and an increased risk of infections.

Treatment with vinorelbine is usually prescribed by a physician according to an individualized course of the disease and requires careful monitoring of the patient throughout treatment.

Indications Vinorelbina

Vinorelbine, as an antitumor drug, is used to treat various types of cancer. Its indications for use may include, but are not limited to, the following:

1. Breast Cancer: May be used as monotherapy or in combination with other anticancer drugs for the treatment of breast cancer in both first and subsequent lines of therapy.
2. Lung cancer: May be used as monotherapy or in combination with other drugs for the treatment of lung cancer, especially in cases of advanced or metastatic cancer, when systemic chemotherapy is required.
3. Ovarian Cancer: May be part of comprehensive chemotherapy for the treatment of ovarian cancer, especially in combination with other chemotherapy drugs.
4. Cervical Cancer: In some cases, vinorelbine may be used in the treatment of cervical cancer as part of combination therapy.

Release form

1. Solution for injection: This is the most common form of vinorelbine. The solution for injection is intended for intravenous or intraoral administration and is supplied in ampoules or vials.
2. Capsules: Some manufacturers may offer the drug in capsule form for oral administration. This form may be convenient for patients who prefer oral medication.
3. Lyophilizate for preparation of solution: In some cases, vinorelbine may be supplied as a powder in ampoules or vials. This powder is for preparing a solution before administration.
4. Other forms: In some countries or individual clinics, vinorelbine may also be available in other forms, such as tablets or inhaled form, but these are less common options.

Pharmacodynamics

Vinorelbine (also known as vincristine) is an anti-cancer drug that acts as an antimitotic agent. Its mechanism of action is based on its interaction with microtubules, structural components of cells that play an important role in the process of cell division.

Vinorelbine binds to microtubule beta-tubulin, inhibiting its polymerization into microtubules, which leads to impaired function of the mitotic apparatus of the cell. This ultimately leads to impaired cell division, blocks mitosis metaphase and induces apoptosis (programmed cell death).

Thus, vinorelbine affects rapidly dividing cells, including cancer cells, making it effective in chemotherapy for various types of cancer. However, it is also worth noting that because of its effect on rapidly dividing cells, normal cells may also be affected, causing side effects associated with its use.

Pharmacokinetics

Here are the main aspects of the pharmacokinetics of vinorelbine:

1. Absorption: Vinorelbine is usually injected into the body intravenously. It is rapidly absorbed into the bloodstream after injection.
2. Distribution: Vinorelbine has a large volume of distribution, which means that it is rapidly distributed in body tissues. It penetrates the blood-brain barrier and may accumulate in some organs.
3. Metabolism: Vinorelbine is metabolized in the liver with formation of inactive metabolites. Mainly, vinorelbine metabolism occurs via oxidation and dehydroepoxidation.
4. Excretion: Final excretion of vinorelbine from the body occurs mainly through bile. Part of the drug is also excreted with urine.
5. Half-life: The half-life of vinorelbine from the blood is approximately 24 to 90 hours, depending on the dose and regimen.
6. Dosekinetics: The dose kinetics of vinorelbine may be linear or non-linear, depending on the dose and dosage regimen. A change in dose may or may not proportionally change the blood concentration of the drug.

Dosing and administration

The method of use and dosage of vinorelbine may vary depending on the type of cancer, stage of the disease, general condition of the patient and other factors. Usually, vinorelbine doses are set by an oncologist or other chemotherapy specialist and should be strictly followed.

Examples of standard vinorelbine dosing regimens may include the following:

1. Lung cancer:

   • It can be used in monotherapy or in combination with other anticancer drugs.
   • Typical adult dose: 25-30 mg/m² body surface area, usually once a week.

2. Breast cancer:

   • It may be used in combination with other drugs such as cyclophosphamide or doxorubicin.
   • Typical adult dose: 25-30 mg/m² body surface area, usually once a week.

3. Stomach cancer:

   • It can be used in monotherapy or in combination with other chemotherapeutic agents such as 5-fluorouracil.
   • Typical adult dose: 25-30 mg/m² body surface area, usually once a week.

4. Non-Hodgkin's lymphomas:

   • Can be used in combination with other anticancer drugs.
   • Typical adult dose: 25-30 mg/m² body surface area, usually once a week.

The dosage and schedule of vinorelbine may be adjusted according to treatment response and toxicity.

Use Vinorelbina during pregnancy

The use of vinorelbine during pregnancy is generally not recommended because of potential risks to the fetus. Antineoplastic drugs such as vinorelbine may have teratogenic effects, that is, the ability to cause congenital abnormalities in the fetus, especially in the first trimester of pregnancy when the baby's organs are forming.

Doctors usually try to avoid using chemotherapy during pregnancy if possible. However, in some cases, when the risk to the mother from nonproliferation of cancer is too great and the benefits of treatment outweigh the potential risks to the fetus, doctors may consider using anticancer drugs, including vinorelbine, during pregnancy.

If a woman is diagnosed with cancer during pregnancy, or if she requires chemotherapy following a diagnosis of cancer during pregnancy, it is important to carefully discuss all possible risks and benefits of treatment with her doctor. In such cases, treatment decisions should be made on an individual basis, taking into account the specific circumstances and the nature of the disease. It is also important to consider the woman's own wishes and preferences.

Contraindications

1. Allergic reaction: People with a known allergy to vinorelbine or other vincalkaloids should avoid its use.
2. Pregnancy and breastfeeding: Vinorelbine may be harmful to the fetus during pregnancy and may pass into breast milk, therefore its use should be discussed with a doctor in these cases.
3. Reduced medullary function: Patients with existing reduced medullary function, caused for example by previous chemotherapy or radiotherapy, may have an increased risk of developing toxic effects from vinorelbine.
4. Severe hepatic impairment: Vinorelbine is metabolized in the liver, therefore patients with severe hepatic impairment should avoid its use or use with caution under strict medical supervision.
5. Neuropathy: In patients with preexisting neurologic disorders or neuropathy, use of vinorelbine may worsen symptoms or cause additional neurologic complications.
6. Cardiovascular disease: Patients with serious cardiovascular disease may have an increased risk of cardiac complications from vinorelbine, so use should be with caution.
7. Paralytic intestinal obstruction: The drug may aggravate symptoms of intestinal obstruction, therefore in its presence the use of vinorelbine may be undesirable.

Side effects Vinorelbina

Vinorelbine, like any chemotherapy drug, can cause a number of side effects. Here are some of them:

1. Hematologic side effects: Vinorelbine may cause a decrease in the number of blood-forming cells such as white blood cells, red blood cells, and platelets. This may increase the risk of infections, anemia, and bleeding.
2. Liver Toxicity: Patients receiving vinorelbine may develop elevated levels of liver enzymes in the blood, indicating liver damage.
3. Neuropathy: Vinorelbine may cause neuropathy manifested as numbness, tingling, or pain in the extremities.
4. Nausea and Vomiting: These side effects may also occur in patients taking Vinorelbine.
5. Alopecia: Vinorelbine may cause hair loss.
6. Skin reactions: Include rashes, itching, and other skin problems.
7. Asthenia and weakness: Patients may experience weakness and fatigue.
8. Bone pain: Some patients may experience bone pain during treatment with vinorelbine.
9. Hypersensitivity to sunlight: Patients should avoid prolonged exposure to sunlight during treatment with vinorelbine, as it may cause sunburn.
10. Other side effects: Include diarrhea, changes in taste, appetite disturbances, and others.

These side effects can be moderate to severe and may vary depending on the dose, treatment regimen, and individual patient characteristics.

Overdose

An overdose of vinorelbine can lead to serious consequences, including increased toxic effects of the drug. As with any anticancer drug, it is important to strictly follow the doctor's recommendations on dosage and schedule of administration.

Symptoms of a vinorelbine overdose may include:

1. Severe nausea and vomiting.
2. Increased blood toxicity such as decreased white blood cell counts (leukopenia), platelet counts (thrombocytopenia), and red blood cell counts (anemia).
3. Neuropathy (damage to peripheral nerves) manifested by numbness, weakness, or pain in the extremities.
4. Fever and general weakness.

In case of suspected vinorelbine overdose, it is necessary to seek immediate medical attention. Treatment of overdose may include symptomatic therapy to relieve toxic effects, maintenance of functions of organs and systems of the body, as well as recovery measures depending on the specific situation.

Interactions with other drugs

Vinorelbine (Vinorelbine) may interact with other drugs, which may affect its effectiveness, safety, or cause unwanted side effects. Here are some of the known interactions:

1. Myelosuppressive drugs: Drugs that also decrease bone marrow activity, such as other chemotherapy drugs (e.g., cytotoxic antibiotics) or drugs used in the treatment of rheumatoid arthritis (e.g., methotrexate), may increase the myelosuppressive effects of vinorelbine.
2. Neuropathy-inducing drugs: Drug s that may cause neuropathy or increase its symptoms, such as thioridazine or nitrates, may increase the neurotoxicity of vinorelbine.
3. Drugscausing cardiotoxicity: Drugs that may cause cardiotoxicity or alter cardiac conduction, such as antiarrhythmic drugs or beta-adrenoblockers, may increase the cardiotoxicity of vinorelbine.
4. Drugsaffecting hepatic activity: Drugs that may affect hepatic activity or metabolism of vinorelbine via cytochrome P450 enzymes (e.g., ketoconazole, clarithromycin) may alter its blood levels and affect its efficacy and safety.
5. Drugsaffecting bleeding: Drugs such as aspirin, nonsteroidal anti-inflammatory drugs (NSAIDs), or anticoagulants may increase the risk of bleeding when used concomitantly with vinorelbine.
6. Drugs thatcause intestinal obstruction: Drugs that may increase symptoms of intestinal obstruction, such as opioid analgesics or antispasmodics, may increase symptoms associated with vinorelbine.

Storage conditions

Storage conditions are important to maintain the drug's effectiveness and safety. Here are general recommendations for storage conditions for vinorelbine:

1. Storage temperature: Vinorelbine should normally be stored between 2°C and 8°C. This usually means that it should be stored in a refrigerator.
2. Protection from light: The drug should be stored in the original package or in a dark container to protect it from light, which may affect its stability.
3. Packaging: Before using vinorelbine, the packaging should be checked for integrity. If the packaging is damaged or broken, the drug may not be suitable for use.
4. Avoid freezing: Vinorelbine should be protected from freezing. The drug should be allowed to warm to room temperature before use if it has been stored in the refrigerator.
5. Children and pets: Keep vinorelbine out of the reach of children and pets.
6. Shelf life: It is important to observe the expiration date indicated on the package. Do not use vinorelbine after the expiration date.
7. Special instructions: Some manufacturers may provide additional special storage instructions, so it is important to read them before storing the medication.