Vinorelbine (vinca alkaloid produced by semi-synthetic) -. Vinca alkaloids antitumor agent of the group
violate tubulin polymerization during cell mitosis. Blocks mitosis in phase G2 + M and causes destruction of cells in interphase or at the following mitosis. It acts primarily on mitotic microtubules; with high doses may affect the axonal microtubules. The define equipoise effect of helix tubulin caused by vinorelbine, is less pronounced than that of vincristine.
Pharmacokinetics . After intravenous administration of the drug can be traced three-phase kinetics. The average half-life in the terminal phase is 40 (27,7-43,6) hours.
The connection to plasma proteins is 79,6-91,2%. Intensively binds to platelets, lymphocytes, alpha1-acid glycoprotein, lipoproteins and albumin. It penetrates into the fabric and retained therein for a long time. Large amounts determined in spleen, liver, kidney, lung, and thymus, moderate – and heart muscles, the minimum -. In adipose tissue, brain and bone marrow
concentration in the lungs of 300 times the concentration in plasma. It forms a number of metabolites; One of the metabolites – diatsetilvinorelbin retains antitumor activity. It is metabolized in the liver. Write mainly in the bile.
non-small cell lung cancer;
- mammary cancer.Contraindications
- hypersensitivity to vinca alkaloids;
- expressed human liver;
- initial neutrophil count <1000 cells / microliter of blood
- Radiotherapy hepatobiliary define equipoise area
- pregnancy and lactation;With care – respiratory failure, inhibition of bone marrow hematopoiesis (including after previous chemotherapy or radiation therapy), constipation or intestinal obstruction phenomena in history, a history of neuropathy.Dosage and administration
Vinorelbine is used both as a monotherapy and in combination with other anticancer drugs. When choosing the dose and mode of administration in each individual case should be referred to the specialized literature.
Vinorelbine is administered intravenously as a strictly 15-20 minute infusion.
In monotherapy the usual dose is 25-30 mg / m² body surface area once a week.The drug was diluted in 0.9% sodium chloride or 5% dextrose solution to a concentration of 1.5-3.0 mg / ml.After administration the vein should be flushed by introducing an additional 50-100 mL of 0.9% sodium chloride solution.
Granulocytopenia, anemia, and rarely – thrombocytopenia smallest number of granulocytes occurs 7-10 days after initiation of therapy, recovery occurs in the next 7-14 days. From the nervous system: the reduction or loss of deep tendon reflexes, paresthesia , hypersthesia, weakness in the legs, pain in the jaw, headache, paresis bowel, rarely paralytic ileus. On the part of the digestive system: nausea, vomiting, anorexia, constipation, diarrhea, dysphagia, mucositis, pancreatitis, increased bilirubin levels and increased activity “liver” transaminases. On the part of the respiratory system: difficulty breathing, shortness of breath, bronchospasm, interstitial pneumonia, acute respiratory distress syndrome. Since the cardiovascular system: chest pain, increased or decreased blood pressure, tachycardia, rarely – myocardial infarction , pulmonary edema Local reactions: pain or redness at the injection site; when extravasation – cellulitis, phlebitis, and possibly necrosis of surrounding tissues. Other: fatigue, alopecia, myalgia, arthralgia, skin rashes, allergic reactions, hot flashes to the face, increased creatinine, hyponatraemia, hemorrhagic cystitis and the syndrome of inappropriate secretion of antidiuretic hormone.
A specific antidote is not known. In the case of an overdose the patient should be hospitalized and carefully monitor the function of vital organs. The main expected manifestations of overdose include bone marrow suppression and peripheral neuropathy. Treatment is symptomatic.
Interaction with other medicinal products and other forms of interaction
When combined with mitomycin C may develop acute respiratory failure.
When used in conjunction with paclitaxel increases the risk of neurotoxicity.
When used in conjunction with cisplatin is enhanced granulocytopenia.
Application to the background radiation therapy leads to radiosensitization.
The drug should be used with caution with inhibitors of cytochrome P450-FOR.
Treatment of vinorelbine should be carried out under the supervision of a physician who has experience with anticancer drugs.
Treatment vinorelbine carried out under strict hematological control, determining the number of white blood cells, granulocytes, and hemoglobin level prior to each regular injection.
If abnormal liver function the dose of vinorelbine should be reduced If the kidney function the need to strengthen monitoring of the patient.
If signs of neurotoxicity of drug treatment should be discontinued.
in case of shortness of breath, cough, or hypoxia of unknown etiology should examine the patient to rule out pulmonary toxicity.
If extravasation of drug infusion should be discontinued immediately, the remaining dose administered define equipoise in another vein.
During and for at least three months after cessation of therapy is necessary to use reliable methods of contraception.
in case of contact with eyes vinorelbine should be abundantly and thoroughly with water.
Running low dose t3 clen cycle trying to lose bodyfat isn’t a real hot idea imo.