Included in the formulation
АТХ:L.01.X.E.07 Lapatinib
Pharmacodynamics:An antitumor drug, a selective and reversible inhibitor of intracellular tyrosine kinase. Binds receptors epidermal factor a growth (human epidermal growth factor receptor - HER2 + / neu / ErbB2 + and epidermal growth factor receptor - EGFR / ErbB1). The dissociation period of 50% of the ligand from the ligand-receptor complex continues for 300 minutes.
Pharmacokinetics:Absorbed in the gastrointestinal tract after ingestion. The maximum concentration in the plasma is reached 4 hours after taking the drug. In 99% it binds to blood plasma proteins. Metabolized by oxidation to inactive metabolites.
The half-life is 24 hours.
Elimination of the intestine - 27% unchanged. 2% of the dose - kidney in the form of metabolites and unchanged.
Indications:It is used for malignant, widespread, metastatic breast tumors in complex therapy with capecitabine.
II.C50.C50 Malignant neoplasm of breast
Contraindications:Individual intolerance, children under 18 years.
Carefully:Violations of liver function of moderate or severe severity
Pregnancy and lactation:Pregnancy and lactation: recommendations for FDA - category D. The use of the drug is contraindicated in pregnancy and lactation.
Dosing and Administration: Used internally at 1250 mg per day at a time every day. When toxic effects appear, the dose is reduced to 1000 mg per day.
The highest daily dose: 1250 mg.
The highest single dose: 1250 mg.
Side effects:The cardiovascular system: heart palpitations, heart failure, dyspnea.
Respiratory system: pneumonitis - interstitial pulmonary process.
Digestive system: anorexia, diarrhea, nausea, vomiting.
Leather: acne, rash.
Allergic reactions.
Overdose:Acute left ventricular failure.
Treatment is symptomatic.
Interaction:When used simultaneously with inducers CYP3A4 (carbamazepine, rifampicin, phenytoin), careful monitoring of the patient's condition is recommended to prevent unwanted side reactions.
Special instructions:At the first symptoms of diarrhea, the use of antidiarrhoeal agents is recommended.
Before treatment and then monthly monitored the activity of transaminases, alkaline phosphatase, and bilirubin. If necessary, the dose of lapatinib is adjusted.