Pazopanib - instructions for use, doses, side effects, contraindications

Clinical and pharmacological group: & nbsp

Antineoplastic agents - inhibitors of protein kinases

Included in the formulation

Votrient

pills inwards

Novartis Pharma AG Switzerland

АТХ:

L.01.X.E Protein kinase inhibitors

L.01.X.E.11 Pazopanib

Pharmacodynamics:

Connectionsis with receptors of endothelial growth factors of vessels, stem cells and platelets, inhibits tyrosine kinases receptors to VEGF-1, VEGF-2, VEGF-3; PDGF-α and PDGF-β. Thekzhe inhibits tyrosine kinase receptors of growth factors of fibroblasts, intreleukin-2, cytokinin, transmembrane glycoprotein receptor tyrosine kinase and leukocyte-specific protein-thyrokinase. The dissociation period of 50% of the ligand from the ligand-receptor complex continues for 300 minutes.

Pharmacokinetics:

After oral administration, the empty stomach is completely absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 3 hours. The connection with plasma proteins is 99%.

Therapeutic effect develops after the reception. Metabolism in the liver.

Half-life is 30 hours. Elimination of the intestine - 27% unchanged. 2% of the dose - kidney in the form of metabolites and unchanged.

Indications:

It is used to treat common renal cell carcinoma, common soft tissue sarcoma in patients after a course of chemotherapy.

ICD-10

II.C45-C49 Malignant neoplasms of mesothelial and soft tissues

II.C64-C68.C64 Malignant neoplasm of kidney, except for renal pelvis

Contraindications:

Severe renal and hepatic insufficiency, individual intolerance, children under 18 years of age.

Carefully:

Hepatic and renal failure of moderate severity.

Pregnancy and lactation:Recommendations for FDA - category D. The use of the drug is contraindicated in pregnancy and lactation.

Dosing and Administration:

Inside 1 hour before meals, or 2 hours after eating, 800 mg 2 times a day.

The highest daily dose: 800 mg.

The highest single dose: 800 mg.

Side effects:

Central and peripheral nervous system: headache, transient ischemic stroke, rarely - ischemic stroke.

Respiratory system: dyspnoea, cough, pneumothorax, dysphonia.

The system of hematopoiesis: neurocytopenia, thrombocytopenia.

Blood coagulation system: nosebleeds, thromboembolic complications, gastrointestinal bleeding.

The cardiovascular system: increased blood pressure, myocardial infarction, rarely - ventricular tachycardia.

Digestive system: abdominal pain, dyspeptic disorders, diarrhea, stomatitis.

Musculoskeletal system: myalgia, ossalgia.

Dermatological reactions: alopecia, depigmentation of hair, dry skin, nail damage, exfoliative rash.

Sense organs: decreased visual acuity.

Urinary system: proteinuria.

Allergic reactions.

Overdose:

Increased side effects.

Treatment is symptomatic.

Interaction:

When used simultaneously with inducers CYP3A4 (carbamazepine, rifampicin, phenytoin), careful monitoring of the patients' 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, dose correction of pazopanib is performed.

Instructions

Pazopanib (Pazopanibum)