PLAKSAT

Active material: Oxaliplatin
When ATH: L01XA03
CCF: Anticancer drug
When CSF: 22.01.02
Manufacturer: ACTAVIS GROUP hf. (Iceland)

Pharmaceutical form, composition and packaging

Lyophylisate dlya solution for infusion white or nearly white pressed or porous mass, or pieces.

[Ring] lactose monohydrate.

Glass Bottles (1) – packs cardboard.

Valium for solution for infusion white or nearly white pressed or porous mass, or pieces.

[Ring] lactose monohydrate.

Glass Bottles (1) – packs cardboard.

DESCRIPTION OF ACTIVE SUBSTANCES

Pharmacological action

The antitumor agent, platinum derivatives. Oxaliplatin яvlяetsя stereoizomerom, molecule in which the central atom of platinum surrounded oxalate and diaminocyclohexane, arranged in a trans-position. Like other platinum derivatives, oxaliplatin interacts with DNA, forming inside- and linking mezhspiralnye, that block its synthesis and subsequent replication. Synthesis links oxaliplatin DNA fast and a maximum 15 m (cisplatin at a two-phase process with delayed 4-8 hour phase). Violation of DNA synthesis leads to inhibition of RNA synthesis and cellular protein. Oxaliplatin is effective on some lines resistant to cisplatin.

Pharmacokinetics

Oxaliplatin is extensively metabolized by the end of 2 hours of a dose of 130 mg / m² not determinable, wherein 15% the administered dose is in the blood, and the remaining 85% rapidly distributed in tissues (or excreted in the urine). Platinum is bound to plasma albumin.

Excreted in the urine within the first 48 no.

By the fifth day around 54% total dose is found in the urine and less 3% – Calais.

In renal failure showed a significant decrease in the clearance with 17.55 ± 2.18 l / h to 9.95 ± 1.91 L / h, and V_d from 330 ± 40.9 to 241 ± 36.1 l. Influence of severe renal impairment on platinum clearance has not been studied.

Testimony

Metastatic colorectal cancer as monotherapy or in combination therapy with a fluoropyrimidine.

Ovarian Cancer.

Dosage regimen

Establish individually, depending on the evidence and disease stage, the state of the hematopoietic system, scheme anticancer therapy.

Side effect

From the hematopoietic system: anemia, leukopenia, granulocytopenia, thrombocytopenia.

From the digestive system: nausea, vomiting, diarrhea.

From the central and peripheral nervous system: often – perifericheskie neuropathy, characterized by limb paresthesia; may be accompanied by convulsions, dysesthesia perioral area, or upper respiratory tract (that can simulate the clinical picture of reversible laryngospasm) and gastrointestinal tract. The emergence of such symptoms are often caused by exposure to cold. Paraesthesia, primarily, regress between courses of treatment, but it may take a permanent nature and cause functional impairment usually after exceeding the total dose 800 mg / m² (6 rates).

Other: in some cases – temperature rise, skin rash.

Contraindications

Myelosuppression prior to the first course of therapy when the level of neutrophils less 2 x 10⁹/L and / or platelets less 100 x 10⁹/l, peripheral neuropathy sensitivity before the first course of therapy, severe renal dysfunction (CC less than 30 ml / min), pregnancy, lactation (breast-feeding), hypersensitivity to oxaliplatin.

Pregnancy and lactation

Oxaliplatin is contraindicated during pregnancy and lactation.

Cautions

Oxaliplatin may be used only by a qualified doctor, with experience in cancer chemotherapy.

Before treatment and before the next administration of oxaliplatin is necessary to conduct a study of peripheral blood, In addition, periodic neurological examination, especially while the use of drugs, with potential neurotoxicity.

For the prevention and treatment of nausea and vomiting is recommended that the use of antiemetics.

In cases of hematological disorders (leukopenia <2000/l and / or thrombocytopenia <50 000/l) the next administration should be delayed until normal blood picture.

Drug Interactions

When using oxaliplatin in combination with 5-fluorouracil marked synergistic cytotoxic effects in vitro and in vivo, exacerbated by the severity of neutropenia and thrombocytopenia.