Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
An antineoplastic agent, a derivative of platinum. Oxaliplatin is a stereoisomer, in the molecule of which the central atom of platinum is surrounded by oxalate and diaminocyclohexane located in trans positions. Like other platinum derivatives, oxaliplatin interacts with DNA, forming intra- and inter-helical cross-links, which blocks its synthesis and subsequent replication. Synthesis of oxaliplatin-DNA bonds is fast and is a maximum of 15 min (in cisplatin this process is biphasic with a delayed 4-8-hour phase). Violation of DNA synthesis leads to inhibition of the synthesis of RNA and cellular protein. Oxaliplatin is effective on some lines resistant to cisplatin.
PHARMACOKINETICS
Oxaliplatin is intensively metabolized and at the end of a 2-hour administration at a dose of 130 mg / m 2 is no longer detectable, with 15% of the administered dose being in the blood, and the remaining 85% are quickly distributed in the tissues (or excreted in the urine). Platinum binds to plasma albumin.
It is excreted in the urine within the first 48 hours.
By the fifth day, about 54% of the total dose is found in the urine and less than 3% in the stool.
In renal insufficiency, a significant decrease in clearance was observed from 17.55 В± 2.18 l / h to 9.95 В± 1.91 l / h and V d from 330 В± 40.9 to 241 В± 36.1 l. The effect of severe renal failure on the clearance of platinum has not been studied.
INDICATIONS
Metastatic colorectal cancer as a monotherapy or as part of a combination therapy with fluoropyrimidines.
Cancer of the ovaries.
DOSING MODE
Established individually, depending on the indications and stage of the disease, the state of the hematopoiesis system, the scheme of antitumor therapy.
SIDE EFFECT
On the part of the hematopoiesis system: anemia, leukopenia, granulocytopenia, thrombocytopenia.
From the digestive system: nausea, vomiting, diarrhea.
From the side of the central nervous system and peripheral nervous system: often - peripheral neuropathies, characterized by paresthesia of the limbs; may be accompanied by cramps, dysesthesia of the perioral region or upper respiratory tract (which can simulate the clinical picture of reversible laryngospasm) and gastrointestinal tract. The appearance of such symptoms is often due to the effects of cold. Paresthesia, in general, regresses between treatment courses, but can become permanent and cause functional impairment usually after exceeding the total dose of 800 mg / m 2 (6 courses).
Other: in some cases - fever, skin rash.
CONTRAINDICATIONS
Myelosuppression before the first course of therapy with a neutrophil level of less than 2 Г— 10 9 / L and / or platelets of less than 100 Г— 10 9 / L, peripheral sensory neuropathy before the start of the first course of therapy, severe renal dysfunction (KC less than 30 ml / min) pregnancy, lactation (breastfeeding), hypersensitivity to oxaliplatinum.
PREGNANCY AND LACTATION
Oxaliplatin is contraindicated in pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe violations of kidney function (QC less than 30 ml / min).
SPECIAL INSTRUCTIONS
Oxaliplatinum can be used only by a qualified physician who has experience in carrying out antitumoral chemotherapy.
Before the start of treatment and before the next administration of oxaliplatin, a study of peripheral blood should be carried out, in addition, a neurological examination should be carried out regularly, especially when used with drugs with potential neurotoxicity.
For the prevention and treatment of nausea and vomiting, antiemetics are recommended.
In cases of hematological disorders (leukopenia less than 2 Г— 10 9 / L and / or thrombocytopenia less than 50 Г— 10 9 / L), the next administration should be postponed until the normal picture of blood is restored.
DRUG INTERACTION
When oxaliplatin is used in combination with 5-fluorouracil, a synergistic cytotoxic effect is observed in vitro and in vivo, and the severity of neutropenia and thrombocytopenia is exacerbated.
