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1 ml of solution of drug of Erbituks can contain 5 mg or 2 mg of a tsetuksimab.
Additional substances: polysorbate 80, glycine, monohydrate of citric acid, sodium chloride, water, sodium hydroxide.
Transparent or a little opalescent yellowish solution.
- Solution of 5 mg / 1 ml is issued in glass colourless bottles on 20, 10, 50 or 100 ml in paper packaging.
- Solution of 2 mg / 1 ml is issued in glass colourless bottles on 50 ml in paper packaging.
Pharmacodynamics and pharmacokinetics
Tsetuksimab is the monoclone of himerny type of the class IgG1 which is selectively contacting an epidermal receptor of a growth factor (further EGFR). EGFR plays a role in control of mechanisms of a survival of a cell, an angiogenesis, cellular cycle, migration of cells and innidiations.
Specificity of linkng of active agent with EGFR is 6-8 times higher in comparison with endogenous ligands that causes blocking of work of the last. Tsetuksimab also stimulates the internalization of EGFR causing blocking of function of a receptor. Drug sensibilizes cytocidal effector immune cells against the tumor cells capable to express EGFR.
Tsetuksimab slows down proliferation and induces death of the tumor cells expressing EGFR. Brakes products of the factors stimulating an angiogenesis tumor cells and stops migration of endothelial cells. Causes lowering of neovascularization and weakening of processes of innidiation of a tumor.
The pharmacokinetics has dozozavisimy character. Tsetuksimab possesses a long elimination half-life to equal 3-4 days. Average value of a maximum level is equal to about 152 mkg/ml. All ways of a metabolism include a stage of division of antibodies to small molecules. Pharmacokinetic indicators do not depend on a floor, race or age.
Indications to use
- Colorectal cancer of metastatic type with an expression of EGFR and wild genes of RAS for monotherapy against inefficiency of last chemotherapy Irinotekan and Oksaliplatin or at their intolerance.
- Colorectal cancer of metastatic type with an expression of EGFR and wild genes of RAS for the combined therapy on the basis of Irinotekan or long administration of mix from Ftoruratsil and Folinat of calcium with Oksaliplatin.
- Planocellular malignant new growth of the head and neck of locally-spread type together with radiation therapy.
- Planocellular malignant new growth of the head and neck of recurrent or metastatic type for therapy in a combination with chemotherapy platinum drugs.
- Planocellular malignant new growth of the head and neck of recurrent or metastatic type for therapy at inefficiency of chemotherapy platinum drugs.
- Strong hypersensitivity to a tsetuksimab.
- Erbituks's use against oksaliplatinsoderzhashchy therapy at persons with a colorectal cancer of metastatic type with mutant genes of RAS or with RAS genes with the unknown status.
- Pregnancy or lactation.
- Children's age.
Before carrying out a combination therapy it is recommended to estimate contraindications for radiation therapy and contraindication to use of the accompanying himiopreparat.
Medicine with care is applied at disturbances of work of a liver or kidneys, cardiopulmonary diseases, disorders of marrowy blood formation, at advanced age.
- Frustration from nervous activity: headache, meningitis.
- Visual disturbances: blepharitis, conjunctivitis, keratitis.
- Disorders of breath: intersticial illness, pulmonary embolism.
- Digestive disturbances: nausea, diarrhea, vomiting.
- Disorders of skin: aknepodobny rash, itch, xeroderma, hypertrichosis, damage of nails, peeling, Stephens-Johnson's syndrome, necrotic fasciitis, toxic staphylococcal epidermal syndrome, sepsis. The majority of similar reactions develop in the first 21 day of treatment and usually take place after the drug therapy termination.
- Frustration of a metabolism: hypomagnesiemia, hypocalcemia, dehydration, anorexia.
- Frustration from blood circulation: deep vein thrombosis.
- The disorders of the general character caused with administration of drug: infuzionnozavisimy reactions, mukozita, small tortoiseshell, bronchospasm, change of pressure, loss of consciousness, stenocardia, myocardial infarction, fatigue.
- Frustration from gepatobiliarny system: increase in the ACT, ALT level or alkaline phosphatase.
At use of a tsetuksimab together with himiopreparata it is necessary to study the instruction for use of these drugs.
- At treatment tsetuksimaby along with chemotherapy drugs of platinum did not exclude increase of frequency of development of a heavy leukopenia or neutropenia and, as a result, increase of risk of infectious complications (pneumonia, a febrile neutropenia, sepsis).
- At treatment tsetuksimaby together with ftorpirimidina increase of frequency of development of ischemia of a myocardium (a myocardial infarction, heart failure of congestive type, a palmar and bottom syndrome) in comparison with treatment only of a ftorpirimidinama came to light.
- At treatment by Tsetuksimab together with local radiation therapy of the head and neck emergence of the additional side effects characteristic of radiation therapy is possible (beam dermatitis, mukozit, a dysphagy, a leukopenia).
Application instruction (Way and dosage)
The drug is administered infusionally under supervision of the doctor with experience of use of antineoplastic medicines.
Erbituks, application instruction
During introduction and within an hour after its termination carry out careful monitoring of vital signs of the patient. The resuscitation equipment has to be prepared. Before the 1st and each following infusion premedication is recommended by antihistamines or glucocorticosteroids.
At any indications drug of Erbituks is used once a week. The dosage at the first introduction which continues 2 hours makes 400 mg/sq.m. The subsequent infusions are entered in a dosage of 250 mg/sq.m and last 1 hour. The maximum rate of administering should not be more than 10 mg/min.
At patients with a colorectal cancer of metastatic type medicine is used in combination with chemotherapy or odinochno. To the first it is necessary to determine by its use a type of genes of RAS.
At the combined therapy consults to adhere to recommendations about change of doses jointly of the used chemotherapeutic drugs, the specified their instructions. The specified drugs, anyway, have to be administered with a break at least 1 hour after completion of infusion of Erbituks. Therapy by Erbituks needs to be continued before emergence of symptoms of progressing of cancer.
Planocellular cancer of the head and neck
At patients with a planocellular malignant tumor of the head and neck drug is used together with radiation therapy. It is recommended to begin therapy with drug in a week prior to the beginning of radiotheraphy and to continue before its termination. At patients with recurrent or metastatic types of cancer medicine is used in combination with chemotherapy platinum drugs. Erbituks it is used as a maintenance therapy before development of symptoms of progressing of a disease. The specified drugs have to be administered with a break at least 1 hour after completion of infusion of Erbituks.
At patients with a planocellular malignant tumor of the head and neck of recurrent or metastatic type which is not giving in to treatment by chemotherapy, Erbituks is applied in the form of monotherapy. Treatment by drug of Erbituks is usually continued before emergence of symptoms of progress of a disease.
Councils for correction of dosages
At emergence of skin reaction it is recommended to interrupt administration of drug. Treatment is allowed to be continued after reaction stopping. If similar skin reaction in a severe form arose for the first time, therapy is resumed in a former dosage.
In case of recurrence of a severe form of skin reaction, Erbituks also it has to be cancelled before reaction stopping. Treatment in that case can be started over again only in a reduced dosage (200 mg/sq.m).
If the severe form of skin reaction developed in the 4th time or was not stopped against a treatment stop, drug use is contraindicated further.
Councils for preparation of solution for infusion and to ways of introduction
Erbituks it is entered intravenously with use of an infusional or spray pomp, drop system. The described medicine is compatible only to sterile physical solution. It should not be mixed with other drugs or solutions. For introduction it is necessary to use separate system for infusions, at the end of introduction the used system is washed out sterile physical solution.
Erbituks it is compatible with:
- polyethylene, ethylvinylacetate or PVC tanks for infusion solutions;
- polyethylene, polyurethane, ethylvinylacetate, PVC or the polyolefin systems for infusions;
- the polypropylene syringes used to a spray pomp.
At preparation of solution it is necessary to meet aseptic conditions as drug does not contain antibacterial substances. It is strongly recommended to administer the drug immediately after opening of a bottle.
Experience of use of the dosages exceeding 400 mg/sq.m is limited. And its treatment it is not enough data on signs of overdose.
Tsetuksimab in combination with chemotherapy platinum drugs in comparison with monotherapy by drugs of platinum increases the frequency of development of a strong leukopenia and strong neutropenia, the followed infectious complications.
Use of a tsetuksimab in combination with ftorpirimidina in comparison with monotherapy of a ftorpirimidinama can provoke increase of frequency of development of ischemia of a myocardium, including a myocardial infarction and heart failure of congestive type.
Terms of sale
According to the recipe.
At a temperature of 2-8 °C (not to freeze). To protect from children.
Period of validity
Infuzionnozavisimy side reactions
At emergence of infuzionnozavisimy side reaction of easy or moderate weight it is necessary to lower medicine rate of administering. During the subsequent infusions it is necessary to adhere to the reduced rate of administering.
At emergence of the expressed infuzionnozavisimy reaction it is necessary to cancel immediately drug and if necessary to start emergency treatment. Repeated administration of drug in the described case is contraindicated.
Skin side reactions
Similar reactions are observed rather often, as a result of their emergence can be required having rummaged in treatment or its full cancellation. For prevention of reactions from skin oral administration of Tetracycline and local uses of 1% of cream of a hydrocortisone within 6-8 weeks is recommended.
For therapy of skin reactions also appoint local forms of glucocorticosteroids or peroral tetracyclines.
Electrolytic disturbances of blood
The progressing lowering of the level of magnesium in blood is capable to lead to the expressed hypomagnesiemia which is reversible if to make drug withdrawal. Also the hypopotassemia against diarrhea can come to light. It is recommended to investigate electrolytic composition of blood and to carry out correction of electrolytic frustration prior to therapy and it is regular in the course of therapy.
Use for elderly persons
Correction of dosages of drug is not required from this category of patients.
The therapeutic effectiveness of a tsetuksimab at patients is younger than 18 years is not established.
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