TRASTUZUMAB (Trastuzumab)

     Synonym: Gertseptin, Herceptin.

     Description: White or pale yellow powder.

     Pharmacology: Farmakologicheskoe action-Vaccination (cytostatics).

Gumanizirovannye recombinant monoclonal antibody, derived DNA to IgG1, a human framework regions and komplementarno- defining regions èþíÿ r185 HER2 antibody. Antibodies selectively interact with the extracellular domain belka- receptor? 2 epidermalnomu rostovomu factor Rights (HER2) on the surface of malignant cells and inhibited their proliferation. Indirect cellular cytotoxicity more evident in relation to Tumor cells, giperekspressiruyuschim HER2. Monotherapy metastaziruyuschego breast cancer in the face giperekspressii HER2 accompanied by the development of remission in 15% and a mean survival period of 13 months. In combination with paklitakselom increases the average time to the disease progressing to 6.9 months.

In the pilot study, it was noted normal development of embryos in rodents with HER2 receptor type and mutant mouse embryos death in the absence of HER2 receptor type.

When the / in a dose of 10, 50, 100, 250 and 500 mg pharmacokinetics parameters have dozozavisimy nature. With increasing doses higher value T1 / 2 and declining - Cl. T 1 / 2 after loading (4 mg / kg) and supportive (2 mg / kg weekly) dose-an average of 5.8 days (range 1-32 days). The equilibrium concentration in the range of 79-123 ug / ml obtained between 16 th and 32 th week. Penetrates through the placenta barrier. With Cynomolgus monkey in a dose, 25 times more than a one-week dose of support for the rights (2 mg / kg), no effect on fertility and damaging actions of fruit (permeates through the placenta from 20 to 50 and 120 to 150 days of pregnancy ), sekretiruetsya in breast milk. A serum - born monkeys will not influence their growth and development from birth to 1 month.

     Application: Disseminirovanny breast cancer with giperekspressiey HER2 (monotherapy after one or more courses of chemotherapy metastaticheskoy stage or in combination with paklitakselom as first-line therapy).

     Contraindications: Hypersensitivity.

     Restrictions apply to: Odyshka alone caused metastaticheskim destruction or related lung diseases (elevated risk of fatal infusion reactions); Patients at risk for kardiotoksichnosti (cardiac failure, arterial hypotension, IBS, pre-treatment drugs and tsiklofosfamidom antratsiklinovogo series), a children's age (security and the effectiveness of the children are not identified).

     Application of pregnancy and breast feeding: Perhaps if the expected effect of therapy over the potential risk to the fetus. At the time of treatment should stop breastfeeding.

     Adverse actions: So part of the furniture: nausea, vomiting, diarrhoea phenomenon, anorexia, Constipation, rarely disruption of the liver, hepatitis, liver failure, jaundice, pancreatitis.

From the cardiovascular system and blood (blood, hemostasis): tachycardia, vazodilatatsiya, hypotension, cardiac failure, shock kardiogenny, cardiomyopathy, heart; Leukopenia, rarely violation heart rhythm, reduced emissions factions, thrombocytopenia, anemia; Reducing protrombina.

From skin cover: itching, Hyperhidrosis, drought skin, acne, rashes makulo- papuleznaya, defeated nails, hair.

On the part of the respiratory system: bronchospasm, cough, fatigue, nasal bleeding, infection with mild chest, pharyngitis, rhinitis, sinusitis; Swelling light; Hypoxy, swelling throat, distress- acute respiratory syndrome.

From the nervous system and sensory organs: dizziness, drowsiness or insomnia, paresthesia, ataxia, tremor, parezy, anxiety, depression, menopausal, deafness, coma rarely, meningitis, brain swelling, intellectual violations.

Allergic reactions: eg insights and Anaphylaxis shock.

Other: general malaise, asthenia, fever, chills, grippopodobny syndrome, the development of infection, sepsis, peripheral swelling, pain syndrome (pain in the abdomen, in the chest, head, joints, bones, muscles, back, neck); Infusion reactions, coupled syndromic: 1) fever, fever, nausea, vomiting, asthenia, tremor, pain, including headaches, dizziness, fatigue, hypotension, cough, rash (kupiruyutsya nenarkoticheskimi analgesics and pain means); 2) short, hypotension, bronchospasm, hypoxy, a man in the lungs, tachycardia (may lead to fatal require termination limited, kupiruyutsya beta - adrenolitikami, stimulation, kislorodoterapiey).

     Interaction: Do not grow in 5% glucose solution (cause protein aggregation), and mixed breeds or with other drugs.

     Dosing and Administration: W / in, infuzionno in dose 4 mg / kg over 90 min, followed by supporting dose of 2 mg / kg within 30 minutes (with a bad long-term portability) 1 once a week.

     Precautions: Treatment should be supervised onkologa. Before treatment necessarily testing Tumor expression H E R2. During treatment every 3 months must carefully monitor heart function for the early detection of kardiotoksichnosti (in the case of violations of asymptomatic heart of every 6-8 weeks). When resistant asymptomatic or clinically manifestiruyuschem reducing heart release should consider discontinuing treatment or appointment symptomatic therapy (DIURETICS, cardiac glycosides, inhibitors APF). Bakteriostaticheskaya water for injection, supplied with the product as konservanta contains 1.1% Benzyl alcohol, which has toxic effects on infants and children up to three years. In patients with Hypersensitivity to benzilovomu alcohol as a solvent to be used for water injection.

     Special instructions: The solution should be prepared in aseptic conditions; Caution and not shaking (perhaps Foam Blowing). Solution Preparation: In gm vial of dried powder slowly add 20 ml bakteriostaticheskoy water for injection, gently gm vial Rock the rotating motion (in the case of the foam to stand 5 minutes). Then a vial prepared to concentrate solution (21 mg / ml) recruited necessary and entered into the pump package with 250 ml of 0.9% sodium chloride solution. The volume of solution required for a fan or supporting dose determined by the formula: weight (kg) x necessary dose (mg / kg) / 21 mg / ml. The solution should be imposed immediately after cooking. Compatible with PVC and PE Hotel packages.

Materials allowed to copy only with the active hyperlink to the handbook of medicines