Universal reference book for medicines
Product name: TAUTAX (TAUTAX)

Active substance: docetaxel

Type: Antitumor preparation

Manufacturer: LENS-PHARM (Russia), a subsidiary of VEROPHARM (Russia)
Composition, form of production and packaging
Concentrate for the preparation of a solution for infusions is
transparent, light yellow in color.

1 ml

docetaxel anhydrous 20 mg

[PRING] polysorbate 80, citric acid anhydrous (10% solution in anhydrous ethanol), ethanol anhydrous.

1 ml - bottles (1) - packs of cardboard.

Concentrate for the preparation of a solution for infusions is transparent, light yellow in color.

1 ml of 1 fl.

docetaxel anhydrous 20 mg 80 mg

[PRING] polysorbate 80, citric acid anhydrous (10% solution in anhydrous ethanol), ethanol anhydrous.

4 ml - vials (1) - packs cardboard.

INSTRUCTION FOR THE SPECIALIST.

The product description was approved by the manufacturer for the 2009 print edition.

PHARMACHOLOGIC EFFECT

An antitumor preparation of plant origin from the taxoid group.
Accumulates tubulin in microtubules, prevents their disintegration, which disrupts the phase of mitosis and interfacial processes in tumor cells.
In addition, docetaxel is active against certain cells producing an excess amount of P-glycoprotein, which is encoded by a multiple-resistance gene.

In vivo docetaxel has a broad spectrum of activity against tumors of mice and transplanted human tumor cells.

PHARMACOKINETICS

The kinetics of docetaxel is dose-dependent and corresponds to a three-phase pharmacokinetic model.

Distribution

Docetaxel binds more than 95% to plasma proteins.
The concentration of docetaxel in tumor cells is high.
Metabolism and excretion

Docetaxel is metabolized in the liver.

75% of the drug is excreted with bile, with urine released no more than 10%.
T 1/2 in the final phase is 11.1-18.5 h.
Pharmacokinetics in special clinical cases

The clearance of docetaxel depends on the surface of the body, the function of the liver and the concentration of plasma proteins.
The sequence of drug administration during polychemotherapy can change the clearance of docetaxel.
In hepatic failure, clearance of docetaxel is reduced by approximately 30%.

INDICATIONS

- locally advanced or metastatic breast cancer (as 1st line therapy - in combination with doxorubicin, as second line therapy - in monotherapy or in combination with capecitabine);

- inoperable, locally advanced or metastatic non-small cell lung cancer (as 1st line therapy - in combination with cisplatin or carboplatin, as second line therapy in monotherapy);

- metastatic ovarian cancer (2nd line therapy);

- metastatic squamous cell carcinoma of the soft tissues of the head and neck (2nd line therapy).

DOSING MODE

To prevent reactions of hypersensitivity, and to reduce fluid retention, all patients before the introduction of Tautax should undergo premedication of GCS, for example, dexamethasone at a dose of 16 mg / day (8 mg 2 times / day) inside, for 3 days, starting 1 day before the introduction of Tautakes.

Tautax is administered as a one-hour intravenous infusion.

In breast cancer, Tautax is administered at a dose of 100 mg / m 2 every 3 weeks with monotherapy.
In combination with doxorubicin (50 mg / m 2 ) or capecitabine (1250 mg / m 2 orally 2 times / day for 2 weeks followed by a weekly break), Tautax is administered at a dose of 75 mg / m 2 every 3 weeks.
In non-small cell lung cancer, Tautax is administered at a dose of 75 mg / m 2 with monotherapy and 75 mg / m 2 in combination with platinum drugs every 3 weeks.

In metastatic ovarian cancer, Tautax is administered at a dose of 100 mg / m 2 every 3 weeks.

In metastatic squamous cell carcinoma of the soft tissues of the head and neck, Tautax is administered at a dose of 100 mg / m 2 every 3 weeks.

Correction of dose

Tautax is administered at a neutrophil count of? 1500 / μL.
With a decrease in the number of neutrophils <500 / μl, which was observed for more than 1 week, with the development of febrile neutropenia, the development of severe skin reactions or severe peripheral neuropathy, the dose for the following administrations should be reduced from 100 to 75 mg / m 2 and / or from 75 to 60 mg / m 2 . If such complications occur when Tautakes is administered at a dose of 60 mg / m 2 , treatment should be discontinued.
With the combined use of Tautakes and capecitabine for the first appearance of grade 2 toxicity that persists before the beginning of the next cycle of therapy, treatment should be deferred until toxicity decreases to 0-1 degree, with 100% of the original dose of Tautakes being introduced during the next treatment cycle.

In patients with repeated development of grade 2 toxicity or the first development of grade 3 toxicity at any time of the therapy cycle, treatment is delayed until toxicity is reduced to 0-1 degree, then treatment with Tautakes resumes at a dose of 55 mg / m 2 .

With any subsequent manifestations of toxicity or the appearance of any toxicity type 4, the administration of Tautakes should be discontinued.

Regarding dose adjustment for capecitabine, when combined with Tautakes, instructions for the administration of capecitabine should be followed.

When Tautakes was used at a dose of 75 mg / m 2 in combination with cisplatin in patients whose platelet count decreased to <25,000 / mm3 in the previous treatment cycle, or in patients who developed febrile neutropenia, or in patients with severe non- toxicity, the dose of Tautakes in the next cycle should be reduced to 65 mg / m2 .
When correcting the dose of cisplatin, the instructions for the use of cisplatin should be followed.
Alternatively, in patients who developed febrile neutropenia or severe infection during the last of the cycles, a granulocyte colony-stimulating factor may be used to maintain the clinically important intensity of the dosing regimen.

For patients with hepatic impairment at ALT and / or AST level exceeding the upper limit of the norm (VGN) or more than 1.5 times the level of HGV more than 1.5 times, the recommended dose is 75 mg / m 2 .
In patients with elevated levels of bilirubin and / or increased activity of ALT and AST (> 3.5 VGN) in combination with an increase in the level of alkaline phosphatase (> 6 VGN), Tautax is not recommended.
Given the analysis of pharmacokinetic data, there are no specific recommendations for the use of Tautakes in elderly patients .

Preparation of a solution for infusions

The required volume of concentrate in accordance with the required dose is introduced into a vial containing 250 ml of a 5% dextrose solution or 0.9% sodium chloride solution.
If the required dose of docetaxel is greater than 200 mg, a larger volume of infusion fluid should be used so that the docetaxel concentration is not above 0.74 mg / ml.
The resulting solution should be gently mixed and used for 4 hours at room temperature and normal conditions of illumination.

A Tautakes solution for infusions should be inspected before administration;
In the presence of sediment, the solution should be destroyed.
SIDE EFFECT

From the hemopoietic system: often - reversible neutropenia, in some cases accompanied by fever.
The number of neutrophils is reduced to the minimum values ​​on average for 7 days (in patients who received previous chemotherapy, this period may be shorter), the average duration of severe neutropenia (<500 / μL) is 7 days.Possible development of thrombocytopenia and anemia.
Allergic reactions: Moderately severe hypersensitivity reactions usually occur within a few minutes after the onset of infusion (hot flashes, rash, itching, chest tightness, back pain, dyspnea, drug fever, or chills);
possibly the development of severe reactions (arterial hypotension and / or bronchospasm, generalized rash and erythema), which disappeared after discontinuation of infusion and the appointment of adequate therapy; in some cases - bullous rash (Lyell's syndrome or Stevens-Johnson syndrome).
Dermatological reactions: alopecia, mild and moderately expressed skin reactions;
Rarely expressed reactions (rash accompanied by itching, or limited erythema of the skin of the palms and feet with swelling and subsequent desquamation), hypo- or hyperpigmentation of the nails, onycholysis.
On the part of water metabolism: peripheral edema, pleural or pericardial effusion, ascites, weight gain.
Peripheral edema usually appears on the lower limbs, and then can become generalized, leading to an increase in body weight of 3 kg or more. The frequency and severity of fluid retention increases with repeated administration of the drug; the average total docetaxel dose at which fluid retention was observed was 818.9 mg / m 2 and 489.7 mg / m 2 premedication without premedication.However, in some cases, swelling occurred during the first course of therapy. The fluid retention was not accompanied by acute episodes of oliguria or arterial hypotension. In some cases, the reported development of dehydration and pulmonary edema.
On the part of the digestive system: nausea, vomiting, diarrhea, anorexia, constipation, stomatitis, taste disorder, esophagitis, epigastric pain, increased activity of ALT, AST, APF and bilirubin level in serum;
rarely - gastrointestinal bleeding; in isolated cases - intestinal obstruction.
From the side of the central nervous system and peripheral nervous system: peripheral neuropathy (in the form of easy or poorly expressed paresthesias, hyperesthesias, dysesthesia, pain, including burning sensation), weakness (these changes pass independently for 3 months);
in some cases - convulsions and a transient loss of consciousness.
From the cardiovascular system: heart rhythm disturbances (sinus tachycardia, atrial fibrillation), unstable angina, heart failure, arterial hypo- or hypertension;
in some cases - venous thromboembolism, myocardial infarction.
From the side of the organ of vision: rarely - the development of lacrimation in conjunction with conjunctivitis (or without it), transient visual disturbances (flashes of light in the eyes, the appearance of cattle), usually occurring during the administration of the drug and combined with the development of hypersensitivity reactions that disappeared after discontinuation of the infusion ;
in isolated cases - in patients receiving simultaneously other antitumor drugs, it is possible to develop occlusion of the lacrimal canal, leading to excessive lacrimation.
Local reactions: hyperpigmentation, inflammation, redness, dry skin, phlebitis, hemorrhage, edema of veins.

Other: arthralgia, myalgia, asthenia, muscle weakness, shortness of breath, generalized or local pain, including chest pain, not related to heart or lung disease, sepsis;in isolated cases - acute respiratory distress syndrome, interstitial pneumonia, pulmonary fibrosis and increased reaction to irradiation.

With the use of Tautakes in combination with capecitabine, side effects from the digestive system, palmar-plantar syndrome, dehydration, lacrimation, arthralgia, severe thrombocytopenia and anemia, hyperbilirubinemia were more frequent, but the more rare development of severe neutropenia, alopecia, nail abnormalities, asthenia, myalgia, swelling of the lower extremities.

CONTRAINDICATIONS

- initial number of neutrophils <1500 / μl;

- pronounced violations of the liver function;

- Pregnancy;

- the period of lactation (breastfeeding);

- Hypersensitivity to docetaxel or other components of the drug.

PREGNANCY AND LACTATION

Tautax is contraindicated in pregnancy and lactation (breastfeeding).

Patients of childbearing age should use reliable methods of contraception during the use of the drug and for at least 3 months after its withdrawal.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

For patients with hepatic impairment at ALT and / or AST level exceeding the upper limit of the norm (VGN) or more than 1.5 times the level of HGV more than 1.5 times, the recommended dose is 75 mg / m 2 .
In patients with elevated levels of bilirubin and / or increased activity of ALT and AST (> 3.5 VGN) in combination with an increase in the level of alkaline phosphatase (> 6 VGN), Tautax is not recommended.
APPLICATION FOR CHILDREN

The safety and efficacy of Tautakes in children have not been adequately studied.

APPLICATION IN ELDERLY PATIENTS

Given the analysis of pharmacokinetic data, there are no specific recommendations for the use of Tautakes in elderly patients .

SPECIAL INSTRUCTIONS

Treatment Tautakesom conducted only under the supervision of a specialist who has experience of antitumor therapy, in a specialized hospital.

A systematic control of the picture of peripheral blood during the period of treatment with Tautakes is necessary.
With the development of severe neutropenia (<500 / μL for 7 days or more), it is recommended to reduce the dose of the drug.
To identify the reactions of hypersensitivity patients should be carefully monitored, especially during the first and second infusions.
Light manifestations of hypersensitivity (redness of the face or localized skin reactions) do not require an interruption in the administration of the drug. Severe hypersensitivity reactions (decreased blood pressure, bronchospasm or generalized rash / erythema) require immediate withdrawal of the drug and the adoption of appropriate therapeutic measures to stop these complications. Reusing Tautakes in these cases is prohibited.
In patients with impaired hepatic function, the risk of severe adverse effects (sepsis, gastrointestinal bleeding, febrile neutropenia, infections, thrombocytopenia, stomatitis and asthenia) is extremely high, and therefore functional liver samples should be determined before the therapy is started and before each subsequent cycle of Tautakes therapy.

In connection with the possibility of the development of edematous syndrome, it is necessary to observe patients with ascites, effusion to the pleural cavity or pericardium.
When there is edema, the salt and drinking regimen and the appointment of diuretics are shown.
In patients over the age of 60 who received combination therapy with Tautakes and capecitabine, a more frequent development of toxicity of 3-4 degrees is observed in comparison with patients of younger age.

Precautions should be taken when preparing the Tautakes Solution.
It is necessary to use gloves, a mask and glasses.
If the product gets on the skin, immediately wash it with soap and water.
If the product gets on mucous membranes, immediately rinse with water.
Use in Pediatrics

The safety and efficacy of Tautakes in children have not been adequately studied.

OVERDOSE

Symptoms: suppression of bone marrow function, peripheral neuropathy, inflammation of the mucous membranes.

Treatment: there is no specific antidote.
In case of an overdose, the patient should be hospitalized in a specialized department and carefully monitor the function of vital organs. Assign a granulocyte colony-stimulating factor. If necessary, conduct symptomatic therapy.
DRUG INTERACTION

In vitro studies have shown that the biotransformation of the drug can change with the simultaneous use of substances inducing, inhibiting or metabolizing the isoenzyme CYP3A4 (cyclosporine, terfenadine, ketoconazole, erythromycin, trolleandomycin).
In this regard, care must be taken when concurrently prescribed with such drugs, given the possibility of interaction.
In vitro drugs characterized by high protein binding, such as erythromycin, diphenhydramine, propranolol, propafenone, phenytoin, salicylate, sulfamethoxazole, sodium valproate, did not affect the binding of docetaxel to proteins.

Docetaxel does not affect the binding of digitoxin.

Pharmacokinetic interaction

When docetaxel was used in combination with doxorubicin, clearance of docetaxel increased while maintaining its effectiveness.

At the same time, the clearance of doxorubicin and the level of doxorubicinol (doxorubicin metabolite) in plasma did not change.

The clearance of docetaxel in combination with cisplatin or carboplatin was similar to that observed with monotherapy with docetaxel.

The pharmacokinetic profile of cisplatin when it was administered immediately after intravenous infusion of docetaxel was similar to that observed with the administration of a single cisplatin.

There was no effect of docetaxel on the pharmacokinetics (C max , AUC) of the main metabolite capecitabine (5DFUR) and the effect of capecitabine on the pharmacokinetics (C max , AUC) of docetaxel.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be stored in a place protected from light, inaccessible to children at a temperature of 2 ° to 8 ° C.
Shelf life - 2 years.
The prepared infusion solution should be used for 4 hours (including one hour infusion) at room temperature and under normal light conditions.

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