Temodal

Description overdue on 04/12/2014

• Latin name: Temodal
• ATC code: L01AX03
• Active substance: Temozolomide (Temozolomide)
• Manufacturer: Orion Pharma (Finland, Denmark), Schering-Plough Labo NV (Belgium, Germany)

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• Composition
• Product form
• Pharmacological action
• Pharmacodynamics and Pharmacokinetics
• Indications
• Contraindications
• Side effects
• Instructions for use Temodal
• Overdose
• Cooperation
• Terms of sale
• Storage conditions
• Shelf life
• Analogs
• Reviews
• Price, where to buy

Composition

In 1 capsule contains 5, 20, 100, 140, 180 or 250 mg of active substance - temozolomide .

As auxiliary substances are used: lactose anhydrous, colloidal silicon dioxide, tartaric acid and stearic acid, and sodium carboxymethyl starch.

Product form

The medicament is in the form of hard gelatin capsules, the housing of which is white. Capsules completely opaque. Inside the capsule contains powder light color (hue can vary from pure white to slightly greenish and slightly pinkish).

Capsules are hard gelatin shell, which includes a "cap" saturated shade of blue. On the surface of the capsules themselves have two strips that are parallel to each other, as well as marking SP and the level of temozolomide. For example, capsules of 180 mg are marked "180 mg" capsules 250 mg - "250 mg" etc. In the name of the drug coated cap.

Medicament Temodal produced in the following forms:

• 5 mg capsules, № 5, № 20;
• 20 mg capsules, № 5, № 20;
• 100 mg capsules, № 5, № 20;
• 140 mg capsules, № 5, № 20;
• 180 mg capsules, № 5, № 20;
• 250 mg capsules, № 5, № 20;
• lyophilisate for solution for infusion 100 mg.

Pharmacological action

The drug has Temodal antitumor effects .

After entering the active agent into the systemic circulation, at physiological pH undergoes rapid nonenzymatic conversion   - Conversion to the active compound monometiltriazenoimidazolkarboksamid (MTIK). Cytotoxicity MTIK is believed to be caused by the process of alkylation of DNA.

Alkylation (methylation) guanine In turn, it occurs mainly in the position O 6 N 7. Apparently, cytotoxic damage that arise as a consequence of the process to act as a redox reaction promoter methyl residue.

Pharmacodynamics and Pharmacokinetics

Absorption:

Temozolomide (Temozolomide) is rapidly and completely absorbed and peak plasma concentrations are achieved on average after 60 minutes. Food decreases the rate and extent of absorption of temozolomide. Mean peak plasma concentration decreased by 32% and the effect of the active substance is increased by 2 times (from 1 to 2.25 hours). This occurs when the drug is taken immediately after a hearty breakfast consisting of fatty, carbonaceous products.

Allocation:

Temozolomide volume distributed mean 0, 4 L / kg (% CV = 13%). With human plasma proteins very weakly connected. The mean percentage of total radioactivity is 15%.

Metabolism and excretion:

Temozolomide occurs spontaneously hydrolyzed at physiological pH to the active species monometiltriazenoimidazolkarboksamid (MTIK) and Temozolomide acid metabolite. MTIK further hydrolyzed to 5-amino-imidazole-4-carboxamide (APC), which is known, it is an intermediate element in the biosynthesis of purines and nucleic acids, and methylhydrazine. Cytochrome P450 enzymes in the metabolism of temozolomide and MTIK play a minor role. With respect to the AUC of temozolomide and MTIC impact APC is 2, 4% and 23%, respectively.

Withdrawal:

About 38% of the total radioactivity administered temozolomide dose excreted within 7 days: 37, 7% of the urine, and 0 to 8% in the faeces.

Withdrawal times the active substance from the plasma is less than 2 hours. Basically, the drug eliminated via the kidneys. After a day after taking the drug for about 10% of the substance is excreted in urine. The substance can be withdrawn from the body in the form of polar metabolites that can not be identified. Clearance and T1 / 2 of the norm does not depend on the reception.

Indications

Means prescribed for the treatment of the following diseases:

• Glioblastoma multiforme   It revealed for the first time. In this case, the drug must be used in combination with radiation therapy, with the necessity of maintenance treatment.
• Malignant glioma . The drug Temodal is indicated for the treatment of the disease at relapse, or in the case of disease progression even after the application of standard therapeutic measures.
• Melanoma   in the form of widespread metastatic cancer. The drug is given as a primary treatment.

Contraindications

Medicament Temodal contraindicated for use in patients who have an increased hypersensitivity to the active substance or one of the elements constituting its framework.

Hypersensitivity is expressed in the form of, for example, hives , Allergic reactions, including anaphylaxis   and other manifestations of allergy.

In addition, the drug is not recommended for the treatment of patients with increased sensitivity to dacarbazine (DTIC) Because it occurs in the metabolization of 5- (3-methyltriazen-1-yl) imidazole-4-carboxamide (MTIK).

Gestation The period of feeding the baby and children's age are also included in the list of contraindications to the drug.

Side effects

As with all drugs of this group, receiving Temodal can cause side effects manifestation. Among the most common - nausea . vomiting . loss of appetite . constipation . fatigue . weakness   and headache .

Nausea and vomiting can be severe. Drug treatment may be necessary to prevent or alleviate nausea and vomiting. Changes in diet and lifestyle can help reduce some of these effects. If any of these side effects persist or worsen, you need to quickly notify your doctor or pharmacist.

Less often, the drug triggers temporary hair loss . Normal hair growth should return after treatment.

Temodal can cause a manifestation of the very rare, but no less serious side effects, such as oral ulcers . swelling of the ankles or feet . light bleeding   or bruising . labored breathing . This drug may reduce the body's ability to withstand infections.

Although temozolomide   It is used to treat cancer Very rarely in some patients it may increase the risk of developing other forms of cancer (eg, cancer of the bone marrow ).

With swollen glands , Unexplained or sudden weight loss . heavy sweating   during treatment, you must immediately contact your doctor.

A serious allergic reaction to this drug is very rare, but they are possible. Serious reactions occur in the following symptoms: rash .   itch . edema (especially of the face, tongue, throat) severe dizziness , Trouble breathing.

Instructions for use Temodal

Instructions on Temodal has certain characteristics, so please give details.

The drug is taken in the dose of 75 mg / m ²   once a day for 42 days to conduct related activities radiation therapy   (for a total dose of 60 Gy administered in 30 fractions).

Interruption of the drug is not recommended, but in rare cases can be assigned a doctor (at a stable manifestation of adverse reactions). In the case of discontinuation of Temodal treatment should be resumed within the 42-day concomitant period, but the period may be delayed for 49 days if all the following conditions:

• absolute number neutrophil   greater than or equal to 1, 5 × 10 ⁹ / l Platelet   greater than or equal to 100 × 10 ⁹ / L;
• general criterion of toxicity is less than or equal to 1 (an exception may be alopecia . nausea   and vomiting ).

In carrying out therapeutic measures using this drug blood test   should be carried out regularly. Frequency - once a week. Drug treatment should be interrupted or discontinued in accordance with the criteria of toxicity from the list 1.

List 1: Dosage of suspension or discontinuation

• toxicity if ANC is greater than or equal to 0 and less than 5 1, 5 × 10 ⁹ / l, the drug should be interrupted;
• If toxicity than 0, 5 × 10 ⁹ / l, the drug should be stopped;
• If the platelet count is greater than or equal to 10 and less than 100 × 10 ⁹ / l, the drug should be interrupted;
• If the platelet count is less than 10 × 10 ⁹ / l, it is necessary to interrupt the receiving Temodal;
• If CTC hematological toxicity (nausea, vomiting and alopecia are the exception) on the second level, the drug should be interrupted;
• If CTC hematological toxicity (nausea, vomiting and alopecia are the exception) at 3 and 4, can not continue to take the drug.

Note: The abbreviation means ANC absolute neutrophil count   (hereinafter referred to all the lists in this section).

Cycle 1

When it completed the first phase, after one month Temodal + RT   drug is given for an additional 6 cycles of maintenance treatment. Dosage in one cycle is 150 mg / m ²   daily for 5 days, after which a 23 days treatment is stopped.

Cycles 2-6

At the beginning of cycle 2 can increase the number of the received active substance up to 200 mg / m ² If nonhematologic toxicity for cycle 1 STS is less than or equal to 2, the absolute neutrophil count is greater than or equal to 1 × 10 5 ⁹ / L and platelet levels greater than or equal to 100 × 10 ⁹ / l. Portion of 200 mg / m ²   day assigned to receive during the 5 days of each subsequent cycle. If no portion was increased to 2 cycle, this should not be done in subsequent cycles.

During the second phase of the fall in the rate of the drug should be used according to Schedule 2 and 3.
During the period of drug administration in three weeks after the first dose of Temodal need to do a complete blood count.

List 2: Levels of temozolomide maintenance therapy

• If dose level 1, a portion of 100 (mg / m ² / Day), you need to decrease the pre toxicity;
• If dose level 0, portion 150 (mg / m ² / Day) - this is the norm in the first cycle of treatment;
• If dose level 1, a portion of 200 (mg / m ² / Day) - this is the norm in the 2-6 cycle of treatment in the absence of toxicity.

List 3: reduction or discontinuation during maintenance therapy

• If toxicity ANC less than 1.0 x 10 ⁹ / L, the drug is necessary to reduce the TMP at 1 dose level;
• the medication should be stopped, if necessary, dose reduction;
• If the platelet count less than 100 × 10 ⁹ / l, the medication should be reduced TMZ by 1 dose level;
• If CTC hematological toxicity (nausea, vomiting and alopecia are the exception) on the third level, it is necessary to reduce inventories by 1 dose level;
• If CTC hematological toxicity (nausea, vomiting and alopecia are the exception) at level 4, you can not continue to take the drug.

Overdose

Doses of 500, 750, 1000 and 1250 mg / m ²   (total batch cycle for five days) was evaluated for patients. Portia limiting toxicity was hematologic toxicity observed at any dose received. Therefore, the higher portion of taking the drug, the greater the level of hematologic toxicity.

Overdosing the patient noted when taking the drug in an amount of 2000 mg per day. Course duration was five days. In this case, the patient experiences side effects, such as pancytopenia . hyperthermia , Lack many of the internal organs, and death. There are reports of patients who the drug was assigned to receive during the period of more than 5 days (two months), which resulted in the manifestation of side effects such as bone marrow depression   and death.

Interaction with other drugs

The degree of absorbability of the drug does not affect his joint appointment with Ranitidine . Clearance Temozolomide   It does not change while taking Dexamethasone, prochlorperazine, phenytoin, carbamazepine, ondansetron histamine H2-receptor   or phenobarbital .

Reduced clearance of the active substance of the drug Temodal is observed while taking a valproic acid . Reduced clearance in this case is the value of a weakly expressed.

Admission Temodal with preparations containing substances having bone marrow suppressive action, increases the likelihood of mielosupression .

Terms of sale

The drug is in all forms of release is released only at the pharmacy on prescription.

Storage conditions

Temodal should be stored in a dry place at a temperature of not less than 2 and not more than 30 degrees Celsius.

Shelf life

Up to 2 years.

Analogs of Temodal

By Temodal analogs include drugs:

• Temozolomide
• Temozolomide-Rousse
• Temozolomide Teva-
• Temomid
• Temtsital

Reviews of Temodal

Reviews of Temodal a lot, but they all tend to converge to the fact that the drug has an effective action and does not cause adverse reactions in most patients. The exception is the headache and nausea - this is the side effects observed in every third patient taking this drug.

Price Temodal

Buy Temodal in drugstores of Moscow can be as low as 8640 to 66,671 rubles, depending on the dosage of the active substance and the form of the drug. The specialists do not recommend that patients who want to buy the drug to respond to classified ads in "selling", as in this case, there is no guarantee that the drug will be original and will help cope with the disease. Do not forget that the price of Temodal may not be below the manufacturer, so buy the drug should only be allowed in special pharmaceutical outlets (pharmacies).

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