Temodal

Темодал Drug photo

The description is actual on 04.12.2014

  • Latin name: Temodal
  • ATH code: L01AX03
  • Active ingredient: Temozolomid (Temozolomide)
  • Producer: Orion Pharma (Finland, Denmark), Schering-Plough Labo N.V. (Belgium, Germany)

Structure

1 capsule contains 5, 20, 100, 140, 180 or 250 mg of active ingredient – a temozolomid.

As excipients use: anhydrous lactose, silicon dioxide colloid, tartaric and stearic acid and carboxymethylstarch of sodium.

Release form

This medicine is made in the form of solid gelatinous capsules which body has white color. Capsules are absolutely opaque. In capsules powder of light color contains (the shade can vary from absolutely white to slightly greenish and slightly pinkish).

Capsules have a firm gelatinous cover at which there is "lid" of a saturated blue shade. On a surface of capsules there are two strips located in parallel to each other and also marking SP and level of maintenance of a temozolomid. For example, capsules of 180 mg have marking of "180 mg", capsules of 250 mg — "250 mg", etc. The name of drug is applied on a lid.

Medicine Temodal is made in the following forms:

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

Pharmacological action

Drug Temodal makes antineoplastic impact.

After hit of active agent in a system blood stream, at physiological value rn is exposed to fast not euzymatic conversion – transformation to active connection of a monometiltriazenoimidazolkarboksamid (MTIK). Cytotoxicity of MTIK as believe, is caused by process of alkylation of DNA.

Alkylation (methylation) of guanine, in turn, happens generally in the situation O 6 and N 7. Apparently, cytotoxic damages which arise as a result of this process work as the activator of recovery reaction of the methyl rest.

Pharmacodynamics and Pharmacokinetics

Absorption

Temozolomid (Temozolomide) is quickly and completely soaked up and peak concentration of plasma is reached on average 60 minutes later. The food reduces the speed and extent of absorption of a temozolomid. Average peak concentration in plasma decreased by 32% and time of effect of active agent increases twice (from 1 to 2:25 o'clock). It occurs when drug is accepted right after the big breakfast consisting of fat, carbonaceous products.

Distribution

Temozolomid is distributed with an average capacity of 0,4 l/kg (% of CV = 13%). With proteins of plasma of the person it is connected very poorly. The average percent of the general radioactivity makes 15%.

Metabolism

Temozolomid's hydrolyzation occurs spontaneously at physiological value rn to active types, a monometiltriazenoimidazolkarboksamid (MTIK) and a temozolomid of acid of a metabolite. MTIK is hydrolyzed further to a 5-amino-imidazole-4-karboksamida (agrarian and industrial complex) which, as we know, is an intermediate element in biosynthesis of purine and nucleic acids, and a methylhydrazine. P450 cytochrome enzymes in a metabolism temozolomidy and MTIK are of little importance. In relation to PPK of a temozolomid, influence of MTIC and agrarian and industrial complex makes 2,4% and 23%, respectively.

Removal

About 38% of the entered temozolomid of the general radioactive dose are removed within 7 days: 37,7% with urine and 0,8% with a stake.

Time of removal of active agent from plasma makes slightly less than 2 hours. Generally drug is removed through kidneys. Days later from the moment of administration of drug about 10% of substance are removed with urine. Substance can be removed from an organism and in the form of polar metabolites which are not subject to identification. The clearance and T1/2 does not depend on norm of reception.

Indications to use

Means is appointed for treatment of the following diseases:

  • The Multiformny glioblastoma revealed for the first time. In this case it is necessary to use drug in a complex with radiation therapy, with need of carrying out the supporting treatment.
  • Malignant glioma. Drug Temodal is appointed for treatment of the specified diseases at recurrence or in case of progressing of a disease even after use of standard therapeutic measures.
  • Melanoma in the form of the widespread metastasizing malignant tumor. Drug is appointed as the main treatment.

Contraindications

Medicine Temodal is contraindicated to use to patients who have the increased hypersensitivity to active agent or one of the elements making its basis.

Hypersensitivity is expressed in the form of, for example, small tortoiseshell, allergic reactions, including an anaphylaxis and other displays of an allergy.

Besides drug is not recommended to be used for treatment of the patients having hypersensitivity to a dakarbazin (DTIC) because the metabolization occurs in 5 (3-methyltriazen-1-silt) of imidazole-4-karboksamid (MTIK).

Pregnancy, the period of feeding of the newborn and children's age are also included into the list of contraindications to administration of drug.

Side effects

As well as manifestation of side effects can provoke all drugs of this group, Temodal's reception. Among the most frequent — nausea, vomiting, appetite loss, a lock, fatigue, weakness and a headache.

Nausea and vomiting can be very serious. Drug treatment can become necessary to prevent or facilitate nausea and vomiting. Changes in a food allowance and way of life can help to reduce some of these effects. If any of these side effects remain or worsen, it is necessary to inform the doctor or the druggist quickly.

More rare, administration of drug provokes temporary loss of hair. Normal growth of hair has to return after the end of treatment.

Temodal can provoke manifestation of very rare, but not less serious side reactions, such as ulcers in oral cavities, hypostasis of anklebones or legs, slight bleeding or bruises, the complicated breath. This drug can reduce ability of an organism to resist to influence of infections.

In spite of the fact that temozolomid it is used for a cancer therapy, very seldom at some patients it can increase risk of development of other form of cancer (for example, a marrow cancer).

When swelling glands, inexplicable or sudden loss of weight, strong sweating during administration of drug, it is necessary to see the attending physician immediately.

Serious allergic reactions to this drug are shown extremely seldom, but nevertheless they are possible. Serious reactions are shown in the form of the following symptoms: rash, itch, hypostasis (especially persons, language, throats), severe dizziness, trouble breathing.

Application instruction of Temodal

The instruction on Temodal possesses certain specifics therefore it is given in detail.

Drug accept in portion 75 mg/sq.m for 42 days once a day with carrying out the accompanying actions of radiation therapy (on a total dose of 60 Gr enter into 30 fractions).

Interruption of administration of drug is not recommended, but can be in rare instances appointed the doctor (at manifestation of stable side reactions). In case of interruption of reception of Temodal it is necessary to resume treatment during the 42-day accompanying period, but the period can drag on for 49 days if all following conditions are met:

  • the absolute number of neutrophils are more or is equal 1,5 × 109/l, it is more thrombocytes or equally 100 × 109/l;
  • the general criterion of toxicity is less or is equal 1 (an exception the alopecia, nausea and vomiting can make).

In the course of implementation of therapeutic actions with use of this drug blood test needs to be carried out regularly. Carrying out frequency — once a week. Treatment by drug has to be interrupted or stopped according to criteria of toxicity from the list 1.

List 1: Dosing of suspension or termination of administration of drug

  • if toxicity of AChN is more or equally 0,5 and less than 1,5 × 109/l, administration of drug needs to be interrupted;
  • if toxicity less than 0,5 × 109/l, administration of drug need to be stopped;
  • if the level of maintenance of thrombocytes exceeds or is equal 10 and less, than 100 × 109/l, administration of drug needs to be interrupted;
  • if the level of maintenance of thrombocytes is less, than 10 × 109/l, Temodal's reception should be interrupted;
  • if CTC of not hematologic toxicity (nausea, vomiting and an alopecia are an exception) at the second level, administration of drug has to be interrupted;
  • if CTC of not hematologic toxicity (nausea, vomiting and an alopecia are an exception) at the level of 3 and 4, it is impossible to accept drug further.

Note: the abbreviation of AChN means absolute number of neutrophils (further to all lists of the section).

Cycle 1

When the first stage comes to the end, one month of Temodal later + RT drug is appointed during additional 6 cycles of a maintenance therapy. The dosage in a cycle 1 makes 150 mg/sq.m daily within 5 days then for 23 days treatment stops.

Cycles 2-6

At the beginning of a cycle 2 it is possible to increase amount of the accepted active agent to 200 mg/sq.m if not hematologic toxicity of STS for a cycle 1 is less or it is equal 2, the absolute quantity of neutrophils exceeds or is equal 1,5 × 109/l, and the level of maintenance of thrombocytes exceeds or 100 × 109/l is equal. The portion of 200 mg/sq.m a day is appointed to reception for 5 days of each subsequent cycle. If the portion was not increased on the 2nd cycle, it is not necessary to do it also in the subsequent cycles.

In the period of the second phase lowering of norm of administration of drug has to be applied in compliance about lists 2 and 3.
During reception of medicine in three weeks from the moment of the first dose of Temodal it is necessary to make an integrated analysis of blood.

List 2: Levels of a temozolomid for a maintenance therapy

  • if the level of a dose-1, a portion of 100 (mg/sq.m/day), decrease in preliminary toxicity is necessary;
  • if the level of a dose 0, a portion of 150 (mg/sq.m/day) are a norm in the first cycle of treatment;
  • if the level of a dose 1, a portion of 200 (mg/sq.m/day) are a norm in 2-6 cycle of treatment in the absence of toxicity.

List 3: reduction or the termination during a maintenance therapy

  • if toxicity AChN less than 1.0 x 109/l, drug intake it is necessary to reduce TMZ by 1 level of a dose;
  • drug intake should be stopped in need of a dose decline;
  • if the level of maintenance of thrombocytes less, than 100 × 109/l, drug intake it is necessary to reduce TMZ by 1 level of a dose;
  • if CTC of not hematologic toxicity (nausea, vomiting and an alopecia are an exception) at the third level, it is necessary to reduce TMZ by 1 level of a dose;
  • if CTC of not hematologic toxicity (nausea, vomiting and an alopecia are an exception) at the level of 4, it is impossible to accept drug further.

Overdose

Doses 500, 750, 1000 and 1250 mg/sq.m (the general portion for a cycle in five days) were estimated on patients. Portion of restriction of toxicity was a hematologic toxicity noted at reception of any dose of drug. Therefore, the portion of the accepted drug is higher, the level of hematologic toxicity is more.

Overdose was noted at reception by the patient of drug in number of 2000 mg a day. Duration of reception made five days. In this case at the patient such side reactions as a pancytopenia, a hyperthermia, insufficiency of many internals and death were noted. There is information on patients to whom drug was appointed to inclusion in the period more than 5 days (about two months), manifestation of such side effects as oppression of marrow and death turned out to be consequence of what.

Interaction with other medicines

Degree of absorbability of drug is not influenced by its joint reception with Ranitidine. The clearance of a temozolamid does not change at a concomitant use of Dexamethasone, Prochlorperazine, Phenytoinum, Carbamazepine, Ondansetrona, blockers of histamine H2 receptors or phenobarbital.

Decrease in clearance of active agent of drug Temodal is observed at a concomitant use with valproic acid. Decrease in clearance at the same time has slight value.

Temodal's reception with the drugs containing the substances making the oppressing impact on marrow increases probability of a miyelosupressiya.

Terms of sale

Drug in all forms of release is released in a drugstore only according to the recipe of the doctor.

Storage conditions

Temodal it is necessary to store in the dry place at a temperature not below 2 and not above the 30th degree Celsius.

Period of validity

Till 2 flyings.

Temodal's analogs

Coincidence on the ATH code of the 4th level:

The following medicines belong to Temodal's analogs:

  • Temozolomid
  • Temozolomid-Rus
  • Temozolomid-Teva
  • Temomid
  • Temtsital

About Temodale

There is a lot of reviews of Temodala, but all of them as a rule meet to the fact that drug has effective effect and does not cause side reactions in most of patients. An exception is the headache and nausea – it side effects are observed at every 3rd patient accepting this drug.

Zdravzona

  • Temodal of 20 mg No. 5 kapsulyschering-Plough
  • Temodal of 250 mg No. 5 kapsulyschering-Plough
  • Temodal of 100 mg No. 5 kapsulyschering-Plough
  • Temodal lyophilisate for solution 100 of mg No. 1 flakonschering-Plough
  • Temodal of 140 mg No. 5 kapsulyschering-Plough
to show still

Apteka24

  • Temodal kaps. 140 mg No. to a 5shering-Pla (Italy-USA)
  • Temodal kaps. 20 mg No. 5
  • Temodal kaps. 180 mg No. to a 5shering-Pla (Italy-USA)
  • Temodal kaps. 250 mg of a sachet No. to a 5shering-Pla (Italy-USA)
Section: Antineoplastic
in more detail

Education: East Kazakhstan state university of S. Amanzholov, Ust-Kamenogorsk. Specialty "Valueology".

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