Temodal - Instructions For The Use Of The Drug, Reviews, Price, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Temodal

Temodal: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Temodal

ATX code: L01AX03

Active ingredient: Temozolomide (Temozolomide)

Producer: Orion Pharma (Finland, Denmark), Schering-Plow Labo NV (Belgium, Germany)

Description and photo update: 2019-07-08

Prices in pharmacies: from 5945 rubles.

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Temodal is an antitumor and alkylating drug.

Release form and composition

• 5 mg capsules: opaque, with a green cap and a white body, size No. 3, with inscriptions in black ink: "5 mg" and the manufacturer's trademark on the body, TEMODAL on the cap;
• capsules 20 mg: opaque, with a yellow cap and a white body, size No. 2, with inscriptions in black ink: "20 mg" and the manufacturer's trademark - on the body, TEMODAL - on the cap;
• capsules 100 mg: opaque, with a pink lid and white body, size No. 1, with inscriptions in black ink: “100 mg” and the manufacturer's trademark on the body, TEMODAL on the lid;
• capsules 140 mg: opaque, with a blue cap and a white body, size No. 0, with inscriptions in black ink: "140 mg" and the manufacturer's trademark - on the body, TEMODAL - on the cap;
• capsules 180 mg: opaque, with a red-brown cap and a white body, size No. 0, with inscriptions in black ink: "180 mg" and the manufacturer's trademark - on the body, TEMODAL - on the cap;
• capsules 250 mg: opaque, with a white cap and a white body, size No. 0, with inscriptions in black ink: "250 mg" and the manufacturer's trademark - on the body, TEMODAL - on the cap;
• lyophilisate for preparation of solution for infusion: white with a pink tint, no mechanical inclusions (in colorless glass vials with a capacity of 100 ml, in a cardboard box 1 bottle).

The contents of all capsules are white to light yellow-brown or light pink powder.

The capsule packaging is standard and does not depend on the dosage: 5 pcs. or 20 pcs. in dark glass vials, in a cardboard box 1 bottle; 1 pc. in a sachet made of aluminum foil, in a cardboard box 5 or 20 sachets.

Composition for 1 capsule:

• active substance: temozolomide - 5 mg, 20 mg, 100 mg, 140 mg, 180 mg or 250 mg;
• excipients: tartaric acid, colloidal silicon dioxide, lactose, sodium carboxymethyl starch, stearic acid;
• capsule body and cap: sodium lauryl sulfate, gelatin, yellow iron oxide dye (for Temodal 5 mg, 20 mg and 180 mg), indigo carmine (for Temodal 5 mg and 140 mg), red iron oxide dye (for Temodal 100 mg and 180 mg), titanium dioxide;
• ink: black dye (ethanol, propylene glycol, butanol, aqueous ammonia, potassium hydroxide, shellac, black iron oxide dye, isopropanol, purified water).

Composition for 1 bottle with lyophilisate for preparation of solution for infusion:

• active substance: temozolomide - 100 mg;
• excipients: mannitol, polysorbate 80, sodium citrate dihydrate, concentrated hydrochloric acid, threonine.

Pharmacological properties

Pharmacodynamics

Temodal is an imidazotetrazine alkylating drug with an antitumor effect. When it enters the systemic circulation (subject to pH values in physiological norms), it quickly turns into an active compound - MTIK (monomethyltriazenoimidazolecarboxamide). The cytotoxic effect of MTIK is due to the alkylation of guanine at the O ⁶ position, as well as additional alkylation at the N ⁷ position. It is assumed that the resulting cytotoxic damage involves a mechanism of aberrant reduction of the methyl residue.

Pharmacokinetics

After oral administration, the drug is rapidly absorbed. It crosses the blood-brain barrier and is found in cerebrospinal fluid. The maximum plasma concentration of Temodal is reached in 0.5-1.5 hours after taking the drug. The half-life is approximately 1.8 hours. Plasma protein binding is insignificant (about 12-16% of Temodal binds to plasma proteins). The half-life, volume of distribution and clearance do not depend on the dose of the drug.

The main route of excretion of Temodal is through the kidneys with urine. With feces, about 0.8% of the drug is excreted within 7 days (this indicates complete absorption of Temodal). 24 hours after ingestion, approximately 5-10% of the dose taken is determined in the urine unchanged, the rest is excreted in the form of metabolites.

When the drug is taken simultaneously with food, the maximum plasma concentration decreases by 33% and the AUC indicator decreases by 9%.

Plasma clearance of Temodal does not depend on the patient's age, tobacco consumption or renal function. In patients with moderate and mild liver dysfunction, pharmacokinetic parameters do not differ from those in patients with normal liver function.

The AUC indicator in children is slightly higher than in adults, and the maximum tolerated dose of Temodal is the same for adult patients and children and is 1000 mg / m ² per therapy cycle.

Indications for use

• first detected glioblastoma multiforme (combined treatment with radiation therapy and further adjuvant monotherapy);
• malignant glioma that occurs during the progression or relapse of the disease after standard therapy (glioblastoma multiforme, anaplastic astrocytoma);
• malignant widespread melanoma with metastases (Temodal is a first-line drug).

Contraindications

• severe myelosuppression;
• syndrome of glucose-galactose malabsorption, deficiency of the enzyme lactase or galactose intolerance (for capsules);
• pregnancy;
• lactation period;
• children under 3 years of age (with recurrence or progression of malignant glioma);
• age up to 18 years (with malignant melanoma or glioblastoma multiforme, detected for the first time);
• increased individual sensitivity to any component of the drug and / or dacarbazine.

Temodal is prescribed with caution to patients with severe renal and / or hepatic insufficiency, as well as to persons over 70 years of age.

Instructions for use of Temodal: method and dosage

The capsules are intended for oral administration on an empty stomach. They should not be chewed or opened, but should be swallowed whole with a glass of water. A single dose of Temodal should contain the minimum possible number of capsules.

To prepare a solution for infusion, 41 ml of water for injection is added to a vial with a lyophilisate. The concentration of the active substance in the reconstituted solution is 2.5 mg / ml. The prepared solution for infusion is usable within 14 hours (including the time required for drug administration).

Temodal solution is intended for intravenous administration, the duration of the infusion is 90 minutes. An isotonic sodium chloride solution can be used as a secondary solvent. Temozolomide should not be mixed with dextrose solution.

In case of glioblastoma multiforme, detected for the first time, primary treatment with the drug is carried out in combination with radiation therapy. Temodal is prescribed at a dose of 75 mg / m2 ^of body surface. The drug is taken daily for 42 days. It is not recommended to reduce the dose, however, treatment may be intermittent, depending on the tolerability of temozolomide. Treatment can be resumed throughout the cycle, up to 49 days. To resume therapy, the following conditions must be met: the absolute number of neutrophils is not less than 1500 / μl, the number of platelets is not less than 100,000 / μl, the general criterion of toxicity is not higher than the 1st degree.

During the period of drug treatment, it is necessary to donate blood for analysis every week to count the number of cells. Based on the results obtained, the doctor reduces the Temodal dose or cancels it.

One month after the end of the combination therapy, the patient is prescribed adjuvant treatment, which includes six additional cycles:

• cycle 1 (duration 5 days): 150 mg / m ² per day, then a break for 23 days;
• cycle 2 (duration 5 days): 200 mg / m ² per day (increasing the dose to 200 mg / m ^{2 is} possible only if the absolute number of neutrophils is at least 1500 / μl, the number of platelets is at least 100,000 / μl, and the general criterion of toxicity is not higher than the 2nd degree); then a break for 23 days;
• cycles 3–6 (each duration is 5 days): 150 mg / m ² per day (if the dose in cycle 2 was not increased) or 200 mg / m ² per day (if the dose in cycle 2 was increased); after each cycle, a break of 23 days.

Periodic monitoring of the blood cell count is also required during adjuvant treatment. Taking into account the toxicity of the drug, the dose is adjusted or temporarily canceled by temozolomide.

In case of malignant glioma (recurrent or progressive) and metastatic widespread malignant melanoma in patients who have not received chemotherapy, Temodal is prescribed at a dose of 200 mg / m ². The drug is taken once a day for 5 days, followed by a break of 23 days, that is, the duration of one course is 28 days.

Patients undergoing chemotherapy previously prepared Temodal at an initial dose of 150 mg / m ² per day. In cycle 2, it is possible to increase the dose to 200 mg / m ² (if on the first day of cycle 2 the absolute number of neutrophils is at least 1500 / μl, and the number of platelets is at least 100,000 / μl).

Treatment is accompanied by a complete CBC on day 22, followed by weekly blood cell counts. If necessary, the dose of the drug is adjusted. Possible doses of temozolomide: the minimum recommended is 100 mg / m ², the standard therapeutic dose is 150 mg / m ² or 200 mg / m ².

The duration of drug treatment is up to 2 years (maximum). When the disease progresses, it is necessary to cancel temozolomide.

Side effects

Possible side effects in the treatment of first diagnosed glioblastoma multiforme (in adults):

• cardiovascular system: palpitations, edema (including peripheral), pulmonary embolism, hemorrhages, arterial hypertension, deep vein thrombosis, cerebral hemorrhage;
• respiratory system: nasal congestion, upper respiratory tract infections, cough, sinusitis, bronchitis, pneumonia, shortness of breath;
• gastrointestinal tract: constipation, abdominal pain, bloating, diarrhea, dyspepsia, gastroenteritis, fecal incontinence, increased liver enzyme activity, nausea, dry mouth, vomiting, taste disturbances, stomatitis, dental diseases, discoloration of the tongue, dysphagia, anorexia, hemorrhoids;
• hematopoietic system: neutropenia, anemia, leukopenia, thrombocytopenia;
• endocrine system: hypercortisolism;
• sense organs: dry eyes, pain in the eye, blurred vision, blurred vision, diplopia, decreased visual acuity, limitation of visual fields, pain and ringing in the ears, hearing impairment (up to deafness), hyperacusis;
• nervous system: insomnia or drowsiness, behavioral disorders, headache, amnesia, dizziness, depression, neurological disorders, seizures, impaired concentration, memory impairment, decreased and confused consciousness, apathy, thirst, olfactory hallucinations, anxiety, tremors, muscle weakness in one half body, balance disorders, speech disorders, paresthesias, hypersensitivity, hallucinations, neuropathy, impaired perception, emotional lability, extrapyramidal disorders, gait disorders, status epilepticus;
• musculoskeletal system: back pain, muscle and joint pain, myopathy, musculoskeletal pain, muscle weakness;
• skin and subcutaneous tissue: alopecia, dermatitis, pruritus, petechiae, increased sweating, erythema, rash, facial edema, exfoliation, dry skin, pigmentation disorders, photosensitivity, pain in the mammary gland;
• reproductive system: vaginitis, menorrhagia, amenorrhea, vaginal bleeding, impotence;
• urinary system: dysuria, frequent urination, urinary incontinence;
• laboratory tests: myelosuppression;
• metabolism: hyperglycemia, hypokalemia, increase or decrease in body weight;
• resistance to infectious diseases: herpes simplex virus, flu-like symptoms, oral candidiasis, pharyngitis, shingles, wound infection;
• general reactions: fever, hot flashes, pain syndrome, allergic reactions, chills, fatigue, radiation damage, asthenia, deterioration.

Possible side effects in the treatment of malignant glioma (progressive or recurrent) and malignant melanoma:

• gastrointestinal tract: nausea, vomiting, taste perversion, anorexia, diarrhea or constipation, dyspeptic disorders, abdominal pain;
• hematopoietic system: anemia, neutropenia, leukopenia, thrombocytopenia, lymphopenia, pancytopenia;
• nervous system: headache, paresthesia, drowsiness, dizziness, asthenia;
• skin and subcutaneous tissue: rash, exanthema, erythroderma, pruritus, alopecia, petechiae, urticaria, erythema multiforme, toxic epidermal necrolysis;
• general reactions: fever, general malaise, shortness of breath, chills, increased fatigue, opportunistic infections, weight loss, allergic reactions; very rarely - prolonged pancytopenia, secondary malignant processes, myelodysplastic syndrome, irreversible infertility.

Overdose

When the drug is used in doses of 500, 750, 1000 and 1250 mg / m ² (these are the total doses that patients receive in one 5-day cycle), the dose-limiting toxicity is hematological toxicity. It is observed when taking any dose, but is especially pronounced when using Temodal in high doses.

There is information about an overdose case (when taking the drug at a dose of 2000 mg per day for 5 days), which caused the development of pyrexia, pancytopenia, multiple organ failure and death. When Temodal was taken for more than 5 days (up to 64 days), hematopoiesis suppression was also noted, sometimes complicated by infection, and in some cases severe and prolonged, with a fatal outcome.

The antidote to Temodal is unknown. It is recommended to carry out regular monitoring of hematological parameters, and, if necessary, prescribe symptomatic treatment.

special instructions

When treating glioblastoma multiforme diagnosed for the first time, it is recommended to carry out antiemetic therapy (preferably before the start of combined treatment and strongly - during adjuvant treatment). Antiemetics can be taken before and after taking Temodal.

In patients receiving combined treatment with radiation therapy, prophylactic treatment is recommended against the pathogen Pneumocystis carinii, which causes pneumonia.

Avoid getting the lyophilisate or the contents of the capsule on the mucous membranes and skin, otherwise it is necessary to rinse the areas that have gotten the drug with plenty of water.

During treatment, care should be taken when driving vehicles and performing other potentially dangerous work, since some side effects (dizziness, fatigue, drowsiness, etc.) can negatively affect the speed of psychomotor reactions and concentration.

Application during pregnancy and lactation

The drug is contraindicated during pregnancy and lactation.

Women and men of reproductive age while taking Temodal and for at least 6 months after the end of therapy should use reliable methods of contraception.

During treatment with the drug, the development of irreversible infertility is possible, therefore, male patients before prescribing Temodal should discuss the possibility of cryopreservation of semen with a doctor.

Pediatric use

The drug is contraindicated in children under 3 years of age in the treatment of progressive or recurrent glioma and in children and adolescents under 18 years of age with malignant melanoma or newly diagnosed glioblastoma multiforme.

With impaired renal function

Temodal is prescribed with caution to patients with severe renal impairment.

For violations of liver function

Temodal is prescribed with caution to patients with severe liver dysfunction.

Use in the elderly

According to the instructions, Temodal is prescribed with caution to patients aged 70 and over.

Drug interactions

With simultaneous use with valproic acid, a mild, but clinically significant decrease in the clearance of temozolomide occurs.

Phenytoin, phenobarbital, dexamethasone, carbamazepine, prochlorperazine, histamine H ₂ receptor blockers and ondansetron do not alter the clearance of temozolomide.

When used together with other drugs that depress the bone marrow, the risk of developing myelosuppression increases.

Analogs

Temodal's analogues are: Astroglyph, Temomid, Temozolomid, Temozolomid-Rus, Temozolomid-Teva, Temtsital.

Terms and conditions of storage

Store at a temperature of + 2 … +30 ° C (capsules) or + 2 … +8 ° C (lyophilisate for preparation of solution for infusion). Keep out of the reach of children.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Temodal

On medical forums and portals, reviews about Temodal are often found. Patients describe the drug as an expensive but very effective drug that rarely causes side effects. An exception is nausea and headache, which are observed in almost every third patient taking temozolomide.

Price for Temodal in pharmacies

The cost of the drug is quite high and varies greatly depending on the form of release and dosage. Average prices for Temodal today:

• capsules 100 mg (5 pcs. in a sachet or glass bottle) - 6460-6536 rubles;
• capsules 140 mg (5 pcs. in a sachet or glass bottle) - 12 942-12 999 rubles;
• capsules 180 mg (5 pcs. in a sachet or glass bottle) - 16 860–20 500 rubles;
• capsules 250 mg (5 pieces in a sachet or glass bottle) - 46,000 rubles;
• lyophilisate for the preparation of a solution for infusion 100 mg - 9,000 rubles.

Temodal: prices in online pharmacies

Drug name Price Pharmacy

Temodal 100 mg capsules 5 pcs. 5945 RUB Buy

Temodal 100 mg capsules 5 pcs. RUB 6148 Buy

Temodal 100 mg lyophilisate for preparation of solution for infusion 1 pc. RUB 11359 Buy

Temodal 140 mg capsules 5 pcs. RUB 11,999 Buy

Temodal 140 mg capsules 5 pcs. 12500 RUB Buy

Temodal 180 mg capsules 5 pcs. RUB 15949 Buy

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!