Temodal替莫唑胺 temozolomide泰道

[Function and indication] This product is used to treat: newly diagnosed glioblastoma multiforme, initially combined with radiotherapy, and then as adjuvant therapy; recurrent or progressive glioblastoma multiforme or anaplastic astrocytoma after conventional treatment.

[Model and specification] 100mg, 5 tablets

[Usage and dosage] Adult patients with newly diagnosed glioblastoma multiforme:
Concurrent chemoradiotherapy period: Oral administration of this product, 75 mg/m2/day, for 42 days, and radiotherapy at the same time. Then receive 6 cycles of adjuvant therapy with this product. The drug can be suspended according to the patient’s tolerance, but there is no need to reduce the dose.
Adjuvant therapy period: 4 weeks after the end of the synchronous chemoradiotherapy period, 6 cycles of this product monotherapy are performed. Starting dose: 150 mg/m2/day, for 5 days, and then stop for 23 days. One cycle is 28 days. Starting from the second cycle, the dose can be increased to 200 mg/m2/day, or reduced to 100 mg/m2, depending on the adverse reactions in the previous cycle.
Patients with glioblastoma multiforme or anaplastic astrocytoma who have relapsed or progressed after conventional treatment:
Adult patients: The starting dose for those who have previously received chemotherapy is 150 mg/m2/day for 5 days. The starting dose for adults who have not received other chemotherapy is 200 mg/m2/day, both for 5 consecutive days, 28 days as a cycle. Treatment can continue until the disease progresses, up to 2 years.
Pediatric patients:
For children aged 3 years or older who have previously received chemotherapy, the starting oral dose of this product is 150 mg/m2/day for 5 days in each 28-day cycle. If no toxicity occurs, the dose is increased to 200 mg/m2/day in the next cycle. Treatment can continue until the disease progresses, up to 2 years.
All patients:
This product should be taken on an empty stomach (at least one hour before meals). Antiemetics may be used before and after taking this product. If vomiting occurs after taking the medicine, the second dose cannot be taken on the same day.
This product cannot be opened or chewed, and should be swallowed whole with a glass of water. If the capsule is damaged, avoid contact between the skin or mucous membranes and the powdered contents of the capsule.

[Clinical Studies] At physiological pH, temozolomide spontaneously hydrolyzes into the active fragment MTIC and temozolomide acid metabolites. MTIC is further hydrolyzed into 5-amino-imidazole-4-amide (AIC) and methylhydrazine, the former is an intermediate in purine and nucleic acid biosynthesis, and the latter is considered to be an alkylated active fragment. Cytochrome P450 plays only a minor role in the metabolism of temozolomide and MTIC. Compared with the AUC of temozolomide, the exposure of MTIC and AIC was 2.4% and 23%, respectively. 7 days after administration, 38% of the total radioactive dose was recovered; 37.7% in urine and 0.8% in feces. Most of the radioactivity recovered in urine is unchanged temozolomide (5.6%), AIC (12%), temozolomide acid metabolites (2.3%) and unknown polar metabolites (17%). The overall clearance of temozolomide is about 5.5 L.h-1.m-2.

[Precautions] Prevention of Pneumocystis carinii pneumonia is required for patients receiving 42-49 days of combined treatment. Male patients should use contraception during treatment and within 6 months after the end of treatment, and sperm should be frozen before receiving this treatment. Use with caution in patients with severe liver or kidney dysfunction. This drug should not be used in breastfeeding women. There is currently no clinical experience of using this drug in children with glioblastoma multiforme under 3 years old.

[Adverse Reactions and Contraindications] Mild to moderate gastrointestinal dysfunction, which is self-limiting or easily controlled by standard antiemetics. Bone marrow suppression (usually on the 21st to 28th day of the first few cycles), usually recovers rapidly within 1-2 weeks. Other adverse reactions include: oral candidiasis, infection, abnormal blood count, weight loss, anxiety, depression, emotional instability, insomnia, headache, convulsion, dizziness and other neurological symptoms, visual impairment, hearing loss, tinnitus, lower limb edema, bleeding, deep vein thrombosis, cough, dyspnea, hair loss, dry skin, muscle weakness, urinary incontinence, fatigue, fever, pain, allergic reaction, radiation damage, abnormal taste, SGPT increase.

[Contraindications] Patients who are allergic to this drug or dacarbazine, pregnant women, and patients with severe bone marrow suppression are contraindicated.

[Pregnant women use] FDA pregnancy classification: D, there is clear evidence that the drug is harmful to the human fetus and should not be routinely used in pregnant women. If the drug must be used during pregnancy, the patient should be informed of the potential risks to the fetus. Women who may become pregnant should be discouraged from becoming pregnant while receiving temozolomide treatment or within 6 months after terminating temozolomide treatment.

[Pediatric Use] There is no clinical experience of using this drug in children with glioblastoma multiforme under 3 years old; for children with glioma over 3 years old, there is limited clinical experience of using this drug.

[Drug Interactions] When taking valproic acid at the same time, the clearance of temozolomide is slightly reduced. When used in combination with other drugs that can cause bone marrow suppression, bone marrow suppression may be aggravated.

[Manufacturer] NATCO, India