Generic
Temozolomide Hydrochloride
5 brands available in the market
At a glance
Temozolomide Hydrochloride is an anti-cancer drug used for glioblastoma multiforme, anaplastic astrocytoma, and metastatic melanoma. It inhibits cell division by alkylating DNA in cancer cells.
Description
Temozolomide is a triazene compound that is an inactive prodrug. It is chemically hydrolyzed to MTIC (3-methyl-(triazen-1-yl)imidazole-4-carboxamide), the active metabolite of dacarbazine. MTIC alkylates DNA at the O6 and N7 positions of guanine, causing cytotoxicity and inhibiting cancer cell growth and proliferation.
Indications
- Glioblastoma multiforme (adults) – with focal radiotherapy
- Anaplastic astrocytoma (recurrent or progressive)
- Metastatic melanoma
Therapeutic class
Cytotoxic Chemotherapy
Pharmacological class
Alkylating Agent
Pharmacology
Temozolomide is an inactive prodrug that hydrolyzes at physiological pH to the active metabolite MTIC. MTIC alkylates DNA at O6 and N7 positions of guanine, causing DNA cross-linking and strand breaks, which arrests the cell cycle and induces apoptosis in cancer cells.
Mechanism of action
Inhibits cell division by alkylating DNA in cancer cells.
Dosage
Adult Dose (Oral):
- Glioblastoma (concomitant): 75 mg/m²/day (42 days) + radiotherapy
- Glioblastoma (adjuvant): 150-200 mg/m²/day (5 days) – 23 days break (6 cycles)
- Recurrent/progressive glioma (chemotherapy-naive): 200 mg/m²/day (5 days) – 23 days break
- Recurrent/progressive glioma (prior chemo): 150 mg/m²/day (5 days) – 23 days break; increase to 200 mg/m² for cycle 2
- Metastatic melanoma: 200 mg/m²/day (5 days) – every 28 days
Administration
- Take on an empty stomach (1 hour before meals)
- Swallow capsule whole; do not chew, crush, or break
- Take at the same time each day
Missed dose
If you miss a dose, take it as soon as you remember; if almost time for the next dose, skip it; do not double the dose.
Side effects
Common Side Effects:
- Nausea, vomiting, constipation
- Headache, fatigue, weakness
- Diarrhea, dizziness, fever
- Hair loss, loss of appetite, insomnia
- Rash, viral infection
Serious:
- Myelosuppression (neutropenia, thrombocytopenia)
- Opportunistic infections (PCP)
- Secondary leukemia
Precautions & warnings
- Highly unsafe in pregnancy (Category D)
- Do not use in severe myelosuppression
- Risk of infection; avoid contact with sick individuals
- Regular blood tests (CBC, liver, kidney function) required
- Both males and females should use effective contraception (during treatment and 6 months after)
Contraindications
- Hypersensitivity to dacarbazine
- Severe myelosuppression
- Pregnancy
Drug interactions
- Valproic acid: Decreased temozolomide clearance
- Other myelosuppressive agents: Additive myelosuppression
Food interactions
It is not known whether alcohol is safe with Temozolomide Hydrochloride; consult your doctor.
Use in pregnancy
Use in Pregnancy: Highly unsafe (Category D); evidence of fetal risk; use only in life-threatening situations; consult your doctor.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Highly unsafe; drug may cause toxicity to the baby; do not use; consult your doctor.
Pediatric use
Indicated for children >3 years (recurrent/progressive glioma)
Geriatric use
Caution required in elderly patients
Renal / hepatic impairment
Renal Impairment: Safe in kidney disease; dose adjustment may not be needed; caution in severe kidney disease; consult your doctor.
Hepatic Impairment: Mild-moderate: no dose adjustment; severe: caution; consult your doctor.
Overdose effects
Overdose may cause myelosuppression; no specific antidote; provide supportive care; hemodialysis is not effective.
Storage conditions
Store in a cool and dry place, protected from light; keep out of reach of children.
Chemical structure
Temozolomide