temozolomide

Action and Spectrum

Action and spectrum: 

Temozolomide crosses the blood-brain barrier and is used for DNA alkylation, methylation, and cell cycle arrest. It is effective in treating GBM, anaplastic astrocytoma, melanoma, refractory solid tumors, and pediatric brain tumors. 

Drug Interaction

Adverse Reaction

Adverse drug reactions:   

Frequency Defined  

>10%  

Nausea (53%)  

Vomiting (42%)  

Alopecia (55-69%)  

Lymphopenia (55%)  

Headache (41%)  

Convulsions (23%)  

Thrombocytopenia (19%)  

Rash (8-19%)  

Fatigue (34%)  

Constipation (33%)  

Anorexia (9-27%)  

Hemiparesis (18%)  

Dizziness (12%)  

Peripheral edema (11%)  

Viral infections (11%)  

Diarrhea (16%)  

Neutropenia (14%)  

Fever (13%)  

Asthenia (13%)  

1-10%   

Amnesia (10%)  

Back pain (8%)  

Paresis (8%)  

Ataxia (8%)  

URI (8%)  

Abdominal pain (5-9%)  

Insomnia (10%)  

Urinary incontinence (8%)  

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindication/caution: 

Hypersentitive 

Pregnancy / Lactation

Pregnancy warnings:     

AU TGA pregnancy category: D 

US FDA pregnancy category: D 

Lactation: 

Excreted into human milk is Unknown 

Pregnancy Categories:       

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester.       
• Category B: No evidence shown of risk to the fetus found in animal reproduction studies, and there are not enough studies on pregnant women       
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a result in humans must take care of potential risks in pregnant women       
• Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.       
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.       
• Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

Temozolomide is an oral alkylating agent that methylates DNA at O6 and N7 positions which causing DNA damage and tumor cell apoptosis. 

Pharmacokinetics: 

Absorption 

It is well absorbed orally. 

Distribution 

Distributes widely into tissues. 

Metabolism 

Metabolized in liver by non-enzymatic conversion to MTIC. 

Excretion 

Drug is eliminated through urine is 20-30%. 

Adminstartion

Patient Information Leaflet

Patient Information Leaflet  

Generic Name: temozolomide 

Why do we use temozolomide? 

temozolomide is an alkylating agent which is used to treat Anaplastic Astrocytoma and Glioblastoma Multiforme