Temodar (temozolomide)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Temozolomide, a prodrug that is converted in vivo to a cytotoxic alkylating metabolite, is an alkylating antineoplastic agent.
Temozolomide, an imidazotetrazine derivative, is an antineoplastic agent. Temozolomide is a prodrug and has little, if any, pharmacologic activity until hydrolyzed in vivo to 5-(3-methyltriazen-1-yl)imidazole-4-carboxamide (MTIC). Following administration of temozolomide, the drug undergoes rapid, nonenzymatic hydrolysis at physiologic pH to MTIC.
MTIC is thought to exert its cytotoxic effects by acting as an alkylating agent at the O6 and N7 positions of guanine in DNA.
Temozolomide is rapidly and completely absorbed after oral administration, with nearly 100% bioavailability. Peak plasma concentrations usually are attained within 1 hour. The bioequivalence of temozolomide (with respect to both peak plasma concentration and AUC) administered orally or as an IV infusion over 90 minutes at a dosage of 150 mg/m2 has been demonstrated.
Food decreases the rate and extent of absorption after oral administration. A modified high fat breakfast decreased mean peak plasma temozolomide concentrations (32%) and AUC (9%).
Temozolomide efficiently crosses the blood brain barrier. It is not known if temozolomide is distributed into human milk. Plasma protein binding is approximately 15%.
MTIC, the main active metabolite, is further hydrolyzed to 5-amino-imidazole-4-carboxamide (AIC) and to methylhydrazine. CYP isoenzymes play only a minor role in metabolism of temozolomide and MTIC. About 38% of an administered dose is recovered over 7 days, principally in urine with <1% in feces.
The mean elimination half-life of temozolomide is 1.8 hours. Apparent half-lives for metabolites MTIC and AIC are 2.1 and 2.6 hours, respectively.
In patients with mild to moderate hepatic impairment, the pharmacokinetic profile resembles that in patients with normal hepatic function. Temozolomide has not been studied in patients with severe hepatic impairment. The pharmacokinetic profile of temozolomide is not affected by renal function in patients with creatinine clearance 36-130 mL/minute per m2.
The drug has not been studied in patients with severe renal impairment (creatinine clearance <36 mL/minute per m2) or in patients with end-stage renal disease receiving dialysis.
USES: This medication is used to treat certain types of brain cancer. Temozolomide belongs to a class of drugs known as alkylating agents. It works by slowing or stopping the growth of cancer cells.
Generic name: temozolomide
Pronunciation: (TEM-oh-ZOL-oh-mide)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Temodar
Indications
The following indications are listed for Temodar:
- Anaplastic Astrocytoma
- Glioblastoma Multiforme
Also known as: Grade Iii Astrocytoma, Grade Iv Astrocytoma, Malignant Astrocytoma.
Dosing
No dosing information is available for this tab.
No dosing information is available for this tab.
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Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*History of serious hypersensitivity reactions to temozolomide, any other ingredients in temozolomide, and dacarbazine, which is metabolized to the same active metabolite as temozolomide.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse reactions (>=20%) include: alopecia, fatigue, nausea, vomiting, headache, constipation, anorexia, and convulsions.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy in pediatric patients have not been established. Efficacy was not demonstrated in open-label studies of children 3-18 years of age receiving temozolomide mostly for CNS tumors. Similar toxicity was observed in pediatric patients and adults.
Temozolomide can cause fetal harm.
It is not known whether temozolomide or its metabolites are distributed in human milk. The effects of the drug on breast-fed infants or on the production of milk are also unknown. Patients should discontinue breast-feeding during therapy and for at least 1 week after the last dose because of potential risk, including myelosuppression, in breast-fed infants.
The manufacturer makes no specific recommendations regarding dosage adjustment in geriatric patients other than usual adjustment for ANC and platelet counts.
Experience in those 65 years of age and older with newly diagnosed glioblastoma is insufficient to determine whether they respond differently than younger adults.
An increased incidence of grade 4 thrombocytopenia and/or neutropenia has been reported in patients 70 years of age or older compared with younger patients receiving temozolomide for refractory anaplastic astrocytoma.
Similar toxicity was observed in patients 65 years of age or older and younger patients receiving temozolomide for newly diagnosed glioblastoma multiforme.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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