temozolomide

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temozolomide

 [tem″ah-zo´lah-mīd]
a cytotoxic alkylating agent used as an antineoplastic in the treatment of refractory anaplastic astrocytoma, administered orally.

temozolomide

Temodal, Temodar

Pharmacologic class: Alkylating agent

Therapeutic class: Antineoplastic

Pregnancy risk category D

Action

Rapidly converts to monomethyl triazeno imidazole carboxamide, an active compound that prevents DNA transcription

Availability

Capsules: 5 mg, 20 mg, 100 mg, 140 mg, 180 mg, 250 mg

Injection (powder for solution, lyophilized): 100 mg

Indications and dosages

Refractory anaplastic astrocytoma

Adults: 150 mg/m2 P.O. or by 90-minute I.V. infusion daily for 5 consecutive days of each 28-day treatment cycle. Adjust dosage as appropriate based on absolute neutrophil count.

Newly diagnosed glioblastoma multiforme with radiotherapy

Adults: 75 mg/m2 P.O. or by 90-minute I.V. infusion for 42 days with focal radiotherapy (RT), followed by initial maintenance dose of 150 mg/m2 P.O. or by 90-minute I.V. infusion daily for days 1 to 5 of a 28-day cycle for six cycles. Four weeks after completing the drug plus RT phase, administer drug for an additional six cycles of maintenance treatment. Dosage in maintenance cycle 1 is 150 mg/m2 P.O. or by 90-minute I.V. infusion daily for 5 days, followed by 23 days without treatment. At start of maintenance cycle 2, dosage may be escalated to 200 mg/m2 based on absolute neutrophil and platelet counts. Continue dosage at 200 mg/m2 daily for first 5 days of each subsequent cycle except if toxicity occurs. If dosage wasn't escalated at maintenance cycle 2, escalation shouldn't be done in subsequent cycles.

Dosage adjustment

• Neutropenia, thrombocytopenia

Contraindications

• Hypersensitivity to drug, its components, or dacarbazine

Precautions

Use cautiously in:

• severe hepatic or renal impairment, active infection, decreased bone marrow reserve, other chronic debilitating illness

• elderly patients

• pregnant or breastfeeding patients

• children (safety not established).

Administration

• Follow facility policy for handling and disposing of chemotherapeutic drugs.

• Give capsules whole daily with a full glass of water, consistently either with or without food.

• Bring powder for injection to room temperature before reconstituting with 41 ml sterile water for injection that results in a 2.5-mg/ml solution. Gently swirl but don't shake vials. Don't further dilute reconstituted solution. Use reconstituted solution within 14 hours, including infusion time. Withdraw prescribed dose and transfer into empty 250-ml infusion bag. Give reconstituted solution only by I.V. infusion using infusion pump over 90 minutes. Flush lines before and after each infusion.

• Know that drug may be given in same I.V. line with normal saline solution for injection only.

• Be aware that dosages in 28-day cycle depend on nadir neutrophil and platelet counts.

Adverse reactions

CNS: fatigue, headache, dysphasia, poor coordination, ataxia, anxiety, depression, dizziness, drowsiness, confusion, amnesia, insomnia, mental status changes, weakness, paresis, hemiparesis, paresthesias, seizures

CV: peripheral edema

EENT: abnormal vision, diplopia, pharyngitis, sinusitis

GI: nausea, vomiting, constipation, diarrhea, abdominal pain, anorexia

GU: urinary incontinence or frequency, urinary tract infection, breast pain (in women)

Hematologic: anemia, leukopenia, thrombocytopenia

Metabolic: adrenal hypercorticism

Musculoskeletal: abnormal gait, back pain, myalgia

Respiratory: cough, upper respiratory infection

Skin: pruritus, rash

Other: fever, viral infection, weight gain

Interactions

Drug-drug. Antineoplastics: additive bone marrow depression

Live-virus vaccines: decreased antibody response to vaccine, greater risk of adverse reactions

Valproic acid: decreased oral clearance of temozolomide

Drug-diagnostic tests. Neutrophils, platelets: decreased counts

Drug-food. Any food: reduced rate and extent of temozolomide absorption

Patient monitoring

Monitor CBC with white cell differential. Stay alert for evidence of bone marrow depression.

• Assess neurologic status carefully.

• Monitor fluid intake and output, and weigh patient regularly.

• Be aware that Pneumocystis jiroveci pneumonia prophylaxis is required during concomitant administration of RT and should be continued in patients who develop lymphocytopenia until recovery from lymphocytopenia (circulating tumor cells Grade 1 or less).

Patient teaching

• Tell patient to take capsules consistently with or without food, and with a full glass of water.

• Instruct patient to swallow capsules whole without opening or chewing them and if capsules are accidentally opened or damaged, to avoid inhalation or contact with the skin or mucous membranes.

• If drug causes nausea or vomiting, advise patient to take it 1 hour before or 2 hours after a meal.

• Inform patient that drug may cause abnormal gait and dizziness.

Instruct patient to immediately report unusual bleeding or bruising.

• Advise patient to avoid live-virus vaccines.

• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration, alertness, and vision.

• Instruct patient to report suspected pregnancy. Caution her not to breastfeed.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.

temozolomide

/tem·o·zo·lo·mide/ (tem″ah-zo´lah-mīd) a cytotoxic alkylating agent used as an antineoplastic in the treatment of refractory anaplastic astrocytoma.

temozolomide

a miscellaneous antineoplastic agent.
indication It is used to treat anaplastic astrocytoma with relapse.
contraindications Pregnancy, lactation, and known hypersensitivity to this drug or to carbazine prohibit its use.
adverse effects Life-threatening effects are thrombocytopenia, leukopenia, and seizures. Other adverse effects include anemia, urinary incontinence, urinary tract infection, urinary frequency, upper respiratory infection, pharyngitis, sinusitis, cough, headache, fatigue, asthenia, fever, edema, back pain, weight increase, and diplopia. Common side effects include nausea, anorexia, vomiting, hemiparesis, dizziness, poor coordination, amnesia, insomnia, paresthesia, somnolence, paresis, ataxia, anxiety, dysphagia, depression, confusion, rash, and pruritus.

temozolomide

Temodal® Oncology An alkylating agent used for recurrent gliomas–eg, anaplastic astrocytoma, and possibly melanoma and other solid tumors. See Astrocytoma, Glioblastoma multiforme.
References in periodicals archive ?
Temodal was developed by Cancer Research Campaign scientists.
Figures released today showed that sales of Temodal have delivered more than pounds 1m in royalties to the Cancer Research Campaign, whose scientists developed the drug.
M) BoEte de 1 Seringue preremplie de 0,3 ml 19 646,10 11 752,00 20 248,47 TEMODAL 250mg Gelule dans sachets-doses BoEte de 5 - 6 392,00 18 341,03 TRITAZIDE 10 mg/12,5 mg Comprime secable BoEte de 28 234,00 63,30 215,87 XYZALL 5 MG Comprime pellicule BoEte de 14 88,00 45,20 50,21 ZOLOFT 50 mg Gelule BoEte de 15 180,00 71,00 78,80 FEMARA 2,5 mg Comprime pellicule BoEte de 30 1 284,30 1 021,00 1559,29 ACTONEL 5 mg Comprime pellicule BoEte de 28 569,00 296,00 353,53
Figures released yesterday showed that sales of Temodal over the past two years have delivered more than pounds 1m in royalties to the Cancer Research Campaign, whose scientists developed the drug.
Figures released today show sales of Temodal over the last two years have delivered more than pounds 1 million in royalties to the Cancer Research Campaign, whose scientists developed the drug.
Temodal is by far the most effective drug for brain cancer but drug companies can't be bothered going round all these trusts to negotiate.
Developed by the Cancer Research Campaign, it will be available on the NHS next month - marketed as Temodal.
In trials, temozolomide - to be marketed as Temodal in a deal aimed to bring substantial royalties to the cancer group - boosted survival rates and reduced debilitating side effects.
In the life and health sciences' vision science group we have Britain's only whole-head MEG Brain Scanner, which is a national resource, while pharmacy has recently seen the launch of the new cancer drug, Temodal, originally developed at Aston.
We also focused on taxol (ovarian cancer), taxotere (breast cancer), irinotecan (bowel cancer), temodal (brain cancer), rilutek (motor neurone disease), beta interferon (multiple sclerosis) and aricept (Alzheimer's).
The results have included the brain cancer drug Temodal.