Temozolomide

What is Temozolomide?

• Temozolomide (Temodar) is an alkylating drug used to treat some brain tumors such as glioblastoma multiforme or anaplastic astrocytoma.

Temozolomide

Temozolomide-3D-balls

What are the uses of this medicine?

• Temodar (temozolomide) is an alkylating drug for the treatment of adult patients with newly diagnosed glioblastoma multiforme and refractory anaplastic astrocytoma.
• Temodar blocks cell growth, especially cells that grow fast, such as cancer cells. Temodar may decrease the size of certain brain tumors in some patients.

How does this medicine work?

• A triazene analog of dacarbazine with antineoplastic activity.
• As a cytotoxic alkylating agent, temozolomide is converted at physiologic pH to the short-lived active compound, monomethyl triazeno imidazole carboxamide (MTIC).
• The cytotoxicity of MTIC is due primarily to methylation of DNA at the O6 and N7 positions of guanine, resulting in inhibition of DNA replication.
• Unlike dacarbazine, which is metabolized to MITC only in the liver, temozolomide is metabolized to MITC at all sites.
• Temozolomide is administered orally and penetrates well into the central nervous system.

Who Should Not Use this medicine ?

This medicine cannot be used in patients:

• who have a history of hypersensitivity reaction (such as urticaria, allergic reaction including anaphylaxis, toxic epidermal necrolysis, and Stevens-Johnson syndrome) to any of its components.

What drug interactions can this medicine cause?

• Administration of valproic acid decreases oral clearance of temozolomide by about 5%.
• Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements.
• Especially tell your doctor if you take a medicine that contains valproic acid (Stavzor®, Depakene®).

Is this medicine FDA approved?

• It was approved for medical use in the United States in August 1999.
• The intravenous formulation was approved in the United States in February 2009.

How should this medicine be used?

Recommended dosage: Newly Diagnosed glioblastoma multiforme (GBM):

• 75 mg/m2 for 42 days concomitant with focal radiotherapy followed by initial maintenance dose of 150 mg/m2 once daily for Days 1–5 of a 28-day cycle of Temodar for 6 cycles.

Refractory Anaplastic Astrocytoma:

• Initial dose 150 mg/m2 once daily for 5 consecutive days per 28-day treatment cycle.

• The recommended dose for Temodar as an intravenous infusion over 90 minutes is the same as the dose for the oral capsule formulation. Bioequivalence has been established only when Temodar for Injection was given over 90 minutes.

Administration:

• Temodar may be taken by mouth as a capsule at home, or you may receive Temodar by injection into a vein (intravenous). Your doctor will decide the best way for you to take Temodar.

Temodar Capsules:

• Take Temodar Capsules exactly as prescribed.
• Temodar Capsules come in different strengths. Each strength has a different color cap. Your doctor may prescribe more than one strength of Temodar Capsules for you, so it is important that you understand how to take your medicine the right way. Be sure that you understand exactly how many capsules you need to take on each day of your treatment, and what strengths to take. This may be different whenever you start a new cycle.
• Talk to your doctor before you take your dose if you are not sure how much to take. This will help to prevent taking too much Temodar and decrease your chances of getting serious side effects.
• Take each day's dose of Temodar Capsules at one time, with a full glass of water.
• Swallow Temodar Capsules whole. Do not chew, open, or split the capsules.
• If Temodar capsules are accidentally opened or damaged, be careful not to breathe in (inhale) the powder from the capsules or get the powder on your skin or mucous membranes (for example, in your nose or mouth). If contact with any of these areas happens, flush the area with water.
• If you vomit Temodar Capsules, do not take any more capsules. Wait and take your next planned dose.
• The medicine is used best by your body if you take it at the same time every day in relation to a meal.
• To lessen nausea, try to take Temodar on an empty stomach or at bedtime. Your doctor may prescribe medicine to prevent or treat nausea, or other medicines to lessen side effects with Temodar.
• See your doctor regularly to check your progress. Your doctor will check you for side effects that you might not notice.
• If you miss a dose of Temodar, talk with your doctor for instructions about when to take your next dose of Temodar.
• Call your doctor right away if you take more than the prescribed amount of Temodar. It is important that you do not take more than the amount of Temodar prescribed for you.

Temodar for Injection:

• You will receive Temodar as an infusion directly into your vein. Your treatment will take about 90 minutes.
• Your doctor may prescribe medicine to prevent or treat nausea, or other medicines to relieve side effects with Temodar.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As 5-mg, 20-mg, 100-mg, 140-mg, 180-mg, and 250-mg capsules.
• 100-mg powder for injection.

This medicine is available in fallowing brand namesː

• Temodar

What side effects can this medication cause?

The most common side effects of this medicine include:

• nausea and vomiting. Your doctor can prescribe medicines that may help reduce these symptoms.
• headache
• feeling tired
• loss of appetite
• hair loss
• constipation
• bruising
• rash
• paralysis on one side of the body
• diarrhea
• weakness
• fever
• dizziness
• coordination problems
• viral infection
• sleep problems
• memory loss
• pain, irritation, itching, warmth, swelling or redness at the site of infusion
• bruising or small red or purple spots under the skin

Temodar can cause serious side effects include:

• cause birth defects
• Decreased blood cells
• Pneumocystis carinii Pneumonia (PCP)
• Secondary cancers
• Convulsions

What special precautions should I follow?

• Temodar can cause fetal harm when administered to a pregnant woman. Female patients and female partners of male patients should avoid becoming pregnant while taking Temodar.
• Patients treated with Temodar may experience myelosuppression, including prolonged pancytopenia, which may result in aplastic anemia, which in some cases has resulted in a fatal outcome. Monitor Absolute Neutrophil Count (ANC) and platelet count prior to dosing and throughout treatment. Geriatric patients and women have a higher risk of developing myelosuppression.
• Cases of myelodysplastic syndrome and secondary malignancies, including myeloid leukemia, have been observed.
• prophylaxis required for all patients receiving concomitant Temodar and radiotherapy for the 42-day regimen for the treatment of newly diagnosed glioblastoma multiforme. There may be a higher occurrence of PCP when temozolomide is administered during a longer dosing regimen. All patients, particularly those receiving steroids, should be observed closely for the development of lymphopenia and PCP.
• Complete blood counts should be obtained throughout the treatment course as specified.
• As bioequivalence has been established only when given over 90 minutes, infusion over a shorter or longer period of time may result in suboptimal dosing; the possibility of an increase in infusion-related adverse reactions cannot be ruled out.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• pancytopenia
• pyrexia
• multi-organ failure
• death
• hematologic toxicity
• bone marrow suppression
• infections

Management of overdosage:

• In the event of an overdose, hematologic evaluation is needed.
• Supportive measures should be provided as necessary.

Can this medicine be used in pregnancy?

• Temodar can cause fetal harm when administered to a pregnant woman.
• There are no adequate and well-controlled studies in pregnant women.
• Women of childbearing potential should be advised to avoid becoming pregnant during therapy with Temodar.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Temodar Capsules: Active ingredient: temozolomide. Inactive ingredients: lactose anhydrous, colloidal silicon dioxide, sodium starch glycolate, tartaric acid, stearic acid.

The body of the capsules are made of gelatin and are opaque white. The cap is also made of gelatin, and the colors vary based on the dosage strength. The capsule body and cap are imprinted with pharmaceutical branding ink, which contains shellac, dehydrated alcohol, isopropyl alcohol, butyl alcohol, propylene glycol, purified water, strong ammonia, potassium hydroxide, and ferric oxide.

• Temodar 5 mg: The green cap contains gelatin, titanium dioxide, iron oxide yellow, sodium lauryl sulfate, and FD&C Blue #2.
• Temodar 20 mg: The yellow cap contains gelatin, sodium lauryl sulfate, and iron oxide yellow.
• Temodar 100 mg: The pink cap contains gelatin, titanium dioxide, sodium lauryl sulfate, and iron oxide red.
• Temodar 140 mg: The blue cap contains gelatin, sodium lauryl sulfate, and FD&C Blue #2.
• Temodar 180 mg: The orange cap contains gelatin, iron oxide red, iron oxide yellow, titanium dioxide, and sodium lauryl sulfate.
• Temodar 250mg: The white cap contains gelatin, titanium dioxide, and sodium lauryl sulfate.

Temodar for Injection:

• Active ingredient: temozolomide.
• Inactive ingredients: mannitol, L-threonine, polysorbate 80, sodium citrate dihydrate, and hydrochloric acid.

Who manufactures and distributes this medicine?

Temodar Capsules

• Manufactured by: Schering Corporation, a subsidiary of MERCK & CO., INC., Whitehouse Station, NJ , USA

Temodar for Injection

• Manufactured by: Baxter Oncology GmbH, Halle/Westfalen, Germany
• Distributed by: Schering Corporation, a subsidiary of MERCK & CO., INC., Whitehouse Station, NJ, USA

What should I know about storage and disposal of this medication?

• Store Temodar Capsules at 77°F.
• Storage at 59° to 86°F (15° to 30°C) is permitted occasionally.

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• Dailymed label info on Temozolomide
• FDA Temozolomide

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