Temodar 140mg Capsules
It is used to treat brain cancer.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Antineoplastic agent
Pharmacologic Class
Alkylating agent; Imidazotetrazine derivative
Pregnancy Category
Category D
FDA Approved
Aug 1999
DEA Schedule
Not Controlled
Overview
What is this medicine?
Temozolomide is a chemotherapy medicine used to treat certain types of brain tumors. It works by damaging the DNA of cancer cells, which helps to stop their growth and spread. It's often taken as a capsule by mouth.
How to Use This Medicine
Taking Your Medication Correctly
To ensure you get the most benefit from your medication, follow these steps:
Take your medication exactly as directed by your doctor. Read all the information provided to you and follow the instructions carefully.
Take your medication at the same time every day. You can take it with or without food, but be consistent in how you take it each time. If you choose to take it with food, always take it with food. If you prefer to take it on an empty stomach, always take it that way. Taking it on an empty stomach may help prevent stomach upset, and taking it at bedtime may also be beneficial. Consult with your doctor to determine the best approach for you.
To minimize side effects, your doctor may prescribe other medications to take with this one.
Swallow your medication whole with a full glass of water. Do not chew, break, crush, or dissolve the capsule.
Continue taking your medication as directed by your doctor or healthcare provider, even if you start feeling better.
Your dose may consist of two or more different strengths and colors of capsules.
If you vomit after taking your medication, do not take another dose. Instead, follow your doctor's instructions.
When handling your medication, take special precautions. Consult with your doctor or pharmacist for guidance on how to handle it safely.
Wear gloves when touching your medication. If the capsule is opened or broken, avoid touching the contents. Do not inhale the contents of the capsule. If you accidentally touch the contents or get them in your eyes, wash your hands or eyes immediately.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from the bathroom.
What to Do If You Miss a Dose
* If you miss a dose, contact your doctor to find out what to do next.
To ensure you get the most benefit from your medication, follow these steps:
Take your medication exactly as directed by your doctor. Read all the information provided to you and follow the instructions carefully.
Take your medication at the same time every day. You can take it with or without food, but be consistent in how you take it each time. If you choose to take it with food, always take it with food. If you prefer to take it on an empty stomach, always take it that way. Taking it on an empty stomach may help prevent stomach upset, and taking it at bedtime may also be beneficial. Consult with your doctor to determine the best approach for you.
To minimize side effects, your doctor may prescribe other medications to take with this one.
Swallow your medication whole with a full glass of water. Do not chew, break, crush, or dissolve the capsule.
Continue taking your medication as directed by your doctor or healthcare provider, even if you start feeling better.
Your dose may consist of two or more different strengths and colors of capsules.
If you vomit after taking your medication, do not take another dose. Instead, follow your doctor's instructions.
When handling your medication, take special precautions. Consult with your doctor or pharmacist for guidance on how to handle it safely.
Wear gloves when touching your medication. If the capsule is opened or broken, avoid touching the contents. Do not inhale the contents of the capsule. If you accidentally touch the contents or get them in your eyes, wash your hands or eyes immediately.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from the bathroom.
What to Do If You Miss a Dose
* If you miss a dose, contact your doctor to find out what to do next.
Lifestyle & Tips
- Take the capsules on an empty stomach (at least 1 hour before or 2 hours after a meal) or at bedtime to help reduce nausea and vomiting. Swallow capsules whole with a glass of water; do not open, chew, or crush them.
- Wear gloves if handling broken capsules.
- Take anti-nausea medication as prescribed by your doctor.
- Maintain good hydration.
- Avoid contact with people who are sick or have infections, as your immune system may be weakened.
- Report any signs of infection (fever, chills, sore throat) or unusual bleeding/bruising immediately.
- Avoid live vaccines during treatment.
- Use effective contraception during treatment and for at least 6 months after for females, and 3 months for males, due to potential harm to a fetus.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
Varies significantly by indication and phase of treatment. For newly diagnosed glioblastoma multiforme (GBM): Concomitant phase: 75 mg/m² orally once daily for 42 days (up to 49 days) with concomitant focal radiotherapy. Adjuvant phase: 150 mg/m² orally once daily for 5 days, repeated every 28 days for 6 cycles. Dose may be escalated to 200 mg/m² if tolerated.
Dose Range:
75 - 200 mg
Condition-Specific Dosing:
newlyDiagnosedGBM_concomitant:
75 mg/m² daily for 42-49 days
newlyDiagnosedGBM_adjuvant:
150-200 mg/m² daily for 5 days every 28 days for 6 cycles
refractoryAnaplasticAstrocytoma:
Initial: 150 mg/m² daily for 5 days every 28 days; escalate to 200 mg/m² if tolerated for subsequent cycles.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Dosing is complex and typically based on body surface area, similar to adult dosing, but often used in specific protocols for pediatric brain tumors (e.g., high-grade glioma, medulloblastoma). Specific dosing should be guided by pediatric oncology protocols.
Adolescent:
Dosing is complex and typically based on body surface area, similar to adult dosing, but often used in specific protocols for pediatric brain tumors (e.g., high-grade glioma, medulloblastoma). Specific dosing should be guided by pediatric oncology protocols.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
No specific dose adjustment recommended.
Severe:
Use with caution; data are limited. Not recommended for patients with severe renal impairment (CrCl < 30 mL/min) unless potential benefit outweighs risk.
Dialysis:
Not available; temozolomide is not significantly dialyzable.
Hepatic Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
No specific dose adjustment recommended.
Severe:
Use with caution; data are limited. Not recommended for patients with severe hepatic impairment unless potential benefit outweighs risk.
Pharmacology
Mechanism of Action
Temozolomide is an imidazotetrazine derivative that undergoes rapid chemical conversion at physiological pH to the active compound monomethyl triazenoimidazole carboxamide (MTIC). MTIC is an alkylating agent that primarily methylates DNA at the O6 and N7 positions of guanine. This methylation leads to DNA damage, triggering cell cycle arrest (G2/M phase) and ultimately apoptosis in rapidly dividing cells, including tumor cells.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 100% (oral)
Tmax:
0.5-1.5 hours
FoodEffect:
Food decreases Cmax by 33% and AUC by 9%. However, the clinical significance of this effect is not considered major, and temozolomide can be taken with or without food, though taking it on an empty stomach or at bedtime may reduce nausea.
Distribution:
Vd:
Approximately 0.4 L/kg
ProteinBinding:
10-15%
CnssPenetration:
Yes, readily crosses the blood-brain barrier, achieving CSF concentrations approximately 20% of plasma AUC.
Elimination:
HalfLife:
Approximately 1.8 hours
Clearance:
Approximately 5.5 L/hr/m²
ExcretionRoute:
Primarily renal (5-10% unchanged drug, remainder as metabolites)
Unchanged:
5-10%
Pharmacodynamics
OnsetOfAction:
Not directly applicable for chemotherapy; effects are cumulative over treatment cycles.
PeakEffect:
Not directly applicable for chemotherapy; peak plasma concentration of active metabolite (MTIC) occurs shortly after temozolomide peak.
DurationOfAction:
Not directly applicable; DNA damage and cellular effects persist beyond drug elimination.
Safety & Warnings
BLACK BOX WARNING
Myelosuppression: Temozolomide causes severe myelosuppression (myelosuppression, including pancytopenia, leukopenia, thrombocytopenia, and anemia), which may be dose-limiting and may result in opportunistic infections, including fatal cases. Obtain a complete blood count (CBC) on Day 22 (or Day 29) of each 28-day cycle and weekly during the concomitant phase. Do not administer Temodar if ANC is < 1.5 x 10^9/L or platelet count is < 100 x 10^9/L.
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor immediately or seek emergency medical attention:
Signs of an allergic reaction, such as:
+ Rash or hives
+ Itching or red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing or tightness in the chest or throat
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness or swelling of the mouth, face, lips, tongue, or throat
Signs of infection, including:
+ Fever or chills
+ Severe sore throat, ear or sinus pain, or cough
+ Increased or discolored sputum
+ Painful urination or mouth sores
+ Wounds that do not heal
Unexplained bruising or bleeding
Shortness of breath, sudden weight gain, or swelling in the arms or legs
Weakness on one side of the body, difficulty speaking or thinking, balance problems, or drooping on one side of the face
Blurred vision or confusion
Mood changes or trouble swallowing
Loss of bladder control or memory problems
Abnormal burning, numbness, or tingling sensations
Seizures or changes in vision
Pinpoint red spots on the skin or breast pain
Severe Liver Problems: A Rare but Serious Side Effect
This medication can cause severe and potentially life-threatening liver problems. If you experience any of the following symptoms, contact your doctor immediately:
Dark urine
Fatigue or decreased appetite
Nausea or stomach pain
Vomiting or pale stools
Yellowing of the skin or eyes
Other Possible Side Effects
Most people do not experience severe side effects, but some may occur. If you notice any of the following symptoms and they bother you or do not go away, contact your doctor:
Hair loss
Headache
Dizziness, drowsiness, fatigue, or weakness
Constipation, diarrhea, stomach pain, nausea, vomiting, or decreased appetite
Difficulty sleeping
Back, muscle, or joint pain
Dry skin or changes in taste
Weight gain or signs of a common cold
* Mouth irritation or mouth sores
Reporting Side Effects
If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor immediately or seek emergency medical attention:
Signs of an allergic reaction, such as:
+ Rash or hives
+ Itching or red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing or tightness in the chest or throat
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness or swelling of the mouth, face, lips, tongue, or throat
Signs of infection, including:
+ Fever or chills
+ Severe sore throat, ear or sinus pain, or cough
+ Increased or discolored sputum
+ Painful urination or mouth sores
+ Wounds that do not heal
Unexplained bruising or bleeding
Shortness of breath, sudden weight gain, or swelling in the arms or legs
Weakness on one side of the body, difficulty speaking or thinking, balance problems, or drooping on one side of the face
Blurred vision or confusion
Mood changes or trouble swallowing
Loss of bladder control or memory problems
Abnormal burning, numbness, or tingling sensations
Seizures or changes in vision
Pinpoint red spots on the skin or breast pain
Severe Liver Problems: A Rare but Serious Side Effect
This medication can cause severe and potentially life-threatening liver problems. If you experience any of the following symptoms, contact your doctor immediately:
Dark urine
Fatigue or decreased appetite
Nausea or stomach pain
Vomiting or pale stools
Yellowing of the skin or eyes
Other Possible Side Effects
Most people do not experience severe side effects, but some may occur. If you notice any of the following symptoms and they bother you or do not go away, contact your doctor:
Hair loss
Headache
Dizziness, drowsiness, fatigue, or weakness
Constipation, diarrhea, stomach pain, nausea, vomiting, or decreased appetite
Difficulty sleeping
Back, muscle, or joint pain
Dry skin or changes in taste
Weight gain or signs of a common cold
* Mouth irritation or mouth sores
Reporting Side Effects
If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Fever (100.4°F or higher) or chills
- Sore throat or other signs of infection
- Unusual bleeding or bruising
- Severe nausea or vomiting that doesn't improve with medication
- Severe fatigue or weakness
- Yellowing of skin or eyes (jaundice)
- Dark urine or pale stools
- Severe headache or new neurological symptoms (e.g., seizures, confusion, vision changes)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced.
A specific allergy to dacarbazine.
If you have a low white blood cell count (leukopenia) or a low platelet count (thrombocytopenia).
If you are breastfeeding. You should not breastfeed while taking this medication and for 1 week after your last dose.
To ensure safe treatment, it is crucial to discuss the following with your doctor and pharmacist:
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins.
Any existing health problems.
* Potential interactions between this medication and other substances or health conditions.
Do not start, stop, or change the dose of any medication without first consulting your doctor to confirm it is safe to do so.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced.
A specific allergy to dacarbazine.
If you have a low white blood cell count (leukopenia) or a low platelet count (thrombocytopenia).
If you are breastfeeding. You should not breastfeed while taking this medication and for 1 week after your last dose.
To ensure safe treatment, it is crucial to discuss the following with your doctor and pharmacist:
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins.
Any existing health problems.
* Potential interactions between this medication and other substances or health conditions.
Do not start, stop, or change the dose of any medication without first consulting your doctor to confirm it is safe to do so.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Regular blood tests will be necessary, as directed by your doctor, to monitor your condition. Discuss any concerns or questions you have with your doctor.
Before receiving any vaccinations, consult with your doctor, as certain vaccines may not be effective or may increase the risk of infection when taken with this medication.
If you experience stomach upset, vomiting, diarrhea, or loss of appetite, consult with your doctor, as there may be ways to minimize these side effects.
This medication can cause low blood cell counts, which may lead to bleeding problems, infections, or anemia. In severe cases, low blood cell counts can be life-threatening and may require hospitalization or blood transfusions. If you have any questions or concerns, discuss them with your doctor.
You may be more susceptible to infections due to this medication. To reduce the risk of infection, practice good hygiene by washing your hands frequently and avoid close contact with people who have infections, colds, or flu.
Be cautious, as this medication may increase the risk of bleeding. Take precautions to avoid injury, and use a soft toothbrush and an electric razor to minimize the risk of bleeding.
Rare but serious side effects of this medication include bone marrow problems and the development of secondary cancers. Discuss these risks with your doctor.
If you are 70 years or older, use this medication with caution, as you may be more prone to side effects.
This medication may affect fertility in men. Discuss any concerns you have with your doctor.
This medication is present in semen, and you should not donate semen while taking this medication or for 3 months after your last dose.
Women of childbearing age should be aware that this medication may harm an unborn baby. A pregnancy test will be conducted before starting this medication to confirm that you are not pregnant. If you or your partner may become pregnant, use effective birth control during treatment and for a period after the last dose, as advised by your doctor. If you or your partner becomes pregnant, notify your doctor immediately.
Before receiving any vaccinations, consult with your doctor, as certain vaccines may not be effective or may increase the risk of infection when taken with this medication.
If you experience stomach upset, vomiting, diarrhea, or loss of appetite, consult with your doctor, as there may be ways to minimize these side effects.
This medication can cause low blood cell counts, which may lead to bleeding problems, infections, or anemia. In severe cases, low blood cell counts can be life-threatening and may require hospitalization or blood transfusions. If you have any questions or concerns, discuss them with your doctor.
You may be more susceptible to infections due to this medication. To reduce the risk of infection, practice good hygiene by washing your hands frequently and avoid close contact with people who have infections, colds, or flu.
Be cautious, as this medication may increase the risk of bleeding. Take precautions to avoid injury, and use a soft toothbrush and an electric razor to minimize the risk of bleeding.
Rare but serious side effects of this medication include bone marrow problems and the development of secondary cancers. Discuss these risks with your doctor.
If you are 70 years or older, use this medication with caution, as you may be more prone to side effects.
This medication may affect fertility in men. Discuss any concerns you have with your doctor.
This medication is present in semen, and you should not donate semen while taking this medication or for 3 months after your last dose.
Women of childbearing age should be aware that this medication may harm an unborn baby. A pregnancy test will be conducted before starting this medication to confirm that you are not pregnant. If you or your partner may become pregnant, use effective birth control during treatment and for a period after the last dose, as advised by your doctor. If you or your partner becomes pregnant, notify your doctor immediately.
Overdose Information
Overdose Symptoms:
- Severe myelosuppression (e.g., profound neutropenia, thrombocytopenia, anemia)
- Severe gastrointestinal toxicity (e.g., nausea, vomiting, diarrhea)
- Hepatotoxicity
What to Do:
There is no known antidote for temozolomide overdose. Management is supportive, including close monitoring of blood counts and liver function, and administration of appropriate supportive care (e.g., antiemetics, blood transfusions, growth factors for myelosuppression). Call 1-800-222-1222 (Poison Control) or seek immediate medical attention.
Drug Interactions
Major Interactions
- Live vaccines (due to immunosuppression)
- Other myelosuppressive agents (additive myelosuppression)
Moderate Interactions
- Valproic acid (decreases temozolomide clearance by 5%, clinical significance uncertain but monitor for increased toxicity)
- Phenytoin (potential for decreased temozolomide exposure, monitor)
Confidence Interactions
Monitoring
Baseline Monitoring
Complete Blood Count (CBC) with differential and platelets
Rationale: To establish baseline hematologic parameters, as myelosuppression (neutropenia, thrombocytopenia) is a dose-limiting toxicity.
Timing: Prior to initiation of treatment.
Liver Function Tests (LFTs)
Rationale: To assess baseline hepatic function, as temozolomide is metabolized in the liver and can cause hepatotoxicity.
Timing: Prior to initiation of treatment.
Renal Function Tests (Creatinine, BUN)
Rationale: To assess baseline renal function, as temozolomide is primarily renally excreted.
Timing: Prior to initiation of treatment.
Routine Monitoring
Complete Blood Count (CBC) with differential and platelets
Frequency: Weekly during concomitant phase; prior to each cycle (Day 1) and on Day 22 (or Day 29) of each 28-day adjuvant cycle.
Target: ANC ≥ 1.5 x 10^9/L, Platelets ≥ 100 x 10^9/L for dose initiation/escalation.
Action Threshold: Dose reduction or interruption if ANC < 1.5 x 10^9/L or platelets < 100 x 10^9/L. Specific dose modifications based on nadir counts.
Liver Function Tests (LFTs)
Frequency: Prior to each cycle.
Target: Within normal limits or acceptable for treatment.
Action Threshold: Significant elevations may require dose modification or discontinuation.
Symptom Monitoring
- Signs of myelosuppression (fever, chills, sore throat, unusual bleeding or bruising, fatigue)
- Gastrointestinal symptoms (nausea, vomiting, constipation, diarrhea)
- Neurological changes (headache, seizures, fatigue, confusion)
- Skin reactions (rash)
- Signs of opportunistic infections (e.g., Pneumocystis jirovecii pneumonia - PJP prophylaxis is often required)
- Signs of hepatotoxicity (jaundice, dark urine, abdominal pain)
Special Patient Groups
Pregnancy
Temozolomide is classified as Pregnancy Category D. It can cause fetal harm when administered to a pregnant woman. Advise pregnant women of the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during treatment and for at least 6 months after the last dose. Advise males with female partners of reproductive potential to use effective contraception during treatment and for at least 3 months after the last dose.
Trimester-Specific Risks:
First Trimester:
High risk of major birth defects and fetal loss due to its cytotoxic and genotoxic effects.
Second Trimester:
Risk of fetal growth restriction, organ toxicity, and other adverse effects.
Third Trimester:
Risk of fetal growth restriction, myelosuppression, and other adverse effects.
Lactation
It is not known whether temozolomide or its metabolites are excreted in human milk. Because of the potential for serious adverse reactions in breastfed infants, advise women not to breastfeed during treatment with temozolomide and for at least 1 week after the last dose.
Infant Risk:
High risk of serious adverse effects, including myelosuppression and other toxicities, due to its cytotoxic nature.
Pediatric Use
Safety and effectiveness have not been established in pediatric patients. However, temozolomide is used off-label or in clinical trials for certain pediatric brain tumors (e.g., high-grade glioma, medulloblastoma) based on adult data and specific protocols. Dosing and monitoring require specialized pediatric oncology expertise.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly patients (≥65 years) and younger patients, but a higher incidence of myelosuppression (especially thrombocytopenia and neutropenia) has been reported in elderly patients. Close monitoring of blood counts is particularly important in this population.
Clinical Information
Clinical Pearls
- Temozolomide is a prodrug that undergoes non-enzymatic conversion to its active form, MTIC, making it less susceptible to drug-drug interactions via CYP450 enzymes.
- Pneumocystis jirovecii pneumonia (PJP) prophylaxis is strongly recommended for all patients receiving temozolomide with concomitant radiation, and should be considered for patients receiving temozolomide as monotherapy, especially those with lymphopenia.
- Capsules should be swallowed whole with water. If capsules are opened or damaged, the powder can be irritating to skin and mucous membranes; wear gloves for handling.
- Dose adjustments are primarily based on nadir blood counts (ANC and platelets) from the previous cycle.
- Nausea and vomiting are common side effects; prophylactic antiemetics are often necessary, especially with higher doses.
Alternative Therapies
- Lomustine (CCNU)
- Carmustine (BCNU) wafers (Gliadel)
- Bevacizumab
- Radiation therapy
- Surgical resection
- Tumor Treating Fields (TTFields, Optune)
Cost & Coverage
Average Cost:
Varies widely, typically several thousand USD per 30 capsules (e.g., 100mg strength)
Generic Available:
Yes
Insurance Coverage:
Specialty Tier (Tier 4 or higher) for most commercial and Medicare Part D plans. Requires prior authorization and often step therapy.
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.