Temodar 250mg 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
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 capsules, sometimes with radiation therapy.
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 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. For example, if you take it with food one day, take it with food every day. Alternatively, if you take it on an empty stomach, continue to take it on an empty stomach.
To minimize the risk of an upset stomach, consider taking your medication with food or at bedtime. Consult with your doctor for personalized advice.
In some cases, your doctor may prescribe other medications to help prevent side effects. Take these medications as directed.
Swallow your medication whole with a full glass of water. Do not chew, break, crush, or dissolve the capsule.
Continue taking your medication as instructed by your doctor or healthcare provider, even if you start to feel better.
Your medication dose may consist of two or more different strengths and colors of capsules.
If you vomit after taking your medication, do not take an additional dose. Instead, follow your doctor's instructions.
When handling your medication, take special precautions. Consult with your doctor or pharmacist for guidance on safe handling procedures.
Wear gloves when touching your medication to minimize exposure. 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 bathrooms.
If you miss a dose, contact your doctor for advice on 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 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. For example, if you take it with food one day, take it with food every day. Alternatively, if you take it on an empty stomach, continue to take it on an empty stomach.
To minimize the risk of an upset stomach, consider taking your medication with food or at bedtime. Consult with your doctor for personalized advice.
In some cases, your doctor may prescribe other medications to help prevent side effects. Take these medications as directed.
Swallow your medication whole with a full glass of water. Do not chew, break, crush, or dissolve the capsule.
Continue taking your medication as instructed by your doctor or healthcare provider, even if you start to feel better.
Your medication dose may consist of two or more different strengths and colors of capsules.
If you vomit after taking your medication, do not take an additional dose. Instead, follow your doctor's instructions.
When handling your medication, take special precautions. Consult with your doctor or pharmacist for guidance on safe handling procedures.
Wear gloves when touching your medication to minimize exposure. 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 bathrooms.
If you miss a dose, contact your doctor for advice on what to do next.
Lifestyle & Tips
- Take on an empty stomach (at least 1 hour before or 2 hours after a meal), preferably at bedtime, to help reduce nausea and vomiting.
- Take anti-nausea medication as prescribed by your doctor.
- Swallow capsules whole with a glass of water. Do not open, chew, or crush the capsules.
- If a capsule breaks, avoid contact with skin or mucous membranes. If contact occurs, wash thoroughly with soap and water.
- Wear gloves when handling the capsules.
- Store capsules at room temperature, away from moisture and heat.
- Maintain good hydration unless otherwise instructed by your doctor.
- Avoid live vaccines during treatment.
- Report any signs of infection (fever, chills, sore throat) or unusual bleeding/bruising immediately.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
Varies significantly based on indication and prior treatment. For newly diagnosed glioblastoma: 75 mg/m² orally once daily for 42 days concurrently with focal radiotherapy, followed by 150-200 mg/m² orally once daily for 5 days every 28 days for 6 cycles. For refractory anaplastic astrocytoma: 150 mg/m² orally once daily for 5 days every 28 days, increasing to 200 mg/m² if tolerated.
Dose Range:
75 - 200 mg
Condition-Specific Dosing:
newly_diagnosed_glioblastoma:
75 mg/m² daily for 42 days (concurrent phase), then 150-200 mg/m² daily for 5 days every 28 days (adjuvant phase)
refractory_anaplastic_astrocytoma:
150 mg/m² daily for 5 days every 28 days, escalating to 200 mg/m² if tolerated
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Safety and efficacy not established in pediatric patients <3 years old. Limited data for children ≥3 years old, often extrapolated from adult dosing with careful monitoring.
Adolescent:
Dosing typically based on body surface area, similar to adult protocols, with careful monitoring for myelosuppression.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
No specific dose adjustment recommended.
Severe:
Use with caution; no specific dose recommendations due to limited data.
Dialysis:
Not available; use with caution due to limited data.
Hepatic Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
No specific dose adjustment recommended.
Severe:
Use with caution; no specific dose recommendations due to limited data.
Pharmacology
Mechanism of Action
Temozolomide is an imidazotetrazine derivative that undergoes rapid chemical conversion at physiological pH to the active compound 5-(3-methyltriazen-1-yl)imidazole-4-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 and apoptosis, particularly in rapidly dividing tumor cells.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 100%
Tmax:
0.5 to 1.5 hours (median 1 hour)
FoodEffect:
Food decreases the rate and extent of absorption (Cmax decreased by 33%, AUC decreased by 9%). Should be taken on an empty stomach.
Distribution:
Vd:
0.37 to 0.49 L/kg
ProteinBinding:
10% to 15%
CnssPenetration:
Yes (readily crosses the blood-brain barrier)
Elimination:
HalfLife:
Approximately 1.8 hours
Clearance:
Not available (primarily non-enzymatic conversion)
ExcretionRoute:
Renal (approximately 38% of dose excreted in urine over 7 days, with 5-10% as unchanged drug)
Unchanged:
5-10%
Pharmacodynamics
OnsetOfAction:
Not directly applicable for chronic oncology treatment; effects are cumulative over cycles.
PeakEffect:
Not directly applicable; therapeutic effect is achieved through sustained exposure and DNA damage over treatment cycles.
DurationOfAction:
Not directly applicable; effects persist as long as DNA damage is present and cells attempt repair.
Safety & Warnings
BLACK BOX WARNING
Myelosuppression: Temozolomide causes severe myelosuppression, including prolonged pancytopenia, which can result in aplastic anemia and death. Complete blood counts (CBCs) must be obtained on Day 22 (21 days after the first dose) of each 28-day cycle and weekly until recovery if ANC <1.5 x 10^9/L or platelet count <100 x 10^9/L. Temozolomide should be interrupted or discontinued if ANC or platelet counts fall below specified thresholds.
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 or seek medical attention immediately:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of infection, including:
+ Fever
+ Chills
+ Severe sore throat
+ Ear or sinus pain
+ Cough
+ Increased or changed sputum production
+ Pain while urinating
+ Mouth sores
+ Wounds that won't heal
Unexplained bruising or bleeding
Shortness of breath, significant weight gain, or swelling in the arms or legs
Weakness on one side of the body, trouble speaking or thinking, balance changes, drooping on one side of the face, or blurred vision
Confusion
Mood changes
Difficulty swallowing
Loss of bladder control
Memory problems or loss
Abnormal burning, numbness, or tingling sensations
Seizures
Changes in vision
Pinpoint red spots on the skin
Breast pain
Signs of severe and potentially life-threatening liver problems, including:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, contact your doctor or seek medical help:
Hair loss
Headache
Dizziness, drowsiness, fatigue, or weakness
Constipation, diarrhea, stomach pain, upset stomach, vomiting, or decreased appetite
Trouble sleeping
Back, muscle, or joint pain
Dry skin
Changes in taste
Weight gain
Signs of a common cold
* Mouth irritation or mouth sores
Reporting Side Effects
This list is not exhaustive, and you may experience other 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 or seek medical attention immediately:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of infection, including:
+ Fever
+ Chills
+ Severe sore throat
+ Ear or sinus pain
+ Cough
+ Increased or changed sputum production
+ Pain while urinating
+ Mouth sores
+ Wounds that won't heal
Unexplained bruising or bleeding
Shortness of breath, significant weight gain, or swelling in the arms or legs
Weakness on one side of the body, trouble speaking or thinking, balance changes, drooping on one side of the face, or blurred vision
Confusion
Mood changes
Difficulty swallowing
Loss of bladder control
Memory problems or loss
Abnormal burning, numbness, or tingling sensations
Seizures
Changes in vision
Pinpoint red spots on the skin
Breast pain
Signs of severe and potentially life-threatening liver problems, including:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, contact your doctor or seek medical help:
Hair loss
Headache
Dizziness, drowsiness, fatigue, or weakness
Constipation, diarrhea, stomach pain, upset stomach, vomiting, or decreased appetite
Trouble sleeping
Back, muscle, or joint pain
Dry skin
Changes in taste
Weight gain
Signs of a common cold
* Mouth irritation or mouth sores
Reporting Side Effects
This list is not exhaustive, and you may experience other 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 or persistent nausea, vomiting, or diarrhea
- Extreme fatigue or weakness
- Yellowing of the skin or eyes (jaundice)
- Dark urine or pale stools
- New or worsening headache
- Seizures
- Vision changes
- Confusion or changes in mental status
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, including any symptoms.
A known 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 at least 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, including any symptoms.
A known 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 at least 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. Be sure to discuss your test results 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 a decrease in 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 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.
Additionally, you may be at a higher risk of bleeding easily. 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 experiencing side effects.
This medication may affect fertility in men. Discuss any concerns with your doctor.
It is also important to note that this medication is present in semen. Do not donate semen while taking this medication or for 3 months after your last dose.
This medication can cause harm to an unborn baby. A pregnancy test will be conducted before starting treatment 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 a decrease in 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 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.
Additionally, you may be at a higher risk of bleeding easily. 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 experiencing side effects.
This medication may affect fertility in men. Discuss any concerns with your doctor.
It is also important to note that this medication is present in semen. Do not donate semen while taking this medication or for 3 months after your last dose.
This medication can cause harm to an unborn baby. A pregnancy test will be conducted before starting treatment 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 (prolonged pancytopenia, aplastic anemia)
- Severe nausea and vomiting
- Diarrhea
- Fatigue
- Hepatotoxicity
What to Do:
There is no known antidote for temozolomide overdose. Management is supportive and includes close monitoring of blood counts and liver function, and treatment of symptoms. Call 1-800-222-1222 (Poison Control Center) immediately.
Drug Interactions
Major Interactions
- Valproic acid (may decrease temozolomide clearance, leading to increased systemic exposure and potential for increased toxicity)
- Other myelosuppressive agents (additive myelosuppression)
Moderate Interactions
- Phenytoin (potential for altered temozolomide levels, monitor)
- Dexamethasone (commonly co-administered, but monitor for potential interactions)
Monitoring
Baseline Monitoring
Complete Blood Count (CBC) with differential
Rationale: To establish baseline hematopoietic function, as temozolomide causes significant myelosuppression.
Timing: Prior to initiation of treatment.
Liver Function Tests (LFTs)
Rationale: To assess baseline hepatic function, as temozolomide 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
Frequency: Weekly during the concurrent phase (with radiation) and on Day 22 (21 days after the first dose) of each 28-day cycle, and then weekly until ANC >1.5 x 10^9/L and platelet count >100 x 10^9/L.
Target: Absolute Neutrophil Count (ANC) >1.5 x 10^9/L; Platelet count >100 x 10^9/L
Action Threshold: Dose interruption or reduction if ANC <1.5 x 10^9/L or platelet count <100 x 10^9/L. Significant dose reduction or discontinuation for severe myelosuppression.
Liver Function Tests (LFTs)
Frequency: Periodically during treatment, especially if clinically indicated.
Target: Within normal limits or stable from baseline.
Action Threshold: Elevations in transaminases or bilirubin may require dose modification or discontinuation.
Symptom Monitoring
- Nausea and vomiting (common, often managed with antiemetics)
- Fatigue
- Headache
- Constipation or diarrhea
- Anorexia
- Rash
- Fever, chills, signs of infection (due to myelosuppression)
- Unusual bleeding or bruising (due to thrombocytopenia)
- Neurological changes (e.g., seizures, cognitive changes, vision changes)
- Signs of opportunistic infections (e.g., Pneumocystis jirovecii pneumonia - PCP prophylaxis is often recommended)
Special Patient Groups
Pregnancy
Temozolomide can cause fetal harm when administered to a pregnant woman. It is genotoxic and teratogenic in animals. Advise pregnant women of the potential risk to the fetus. Women of reproductive potential should use effective contraception during treatment and for at least 6 months after the last dose. Males with female partners of reproductive potential should 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 organogenesis.
Second Trimester:
Risk of fetal growth restriction and other developmental abnormalities.
Third Trimester:
Risk of fetal growth restriction and potential for adverse effects on developing organ systems.
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 potential carcinogenicity.
Pediatric Use
Safety and effectiveness have not been established in pediatric patients. Limited data suggest that temozolomide may be used in children ≥3 years old with recurrent or refractory brain tumors, but dosing and toxicity profiles may differ from adults. Close monitoring for myelosuppression is crucial.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly patients (≥65 years) and younger patients in clinical trials, but greater sensitivity of some older individuals cannot be ruled out. Elderly patients may be more susceptible to myelosuppression and should be monitored closely.
Clinical Information
Clinical Pearls
- Temozolomide is a prodrug that undergoes non-enzymatic conversion to its active form, MTIC, which simplifies its metabolism and reduces potential for CYP450 interactions.
- Administering temozolomide at bedtime on an empty stomach can help mitigate nausea and vomiting, which are common side effects.
- Pneumocystis jirovecii pneumonia (PCP) prophylaxis is strongly recommended for all patients receiving temozolomide with concomitant radiation therapy, and should be considered for patients receiving adjuvant temozolomide, especially those with lymphopenia.
- Patients should be educated on the importance of strict adherence to the dosing schedule and the need for frequent blood count monitoring due to the risk of severe myelosuppression.
- Capsules should not be opened or crushed due to the irritant nature of the drug and potential for exposure.
Alternative Therapies
- Lomustine (CCNU)
- Carmustine (BCNU)
- Procarbazine
- Vincristine
- Bevacizumab
- Radiation therapy alone
- Tumor Treating Fields (Optune)
Cost & Coverage
Average Cost:
Varies widely, typically several thousand USD per 5-day cycle
Generic Available:
Yes
Insurance Coverage:
Specialty Tier (requires prior authorization, often covered by major medical plans for approved indications)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, 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. If you have any questions or concerns about your medication, don't hesitate to discuss them with 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 reporting the incident, be prepared to provide detailed information, including the name of the medication taken, the amount, and the time it occurred.