Temozolomide 100mg 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 slow or stop their growth. It's often taken as capsules by mouth.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely.
Take your medication at the same time every day.
You can take your medication 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 choose to take it on an empty stomach, always take it on an empty stomach. Taking it on an empty stomach may help prevent stomach upset.
Consider taking your medication at bedtime, as this may also help minimize stomach upset. However, consult with your doctor before making any changes to your dosing schedule.
Your doctor may prescribe other medications to be taken with this drug to help reduce side effects.
Swallow your medication whole with a full glass of water. Do not chew, break, crush, or dissolve the capsules.
Continue taking your medication as directed by your doctor or healthcare provider, even if you start feeling well.
Important Handling Instructions
Your 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.
Handle your medication with care. Consult your doctor or pharmacist for specific guidance on handling this medication.
Wear gloves when touching the capsules.
If a 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 for guidance on what to do next.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely.
Take your medication at the same time every day.
You can take your medication 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 choose to take it on an empty stomach, always take it on an empty stomach. Taking it on an empty stomach may help prevent stomach upset.
Consider taking your medication at bedtime, as this may also help minimize stomach upset. However, consult with your doctor before making any changes to your dosing schedule.
Your doctor may prescribe other medications to be taken with this drug to help reduce side effects.
Swallow your medication whole with a full glass of water. Do not chew, break, crush, or dissolve the capsules.
Continue taking your medication as directed by your doctor or healthcare provider, even if you start feeling well.
Important Handling Instructions
Your 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.
Handle your medication with care. Consult your doctor or pharmacist for specific guidance on handling this medication.
Wear gloves when touching the capsules.
If a 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 for guidance on what to do next.
Lifestyle & Tips
- Take the capsules on an empty stomach (at least 1 hour before or 2 hours after a meal) to reduce nausea, or consistently with food if that helps manage side effects.
- Take the capsules at the same time each day, preferably at bedtime to minimize nausea and vomiting.
- Swallow capsules whole with a glass of water. Do not open, chew, or crush the capsules.
- Wear gloves if handling broken capsules to avoid skin contact.
- Stay well-hydrated by drinking plenty of fluids.
- Avoid contact with people who are sick or have infections, as your immune system will be weakened.
- Report any signs of infection (fever, chills, sore throat) immediately.
- Use effective contraception during treatment and for at least 6 months after for males and 6 months after for females, as temozolomide can cause birth defects.
Available Forms & Alternatives
Available Strengths:
- Temozolomide 100mg Capsules
- Temozolomide 5mg Capsules
- Temozolomide 5mg Capsules
- Temozolomide 250mg Capsules
- Temozolomide 20mg Capsules
- Temozolomide 180mg Capsules
- Temozolomide 140mg Capsules
- Temozolomide 20mg Capsules
- Temozolomide 100mg Capsules
- Temozolomide 140mg Capsules
- Temozolomide 180mg Capsules
- Temozolomide 250mg Capsules
- Temozolomide 250mg Capsules
Dosing & Administration
Adult Dosing
Standard Dose:
For newly diagnosed glioblastoma multiforme: Concomitant phase: 75 mg/m² orally once daily for 42 days (up to 49 days) with concomitant focal radiotherapy. Adjuvant phase: 150-200 mg/m² orally once daily for 5 days every 28 days for 6 cycles.
Dose Range:
75 - 200 mg
Condition-Specific Dosing:
anaplasticAstrocytoma:
Initial: 150 mg/m² orally once daily for 5 days every 28 days. If well tolerated, increase to 200 mg/m² for subsequent cycles.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
For refractory high-grade glioma (off-label): Dosing varies, often 150-200 mg/m² orally once daily for 5 days every 28 days, or 75 mg/m² daily for 42 days with radiation.
Adolescent:
For newly diagnosed glioblastoma multiforme: Dosing generally follows adult guidelines (75 mg/m² daily with radiation, then 150-200 mg/m² for 5 days every 28 days).
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment required.
Moderate:
No specific dose adjustment required.
Severe:
Use with caution; data are limited. Monitor hematologic parameters closely.
Dialysis:
Not available; temozolomide is dialyzable, but clinical data are limited. Use with caution and close monitoring.
Hepatic Impairment:
Mild:
No specific dose adjustment required.
Moderate:
No specific dose adjustment required.
Severe:
Use with caution; data are limited. Monitor hematologic parameters closely.
Confidence:
High
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 the active alkylating metabolite, which primarily methylates DNA at the O6 and N7 positions of guanine. This DNA methylation leads to DNA strand breaks and ultimately triggers apoptosis, inhibiting tumor cell proliferation.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 100%
Tmax:
0.5-1.5 hours
FoodEffect:
Food decreases Cmax by 33% and AUC by 9%, but this is not considered clinically significant for efficacy. Can be taken with or without food, but consistently.
Distribution:
Vd:
Approximately 0.4 L/kg
ProteinBinding:
10-15%
CnssPenetration:
Yes
Elimination:
HalfLife:
Approximately 1.8 hours
Clearance:
Not available (primarily non-enzymatic conversion)
ExcretionRoute:
Renal (primarily), Fecal
Unchanged:
Approximately 38% (renal)
Pharmacodynamics
OnsetOfAction:
Rapid (due to quick conversion to active metabolite)
PeakEffect:
Not directly applicable for chemotherapy; peak plasma concentration of active metabolite occurs within 1-2 hours.
DurationOfAction:
Not directly applicable; effects are cumulative over treatment cycles.
Confidence:
High
Safety & Warnings
BLACK BOX WARNING
Myelosuppression: Temozolomide causes severe myelosuppression, including prolonged pancytopenia, which can result in aplastic anemia, and may lead to hospitalization and death. Patients should have a baseline ANC ≥ 1.5 x 10^9/L and platelet count ≥ 100 x 10^9/L before dosing. Obtain a CBC on Day 22 (21 days after the first dose) or within 48 hours of dosing, and weekly thereafter until ANC > 1.5 x 10^9/L and platelet count > 100 x 10^9/L. Do not administer temozolomide if ANC < 1.5 x 10^9/L or platelet count < 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 won't 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, trouble speaking or thinking, balance changes, drooping on one side of the face, or blurred vision
Confusion or mood changes
Difficulty 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
Breast pain
Signs of severe liver problems, including:
+ Dark urine
+ Fatigue or decreased appetite
+ Nausea or stomach pain
+ Light-colored stools or vomiting
+ Yellowing of the skin or eyes
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people experience no side effects or only mild 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 for guidance:
Hair loss
Headache
Dizziness, drowsiness, fatigue, or weakness
Constipation, diarrhea, stomach pain, nausea, vomiting, or decreased appetite
Sleep disturbances
Back, muscle, or joint pain
Dry skin
Changes in taste
Weight gain
Common cold symptoms
Mouth irritation or mouth sores
This list is not exhaustive. If you have questions or concerns about side effects, consult 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 won't 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, trouble speaking or thinking, balance changes, drooping on one side of the face, or blurred vision
Confusion or mood changes
Difficulty 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
Breast pain
Signs of severe liver problems, including:
+ Dark urine
+ Fatigue or decreased appetite
+ Nausea or stomach pain
+ Light-colored stools or vomiting
+ Yellowing of the skin or eyes
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people experience no side effects or only mild 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 for guidance:
Hair loss
Headache
Dizziness, drowsiness, fatigue, or weakness
Constipation, diarrhea, stomach pain, nausea, vomiting, or decreased appetite
Sleep disturbances
Back, muscle, or joint pain
Dry skin
Changes in taste
Weight gain
Common cold symptoms
Mouth irritation or mouth sores
This list is not exhaustive. If you have questions or concerns about side effects, consult 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, cough, or other signs of infection
- Unusual bleeding or bruising
- Extreme tiredness or weakness
- Severe nausea, vomiting, or diarrhea that doesn't improve
- Yellowing of the skin or eyes (jaundice)
- Dark urine or pale stools
- Severe headache or new neurological symptoms
- Skin rash or severe allergic reaction
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. Be sure to discuss your test results with your doctor.
Before receiving any vaccinations, consult with your doctor, as some 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, talk to 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 concerns, discuss them with your doctor.
You may be more susceptible to infections due to this medication. To reduce the risk of infection, wash your hands frequently and avoid close contact with people who have infections, colds, or flu.
Be cautious, as this medication can increase the risk of bleeding. Use a soft toothbrush and an electric razor to minimize the risk of injury. Rarely, this medication can cause severe bone marrow problems or 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 this potential risk with your doctor.
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 harm 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 specified 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 some 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, talk to 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 concerns, discuss them with your doctor.
You may be more susceptible to infections due to this medication. To reduce the risk of infection, wash your hands frequently and avoid close contact with people who have infections, colds, or flu.
Be cautious, as this medication can increase the risk of bleeding. Use a soft toothbrush and an electric razor to minimize the risk of injury. Rarely, this medication can cause severe bone marrow problems or 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 this potential risk with your doctor.
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 harm 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 specified 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 (pancytopenia, aplastic anemia)
- Severe nausea and vomiting
- Diarrhea
- Fatigue
- Liver toxicity
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 blood products or growth factors as needed. Call 1-800-222-1222 (Poison Control Center) immediately.
Drug Interactions
Moderate Interactions
- Valproic acid
Monitoring
Baseline Monitoring
Complete Blood Count (CBC) with differential and platelets
Rationale: To establish baseline hematologic status and assess bone marrow reserve, as myelosuppression is a dose-limiting toxicity.
Timing: Prior to initiation of treatment.
Liver Function Tests (LFTs) including AST, ALT, bilirubin
Rationale: To assess baseline hepatic function, as liver toxicity can occur.
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 21 days after previous dose) during adjuvant phase.
Target: Absolute Neutrophil Count (ANC) ≥ 1.5 x 10^9/L, Platelets ≥ 100 x 10^9/L for dose continuation/initiation.
Action Threshold: ANC < 1.5 x 10^9/L or Platelets < 100 x 10^9/L: Hold or reduce dose. ANC < 1.0 x 10^9/L or Platelets < 50 x 10^9/L: Hold dose and consider dose reduction upon recovery.
Liver Function Tests (LFTs)
Frequency: Prior to each cycle or as clinically indicated.
Target: Within normal limits or stable.
Action Threshold: Significant elevations (e.g., >3-5x ULN): Investigate and consider dose modification or discontinuation.
Renal Function Tests
Frequency: Prior to each cycle or as clinically indicated.
Target: Within normal limits or stable.
Action Threshold: Significant impairment: Use with caution.
Pneumocystis jirovecii Pneumonia (PJP) prophylaxis
Frequency: Throughout concomitant phase and for 28 days after last dose, or longer if lymphopenia persists.
Target: Not applicable (prophylaxis)
Action Threshold: Not applicable (prophylaxis)
Symptom Monitoring
- Signs of myelosuppression (fever, chills, sore throat, unusual bleeding/bruising, fatigue)
- Signs of infection (fever, cough, dyspnea)
- Nausea, vomiting, constipation, diarrhea
- Headache, fatigue, dizziness
- Skin rash
- Signs of liver dysfunction (jaundice, dark urine, abdominal pain)
- Signs of opportunistic infections (e.g., PJP, CMV, HSV, fungal infections)
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 the fetus. Females 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 6 months after the last dose.
Trimester-Specific Risks:
First Trimester:
High risk of major birth defects and fetal loss due to its genotoxic and cytotoxic effects.
Second Trimester:
Continued risk of fetal harm, including growth restriction and organ toxicity.
Third Trimester:
Continued risk of fetal harm, including myelosuppression in the neonate.
Confidence Trimester:
High
Lactation
Lactation Risk Category L5 (Contraindicated). 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 in pediatric patients have not been established for newly diagnosed glioblastoma. However, temozolomide has been used off-label in pediatric patients with high-grade gliomas. Dosing is often weight-based or body surface area-based. Pediatric patients may be more susceptible to myelosuppression and other toxicities. Close monitoring of blood counts is essential.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly patients (≥65 years) and younger patients in clinical trials. However, elderly patients may be more susceptible to myelosuppression and other adverse effects. Dose adjustments are generally not required based on age alone, but careful monitoring is warranted.
Clinical Information
Clinical Pearls
- Temozolomide capsules should be swallowed whole with a glass of water. Do not open, chew, or crush them. If capsules are accidentally opened or damaged, avoid contact with skin or mucous membranes. If contact occurs, wash thoroughly with water.
- Administer temozolomide on an empty stomach (at least one hour before or two hours after a meal) to minimize nausea and vomiting, or consistently with food if that helps manage GI side effects.
- Prophylaxis for Pneumocystis jirovecii Pneumonia (PJP) is strongly recommended during the concomitant phase of treatment and for at least 28 days after the last dose, or longer if lymphopenia persists, due to the risk of opportunistic infections.
- Myelosuppression is the dose-limiting toxicity. Close and frequent monitoring of CBC with differential and platelets is crucial, especially during the adjuvant phase.
- Patients should be educated on signs of myelosuppression (fever, bleeding, bruising) and instructed to report them immediately.
- Consider antiemetic prophylaxis (e.g., 5-HT3 antagonists) to manage nausea and vomiting, which are common side effects.
Alternative Therapies
- Surgery (resection of tumor)
- Radiation therapy
- Other chemotherapy agents (e.g., carmustine wafers, lomustine)
- Targeted therapies (e.g., bevacizumab)
- Tumor Treating Fields (TTFields, Optune)
- Clinical trials investigating novel agents or combinations
Cost & Coverage
Average Cost:
Varies widely, typically several thousand USD per 30 capsules
Generic Available:
Yes
Insurance Coverage:
Specialty Tier / Tier 4 (requires prior authorization, often covered under medical benefit for oncology)
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 is a good idea to consult with your pharmacist. If you have any questions or concerns about this medication, do not 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 quantity, and the time it occurred.