Temodar 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 is often given along with radiation therapy or after surgery.
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.
Taking your medication with food may help prevent stomach upset. Your doctor may also recommend taking it at bedtime.
In some cases, your doctor may prescribe other medications to help minimize side effects. Be sure to take these medications as directed.
Swallow your medication whole with a full glass of water. Do not chew, break, crush, or dissolve the capsules.
Continue taking your medication as prescribed 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, consult with your doctor for guidance.
Handling Your Medication: It's essential to handle your medication with care. Consult with your doctor or pharmacist for specific instructions on how to handle your medication safely.
When handling your medication, wear gloves to avoid skin contact. If the capsule is opened or broken, avoid touching the contents. Inhaling the contents or getting them in your eyes can be harmful. 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.
If you miss a dose, contact your doctor to determine the best course of action.
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.
Taking your medication with food may help prevent stomach upset. Your doctor may also recommend taking it at bedtime.
In some cases, your doctor may prescribe other medications to help minimize side effects. Be sure to take these medications as directed.
Swallow your medication whole with a full glass of water. Do not chew, break, crush, or dissolve the capsules.
Continue taking your medication as prescribed 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, consult with your doctor for guidance.
Handling Your Medication: It's essential to handle your medication with care. Consult with your doctor or pharmacist for specific instructions on how to handle your medication safely.
When handling your medication, wear gloves to avoid skin contact. If the capsule is opened or broken, avoid touching the contents. Inhaling the contents or getting them in your eyes can be harmful. 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.
If you miss a dose, contact your doctor to determine the best course of action.
Lifestyle & Tips
- Take the capsules on an empty stomach, at least one hour before or two hours after a meal, preferably at bedtime to reduce nausea.
- 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.
- Do not take a double dose if you miss one. Take the next dose at the regularly scheduled time.
- Avoid live vaccines during treatment and for a period after, as your immune system will be weakened.
- Use effective contraception during treatment and for at least 6 months after for females and 3 months after for males, as temozolomide can cause birth defects.
- Stay well-hydrated to help prevent side effects.
- Report any signs of infection (fever, chills, sore throat) immediately.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
Varies significantly based on indication and concomitant therapy. For newly diagnosed glioblastoma multiforme (GBM) with concomitant radiotherapy: 75 mg/m² orally once daily for 42 days, followed by 4 weeks rest, then 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_gbm_concomitant:
75 mg/m² daily for 42 days (with radiotherapy), then 150-200 mg/m² daily for 5 days every 28 days for 6 cycles.
refractory_anaplastic_astrocytoma:
150 mg/m² daily for 5 days every 28 days, increasing to 200 mg/m² if tolerated.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Dosing is individualized based on body surface area and indication, typically for children >3 years old. Similar to adult dosing regimens for specific brain tumors, but requires careful monitoring.
Adolescent:
Dosing is individualized based on body surface area and indication, similar to adult dosing regimens for specific brain tumors.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment required.
Moderate:
No specific dose adjustment required.
Severe:
Use with caution; no specific dose recommendations available. Consider risk-benefit.
Dialysis:
Not available; temozolomide is rapidly hydrolyzed, and dialysis efficacy is unknown.
Hepatic Impairment:
Mild:
No specific dose adjustment required.
Moderate:
No specific dose adjustment required.
Severe:
Use with caution; no specific dose recommendations available. Consider risk-benefit.
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 proliferating cells, including tumor cells.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 100%
Tmax:
0.5-1.5 hours (oral)
FoodEffect:
Food decreases the rate and extent of absorption (Cmax decreased by 33%, AUC by 9%). Should be taken on an empty stomach.
Distribution:
Vd:
0.4 L/kg (approximately 10.5 L)
ProteinBinding:
10-15%
CnssPenetration:
Yes (readily crosses the blood-brain barrier)
Elimination:
HalfLife:
1.8 hours (parent drug)
Clearance:
Not available (rapid non-enzymatic conversion)
ExcretionRoute:
Renal (approximately 38% of dose excreted in urine over 7 days, with 5-10% as unchanged drug and the remainder as metabolites)
Unchanged:
5-10%
Pharmacodynamics
OnsetOfAction:
Rapid (due to quick conversion to active metabolite)
PeakEffect:
Not directly applicable as effect is cumulative DNA damage, but peak plasma levels of MTIC occur shortly after Tmax of temozolomide.
DurationOfAction:
Related to the persistence of DNA damage, which can lead to cell death over days to weeks.
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 hospitalization and/or death. Patients should have baseline and weekly complete blood counts (CBCs) with differential and platelet counts during the concomitant phase and on Day 22 of each cycle and prior to each subsequent cycle during the adjuvant phase. Dose reductions or interruptions may be necessary.
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, 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 and potentially life-threatening 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 may not experience any side effects or only minor ones, it is 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 advice:
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
Changes in taste
Weight gain
Common cold symptoms
Mouth irritation or mouth sores
This list is not exhaustive, and you may experience other side effects not mentioned here. 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 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, 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 and potentially life-threatening 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 may not experience any side effects or only minor ones, it is 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 advice:
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
Changes in taste
Weight gain
Common cold symptoms
Mouth irritation or mouth sores
This list is not exhaustive, and you may experience other side effects not mentioned here. 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
- Unusual bleeding or bruising
- Severe fatigue or weakness
- Persistent nausea, vomiting, or diarrhea
- Severe headache or new seizures
- Yellowing of skin or eyes (jaundice)
- Dark urine or pale stools
- Signs of allergic reaction (rash, itching, swelling, severe dizziness, trouble breathing)
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. Be sure to describe the allergic reaction and its 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 1 week after your last dose.
To ensure safe treatment, tell your doctor and pharmacist about:
All medications you are taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins.
Any existing health problems.
It is crucial to verify that it is safe to take this medication with all your other medications and health conditions. Do not start, stop, or change the dose of any medication without first consulting 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. Be sure to describe the allergic reaction and its 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 1 week after your last dose.
To ensure safe treatment, tell your doctor and pharmacist about:
All medications you are taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins.
Any existing health problems.
It is crucial to verify that it is safe to take this medication with all your other medications and health conditions. Do not start, stop, or change the dose of any medication without first consulting your doctor.
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 individuals who have infections, colds, or flu.
Additionally, you may be more prone to bleeding easily. To minimize this risk, be cautious and avoid injuries. Use a soft-bristled toothbrush and an electric razor for shaving.
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 likely to experience side effects.
This medication may affect fertility in men. Discuss this potential risk 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 required 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 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 individuals who have infections, colds, or flu.
Additionally, you may be more prone to bleeding easily. To minimize this risk, be cautious and avoid injuries. Use a soft-bristled toothbrush and an electric razor for shaving.
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 likely to experience side effects.
This medication may affect fertility in men. Discuss this potential risk 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 required 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 (e.g., profound leukopenia, thrombocytopenia, pancytopenia)
- Severe gastrointestinal toxicity (e.g., nausea, vomiting, diarrhea)
What to Do:
There is no known antidote for temozolomide overdose. Management is supportive, including close monitoring of blood counts and appropriate medical interventions (e.g., transfusions, antiemetics, antibiotics for infection). Call 1-800-222-1222 (Poison Control Center) or seek immediate medical attention.
Drug Interactions
Major Interactions
- Valproic acid (decreases temozolomide clearance, potentially increasing myelosuppression)
- Live or attenuated vaccines (due to immunosuppression)
Moderate Interactions
- Other myelosuppressive agents (e.g., other chemotherapies, radiation therapy - additive myelosuppression)
- Phenytoin (potential for decreased phenytoin levels, though not consistently reported)
Monitoring
Baseline Monitoring
Complete Blood Count (CBC) with differential and platelet count
Rationale: To establish baseline hematologic status before initiating myelosuppressive therapy.
Timing: Prior to first dose
Liver Function Tests (LFTs) - AST, ALT, bilirubin
Rationale: To assess baseline hepatic function, as temozolomide is metabolized in the liver and can cause hepatotoxicity.
Timing: Prior to first dose
Renal Function Tests (Creatinine, BUN)
Rationale: To assess baseline renal function, as temozolomide and its metabolites are renally excreted.
Timing: Prior to first dose
Routine Monitoring
Complete Blood Count (CBC) with differential and platelet count
Frequency: Weekly during concomitant phase with radiotherapy; prior to each cycle and on Day 22 of each cycle during adjuvant phase.
Target: 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 (consider dose reduction or delay)
Liver Function Tests (LFTs)
Frequency: Periodically, especially if abnormalities are noted or symptoms of hepatic dysfunction occur.
Target: Within normal limits or stable
Action Threshold: Significant elevation (e.g., >3-5x ULN) may require dose modification or discontinuation.
Renal Function Tests
Frequency: Periodically, especially if abnormalities are noted.
Target: Within normal limits or stable
Action Threshold: Significant decline 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, confusion, weakness)
- Signs of infection
- Signs of hepatotoxicity (jaundice, dark urine, abdominal pain)
- Skin reactions (rash)
- Pneumocystis jirovecii pneumonia (PJP) symptoms (cough, dyspnea, fever) - especially if lymphopenia is present
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. 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 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, myelosuppression, 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 one week after the last dose.
Infant Risk:
High risk of serious adverse effects, including myelosuppression and potential carcinogenicity.
Pediatric Use
Safety and effectiveness have been established in pediatric patients 3 years of age and older with refractory anaplastic astrocytoma. Dosing is based on body surface area and requires careful monitoring. Not recommended for children under 3 years due to lack of data.
Geriatric Use
Elderly patients (≥70 years) may be at increased risk of myelosuppression, particularly lymphopenia and thrombocytopenia. Close monitoring of blood counts is essential. No specific dose adjustment is generally required based solely on age, but individual patient tolerance and comorbidities should be considered.
Clinical Information
Clinical Pearls
- Administer temozolomide on an empty stomach to minimize nausea and vomiting, preferably at bedtime.
- Prophylaxis for Pneumocystis jirovecii pneumonia (PJP) is recommended for all patients receiving temozolomide with concomitant radiotherapy, and for patients with lymphopenia during the adjuvant phase.
- Capsules should be swallowed whole; do not open, chew, or crush. If capsules are damaged, avoid contact with skin or mucous membranes.
- Patients should be educated on the signs and symptoms of myelosuppression and instructed to report them immediately.
- Dose adjustments are primarily based on hematologic toxicity (ANC and platelet counts) rather than renal or hepatic impairment, unless severe.
Alternative Therapies
- Lomustine (CCNU)
- Carmustine (BCNU) wafers (Gliadel)
- Procarbazine, Lomustine, Vincristine (PCV regimen)
- Radiation therapy alone
- Surgical resection
Cost & Coverage
Average Cost:
$5,000 - $15,000+ per 30 capsules (100mg)
Generic Available:
Yes
Insurance Coverage:
Tier 3 or 4 (Specialty Drug), often requires prior authorization and may be subject to co-pay assistance programs.
General Drug Facts
If your symptoms or health issues persist or worsen, it's 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 be sure to check with your pharmacist for more information. If you have any questions or concerns about your 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 medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.