Temodar 5mg 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 them from growing and spreading. It's often given in cycles, meaning you take it for a few days, then have a break, and then repeat the cycle.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, it's essential to take it exactly as directed by your doctor. 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 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 your medication on an empty stomach may help minimize stomach upset. Your doctor may also recommend taking it at bedtime.
In some cases, your doctor may prescribe other medications to help prevent side effects when taking this drug.
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're feeling well.
Important Handling Instructions
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.
When handling your medication, take special precautions. Consult your doctor or pharmacist for guidance on how to handle it safely.
Wear gloves when touching your medication to minimize exposure.
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 to determine the best course of action.
To get the most benefit from your medication, it's essential to take it exactly as directed by your doctor. 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 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 your medication on an empty stomach may help minimize stomach upset. Your doctor may also recommend taking it at bedtime.
In some cases, your doctor may prescribe other medications to help prevent side effects when taking this drug.
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're feeling well.
Important Handling Instructions
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.
When handling your medication, take special precautions. Consult your doctor or pharmacist for guidance on how to handle it safely.
Wear gloves when touching your medication to minimize exposure.
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 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 is accidentally opened or damaged, avoid contact with skin or mucous membranes. If contact occurs, wash thoroughly with soap and water.
- Wear gloves when handling the capsules.
- Take anti-nausea medication as prescribed by your doctor.
- Maintain good hydration.
- Report any signs of infection (fever, chills, sore throat) immediately.
- Avoid contact with people who are sick or have infections.
- 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 prior 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 (escalated to 200 mg/m² if tolerated). For refractory anaplastic astrocytoma: 150 mg/m² orally once daily for 5 days, repeated every 28 days (escalated to 200 mg/m² if tolerated).
Dose Range:
75 - 200 mg
Condition-Specific Dosing:
newly_diagnosed_gbm_concomitant:
75 mg/m² orally once daily for 42 days (up to 49 days) with concomitant focal radiotherapy.
newly_diagnosed_gbm_adjuvant:
Initial: 150 mg/m² orally once daily for 5 days, repeated every 28 days for 6 cycles. If tolerated, may escalate to 200 mg/m² for subsequent cycles.
refractory_anaplastic_astrocytoma_initial:
150 mg/m² orally once daily for 5 days, repeated every 28 days. If tolerated, may escalate to 200 mg/m² for subsequent cycles.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established for children under 3 years. For children 3 years and older with refractory anaplastic astrocytoma: Dosing is similar to adults, based on BSA (150-200 mg/m² for 5 days every 28 days), but safety and efficacy are not fully established.
Adolescent:
Dosing is similar to adults, based on BSA (150-200 mg/m² for 5 days every 28 days).
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
No specific dose adjustment recommended.
Severe:
Use with caution; no specific dose recommendations available. Data are limited.
Dialysis:
Not available; use with caution. Temozolomide is a small molecule, but data on dialysis clearance are lacking.
Hepatic Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
No specific dose adjustment recommended.
Severe:
Use with caution; no specific dose recommendations available. Data are limited.
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 apoptosis and cell death, particularly in rapidly dividing cells like cancer 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 (similar to total body water)
ProteinBinding:
10-15%
CnssPenetration:
Yes (readily crosses the blood-brain barrier, achieving concentrations in CSF approximately 30% of plasma AUC)
Elimination:
HalfLife:
1.8 hours (plasma)
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:
Rapid (due to quick conversion to active metabolite)
PeakEffect:
Not directly quantifiable for anti-tumor effect; related to DNA damage over time.
DurationOfAction:
Not directly quantifiable; cytotoxic effects persist as long as DNA damage is present and unrepaired.
Safety & Warnings
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. Many people experience no side effects or only mild ones. If you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical attention if they bother you or persist:
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
Common cold symptoms
* Mouth irritation or mouth sores
This is not an exhaustive list of possible side effects. 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 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. Many people experience no side effects or only mild ones. If you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical attention if they bother you or persist:
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
Common cold symptoms
* Mouth irritation or mouth sores
This is not an exhaustive list of possible side effects. 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)
- Chills
- Sore throat
- Unusual bleeding or bruising
- Extreme fatigue or weakness
- Severe nausea or vomiting that doesn't improve with medication
- Severe headache
- Seizures
- Changes in vision or speech
- Yellowing of skin or eyes (jaundice)
- Dark urine
- Severe rash or skin reactions
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.
Potential Interactions with Other Medications or Health Conditions
This medication may interact with other medications or health problems. To ensure your safety, it is crucial to:
Inform your doctor and pharmacist about all medications you are taking, including prescription and over-the-counter medications, natural products, and vitamins.
Discuss your health problems with your doctor.
Verify that it is safe to take this medication with your other medications and health conditions.
Do not start, stop, or change the dose of any medication without 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.
Potential Interactions with Other Medications or Health Conditions
This medication may interact with other medications or health problems. To ensure your safety, it is crucial to:
Inform your doctor and pharmacist about all medications you are taking, including prescription and over-the-counter medications, natural products, and vitamins.
Discuss your health problems with your doctor.
Verify that it is safe to take this medication with your other medications and health conditions.
Do not start, stop, or change the dose of any medication without 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 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 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 can increase the risk of bleeding. To minimize this risk, use a soft toothbrush, an electric razor, and avoid injuries.
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 this potential side effect with your doctor.
This medication is present in semen, so 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 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 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 can increase the risk of bleeding. To minimize this risk, use a soft toothbrush, an electric razor, and avoid injuries.
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 this potential side effect with your doctor.
This medication is present in semen, so 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 (bone marrow suppression leading to very low white blood cell, red blood cell, and platelet counts)
- Fatigue
- Nausea
- Vomiting
- Diarrhea
What to Do:
There is no known antidote for temozolomide overdose. Management is supportive, including close monitoring of blood counts and administration of blood products or growth factors as needed. Call 1-800-222-1222 (Poison Control) immediately or seek emergency medical attention.
Drug Interactions
Major Interactions
- Valproic acid (may decrease temozolomide clearance, requiring dose reduction of temozolomide)
- Other myelosuppressive agents (additive myelosuppression)
Moderate Interactions
- Phenytoin (potential for altered temozolomide levels, though not well-established)
- Dexamethasone (commonly co-administered, but can increase risk of hyperglycemia and other steroid-related side effects)
Monitoring
Baseline Monitoring
Complete Blood Count (CBC) with differential and platelets
Rationale: To establish baseline hematologic parameters before initiating myelosuppressive therapy.
Timing: Within 1 week prior to initiation of treatment.
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 initiation of treatment.
Renal Function Tests (RFTs) - Creatinine, BUN
Rationale: To assess baseline renal function, as temozolomide and its metabolites are renally excreted.
Timing: Prior to initiation of treatment.
Routine Monitoring
Complete Blood Count (CBC) with differential and platelets
Frequency: Weekly during concomitant phase with radiation; on Day 22 (Day 1 of next cycle) and weekly until ANC >1.5 x 10^9/L and platelets >100 x 10^9/L during adjuvant phase.
Target: ANC >1.5 x 10^9/L, Platelets >100 x 10^9/L
Action Threshold: ANC <1.5 x 10^9/L or Platelets <100 x 10^9/L (requires dose modification or delay).
Liver Function Tests (LFTs)
Frequency: Periodically during treatment, especially with prolonged use.
Target: Within normal limits or stable baseline.
Action Threshold: Significant elevations (e.g., >3-5x ULN) may require dose modification or discontinuation.
Symptom Monitoring
- Nausea
- Vomiting
- Fatigue
- Headache
- Constipation
- Diarrhea
- Alopecia
- Rash
- Fever
- Chills
- Sore throat (signs of infection due to myelosuppression)
- Unusual bleeding or bruising (signs of thrombocytopenia)
- Shortness of breath or pallor (signs of anemia)
- Signs of opportunistic infections (e.g., Pneumocystis jirovecii pneumonia, especially with concomitant steroids)
Special Patient Groups
Pregnancy
Temozolomide can cause fetal harm when administered to a pregnant woman. It is classified as Pregnancy Category D. Advise pregnant women of the potential risk to a fetus. Females of reproductive potential should be advised to use effective contraception during treatment and for at least 6 months after the last dose. Males with female partners of reproductive potential should be advised to use effective contraception during treatment and for at least 3 months after the last dose.
Trimester-Specific Risks:
First Trimester:
Highest risk of major congenital malformations and fetal loss due to organogenesis.
Second Trimester:
Risk of fetal growth restriction, myelosuppression, and other adverse effects.
Third Trimester:
Risk of fetal myelosuppression and other adverse effects.
Lactation
It is not known whether temozolomide or its metabolites are excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in breastfed infants from temozolomide, a decision should be made whether to discontinue breastfeeding or to discontinue the drug, taking into account the importance of the drug to the mother. Lactation risk is L5 (Contraindicated).
Infant Risk:
High risk of serious adverse effects, including myelosuppression, in the breastfed infant.
Pediatric Use
Safety and effectiveness in pediatric patients under 3 years of age have not been established. In pediatric patients 3 years of age and older, experience is limited, and dosing is generally based on BSA, similar to adults. Myelosuppression is a significant concern.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly patients and younger patients. However, elderly patients (≥70 years) may be at increased risk of myelosuppression and infection, 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 pharmacokinetic profile and reduces drug-drug interactions related to CYP450 enzymes.
- Administering temozolomide at bedtime on an empty stomach can help mitigate nausea and vomiting, which are common side effects.
- Prophylaxis for Pneumocystis jirovecii pneumonia (PJP) is recommended for all patients receiving temozolomide with concomitant radiotherapy, and for patients receiving temozolomide in the adjuvant phase who are also on corticosteroids, due to the increased risk of opportunistic infections.
- Dose adjustments are primarily based on nadir blood counts (lowest blood cell counts) during the previous cycle, not on baseline values.
- Capsules must not be opened, chewed, or crushed due to the cytotoxic nature of the drug and potential for exposure.
Alternative Therapies
- Radiation therapy (often used concomitantly or as primary treatment)
- Other alkylating agents (e.g., Lomustine, Carmustine - though less common for primary brain tumors)
- Targeted therapies (e.g., Bevacizumab for recurrent GBM)
- Tumor Treating Fields (TTFields, Optune) in combination with temozolomide for newly diagnosed GBM.
- Surgical resection
Cost & Coverage
Average Cost:
Not available Not available
Generic Available:
Yes
Insurance Coverage:
Tier 4 (Specialty Drug) or higher, often requiring prior authorization and medical necessity documentation.
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 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 medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to facilitate prompt and effective treatment.