Topotecan 4mg Inj, 1 Vial
WARNING: Low blood cell counts may happen with this drug. Low blood cell counts may raise the chance of needing a blood transfusion or getting an infection or bleeding. If you have questions, talk with the doctor.Have your blood work and other lab tests checked as you have been told by your doctor. @ COMMON USES: It is used to treat cancer.
Drug Class
Antineoplastic agent
Pharmacologic Class
Topoisomerase I inhibitor
Pregnancy Category
Category D
FDA Approved
May 1996
DEA Schedule
Not Controlled
Overview
What is this medicine?
Topotecan is a chemotherapy medicine used to treat certain types of cancer, including ovarian, lung, and cervical cancer. It works by stopping cancer cells from growing and dividing, which helps to shrink tumors.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided to you. It is essential to follow the instructions carefully. This medication is administered as an infusion into a vein over a specified period.
Storing and Disposing of Your Medication
If you need to store this medication at home, consult with your doctor, nurse, or pharmacist to determine the proper storage procedure.
Missing a Dose
If you miss a dose, contact your doctor to receive guidance on the next steps to take.
To use this medication correctly, follow your doctor's instructions and read all the information provided to you. It is essential to follow the instructions carefully. This medication is administered as an infusion into a vein over a specified period.
Storing and Disposing of Your Medication
If you need to store this medication at home, consult with your doctor, nurse, or pharmacist to determine the proper storage procedure.
Missing a Dose
If you miss a dose, contact your doctor to receive guidance on the next steps to take.
Lifestyle & Tips
- Avoid contact with people who are sick or have infections, as your immune system will be weakened.
- Practice good hand hygiene.
- Report any signs of fever, chills, or infection immediately.
- Avoid activities that could cause bleeding or injury (e.g., contact sports, sharp objects) due to increased risk of bleeding.
- Maintain good oral hygiene to prevent mouth sores.
- Stay well-hydrated and eat a balanced diet as tolerated.
- Discuss any planned vaccinations with your doctor, as live vaccines should be avoided.
- Use effective contraception during treatment and for a period after, as topotecan can harm a developing baby.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Varies by indication. For ovarian cancer/SCLC: 1.5 mg/m² IV daily for 5 consecutive days, repeated every 21 days. For cervical cancer: 0.75 mg/m² IV daily for 3 consecutive days, repeated every 21 days, in combination with cisplatin.
Dose Range:
0.75 - 1.5 mg
Condition-Specific Dosing:
Ovarian Cancer (recurrent):
1.5 mg/m² IV daily for 5 consecutive days, repeated every 21 days.
Small Cell Lung Cancer (SCLC) (recurrent):
1.5 mg/m² IV daily for 5 consecutive days, repeated every 21 days.
Cervical Cancer (in combination with cisplatin):
0.75 mg/m² IV daily for 3 consecutive days, repeated every 21 days.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment for CrCl > 60 mL/min.
Moderate:
For CrCl 20-39 mL/min: Reduce dose by 50% (e.g., 0.75 mg/m² for ovarian/SCLC indications).
Severe:
For CrCl < 20 mL/min: Not recommended due to insufficient data and potential for increased toxicity.
Dialysis:
Not recommended. Topotecan is not significantly removed by hemodialysis.
Hepatic Impairment:
Mild:
No specific adjustment recommended.
Moderate:
No specific adjustment recommended, but use with caution.
Severe:
Not well studied; use with extreme caution or avoid.
Pharmacology
Mechanism of Action
Topotecan is a topoisomerase I inhibitor. It binds to the topoisomerase I-DNA complex, preventing religation of the DNA single-strand breaks. This leads to accumulation of DNA single-strand breaks, which are converted to double-strand breaks during DNA replication, ultimately leading to cell death.
Pharmacokinetics
Absorption:
Bioavailability:
100% (IV administration)
Tmax:
Not applicable (IV bolus/infusion)
FoodEffect:
Not applicable (IV administration)
Distribution:
Vd:
Approximately 60 L/m²
ProteinBinding:
Approximately 35%
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 2-3 hours (lactone form)
Clearance:
Approximately 67 L/h/m²
ExcretionRoute:
Renal (30-60% unchanged), fecal/biliary (minor)
Unchanged:
30-60% (renal)
Pharmacodynamics
OnsetOfAction:
Rapid (systemic exposure achieved immediately after IV administration)
PeakEffect:
Not applicable (continuous cytotoxic effect)
DurationOfAction:
Dependent on exposure and cell cycle effects; cytotoxic effects persist beyond drug elimination.
Safety & Warnings
BLACK BOX WARNING
Topotecan can cause severe myelosuppression, including neutropenia, thrombocytopenia, and anemia. Febrile neutropenia and neutropenic sepsis, sometimes fatal, have occurred. Monitor complete blood counts frequently. Do not administer Topotecan to patients with baseline neutrophil counts less than 1,500 cells/mm³ or platelet counts less than 100,000 cells/mm³.
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 immediate medical attention:
Allergic reactions: Rash, hives, itching, redness, swelling, blistering, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Infections: Fever, chills, severe sore throat, ear or sinus pain, cough, increased or discolored sputum, painful urination, mouth sores, or a wound that won't heal.
Bleeding: Vomiting or coughing up blood, coffee ground-like vomit, blood in the urine, black, red, or tarry stools, gum bleeding, abnormal vaginal bleeding, unexplained bruises, or uncontrollable bleeding.
Severe diarrhea: Diarrhea accompanied by stomach cramps, nausea, vomiting, fever, or excessive fluid loss.
Lung problems: Shortness of breath, difficulty breathing, new or worsening cough, or fever. These lung problems can be life-threatening and require immediate medical attention.
Bowel problems: Stomach pain (with or without fever), tender stomach, or diarrhea. These bowel problems can be severe and potentially life-threatening, and may occur as early as the first day of symptoms.
Tissue damage: If the medication leaks from the vein, it can cause tissue damage. Notify your nurse immediately if you experience redness, burning, pain, swelling, blisters, skin sores, or fluid leakage at the injection site.
Other Possible Side Effects
Most people experience few or no side effects, but some may occur. If you're bothered by any of the following side effects or if they persist, contact your doctor:
Fatigue or weakness
Hair loss
Mouth irritation or sores
Constipation
Stomach pain
* Diarrhea, vomiting, nausea, or decreased appetite (common side effects that may be manageable with guidance from your doctor)
If any of these side effects are severe, persistent, or troublesome, consult your doctor for advice on managing them.
Reporting Side Effects
For any 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 immediate medical attention:
Allergic reactions: Rash, hives, itching, redness, swelling, blistering, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Infections: Fever, chills, severe sore throat, ear or sinus pain, cough, increased or discolored sputum, painful urination, mouth sores, or a wound that won't heal.
Bleeding: Vomiting or coughing up blood, coffee ground-like vomit, blood in the urine, black, red, or tarry stools, gum bleeding, abnormal vaginal bleeding, unexplained bruises, or uncontrollable bleeding.
Severe diarrhea: Diarrhea accompanied by stomach cramps, nausea, vomiting, fever, or excessive fluid loss.
Lung problems: Shortness of breath, difficulty breathing, new or worsening cough, or fever. These lung problems can be life-threatening and require immediate medical attention.
Bowel problems: Stomach pain (with or without fever), tender stomach, or diarrhea. These bowel problems can be severe and potentially life-threatening, and may occur as early as the first day of symptoms.
Tissue damage: If the medication leaks from the vein, it can cause tissue damage. Notify your nurse immediately if you experience redness, burning, pain, swelling, blisters, skin sores, or fluid leakage at the injection site.
Other Possible Side Effects
Most people experience few or no side effects, but some may occur. If you're bothered by any of the following side effects or if they persist, contact your doctor:
Fatigue or weakness
Hair loss
Mouth irritation or sores
Constipation
Stomach pain
* Diarrhea, vomiting, nausea, or decreased appetite (common side effects that may be manageable with guidance from your doctor)
If any of these side effects are severe, persistent, or troublesome, consult your doctor for advice on managing them.
Reporting Side Effects
For any 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 (temperature of 100.4°F or 38°C or higher)
- Chills or shaking
- Sore throat, cough, or difficulty breathing
- Unusual bleeding or bruising (e.g., nosebleeds, bleeding gums, dark or bloody stools, red spots on skin)
- Severe fatigue or weakness
- Severe nausea, vomiting, or diarrhea that does not improve
- Mouth sores or pain when eating/drinking
- Severe abdominal pain
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.
Certain health conditions, such as:
+ Low white blood cell count (leukopenia)
+ Low platelet count (thrombocytopenia)
+ Low red blood cell count (anemia)
If you are breastfeeding, as you should not breastfeed while taking this medication and for 1 week after your last dose.
This medication may interact with other medications or health conditions. Therefore, 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 to ensure it is safe to take this medication.
Never start, stop, or change the dose of any medication without consulting your doctor first.
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.
Certain health conditions, such as:
+ Low white blood cell count (leukopenia)
+ Low platelet count (thrombocytopenia)
+ Low red blood cell count (anemia)
If you are breastfeeding, as you should not breastfeed while taking this medication and for 1 week after your last dose.
This medication may interact with other medications or health conditions. Therefore, 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 to ensure it is safe to take this medication.
Never start, stop, or change the dose of any medication without consulting your doctor first.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
When starting this medication, avoid driving and other activities that require alertness until you understand how it affects you. You may be at a higher risk of developing infections, some of which can be severe or life-threatening. To minimize this risk, practice good hygiene by washing your hands frequently and avoid close contact with individuals who have infections, colds, or flu.
This medication may increase your risk of bleeding. To reduce this risk, be cautious to avoid injuries, use a soft-bristled toothbrush, and consider using an electric razor for shaving.
If you experience diarrhea, consult your doctor before attempting to treat it. Your doctor will provide guidance on the best course of action.
Before receiving any vaccinations, discuss the potential risks and benefits with your doctor, as certain vaccines may not be effective or may increase the risk of infection when taken with this medication.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
This medication may affect fertility, potentially leading to difficulties in becoming pregnant or fathering a child. If you plan to conceive, consult your doctor before initiating treatment.
There is a risk of harm to an unborn baby if you become pregnant while taking this medication. A pregnancy test will be conducted before starting the medication to confirm that you are not pregnant. If you may become pregnant, use effective birth control throughout the treatment period and for 6 months after the last dose, unless otherwise advised by your doctor. It is crucial to understand the duration for which you need to use birth control. If you become pregnant, notify your doctor immediately.
If your partner may become pregnant, you may need to use birth control during treatment and for a period after the last dose. Consult your doctor to determine the best approach.
When starting this medication, avoid driving and other activities that require alertness until you understand how it affects you. You may be at a higher risk of developing infections, some of which can be severe or life-threatening. To minimize this risk, practice good hygiene by washing your hands frequently and avoid close contact with individuals who have infections, colds, or flu.
This medication may increase your risk of bleeding. To reduce this risk, be cautious to avoid injuries, use a soft-bristled toothbrush, and consider using an electric razor for shaving.
If you experience diarrhea, consult your doctor before attempting to treat it. Your doctor will provide guidance on the best course of action.
Before receiving any vaccinations, discuss the potential risks and benefits with your doctor, as certain vaccines may not be effective or may increase the risk of infection when taken with this medication.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
This medication may affect fertility, potentially leading to difficulties in becoming pregnant or fathering a child. If you plan to conceive, consult your doctor before initiating treatment.
There is a risk of harm to an unborn baby if you become pregnant while taking this medication. A pregnancy test will be conducted before starting the medication to confirm that you are not pregnant. If you may become pregnant, use effective birth control throughout the treatment period and for 6 months after the last dose, unless otherwise advised by your doctor. It is crucial to understand the duration for which you need to use birth control. If you become pregnant, notify your doctor immediately.
If your partner may become pregnant, you may need to use birth control during treatment and for a period after the last dose. Consult your doctor to determine the best approach.
Overdose Information
Overdose Symptoms:
- Severe myelosuppression (profound neutropenia, thrombocytopenia, anemia)
- Severe gastrointestinal toxicity (mucositis, diarrhea)
What to Do:
There is no known antidote for topotecan overdose. Management is supportive, including close monitoring of blood counts, administration of blood products as needed, and aggressive management of infections and gastrointestinal symptoms. Call 1-800-222-1222 (Poison Control Center) for further guidance.
Drug Interactions
Major Interactions
- Myelosuppressive agents (e.g., other chemotherapies, radiation therapy): Increased risk of severe myelosuppression.
- G-CSF (Granulocyte Colony-Stimulating Factor): Concurrent administration may prolong myelosuppression. Administer G-CSF at least 24 hours after completion of topotecan administration.
Moderate Interactions
- Strong CYP3A4 inhibitors/inducers: May theoretically alter metabolism, though topotecan's metabolism via CYP3A4 is minor.
- Live vaccines: Increased risk of infection due to immunosuppression.
Monitoring
Baseline Monitoring
Complete Blood Count (CBC) with differential and platelet count
Rationale: To establish baseline hematologic parameters and assess for pre-existing myelosuppression, which is a dose-limiting toxicity.
Timing: Prior to initiation of treatment.
Renal function tests (serum creatinine, CrCl)
Rationale: Topotecan is primarily renally eliminated; dose adjustments are required for renal impairment.
Timing: Prior to initiation of treatment.
Hepatic function tests (ALT, AST, bilirubin)
Rationale: To assess baseline liver function, as hepatic impairment may affect drug clearance.
Timing: Prior to initiation of treatment.
Routine Monitoring
Complete Blood Count (CBC) with differential and platelet count
Frequency: Weekly or prior to each cycle, and as clinically indicated.
Target: Absolute Neutrophil Count (ANC) ≥ 1,500 cells/mm³, Platelets ≥ 100,000 cells/mm³ (for next cycle initiation).
Action Threshold: Hold dose if ANC < 1,500 cells/mm³ or platelets < 100,000 cells/mm³; consider dose reduction for subsequent cycles based on nadir counts and duration of myelosuppression.
Renal function tests
Frequency: Periodically, or as clinically indicated.
Target: Not applicable (monitor for changes)
Action Threshold: Adjust dose if CrCl falls to 20-39 mL/min; discontinue if CrCl < 20 mL/min.
Hepatic function tests
Frequency: Periodically, or as clinically indicated.
Target: Not applicable (monitor for changes)
Action Threshold: Monitor closely for worsening function; consider dose modification or discontinuation if severe hepatic dysfunction develops.
Symptom Monitoring
- Signs of infection (fever, chills, sore throat, cough)
- Unusual bleeding or bruising (petechiae, epistaxis, melena)
- Severe fatigue or weakness
- Severe nausea, vomiting, or diarrhea
- Abdominal pain
- Oral mucositis/stomatitis
- Skin rash
Special Patient Groups
Pregnancy
Topotecan 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 the fetus. Women of childbearing potential should be advised to use effective contraception during treatment.
Trimester-Specific Risks:
First Trimester:
High risk of major birth defects and fetal loss due to rapid cell division during organogenesis.
Second Trimester:
Risk of fetal growth restriction, myelosuppression, and other adverse effects.
Third Trimester:
Risk of fetal myelosuppression and other adverse effects; potential for premature birth.
Lactation
It is not known whether topotecan is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants, breastfeeding is contraindicated during topotecan treatment.
Infant Risk:
High risk of serious adverse effects, including myelosuppression, in the nursing infant.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Limited data suggest similar toxicities as in adults, particularly myelosuppression.
Geriatric Use
Clinical studies did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. However, elderly patients may be at increased risk for myelosuppression and should be monitored closely.
Clinical Information
Clinical Pearls
- Topotecan is a potent myelosuppressive agent; close monitoring of CBC is critical before each dose and throughout treatment.
- Dose adjustments are essential for patients with moderate renal impairment (CrCl 20-39 mL/min).
- Administer G-CSF at least 24 hours after the last dose of topotecan to avoid exacerbating myelosuppression.
- Patients should be educated on signs of infection and bleeding and instructed to report them immediately.
- Hydration and antiemetics are important for managing gastrointestinal side effects.
Alternative Therapies
- Paclitaxel (for ovarian cancer, SCLC)
- Docetaxel (for ovarian cancer, SCLC)
- Etoposide (for SCLC)
- Irinotecan (another topoisomerase I inhibitor, for colorectal cancer)
- Gemcitabine (for ovarian cancer, SCLC)
- Pemetrexed (for NSCLC)
Cost & Coverage
Average Cost:
Varies significantly, typically several hundred to over a thousand USD per vial depending on strength and supplier. per 4mg vial
Generic Available:
Yes
Insurance Coverage:
Specialty Tier (often requires prior authorization and is covered under medical benefit for oncology indications)
General Drug Facts
If your symptoms or health problems persist or worsen, it is essential to contact your doctor for further guidance. To ensure safe use, never share your medication with others, and do not take medication prescribed for someone else. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion. Dispose of unused or expired medications properly. Unless instructed to do so by a healthcare professional, avoid flushing medications down the toilet or pouring them down the drain. If you are unsure about the proper disposal method, consult your pharmacist, who can also inform you about potential drug take-back programs in your area. Some medications may come with an additional patient information leaflet, which your pharmacist can provide. If you have any questions or concerns about your medication, discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately contact your local poison control center or seek medical attention. Be prepared to provide information about the medication taken, the amount, and the time it occurred.