Hycamtin 0.25mg Capsules
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
Oct 2007
DEA Schedule
Not Controlled
Overview
What is this medicine?
Topotecan is a chemotherapy medicine used to treat certain types of cancer. It works by interfering with the cancer cells' ability to grow and divide, causing them to die. It is taken as a capsule by mouth.
How to Use This Medicine
Taking Your Medication Correctly
To ensure you get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided to you and follow the instructions closely. When handling this medication, take special precautions. Consult your doctor or pharmacist for guidance on how to handle it safely.
You can take this medication with or without food. Swallow the capsule whole - do not chew, open, or crush it. Your dose may consist of two or more different strengths and colors of capsules. If you vomit after taking a dose, do not take an additional dose. Instead, take your next dose at the scheduled time.
If the capsule is accidentally opened or broken, avoid touching the contents. If you do come into contact with the contents or get them in your eyes, wash your hands or eyes immediately.
Storing and Disposing of Your Medication
Store your medication in the refrigerator, but do not freeze it. Keep it in its original container to protect it from light.
What to Do if You Miss a Dose
If you miss a dose, skip it and take your next dose at the scheduled time. Do not take two doses at the same time or take extra doses to make up for the missed one.
To ensure you get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided to you and follow the instructions closely. When handling this medication, take special precautions. Consult your doctor or pharmacist for guidance on how to handle it safely.
You can take this medication with or without food. Swallow the capsule whole - do not chew, open, or crush it. Your dose may consist of two or more different strengths and colors of capsules. If you vomit after taking a dose, do not take an additional dose. Instead, take your next dose at the scheduled time.
If the capsule is accidentally opened or broken, avoid touching the contents. If you do come into contact with the contents or get them in your eyes, wash your hands or eyes immediately.
Storing and Disposing of Your Medication
Store your medication in the refrigerator, but do not freeze it. Keep it in its original container to protect it from light.
What to Do if You Miss a Dose
If you miss a dose, skip it and take your next dose at the scheduled time. Do not take two doses at the same time or take extra doses to make up for the missed one.
Lifestyle & Tips
- Avoid contact with people who are sick or have infections, as your immune system will be weakened.
- Practice good hand hygiene (frequent hand washing).
- Avoid crowded places during periods of low blood counts.
- Report any signs of infection (fever, chills) immediately.
- Avoid activities that could cause injury or bleeding.
- Maintain good oral hygiene to prevent mouth sores.
- Stay well-hydrated and eat a balanced diet as tolerated.
- Discuss any vaccinations with your doctor before receiving them.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Small Cell Lung Cancer (SCLC): 2.3 mg/m² orally once daily for 5 consecutive days, repeated every 21 days.
Condition-Specific Dosing:
Small Cell Lung Cancer (SCLC):
2.3 mg/m² orally once daily for 5 consecutive days, repeated every 21 days. Dose adjustments required for myelosuppression.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
CrCl 40-60 mL/min: No specific dose adjustment recommended, but monitor closely.
Moderate:
CrCl 20-39 mL/min: Reduce dose to 0.75 mg/m² orally once daily for 5 consecutive days, repeated every 21 days.
Severe:
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 dose adjustment recommended.
Moderate:
No specific dose adjustment recommended.
Severe:
Not studied. Use with caution and monitor closely.
Pharmacology
Mechanism of Action
Topotecan is a topoisomerase I inhibitor. It binds to the topoisomerase I-DNA complex, preventing religation of the DNA strand and leading to DNA damage. This results in the accumulation of DNA strand breaks, which ultimately leads to cell death.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 40%
Tmax:
1-2 hours
FoodEffect:
Food reduces Cmax and AUC of topotecan by approximately 20-30% and delays Tmax. Administer without regard to food, but consistency is recommended.
Distribution:
Vd:
Approximately 60 L/m²
ProteinBinding:
Approximately 35%
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 2-3 hours (for lactone form)
Clearance:
Approximately 60 L/hr/m²
ExcretionRoute:
Primarily renal (30-60% unchanged), with some fecal excretion.
Unchanged:
30-60%
Pharmacodynamics
OnsetOfAction:
Not directly applicable for chemotherapy; effects are cumulative over cycles.
PeakEffect:
Not directly applicable for chemotherapy; effects are cumulative over cycles.
DurationOfAction:
Not directly applicable for chemotherapy; effects are cumulative over cycles.
Safety & Warnings
BLACK BOX WARNING
Myelosuppression (primarily neutropenia, but also thrombocytopenia and anemia) is the dose-limiting toxicity of topotecan. Severe myelosuppression, including febrile neutropenia, may occur, leading to infection and death. Frequent monitoring of complete blood counts is essential.
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:
Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, 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.
Signs of infection: 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.
Signs of 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 bruises that enlarge, or uncontrollable bleeding.
Severe diarrhea or 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. (Note: Lung problems can be fatal, so it's essential to seek medical help immediately.)
Severe bowel problems: stomach pain (with or without fever), tender stomach, or diarrhea. (Note: Bowel problems can be life-threatening and may occur as early as the first day of symptoms.)
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects, contact your doctor or seek medical help if they bother you, persist, or worsen:
Fatigue or weakness
Hair loss
* Diarrhea, vomiting, nausea, upset stomach, and decreased appetite (common side effects that can be managed with your doctor's guidance)
Reporting Side Effects
If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, 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.
Signs of infection: 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.
Signs of 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 bruises that enlarge, or uncontrollable bleeding.
Severe diarrhea or 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. (Note: Lung problems can be fatal, so it's essential to seek medical help immediately.)
Severe bowel problems: stomach pain (with or without fever), tender stomach, or diarrhea. (Note: Bowel problems can be life-threatening and may occur as early as the first day of symptoms.)
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects, contact your doctor or seek medical help if they bother you, persist, or worsen:
Fatigue or weakness
Hair loss
* Diarrhea, vomiting, nausea, upset stomach, and decreased appetite (common side effects that can be managed with your doctor's guidance)
Reporting Side Effects
If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Fever (100.4°F or higher) or chills
- Sore throat, cough, or other signs of infection
- Unusual bleeding (nosebleeds, bleeding gums, blood in urine or stool)
- Easy bruising
- Severe fatigue or weakness
- Severe nausea, vomiting, or diarrhea
- Severe mouth sores
- Shortness of breath
- Yellowing of skin or eyes
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 a low white blood cell count, low platelet count, or low red blood cell count.
If you are breastfeeding. 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 provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
Your health problems, including any medical conditions or allergies
Before starting, stopping, or changing the dose of any medication, including this one, you must consult with your doctor to ensure your safety. It is your responsibility to verify that it is safe to take this medication with all your other medications and health conditions.
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 a low white blood cell count, low platelet count, or low red blood cell count.
If you are breastfeeding. 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 provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
Your health problems, including any medical conditions or allergies
Before starting, stopping, or changing the dose of any medication, including this one, you must consult with your doctor to ensure your safety. It is your responsibility to verify that it is safe to take this medication with all your other medications and health conditions.
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 even 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.
Be aware that this medication can increase your risk of bleeding. Take precautions to prevent injuries, and when possible, use a soft toothbrush and an electric razor for personal grooming.
The oral form of this medication can cause severe diarrhea, which in some cases may be life-threatening and require hospitalization. If you experience diarrhea, consult your doctor immediately. Do not attempt to treat diarrhea without first discussing it with your doctor.
Before receiving any vaccinations, consult 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, discuss this with your doctor before starting the medication.
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 initiating treatment to confirm you are not pregnant. If there is a chance you may become pregnant, use effective birth control during treatment and for 6 months after your last dose, unless otherwise advised by your doctor. It is crucial to understand how long 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 while taking this medication and for a period after the last dose. Discuss this with your doctor to determine the best course of action.
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 even 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.
Be aware that this medication can increase your risk of bleeding. Take precautions to prevent injuries, and when possible, use a soft toothbrush and an electric razor for personal grooming.
The oral form of this medication can cause severe diarrhea, which in some cases may be life-threatening and require hospitalization. If you experience diarrhea, consult your doctor immediately. Do not attempt to treat diarrhea without first discussing it with your doctor.
Before receiving any vaccinations, consult 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, discuss this with your doctor before starting the medication.
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 initiating treatment to confirm you are not pregnant. If there is a chance you may become pregnant, use effective birth control during treatment and for 6 months after your last dose, unless otherwise advised by your doctor. It is crucial to understand how long 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 while taking this medication and for a period after the last dose. Discuss this with your doctor to determine the best course of action.
Overdose Information
Overdose Symptoms:
- Severe myelosuppression (very low white blood cell, red blood cell, and platelet counts)
- Severe gastrointestinal toxicity (nausea, vomiting, diarrhea, mucositis)
What to Do:
There is no specific antidote for topotecan overdose. Management is supportive, including transfusions (blood, platelets), antibiotics for infection, and antiemetics. Call 1-800-222-1222 (Poison Control) or seek immediate medical attention.
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 duration of neutropenia. Administer G-CSF no earlier than 24 hours after the last dose of topotecan.
Moderate Interactions
- Strong CYP3A4 inhibitors/inducers: While topotecan is not primarily metabolized by CYP450, some minor pathways or transporter interactions could occur. Monitor for altered efficacy/toxicity.
- P-glycoprotein (P-gp) inhibitors/inducers: Topotecan is a substrate for P-gp. Co-administration with P-gp inhibitors (e.g., cyclosporine, verapamil) may increase topotecan exposure; P-gp inducers (e.g., rifampin, carbamazepine) may decrease exposure. Clinical significance for oral formulation is less clear than IV.
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 therapy.
Renal function tests (serum creatinine, BUN, CrCl)
Rationale: Topotecan is primarily renally eliminated; renal impairment requires dose adjustment.
Timing: Prior to initiation of therapy.
Hepatic function tests (ALT, AST, bilirubin)
Rationale: To assess baseline liver function, as hepatic impairment may affect drug clearance.
Timing: Prior to initiation of therapy.
Routine Monitoring
Complete Blood Count (CBC) with differential and platelet count
Frequency: Weekly during treatment cycles and prior to each new cycle.
Target: Absolute Neutrophil Count (ANC) ≥ 1,500 cells/mm³ and platelet count ≥ 100,000 cells/mm³ for dose administration.
Action Threshold: If ANC < 1,500 cells/mm³ or platelets < 100,000 cells/mm³, delay treatment or reduce dose as per protocol. If severe neutropenia (ANC < 500 cells/mm³) or thrombocytopenia (platelets < 25,000 cells/mm³) occurs, consider dose reduction or G-CSF support.
Renal function tests (serum creatinine)
Frequency: Periodically, especially if renal function changes or if patient is elderly or has comorbidities.
Target: Not applicable (monitor trends)
Action Threshold: If CrCl falls below 40 mL/min, dose adjustment is required.
Symptom Monitoring
- Signs of infection (fever, chills, sore throat, cough)
- Unusual bleeding or bruising (petechiae, epistaxis, melena)
- Severe fatigue or weakness
- Nausea, vomiting, diarrhea, constipation
- Abdominal pain
- Oral mucositis/stomatitis
- Hair loss
Special Patient Groups
Pregnancy
Topotecan can cause fetal harm when administered to a pregnant woman. It is teratogenic and embryotoxic in animals. Advise pregnant women of the potential risk to the fetus. Women of childbearing potential should use effective contraception during treatment and for 6 months after the last dose. Males with female partners of childbearing potential should use effective contraception during treatment and for 3 months after the last dose.
Trimester-Specific Risks:
First Trimester:
High risk of major birth defects and embryo-fetal toxicity.
Second Trimester:
Risk of fetal toxicity, including myelosuppression and growth restriction.
Third Trimester:
Risk of fetal toxicity, including myelosuppression and growth restriction.
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 and for 1 week after the last dose.
Infant Risk:
High risk of serious adverse reactions, including myelosuppression.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Use in pediatric patients is generally not recommended outside of clinical trials.
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 more susceptible to myelosuppression and may require closer monitoring and dose adjustments.
Clinical Information
Clinical Pearls
- Oral topotecan is often used in the maintenance or palliative setting for SCLC, offering convenience over IV administration.
- Myelosuppression, particularly neutropenia, is the primary dose-limiting toxicity. Close monitoring of CBCs is crucial.
- Dose reductions are frequently required based on nadir blood counts in previous cycles.
- Patients should be educated on signs of infection and bleeding and instructed to report them immediately.
- The oral formulation has lower bioavailability than the IV form, and doses are not directly interchangeable (oral dose is higher than IV dose for equivalent exposure).
Alternative Therapies
- Other topoisomerase I inhibitors (e.g., Irinotecan - IV only)
- Other chemotherapeutic agents used in SCLC (e.g., platinum agents, etoposide, lurbinectedin)
- Other chemotherapeutic agents used in ovarian/cervical cancer (e.g., platinum agents, taxanes, bevacizumab, paclitaxel)
Cost & Coverage
Average Cost:
High per capsule/cycle
Generic Available:
Yes
Insurance Coverage:
Tier 4 (Specialty Drug) or Tier 5 (Specialty Drug)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. 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 it's a good idea to check with your pharmacist. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide detailed information about the overdose, including the substance taken, the amount, and the time it occurred.