Esperoct 500iu Inj
It is used to treat or prevent bleeding in people with hemophilia.
Drug Class
Antihemophilic Agent
Pharmacologic Class
Coagulation Factor VIII (Recombinant, Pegylated)
Pregnancy Category
Not available
FDA Approved
Feb 2019
DEA Schedule
Not Controlled
Overview
What is this medicine?
Esperoct is a medicine used to treat and prevent bleeding in people with hemophilia A. It works by replacing a missing clotting protein (Factor VIII) in the blood, which helps the blood to clot properly and stop bleeding.
How to Use This Medicine
Proper Use of This Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. This medication is administered as an injection into a vein. If you will be self-administering the injection, your doctor or nurse will instruct you on the proper technique. Before and after handling the medication, wash your hands thoroughly.
If the medication has been stored in the refrigerator, allow it to reach room temperature before mixing. Do not heat the medication. You can warm it to room temperature by holding the vial in your hands until it feels as warm as your body temperature.
Before use, this medication must be mixed according to the instructions provided by your doctor. Do not shake the vial. After mixing, use the medication within 4 hours if stored at room temperature. Alternatively, the mixture can be stored in the refrigerator for up to 24 hours. However, do not use the medication if the solution appears cloudy, is leaking, or contains particles. Additionally, do not use the medication if the solution has changed color.
After using the medication, discard any remaining balance in the opened vial. Dispose of needles and other sharp objects in a designated needle/sharp disposal box. Do not reuse needles or other items. When the disposal box is full, follow local regulations for proper disposal. If you have any questions or concerns, consult your doctor or pharmacist.
Storage and Disposal
Store unopened vials of this medication in the refrigerator, but do not freeze.
Missed Dose
If you miss a dose, contact your doctor to determine the best course of action.
To use this medication correctly, follow your doctor's instructions and read all the information provided. This medication is administered as an injection into a vein. If you will be self-administering the injection, your doctor or nurse will instruct you on the proper technique. Before and after handling the medication, wash your hands thoroughly.
If the medication has been stored in the refrigerator, allow it to reach room temperature before mixing. Do not heat the medication. You can warm it to room temperature by holding the vial in your hands until it feels as warm as your body temperature.
Before use, this medication must be mixed according to the instructions provided by your doctor. Do not shake the vial. After mixing, use the medication within 4 hours if stored at room temperature. Alternatively, the mixture can be stored in the refrigerator for up to 24 hours. However, do not use the medication if the solution appears cloudy, is leaking, or contains particles. Additionally, do not use the medication if the solution has changed color.
After using the medication, discard any remaining balance in the opened vial. Dispose of needles and other sharp objects in a designated needle/sharp disposal box. Do not reuse needles or other items. When the disposal box is full, follow local regulations for proper disposal. If you have any questions or concerns, consult your doctor or pharmacist.
Storage and Disposal
Store unopened vials of this medication in the refrigerator, but do not freeze.
Missed Dose
If you miss a dose, contact your doctor to determine the best course of action.
Lifestyle & Tips
- Adhere strictly to the prescribed dosing schedule for prophylaxis to prevent bleeding episodes.
- Learn to recognize signs of bleeding and administer on-demand doses as instructed by your healthcare provider.
- Carry your medication and supplies with you, especially when traveling.
- Maintain good dental hygiene to prevent gum bleeding.
- Avoid activities that carry a high risk of injury or bleeding.
- Inform all healthcare providers (including dentists) about your hemophilia and medication.
- Consider wearing a medical alert bracelet or carrying an identification card.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Prophylaxis: 50 IU/kg every 4 days or 60 IU/kg twice weekly. On-demand: Dose based on target Factor VIII level and patient weight (e.g., 1 IU/kg increases FVIII by ~2% of normal activity).
Condition-Specific Dosing:
Prophylaxis:
50 IU/kg every 4 days or 60 IU/kg twice weekly
On-demand treatment of bleeding episodes:
Initial dose 20-50 IU/kg for minor to moderate bleeding, 40-60 IU/kg for major bleeding. Subsequent doses and frequency based on clinical response and FVIII levels.
Perioperative management:
Target FVIII levels based on type of surgery (e.g., 80-100% for major surgery).
Pediatric Dosing
Neonatal:
Not established (limited data in neonates, generally not indicated for routine use in this age group unless specific circumstances)
Infant:
Dosing based on body weight, similar to older children/adults (e.g., prophylaxis 50 IU/kg every 4 days or 60 IU/kg twice weekly).
Child:
Dosing based on body weight, similar to adults (e.g., prophylaxis 50 IU/kg every 4 days or 60 IU/kg twice weekly).
Adolescent:
Dosing based on body weight, similar to adults (e.g., prophylaxis 50 IU/kg every 4 days or 60 IU/kg twice weekly).
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended.
Moderate:
No specific adjustment recommended.
Severe:
No specific adjustment recommended, as Factor VIII is not renally eliminated. Use with caution and monitor for fluid overload if severe renal impairment.
Dialysis:
No specific adjustment recommended. Factor VIII is not dialyzable.
Hepatic Impairment:
Mild:
No specific adjustment recommended.
Moderate:
No specific adjustment recommended.
Severe:
No specific adjustment recommended, as Factor VIII is not primarily metabolized by the liver in a way that would require dose adjustment. Monitor clinical response.
Pharmacology
Mechanism of Action
Esperoct (turoctocog alfa pegol) is a recombinant DNA-derived, pegylated coagulation Factor VIII (FVIII) product. It temporarily replaces the missing coagulation FVIII that is necessary for effective hemostasis in patients with hemophilia A. FVIII acts as a cofactor for activated Factor IX (FIXa) in the intrinsic coagulation pathway, accelerating the conversion of Factor X (FX) to activated Factor X (FXa). FXa, in turn, converts prothrombin to thrombin, which then converts fibrinogen to fibrin, leading to clot formation.
Pharmacokinetics
Absorption:
Bioavailability:
100% (intravenous administration)
Tmax:
Not applicable (IV administration, peak activity is at end of infusion)
FoodEffect:
Not applicable (IV administration)
Distribution:
Vd:
Approximately 50 mL/kg
ProteinBinding:
Binds to von Willebrand factor (vWF) in plasma, which stabilizes FVIII and prolongs its half-life.
CnssPenetration:
Limited (does not cross the blood-brain barrier)
Elimination:
HalfLife:
Terminal half-life: Approximately 19 hours (range 12.5 to 27.7 hours) in adults and adolescents; slightly shorter in children.
Clearance:
Approximately 2.5 mL/hr/kg (range 1.5 to 3.9 mL/hr/kg) in adults and adolescents.
ExcretionRoute:
Primarily via degradation and cellular uptake, not renal or hepatic excretion of intact protein.
Unchanged:
Not applicable (protein degradation)
Pharmacodynamics
OnsetOfAction:
Immediate (upon intravenous administration)
PeakEffect:
At the end of infusion (for FVIII activity levels)
DurationOfAction:
Prolonged due to pegylation, allowing for less frequent dosing (e.g., every 4 days or twice weekly for prophylaxis).
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
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
Chest pain
Dizziness or fainting
Other Possible Side Effects
Like all medications, this drug can cause side effects. Although many people do not experience any side effects or only have mild ones, it is essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Irritation at the injection site
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, consult your doctor. For medical advice about side effects, you can also contact your doctor. Additionally, you can report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
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
Chest pain
Dizziness or fainting
Other Possible Side Effects
Like all medications, this drug can cause side effects. Although many people do not experience any side effects or only have mild ones, it is essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Irritation at the injection site
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, consult your doctor. For medical advice about side effects, you can also contact your doctor. Additionally, you can 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:
- Signs of bleeding: new or worsening joint pain/swelling, unusual bruising, prolonged bleeding from cuts, nosebleeds, blood in urine or stool, severe headache, vision changes, slurred speech (may indicate internal bleeding).
- Signs of allergic reaction: rash, hives, itching, facial swelling, difficulty breathing, chest tightness, dizziness, feeling faint.
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you have an allergy to hamsters, discuss this with your doctor, as it may be relevant to your treatment.
Potential interactions with other medications or health conditions. To ensure safe treatment, provide your doctor and pharmacist with a comprehensive list of all your medications, including:
+ Prescription and over-the-counter (OTC) drugs
+ Natural products
+ Vitamins
Any existing health problems, as they may affect the safety and efficacy of this medication.
Remember to consult with your doctor before making any changes to your medication regimen, including starting, stopping, or adjusting the dose of any drug. This will help ensure your safety and the effectiveness of your treatment.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you have an allergy to hamsters, discuss this with your doctor, as it may be relevant to your treatment.
Potential interactions with other medications or health conditions. To ensure safe treatment, provide your doctor and pharmacist with a comprehensive list of all your medications, including:
+ Prescription and over-the-counter (OTC) drugs
+ Natural products
+ Vitamins
Any existing health problems, as they may affect the safety and efficacy of this medication.
Remember to consult with your doctor before making any changes to your medication regimen, including starting, stopping, or adjusting the dose of any drug. This will help ensure your safety and the effectiveness of your treatment.
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 and other laboratory assessments should be conducted as directed by your doctor to monitor your condition.
If you experience unexplained bruising, bleeding, or if bleeding does not stop after taking this medication, contact your doctor immediately. This could be an indication that your current dose is not effective.
Before traveling, consult with your doctor to ensure you have an adequate supply of this medication for the duration of your trip.
If you are pregnant, planning to become pregnant, or are breastfeeding, notify your doctor. You and your doctor will need to discuss the potential benefits and risks of this medication to both you and your baby.
Regular blood tests and other laboratory assessments should be conducted as directed by your doctor to monitor your condition.
If you experience unexplained bruising, bleeding, or if bleeding does not stop after taking this medication, contact your doctor immediately. This could be an indication that your current dose is not effective.
Before traveling, consult with your doctor to ensure you have an adequate supply of this medication for the duration of your trip.
If you are pregnant, planning to become pregnant, or are breastfeeding, notify your doctor. You and your doctor will need to discuss the potential benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- No specific symptoms of overdose have been reported with Factor VIII products. Very high levels of Factor VIII may theoretically increase the risk of thrombosis, but this is rare in hemophilia patients.
What to Do:
In case of suspected overdose, contact your healthcare provider or emergency services immediately. Management is generally supportive. Call 1-800-222-1222 (Poison Control Center) for advice.
Drug Interactions
Monitoring
Baseline Monitoring
Factor VIII activity level
Rationale: To establish baseline FVIII deficiency and guide initial dosing.
Timing: Prior to initiation of therapy.
Inhibitor (neutralizing antibody) screen (Bethesda assay)
Rationale: To detect pre-existing FVIII inhibitors, which can render therapy ineffective.
Timing: Prior to initiation of therapy.
Routine Monitoring
Factor VIII activity level
Frequency: Periodically, especially when initiating therapy, changing dose, or in response to bleeding episodes. For prophylaxis, trough levels may be monitored.
Target: Depends on clinical situation (e.g., >1% for prophylaxis, higher for bleeding/surgery).
Action Threshold: If FVIII levels are unexpectedly low or if bleeding occurs despite adequate dosing, consider inhibitor development.
Inhibitor (neutralizing antibody) screen (Bethesda assay)
Frequency: Regularly (e.g., every 3-6 months, or more frequently in high-risk patients like previously untreated patients (PUPs) or after switching products), and whenever there is a lack of clinical response to treatment.
Target: <0.6 Bethesda Units (BU)/mL
Action Threshold: >0.6 BU/mL indicates presence of inhibitors, requiring alternative treatment strategies.
Clinical response to treatment
Frequency: Continuously during bleeding episodes or perioperative period.
Target: Cessation of bleeding, adequate hemostasis.
Action Threshold: Persistent bleeding or inadequate hemostasis despite appropriate FVIII dosing.
Symptom Monitoring
- Signs of bleeding (e.g., joint pain/swelling, bruising, prolonged bleeding from minor cuts, blood in urine/stools, nosebleeds, headaches, vision changes)
- Signs of allergic or hypersensitivity reactions (e.g., rash, hives, itching, facial swelling, shortness of breath, chest tightness, dizziness, faintness)
Special Patient Groups
Pregnancy
There are no adequate and well-controlled studies of Esperoct in pregnant women. Animal reproduction studies have not been conducted. Esperoct should be used during pregnancy only if clearly needed and the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Risk unknown. Use only if clearly indicated.
Second Trimester:
Risk unknown. Use only if clearly indicated.
Third Trimester:
Risk unknown. Use only if clearly indicated. Hemophilia A in pregnant women is rare, but management of bleeding during labor and delivery would be critical.
Lactation
It is not known whether Esperoct is excreted in human milk. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for Esperoct and any potential adverse effects on the breastfed infant from Esperoct or from the underlying maternal condition. Use with caution.
Infant Risk:
Risk unknown. Factor VIII is a large protein and unlikely to be absorbed intact by the infant. Monitor breastfed infants for any adverse reactions.
Pediatric Use
Esperoct is approved for use in pediatric patients, including neonates, infants, children, and adolescents. Dosing is weight-based and similar to adults. Pharmacokinetic data suggest a slightly shorter half-life in younger children, which may necessitate more frequent monitoring or dose adjustments.
Geriatric Use
Clinical studies of Esperoct did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. In general, dose selection for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
Clinical Information
Clinical Pearls
- Esperoct is a pegylated Factor VIII product, offering a prolonged half-life compared to conventional Factor VIII products, allowing for less frequent prophylactic dosing (e.g., every 4 days or twice weekly).
- Patients should be educated on proper reconstitution and administration techniques, as it is administered intravenously.
- Regular monitoring for Factor VIII inhibitors is crucial, especially in previously untreated patients (PUPs) and after switching products, as inhibitor development can render treatment ineffective.
- Patients should carry a medical identification card or bracelet indicating their hemophilia A and treatment regimen.
- While rare, allergic-type hypersensitivity reactions are possible; patients should be advised on symptoms and immediate action.
Alternative Therapies
- Other recombinant Factor VIII products (e.g., Advate, Eloctate, Adynovate, Jivi, Nuwiq, Xyntha)
- Plasma-derived Factor VIII products
- Emicizumab (Hemlibra) - a bispecific antibody that mimics FVIIIa, used for prophylaxis in hemophilia A with or without inhibitors.
- Bypassing agents (e.g., FEIBA, NovoSeven RT) - for patients with FVIII inhibitors.
Cost & Coverage
Average Cost:
Highly variable, typically several thousand to tens of thousands of dollars per vial depending on strength and quantity. per vial
Insurance Coverage:
Specialty Tier (requires prior authorization, often covered by major medical and pharmacy benefit plans for hemophilia A)
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 emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.