Eculizumab

Name: Eculizumab

What Is Eculizumab?

Eculizumab is a monoclonal antibody. Eculizumab binds to proteins in the blood that can destroy red blood cells in people with genetic conditions that affect the natural defenses of red blood cells.

Eculizumab is used to prevent the breakdown of red blood cells in people with paroxysmal nocturnal hemoglobinemia (PNH).

Eculizumab is also used to treat a rare chronic blood disease called atypical hemolytic uremic syndrome (aHUS)

Eculizumab may also be used for purposes not listed in this medication guide.

Eculizumab is used to prevent the breakdown of red blood cells in people with paroxysmal nocturnal hemoglobinemia (PNH).

You should not use this medication if you have bacterial meningitis or if you have not been vaccinated against meningitis. Tell your doctor if you have a fever or any type of infection.

Eculizumab affects your immune system, and using this medication may increase your risk of serious infection such as meningitis. You must be vaccinated against meningococcal infection at least 2 weeks before you start treatment with eculizumab. Even if you have been vaccinated in the past, you may need a booster dose.

Seek emergency medical attention or call your doctor right away if you notice any of these symptoms of meningitis: headache and fever with nausea or vomiting, high fever (103 degrees or higher), body aches, flu symptoms, confusion, increased sensitivity to light, stiffness in your neck or back.

With your medication you will receive a Patient Safety Card listing the symptoms of meningitis. Carry this card with you at all times.

Do not stop using eculizumab without first talking to your doctor. Stopping or interrupting your treatment could cause sudden and serious effects on your red blood cells.

Eculizumab affects your immune system, and using this medication may increase your risk of serious infection such as meningitis.

You must be vaccinated against meningococcal infection at least 2 weeks before you start treatment with eculizumab. Even if you have been vaccinated in the past, you may need a booster dose.

It is best to stay current on all of your vaccinations while you are using eculizumab, and your doctor may recommend other vaccines before or during treatment.

Children being treated with eculizumab may also need to be vaccinated against influenza or pneumonia before treatment begins.

You should not use this medication if you are allergic to eculizumab, if you have bacterial meningitis, or if you have not been vaccinated against meningitis.

To make sure you can safely use eculizumab, tell your doctor if you have a fever or any type of infection.

FDA pregnancy category C. It is not known whether eculizumab will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication.

It is not known whether eculizumab passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby.

Eculizumab is available only under a special program called Soliris REMS. You must be registered in the program and sign documents stating that you understand the risks and benefits of taking this medication.

Administration

IV Administration

Dilute to 5 mg/mL by first adding dose to infusion bag, and then add appropriate amount of D5W, NS, ┬ŻNS, or Ringers

Adults: Infuse IV over at least 35 min; may slow/stop infusion if adverse effect occurs, but total infusion time should not exceed 2 hr

Children: Infuse IV over 1-4 hr

Administer by IV infusion, do NOT give IV push or bolus

Warnings

Included as part of the "PRECAUTIONS" Section

Eculizumab Overview

Eculizumab is a prescription medication used to treat Paroxysmal Nocturnal Hemoglobinuria (PNH) and atypical Hemolytic Uremic Syndrome (aHUS). These are diseases affecting red blood cells, blood vessels, kidneys, and other organs. Eculizumab belongs to a group of drugs monoclonal antibodies. It works by blocking the activity of the part of the immune system that damages blood cells or causes clots.

This medication comes in an injectable form to be given directly into a vein (IV) by a healthcare provider. It is usually given once a week for 5 weeks, and then once every other week.

Common side effects of eculizumab are headache, runny nose, and sore throat.

Uses of Eculizumab

Eculizumab is a prescription medicine used to treat people with:

  • a disease called Paroxysmal Nocturnal Hemoglobinuria (PNH). PNH affects red blood cells.
  • a disease called atypical Hemolytic Uremic Syndrome (aHUS). aHUS affects the blood system, kidney, and sometimes other body organs.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Eculizumab Usage

  • Eculizumab is given through a vein (I.V. or intravenous infusion) usually over 35 minutes. If you have an allergic reaction during your eculizumab infusion, your doctor may decide to give eculizumab more slowly or stop your infusion.
  • If you are an adult, you will usually receive a eculizumab infusion by your doctor:
    • weekly for five weeks, then
    • every 2 weeks
  • If you are less than 18 years of age, your doctor will decide how often you will receive eculizumab depending on your age and body weight.
  • After each infusion, you should be monitored for one hour for allergic reactions. 
  • If you forget or miss a eculizumab infusion, call your doctor right away.
  • If you have PNH, your doctor will need to monitor you closely for at least 8 weeks after stopping eculizumab. Stopping treatment with eculizumab may cause breakdown of your red blood cells due to PNH.
    Symptoms or problems that can happen due to red blood cell breakdown include:
    • drop in the number of your red blood cells
    • drop in your platelet count
    • confusion
    • chest pain
    • kidney problems
    • blood clots
    • difficulty breathing
  • If you have aHUS, your doctor will need to monitor you closely during and for at least 12 weeks after stopping treatment for signs of worsening aHUS symptoms or problems related to abnormal clotting (thrombotic microangiopathy).
    Symptoms or problems that can happen with abnormal clotting may include:
    • stroke
    • confusion
    • seizures
    • chest pain (angina)
    • difficulty breathing
    • kidney problems
    • swelling in arms or legs
    • a drop in your platelet count

Eculizumab Overdose

Eculizumab is usually administered by a healthcare provider in a medical setting making it unlikely for an overdose to occur. However, if overdose is suspected, seek emergency medical attention.

What is eculizumab (soliris)?

Eculizumab is a monoclonal antibody. Eculizumab binds to proteins in the blood that can destroy red blood cells in people with genetic conditions that affect the natural defenses of red blood cells.

Eculizumab is used to prevent the breakdown of red blood cells in people with paroxysmal nocturnal hemoglobinemia (PNH).

Eculizumab is also used to treat a rare chronic blood disease called atypical hemolytic uremic syndrome (aHUS)

Eculizumab may also be used for purposes not listed in this medication guide.

Eculizumab side effects

Get emergency medical help if you have signs of an allergic reaction: hives; chest pain, difficult breathing; feeling like you might pass out; swelling of your face, lips, tongue, or throat. Signs of allergic reaction may occur while you are receiving your eculizumab injection.

Seek emergency medical attention or call your doctor right away if you notice any of these symptoms of meningitis:

  • fever and a headache or skin rash;

  • headache with nausea and vomiting;

  • high fever (103 degrees F or higher), body aches, flu symptoms;

  • confusion, increased sensitivity to light; or

  • stiffness in your neck or back.

With your medication you will receive a Patient Safety Card listing the symptoms of meningococcal infection. Carry this card with you at all times during treatment and for 3 months after your last dose of eculizumab.

Call your doctor at once if you have any of these side effects during or after your treatment with eculizumab:

  • fever;

  • pain or burning when you urinate;

  • kidney problems--little or no urination, painful or difficult urination, swelling in your feet or ankles, feeling tired or short of breath;

  • signs of a blood cell disorder--pale skin, easy bruising, unusual bleeding, confusion, chest pain, trouble breathing, seizure (convulsions); or

  • signs of a blood clot--sudden numbness or weakness, problems with speech or balance, rapid breathing, coughing up blood, pain or swelling in your arms or legs.

Common side effects may include:

  • headache;

  • increased blood pressure (severe headache, blurred vision, pounding in your neck or ears, nosebleed, anxiety);

  • nausea, vomiting, diarrhea, stomach pain;

  • swelling in your hands or feet;

  • back pain; or

  • cold symptoms such as stuffy nose, runny nose, sinus pain, sore throat.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Uses for Eculizumab

Paroxysmal Nocturnal Hemoglobinuria

Treatment of paroxysmal nocturnal hemoglobinuria (PNH) to reduce hemolysis; designated an orphan drug by FDA for this use.1 2 3 4 10 16 17

Improves symptoms of PNH by reducing hemolysis, stabilizing hemoglobin concentrations, and reducing transfusion requirements.1 3 4 6 10 16 17 Reduced fatigue and improved quality of life also reported.1 3 6 Only curative treatment of PNH to date is stem cell transplantation.8 10 20

Atypical Hemolytic Uremic Syndrome

Treatment of atypical hemolytic uremic syndrome (aHUS) to inhibit complement-mediated thrombotic microangiopathy; designated an orphan drug by FDA for this use.1 2 22 31

Improves outcomes related to thrombotic microangiopathy (e.g., increased platelet counts, normalization of hematologic parameters) and improves renal function.1 22 25 26 27 29 30 31 32

Eculizumab Pharmacokinetics

Absorption

Plasma Concentrations

Plasma concentrations ≥35 mcg/mL required to block complement.16 17

Duration

Complement activity inhibited for ≤2 weeks following single dose.19

Reduction of hemolysis (as determined by reduction in LDH concentrations) maintained at least 52 weeks in open-label study.1 17

Distribution

Extent

Human IgG crosses placenta and is distributed into milk.1 Potential exists for eculizumab to cross placenta and distribute into milk.1

Elimination

Metabolism

Metabolic fate of immunoglobulins not well characterized; catabolized in various tissues via diffuse cellular processes.15

Elimination Route

Minimal excretion in urine expected due to large molecular size.1 15 Small quantities of immunoglobulin found in bile.15

Half-life

Patients with PNH: Approximately 272 hours.1

Patients with aHUS: Approximately 291 hours.1

Special Populations

In patients with aHUS undergoing plasma exchange interventions, clearance was increased and half-life reduced (to 1.26 hours).1

What do I need to tell my doctor BEFORE I take Eculizumab?

  • If you have an allergy to eculizumab or any other part of this medicine.
  • If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
  • If you did not get a meningococcal vaccine.
  • If you have a meningococcal infection.

This is not a list of all drugs or health problems that interact with eculizumab.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take this medicine with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take Eculizumab?

  • Tell all of your health care providers that you take eculizumab. This includes your doctors, nurses, pharmacists, and dentists.
  • You may have more chance of getting an infection. Wash hands often. Stay away from people with infections, colds, or flu.
  • Make sure you are up to date with all your vaccines before treatment with this medicine.
  • Vaccines lower the risk of infections; they do not get rid of the risk of infections. Talk with the doctor.
  • Have patient safety card with you at all times and for 3 months after drug is stopped.
  • Have blood work checked as you have been told by the doctor. Talk with the doctor.
  • Some patients have very bad side effects during the infusion. Tell your doctor if you have any bad effects during the infusion.
  • Some health problems may happen after eculizumab is stopped. You will need to be watched closely for several weeks after you stop this medicine. Follow up with your doctor as you have been told. After stopping eculizumab, call your doctor right away if you have a change in how much urine is passed; dark urine; swelling, warmth, or pain in the leg or arm; chest pain or pressure; coughing up blood; trouble breathing; weakness on 1 side of the body, trouble speaking or thinking, change in balance, or change in eyesight; change in thinking clearly and with logic; any bruising or bleeding that is not normal; or seizures.
  • Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using this medicine while you are pregnant.
  • Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

What are some other side effects of Eculizumab?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

  • Headache.
  • Nose and throat irritation.
  • Runny nose.
  • Back pain.
  • Upset stomach or throwing up.
  • Loose stools (diarrhea).
  • Feeling tired or weak.
  • Belly pain.
  • Not able to sleep.
  • Hard stools (constipation).
  • Muscle or joint pain.
  • Pain in arms or legs.
  • Muscle spasm.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-FDA-1088. You may also report side effects at http://www.fda.gov/medwatch.

If OVERDOSE is suspected

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

Pharmacology

Terminal complement-mediated intravascular hemolysis is a key clinical feature of paroxysmal nocturnal hemoglobinuria (PNH); blocking the formation of membrane attack complex (MAC) results in stabilization of hemoglobin and a reduction in the need for RBC transfusions. Impairment of complement activity regulation leads to uncontrolled complement activation in atypical hemolytic uremic syndrome (aHUS). Eculizumab is a humanized monoclonal IgG antibody that binds to complement protein C5, preventing cleavage into C5a and C5b. Blocking the formation of C5b inhibits the subsequent formation of terminal complex C5b-9 or MAC.

Distribution

PNH: 7.7 L; aHUS: 6.14 L

Drug Interactions

BCG (Intravesical): Immunosuppressants may diminish the therapeutic effect of BCG (Intravesical). Avoid combination

Belimumab: Monoclonal Antibodies may enhance the adverse/toxic effect of Belimumab. Avoid combination

Coccidioides immitis Skin Test: Immunosuppressants may diminish the diagnostic effect of Coccidioides immitis Skin Test. Monitor therapy

Denosumab: May enhance the adverse/toxic effect of Immunosuppressants. Specifically, the risk for serious infections may be increased. Monitor therapy

Echinacea: May diminish the therapeutic effect of Immunosuppressants. Consider therapy modification

Fingolimod: Immunosuppressants may enhance the immunosuppressive effect of Fingolimod. Management: Avoid the concomitant use of fingolimod and other immunosuppressants when possible. If combined, monitor patients closely for additive immunosuppressant effects (eg, infections). Consider therapy modification

Leflunomide: Immunosuppressants may enhance the adverse/toxic effect of Leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Management: Consider not using a leflunomide loading dose in patients receiving other immunosuppressants. Patients receiving both leflunomide and another immunosuppressant should be monitored for bone marrow suppression at least monthly. Consider therapy modification

Meningococcal Group B Vaccine: May diminish the therapeutic effect of Eculizumab. The meningococcal vaccine may result in increased complement activation, possibly worsening the symptoms of any underlying complement-mediated diseases, such as hemolysis and anemia. Eculizumab may diminish the therapeutic effect of Meningococcal Group B Vaccine. Consider therapy modification

Natalizumab: Immunosuppressants may enhance the adverse/toxic effect of Natalizumab. Specifically, the risk of concurrent infection may be increased. Avoid combination

Nivolumab: Immunosuppressants may diminish the therapeutic effect of Nivolumab. Consider therapy modification

Ocrelizumab: May enhance the immunosuppressive effect of Immunosuppressants. Monitor therapy

Pimecrolimus: May enhance the adverse/toxic effect of Immunosuppressants. Avoid combination

Roflumilast: May enhance the immunosuppressive effect of Immunosuppressants. Consider therapy modification

Sipuleucel-T: Immunosuppressants may diminish the therapeutic effect of Sipuleucel-T. Monitor therapy

Tacrolimus (Topical): May enhance the adverse/toxic effect of Immunosuppressants. Avoid combination

Tertomotide: Immunosuppressants may diminish the therapeutic effect of Tertomotide. Monitor therapy

Tofacitinib: Immunosuppressants may enhance the immunosuppressive effect of Tofacitinib. Management: Concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted, and this warning seems particularly focused on more potent immunosuppressants. Consider therapy modification

Trastuzumab: May enhance the neutropenic effect of Immunosuppressants. Monitor therapy

Vaccines (Inactivated): Immunosuppressants may diminish the therapeutic effect of Vaccines (Inactivated). Management: Vaccine efficacy may be reduced. Complete all age-appropriate vaccinations at least 2 weeks prior to starting an immunosuppressant. If vaccinated during immunosuppressant therapy, revaccinate at least 3 months after immunosuppressant discontinuation. Consider therapy modification

Vaccines (Live): Immunosuppressants may enhance the adverse/toxic effect of Vaccines (Live). Immunosuppressants may diminish the therapeutic effect of Vaccines (Live). Management: Avoid use of live organism vaccines with immunosuppressants; live-attenuated vaccines should not be given for at least 3 months after immunosuppressants. Avoid combination

Dose Adjustments

Supplemental dosing of eculizumab is required in the setting of concomitant support with PE/PI (plasmapheresis or plasma exchange/fresh frozen plasma infusion):
PLASMAPHERESIS OR PLASMA EXCHANGE (PE):
-If the most recent eculizumab dose is 300 mg, supplement the dose by 300 mg per each PE session within 60 minutes after each PE exchange
-If the most recent eculizumab dose is 600 mg or more, supplement the dose by 600 mg per each PE session within 60 minutes after each PE exchange
FRESH FROZEN PLASMA INFUSION (PI):
-If the most recent eculizumab dose is 300 mg or more, supplement the dose by 300 mg per each PI session 60 minutes prior to each PI infusion

Dialysis

Data not available

Administrative Information

LactMed Record Number

999

Last Revision Date

20170502

Disclaimer

Information presented in this database is not meant as a substitute for professional judgment. You should consult your healthcare provider for breastfeeding advice related to your particular situation. The U.S. government does not warrant or assume any liability or responsibility for the accuracy or completeness of the information on this Site.

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