Eltrombopag (Oral)

Classed as a small-molecule TPO-receptor agonist, eltrombopag works to increase the blood platelet count in patients who have thrombocytopenia (low platelet counts) due to conditions including chronic immune thrombocytopenia purpura (ITP), chronic hepatitis C and in some cases, severe aplastic anemia (SAA).

Overview

Also referred to by its brand name Promacta, eltrombopag is classed as a small-molecule TPO-receptor agonist and is used to increase the blood platelet count in patients who have thrombocytopenia (decreased blood platelets). Eltrombopag is predominantly used to treat patients who have thrombocytopenia as a result of conditions such as chronic idiopathic thrombocytopenic purpura (ITP) or chronic hepatitis C. In patients with chronic hepatitis C, eltrombopag is usually used alongside interferon therapy.

Chronic idiopathic thrombocytopenic purpura (ITP) is a long-term condition that can cause abnormal bleeding or bruises due to an abnormally low number of platelets in the blood. Patients who have this are being treated are usually prescribed eltrombopag following certain treatments and medicines that are used to increase blood platelets, showing insufficient results. These treatments often include surgery to remove the spleen (a splenectomy) and the administration of other medications such as immunoglobulin or steroids. Additionally, eltrombopag can also be used to treat patients who have severe aplastic anemia (SAA) and who have shown an inadequate response to other medications to treat SAA.

A low number of platelets in the blood (thrombocytopenia) can cause a patient to have various bleeding problems that may be particularly dangerous following surgical procedures or in people who are more susceptible to bleeding and injury. Platelets are an essential component in blood clotting, working to stop bleeding by creating clumps that plug and stop blood vessel injuries.

Symptoms of thrombocytopenia can include bleeding from your gums or nose, blood in urine or stools, prolonged bleeding from cuts, fatigue and easy or excessive bleeding. In rare cases, the number of a patient's platelets can become so low that serious internal bleeding can happen.

Eltrombopag is an effective treatment to increase the number of platelets found in blood, acting by causing the bone marrow to produce more platelets.

It can be used in adults and pediatric patients who are older than one year of age, and must only be prescribed and directed by a doctor.

It is taken orally and is available in the dosage forms of tablets or powder for suspension.

Conditions treated

    Chronic immune thrombocytopenia (ITP)
    Chronic Hepatitis C
    Severe aplastic anemia (SAA)

Type of medicine

  • Small-molecule TPO-receptor agonist.

Side effects

Eltrombopag has the potential to cause serious and unwanted side effects, with the most common side effects including a decrease in appetite, difficulty with moving, thinning hair or hair loss, a feeling of weakness, muscles aches, cramps and stiffness or swollen joints. In less common cases, individuals may experience stomach acid, indigestion or heartburn, back pain, belching, a dry mouth or general stomach upset. These are all side effects that are likely to go away once your body becomes adjusted to the medication and may not need medical attention. However, if you become at all concerned by them, make sure to discuss it with your healthcare professional.

Common side effects of this medication that should be brought to the attention of a doctor include:

    Face, hands, arms, legs, or feet bloating and swelling
    Body aching or pain
    Chills or fever
    Cough
    Headache
    Voice loss
    Pale skin
    Sudden weight gain
    runny nose
    sore throat
    Tingling sensations in the feet or hands
    Abnormal weight gain or loss

Some patients may experience other side effects that are less common. If you experience any of the following symptoms, make sure to bring them to the attention of your doctor when possible:

    Bladder pain
    Bruising
    Burning, itching, numbness, prickling or tingling sensations
    Diarrhea
    A widespread feeling of discomfort or illness
    Hoarseness
    Joint or muscle pain
    Lower back or side pain
    Nausea or vomitin
    n-prick red spots on the skin
    Redness of the eye
    Fever-like symptoms such as sweating, chills and tender, swollen glands in the neck
    Difficulty sleeping
    Difficulty swallowing
    Voice changes

Some of these side effects can be extremely unpleasant and can be indicators of more serious conditions or reactions to eltrombopag. Make sure to discuss any of these problems with a healthcare professional when possible.

Patients who have chronic hepatitis C and are who taking eltrombopag in combination with other medications called interferon have a higher risk of developing severe liver damage. If you experience yellowing of the skin or eyes, darkened urine, extreme tiredness, confusion or pain in the upper right part of the stomach or swelling in the stomach area, make sure to contact a healthcare professional as soon as possible as it is likely that you will require immediate treatment.

Problems with blood clotting may also occur in patients who are taking this medicine. If you experience any pain, swelling or tenderness in your leg or a pain in your chest and a shortness of breath, make sure to see a doctor as soon as possible. These symptoms can develop into serious conditions such as deep vein thrombosis or a pulmonary embolism.

Additionally, there is the possibility of eltrombopag causing cataracts or making previous ones worsen. If you notice any changes in vision, difficulty in reading or blurred vision, make sure to check with your doctor. It is likely that your doctor will want your eyes to be reviewed by an ophthalmologist.

Dosage

The dose that you will be prescribed by your doctor will be dependent on a number of factors including your weight, current health conditions and other medications that they may be taking.

This medication is also available at different strengths, which will affect the amount of medicine that you will take, the number of doses that you administer, the amount of time between each dose and the duration that your treatment will last for.

If you are taking any multivitamins, supplements, antacids or food products that contain calcium, magnesium, aluminium, iron, selenium, or zinc, make sure to take them at a minimum of four hours in advance or two hours after taking eltrombopag.

For the best results and effective treatment, it is also important to take this medicine on an empty stomach or at least one or two hours following a meal.

If you are taking the tablet form of this medicine, you must swallow it whole without crushing, breaking or chewing the tablet. You must also remember to no mix it with food or drinks.

If you are taking the oral suspension dose of eltrombopag, you must only ever mix the powder with cold water and use the dosing syringe that comes with the medicine. This will ensure the correct amount of medicine as the standard household teaspoon may not hold the correct amount of liquid. You must also remember to take the oral suspension immediately after you mix it.

The standard dose for adult patients who are being treated with eltrombopag for severe aplastic anemia is an initial 50 mg taken once a day. This dose may be lower in some patients and when decided by a doctor, can be adjusted up to a maximum of 150 mg a day. In pediatric patients with severe aplastic anemia, the dose must be decided by a doctor.

For patients being treated with eltrombopag for thrombocytopenia with ITP, adults and children over six years old will usually be prescribed 50 mg per day. This dose can be adjusted by your doctor but should not exceed 75 mg per day. In children of one to five years of age, this dose will usually be 25 mg taken once a day. It can also be adjusted by a doctor if needed, but should not go over 75 mg per day. In children younger than one year of age, eltrombopag can be used in some cases but it must be determined and directed by your doctor.

In patients who have chronic hepatitis C, this dose is often lower as to avoid any adverse liver reactions. In adults, this dose is usually 25 mg taken once a day and it can be adjusted to a maximum of 100 mg per day. In children, the use and dose of eltrombopag must be determined and instructed by a doctor.

In all cases with this medicine's dosage, it is important to never double dose if you have missed a day's dose. Instead, if you have missed a dose of eltrombopag you should skip the missed dose and return to your regular dosing schedule.

Interactions

Before taking eltrombopag, you must make sure that your doctor is aware of any other prescription or over-the-counter medications that you may be taking, as to avoid any adverse reactions. You should also include vitamins, herbal remedies and supplements in this list as to avoid any ones worsen interactions with your medication. In particular, any vitamins or supplements containing calcium, aluminium, iron, selenium, zinc, or magnesium or antacids should be discussed with your doctor. These can all make eltrombopag less effective and negatively affect your treatment.

Alongside many forms of cholesterol-lowering drugs, the following medications can all increase your risk of adverse side effects to eltrombopag:

Bosentan

Ezetimibe

Glyburide

Olmesartan

Repaglinide

Rifampin

Valsartan

Imatinib

Lapatinib

Mitoxantrone

Sulfasalazine

Topotecan

In addition to medicines, it is important that your doctor is aware of your lifestyle and diet. This is because foods that contain calcium can cause eltrombopag to be less effective. This includes dairy products including milk and cheese.

Warnings

It is vital that your doctor is aware of any medical conditions that you may have, as some can cause serious interactions with this medication. In particular, patients with myelodysplastic syndrome (MDS), liver problems or blood clotting problems are all at higher risk of developing harmful effects that may exacerbate your condition. It is also important to let your doctor know if you have east Asian relatives such as Chinese, Japanese, Korean or Filipino. This is because your genetics may require you to have a lower dose of eltrombopag as to avoid harmful side effects.

Eltrombopag has been classed as a category C pregnancy drug. This means that wither Research in animals has shown adverse effects or that there are inadequate human studies to know its effects of pregnancy. For this reason, it is important that you tell your doctor if you are pregnant or plan to become pregnant the number of taking this medication.

For patients who are breastfeeding, there is a possibility that the medication may be transferred to your child through breast milk. This can cause harm to an infant and must be avoided. Please discuss your options with a doctor before making your decision.

When stopping your treatment with eltrombopag, it is essential that you do not suddenly stop your medicine without the approval of your doctor. They will need to monitor your blood platelet levels and progress when you discontinue eltrombopag as to avoid any harmful effects.

Storage

This medicine should be stored in a closed container, out of the reach of children, pets and vulnerable adults. It should be kept at room temperature, away from direct heat moisture and light.

Make sure to dispose of your medicine if it reaches its expiry date or appears to be damaged. If you are taking the oral suspension dose of eltrombopag, you must throw away any liquid within 30 minutes of mixing it, to avoid consumption and harmful reactions.

Summary

Eltrombopag provides patients with effective treatment to thrombocytopenia (low platelet counts) that are the result of conditions including chronic immune thrombocytopenia purpura (ITP), chronic hepatitis C or severe aplastic anemia (SAA). Sometimes prescribed as part of a treatment regime and to be taken with other medicines, it works to increase the number of blood platelets by stimulating the bone marrow production of platelets.

Low platelet counts can be extremely harmful to patients, causing unusual bruising, bleeding and in extreme cases, internal bleeding. Not having enough platelets can severely affect recovery of surgery and certain conditions, as well as interact with conditions like chronic hepatitis C, to worsen and increase harmful effects.

Working to help your body clot blood effectively, this medication is taken orally, either in the forms of a tablet or oral suspension solution, once a day. To gain the most effective results and a higher chance of no side effects, eltrombopag requires commitment and responsibility to a strict dosing schedule which can be daunting to some. It is important that patients take this medicine on an empty stomach, as well as avoid consuming certain foods, vitamins or supplements four hours before taking the medication or two hours after. Magnesium, aluminium, iron, selenium, or zinc, can all cause the medication to be less effective and must be monitored closely before and immediately after administration. For guidance on your dosing schedule, food and on remembering when to take medication, your doctor or pharmacist will be able to provide you with useful information and tips. Before taking eltrombopag, you will be given instructions and documentation that will help your treatment process. It is important that you read all information and raise any questions with your healthcare professional before your treatment begins.

During your treatment with eltrombopag, it is important that you monitor any side effects and reactions that you may be having as a response to the medication. The most common effects tend to be stomach related, with a decrease in appetite, indigestion, heartburn and general stomach upset all being recorded. However, patients may also experience hair thinning, weakness and muscle cramps or stiffness. Rarer side effects can cause serious conditions that will require immediate medical attention and can include liver damage, blood clotting problems and allergic reactions. For this reason, it is vital that you are mindful of how your body is responding to the medicine. You will also be expected to have regular visits to your doctor to keep track of any side effects as well as ensure that the medicine is working effectively. These visits are likely to include blood tests.