Betaseron: Uses, Side Effects and Dosage

What is Betaseron used for?

Betaseron (BAY-tah-SEER-on) is used for the treatment of relapsing forms of multiple sclerosis (MS) to reduce the frequency of flare-ups in ambulatory patients (ie, patients who are able to walk without help).

Betaseron is also used for the treatment of secondary- progressive multiple sclerosis to slow the progression of disability and to reduce the frequency of flare-ups.

Betaseron is also approved for use in patients who have symptoms which are likely to be a first sign of multiple sclerosis (single clinical event suggestive of multiple sclerosis). Any other reasons which could explain the symptoms have to be ruled out. Your doctor will perform a test using an imaging machine (magnetic resonance imaging [MRI]). This test has to show at least two signs of inflammation in the central nervous system suggestive of multiple sclerosis.

How does Betaseron work?

Multiple sclerosis is a life-long disease that affects your nervous system (ie, brain and spinal cord) by destroying the protective covering (myelin) that surrounds your nerve fibers. An abnormal response by the body’s immune system is thought to play an important part in the process which damages the nervous system.

Betaseron is a form of protein called interferon beta that occurs naturally in the body. Interferon beta has been shown to modify the immune system response, but the exact way that Betaseron works in MS is unknown. Betaseron will not cure MS but it has been shown to decrease the number of flare-ups and slow the occurrence of some of the physical disabilities that are common in people with MS.

What are the ingredients in Betaseron?

Medicinal ingredients: interferon beta-1b.

Non-medicinal ingredients: human albumin, mannitol, sodium chloride, water for injection

Betaseron comes in the following dosage forms:

Betaseron (interferon beta-1b) is presented in single-use vials of lyophilized powder. To make a solution for injection, the powder must be dissolved using the supplied prefilled diluent syringe and vial adapter (see Steps 1, 2, 3, and 4).

Do not use Betaseron if:

• you have had previous allergic reactions, such as difficulty breathing, itching, flushing or hives, to interferon beta or to any of the nonmedicinal ingredients (see above).
• you have decompensated liver disease

To help avoid side effects and ensure proper use, talk to your healthcare professional before you take Betaseron. Talk about any health conditions or problems you may have, including:

• Depression, anxiety (feeling uneasy, nervous or fearful for no reason) or trouble sleeping;
• Liver problems;
• Epilepsy or a history of seizures;
• Heart problems;
• Problems with your thyroid gland;
• Problems with your kidneys;
• Are breast-feeding or are planning to become pregnant.

Other warnings you should know about:

Allergic reactions: Some patients taking Betaseron have had severe allergic reactions leading to difficulty breathing and swallowing; these reactions can happen quickly. Allergic reactions can happen after your first dose or may not happen until after you have taken Betaseron many times. Less severe allergic reactions such as rash, itching, skin bumps, or swelling of the mouth or tongue can also happen. If you think you are having an allergic reaction, stop using Betaseron immediately and call your doctor.

Depression: Some patients treated with interferons, including Betaseron, have become seriously depressed (feeling sad). Some patients have thought about or have attempted to kill themselves. Depression (a sinking of spirits or sadness) is not uncommon in people with multiple sclerosis. However, if you are feeling noticeably sadder or helpless, or feel like hurting yourself or others, you should tell a family member or friend right away and call your doctor or healthcare provider as soon as possible. Your doctor may ask that you stop using Betaseron. Before starting Betaseron, you should also tell your doctor if you have ever had any mental illness, including depression, and if you take any medications for depression.

Kidney problems: Blood clots in the small blood vessels may occur during your treatment. These blood clots could affect your kidney (thrombotic thrombocytopenic purpura or haemolytic uremic syndrome). This might happen several weeks to several years after starting Betaseron and may cause death. Talk to your doctor if you experience the following symptoms: increased bruising, bleeding, extreme weakness, headache, dizziness or light-headedness. Your doctor may want to check your blood pressure, blood (platelet count) and the function of your kidney.

Inform your doctor if you notice paleness, yellow skin or dark-coloured urine that may be accompanied by unusual dizziness, tiredness and shortness of breath. These may be symptoms of a breakdown of red blood cells. This might happen several weeks to several years after starting Betaseron. Inform your doctor as well about other drugs that you are taking.

Liver problems: Betaseron, like other interferon beta products, may cause severe liver problems. Your liver function may be affected. Elevations of liver function values occurred very commonly in patients treated with Betaseron in clinical studies and in most cases were mild and temporary. Rare cases of severe liver injury have been reported. Your healthcare provider may ask you to have regular blood tests to make sure that your liver is working properly. Some of the symptoms of liver problems are yellowing of the skin and whites of the eyes, malaise (a vague feeling of discomfort), fatigue, nausea, vomiting, abdominal pain, dark urine and itching of the skin. If you develop these symptoms while taking Betaseron, you should call your doctor right away.

Seizures: Some patients have had seizures while taking interferons. It is not known whether the seizures are related to the effects of MS, to interferons, or to a combination of both. If you have a seizure while taking Betaseron, you should call your doctor right away.

Heart problems: During treatment with Betaseron, cardiomyopathy (a disease of the heart muscle) has been reported in rare cases. If you experience symptoms like irregular heartbeat, fluid retention (swelling) in the lower parts of your body (eg, ankles, legs), or shortness of breath, call your doctor immediately.

Thyroid problems: Some people taking Betaseron may develop changes in the function of their thyroid. Symptoms of these changes include feeling hot or cold much of the time or change in your weight (gain or loss) without a change in your diet or the amount of exercise you are getting.

Gastrointestinal problems: In rare cases, an inflammation of the pancreas has been observed with Betaseron use, often associated with an increase of triglycerides (a type of fat in the blood). If you have suffered from increased triglycerides or have had problems with your pancreas, please tell your doctor.

Women of childbearing potential: If you are a woman of childbearing potential and are taking Betaseron, you should use effective methods of contraception unless you are planning to become pregnant and have talked to your doctor about the potential risks and benefits of staying on Betaseron. It is not known if interferons interfere with hormonal contraceptives.

Available data with the use of Betaseron in pregnant women (mostly during the first trimester) suggest that spontaneous abortions (miscarriage) and congenital abnormalities (malformations) in their children did not happen more often than in the general population. Spontaneous abortions (miscarriage) have been reported in patients with multiple sclerosis in clinical studies, however not more often than in the general population. Administration of doses that were higher than the dose normally used to treat patients with multiple sclerosis caused an increased rate of miscarriages in studies done in monkeys. However, when pregnancies in these studies were carried to term, the animals were born without malformations.

Breast-feeding: You should talk to your doctor if you are breast-feeding an infant. It is not known if Betaseron can be passed to an infant in mother’s milk, however you should discuss the matter with your doctor and make a decision whether to stop breast-feeding or stop using Betaseron.

Immune system problems: The administration of interferons to patients with a pre-existing rare disturbance of the immune system where abnormal proteins are found in the blood (monoclonal gammopathy) has been associated with problems with small blood vessels leading to shock (collapse) and, in some cases, death.

Human albumin: This product contains a protein (albumin) extracted from human blood and so carries an extremely remote risk for transmission of viral diseases. A theoretical risk for transmission of a disease affecting the nervous system (Creutzfeld-Jakob disease) is also considered extremely remote.

Injection site reactions: Injection site reactions are common. They include redness, pain, swelling, infection, and discoloration. Less frequently, injection site necrosis (skin breakdown and tissue destruction) has been observed. To minimize the chance of a reaction, such as infection, change injection areas every time you inject yourself and wait at least one week before reusing an area. Do not inject into skin that is tender, red, or hard. Do not use any areas where you feel lumps, depressions, pain, or discoloration. Injection site reactions may occur less frequently if you use an autoinjector and by rotating injection sites. Talk to your doctor or nurse if one of your injection sites becomes swollen and painful or the area looks infected and it doesn’t heal within a few days. If you experience a break in the skin or drainage of fluid from the injection site, consult your doctor. The occurrence of injection site reactions decreases over time.

Tell your healthcare professional about all the medicines you take, including any drugs, vitamins, minerals, natural supplements or alternative medicines.

The following may interact with Betaseron:

With the exception of steroids or ACTH (anti-inflammatory medicines), the use of Betaseron together with other substances that modify the immune system response was not studied. Caution should be exercised when interferons are given in combination with other drugs which need a certain liver enzyme system (the cytochrome P450 system) for their metabolism. These drugs include some commonly used drugs against fever and pain.

You should tell your doctor if you are taking any other prescription or nonprescription medicines, including vitamin and mineral supplements and herbal products.

How to take Betaseron:

Betaseron is intended for use under the guidance and supervision of a physician. Your physician or his/her delegate should instruct you in the preparation and self-injection technique of Betaseron. Do not begin your Betaseron treatment without training.

Usual dose:

Betaseron should be used as prescribed by your doctor. The usual dose is 1 mL of prepared Betaseron solution injected subcutaneously (under the skin) every other day. This is equal to 0.25 mg (8 MIU).

If you have been prescribed Betaseron because you have symptoms likely to be a first sign of multiple sclerosis, your treatment should be started at a low dose of 0.25 mL (0.0625 mg or 2 MIU). Your dose will then be increased slowly until you reach a dose of 1 mL. Your individual tolerability of Betaseron will determine the rate of dose increase. Your doctor will decide this with you.

Your injections should be about 48 hours (two days) apart, so it is best to take them at the same time each day, preferably in the evening before bedtime.

Self-Injection Procedure

SAFETY TIPS

• Use only the supplies that come with your Betaseron package.
• Use only the diluent from the prefilled syringe.
• Wash your hands thoroughly with soap and water before starting.
• Keep the items sterile. Do not touch the needle, the piercing spike of the vial adapter, or the top of the cleaned vial.
• Make sure none of the items in your package have been opened or are damaged.
• Do not reuse opened materials. Throw away any unused portions of Betaseron and diluent.
• Throw away used syringes and needles in the proper disposal container.

STEP 1: CHOOSING AN INJECTION SITE

Betaseron should be injected into subcutaneous tissue (under the skin, between the fat layer and the muscles beneath). The best areas for injection are loose and soft, away from joints.

• Choose an injection site from the following areas (Figure 6):

  A Right arm, upper back portion (at least 10-15 cm below the shoulder and 10-15 cm above the elbow)

  B Left arm, upper back portion (at least 10-15 cm below the shoulder and 10-15 cm above the elbow)

  C-D Abdomen, above the waistline (at least 5 cm on either side of the navel)

  E Right thigh (at least 5 cm above the knee and 5 cm below the groin)

  F Left thigh (at least 5 cm above the knee and 5 cm below the groin)

  G Left buttock (upper, outer portion)

  H Right buttock (upper, outer portion)

• Change injection areas every time you inject yourself. Give the site time to recover from the last injection. This will help prevent injection site reactions. Wait at least one week before reusing an area.

• Do not use any areas where you feel lumps, depressions, pain, or discoloration; talk to your healthcare professional about anything you find.

  Figure 6

Front

Back

• Keep a record of when and where you are giving yourself injections. Use the Betaseron diary in your training kit.

STEP 2: CHECKING THE CONTENTS OF THE PACK

Place the Betaseron single-use carton on a clean, flat surface in a well-lighted area. Ensure the pack contains:

• Vial of Betaseron
• Prefilled diluent syringe
• Vial adapter with attached 30-gauge, ½” needle in blister pack

NOTE: Please ensure you have two (2) alcohol wipes, and a clean, dry cotton ball or gauze prior to preparing Betaseron for injection.

STEP 3: INITIAL PREPARATION

1. 1. Wash your hands thoroughly with soap and water.
2. 2. Take out all the contents.

NOTE: Be sure the vial adapter blister pack is sealed and the rubber cap is firmly attached to the diluent syringe.

1. 3. Check the expiry date on the Betaseron vial and the prefilled diluent syringe.

STEP 4: RECONSTITUTING Betaseron

1. 1. Take the protective cap off the vial.
2. 2. Use an alcohol wipe to clean the top of the vial. Move the wipe in one direction only. NOTE: Leave the alcohol wipe on top of the vial until Step 4, point 4.
3. 3. Peel off the vial adapter blister pack label but do not remove the vial adapter. NOTE: Be sure to avoid touching the vial adapter, in order to maintain its sterility.
4. 4.

   Remove the alcohol wipe on top of the Betaseron vial. Place the vial adapter (still in the blister packaging) on top of the Betaseron vial by pushing it until it pierces the rubber top of the Betaseron vial and snaps in place (Figure 7). Remove the blister packaging from the vial adapter.

   Figure 7

1. 5. Remove the rubber cap from the diluent syringe with a twist and pull motion. Discard the rubber cap.
2. 6.

   Connect the syringe with the vial adapter by turning clockwise and tighten carefully. This will form the syringe assembly (Figure 8).

   Figure 8

1. 7.

   It is important to slowly push the plunger of the diluent syringe all the way in, keeping the syringe assembly at an angle. This will transfer all of the diluent drop by drop into the Betaseron vial (Figure 9).

   Figure 9

1. 8. Keeping the plunger depressed, with the syringe assembly attached, swirl the vial gently to completely dissolve the white cake of Betaseron. (DO NOT SHAKE.)
2. 9. Look closely at the Betaseron solution for particles. It should be clear. NOTE: If the mixture contains particles or is discolored, discard it and start again. Foaming may occur during reconstitution, or if it is swirled or shaken too vigorously. If so, allow the vial to sit undisturbed until the foam settles.

STEP 5: PREPARING THE INJECTION

1. 1. Keeping the plunger depressed, turn the assembly upside down (ie, 180 degrees) so that the vial is on top. The syringe remains horizontal (Figure 10).
2. 2. Slowly pull the plunger back to withdraw the entire contents of the Betaseron vial into the syringe (Figure 10).

NOTE: If 1 mL of clear solution cannot be withdrawn from the vial, discard the vial and syringe and start over.

Figure 10

1. 3. Turn the syringe assembly so that the needle end is pointing up. Tap the syringe gently so any air bubbles will rise to the top. Tap the syringe with the side of your finger. Do not tap the syringe with a hard object because the glass syringe could break. Push the plunger to the 1 mL mark (or to the amount prescribed by your doctor) to remove any air bubbles. If you are injecting less than 1.0 mL, there might not be any air bubbles; however, for the full dose injection, some air bubbles might be seen. Remove them by gently tapping the syringe and pushing the plunger to the respective marking on the syringe. NOTE: If too much solution is expelled into the vial, repeat Step 5, points 1, 2, and 3.
2. 4.

   Remove the vial adapter and the vial from the syringe by grasping the plastic cap of the vial adapter and twisting it clockwise, as shown in Figure 11. This will release the vial adapter, with the vial, from the syringe but leave the needle on the syringe (Figure 11).

   Figure 11

1. 5. You have now reconstituted your Betaseron and are ready to be injected.

The injection should be administered immediately after mixing. If you are unable to give the injection immediately, you may refrigerate the medication in the syringe and inject within three hours. Do not freeze.

STEP 6: INJECTING Betaseron

Optional - Autoinjector: If you have been given an autoinjector, you should follow the detailed instructions that are supplied with it.

The Single-use carton can only be used with the BETAJECT® Lite, BETACOMFORT® or BETACONNECT® autoinjector.

1. 1. Use a fresh alcohol wipe to clean the skin at the injection site. Use a circular motion from the center of the injection site outward. Let the alcohol dry.
2. 2. Throw away the wipe.
3. 3. Remove the protective needle guard from the needle by pulling it without turning.
4. 4. Gently pinch the skin around the site to lift it up a bit.
5. 5. Stick the needle straight into the skin at a 90° angle with a quick, firm motion.
6. 6. Inject the drug by using a slow, steady push (push the plunger all the way in until the syringe is empty).
7. 7. Remove the needle from the skin.
8. 8. Gently massage the injection site with a clean, dry cotton ball or gauze (or as directed by your healthcare professional).
9. 9. Throw away the syringe in the disposal unit.
10. 10. Discard all other components.

Overdose:

If you accidentally take more than your prescribed dose, or take it two days in a row, call your doctor right away.

Missed Dose:

If you miss a dose, you should take your next dose as soon as you remember or are able to take it. Your next injection should be given about 48 hours (two days) after that dose.

What are possible side effects from using Betaseron?

These are not all the possible side effects you may have when taking Betaseron. If you experience any side effects not listed here, tell your healthcare professional.

As with any prescription medication, side effects related to therapy can occur. Consult your doctor if you have any problems, whether or not you think they may be related to Betaseron.

Flu-like symptoms: Flu-like symptoms are also common. They include fever, chills, sweating, fatigue, and muscle aches. For many patients, these symptoms will lessen or go away over time. Taking Betaseron at night may help lessen the impact of flu-like symptoms. You should talk to your doctor about whether you should take an over-the-counter medicine for pain or fever reduction (nonsteroidal anti-inflammatory drugs [NSAIDs] or acetaminophen) before or after taking your dose of Betaseron.

Serious side effects and what to do about them

If you have a troublesome symptom or side effect that is not listed here or becomes bad enough to interfere with your daily activities, tell your healthcare professional.

Reporting Side Effects

Storage:

Before reconstitution: Store between 2°C to 30°C. Do not freeze.

After reconstitution: If not used immediately, reconstituted Betaseron must be refrigerated and used within three hours. Do not freeze.

Keep out of reach and sight of children. Keep syringes and needles away from children.

Do not reuse needles or syringes. Discard used syringes and needles in a syringe disposal unit. Do not throw away any medicines in the garbage or down the sink or toilet. Ask your pharmacist how to throw away unused Betaseron. These measures will help to protect the environment.

If you want more information about Betaseron:

• Talk to your healthcare professional
• Find the full product monograph that is prepared for healthcare professionals and includes this Patient Medication Information by visiting the Health Canada website: https://www.canada.ca/en/health-canada/services/drugs-health-products/drug-products/drug-product-database.html; the manufacturer’s http://www.bayer.ca, or by contacting Bayer Medical Information at 1-800-265-7382 or canada.medinfo@bayer.com.

Last Revised August 10, 2023

© 2023, Bayer Inc.

® TM see www.bayer.ca/tm-mc