Myalepta: Uses, Side Effects and Dosage

Serious Warnings and Precautions

What is Myalepta used for?

Myalepta is used to treat the complications of not having enough leptin in patients with lipodystrophy. It is used in adults, adolescents and children 2 years or over:

• who have generalised lipodystrophy (the whole of your body does not have enough fatty tissue)

It is used, when there is ongoing metabolic disease and other treatments have been ineffective, in adults, and adolescents 12 years or over:

• who have partial lipodystrophy which is inherited (also called congenital or familial lipodystrophy)
• or partial lipodystrophy has been caused by your body’s response to something such as a viral illness (also called acquired lipodystrophy).

How does Myalepta work?

Natural leptin is produced by fatty tissue and has many functions in the body including:

• controlling how hungry you feel and your energy levels
• helping the insulin in your body manage sugar levels.

Myalepta works by copying the effects of leptin. This improves the ability of the body to control energy levels.

What are the ingredients in Myalepta?

Medicinal ingredients: metreleptin

Non-medicinal ingredients: Glutamic acid, glycine, polysorbate 20, sodium hydroxide, sucrose

Myalepta comes in the following dosage forms:

Powder for solution, 3 mg/ vial, 5.8 mg/ vial and 11.3 mg/ vial

Do not use Myalepta if you:

• are allergic to any ingredients in this drug
• have general obesity that is not caused by generalised or partial lipodystrophy
• Have HIV-related lipodystrophy

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

• you are pregnant
• you have ever had problems with your blood (such as a low blood count)
• you have ever had inflammation of an organ called the pancreas (‘pancreatitis’)
• you have or ever have had problems with your immune system (autoimmune disease including autoimmune-related liver problems)
• you have ever had a type of cancer called lymphoma

Other warnings you should know about:

Lymphoma

• People with lipodystrophy can get a type of blood cancer called lymphoma, whether or not they are using Myalepta.
• However, you may be at higher risk of getting a lymphoma when using the medicinal product.
• Your doctor will decide if you should use Myalepta and will monitor you during treatment.

Serious and severe infections

• While being treated with Myalepta, your body produces antibodies that may increase the risk of developing serious or severe infections. Tell your doctor straight-away if you develop a high temperature, accompanied by increasing tiredness.

Low blood sugar with insulin or other antidiabetic medicines

• If you are using a medicine such as insulin or other medicines to treat diabetes, your doctor will closely monitor your blood sugar. Your doctor will change your dose of insulin or other medicines if needed.
• This is to prevent your blood sugar from getting too low (‘hypo-glycaemia’). Signs of low blood sugar include shaking, sweating, rapid heartbeat, change in vision, hunger, headache and change in mood.

Autoimmune Disease

• People who have or have had problems with their immune system (autoimmune disease, including autoimmune-related liver problems) may have worsening of their symptoms with

  • . Talk to your healthcare provider about what symptoms you should watch for that would warrant further testing.

Allergic reactions

• While being treated with Myalepta, you may get an allergic reaction. Tell your doctor straight-away if you have any symptoms of an allergic reaction.

Fertility

• Myalepta might increase fertility in women with lipodystrophy.

Pregnancy and breast-feeding

• If you are pregnant or breast-feeding, think you may be pregnant or are planning to have a baby, ask your doctor for advice before using this medicine.
• You should not use Myalepta if you are pregnant or might become pregnant. This is because it is not known how Myalepta will affect your unborn baby.
• Women who could get pregnant should use effective contraception, including non-hormonal methods such as condoms, while using Myalepta.
• Talk to your doctor if you are breast-feeding. You and your doctor will decide whether or not to continue breast-feeding while using this medicine.
• It is not known if Myalepta will pass into breast milk.

Driving and using machines

• Myalepta has minor influence on the ability to drive and use machines. You might feel dizzy or tired when using this medicine. If this happens, do not drive or use any tools or machines. Talk to your doctor if you are not sure.

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 Myalepta:

• statins for reducing cholesterol (such as atorvastatin)
• blood pressure medicines called ‘calcium channel blockers’
• theophylline used in lung problems such as asthma
• blood-thinning medicines (such as warfarin or phenprocoumon)
• medicines for epilepsy or fits (such as phenytoin)
• medicines which suppress the immune system (such as cyclosporine)
• medicines for sleep or anxiety called ‘benzodiazepines’

How to take Myalepta:

• Myalepta is an injection once a day under the skin (‘subcutaneous injection’). This medicine is for use in children aged 2 years and above, adolescents and adults with generalised lipodystrophy; it is also for use in children aged 12 years and above, adolescents and adults with partial lipodystrophy.

• While using this medicine, you or your child will be monitored by your doctor, who will decide the dose you or your child should use.
• See INSTRUCTIONS FOR USE for full administration instructions.

Your doctor may decide that you inject yourself. Your doctor, nurse or pharmacist will show you how to prepare and inject this medicine.

• Do not try to prepare the medicine or inject yourself if you have not been trained.

Usual dose:

How much to inject

Your dose of Myalepta may change over time depending on how this medicine works for you. The Myalepta powder is dissolved by mixing it with water for injections to make the solution for injecting. Sterile water for injection should be used in infants less than 3 years of age, or in adults with a known hypersensitivity to benzyl alcohol. Bacteriostatic water for injection should be used for older children and adults. Read the INSTRUCTIONS FOR USE for how to make the solution before injecting.

Your doctor will have prescribed the correct dose for you, based on the following:

• If you weigh 40 kg or less:

  • A starting dose is 0.06 mg (0.012 mL of solution) for each kilogram of body weight.

• If you are male and weigh more than 40 kg:

  • A starting dose is 2.5 mg (0.5 mL of solution).

• If you are female and weigh more than 40 kg:

  • A starting dose is 5 mg (1 mL of solution).

Your doctor or pharmacist will tell you how much of the solution to inject. If you are not sure how much of the solution to inject, talk to your doctor or pharmacist before injecting.

The syringe you need to use to inject this medicine depends on the dose prescribed for you.

• See the INSTRUCTIONS FOR USE to find out which syringe to use.

To know how much medicine to inject (in mL), you divide your dose (in mg) by 5.

• For example, if you have been prescribed a 5 mg dose of Myalepta, 5 mg divided by 5 gives you 1 mL which is the amount you need to inject of the solution, using a 1 mL syringe.

If your dose is 1.50 mg (0.30 mL of solution) or less, you will need to use a 0.3 mL syringe.

• The 0.3 mL syringe will show the injection amount in ‘Unit’ instead of ‘mL’. See the INSTRUCTIONS FOR USE for more information on reading and using the different syringes.
• To know how much solution to inject (in Units), divide your dose (in mg) by 5, and then multiply it by 100.

If you need to inject 1 mL or more of Myalepta solution, your doctor might tell you to give the dose as two separate injections. This can help make the injections more comfortable.

• You must use a clean syringe and needle for both injections.

If you are not sure how much of the solution to inject, talk to your doctor or pharmacist before injecting.

Overdose:

In one case, an infant received a 10-fold overdose of Myalepta for 8 months. This led to large weight loss causing vitamin deficiency, low iron (anaemia) and malnutrition. The infant got better when the dose was changed.

Missed Dose:

If you forget to inject a dose, inject it as soon as you remember. Then have your normal dose the next day.

Do not use a double dose to make up for a forgotten dose.

If you have injected less Myalepta than you should, talk to your doctor straight away. Your doctor will monitor you for side effects.

What are possible side effects from using Myalepta?

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

• loss of interest in food
• headache
• hair loss
• feeling tired
• weight loss
• joint pain
• back pain
• arm or leg pain
• cough
• constipation
• abdominal pain
• stuffy or runny nose
• vomiting
• ear pain
• a faster than normal heart rate
• chest infection

Serious side effects and what to do about them

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:

Myalepta should be stored in the refrigerator at 2°C to 8°C and protected from light until preparing for use. Keep Myalepta vials in the carton when not in use.

Do not freeze Myalepta.

Do not use this medicine if the solution is not clear, is coloured or has bits or lumps in it.

Use with BWFI: when 11.3 mg Myalepta is reconstituted with BWFI, the vial can be used for multiple doses within 3 days when stored in the refrigerator at 2°C to 8°C and protected from light. The BWFI diluent contains 0.9% benzyl alcohol as a preservative.

Use with SWFI: when Myalepta is reconstituted with SWFI, the vial can be used for a single dose should be administered immediately. Unused reconstituted solution cannot be saved for later use and should be discarded.

After reconstitution, the vials should not be frozen (below 0°C) or shaken vigorously. If the reconstituted product is inadvertently frozen, it should be thrown away.

Keep out of reach and sight of children.

If you want more information about Myalepta:

• 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 website www.amrytpharma.com, or by calling 1-800-696-1341 or emailing medinfo@amrytpharma.com.

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INSTRUCTIONS FOR USE

READ THIS FOR SAFE AND EFFECTIVE USE OF YOUR MEDICINE

MYALEPTA

Metreleptin for injection

Read this carefully before you start taking Myalepta and each time you get a refill. Before you begin self-administering this medicine at home, your doctor, nurse or pharmacist will train you how to prepare and inject Myalepta. Contact them if you are unclear about anything or if you need more information or help. Take your time to carefully prepare and inject your medicine, which when including the period of the vial warming up after being taken out of the fridge, can be approximately 20 minutes in total.

Make sure you have all the supplies listed below BEFORE using Myalepta.

You can get these supplies with a prescription from your healthcare provider, from a retail or hospital pharmacy, or the specialty pharmacy that distributes Myalepta.

• a vial with liquid for mixing Myalepta

  • Sterile water for injection should be used in infants less than 3 years of age, or in adults with a known hypersensitivity to benzyl alcohol
  • Bacteriostatic water for injection should be used for older children and adults
• a 3 mL syringe with a longer needle for mixing Myalepta

• a vial with Myalepta powder

  • 3 mg and 5.8 mg vial are for single use reconstituted with SWFI. Should be used immediately and any remaining reconstituted solution should be discarded.
  • 11.3 mg vial is for multi use reconstituted with BWFI. Should be used within 3 days of reconstitution when stored at 2°C to 8°C and protected from light.

• a syringe for injecting the Myalepta medicine under your skin – this syringe has a much shorter needle.

  • The size of this second syringe will be chosen by your doctor or pharmacist for your dose of Myalepta.

    • If your dose is 1.25 mg or less - you will use a 0.3 mL syringe.
    • If your dose is more than 1.25 mg up to 5 mg - you will use a 1 m syringe.
    • If your dose is more than 5 mg - you will use a 3.0 mL syringe.
• 2 alcohol wipes
• 1 sharps container for throwing away used needles and syringes. See "Disposing of used needles and syringes" at the end of these instructions.
• Stickers to note discard date for mixed medicine

How to read your syringes:

0.3 mL syringe (Figure B)

• The 0.3 mL syringe shows the injection amount in ‘U’ instead of ‘mL’
• 1 U is the same as 0.01 mL. See section 3, “How much to inject” for more information.
• Each 0.05 mL is shown as a number with a big line. This is the same as 5 U.
• Each 0.005 mL is shown as a smaller line between the big lines. This is the same as 0.5 U.

Figure B

1 mL syringe (Figure C)

• Each 0.1 mL is shown as a number with a big line.
• Each 0.05 mL is shown as a medium size line.
• Each 0.01 mL is shown as a smaller line.

Figure C

3.0 mL syringe (Figure D)

• Each 0.5 mL is shown as a number next to a big line.
• Each 0.1 mL is shown as a smaller line between the big lines.

Figure D

The 3 mL syringe has a longer needle (see Figure B).

The 3 mL syringe is the syringe you will use to mix Myalepta. Always fill the 3 mL syringe with 2.2 mL of liquid. Do not inject yourself with the 3 mL syringe.

Figure E

The injection syringes have a shorter needle (see Figures B-D).

• The size of this injection syringe will be chosen by your doctor or pharmacist for your dose of Myalepta.

  • If your dose is 1.25 mg or less - you will use a 0.3 mL syringe.
  • If your dose is more than 1.25 mg up to 5 mg - you will use a 1 mL syringe.
  • If your dose is more than 5 mg - you will use a 3.0 mL syringe.

STEP 1: Getting Started

Your dose of Myalepta may change over time, depending on how Myalepta works for you. So it is important to keep track of your dose. On the line below, write down your dose in mL and the date. Be sure to keep this up-to-date if your dose changes:

Take 1 Myalepta vial out of the refrigerator 10 minutes before you plan to inject to allow it to reach room temperature.

Set 1 vial with the liquid you will need to mix Myalepta on your work surface.

Check the powder in the Myalepta vial. It should be white. Do not use Myalepta if the powder is discolored. Throw it away and get a new one.

Check the expiration date printed on the Myalepta vial. Do not use Myalepta past the expiration date printed on the vial (see Figure F).

Figure F

For this step, you will need:

STEP 2: Filling the 3 mL syringe (used to mix Myalepta) with 2.2 mL of liquid

For this step, you will need:

Pull the needle cover straight off. Do not twist the needle when removing the cover. Put the needle cover in the sharps disposal container.	Pull down the plunger to fill the syringe with air. You must first fill the syringe with air and put that air into the vial to make it easier to later fill the syringe with liquid.	Line up the top rim of the plunger with the black 2.2 mL line.
Set the vial with the liquid on the work surface. Insert the needle into the top of the vial.		Push the plunger down all the way to fill the vial with air.

With the needle still in the vial, turn the vial and syringe upside down. Keep the whole needle in the liquid.	Pull down the plunger until the top rim of the plunger lines up with the black 2.2 mL line.	Check to see if there is an air pocket in the syringe. If you see an air pocket, tap the side of the syringe to move the air pocket to the top of the syringe.	Push the plunger up to remove the air pocket. You must remove the air pocket to be able to fill the syringe with 2.2 mL of liquid.

Tip: You will always fill the 3 mL syringe with 2.2 mL of liquid.

Check to see if there are large air bubbles in the syringe. If you see large air bubbles in the syringe, tap the syringe to move the air bubbles to the top. If there are a few small bubbles left, that is okay.	Push the plunger up to remove as many large air bubbles as you can.	Pull down the plunger so the top rim of the plunger lines up with the black 2.2 mL line. Keep the whole needle in the liquid.	Remove the needle from the vial. Be careful not to move the plunger. Keep the syringe in your hand. Do not set it down. For instructions on how to discard the used vial of liquid, read the carton that contained those vials.

STEP 3: Preparing Myalepta

Note: If you already mixed your Myalepta before today, go to “Using a vial of mixed Myalepta” at the end of this step.

Option 1: Mixing a new vial of Myalepta:

For this step, you will need:

The 3 mL syringe filled with 2.2 mL of liquid (from Step 2)	Vial with powder (from Step 1)	Sharps disposal container

Tip: If your vial of Myalepta is not mixed well, go back to Step 3c. Note: Go to Step 4 if you just mixed a new vial of Myalepta.

Option 2: Using a vial of mixed Myalepta:

Note: For newborns or infants using Myalepta, throw away any unused mixed Myalepta right away. Do not store it for reuse.

For this step, you will need:

Choose a clean, flat work surface large enough to let you prepare the medicine.

Clean the top of the vial with the alcohol wipe.	Check that the Myalepta is mixed well and is clear. You should not see any clumps, powder, bubbles, or foam. If you see clumps, powder, bubbles, or foam, throw away the vial in the sharps disposal container.

Important: Do not mix any liquid or mixed medicine from another vial with the vial you just cleaned.

STEP 4: Filling the syringe used for injecting Myalepta

Ensure the proper size syringe is selected.

For this step, you will need:

Remove the injection syringe from the plastic wrapper. Always use a new syringe.

Hold the vial with the mixed Myalepta. Insert the needle into the top of the Myalepta vial.	Push the plunger down all the way, to fill the vial with air.

With the needle still in the vial, turn the vial and syringe upside down. Keep the whole needle in the liquid. It is okay if the plunger moves down.	Pull down the plunger until the top rim of the plunger lines up with the black line of the dose prescribed by your healthcare provider.	Check to see if there is an air pocket in the syringe. If you see an air pocket, tap the side of the syringe to move the air pocket to the top of the syringe.	Push the plunger up to remove the air pocket. You must remove the air pocket to be able to fill the syringe with a full dose of Myalepta.

STEP 5: Injecting Myalepta

For this step, you will need:

Important:

Inject Myalepta under the skin (subcutaneous). Do not inject Myalepta into a muscle or vein.

Important:

Unused Myalepta mixed with sterile water for injection (for infants less than 3 years of age, or adults with a known hypersensitivity to benzyl alcohol), must be thrown away. Do not store it for reuse.

Myalepta mixed with bacteriostatic water for injection can be stored for reuse.

Important:

Stickers to Note the Last Day You Can Use Myalepta When Mixed with Bacteriostatic Water for Injection

STEP 6: Disposing of used needles and syringes:

Put your used needles and syringes in a sharps disposal container right away after use. Do not throw away (dispose of) loose needles and syringes in your household trash.

If you want more information about Myalepta:

• 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 website www.amrytpharma.com, or by calling 1-800-696-1341.

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