Isentress: Uses, Side Effects and Dosage

What are ISENTRESS and ISENTRESS HD?

ISENTRESS is a prescription medicine used with other HIV-1 medicines to treat Human Immunodeficiency Virus-1 (HIV-1) infection in adults, and in children weighing at least 4.4 pounds (2 kg). HIV is the virus that causes AIDS (Acquired Immune Deficiency Syndrome).

ISENTRESS HD is a prescription medicine used with other HIV-1 medicines to treat HIV-1 infection in adults, and in children weighing at least 88 pounds (40 kg).

ISENTRESS should not be used in children who weigh less than 4.4 pounds (2 kg).

Before you take ISENTRESS or ISENTRESS HD, tell your doctor about all of your medical conditions, including if you:

• have liver problems
• have a history of a muscle disorder called rhabdomyolysis or myopathy
• have increased levels of creatine kinase in your blood
• have phenylketonuria (PKU). ISENTRESS chewable tablets contain phenylalanine as part of the artificial sweetener, aspartame. The artificial sweetener may be harmful to people with PKU.
• receive kidney dialysis treatment

• are pregnant or plan to become pregnant. It is not known if ISENTRESS or ISENTRESS HD can harm your unborn baby.

  Pregnancy Registry: There is a pregnancy registry for women who take ISENTRESS or ISENTRESS HD during pregnancy. The purpose of this registry is to collect information about the health of you and your baby. Talk to your doctor about how you can take part in this registry.

• are breastfeeding or plan to breastfeed. Do not breastfeed if you take ISENTRESS or ISENTRESS HD.

  • You should not breastfeed if you have HIV-1 because of the risk of passing HIV-1 to your baby.
  • It is not known if ISENTRESS or ISENTRESS HD can pass into your breast milk.
  • Talk with your doctor about the best way to feed your baby.

Tell your doctor about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Some medicines interact with ISENTRESS and ISENTRESS HD.

• Keep a list of your medicines to show your doctor and pharmacist.
• You can ask your doctor or pharmacist for a list of medicines that interact with ISENTRESS and ISENTRESS HD.
• Do not start taking a new medicine without telling your doctor. Your doctor can tell you if it is safe to take ISENTRESS or ISENTRESS HD with other medicines.

How should I take ISENTRESS or ISENTRESS HD?

• Take ISENTRESS or ISENTRESS HD exactly as prescribed by your doctor.
• Do not change your dose of ISENTRESS or ISENTRESS HD or stop your treatment without talking with your doctor first.
• Stay under the care of your doctor during treatment with ISENTRESS or ISENTRESS HD.
• ISENTRESS film-coated tablets and ISENTRESS HD film-coated tablets must be swallowed whole.

• ISENTRESS chewable tablets may be chewed or swallowed whole.

  For children who have trouble chewing the 25 mg chewable tablet, the tablet may be crushed and given as follows:

  • Place the tablet(s) in a small, clean cup. For each tablet, add about 1 teaspoonful (5 mL) of liquid (for example, water, juice, or breast milk).
  • Within 2 minutes, the tablet(s) will fall apart in the liquid.
  • Using a spoon, crush any remaining pieces of the tablet(s). Give the child the entire mixture to swallow right away.
  • If any of the dose is left in the cup, add another teaspoonful (5 mL) of liquid, swirl and give to the child right away.
• Do not switch between the film-coated tablet, the chewable tablet, or the oral suspension without talking with your doctor first.
• Do not switch between the ISENTRESS 400 mg film-coated tablet and the ISENTRESS HD 600 mg film-coated tablet if your prescribed dose is 1200 mg.
• Do not run out of ISENTRESS or ISENTRESS HD. The virus in your blood may increase and the virus may become harder to treat. Get a refill of your ISENTRESS or ISENTRESS HD from your doctor or pharmacy before you run out.
• Take ISENTRESS or ISENTRESS HD on a regular dosing schedule as instructed by your doctor. Do not miss doses.
• If you take too much ISENTRESS or ISENTRESS HD, call your doctor or go to the nearest hospital emergency room right away.

If ISENTRESS for oral suspension is prescribed for your child, be sure to read the following information:

• Before giving the first dose of ISENTRESS for oral suspension, read the Instructions for Use booklet that comes with ISENTRESS for oral suspension for information about the correct way to mix and give a dose of ISENTRESS for oral suspension to your child. Keep the booklet and follow it each time you prepare the medicine. Bring this booklet to your child's appointments.
• Make sure your doctor shows you how to mix and give the right dose of ISENTRESS for oral suspension to your child. If you have questions about how to mix or give ISENTRESS for oral suspension, talk with your doctor or pharmacist.
• Give the dose of ISENTRESS for oral suspension within 30 minutes of mixing.
• If your child does not take all of the prescribed dose or spits some of it out, call your doctor to find out what to do.
• Your child's dose will change over time. Make sure you follow your doctor's instructions. Your doctor will tell you if and when to stop giving ISENTRESS to your child.

What are the possible side effects of ISENTRESS or ISENTRESS HD?

ISENTRESS and ISENTRESS HD can cause serious side effects including:

• Severe skin reactions and allergic reactions. Some people who take ISENTRESS or ISENTRESS HD develop severe skin reactions and allergic reactions that can be serious, and may be life-threatening or lead to death.

  • If you develop a rash, call your doctor right away.
  • If you develop a rash with any of the following symptoms, stop using ISENTRESS or ISENTRESS HD and call your doctor or get medical help right away:

• fever
• generally ill feeling
• extreme tiredness
• muscle or joint aches
• blisters or sores in mouth

• blisters or peeling of the skin
• redness or swelling of the eyes
• swelling of the mouth, lips, or face
• problems breathing

Sometimes allergic reactions can affect body organs, such as your liver. Call your doctor right away if you have any of the following signs or symptoms of liver problems:

• yellowing of your skin or whites of your eyes
• dark or tea colored urine
• pale colored stools (bowel movements)

• nausea or vomiting
• loss of appetite
• pain, aching, or tenderness on the right side of your stomach area

• Changes in your immune system (Immune Reconstitution Syndrome) can happen when you start taking HIV-1 medicines. Your immune system may get stronger and begin to fight infections that have been hidden in your body for a long time. Tell your doctor right away if you start having new symptoms after starting your HIV-1 medicine.

The most common side effects of ISENTRESS and ISENTRESS HD include:

• trouble sleeping
• headache

• dizziness
• nausea
• tiredness

Less common side effects of ISENTRESS and ISENTRESS HD include:

• depression
• hepatitis
• genital herpes
• herpes zoster including shingles
• kidney failure

• kidney stones
• indigestion or stomach area pain
• vomiting
• suicidal thoughts and actions
• weakness

Tell your doctor right away if you get unexplained muscle pain, tenderness, or weakness during treatment with ISENTRESS or ISENTRESS HD. These may be signs of a rare serious muscle problem that can lead to kidney problems.

These are not all the possible side effects of ISENTRESS and ISENTRESS HD.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

How should I store ISENTRESS and ISENTRESS HD?

ISENTRESS and ISENTRESS HD film-coated tablets:

• Store ISENTRESS and ISENTRESS HD film-coated tablets at room temperature between 68°F to 77°F (20°C to 25°C).
• Store ISENTRESS and ISENTRESS HD film-coated tablets in the original package with the bottle tightly closed.
• Keep the drying agent (desiccant) in the ISENTRESS and ISENTRESS HD bottle to protect from moisture.

ISENTRESS chewable tablets:

• Store ISENTRESS chewable tablets at room temperature between 68°F to 77°F (20°C to 25°C).
• Store ISENTRESS chewable tablets in the original package with the bottle tightly closed.
• Keep the drying agent (desiccant) in the bottle to protect from moisture.

ISENTRESS for oral suspension:

• Store ISENTRESS for oral suspension at room temperature between 68°F to 77°F (20°C to 25°C).
• Store in the original container. Do not open the foil packet until ready for use.

Keep ISENTRESS and all medicines out of the reach of children.

General information about the safe and effective use of ISENTRESS and ISENTRESS HD

Medicines are sometimes prescribed for purposes other than those listed in a Patient Information Leaflet.

Do not use ISENTRESS or ISENTRESS HD for a condition for which it was not prescribed. Do not give ISENTRESS or ISENTRESS HD to other people, even if they have the same symptoms that you have. It may harm them. You can ask your doctor or pharmacist for information about ISENTRESS or ISENTRESS HD that is written for health professionals.

What are the ingredients in ISENTRESS and ISENTRESS HD?

ISENTRESS 400 mg film-coated tablets:

Active ingredient: raltegravir

Inactive ingredients: calcium phosphate dibasic anhydrous, hypromellose 2208, lactose monohydrate, magnesium stearate, microcrystalline cellulose, poloxamer 407 (contains 0.01% butylated hydroxytoluene as antioxidant), sodium stearyl fumarate.

The film coating contains: black iron oxide, polyethylene glycol 3350, polyvinyl alcohol, red iron oxide, talc and titanium dioxide.

ISENTRESS HD 600 mg film-coated tablets:

Active ingredient: raltegravir

Inactive ingredients: croscarmellose sodium, hypromellose 2910, magnesium stearate, microcrystalline cellulose.

The film coating contains: ferrosoferric oxide, hypromellose 2910, iron oxide yellow, lactose monohydrate, triacetin and titanium dioxide.

The tablet may also contain trace amount of carnauba wax.

ISENTRESS chewable tablets:

Active ingredient: raltegravir

Inactive ingredients: ammonium hydroxide, crospovidone, ethylcellulose 20 cP, fructose, hydroxypropyl cellulose, hypromellose 2910/6cP, magnesium stearate, mannitol, medium chain triglycerides, monoammonium glycyrrhizinate, natural and artificial flavors (orange, banana, and masking that contains aspartame), oleic acid, PEG 400, saccharin sodium, sodium citrate dihydrate, sodium stearyl fumarate, sorbitol, sucralose and yellow iron oxide. The 100 mg chewable tablet also contains red iron oxide.

ISENTRESS for oral suspension:

Active ingredient: raltegravir

Inactive ingredients: ammonium hydroxide, banana with other natural flavors, carboxymethylcellulose sodium, crospovidone, ethylcellulose 20 cP, fructose, hydroxypropyl cellulose, hypromellose 2910/6cP, macrogol/PEG 400, magnesium stearate, maltodextrin, mannitol, medium chain triglycerides, microcrystalline cellulose, monoammonium glycyrrhizinate, oleic acid, sorbitol, sucralose and sucrose.

Distributed by: Merck Sharp & Dohme LLC

Rahway, NJ 07065, USA

For patent information: www.msd.com/research/patent

Copyright © 2007-2022 Merck & Co., Inc., Rahway, NJ, USA, and its affiliates. All rights reserved.

usppi-mk0518-mf-2205r030

For more information go to www.ISENTRESS.com or call 1-800-622-4477.

Bring this booklet to your child's appointments.

ISENTRESS (raltegravir)

for oral suspension

Instructions for Use

for babies and toddlers

Before You Start

• Be sure you understand these instructions before you start. Call your doctor if you have any questions.
• It is very important that you measure the water and ISENTRESS carefully using the correct syringe.
• Before you give ISENTRESS to your child, check the expiration date. The expiration date is printed on the box and the ISENTRESS packets.
• Do not open the ISENTRESS packets until you are ready to mix a dose.

• The amount of ISENTRESS depends on your child's age and weight, so it will change over time.

  Your doctor will tell you the right dose at each check-up after weighing your child.

  Be sure to keep your doctor's appointments so you get new dosing information as your child grows.

  During your child's first week of life, you will give ISENTRESS 1 time a day. After the first week of life, you will give it 2 times a day.

• This booklet tells you how to:

  • Mix ISENTRESS into a liquid form
  • Measure the right dose using a syringe
  • Give mixed ISENTRESS to your child
  • Clean up

Kit Contents

Prescription (on box)		2 mixing cups
Instructions for Use (this booklet) Prescribing Information 6 syringes		60 packets of ISENTRESS

2 blue (10mL) syringes	2 green (3mL) syringes	2 white (1mL) syringes

The kit has an extra cup and set of syringes in case one is lost or damaged.

Do not use any damaged cups or syringes.

Step 1. Get ready

• Put your child in a safe place. You will need both hands to prepare ISENTRESS.
• Wash your hands with soap and water.
• Take out what you need from the kit as shown below to make 1 dose and place on a clean surface:

1 mixing cup (Using the tab on the mixing cup, pull open the lid)	1 packet of ISENTRESS	a clean glass	3 syringes (Have one of each size ready, but you will only need 1 or 2, depending on the prescribed dose)

Step 2. Fill a clean glass with water

Fill a clean glass with room-temperature drinking water from your sink or use bottled water.

Step 3. Fill the blue syringe with water

Push the plunger of the blue syringe into the syringe as far as it goes.
Put the tip of the syringe into the glass of water. Pull back the plunger to draw up water into the syringe. Stop when you get to the 10mL mark.

Step 4. Check for air bubbles

Hold the syringe with tip up. Tap it with your finger to move any air bubbles up towards the tip. Slowly push up on the plunger to make the air come out. You may see some drops of water come out.
	Re-check the amount of water in the syringe. If it is less than 10mL, put the tip back into the water and pull back on the plunger until you get to the 10mL mark.

Step 5. Add the 10mL of water to the mixing cup

Add the 10 mL of water from the syringe to the mixing cup by pushing all the way down on the plunger.

Step 6. Add ISENTRESS to the mixing cup

	Take 1 packet of ISENTRESS and shake the powder to the bottom of the packet.
Tear or cut open the packet at the dotted line and add all of the powder to the water in the mixing cup. Make sure the packet is completely empty.

Step 7. Mix ISENTRESS and water

Snap the lid of the mixing cup shut. Gently swirl the mixing cup for 45 seconds in a circular motion to mix the powder and water. Use a clock or timer to time for 45 seconds. Do not shake the mixture.
	Check to make sure the powder is mixed. If it is not mixed, swirl it some more. The mixture should look cloudy.

Step 8. Check your prescription

Find the dose amount in 'mL' prescribed by your doctor. This is written on the prescription label on the box from your pharmacy.

Remember that the dose may change each time you go to the doctor, so make sure you check the prescribed dose each time. Be sure to go to all of your doctor's appointments so your child gets the right dose!

Step 9. Choose the syringe you need

Your doctor will prescribe the dose in milliliters (mL). Choose the right syringe for your child's dose:

WHITE (1mL) for 1mL or less

GREEN (3mL) for 1.5mL to 3mL

BLUE (10mL) for 3.5mL to 10mL

Then find the mL mark on the syringe that matches your child's dose.

Step 10. Measure ISENTRESS

Push the plunger into the barrel of the syringe as far as it goes.
Put the tip of the syringe into the cup of the mixed ISENTRESS and pull back on the plunger. Stop when you get to the line that matches your child's prescribed dose.

Step 11. Check for air bubbles

Hold the syringe with tip up. Tap it with your finger to move any air bubbles up towards the tip. Slowly push the plunger to make the air come out. You may see some drops of medicine come out.
	Re-check the amount of ISENTRESS in the syringe. If it is less than the prescribed dose, put the tip back into the cup of mixed ISENTRESS and pull back on the plunger until you get to the right dose mark.

Step 12. Give ISENTRESS to your child

Place the tip of the syringe inside your child's mouth so that it touches either the right or left cheek.

Slowly push in the plunger to give the dose of mixed ISENTRESS to your child. If your child fusses, take the tip of the syringe out of the mouth and try again. It is important that your child takes all of the prescribed dose (a little left in the syringe tip is OK).

Step 13. Clean up

Pour the leftover mixed ISENTRESS into the trash.

Do not pour it into the sink.

Pull the plungers out of any syringes you used.

Hand wash the syringes, plungers, and mixing cup with warm water and dish soap. Do not wash in the dishwasher.

Rinse with water and let air dry. Put everything in a clean, dry place.

How should I store ISENTRESS?

Store the ISENTRESS for oral suspension kit at room temperature between 68°F to 77°F (20°C to 25°C).

Store in the original container.

Keep ISENTRESS and all medicines out of the reach of children.

For more information, go to www.ISENTRESS.com or call 1-800-622-4477.