Isentress - Consumer Medicine Information
|Manufacture:||Merck and Co., Inc.|
|Condition:||HIV Infection, Occupational Exposure|
|Class:||Integrase strand transfer inhibitor|
|Ingredients:||raltegravir potassium, calcium phosphate dibasic anhydrous, hypromellose 2208, lactose monohydrate, magnesium stearate, microcrystalline cellulose, poloxamer 407 (contains 0.01% butylated hydroxytoluene as antioxidant), sodium stearyl fumarate; ammonium hydroxide, crospovidone, ethylcellulose 20 cP, fructose, hydroxypropyl cellulose, hypromellose 2910/6cP, macrogol/PEG 400, magnesium stearate, mannitol, medium chain triglycerides, monoammonium glycyrrhizinate, natural and artificial flavors (orange, banana, and masking), oleic acid, phenylalanine (as part of the artificial sweetener, aspartame), saccharin sodium, sodium citrate dihydrate, sodium stearyl fumarate, sorbitol, sucralose and yellow iron oxide;|
raltegravir chewable tablets
(as raltegravir potassium)
About this Medication
What is HIV
HIV is a disease that destroys the body’s ability to protect itself from infection.
- It is caused by a virus (called HIV) that attacks certain white blood cells and weakens the immune system.
- HIV is spread by contact with blood of or sexual contact with an infected person.
What the Medication is Used For
- ISENTRESS is a medicine that helps control HIV infection, in combination with other antiretroviral medications.
- Your physician has prescribed ISENTRESS to help control your HIV infection.
ISENTRESS has not been studied in children less than 2 years of age.
What it Does
ISENTRESS is a medicine that helps to control HIV infection. The term HIV stands for Human Immunodeficiency Virus. It is the virus that causes AIDS (Acquired Immune Deficiency Syndrome).
How does ISENTRESS Work
- ISENTRESS blocks an enzyme which the virus (HIV) needs in order to make more virus. The enzyme that ISENTRESS blocks is called HIV integrase.
- ISENTRESS is used in combination with other HIV medicines to treat adults, adolescents, and children 2 years of age and older who are infected with HIV. Anti-HIV medicines are also called “antiretroviral medicines” or an-ti-re-tro-vi-ral medicines.
When used with other anti-HIV medicines, ISENTRESS may do two things
- It may reduce the amount of HIV in your blood. This is called your “viral load”.
- Reducing the amount of HIV in the blood may keep your immune system healthy.
- This in turn, can help your immune system to fight infection.
- It may also increase the number of white blood cells that help fight the virus (HIV).
- Physicians call them CD4 (T) cells. ISENTRESS may not have these effects in all patients.
When it should not be Used
- Do not take ISENTRESS if you are hypersensitive to any of its ingredients (see What the non-medicinal ingredients are).
What the Medicinal Ingredient Is
What the non-medicinal ingredients are
400 mg raltegravir film-coated tablets
calcium phosphate dibasic anhydrous, hypromellose 2208, lactose monohydrate, magnesium stearate, microcrystalline cellulose, poloxamer 407 (contains 0.01% butylated hydroxytoluene as antioxidant), sodium stearyl fumarate.
In addition, the film coating contains the following inactive ingredients: black iron oxide, polyethylene glycol 3350, polyvinyl alcohol, red iron oxide, talc and titanium dioxide.
25 mg and 100 mg raltegravir chewable tablets
ammonium hydroxide, crospovidone, ethylcellulose 20 cP, fructose, hydroxypropyl cellulose, hypromellose 2910/6cP, macrogol/PEG 400, magnesium stearate, mannitol, medium chain triglycerides, monoammonium glycyrrhizinate, natural and artificial flavors (orange, banana, and masking), oleic acid, phenylalanine (as part of the artificial sweetener, aspartame), saccharin sodium, sodium citrate dihydrate, sodium stearyl fumarate, sorbitol, sucralose and yellow iron oxide.
ISENTRESS 100 mg also contain red iron oxide
What Dosage Forms it Comes In
ISENTRESS 400 film-coated tablets are available as pink, oval shaped, with 227 on one side.
ISENTRESS 100 mg orange-banana flavoured, chewable tablets are available as pale orange, oval shaped scored tablet, debossed with the Merck logo on one side of the score and 477 on the other, and scored on the other side of the tablet.
ISENTRESS 25 mg orange -banana flavoured, chewable tablets are available as pale yellow, round, flat faced, beveled edge tablet debossed with the Merck logo on one side and 473 on the other side of the tablet.
Use in Children
For children 12 years of age and older, ISENTRESS, 400 mg tablets are available.
For children 2 to less than 12 years of age, ISENTRESS chewable tablets are available.
Warnings and Precautions
Tell your physician about all the medicines you take (see INTERACTIONS WITH THIS MEDICATION)
BEFORE you use ISENTRESS talk to your physician or pharmacist if:
- You have any allergies.
- You take antacids. Certain antacids (those containing aluminum and/or magnesium) are not recommended with ISENTRESS.
- 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.
- You are pregnant or plan to become pregnant.
- ISENTRESS is not recommended for use during pregnancy.
- ISENTRESS has not been studied in pregnant women.
- If you take ISENTRESS while you are pregnant, talk to your physician about how you can be included in the Antiviral Pregnancy Registry.
- You are breast-feeding or plan to breast-feed.
- It is recommended that HIV-infected women should not breast-feed their infants. This is because their babies could be infected with HIV through their breast milk.
- Talk with your physician about the best way to feed your baby.
Does ISENTRESS lower the chance of passing HIV to other people
No. ISENTRESS does not reduce the chance of passing HIV to others through sexual contact, sharing needles, or being exposed to your blood.
- Continue to practice safer sex.
- Use latex or polyurethane condoms or other barrier methods to lower the chance of sexual contact with any body fluids. This includes semen from a man, vaginal secretions from a woman, or blood.
- Never re-use, or share needles.
- Ask your physician if you have any questions about safer sex or how to prevent passing HIV to other people.
What else is there to know
- ISENTRESS does not cure HIV infection or AIDS.
- It is very important that you stay under the care of your physician during treatment with ISENTRESS.
Interactions with this Medication
Tell your physician about all the medicines you take. Include the following:
- prescription medicines, including rifampin, which may interact with ISENTRESS
- non-prescription medicines including antacids. It is not recommended to take ISENTRESS with certain antacids containing aluminum and/or magnesium while others are acceptable (e.g. calcium carbonate, omeprazole, famotidine). If needed, talk to your physician about any other antacids you can take
- herbal supplements
Know the medicines you take.
- Keep a list of your medicines. Show the list to your physician and pharmacist when you get a new medicine.
Proper Use of this Medication
Take ISENTRESS exactly as your physician has prescribed.
Take ISENTRESS twice a day, by mouth, with or without food.
ISENTRESS must be used with other anti-HIV medicines.
Do not change your dose, or stop taking ISENTRESS without first talking with your doctor. Do not switch from the 400 mg tablet to the chewable tablets.
Adults and adolescents at least 12 years of age
Take one 400-mg tablet at a time.
Children 2 to less than 12 years of age
- Your child’s healthcare provider will tell you how many tablets your child should take based on your child’s weight.
- The 100 mg chewable tablet is scored and can be split into equal halves.
- Do not take more than 300 mg of the chewable tablet twice a day.
IMPORTANT: Take ISENTRESS exactly as your physician prescribed and at the right times of day because if you don’t:
- The amount of virus (HIV) in your blood may increase if the medicine is stopped for even a short period of time.
- The virus may develop resistance to ISENTRESS and become harder to treat.
- Your medicines may stop working to fight HIV.
- The activity of ISENTRESS may be reduced (due to resistance).
In case of drug overdose, contact a health care practitioner (e.g. doctor), hospital emergency department or the regional poison control centre, even if there are no symptoms.
If you miss a dose, take it as soon as you remember. If you do not remember until it is time for your next dose, skip the missed dose and go back to your regular schedule. Do NOT take two tablets of ISENTRESS at the same time. In other words, do NOT take a double dose.
ISENTRESS must be used with other anti-HIV medicines.
Be sure to keep a supply of your anti-HIV medicines.
- When your ISENTRESS supply starts to run low, get more from your physician or pharmacy.
- Do not wait until your medicine runs out to get more.
Side Effects and what to Do about Them
Like all medicines, ISENTRESS can cause side effects, although not everybody gets them. In studies, side effects usually were mild and did not cause patients to stop taking ISENTRESS. The side effects reported in patients taking ISENTRESS were similar to side effects in patients treated with a tablet containing no medication (a placebo).
The most common side effects of ISENTRESS include:
- difficulty sleeping
- upper respiratory tract infection
- inflammation of the nasal passages and throat
- back pain depression
Additionally, while the medicine has been on the market, some further reactions have occurred:
- Depression and suicidal thoughts have been reported. If you develop these feelings, discuss this with your physician.
- Other side effects that have been reported include low blood platelet count, clumsiness and lack of coordination, rash with or without an increase in some white blood cells, severe skin reaction, liver failure. If you develop any of these reactions, discuss with your physician.
In some patients with advanced HIV infection (AIDS), signs and symptoms of inflammation from opportunistic infections may occur when combination antiretroviral treatment is started. Tell your physician immediately if you notice any symptoms of infection.
Phenylketonuria (PKU). ISENTRESS Chewable Tablets contain phenylalanine as part of the artificial sweetener, aspartame. The artificial sweetener may be harmful to people with PKU.
Contact your physician promptly if you experience unexplained muscle pain, tenderness, or weakness while taking ISENTRESS.
Contact your physician promptly if you develop a rash. Severe and life-threatening skin reactions and allergic reactions have been reported in some patients taking ISENTRESS.
Changes in your immune system (Immune Reconstitution Inflammatory Syndrome) can happen when you start taking HIV medicines. Your immune system may get stronger and begin to fight infections that have been hidden in your body for a long time, or you could develop an autoimmune disease in which your immune system reacts against your own body (e.g. Grave’s disease (which affects the thyroid gland), Guillain-Barre syndrome (which affects the nervous system) or polymyositis (which affects the muscles) and it may develop at any time, sometimes months later after the start of HIV therapy). Sometimes symptoms can be severe, so if you develop high temperature (fever), joint or muscle pain, redness, rash, swelling, or fatigue or any new symptoms contact your physician right away.
Tell your physician if you develop any unusual side effect or if any known side effect does not go away or gets worse. For more information, ask your physician or pharmacist.
Serious Side Effects, how often they Happen and what to Do about Them
|Symptoms / effects||Talk with your|
|Uncommon||Severe skin reactions and allergic reactions: occasionally lifethreatening, with symptoms such as rash, itching or hives on the skin, swelling of the face, lips, tongue or other parts of the body, shortness of breath, wheezing or trouble breathing||✓|
|lack of white blood cells: frequent infections such as fever, severe chills, sore throat or mouth ulcers||✓|
|lack of red blood cells: tiredness, headaches, being short of breath when exercising, dizziness and looking pale||✓|
|severe chest pain||✓|
|stomach problems: pain, nausea, vomiting, heartburn||✓|
|liver disease: liver disease with nausea, vomiting, loss of appetite, feeling generally unwell, fever, itching, yellowing of the skin and eyes, and dark coloured urine||✓|
|kidney disease: nausea, loss of appetite and weakness, pass little or no urine, breathlessness||✓|
|depression, suicidal thoughts and actions||✓|
|disturbance in attention||✓|
This is not a complete list of side effects. For any unexpected effects while taking ISENTRESS, contact your physician or pharmacist.
How to Store It
Store ISENTRESS at room temperature (15°C–30°C).
400 mg tablets:
Keep the desiccant in the bottle.
Chewable tablets 25 mg and 100 mg: Store in the original package with the bottle tightly closed. Keep the desiccant in the bottle to protect from moisture.
Keep ISENTRESS and all medicines out of the reach and sight of children.
Reporting Suspected Side Effects
You can report any suspected adverse reactions associated with the use of health products to the Canada Vigilance Program by one of the following 3 ways:
- Report online at www.healthcanada.gc.ca/medeffect
- Call toll-free at 1-866-234-2345
- Complete a Canada Vigilance Reporting Form and:
- Fax toll-free to 1-866-678-6789, or
- Mail to: Canada Vigilance Program
Postal Locator 0701E
Ottawa, ON K1A 0K9
Postage paid labels, Canada Vigilance Reporting Form and the adverse reaction reporting guidelines are available on the MedEffect Canada Web site at www.healthcanada.gc.ca/medeffect
or at Merck Canada Inc. by one of the following 2 ways:
- Call toll-free at 1-800-567-2594
- Complete a Canada Vigilance Reporting Form and:
- Fax toll-free to1-877-428-8675, or
- Mail to: Merck Canada Inc.
Medical Information Centre
16750 route Transcanadienne
Kirkland, QC H9H 4M7
NOTE: Should you require information related to the management of side effects, contact your health professional. The Canada Vigilance Program or Merck do not provide medical advice.
This document plus the full product monograph, prepared for health professionals can be found at: www.merck.ca or by contacting the sponsor, Merck Canada Inc., at: 1-800-567-2594.