Apretude: Uses, Side Effects and Dosage

Serious Warnings and Precautions

What APRETUDE is used for:

APRETUDE is used to reduce the risk of getting HIV-1 infection in people who are at least 12 years of age and weigh at least 35 kg. This is called pre-exposure prophylaxis (PrEP).

How APRETUDE works:

APRETUDE contains the active ingredient cabotegravir, which belongs to a group of anti-retroviral medicines called integrase inhibitors (INIs).

APRETUDE reduces the risk of getting HIV-1 when the medicine is in your bloodstream before you are exposed to HIV-1.

The ingredients in APRETUDE are:

Tablets

Medicinal ingredients: 30 mg cabotegravir (as cabotegravir sodium)

Non-medicinal ingredients: hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polyethylene glycol, sodium starch glycolate, and titanium dioxide

Cabotegravir Injections (3 mL)

Medicinal ingredients: 600 mg / 3 mL (200 mg / mL) cabotegravir

Non-medicinal ingredients: mannitol, polysorbate 20, polyethylene glycol (PEG) 3350, water for injection.

APRETUDE comes in the following dosage forms:

Tablets, 30 mg

Injectable suspension (extended-release), 600 mg / 3 mL (200 mg / mL)

Do not use APRETUDE if:

• You are allergic (hypersensitive) to cabotegravir or to any of the other ingredients of APRETUDE. See “What are the ingredients in APRETUDE?”.

• You are taking any of these medicines as they may affect the way APRETUDE works:

  • rifampicin or rifapentine (to treat some bacterial infections such as tuberculosis).
  • phenytoin, phenobarbital, carbamazepine or oxcarbazepine (also known as anticonvulsants used to treat epilepsy and prevent fits).
• You do not know your HIV-1 infection status or you already have HIV-1 infection. APRETUDE can only help reduce your risk of getting HIV before you are infected so, you must get tested to make sure you don’t already have HIV infection before taking APRETUDE.

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

• have had an allergic (hypersensitivity) reaction to cabotegravir. See the Serious Side effects and what to do about them table, below, for more information on these and other serious side effects.
• have had liver problems. Let your healthcare professional know if you have liver problems. Your liver function may need to be closely monitored.

Other warnings you should know about:

Depression or Mood Changes

Depression and mood changes, including having thoughts of hurting yourself (suicidal ideation) or trying to hurt yourself (suicide attempt), have been reported in people taking APRETUDE. You may be more likely to experience suicidal ideation and/or a suicide attempt if you have a history of depression or a mental health illness. See the Serious Side effects and what to do about them table, below, for more information on these and other serious side effects.

Pregnancy

Talk to your healthcare professional if you are pregnant or plan to become pregnant. Your healthcare professional will consider the benefit to you and the risk to your baby when taking APRETUDE while you are pregnant.

It is not known if APRETUDE will harm your unborn baby. There is a registry for women who take antiretroviral medicines during pregnancy. The purpose of this registry is to collect information about the health of you and your baby. Talk to your healthcare professional about how you can take part in this registry.

Breastfeeding

If you are thinking about breast-feeding, check with your healthcare professional who will consider the benefit and risk to you and your baby. It is not known whether the ingredients of APRETUDE can pass into breast milk and harm your baby.

Adolescents

Your doctor will discuss your mental health with you before and while receiving APRETUDE. Let your doctor know if you have mental health problems. You may need to be more closely monitored (also see section What are possible side effects from using APRETUDE?).

Just receiving APRETUDE may not stop you getting HIV.

You can still get HIV when taking this medicine, although APRETUDE lowers the risk. HIV infection is spread by sexual contact with someone who has the infection or by transfer of infected blood. To reduce your risk of getting HIV:

• Use a condom when you have oral or penetrative sex.
• Don’t risk blood transfer — for example, don’t share needles.

Discuss with your healthcare professional the additional precautions needed to further decrease the risk getting HIV.

While receiving APRETUDE to reduce the risk of getting HIV:

• If prescribed APRETUDE tablets as an Oral Lead-in, take APRETUDE tablets every day to reduce your risk, not just when you think you have been at risk of HIV infection. Do not miss any doses of APRETUDE tablets or stop taking it. Missing doses may increase your risk of getting HIV infection.
• It is important that you attend your planned appointments to receive your APRETUDE injection. Talk to your healthcare professional if you are thinking about stopping injections as this may increase your risk of getting HIV infection. If you do stop or are late receiving your APRETUDE injection, you will need to take other medicines or precautions to reduce your risk of getting HIV and possibly developing viral resistance.
• Get tested for HIV frequently as recommended by your healthcare professional.
• If you think you were infected with HIV (you may get a flu-like illness), tell your healthcare professional straight away. They may want to do more tests to make sure you are still HIV negative.

For more information on the APRETUDE Education Program (User Guide), log onto https://apretude.ca/en-ca/resources/.

APRETUDE injection is a long acting medication, so if you stop APRETUDE injections, cabotegravir may remain in your system for up to a year or more after your last injection. It is important that you attend your planned appointments to receive APRETUDE injection and talk to your healthcare professional if you are thinking about stopping PrEP. You may need to take other medicines to reduce the risk of getting HIV infection or use other safe sex precautions if you stop APRETUDE Injections.

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

Some medicines can affect how APRETUDE works or make it more likely that you will have side effects. APRETUDE can also affect how some other medicines work.

Do not take APRETUDE tablets and APRETUDE injection with the following:

• carbamazepine, oxcarbazepine, phenobarbital, or phenytoin (also known as anticonvulsants used to treat epilepsy and prevent seizures).
• rifampicin or rifapentine (to treat some bacterial infections such as tuberculosis).

Tell your healthcare professional if you are taking the following:

• rifabutin (to treat some bacterial infections such as tuberculosis). You may need to receive APRETUDE injections more often.

The following may interact with APRETUDE tablets:

• medicines called antacids to treat indigestion and heartburn or laxatives, or other products that contain aluminum and/or calcium carbonate, magnesium or buffered medicines.

  • Taking antacids can stop or reduce APRETUDE Tablets from being absorbed into your body and not make it work as well.
  • Antacids should be taken at least 2 hours before or 4 hours after you take APRETUDE tablets.

How to take APRETUDE tablets:

Tablets

Your healthcare professional may advise you to take APRETUDE tablets before you are given a APRETUDE injection for the first time.

If you are being given APRETUDE injection but you are not able to receive your injection, your healthcare professional may also recommend that you take APRETUDE tablets instead, until you can receive the injection again.

If you are prescribed APRETUDE tablets as an Oral lead-in:

• Take APRETUDE tablets every day exactly as your healthcare professional has told you to, for as long as your healthcare professional has told you to.
• When starting to take APRETUDE tablets for the first time, it should be taken for at least 28 days. See dosing schedule below.

• APRETUDE tablets should be swallowed whole with some liquid. APRETUDE tablets can be taken with or without food.

• Check with your healthcare professional if you are not sure or if you have questions.

Usual dose of APRETUDE tablets:

The usual dose of APRETUDE tablets is one tablet (30 mg cabotegravir) taken once a day.

How to take APRETUDE injection:

If you and your healthcare professional decide to start with APRETUDE injection, see Dosing schedule when starting with APRETUDE injection directly.

APRETUDE injection will be administered by your healthcare professional.

Usual dose of APRETUDE injection:

APRETUDE injection is given by your healthcare professional as one injection into the muscle of your buttocks.

Dosing schedule when taking APRETUDE tablets as an oral lead-in:

^aIt is important to take your oral lead-in tablets, for at least 28 days

^bYou should have your first injection on the same day as your last tablet or no later than 3 days after ^cFirst and second injections one month apart, third injection onwards, every two months

Dosing schedule when starting with APRETUDE injection directly:

^aFirst and second injections one month apart, third injection onwards, every two months

Overdose:

Missed Dose:

If you miss a tablet, take it soon as you remember. If your next dose is due within 12 hours, skip the dose you missed and take the next one at the usual time. Then continue your treatment as before. Don't take a double dose to make up for a missed dose.

Missed Injections:

It is important to not miss any of your planned appointments. If you are going to miss, or have missed, an injection of APRETUDE, talk to your healthcare professional as soon as possible. Your healthcare professional may recommend you take APRETUDE tablets until you are able to take APRETUDE injections again.

Possible side effects from using APRETUDE:

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

The most common side effects of APRETUDE injection are:

• Injection site reactions; such as pain and discomfort, a hardened mass or lump, swelling, redness, itching, bruising (which may include discolouration or a collection of blood under the skin), and warmth at the site of the injection. Tell your healthcare professional if the symptoms you experience at the injection site becomes severe or troublesome.

The most common side effects of APRETUDE tablets and APRETUDE injection are:

• Headache
• Diarrhea
• Feeling hot (pyrexia)

Additional side effects that may occur with APRETUDE tablets and APRETUDE injection include: abnormal dreams, difficulty in sleeping (insomnia), feeling anxious, dizziness, feeling sick (nausea), vomiting, stomach pain (abdominal pain), passing gas (flatulence), rash, muscle pain (myalgia), lack of energy (fatigue), generally feeling unwell (malaise), weight gain.

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:

Store APRETUDE tablets at up to 30°C.

Store APRETUDE injections at or below 30°C in the original carton until ready to use. Do not freeze.

Keep out of reach and sight of children.

If you want more information about APRETUDE:

• 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 Drug Product Database website (Drug Product Database: Access the database) the manufacturer’s website www.viivhealthcare.ca, or by calling 1-877-393-8448.

Date of Authorization: 2025-06-05

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