Telzir: Uses, Side Effects and Dosage

ABOUT THIS MEDICATION

What the medication is used for:

The name of your medicine is TELZIR. TELZIR can only be obtained with a prescription from your doctor. TELZIR is an antiretroviral medication. It is used together with other antiviral medicines to delay the progression of HIV infection in adults and pediatrics of 6 years of age and above.

TELZIR is to be taken in combination with ritonavir. It is therefore important that you carefully read the Consumer Information Leaflet that is provided with that medicine. If you have any further questions about ritonavir please ask your doctor or pharmacist.

What it does:

The Human Immunodeficiency Virus (HIV) is a retrovirus. Infection with HIV damages the immune system and can lead to Acquired Immune Deficiency Syndrome (AIDS) and other related illnesses.

TELZIR is an antiretroviral medication. It belongs to a group of medicines called protease inhibitors. TELZIR in combination with other antiretroviral agents reduces the amount of HIV in your blood. Response to treatment with TELZIR varies among patients. Your doctor will be monitoring the effectiveness of your treatment. TELZIR does not cure AIDS or kill the virus, but may help to prevent further damage to the immune system by slowing the production of new viruses.

When it should not be used:

Do not use TELZIR if:

• You are allergic to ritonavir, fosamprenavir calcium, amprenavir or any of the other ingredients found in TELZIR or ritonavir (See What the important nonmedicinal ingredients are).

  • You are taking any of the following medications with TELZIR because serious or life-threatening problems could occur. Medicines for:

    • heart rhythm (e.g. flecainide, propafenone, amiodarone, lidocaine (systemic))
    • prostate (e.g. alfuzosin)
    • antihistamine
    • infection (rifampin, as this drug reduces the effectiveness of TELZIR)
    • headache (e.g. dihydroergotamine, ergonovine, ergotamine)
    • indigestion
    • mood (St. John’s Wort - Hypericum perforatum)
    • cholesterol (e.g. lovastatin, simvastatin)
    • schizophrenia (e.g. pimozide, quetiapine, lurasidone)
    • bipolar disorder and major depressive disorder (e.g. quetiapine, lurasidone)
    • pulmonary arterial hypertension (sildenafil)
    • anxiety (e.g. midazolam, triazolam, diazepam, flurazepam)
    • HIV infection (delavirdine)

What the medicinal ingredient is:

TELZIR tablets are available for oral administration in a strength of 700 mg of fosamprenavir as fosamprenavir calcium (equivalent to approximately 600 mg of amprenavir).

TELZIR oral suspension contains 50 mg/mL fosamprenavir as calcium salt (equivalent to approximately 43 mg/mL amprenavir).

What the important nonmedicinal ingredients are:

Each 700 mg tablet contains the inactive ingredients colloidal silicon dioxide, croscarmellose sodium, magnesium stearate, microcrystalline cellulose, and povidone K30. The tablet film-coating contains the inactive ingredients hypromellose, iron oxide red, titanium dioxide, and triacetin.

The oral suspension contains hypromellose, sucralose, propylene glycol, methyl parahydroxybenzoate, propyl parahydroxybenzoate, polysorbate 80, calcium chloride dihydrate, artificial grape bubblegum flavour, natural peppermint flavour and purified water.

What dosage forms it comes in:

TELZIR tablets, 700 mg, are available in bottles of 60 tablets.

TELZIR suspension is available in a bottle of 225 mL of 50 mg/mL fosamprenavir calcium oral suspension.

WARNINGS AND PRECAUTIONS

Tell your doctor, before using TELZIR if:

• You are pregnant, planning to become pregnant, or become pregnant while taking TELZIR. It is not known if TELZIR can harm your unborn child. You and your doctor will need to decide if taking TELZIR is right for you. If you take TELZIR while you are pregnant, talk to your doctor about how you can be included in the Antiretroviral Pregnancy Registry.

• You are breastfeeding. It is recommended that HIV infected women do not breastfeed their infants under any circumstances in order to avoid transmission of HIV from mother to child. The active substance in TELZIR may be found in human breast milk and there is no safety data available following treatment with TELZIR in babies. You are recommended not to breastfeed your baby while taking TELZIR.
• You have any medical conditions, including liver disease, hepatitis, as the amount of medicine you are taking may change.
• You have hemophilia. There have been reports of increased bleeding in patients with hemophilia taking protease inhibitors.
• You are taking oral contraceptives, as TELZIR may be harmful to your liver and may decrease the therapeutic effect of the oral contraceptive. Therefore, alternative non-hormonal methods of contraception (e.g. a condom) are recommended to prevent pregnancy while you are taking TELZIR.
• You are using estrogens and /or progestogens as hormone replacement therapy. No data is available on the use of TELZIR with estrogens and/or progestogens as hormone replacement therapy (HRT) for post menopausal women.
• You are allergic to sulfonamide drugs.
• You are taking or planning to take any other drug(s), including those available without a prescription, and herbal medicines such as St. John’s Wort (Hypericum perforatum). Taking this herb may reduce the effectiveness of TELZIR.

Special warnings:

TELZIR oral solution contains propyl and methyl parahydroxybenzoate. These products may cause an allergic reaction in some individuals. This reaction may be delayed.

TELZIR helps to control the amount of HIV found in your blood but is not a cure for HIV infection. You will need to take TELZIR every day. Do not stop taking TELZIR without first talking to your doctor.

HIV is usually spread by sexual contact, blood transfer or by contaminated needles. The risk of spreading HIV still exists during TELZIR therapy; thus, the practice of ‘safe sex’ and avoidance of sharing needles is necessary.

You may continue to develop other infections and other illnesses associated with HIV disease. You should therefore keep in regular contact with your doctor while taking TELZIR.

Mothers with HIV should not breastfeed their infants because HIV in the breastmilk can infect the infant.

Driving and operating machinery

There is no information currently available that suggests taking TELZIR affects the ability to drive or operate machinery.

INTERACTIONS WITH THIS MEDICATION

Some drugs may change the usefulness and safety of TELZIR. It is important that you tell your doctor about all the medicines you are taking or planning to take, including all those that you have bought yourself. This is very important, as using more than one medicine at the same time can strengthen or weaken the effect of the medicine, causing in some cases serious medical conditions. TELZIR may interact with other medicines you are being treated with. Some of the medicines that can interact with amprenavir include:

• bosentan
• colchicines
• phenobarbital
• phenytoin
• salmeterol
• tricyclic antidepressants (e.g. amitriptyline, imipramine)
• warfarin
• PDE5 inhibitors (e.g. vardenafil, tadalafil)
• cholesterol-lowering drugs (atorvastatin)
• anticonvulsants (e.g. carbamazepine)
• anti-inflammatory drugs (e.g. dexamethasone)
• fluticasone
• paroxetine
• trazodone
• methadone
• itraconazole, ketoconazole
• immunosuppresants (e.g. cyclosporine, rapamycin and tacrolimus)
• maraviroc, dolutegravir (used to treat HIV infection)
• anti-hepatitis C drugs
• clarithromycin
• calcium channel blockers (e.g. amlodipine, diltiazem, felodipine, nifedipine, nimodipine, verapamil)
• cancer drugs (e.g. dasatinib, nilotinib, ibrutinib, vinblastine and everolimus)

See ABOUT THIS MEDICATION for a list of drugs that should not be taken with TELZIR.

PROPER USE OF THIS MEDICATION

Both regimens must be administered in combination with other antiretroviral agents.

Once-daily administration of TELZIR/ritonavir combination is not recommended in protease inhibitor-experienced patients.

The twice-daily plus ritonavir dose is supported by pharmacokinetic and safety data.

Take TELZIR tablets as your doctor has advised you. Take TELZIR oral suspension as your doctor has advised you.

Adults (aged 18 years and older):

Low doses of ritonavir may be used to enhance the pharmacokinetic profile of amprenavir. The recommended oral dose of fosamprenavir, in combination with ritonavir is outlined below:

Tablets:

Therapy Naïve Patients:

Once Daily: 1400 mg TELZIR and 200 mg ritonavir

Twice Daily: 700 mg TELZIR and 100 mg ritonavir

Protease Inhibitor-Experienced Patients:

Twice Daily: 700 mg TELZIR and 100 mg ritonavir

TELZIR tablets can be taken with or without food.

Oral Suspension:

Therapy Naïve Patients:

Once Daily: 1400 mg TELZIR and 200 mg ritonavir

Twice Daily: 700 mg TELZIR and 100 mg ritonavir

Protease Inhibitor-Experienced Patients:

Twice Daily: 700 mg TELZIR and 100 mg ritonavir

TELZIR oral suspension should be taken by adults without food and on an empty stomach. Shake the bottle vigorously before use.

Pediatric Patients (aged 6 years and older):

Pediatric patients should take this oral suspension with food to aid in taste and better encourage compliance with dosing. If vomiting occurs within 30 minutes of dose, the oral suspension dose should be taken again.

Oral Suspension:

Therapy Naïve and Protease Inhibitor Experienced:

Twice daily: 18 mg/kg plus ritonavir 3 mg/kg administered twice daily not to exceed the adult dose of 700 mg plus ritonavir 100 mg.

Tablets:

Therapy Naïve and Protease Inhibitor Experienced:

Twice daily: not to exceed 700 mg plus ritonavir 100 mg

The adult tablet regimens of TELZIR/ ritonavir may be used in patients who weigh at least 39 kg (ritonavir tablets may be used in patients who weigh at least 33 kg) and can swallow the tablets whole.

The use of TELZIR has not been studied in pediatric patients below the age of 2.

If you have a liver problem, your dose may be altered. Please follow the instructions of your doctor.

Overdose:

Missed Dose:

If you forget to take TELZIR, take it as soon as you remember. Then continue as before. Do not double dose.

SIDE EFFECTS AND WHAT TO DO ABOUT THEM

The following undesirable effects are thought to be related to treatment with TELZIR: feeling sick, diarrhea, tiredness, headache, abdominal pain, passing gas, rash, kidney stones, higher amounts of a type of fat in the blood and vomiting, and tingling or numbness around lips and mouth.

An increase in body fat has been seen in some patients taking antiretroviral therapy including a protease inhibitor. The cause and long-term health effects of these conditions are not known at this time.

Your doctor will test your blood regularly for increases in blood lipids (blood fat). These have been reported in patients taking TELZIR, which may lead to an increased risk of a heart attack. Heart attacks have occurred in some patients taking TELZIR. Increases in liver enzymes have also been reported. Your blood will also be checked for increases in blood sugar levels, as occasionally protease inhibitors have been shown to cause this.

Changes to your/your child’s immune system (Immune Reconstitution Inflammatory Syndrome) can happen when you/your child start taking HIV-1 medicines. Your/your child’s immune system may get stronger and begin to fight infections that have been hidden in your/your child’s body for a long time.

Autoimmune disorders (when the immune system attacks healthy body tissue), may also occur after you start taking medicines for HIV infection. Examples of this include: Grave's disease (which affects the thyroid gland), Guillain-Barré syndrome (which affects the nervous system), polymyositis (which affects the muscles), or autoimmune hepatitis (which affects the liver). Autoimmune disorders may occur many months after the start of treatment. Look for any other symptoms such as:

• high temperature (fever), redness, rash or swelling
• fatigue
• joint or muscle pain
• numbness or weakness beginning in the hands and feet and moving up towards the trunk of the body
• palpitations (chest pain) or rapid heart rate
• yellowing of the eyes or skin

If you notice these or any symptoms of inflammation or infection, tell your doctor immediately.

Always tell your doctor or pharmacist about any undesirable effects, even those not mentioned in this leaflet. If you feel ill in any other way that you do not understand, tell your doctor or pharmacist.

If you have a severe skin rash, check with your doctor as he may advise you to stop taking TELZIR.

This is not a complete list of side effects. For any unexpected effects while taking TELZIR, contact your doctor or pharmacist.

HOW TO STORE IT

Store TELZIR tablets between 15°C and 30°C.

Store TELZIR suspension between 2°C and 30°C. Do not freeze. Discard the suspension 28 days after first opening.

Do not take TELZIR after the expiry date on the container.

As with all medications, keep TELZIR out of the reach and sight of children.

REPORTING SIDE EFFECTS

MORE INFORMATION

Remember: TELZIR is for you. Never give it to someone else. It may harm them even if their symptoms are the same as yours.

This leaflet does not tell you everything about TELZIR. If you have any questions or are not sure about anything, then ask your doctor or pharmacist. You may need to read this leaflet again. Please do not throw this leaflet away until you are no longer taking TELZIR.

This document plus the full product monograph, prepared for health professionals can be found at:

www.viivhealthcare.ca

or by contacting the sponsor, ViiV Healthcare ULC at:

245, boulevard Armand-Frappier

Laval, Quebec

H7V 4A7

1-877-393-8448

Last revised: July 5, 2019

© 2019 ViiV Healthcare group of companies or its licensor.

Trademarks are owned by or licensed to the ViiV Healthcare group of companies.