Xeplion® Range , Prolonged release 25 mg/50 mg/75 mg/100 mg/150

What XEPLION is

The actual medicine in XEPLION is paliperidone palmitate. XEPLION is an extended release suspension for intramuscular injection.

What XEPLION is used for

XEPLION belongs to the class of antipsychotic medicines and is used to treat schizophrenia in adults (18 years of age and older). XEPLION is used to keep the disorder under control, i.e. to prevent its recurrence.

Do not receive XEPLION:

• If you are allergic to paliperidone tablets or any other ingredient in XEPLION (See under WHAT XEPLION CONTAINS).
• If you are allergic to risperidone.
• If you have Parkinson’s disease or Dementia with Lewy Bodies.
• If you have a moderate to severe loss of kidney function.

Warnings and precautions

Take special care with XEPLION

Elderly Patients

XEPLION has not been studied in elderly patients with dementia. However, elderly patients with dementia may have an increased risk of stroke or death.

All Patients

If you have any of the following conditions, talk to your doctor as he/she may want to adjust your dose or monitor you for a while:

• if you have ever been diagnosed with a condition whose symptoms include high temperature and muscle stiffness (also known as Neuroleptic Malignant Syndrome).
• if you have ever experienced abnormal movements of the tongue or face (Tardive Dyskinesia).
• if you are at risk for diabetes or high blood sugar.
• If you have had breast cancer or a tumour in the pituitary gland in your brain.
• if you have heart disease or heart disease treatment that makes you prone to low blood pressure, or are prone to drop in blood pressure or feeling dizzy when you stand up from lying or sitting positions.
• if you have epilepsy.
• if you have or have had low white blood cell counts in your blood. Let your doctor know right away if you develop a fever or infection while being treated with XEPLION.
• if you have a loss of kidney function. Your doctor may reduce your dose of XEPLION if your kidney function is reduced.
• if you have a loss of liver function.
• if you have prolonged and/or painful erection.
• if you have had problems with body temperature regulation.
• if you have an abnormally high level of the hormone prolactin in your blood or if you have a possible prolactin-dependent tumour.

If you have never before taken XEPLION, paliperidone or risperidone, your doctor will need to make sure you can tolerate the medicine by giving you an oral dosage form daily for a few days before starting XEPLION.

How and when to take XEPLION

XEPLION is a long-acting medicine that a healthcare professional will give you by injection. This means that you do not have to take this medicine every day. When you receive your first dose of XEPLION, you will need to get a second dose one week later. After that you will only need to get a dose once a month.

Your doctor or healthcare provider will give you the injection into the muscle of your upper arm or buttocks. Your doctor will tell you how long your treatment with XEPLION will last. Do not stop treatment early. If you are under the impression that the effect of XEPLION is too strong or too weak, tell your doctor or pharmacist.

If you take more XEPLION than you should

Patients who have been given too much XEPLION may experience the following symptoms: Drowsiness or sleepiness, fast heart rate, low blood pressure, an abnormal electrocardiogram (electrical tracing of the heart) or slow or abnormal movements of the face, body, arms or legs. In the event of overdosage, consult your doctor or pharmacist. If neither is available, contact the nearest hospital or poison control centre.

If you forget to take XEPLION

It is very important to keep all your appointments and get your injections on time. If you think you are going to miss your appointment, call your doctor or treatment team as soon as you can. Your doctor or treatment team will decide what you should do next.

If you stop taking XEPLION

If you stop going for your injections, your symptoms may return. You should not stop receiving injections of this medicine unless you have discussed this with your doctor.

Patients with kidney or liver impairment:

If you have mild kidney problems your doctor may give you a lower dose. If you have moderate or severe kidney problems XEPLION should not be used. If you have severe liver problems XEPLION should be used with caution.

XEPLION can cause side effects. You may experience a severe allergic reaction characterised by fever, swollen mouth, face, lip or tongue, shortness of breath, itching, skin rash and sometimes drop in blood pressure (amounting to an ‘anaphylactic reaction’). If this should occur, seek medical attention immediately.

Even if you have previously tolerated oral risperidone or oral paliperidone, allergic reactions may occur after receiving injections of XEPLION. Seek medical attention right away if you experience a rash, swelling of your throat, itching, or problems breathing as these may be signs of a serious allergic reaction.

Tardive dyskinesia (twitching or jerking movements that you cannot control in your face, tongue, or other parts of your body). Tell your doctor immediately if you experience involuntary rhythmic movements of the tongue, mouth and face. Withdrawal of XEPLION may be needed.

In elderly patients with dementia, medicines in the same group as XEPLION have been associated with side effects including sudden weakness or numbness of the face, arms, or legs, instances of slurred speech, or blurred vision. If any of these should occur, even for a short period of time, seek medical attention immediately (see section 2, take special care with XEPLION).

The most frequently reported side-effects are: Difficulty falling or staying asleep, headache. Common cold symptoms, urinary tract infection, feeling like you have the flu.

XEPLION can raise your levels of a hormone called "prolactin" found on a blood test (which may or may not cause symptoms). When symptoms of high prolactin occur, they may include in men: Breast swelling, difficulty in getting or maintaining erections, or other sexual dysfunction. In women they may include breast discomfort, leakage of milk from the breasts, missed menstrual periods, or other problems with your cycle.

High blood sugar, weight gain, weight loss, high blood triglycerides (a fat). Irritability, depression, anxiety. Parkinsonism: This condition may include: slow or impaired movement, sensation of stiffness or tightness of the muscles (making your movements jerky), and sometimes even a sensation of movement "freezing up" and then restarting. Other signs of Parkinsonism include a slow shuffling walk, a tremor while at rest, increased saliva and/or drooling, and a loss of expression on the face.

Restlessness, feeling sleepy, or less alert. Dystonia: This is a condition involving slow or sustained involuntary contraction of muscles. While it can involve any part of the body (and may result in abnormal posture), dystonia often involves muscles of the face, including abnormal movements of the eyes, mouth, tongue or jaw. Dizziness. Dyskinesia: This is a condition involving involuntary muscle movements, and can include repetitive spastic or writhing movements, or twitching. Tremor (shaking). Slow heart rate, rapid heart rate. High blood pressure. Cough, stuffy nose. Abdominal pain or discomfort, vomiting, nausea, constipation, diarrhoea, indigestion, toothache. Increased liver transaminases in your blood. Rash. Bone or muscle ache, back pain. Fever, weakness, fatigue (tiredness). A reaction at the injection site, including itching, pain or swelling.

Less frequent side-effects include: Pneumonia, infection of the chest (bronchitis), infection of the breathing passages, sinus infection, bladder infection, ear infection, eye infection, tonsillitis, infection of the skin, skin inflammation caused by mites, abscess under the skin. White blood cell count decreased, anaemia, decrease in red blood cells, increase in eosinophils (a type of white blood cell) in your blood. Allergic reaction. Diabetes or worsening of diabetes, increased insulin (a hormone that controls blood sugar levels) in your blood. Increased appetite, loss of appetite resulting in malnutrition and low body weight, increased or decreased appetite. Increased cholesterol in your blood. Sleep disorder, elated mood (mania), confusion, decreased sexual drive, nightmares. Convulsion (fits), fainting, a restless urge to move parts of your body, dizziness upon standing, disturbance in attention, problems with speech, loss or abnormal sense of taste, reduced sensation of skin to pain and touch, a sensation of tingling, pricking, or numbness of skin. Blurry vision, eye infection or "pink eye", dry eye. Sensation of spinning (vertigo), ringing in the ears, ear pain. Atrial fibrillation (an abnormal heart rhythm), an interruption in conduction between the upper and lower parts of the heart, abnormal electrical conduction of the heart, prolongation of the QT interval from your heart, rapid heartbeat upon standing, abnormal electrical tracing of the heart. (electrocardiogram or ECG), a fluttering or pounding feeling in your chest (palpitations). Low blood pressure, low blood pressure upon standing (consequently, some people taking XEPLION may feel faint, dizzy, or may pass out when they stand up or sit up suddenly).

Shortness of breath, lung congestion, wheezing, sore throat, nosebleeds. Stomach or intestinal infection, dry mouth, excessive passing of gas or wind. Increased GGT (a liver enzyme called gamma-glutamyltransferase) in your blood. Increased liver enzymes in your blood. Hives (or "nettle rash"), itching, hair loss, eczema, dry skin, skin redness, acne. Muscle spasms, joint stiffness, neck pain, joint pain. Incontinence (lack of control) of urine, frequent passing of urine, pain when passing urine. Erectile dysfunction, ejaculation disorder, loss of menstrual periods, a delay in menstrual periods, missed menstrual periods or other problems with your cycle (females), development of breasts in men, leakage of milk from the breasts, sexual dysfunction, breast discomfort, vaginal discharge. Swelling of the face, mouth, eyes, or lips, swelling of the body, arms or legs. A change in the way you walk. Chest discomfort, feeling unwell. Hardening of the skin. Fall. Other: Allergic reactions even if you have previously tolerated oral paliperidone or risperidone. Not moving or responding while awake (catatonia); Sleep walking. Sleep related eating disorder. Lack of bowel muscle movement that causes blockage.

Eye problems during cataract surgery. During cataract surgery, a condition called intraoperative floppy iris syndrome (IFIS) can happen if you have taken XEPLION during the last three months. If you need to have cataract surgery, be sure to tell your eye doctor if you have taken XEPLION during the last three months.

Severe or life-threatening rash with blisters and peeling skin that may start in and around the mouth, nose, eyes, and genitals and spread to other areas of the body (Stevens-Johnson syndrome or toxic epidermal necrolysis). The following side-effects have been seen with the use of another medicine called risperidone that is very similar to XEPLION, so these can also be expected with XEPLION: other types of blood vessel problems in the brain, crackly lung sounds, dead skin cells at the injection site, and an ulcer at the injection site. Not all side effects reported for XEPLION are included in this leaflet. Should your general health worsen or if you experience any untoward effects while taking XEPLION, please consult your doctor, pharmacist or other health care professional for advice.

Reporting of side effects

If you get side effects, talk to your doctor, pharmacist or nurse. This includes any possible side effects not listed in this leaflet. You can also report side effects to SAHPRA via the “6.04 Adverse Drug Reaction Reporting Form”, found online under SAHPRA’s publications: https://www.sahpra.org.za/Publications/Index/8. By reporting side effects, you can help provide more information on the safety of XEPLION.

Store all medicines out of the reach of children. Store at or below 25 °C. Protect from light. Keep in outer carton until ready to use. XEPLION is for single use only. Any unused portion should be discarded. Do not use after the expiry date on the label. Return all unused medicine to your pharmacist. Do not dispose of unused medicine in drains or sewerage system (e.g. toilets).