Patient leaflets and SmPCs, drug interaction checker, official and paediatric dosages, pregnancy and breastfeeding guidance, and NHS pharmacy opening hours — all in one place.
Patient leaflets and SmPCs, drug interaction checker, official and paediatric dosages, pregnancy and breastfeeding guidance, and NHS pharmacy opening hours — all in one place.
The name of this medicine is Paliperidone Zentiva 50 mg or 75 mg or 100 mg or 150 mg prolonged release suspension for injection in pre-filled syringe (called Paliperidone Zentiva throughout this leaflet).
Paliperidone Zentiva contains the active substance paliperidone which belongs to the class of antipsychotic medicines and is used as a maintenance treatment for the symptoms of schizophrenia in adult patients stabilised on paliperidone or risperidone.
If you have shown responsiveness to paliperidone or risperidone in the past and have mild to moderate symptoms your doctor may start treatment with Paliperidone Zentiva without prior stabilisation with paliperidone or risperidone.
Schizophrenia is a disease with “positive” and “negative” symptoms. Positive means an excess of symptoms that are not normally present. For example, a person with schizophrenia may hear voices or see things that are not there (called hallucinations), believe things that are not true (called delusions), or feel unusually suspicious of others.
Negative means a lack of behaviours or feelings that are normally present. For example, a person with schizophrenia may appear withdrawn and may not respond at all emotionally or may have trouble speaking in a clear and logical way. People with this disease may also feel depressed, anxious, guilty, or tense.
Paliperidone Zentiva can help alleviate the symptoms of your disease and stop your symptoms from coming back.
Do not use Paliperidone Zentiva • if you are allergic to paliperidone or to any of the other ingredients of this medicine (listed in section 6).
• if you are allergic to another antipsychotic medicine including the substance risperidone.
Warnings and precautions Talk to your doctor, pharmacist or nurse before using Paliperidone Zentiva.
This medicine has not been studied in elderly patients with dementia. However, elderly patients with dementia, who are treated with other similar types of medicine, may have an increased risk of stroke or death (see section 4, possible side effects).
All medicines have side effects and some of the side effects of this medicine can worsen the symptoms of other medical conditions. For that reason, it is important to discuss with your doctor any of the following conditions which can potentially worsen during treatment with this medicine:
• if you have Parkinson’s disease
• 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 know that you have had low levels of white blood cells in the past (which may or may not have been caused by other medicines)
• if you are diabetic or prone to diabetes
• if you have had breast cancer or a tumour in the pituitary gland in your brain
• if you have a heart disease or heart disease treatment that makes you prone to low blood pressure
• if you have low blood pressure when you stand up or sit up suddenly
• if you have epilepsy
• if you have kidney problems
• if you have liver problems
• if you have prolonged and/or painful erection
• if you have problems with controlling core body temperature or overheating
• 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 or someone else in your family has a history of blood clots, as antipsychotics have been associated with formation of blood clots.
If you have any of these conditions, please talk to your doctor as they may want to adjust your dose or monitor you for a while.
As dangerously low numbers of a certain type of white blood cell needed to fight infection in your blood has been seen very rarely with patients taking this medicine, your doctor may check your white blood cell counts.
Even if you have previously tolerated oral paliperidone or risperidone, rarely allergic reactions occur after receiving injections of Paliperidone Zentiva. 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.
This medicine may cause you to gain weight. Significant weight gain may adversely affect your health. Your doctor should regularly measure your body weight.
As diabetes mellitus or worsening of pre-existing diabetes mellitus have been seen with patients taking this medicine, your doctor should check for signs of high blood sugar. In patients with pre-existing diabetes mellitus blood glucose should be monitored regularly.
Since this medicine may reduce your urge to vomit, there is a chance that it may mask the body’s normal response to ingestion of toxic substances or other medical conditions.
During an operation on the eye for cloudiness of the lens (cataract), the pupil (the black circle in the middle of your eye) may not increase in size as needed. Also, the iris (the coloured part of the eye) may become floppy during surgery and that may lead to eye damage. If you are planning to have an operation on your eye, make sure you tell your eye doctor that you are taking this medicine.
Children and adolescents This medicine is not for people who are under 18 years old.
Other medicines and Paliperidone Zentiva Tell your doctor if you are taking, have recently taken or might take any other medicines.
Taking this medicine with carbamazepine (an anti-epileptic and mood stabiliser) may require a change to your dose of this medicine.
Since this medicine works primarily in the brain, interference from other medicines that work in the brain can cause an exaggeration of side effects such as sleepiness or other effects on the brain such as other psychiatric medications, opioids, antihistamines and sleep medication.
Since this medicine can lower blood pressure, care should be taken when this medicine is used with other medicines that lower blood pressure.
This medicine can reduce the effect of medicines against Parkinson’s disease and restless legs syndrome (e.g., levodopa).
This medicine may cause an electrocardiogram (ECG) abnormality demonstrating a long time for an electrical impulse to travel through a certain part of the heart (known as “QT prolongation”). Other medicines that have this effect include some medicines used to treat the rhythm of the heart or to treat infection, and other antipsychotics.
If you are prone to develop convulsions, this medicine may increase your chance of experiencing them. Other medicines that have this effect include some medicines used to treat depression or to treat infection, and other antipsychotics.
Paliperidone Zentiva should be used with caution with medicines that increase the activity of the central nervous system (psychostimulants such as methylphenidate).
Paliperidone Zentiva with alcohol Alcohol should be avoided.
Pregnancy and breast-feeding If you are pregnant or breast-feeding, think you may be pregnant or are planning to have a baby, ask your doctor or pharmacist for advice before taking this medicine. You should not use this medicine during pregnancy unless this has been discussed with your doctor. The following symptoms may occur in newborn babies of mothers that have used paliperidone in the last trimester (last three months of their pregnancy): shaking, muscle stiffness and/or weakness, sleepiness, agitation, breathing problems, and difficulty in feeding. If your baby develops any of these symptoms you may need to contact your doctor.
This medicine can pass from mother to baby through breast milk and may harm the baby. Therefore, you should not breastfeed when using this medicine.
Driving and using machines Dizziness, extreme tiredness and vision problems may occur during treatment with this medicine (see section 4). This should be considered in cases where full alertness is required, e.g., when driving a car or handling machines.
Paliperidone Zentiva contains sodium and polysorbate This medicine contains less than 1 mmol sodium (23 mg) per dose, that is to say essentially ‘sodium-free’.
This medicine contains 12 mg of polysorbate in each ml which is equivalent to 12 mg/ml. Polysorbates may cause allergic reactions. Tell your doctor if you have any known allergies.
This medicine is administered by your doctor or other healthcare professional. Your doctor will tell you when you need your next injection. It is important not to miss your scheduled dose. If you cannot keep your appointment with the doctor, make sure you call them right away so another appointment can be made as soon as possible.
You will receive the first injection (150 mg) and second injection (100 mg) of this medicine in the upper arm approximately one week apart. Thereafter, you will receive an injection (ranging from 50 mg to 150 mg) in either the upper arm or buttocks once a month.
If your doctor is switching you from risperidone long acting injection to this medicine, you will receive the first injection of this medicine (ranging from 50 mg to 150 mg) in either the upper arm or buttocks on the date that your next injection was scheduled. Thereafter, you will receive an injection (ranging from 50 mg to 150 mg) in either the upper arm or buttocks once a month.
Depending on your symptoms, your doctor may increase or decrease the amount of medicine you receive by one dose level at the time of your scheduled monthly injection.
Patients with kidney problems
Your doctor may adjust your dose of this medicine based on your kidney function. If you have mild kidney problems your doctor may give you a lower dose. If you have moderate or severe kidney problems this medicine should not be used.
Elderly
Your doctor may reduce your dose of this medicine if your kidney function is reduced.
If you are given more Paliperidone Zentiva than needed This medicine will be given to you under medical supervision; it is, therefore, unlikely that you will be given too much.
Patients who have been given too much paliperidone may experience the following symptoms: drowsiness or sedation, 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.
If you stop using Paliperidone Zentiva If you stop receiving your injections, you will lose the effects of the medicine. You should not stop using this medicine unless told to do so by your doctor as your symptoms may return.
If you have any further questions on the use of this medicine, ask your doctor or pharmacist.
Like all medicines, this medicine can cause side effects, although not everybody gets them.
Tell your doctor immediately if you: • experience blood clots in the veins, especially in the legs (symptoms include swelling, pain, and redness in the leg), which may travel through blood vessels to the lungs causing chest pain and difficulty breathing. If you notice any of these symptoms seek medical advice immediately.
• have dementia and experience a sudden change in your mental state or sudden weakness or numbness of your face, arms or legs, especially on one side, or slurred speech, even for a short period of time. These may be signs of a stroke.
• experience fever, muscle stiffness, sweating or a lowered level of consciousness (a disorder called “Neuroleptic Malignant Syndrome”). Immediate medical treatment may be needed.
• are a man and experience prolonged or painful erection. This is called priapism. Immediate medical treatment may be needed.
• experience involuntary rhythmic movements of the tongue, mouth and face. Withdrawal of paliperidone may be needed.
• 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’). Even if you have previously tolerated oral risperidone or oral paliperidone, rarely allergic reactions occur after receiving injections of paliperidone.
• are planning to have an operation on your eye, make sure you tell your eye doctor that you are taking this medicine. During an operation on the eye for cloudiness of the lens (cataract), the iris (the coloured part of the eye) may become floppy during surgery (known as “floppy iris syndrome”) that may lead to eye damage.
• are aware of having dangerously low numbers of a certain type of white blood cell needed to fight infection in your blood.
The following side effects may happen:
Very common side effects: may affect more than 1 in 10 people
• difficulty falling or staying asleep.
Common side effects: may affect up to 1 in 10 people
• common cold symptoms, urinary tract infection, feeling like you have the flu
• Paliperidone Zentiva 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) breast discomfort, leakage of milk from the breasts, missed menstrual periods, or other problems with your cycle.
• high blood sugar, weight gain, weight loss, decreased appetite
• 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)
• headache
• rapid heart rate
• high blood pressure
• cough, stuffy nose
• abdominal pain, vomiting, nausea, constipation, diarrhoea, indigestion, toothache
• increased liver transaminases in your blood
• bone or muscle ache, back pain, joint pain
• loss of menstrual periods
• fever, weakness, fatigue (tiredness)
• a reaction at the injection site, including itching, pain or swelling.
Uncommon side effects: may affect up to 1 in 100 people
• pneumonia, infection of the chest (bronchitis), infection of the breathing passages, sinus infection, bladder infection, ear infection, fungal infection of the nails, tonsillitis, infection of the skin
• white blood cell count decreased, decrease in the type of white blood cells that help to protect you against infection, anaemia
• 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
• high blood triglycerides (a fat), increased cholesterol in your blood
• sleep disorder, elated mood (mania), decreased sexual drive, nervousness, nightmares
• 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 this medicine may be needed.
• 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
• 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, slow heart rate, 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 this medicine may feel faint, dizzy, or may pass out when they stand up or sit up suddenly)
• shortness of breath, sore throat, nosebleeds
• abdominal discomfort, stomach or intestinal infection, difficulty swallowing, 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, rash, hair loss, eczema, dry skin, skin redness, acne, abscess under the skin
• an increase of CPK (creatine phosphokinase) in your blood, an enzyme which is sometimes released with muscle breakdown
• muscle spasms, joint stiffness, muscle weakness
• incontinence (lack of control) of urine, frequent passing of urine, pain when passing urine
• erectile dysfunction, ejaculation disorder, missed menstrual periods or other problems with your cycle (females), development of breasts in men, sexual dysfunction, breast pain, leakage of milk from the breasts
• swelling of the face, mouth, eyes, or lips, swelling of the body, arms or legs
• an increase in body temperature
• a change in the way you walk
• chest pain, chest discomfort, feeling unwell
• hardening of the skin
• fall.
Rare side effects: may affect up to 1 in 1,000 people
• eye infection
• skin inflammation caused by mites, flaky itchy scalp or skin
• increase in eosinophils (a type of white blood cell) in your blood
• decrease in platelets (blood cells that help you stop bleeding)
• shaking of the head
• inappropriate secretion of a hormone that controls urine volume
• sugar in the urine
• life threatening complications of uncontrolled diabetes
• low blood sugar
• excessive drinking of water
• not moving or responding while awake (catatonia)
• confusion
• sleep walking
• lack of emotion
• inability to reach orgasm
• neuroleptic malignant syndrome (confusion, reduced or loss of consciousness, high fever, and severe muscle stiffness), blood vessel problems in the brain, including sudden loss of blood supply to brain (stroke or “mini” stroke), unresponsive to stimuli, loss of consciousness, low level of consciousness, convulsion (fits), balance disorder
• abnormal coordination
• glaucoma (increased pressure within the eyeball)
• problems with movement of your eyes, eye rolling, oversensitivity of the eyes to light, increased tears, redness of the eyes
• atrial fibrillation (an abnormal heart rhythm), irregular heartbeat
• blood clot in the lungs causing chest pain and difficulty in breathing. If you notice any of these symptoms seek medical advice immediately
• blood clots in the veins especially in the legs (symptoms include swelling, pain and redness in the leg). If you notice any of these symptoms seek medical advice immediately
• flushing
• trouble breathing during sleep (sleep apnoea)
• lung congestion, congestion of breathing passages
• crackly lung sounds, wheezing
• inflammation of the pancreas, swollen tongue, stool incontinence, very hard stool
• a blockage in the bowels
• chapped lips
• rash on skin related to drug, thickening of skin, dandruff
• breakdown of muscle fibers and pain in muscles (rhabdomyolysis)
• joint swelling
• inability to pass urine
• breast discomfort, enlargement of the glands in your breasts, breast enlargement
• vaginal discharge
• priapism (a prolonged penile erection that may require surgical treatment)
• very low body temperature, chills, feeling thirsty
• symptoms of drug withdrawal
• accumulation of pus caused by infection at injection site, deep skin infection, a cyst at injection site, bruising at injection site.
Not known: frequency cannot be estimated from the available data
• dangerously low numbers of a certain type of white blood cell needed to fight infection in your blood
• severe allergic reaction characterised by fever, swollen mouth, face, lip or tongue, shortness of breath, itching, skin rash and sometimes drop in blood pressure
• dangerously excessive intake of water
• sleep-related eating disorder
• coma due to uncontrolled diabetes
• decreased oxygen in parts of your body (because of decreased blood flow)
• fast, shallow breathing, pneumonia caused by inhaling food, voice disorder
• lack of bowel muscle movement that causes blockage
• yellowing of the skin and the eyes (jaundice)
• 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)
• serious allergic reaction with swelling that may involve the throat and lead to difficulty breathing
• skin discolouration
• abnormal posture
• newborn babies born to mothers who have taken Paliperidone Zentiva during pregnancy may experience side effects of the drug and/or withdrawal symptoms, such as irritability, slow, or sustained muscle contractions, shaking, sleepiness, breathing, or feeding problems
• a decrease in body temperature
• dead skin cells at the injection site and an ulcer at the injection site.
Reporting of side effects If you get any 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 directly via the Yellow card Scheme at: www.mhra.gov.uk/yellowcard or search for MHRA Yellow Card in the Google Play or Apple App Store. By reporting side effects, you can help provide more information on the safety of this medicine.
Keep this medicine out of the sight and reach of children.
Do not use this medicine after the expiry date which is stated on the carton. The expiry date refers to the last day of that month.
Do not store above 30°C. Do not freeze.
Do not throw away any medicines via wastewater or household waste.
Ask your pharmacist how to throw away medicines you no longer use. These measures will help to protect the environment.
What Paliperidone Zentiva contains The active substance is paliperidone.
Each Paliperidone Zentiva 50 mg pre-filled syringe contains 78 mg paliperidone palmitate.
Each Paliperidone Zentiva 75 mg pre-filled syringe contains 117 mg paliperidone palmitate.
Each Paliperidone Zentiva 100 mg pre-filled syringe contains 156 mg paliperidone palmitate.
Each Paliperidone Zentiva 150 mg pre-filled syringe contains 234 mg paliperidone palmitate.
The other ingredients are:
Polysorbate 20
Macrogol 4000
Citric acid monohydrate
Disodium hydrogen phosphate anhydrous
Sodium dihydrogen phosphate monohydrate
Sodium hydroxide (for pH adjustment)
Water for injections
What Paliperidone Zentiva looks like and contents of the pack Paliperidone Zentiva is a white to off-white prolonged release suspension for injection in a pre-filled syringe.
Each pack contains 1 pre-filled syringe and 2 needles.
Not all pack sizes may be marketed.
Marketing Authorisation Holder Zentiva Pharma UK Limited
12 New Fetter Lane
London
EC4A 1JP
United Kingdom
Manufacturer Universal Farma, S.L
Polígono Industrial Miralcampo
C/ El Tejido 2
19200 Azuqueca de Henares – Guadalajara
Spain
OR
Pharmascience International Limited
1st Floor Iacovides Tower
81-83 Griva Digeni Avenue
1090 Nicosia
Cyprus
This leaflet was last revised in January 2026.
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Paliperidone Zentiva 75 mg prolonged-release suspension for injection in pre-filled syringe comes as suspension containing 75 mg. Always follow the dose your doctor or pharmacist has given you, and read the leaflet that comes with the medicine.
The active substance in Paliperidone Zentiva 75 mg prolonged-release suspension for injection in pre-filled syringe is paliperidone palmitate.
Medicines with the same active substance include: Byannli 1000mg prolonged-release suspension for injection in pre-filled syringe, Byannli 700mg prolonged-release suspension for injection in pre-filled syringe, Paliperidone 100 mg prolonged release suspension for injection, Paliperidone 150 mg prolonged release suspension for injection, Paliperidone 25 mg prolonged release suspension for injection, Paliperidone 50 mg prolonged release suspension for injection. They are interchangeable only if your prescriber or pharmacist says so.
This leaflet reproduces the patient information leaflet approved for Paliperidone Zentiva 75 mg prolonged-release suspension for injection in pre-filled syringe, as published on the electronic medicines compendium (emc). The version printed inside your medicine’s packaging is the one that applies to you.
Whether a medicine is available over the counter or on prescription only depends on its licence. Check the leaflet, or ask your pharmacist — they can tell you straight away.
The text above reproduces the patient information leaflet approved for this medicine, restructured for easier reading.
Paliperidone Zentiva is indicated for maintenance treatment of schizophrenia in adult patients stabilised with paliperidone or risperidone.
In selected adult patients with schizophrenia and previous responsiveness to oral paliperidone or risperidone, Paliperidone Zentiva may be used without prior stabilisation with oral treatment if psychotic symptoms are mild to moderate and a long-acting injectable treatment is needed.
Posology
Recommended initiation of Paliperidone Zentiva is with a dose of 150 mg on treatment day 1 and 100 mg one week later (day 8), both administered in the deltoid muscle in order to attain therapeutic concentrations rapidly (see section 5.2). The third dose should be administered one month after the second initiation dose. The recommended monthly maintenance dose is 75 mg; some patients may benefit from lower or higher doses within the recommended range of 25 to 150 mg based on individual patient tolerability and/or efficacy. Patients who are overweight or obese may require doses in the upper range (see section 5.2). Following the second initiation dose, monthly maintenance doses can be administered in either the deltoid or gluteal muscle.
Adjustment of the maintenance dose may be made monthly. When making dose adjustments, the prolonged release characteristics of Paliperidone Zentiva should be considered (see section 5.2), as the full effect of maintenance doses may not be evident for several months.
Switching from oral prolonged release paliperidone or oral risperidone to Paliperidone Zentiva.
Paliperidone Zentiva should be initiated as described at the beginning of section 4.2 above. During monthly maintenance treatment with Paliperidone Zentiva, patients previously stabilised on different doses of paliperidone prolonged release tablets can attain similar paliperdone steady-state exposure by injection. The Paliperidone Zentiva maintenance doses needed to attain similar steady-state exposure are shown as follows:
| Doses of paliperidone prolonged release tablets and Paliperidone Zentiva needed to attain similar steady- state paliperidone exposure during maintenance treatment | |
| Previous paliperidone prolonged release tablet dose | Paliperidone Zentiva injection |
| 3 mg daily | 25-50 mg monthly |
| 6 mg daily | 75 mg monthly |
| 9 mg daily | 100 mg monthly |
| 12 mg daily | 150 mg monthly |
Previous oral paliperidone or oral risperidone can be discontinued at the time of initiation of treatment with Paliperidone Zentiva. Some patients may benefit from gradual withdrawal. Some patients switching from higher paliperidone oral doses (e.g., 9-12 mg daily) to gluteal injections with Paliperidone Zentiva may have lower plasma exposure during the first 6 months after the switch. Therefore, alternatively, it could be considered to give deltoid injections for the first 6 months.
Switching from risperidone long acting injection to Paliperidone Zentiva
When switching patients from risperidone long acting injection, initiate Paliperidone Zentiva therapy in place of the next scheduled injection. Paliperidone Zentiva should then be continued at monthly intervals. The one-week initiation dosing regimen including the intramuscular injections (day 1 and 8, respectively) as described in section 4.2 above is not required. Patients previously stabilised on different doses of risperidone long acting injection can attain similar paliperidone steady-state exposure during maintenance treatment with Paliperidone Zentiva monthly doses according to the following:
| Doses of risperidone long acting injection and Paliperidone Zentiva needed to attain similar paliperidone exposure at steady-state | |
| Previous risperidone long acting injection dose | Paliperidone Zentiva injection |
| 25 mg every 2 weeks | 50 mg monthly |
| 37.5 mg every 2 weeks | 75 mg monthly |
| 50 mg every 2 weeks | 100 mg monthly |
Discontinuation of antipsychotic medicinal products should be made in accordance with appropriate prescribing information. If Paliperidone Zentiva is discontinued, its prolonged release characteristics must be considered. The need for continuing existing extrapyramidal symptoms (EPS) medicine should be re-evaluated periodically.
Missed doses
Avoiding missed doses
It is recommended that the second initiation dose of Paliperidone Zentiva be given one week after the first dose. To avoid a missed dose, patients may be given the second dose 4 days before or after the one-week (day 8) time point. Similarly, the third and subsequent injections after the initiation regimen are recommended to be given monthly. To avoid a missed monthly dose, patients may be given the injection up to 7 days before or after the monthly time point.
If the target date for the second Paliperidone Zentiva injection (day 8 ± 4 days) is missed, the recommended reinitiation depends on the length of time which has elapsed since the patient's first injection.
Missed second initiation dose (< 4 weeks from first injection)
If less than 4 weeks have elapsed since the first injection, then the patient should be administered the second injection of 100 mg in the deltoid muscle as soon as possible. A third Paliperidone Zentiva injection of 75 mg in either the deltoid or gluteal muscles should be administered 5 weeks after the first injection (regardless of the timing of the second injection). The normal monthly cycle of injections in either the deltoid or gluteal muscle of 25 mg to 150 mg based on individual patient tolerability and/or efficacy should be followed thereafter.
Missed second initiation dose (4-7 weeks from first injection)
If 4 to 7 weeks have elapsed since the first injection of Paliperidone Zentiva, resume dosing with two injections of 100 mg in the following manner:
1. a deltoid injection as soon as possible
2. another deltoid injection one week later
3. resumption of the normal monthly cycle of injections in either the deltoid or gluteal muscle of 25 mg to 150 mg based on individual patient tolerability and/or efficacy.
Missed second initiation dose (> 7 weeks from first injection)
If more than 7 weeks have elapsed since the first injection of Paliperidone Zentiva, initiate dosing as described for the initial recommended initiation of Paliperidone Zentiva above.
Missed monthly maintenance dose (1 month to 6 weeks)
After initiation, the recommended injection cycle of Paliperidone Zentiva is monthly. If less than 6 weeks have elapsed since the last injection, then the previously stabilised dose should be administered as soon as possible, followed by injections at monthly intervals.
Missed monthly maintenance dose (> 6 weeks to 6 months)
If more than 6 weeks have elapsed since the last injection of Paliperidone Zentiva, the recommendation is as follows:
For patients stabilised with doses of 25 to 100 mg
1. a deltoid injection as soon as possible at the same dose the patient was previously stabilised on
2. another deltoid injection (same dose) one week later (day 8)
3. resumption of the normal monthly cycle of injections in either the deltoid or gluteal muscle of 25 mg to 150 mg based on individual patient tolerability and/or efficacy.
For patients stabilised with 150 mg
1. a deltoid injection as soon as possible at the 100 mg dose
2. another deltoid injection one week later (day 8) at the 100 mg dose
3. resumption of the normal monthly cycle of injections in either the deltoid or gluteal muscle of 25 mg to 150 mg based on individual patient tolerability and/or efficacy.
Missed monthly maintenance dose (> 6 months)
If more than 6 months have elapsed since the last injection of Paliperidone Zentiva, initiate dosing as described for the initial recommended initiation of Paliperidone Zentiva above.
Special populations
Elderly
Efficacy and safety in elderly > 65 years have not been established.
In general, recommended dosing of Paliperidone Zentiva for elderly patients with normal renal function is the same as for younger adult patients with normal renal function. However, because elderly patients may have diminished renal function, dose adjustment may be necessary (see Renal impairment below for dosing recommendations in patients with renal impairment).
Renal impairment
Paliperidone Zentiva has not been systematically studied in patients with renal impairment (see section 5.2). For patients with mild renal impairment (creatinine clearance ≥ 50 to < 80 ml/min), recommended initiation of Paliperidone Zentiva is with a dose of 100 mg on treatment day 1 and 75 mg one week later, both administered in the deltoid muscle. The recommended monthly maintenance dose is 50 mg with a range of 25 to 100 mg based on patient tolerability and/or efficacy.
Paliperidone Zentiva is not recommended in patients with moderate or severe renal impairment (creatinine clearance < 50 ml/min) (see section 4.4).
Hepatic impairment
Based on experience with oral paliperidone, no dose adjustment is required in patients with mild or moderate hepatic impairment. As paliperidone has not been studied in patients with severe hepatic impairment, caution is recommended in such patients (see section 5.2).
Paediatric population
The safety and efficacy of Paliperidone Zentiva in children and adolescents < 18 years of age have not been established. No data are available.
Method of administration
Paliperidone Zentiva is intended for intramuscular use only. It must not be administered by any other route. It should be injected slowly, deep into the deltoid or gluteal muscle. Each injection should be administered by a healthcare professional. Administration should be in a single injection. The dose should not be given in divided injections.
The day 1 and day 8 initiation doses must each be administered in the deltoid muscle in order to attain therapeutic concentrations rapidly (see section 5.2). Following the second initiation dose, monthly maintenance doses can be administered in either the deltoid or gluteal muscle. A switch from gluteal to deltoid (and vice versa) should be considered in the event of injection site pain if the injection site discomfort is not well tolerated (see section 4.8). It is also recommended to alternate between left and right sides (see below).
For instructions for use and handling of Paliperidone Zentiva, see package leaflet (information intended for medical or healthcare professionals).
Deltoid muscle administration
The recommended needle size for initial and maintenance administration of Paliperidone Zentiva into the deltoid muscle is determined by the patient's weight. For those ≥ 90 kg, the 1½ inch, 22 gauge needle (38.1 mm x 0.72 mm) is recommended. For those < 90 kg, the 1-inch, 23 gauge needle (25.4 mm x 0.64 mm) is recommended. Deltoid injections should be alternated between the two deltoid muscles.
Gluteal muscle administration
The recommended needle size for maintenance administration of Paliperidone Zentiva into the gluteal muscle is the 1½-inch, 22 gauge needle (38.1 mm x 0.72 mm). Administration should be made into the upper-outer quadrant of the gluteal area. Gluteal injections should be alternated between the two gluteal muscles.
Hypersensitivity to the active substance, to risperidone or to any of the excipients listed in section 6.1.
Caution is advised when prescribing Paliperidone Zentiva with medicinal products known to prolong the QT interval, e.g. class IA antiarrhythmics (e.g., quinidine, disopyramide) and class III antiarrhythmics (e.g. amiodarone, sotalol), some antihistaminics, some other antipsychotics and some antimalarials (e.g. mefloquine). This list is indicative and not exhaustive.
Potential for Paliperidone Zentiva to affect other medicines
Paliperidone is not expected to cause clinically important pharmacokinetic interactions with medicinal products that are metabolised by cytochrome P-450 isozymes.
Given the primary central nervous system (CNS) effects of paliperidone (see section 4.8), Paliperidone Zentiva should be used with caution in combination with other centrally acting medicinal products, e.g., anxiolytics, most antipsychotics, hypnotics, opiates, etc. or alcohol.
Paliperidone may antagonise the effect of levodopa and other dopamine agonists. If this combination is deemed necessary, particularly in end-stage Parkinson's disease, the lowest effective dose of each treatment should be prescribed.
Because of its potential for inducing orthostatic hypotension (see section 4.4), an additive effect may be observed when Paliperidone Zentiva is administered with other therapeutic agents that have this potential, e.g., other antipsychotics, tricyclics.
Caution is advised if paliperidone is combined with other medicinal products known to lower the seizure threshold (i.e., phenothiazines or butyrophenones, tricyclics or SSRIs, tramadol, mefloquine, etc.).
Co-administration of oral paliperidone prolonged release tablets at steady-state (12 mg once daily) with divalproex sodium prolonged release tablets (500 mg to 2,000 mg once daily) did not affect the steady-state pharmacokinetics of valproate.
No interaction study between paliperidone and lithium has been performed, however, a pharmacokinetic interaction is not likely to occur.
Potential for other medicines to affect Paliperidone Zentiva
In vitro studies indicate that CYP2D6 and CYP3A4 may be minimally involved in paliperidone metabolism, but there are no indications in vitro nor in vivo that these isozymes play a significant role in the metabolism of paliperidone. Concomitant administration of oral paliperidone with paroxetine, a potent CYP2D6 inhibitor, showed no clinically significant effect on the pharmacokinetics of paliperidone.
Co-administration of oral paliperidone prolonged release once daily with carbamazepine 200 mg twice daily caused a decrease of approximately 37% in the mean steady-state Cmax and AUC of paliperidone. This decrease is caused, to a substantial degree, by a 35% increase in renal clearance of paliperidone likely as a result of induction of renal P-gp by carbamazepine. A minor decrease in the amount of active substance excreted unchanged in the urine suggests that there was little effect on the CYP metabolism or bioavailability of paliperidone during carbamazepine co-administration. Larger decreases in plasma concentrations of paliperidone could occur with higher doses of carbamazepine.
On initiation of carbamazepine, the dose of Paliperidone Zentiva should be re-evaluated and increased if necessary.
Conversely, on discontinuation of carbamazepine, the dose of Paliperidone Zentiva should be re-evaluated and decreased if necessary.
Co-administration of a single dose of an oral paliperidone prolonged release tablet 12 mg with divalproex sodium prolonged release tablets (two 500 mg tablets once daily) resulted in an increase of approximately 50% in the Cmax and AUC of paliperidone, likely as a result of increased oral absorption. Since no effect on the systemic clearance was observed, a clinically significant interaction would not be expected between divalproex sodium prolonged release tablets and Paliperidone Zentiva intramuscular injection. This interaction has not been studied with paliperidone.
Concomitant use of Paliperidone Zentiva with risperidone or with oral paliperidone
Since paliperidone is the major active metabolite of risperidone, caution should be exercised when Paliperidone Zentiva is co-administered with risperidone or with oral paliperidone for extended periods of time. Safety data involving concomitant use of paliperidone with other antipsychotics is limited.
Concomitant use of Paliperidone Zentiva with psychostimulants
The combined use of psychostimulants (e.g., methylphenidate) with paliperidone can lead to extrapyramidal symptoms upon change of either or both treatments (see section 4.4).
Pregnancy
There are no adequate data from the use of paliperidone during pregnancy. Intramuscularly injected paliperidone palmitate and orally administered paliperidone were not teratogenic in animal studies, but other types of reproductive toxicity were seen (see section 5.3). Neonates exposed to paliperidone during the third trimester of pregnancy are at risk of adverse reactions including extrapyramidal and/or withdrawal symptoms that may vary in severity and duration following delivery. There have been reports of agitation, hypertonia, hypotonia, tremor, somnolence, respiratory distress, or feeding disorder. Consequently, newborns should be monitored carefully. Paliperidone Zentiva should not be used during pregnancy unless clearly necessary.
Breast-feeding
Paliperidone is excreted in the breast milk to such an extent that effects on the breast-fed infant are likely if therapeutic doses are administered to breast-feeding women. Paliperidone Zentiva should not be used while breast-feeding.
Fertility
There were no relevant effects observed in the non-clinical studies.
Paliperidone can have minor or moderate influence on the ability to drive and use machines due to potential nervous system and visual effects, such as sedation, somnolence, syncope, vision blurred (see section 4.8). Therefore, patients should be advised not to drive or operate machines until their individual susceptibility to Paliperidone Zentiva is known.
Symptoms
In general, expected signs and symptoms are those resulting from an exaggeration of paliperidone's known pharmacological effects, i.e., drowsiness and sedation, tachycardia and hypotension, QT prolongation, and extrapyramidal symptoms. Torsade de pointes and ventricular fibrillation have been reported in a patient in the setting of overdose with oral paliperidone. In the case of acute overdose, the possibility of multiple drug involvement should be considered.
Management
Consideration should be given to the prolonged release nature of the medicinal product and the long elimination half-life of paliperidone when assessing treatment needs and recovery. There is no specific antidote to paliperidone. General supportive measures should be employed. Establish and maintain a clear airway and ensure adequate oxygenation and ventilation.
Cardiovascular monitoring should commence immediately and should include continuous electrocardiographic monitoring for possible arrhythmias. Hypotension and circulatory collapse should be treated with appropriate measures such as intravenous fluid and/or sympathomimetic agents. In case of severe extrapyramidal symptoms, anticholinergic agents should be administered. Close supervision and monitoring should continue until the patient recovers.
Ask anything about Paliperidone Zentiva 75 mg prolonged-release suspension for injection in pre-filled syringe. The assistant answers only from this leaflet — if the leaflet does not cover it, it will say so. It does not give medical advice.
Answers come from the patient leaflet published on the electronic medicines compendium (emc). They are not medical advice. Ask a pharmacist or your GP if you are unsure. For urgent help call NHS 111, or 999 in an emergency.
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