Paliperidone (Intramuscular)

Paliperidone is an injectable, anti-psychotic medicine used to treat symptoms of schizophrenia, and is also combined with other medicines to treat schizoaffective disorder.

Overview

Paliperidone is an extended-release suspension injected into a muscle (intramuscular) to treat patients with symptoms of schizophrenia. It is given in the same way when treating patients with schizoaffective disorder.

This medicine works by balancing the hormones serotonin and dopamine in the brain, thereby improving the patient's mood, thinking, and behavior.

While it treats schizophrenia, the medicine is not for treating behavioral problems in geriatric patients who suffer from dementia. This may increase the risk of a stroke, mini-stroke or even death in these patients.

Because the medicine may cause some rare but serious side effects that may result in death, certain patients should be treated with extreme caution. Others should not be treated with it at all.

Paliperidone is the generic name for this injection suspension which is sold in the US under the brand names, Invega Sustenna and Invega Trinza. It may be used to treat other psychotic disorders not discussed in this guide.

Conditions Treated

  • Symptoms of Schizophrenia
  • Schizoaffective disorder

Type Of Medicine

Antipsychotic

Side Effects

Prescription medicines, such as Paliperidone, generally cause various side effects. Some of them are necessary and expected as the medicine works in the body.

Some of the side effects caused by this antipsychotic drug may not require medical attention. Others are serious and will need emergency medical care.

Some patients may experience one or more side effects. The following lists of side effects may occur, but not all patients taking Paliperidone may experience them.

Serious side effects

The following are serious side effects. Get emergency medical care if you experience any of them:

Allergic reactions

Paliperidone may cause allergic reactions in some patients. Reactions are hives, itching, tightness in the chest, trouble breathing, swelling of the hands or face, or tingling or swelling in the mouth or throat.

Heart problems, strokes, or death

There is a greater risk of strokes, transient ischemic attacks (TIAs), and even death when patients with behavior problems caused by dementia use Paliperidone.

The risk of a heart attack due to an irregular heartbeat (arrhythmia) or QT prolongation may be greater in certain patients.

Other potentially fatal symptoms you should seek urgent medical care for are pounding heartbeat, dizziness, feeling as if you will faint, or fainting.

Neuroleptic Malignant Syndrome (NMS)

Although it rarely occurs, a patient may experience this condition which can result in death.

Symptoms of neuroleptic malignant syndrome include confusion, high fever, sweating, fainting, loss of consciousness, muscle stiffness, and fast or irregular heartbeat.

Agitated or suicidal behaviors

Patients being treated with Paliperidone injection may feel agitated. They may generally not feel like themselves; or feel anxious, aggressive, emotional, or restless.

Some patients may have thoughts about hurting or killing themselves or hurting others. They may experience these symptoms a few weeks after starting treatment with the injection.

Due to the seriousness of these side effects, your doctor may have to monitor you closely for changes in your emotions, moods, or behavior.

Also seek emergency care if you experience the following:

  • Sexual dysfunction, especially painful or prolonged erection that lasts for more than 4 hours.
  • Hyperprolactinemia (high level of the hormone prolactin in your blood).

Hyperprolactinemia may result in side effects such as problems with erection, breastmilk leakage, missed menstrual periods, or the development of breasts in male patients.

The following list of general side effects may also occur and will require urgent medical attention. Call your doctor immediately if you notice the following effects:

More commonly occur

  • Headache
  • Fever
  • Chills
  • Ear congestion
  • Anxiety
  • Cloudy or bloody urine
  • Inability to sit still
  • Cough
  • Loss of voice
  • Body aches or pain
  • Hyperventilation
  • Bladder pain
  • Irregular heartbeats
  • Difficulty swallowing
  • Need to keep moving
  • Irritability
  • Slurred speech
  • Pain in the lower back or side
  • Dry mouth
  • Mask-like face
  • Shuffling walk
  • Increased urge to urinate
  • Stiffness of the legs and arms
  • Nasal congestion
  • Trouble sleeping
  • Slowed movements
  • Difficulty breathing
  • Nervousness
  • Runny nose
  • Loss of body balance
  • Sore throat
  • Trembling and shaking of the fingers and hands
  • Difficulty, burning, or pain while urinating
  • Jerky movements of the head, neck, face, and mouth
  • Shaking
  • Feeling unusually tired or weak
  • Restlessness
  • Twisting, twitching or other movements of the face, lips, tongue, legs or arms that cannot be controlled
  • Sneezing

Less commonly occur

  • Tremor
  • Difficulty speaking
  • Sticking out of the tongue
  • Drooling
  • Headache
  • Dizziness
  • Pounding sensation in the ears
  • Restlessness
  • Fast or slow heartbeat
  • Blurred vision
  • Stiffness of the limbs
  • Unable to move the eyes
  • Difficulty swallowing, speaking or breathing
  • Increased movements
  • Muscle stiffness, trembling or jerking
  • Twisting movements of the body
  • Uncontrollable, twisting movements of the trunk of the body, neck, legs or arms
  • Unusual facial expressions
  • Loss of balance control
  • Unable to control movements, especially of the neck, back, and face
  • Eyelid spasms or increased blinking

Some side effects may occur that are not considered as “serious” and generally do not need medical attention. These are effects that can be managed by the patient and may go away on their own.

The following are some of those types of side effects. If any occur but get worse, bothersome or do not go away, tell your doctor.

More commonly occur

  • Feeling of pressure
  • Blistering
  • Coldness
  • Bleeding
  • Discoloration of the skin
  • Burning
  • Itching, hives, rash, ulcers, soreness, lumps, inflammation, infection, numbness, pain, stinging, redness, scarring, warmth, tenderness, tingling or swelling at the injection site

Less commonly occur

  • Dry mouth
  • Nausea
  • Joint pain
  • Back pain
  • Pain in the stomach or upper abdomen
  • Vomiting
  • Stiffness or pain in the muscle
  • Nightmares
  • Diarrhea
  • Constipation
  • Tearing of the skin
  • Weight gain
  • Lack or loss of strength
  • Difficulty moving
  • Pain in the legs or arms
  • Swelling of the joints
  • Aching or cramping of the muscle
  • Toothache

If you experience any unusual symptom that bothers you or does not go away, tell your doctor. Your doctor or healthcare professional may give you information on how to prevent or reduce side effects.

You may also call the FDA at 1-800-FDA-1088 to report side effects.

Dosage

Paliperidone extended-release suspension is usually supplied as 50 mg/0.5 mL, 75 mg/0.75 mL, 100 mg/1 mL, or 150 mg/1.5 mL prefilled-syringes.

It is given to patients by a nurse or healthcare professional under the direct supervision of a doctor. This is usually done at a hospital or clinic.

The nurse or healthcare professional will inject the prescribed dosage amount into one of your muscles.

Missed dose

Since you will be given this medication at the hospital or clinic, it is important to keep your appointments to receive it.

If you missed an appointment to take your injection, call your doctor as soon as possible to set a new appointment.

Overdose

Call your doctor, 911 and/or the local poison control center at 1-800-222-1222, if you overdose on this drug. If the patient collapses or is not breathing, call 911.

The following are symptoms of an overdose. Seek emergency medical care right away if you experience them:

  • Seizures
  • Increased or irregular heartbeat
  • Drowsiness
  • Shuffling walk
  • Extreme tiredness
  • Slow movements
  • Unusual or uncontrolled movements of the head, neck, face, mouth, tongue, legs or arms

Interactions

Other medicines or medical problems that increase the risk of side effects or decrease the effectiveness of Paliperidone should be avoided during treatment. Paliperidone may also block the effects of other drugs being used by the patient.

Food, alcohol, and tobacco

Your doctor may tell you whether the use of certain foods, alcohol, or tobacco should be avoided during treatment.

Other medicines

Tell your doctor if you are using antibiotics, medicines for heart rhythm problems, blood pressure or mental illness, or the herbal product, St John's Wort. They may cause significant adverse interactions with the injection.

The following medicines are not recommended to be used with Paliperidone. If your doctor decides to treat you with this injection, some of the other medicines you take may be changed.

  • Piperaquine
  • Amifampridine
  • Sparfloxacin
  • Amisulpride
  • Mesoridazine
  • Saquinavir
  • Bepridil
  • Ziprasidone
  • Cisapride
  • Terfenadine
  • Metoclopramide
  • Pimozide
  • Thioridazine
  • Dronedarone
  • Bromopride

Paliperidone is not usually recommended to be used with any of the following medicines. In some cases, their use may be required.

If any of them are prescribed together with the injection, your doctor may change your dose or how often you use any of your medicines.

  • Morphine Sulfate Liposome
  • Levofloxacin
  • Ofloxacin
  • Escitalopram
  • Hydroxyzine
  • Fingolimod
  • Hydroquinidine
  • Fluoxetine
  • Gemifloxacin
  • Fentanyl
  • Granisetron
  • Leuprolide
  • Histrelin
  • Ketoconazole
  • Hydrocodone
  • Gatifloxacin
  • Nortriptyline
  • Haloperidol
  • Ibutilide
  • Fluconazole
  • Mifepristone
  • Gonadorelin
  • Iloperidone
  • Pentazocine
  • Hydroxychloroquine
  • Ivabradine
  • Lapatinib
  • Flecainide
  • Lopinavir
  • Clarithromycin
  • Lumefantrine
  • Methadone
  • Hydromorphone
  • Nafarelin
  • Halofantrine
  • Nilotinib
  • Norfloxacin
  • Octreotide
  • Meperidine
  • Butorphanol
  • Ondansetron
  • Imipramine
  • Oxymorphone
  • Goserelin
  • Oxycodone
  • Tizanidine
  • Mefloquine
  • Pasireotide
  • Remifentanil
  • Pazopanib
  • Acecainide
  • Perflutren Lipid Microsphere
  • Procainamide
  • Metronidazole
  • Prochlorperazine
  • Anagrelide
  • Propafenone
  • Quetiapine
  • Panobinostat
  • Quinine
  • Ranolazine
  • Pitolisant
  • Morphine
  • Salmeterol
  • Ajmaline
  • Quinidine
  • Buprenorphine
  • Pimavanserin
  • Alfentanil
  • Protriptyline
  • Alfuzosin
  • Citalopram
  • Amitriptyline
  • Trimipramine
  • Amoxapine
  • Dasatinib
  • Aripiprazole
  • Promethazine
  • Artemether
  • Trifluoperazine
  • Azimilide
  • Tramadol
  • Bedaquiline
  • Posaconazole
  • Buserelin
  • Chloroquine
  • Dihydrocodeine
  • Toremifene
  • Sodium Phosphate, Monobasic
  • Ciprofloxacin
  • Sotalol
  • Domperidone
  • Moxifloxacin
  • Clomipramine
  • Asenapine
  • Clozapine
  • Bretylium
  • Codeine
  • Azithromycin
  • Sunitinib
  • Crizotinib
  • Trazodone
  • Cyclobenzaprine
  • Degarelix
  • Zuclopenthixol
  • Tedisamil
  • Delamanid
  • Tacrolimus
  • Dofetilide
  • Telithromycin
  • Dolasetron
  • Apomorphine
  • Droperidol
  • Eliglustat
  • Dabrafenib
  • Erythromycin
  • Sematilide
  • Disopyramide
  • Simeprevir
  • Efavirenz
  • Sodium Phosphate
  • Amiodarone
  • Sodium Phosphate, Dibasic
  • Donepezil
  • Solifenacin
  • Arsenic Trioxide
  • Tetrabenazine
  • Sevoflurane
  • Desipramine
  • Triptorelin
  • Vandetanib
  • Sorafenib
  • Vardenafil
  • Telavancin
  • Sufentanil
  • Vemurafenib
  • Deslorelin
  • Vinflunine
  • Tapentadol
  • Chlorpromazine
  • Voriconazole
  • Sulpiride

There is a potential for an increase in the risk of certain side effects if any of the following medicines are used with Paliperidone injection. However, using them together may be best for your health.

If the injection is prescribed together with any of them, your doctor may change your dose or how often you use any of your medicines.

  • Carbamazepine
  • Paroxetine

Other medical problems

The presence of other medical problems in patients being treated with this antipsychotic medicine may result in adverse interactions. Tell your doctor if you have other medical problems, especially any of those listed below.

To avoid making them worse, use the medicine with caution in patients who have or have a history of the following conditions:

  • Diabetes
  • Neuroleptic malignant syndrome (NMS)
  • Blood or bone marrow problems (such as neutropenia or leukopenia)
  • High blood sugar (Hyperglycemia)
  • Seizures
  • High prolactin in the blood (Hyperprolactinemia)
  • Stomach or bowel problems (such as slowed or blocked bowels)
  • Painful or prolonged erection of the penis (Priapism)

Paliperidone may worsen side effects when used in patients who have or have a history of the following conditions:

  • Stroke
  • Dehydration
  • Heart or blood vessel disease
  • Dementia or Alzheimer's disease
  • Heart rhythm problems (e.g. QT prolongation or arrhythmia)
  • Trouble swallowing
  • Low blood pressure (Hypotension)
  • Heart attack
  • Low amount of blood (Hypovolemia)
  • Parkinson's disease
  • Heart failure

The removal of the medicine from the body may be slowed in patients with the following condition. Use the medicine with caution.

  • Kidney disease

Warnings

  • Do not use Paliperidone injection if you are allergic to it or other medicines such as risperidone. Also, do not use the medicine if you are allergic to any of its inactive ingredients.
  • Tell your doctor if you are allergic to certain foods, dyes, preservatives, or animals.
  • This medicine should not be used to treat children because its safety and efficacy have not been established.
  • Tell your doctor if you are pregnant, may become pregnant or are breastfeeding. There may be a risk of harm to an unborn baby or a breastfeeding infant.

Your doctor should weigh the potential benefits and potential risks involved when deciding to treat you. Your doctor may need to take necessary precautions while treating you.

  • Do not use other medicines while taking Paliperidone unless your doctor approves them.
  • Let your doctor know about all prescription or non-prescription medicines, or vitamins you take. If you are taking herbal supplements, especially St. John's Wort, tell your doctor.
  • Paliperidone may cause adverse interaction with certain medical problems. Tell your doctor about any other medical problem you have or have a history of. This will help the doctor take necessary precautions when deciding to treat you with the injection.
  • Do not use this medicine for treating behavioral problems in elderly patients who suffer from dementia. This may increase the risk of a stroke, mini-stroke or even death in these patients.
  • Do not drive a vehicle or operate machinery while taking the injection. The medicine may cause drowsiness and reduce alertness needed to do these activities.
  • Avoid drinking alcohol during treatment as it increases dizziness and drowsiness and may reduce your ability to remain alert.
  • To prevent severe drowsiness, avoid taking other medicines that cause drowsiness. They include medicines for sleeping, cough, allergy, and pain.
  • Avoid vigorous exercise and exposure to extreme heat. The medicine may cause heavy sweating and makes it difficult for your body to cool down. Drink plenty of water to keep your body cool.
  • Paliperidone may cause a rise in the level of blood sugar (Hyperglycemia) even if you do not have diabetes. Patients with schizophrenia who are taking this drug are more likely to develop diabetes.
  • Call your doctor right away if you experience symptoms of diabetes, such as blurred vison, extreme hunger or thirst, weakness or frequent urination.

Storage

This injection is usually stored at a hospital or clinic.

Summary

Paliperidone extended-release injection suspension is an effective, antipsychotic medicine for treating symptoms of schizophrenia and schizoaffective disorder.

For the medicine to function effectively in the treatment of schizophrenia and schizoaffective disorder, patients are required to keep all their appointments for injection.

In spite of its effectiveness, there is a risk of serious side effects such as neuroleptic malignant syndrome (NMS), sexual dysfunction, diabetes, suicidal behaviors, heart problems, strokes, and death.

As such, precautions must be taken while treating patients, especially those who already have or have a history of certain medical problems.

These include heart or blood vessel problems, heart failure, high prolactin in the blood (Hyperprolactinemia), stroke, and dementia.

Elderly patients with dementia may be placed at an increased risk of developing a stroke or mini-stroke if treated with Paliperidone. Some patients have even died.

Because of these serious and possibly life-threatening effects, the medicine should be prescribed only when the potential benefits outweigh the potential risks involved.