Paliperidone Palmitate CAS NO 199739-10-1 Inquire about Paliperidone Palmitate

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What is Paliperidone?Paliperidone Palmitate

Paliperidone (trade name Invega), also known as 9-hydroxyrisperidone, is an antipsychotic drug developed by Janssen Pharmaceutica. Invega is an extended release formulation of paliperidone that uses the OROS extended release system to allow for once-daily dosing. Paliperidone palmitate (trade name Invega Sustenna, named Xeplion in Europe) is a long-acting injectable formulation of paliperidone palmitoyl ester indicated for once-monthly injection after an initial titration period.

What is Paliperidone used for?

Paliperidone is the primary active metabolite of the older antipsychotic risperidone. While its specific mechanism of action is unknown, it is believed paliperidone and risperidone act via similar, if not identical, pathways.
Paliperidone has antagonist effect at ?1 and ?2 adrenergic receptors and at H1 histamine receptors. It does not bind to muscarinic acetylcholine receptors.

What are the Side effects and adverse reactions?

Adverse effects differ depending on the amount of the dose. The higher the dose the more adverse effects there are and the greater the level of the side effects and vice versa. Also some adverse effects only occur after long-term use of paliperidona. The aim is to use the lowest dose possible of oral or injectable paliperidone. Also if it is used concurrently with another psychiatric medicine it will become very complicated telling which drug is responsible for the side effect. Also people react differently and adverse effects vary between individual users. Furthermore, some adverse effects occur with every user of paliperidona while some adverse effects occur with only a tiny percentage of the users. Usually adverse effects go away after either discontinuation or reducing of the drug but some will stay with the user for his lifetime. The aim is to use psychiatric medications at the lowest level possible to prevent symptoms of the psychiatric disorder. Often many medications at a high level are used during hospitalization to shorten the time and cost of a patient being in the psychiatric hospital and much lower doses are needed for maintenance once the patient is stabilized. Also, sometimes a few side effects may diminish once the body adapts to the medicine.

The most common side effects of paliperidone are restlessness and extrapyramidal disorder, including involuntary movements, tremors and muscle stiffness. Some users reported experiencing sexual dysfunction while administering this drug in combination with serotonin reuptake inhibitors such as sertraline. Invega website’s Important Safety Information page includes this warning: Elderly Patients with dementia-related psychosis treated with atypical antipsychotic drugs are at an increased risk of death compared to placebo. Invega (paliperidone) is not approved for the treatment of patients with dementia-related psychosis.

Neuroleptic malignant syndrome is a rare, but potentially lethal reaction to any antipsychotic medication.

Other risks include:
  • Tardive dyskinesia, a serious, sometimes permanent side effect reported with INVEGA and other neuroleptics. The risk of tardive dyskinesia increases with total dose and thus becomes more likely the longer a person takes Invega.
  • Hyperprolactinemia, or elevated levels of the hormone prolactin, potentially leading to the absence of a menstrual period; breasts producing milk; the enlargement of breasts in males; and erectile dysfunction.
  • Extrapyramidal effects — persistent movement disorders or muscle disturbances, such as restlessness, tremors, and muscle stiffness.
  • Caution should be exercised before prescribing Invega to pregnant or nursing women.

Rare side effects include:

  • Impairment of alertness and driving ability
  • Risk in people with a seizure disorder or a history or health conditions that make seizures more likely

Information on this page is provided for general information purposes. You should not make a clinical treatment decision based on information contained in this page without consulting other references including the package insert of the drug, textbooks and where relevant, expert opinion. We cannot be held responsible for any errors you make in administering drugs mentioned on this page, nor for use of any erroneous information contained on this page.