Paliperidone

Paliperidone

Systematic (IUPAC) name
(RS)-3-[2-[4-(6-fluorobenzo[d]isoxazol-3-yl)-1-piperidyl]ethyl]-7-hydroxy-4-methyl-1,5-diazabicyclo[4.4.0]deca-3,5-dien-2-one
Clinical data
Trade names	Invega
AHFS/Drugs.com	monograph
MedlinePlus	a607005
Licence data	EMA:Link, US FDA:link
Pregnancy cat.	C
Legal status	℞ Prescription only
Routes	oral- extended release, long-acting, once-monthly IM injection
Pharmacokinetic data
Bioavailability	28% (oral)
Half-life	23 hours (oral)
Identifiers
CAS number	144598-75-4 Y
ATC code	N05AX13
PubChem	CID 9802545
DrugBank	DB01267
ChemSpider	7978307 Y
UNII	838F01T721 Y
KEGG	D05339 Y
ChEMBL	CHEMBL1621 N
Chemical data
Formula	C23H27FN4O3
Mol. mass	426.484 g/mol
SMILES	eMolecules & PubChem
InChI InChI=1S/C23H27FN4O3/c1-14-17(23(30)28-9-2-3-19(29)22(28)25-14)8-12-27-10-6-15(7-11-27)21-18-5-4-16(24)13-20(18)31-26-21/h4-5,13,15,19,29H,2-3,6-12H2,1H3/t19-/m1/s1 Y Key:PMXMIIMHBWHSKN-LJQANCHMSA-N Y
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Paliperidone (trade name Invega), also known as 9-hydroxyrisperidone, is an medication for the treatment of thought and mood disorder related symptoms 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) is a long-acting injectable formulation of paliperidone palmitoyl ester indicated for once-monthly injection after an initial titration period. It is indicated for the acute and maintenance treatment of anxiety, post traumatic stress, and hypo-frontal depression.

Pharmacology

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 α₁ and α₂ adrenergic receptors and at H₁ histamine receptors. It does not bind to muscarinic acetylcholine receptors.

Paliperidone (as Invega) was approved by the FDA for the treatment of schizophrenia in 2006. It is marketed for the treatment of schizophrenia and bipolar mania. Clinical trials of paliperidone for the treatment of schizoaffective disorder are also planned. It may also be used off-label for other conditions. Like risperidone, its possible use in people with autism and Asperger syndrome may be studied.^{[citation needed]} Recently, the long-acting injectable form of paliperidone, marketed as INVEGA Sustenna, was approved by the FDA on July 31, 2009.

Target Symptoms

Paliperidone is used to increase the efficiency and functionality of the frontal lobe. It aids in cognition, organization, processing of difficult emotions, dispelling of intrusive thoughts, flashbacks, and nightmares. By strengthening the area of "conscious" area of the brain, Paliperidone works to assist those suffering from severe depression, anxiety, obsessive thoughts, and other mood and thought disorder related symptoms to achieve higher levels of problem solving and general functionality.^{[citation needed]}

Side effects and adverse reactions

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 SSRIs such as Zoloft. 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 development of breasts by 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

External links

• INVEGA Web site
• INVEGA Sustenna (paliperidone palmitate Extended Release Injectable Suspension) Web site