PALIPERIDONE

PALIPERIDONE
PRODUCT IDENTIFICATION
CAS NO.	144598-75-4
EINECS NO.
FORMULA	C₂₃H₂₇FN₄O₃
MOL WT.	426.48
TOXICITY	Oral Rat LD50: 65mg/kg
H.S. CODE	2934.99.3000
SYNONYMS	Paliperidone;
9-Hydroxyrisperidone; Invega; (9RS)-3-(2-(4-(6-Fluoro-1,2-benzisoxazol-3-yl) piperidin-1-yl))ethyl)-9-hydroxy- 2-methyl-6,7,8,9-tetrahydro-4H-pyrido(1,2-a) pyrimidin-4-one; 9-OH-Risperidone; 3-(2-(4-(6-Fluoro-1,2- benzisoxazol-3-yl)-1- piperidinyl)ethyl)-6,7,8,9- tetrahydro-9-hydroxy-2- methyl- 4H-pyrido(1,2-a)pyrimidin -4-one; Other RN: 130049-84-2, 130049-86-4, 147687-18-1
SMILES	c1(F)cc2onc(c2cc1)C1CCN(CC1)CCc1c(nc2n(c1=O)CCC[C@@ H]2O)C
CLASSIFICATION	Psychotropic, Tranquilizing agent, Atypical antipsychotic, Benzisoxazole, Piperidine, Lactam
EXTRA NOTES	Paliperidone is an atypical antipsychotic; active metabolite of risperidone.
PHYSICAL AND CHEMICAL PROPERTIES
PHYSICAL STATE	white to off-white crystalline powder
MELTING POINT	168 - 173 C
BOILING POINT
SPECIFIC GRAVITY
SOLUBILITY IN WATER
SOLVENT SOLUBILITY
pH
VAPOR DENSITY
REFRACTIVE INDEX
NFPA RATINGS	Health hazard: 2, Fire: 0, Reactivity Hazard: 0
AUTOIGNITION
FLASH POINT
STABILITY	Stable under normal conditions.
EXTERNAL LINKS & GENERAL DESCRIPTION
Wikipedia Linking Google Scholar Search Drug Information Portal (U.S. National Library of Medicine) - PALIPERIDONE PubChem Compound Summary - PALIPERIDONE http://ajp.psychiatryonline.org/ Randomized, Double-Blind, Placebo-Controlled Study of Paliperidone Extended-Release and Quetiapine in Inpatients With Recently Exacerbated Schizophrenia http://www.ispub.com/ Paliperidone ER is metabolite of risperidone (9-hydroxy-risperidone) formulated as OROS extended release system, which facilitates its once daily use and improves treatment compliance. It is indicated not only in schizophrenia but also in schizoaffective disorder and bipolar mania. Due to lack of interactions of CYP enzymes, minimal or no pharmacological interactions are evident. Due to favorable pharmacodynamic profile i.e. antagonism of 5HT_2A, α₁ and D₂; it has improved positive and negative symptoms (reduction in PANSS score), reduced extra pyramidal side effects and efficacy. Only renal failure patients demand dose reduction. In various therapeutic trials, paliperidone ER has shown better efficacy than placebo and olanzapine, also delays symptoms recurrence of schizophrenia. Paliperidone ER has caused various adverse effects like akathisia, headache, increase serum prolactin level and weight gain but serum lipid, glucose and insulin level remained unaffected. Paliperidone ER has increased the number of annual stable days and more cost effective than other atypical antipsychotics. http://www.drugbank.ca/ Mechanism of action:l Paliperidone is the major active metabolite of risperidone. The mechanism of action of paliperidone, as with other drugs having efficacy in schizophrenia, is unknown, but it has been proposed that the drug's therapeutic activity in schizophrenia is mediated through a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism.
SALES SPECIFICATION
APPEARANCE	white to off-white crystalline powder
ASSAY	98.0 ~ 102.0%
MELTING POINT	168 ~ 173 C
IMPURITY	Individual Impurity: 0.3% max Total Impurity: 1.0% max
RESIDUAL SOLVENTS	DMF 0.1% max, Acetone 0.5% max
WATER	1.0% max
HEAVY METALS	20ppm max
RESIDUE ON IGNITION	0.25% max
TRANSPORTATION
PACKING
HAZARD CLASS	6.1 (Packing group: III)
UN NO.	2811
SAFETY INFORMATION
GHS	OSHA Hazards: Toxic by ingestion
SIGNAL WORD	Danger
PICTOGRAMS
HAZARD STATEMENTS	H301 Toxic if swallowed.
PRECAUTIONARY STATEMENTS	P301 + P310 IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.
EC DIRECTIVES
HAZARD CODES	T Toxic
RISK PHRASES	25 Toxic if swallowed
SAFETY PHRASES	28 After contact with skin, wash immediately with plenty of ... (to be specified by the manufacturer) 36 Wear suitable protective clothing 45 In case of accident or if you feel unwell, seek medical advice immediately (show label where possible)
PRICE INFORMATION