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Home > Encyclopedia > Paliperidone palmitate

Paliperidone palmitate

pharmaceutical raw materials
Paliperidone palmitate structure

Paliperidone palmitate 

structure
  • CAS No:

    199739-10-1

  • Formula:

    C39H57FN4O4

  • Chemical Name:

    Paliperidone palmitate

  • Synonyms:

    Hexadecanoic acid,3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2-methyl-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl ester;9-Hydroxyrisperidone palmitate;RO 92670;Paliperidone palmitate;Invega Sustenna;Xeplion;Trevicta

  • Categories:

    Active Pharmaceutical Ingredients  >  Nervous System Drugs

Description

3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-2-methyl-4-oxo-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-9-yl hexadecanoate is a fatty acid ester obtained by the formal condensation of the carboxy group of hexadecanoic acid with the hydroxy group of 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one. It is a member of 1,2-benzoxazoles, a heteroarylpiperidine, an organofluorine compound, a pyridopyrimidine and a fatty acid ester.|A benzisoxazole derivative and active metabolite of RISPERIDONE that functions as a DOPAMINE D2 RECEPTOR ANTAGONIST and SEROTONIN 5-HT2 RECEPTOR ANTAGONIST. It is an ANTIPSYCHOTIC AGENT used in the treatment of SCHIZOPHRENIA.

Paliperidone palmitate Basic Attributes

664.907

664.89

N05AX13

Characteristics

88.2

9.85

1.19

736.3±70.0 °C(Predicted)

399.1±35.7 °C

1.590

Safety Information

P201, P202, P260, P263, P264, P270, P281, P301+P310, P308+P313, P321, P330, P405, P501

H301

|Danger|H301 (100%): Toxic if swallowed [Danger Acute toxicity, oral]|P201, P202, P260, P263, P264, P270, P281, P301+P310, P308+P313, P321, P330, P405, and P501|Aggregated GHS information provided by 21 companies from 4 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Trevicta, a 3 monthly injection, is indicated for the maintenance treatment of schizophrenia in adult patients who are clinically stable on 1 monthly paliperidone palmitate injectable product.|Xeplion 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, Xeplion may be used without prior stabilisation with oral treatment if psychotic symptoms are mild to moderate and a long-acting injectable treatment is needed.|Schizoaffective disorder, Schizophrenia|Paliperidone Janssen-Cilag International 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 Janssen-Cilag International may be used without prior stabilisation with oral treatment if psychotic symptoms are mild to moderate and a long acting injectable treatment is needed.

Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus. (See all compounds classified as Antipsychotic Agents.)|Compounds and drugs that bind to and inhibit or block the activation of DOPAMINE D2 RECEPTORS. (See all compounds classified as Dopamine D2 Receptor Antagonists.)|Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes. (See all compounds classified as Serotonin 5-HT2 Receptor Antagonists.)

3-(2-(4-(6-fluoro-3-(1,2-benzisoxazolyl))-1-piperidinyl)ethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido(1,2-a)pyrimidin-4-one

Paliperidone palmitate Use and Manufacturing

Uses

Paliperidone Palmitate is a long-acting injectable atypical antipsychotic used in the treatment of schizophrenia.

Human drugs -> Trevicta (previously Paliperidone Janssen) -> EMA Drug Category|Psycholeptics -> Human pharmacotherapeutic group|Human drugs -> Xeplion -> EMA Drug Category|Human Drugs -> EU pediatric investigation plans|Human drugs -> Paliperidone Janssen-Cilag International -> EMA Drug Category|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:664.9
XLogP3:10.1
Hydrogen Bond Acceptor Count:8
Rotatable Bond Count:20
Exact Mass:664.43638447
Monoisotopic Mass:664.43638447
Topological Polar Surface Area:88.2
Heavy Atom Count:48
Complexity:1090
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Drug Function and Efficacy

No specific description provided

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Registered Holders

  • JUBILANT BIOSYS LTD

    United States United States
    Active
  • MATRIX PHARMACORP PRIVATE LTD

    United States United States
    Active
  • APITORIA PHARMA PRIVATE LTD

    United States United States
    Active

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