Paliperidone palmitate (PP), sold under the brand name Invega Sustenna among others, is an

atypical antipsychotic The atypical antipsychotics (AAP), also known as second generation antipsychotics (SGAs) and serotonin–dopamine antagonists (SDAs), are a group of antipsychotic drugs (antipsychotic drugs in general are also known as major tranquilizers and ne ...

which is used in the treatment of

schizophrenia Schizophrenia is a mental disorder characterized by continuous or relapsing episodes of psychosis. Major symptoms include hallucinations (typically hearing voices), delusions, and disorganized thinking. Other symptoms include social wit ...

and

schizoaffective disorder Schizoaffective disorder (SZA, SZD or SAD) is a mental disorder characterized by abnormal thought processes and an unstable mood. This diagnosis is made when the person has symptoms of both schizophrenia (usually psychosis) and a mood disorder: ...

. It is an

antipsychotic ester An antipsychotic ester is an ester of an antipsychotic. They are used clinically as prodrugs to increase fat solubility and thereby prolong duration when antipsychotics are used as depot injectables. List of clinically used antipsychotic ester ...

– specifically the

palmitate Palmitic acid (hexadecanoic acid in IUPAC nomenclature) is a fatty acid with a 16-carbon chain. It is the most common saturated fatty acid found in animals, plants and microorganisms.Gunstone, F. D., John L. Harwood, and Albert J. Dijkstra. The L ...

ester In chemistry, an ester is a compound derived from an oxoacid (organic or inorganic) in which at least one hydroxyl group () is replaced by an alkoxy group (), as in the substitution reaction of a carboxylic acid and an alcohol. Glycerides a ...

paliperidone Paliperidone, sold under the trade name Invega among others, is an atypical antipsychotic. It is mainly used to treat schizophrenia and schizoaffective disorder. It is marketed by Janssen Pharmaceuticals. An extended release formulation is a ...

– and acts as a long-lasting form of paliperidone. Paliperidone palmitate is formulated as an aqueous suspension and is administered by intramuscular injection into deltoid or gluteal muscle once every 1 or 3 months depending on the formulation. A formulation for injection once every 6 months is also pending regulatory approval as of September 2021. With the once-monthly formulation of paliperidone palmitate, the time to peak is 13 days and the

elimination half-life Biological half-life (also known as elimination half-life, pharmacologic half-life) is the time taken for concentration of a biological substance (such as a medication) to decrease from its maximum concentration ( Cmax) to half of Cmax in the bl ...

is 25 to 49 days, and with the 3-month formulation, the time to peak is 30 to 33 days and the half-life is 84 to 95 days via deltoid muscle and 118 to 139 days gluteally. The peak-to-trough ratio of paliperidone palmitate at

steady state In systems theory, a system or a process is in a steady state if the variables (called state variables) which define the behavior of the system or the process are unchanging in time. In continuous time, this means that for those properties ''p' ...

ranges from 1.56 to 1.70 with the 1- and 3-month formulations. The 3-month formulation of paliperidone palmitate has larger

crystal size Particle size is a notion introduced for comparing dimensions of solid particles ('' flecks''), liquid particles ('' droplets''), or gaseous particles ('' bubbles''). The notion of particle size applies to particles in colloids, in ecology, in ...

s than the 1-month formulation and this allows for its longer duration. No pharmacokinetic data for the 6-month formulation has been released as of January 2021.

References

External links

* Antipsychotic esters Atypical antipsychotics Benzisoxazoles Fluoroarenes Lactams Mood stabilizers Palmitate esters Piperidines Prodrugs Prolactin releasers Pyridopyrimidines {{Nervous-system-drug-stub