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 withdra ...
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 Li ...
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 ar ...
of
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
In chemistry, a suspension is a Mixture#Homogeneous and heterogeneous mixtures, heterogeneous mixture of a fluid that contains solid particles sufficiently large for sedimentation. The particles may be macroscopic, visible to the naked eye, usual ...
and is administered by
intramuscular injection
Intramuscular injection, often abbreviated IM, is the injection of a substance into a muscle. In medicine, it is one of several methods for parenteral administration of medications. Intramuscular injection may be preferred because muscles have ...
into
deltoid or
gluteal muscle
The gluteal muscles, often called glutes are a group of three muscles which make up the gluteal region commonly known as the buttocks: the gluteus maximus muscle, gluteus maximus, gluteus medius muscle, gluteus medius and gluteus minimus 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
Peak-to-trough ratio (PTR), also known as peak-to-trough variation or peak-to-trough fluctuation, is a parameter in pharmacokinetics which is defined as the ratio of Cmax (peak) concentration and Cmin (trough) concentration over a dosing inter ...
of paliperidone palmitate at
steady state
In systems theory, a system or a Process theory, 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 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 gr ...
s than the 1-month formulation and this allows for its longer
duration
Duration may refer to:
* The amount of time elapsed between two events
* Duration (music) – an amount of time or a particular time interval, often cited as one of the fundamental aspects of music
* Duration (philosophy) – a theory of time and ...
.
No
pharmacokinetic
Pharmacokinetics (from Ancient Greek ''pharmakon'' "drug" and ''kinetikos'' "moving, putting in motion"; see chemical kinetics), sometimes abbreviated as PK, is a branch of pharmacology dedicated to determining the fate of substances administered ...
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
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