Invega Sustenna

Invega Sustenna is an atypical antipsychotic indicated for
Treatment of schizophrenia in adults.
Treatment of schizoaffective disorder in adults as monotherapy and as an adjunct to mood stabilizers or antidepressants.

The most common adverse reactions (incidence ≥ 5% and occurring at least twice as often as placebo) were injection site reactions, somnolence/sedation, dizziness, akathisia, and extrapyramidal disorder.

Cerebrovascular Adverse Reactions, Including Stroke, in Elderly Patients with Dementia-Related Psychosis
: Increased incidence of cerebrovascular adverse reactions (e.g. stroke, transient ischemic attack).
Neuroleptic Malignant Syndrome
: Manage with immediate discontinuation of drug and close monitoring.
QT Prolongation
: Avoid use with drugs that also increase QT interval and in patients with risk factors for prolonged QT interval.
Tardive Dyskinesia
: Discontinue drug if clinically appropriate.
Metabolic Changes
: Monitor for hyperglycemia/diabetes mellitus, dyslipidemia and weight gain.
Orthostatic Hypotension and Syncope
: Monitor heart rate and blood pressure and warn patients with known cardiovascular or cerebrovascular disease, and risk of dehydration or syncope.
Leukopenia, Neutropenia, and Agranulocytosis
: Perform complete blood counts (CBC) in patients with pre-existing low white blood cell count (WBC) or history of leukopenia or neutropenia. Consider discontinuing Invega Sustenna if clinically significant decline in WBC in the absence of other causative factors.
Hyperprolactinemia
: Prolactin elevations occur and persist during chronic administration.
Potential for Cognitive and Motor Impairment
: Use caution when operating machinery.
Seizures
: Use cautiously in patients with a history of seizures or with conditions that lower the seizure threshold.

Paliperidone palmitate is hydrolyzed to paliperidone. Paliperidone is the major active metabolite of risperidone. The mechanism of action of paliperidone is unclear. However, the drug’s therapeutic effect in schizophrenia could be mediated through a combination of central dopamine Type 2 (D2 ) and serotonin Type 2 (5HT 2A ) receptor antagonism.
In vitro, paliperidone acts as an antagonist at the central dopamine Type 2 (D2) and serotonin Type 2 (5HT 2A) receptors with binding affinities (Ki values) of 1.6-2.8 nM for D 2 and 0.8-1.2 nM for 5HT 2A receptors. Paliperidone is also active as an antagonist at the α 1 and α 2 adrenergic receptors and H 1 histaminergic receptors, which may explain some of the other effects of the drug. Paliperidone has no affinity for cholinergic muscarinic or β1 and β2-adrenergic receptors. The pharmacological activity of the (+)- and (-)- paliperidone enantiomers is qualitatively and quantitatively similar in vitro.