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Paliperidone

Trade name Invega.

A dopamine antagonist and 5-HT2A antagonist of the atypical antipsychotic class of medications.

An extended release formulation of paliperidone that uses an extended release system to allow for once-daily dosing.

US: C-Risk not ruled out in pregnancy.

Routes of administration oral and IM depot injection.

Bioavailability 28% by mouth.

Biological half-life 23 hours orally.

Long-acting injectable formulation of paliperidone palmitoyl ester indicated for once-every 28 days injection after an initial titration period.

Used to treat mania and at lower doses as maintenance for bipolar disorder.

Also indicated for schizophrenia and schizoaffective disorder.

It is used for the treatment of schizophrenia and schizoaffective disorder.

Side effects include:

Headache

Tachycardia

Somnolence

Hyperprolactinaemia

Cough

Extrapyramidal side effects

Orthostatic hypotension

Weight gain

QT interval prolongation

Nasopharyngitis

Anxiety

Indigestion

Constipation

Death

The primary active metabolite of the older antipsychotic risperidone.

Paliperidone has antagonist effect at α1 and α2 adrenergic receptors and at H1 histamine receptors.[17] It does not bind to muscarinic acetylcholine receptors. In addition, it blocks dopamine and serotonin receptors.

Paliperidone has less affinity for D4 receptors than risperidone.

Food increases the absorption.

Food increases exposure of the drug by up to 50-60%, however, half-life is not significantly affected.

The half life is 24 hours.

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