ABILIFY MAINTENA POWDER, SOLVENT FOR PROLONGED RELEASE SUSPENSION FOR INJECTION 400mg

Aripiprazole

Source of information: Drugbank (External Link). Last updated on: 3rd July 18
*Trade Name used in the content below may not be the same as the HSA-registered product.

Active Ingredient / Synonyms

Abilitat | Aripiprazol | Aripiprazole | Aripiprazolum | OPC 31 | Aripiprazole |

Description

Aripiprazole is an atypical antipsychotic medication used for the treatment of schizophrenia. It has also recently received FDA approval for the treatment of acute manic and mixed episodes associated with bipolar disorder. Aripiprazole appears to mediate its antipsychotic effects primarily by partial agonism at the D2 receptor. In addition to partial agonist activity at the D2 receptor, aripiprazole is also a partial agonist at the 5-HT1A receptor, and like the other atypical antipsychotics, aripiprazole displays an antagonist profile at the 5-HT2A receptor. Aripiprazole has moderate affinity for histamine and alpha adrenergic receptors, and no appreciable affinity for cholinergic muscarinic receptors.

Indication

For the treatment of schizophrenia and related psychotic disorders.

Mechanism of Action

Aripiprazole's antipsychotic activity is likely due to a combination of antagonism at D2 receptors in the mesolimbic pathway and 5HT2A receptors in the frontal cortex. Antagonism at D2 receptors relieves positive symptoms while antagonism at 5HT2A receptors relieves negative symptoms of schizophrenia.

Pharmacodynamics

Aripiprazole is a psychotropic agent belonging to the chemical class of benzisoxazole derivatives and is indicated for the treatment of schizophrenia. Aripiprazole is a selective monoaminergic antagonist with high affinity for the serotonin Type 2 (5HT2), dopamine Type 2 (D2), 1 and 2 adrenergic, and H1 histaminergic receptors. Aripiprazole acts as an antagonist at other receptors, but with lower potency. Antagonism at receptors other than dopamine and 5HT2 with similar receptor affinities may explain some of the other therapeutic and side effects of Aripiprazole. Aripiprazole's antagonism of histamine H1 receptors may explain the somnolence observed with this drug. Aripiprazole's antagonism of adrenergic a1 receptors may explain the orthostatic hypotension observed with this drug.

Pharmacokinetics

Absorption:

Not Available

Distribution:

* 4.9 L/kg

Metabolism:

Hepatic.

Elimination:

Less than 1% of unchanged aripiprazole was excreted in the urine and approximately 18% of the oral dose was recovered unchanged in the feces.

Half-life

75-146 hours

Clearance

Not Available

Toxicity

Not Available

References

  1. Health Science Authority of Singapore - Reclassified POM
  2. Drugbank

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Approval Information

ABILIFY MAINTENA POWDER AND SOLVENT FOR PROLONGED RELEASE SUSPENSION FOR INJECTION 400MG was registered with Health Science Authority of Singapore by LUNDBECK SINGAPORE PTE LTD. It is marketed with the registration number of SIN15192P with effective from 2017-03-14.

This product contains 400mg/vial of Aripiprazole in the form of INJECTION, POWDER, FOR SUSPENSION, EXTENDED-RELEASE.

The medicine was manufactured by Otsuka Pharmaceutical Co.Ltd in JAPAN, and Hameln Pharmaceuticals GmbH (Water for Injection) in GERMANY

It is a Presciption Only Medicine which can only be obtained from a doctor or a dentist, or from a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Anatomical Therapeutic Chemical (ATC) Classification

ATC Code: N05AX12

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