Aripiprazole

7 - {4 - [ 4 - (2,3 -dichlorophenyl) piperazin-1 -yl] - butoxy } -3,4- dihydro-1H- quinolin- 2-one

N05AX12

Antipsychotic

From 139.0 to 139.5 ° C

Template: Infobox chemical / molecular formula search available

Aripiprazole is a drug from the group of atypical antipsychotic indicated for the treatment of schizophrenia and for the treatment of moderate to severe manic episodes in Bipolar I Disorder and for the prevention of new manic episodes. Under the brand name Abilify ® was approved in 2004 in the form of tablets, orodispersible tablets, solution for injection and oral solution across Europe. Holder is Ōtsuka Pharmaceutical Co., Ltd.. , Production and distribution is carried out by Bristol -Myers Squibb, from protection reasons there until April 2015 no generic.

Properties

While previous atypicals act as full antagonists at the dopamine D2 receptor, aripiprazole acts as a partial agonist at the dopamine D2 receptor and the 5 -HT1A receptor. To aripiprazole acts as the other atypical antipsychotics 5-HT2A receptor antagonist as full.

The agonistic effect exploited with relative lack of dopamine in the CNS: The approximately 30% agonism should, for example, come in the frontal brain to bear.

With increased neurotransmission, as it is assumed for schizophrenia (current thesis: oversupply of dopamine in the limbic system, including for the development of emotion competence ), one uses the antagonistic effect, including blockade of D2 receptors ( " dopamine hypothesis ").

Aripiprazole is known due to its partial agonism as a representative of the third generation neuroleptics. In the next three to five years or more of these partial agonists / antagonists are being admitted in Germany (2006 ).

Clinical Effects

Despite the novel mechanism of action of aripiprazole in schizophrenia affects not better than previous neuroleptics, and few data from clinical trials are assessing the public accessible.

Adverse effects

The adverse effects include extrapyramidal motor disorders, however, only half as likely to occur as under haloperidol treatment. The incidence of tardive dyskinesia can be typically assess only some years after launch, one assumes, however, that the risk is as low as with other atypicals.

In individual cases have been reported of an exacerbation of psychotic symptoms. This interference effect is also associated with a particular mechanism of action of aripiprazole.

In addition, the following adverse reactions may occur:

  • Hyperhidrosis
  • Blepharospasm
  • Headache
  • Agitation
  • Anxiety
  • Sleep
  • Indigestion, constipation, nausea and vomiting
  • Dizziness, drowsiness, impaired responsiveness
  • Akathisia
  • Hypersexuality → Individual case reports
  • Depression
  • Hypomania
  • Orthostatic hypotension ( postural hypotension ) → very rare
  • Neuroleptic Malignant Syndrome
  • → fatigue common side effect
  • Weakness → common side effect

In elderly patients with dementia aripiprazole leads to increased mortality; therefore it should not be prescribed for these patients.

CAS registry number PubChem Anatomical Therapeutic Chemical Classification System DrugBank Active ingredient Bristol-Myers Squibb Partialagonist 5-HT receptor Dopamine hypothesis of schizophrenia Psychosis Psychomotor agitation Major depressive disorder Digital Object Identifier PubMed Central
24269
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