Aripiprazole is an atypical antipsychotic drug derived from quinolinone. This drug partially binds to the Dopamine D2 and serotonin 5-HT1A receptor and stimulates the transmission of specific signals through them - it is an agonist. The efficacy of aripiprazole in the treatment of schizophrenia is related to this mechanism of action. Aripiprazole, on the other hand, blocks 5-HT2A receptors, it is its antagonist.In vitro the drug binds to the dopamine D2 and D3 receptors, serotonin 5HT1a and 5HT2a (to a large extent), to the D4, 5HT2c and 5HT7 receptors (to a moderate extent), as well as the a1-adrenergic and histamine H1 receptors (for more information see description antipsychotic drugs).
Oral use of aripiprazole is indicated for the treatment of schizophrenia in adults and children over the age of 15, in the treatment of moderate to severe manic episodes in bipolar I disorder, in the prevention of new manic episodes in patients who respond to aripiprazole treatment and who have there are mainly manic episodes. The intramuscular drug is used to quickly control anxiety and behavioral disorders in patients with schizophrenia or manic episodes in bipolar I disorder when oral treatment is not adequate.
The drug is used orally, once a day, regardless of meals (at a fixed time) and intramuscular. The drug in the form of intramuscular injections should be used for a short time. If longer treatment is indicated, the oral form should be started as soon as possible. Special care should be taken when driving vehicles and operating machinery while it is still known that aripiprazole does not adversely affect the patient.
Aripiprazole after oral administration is well absorbed from the gastrointestinal tract and reaches a maximum serum concentration 3-5 h after administration. The maximum concentration after intramuscular administration is achieved 1-3 h after administration. The oral bioavailability is 87% and after intramuscular administration 100%. Aripiprazole undergoes changes in the liver, e.g. to the active metabolite - dehydro-aripiprazole. 60% of the dose is excreted in the faeces, 27% - in the urine. Approx. 18% of the dose is excreted as unchanged aripiprazole in the faeces and less than 1% in the urine.
More information - see descriptions of preparations