PHARMACOLOGY

PHARMCODYNAMICS  

Aripiprazole is a psychotropic agent belonging to the chemical class of benzisoxazole derivatives and is indicated for the treatment of schizophrenia. Anti-psychotic drugs are called Neuroleptics or major tranquillizers used primarily to treat Schizophrenia but are also effective in other psychotic states like Manic State Psychotic  Symptoms. Pharamcodynamics. 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.

PHARMACOKINETIC PROFILE

ABSORPTION :Aripiprazole is well absorbed after administration of the tablet, with peak plasma concentrations occurring within 3 hours to 5 hours; the absolute oral bioavailability of the tablet formulation is 87%. ARIPRO can be administered with or without food.

DISTRIBUTION :The steady-state volume of distribution of aripiprazole following intravenous administration is high (404 L or 4.9 L/kg), indicating extensive extravascular distribution. At therapeutic concentrations, aripiprazole and its major metabolite are greater than 99% bound to serum proteins, primarily to albumin.

METABOLISM AND ELIMINATION : Aripiprazole is metabolized primarily by three biotransformation pathways: dehydrogenation, hydroxylation, and N-dealkylation. Based on in vitro studies, CYP3A4 and CYP2D6 enzymes are responsible for dehydrogenation and hydroxylation of aripiprazole, and N-dealkylation is catalyzed by CYP3A4. Aripiprazole is the predominant drug moiety in the systemic circulation. At steady-state, dehydroaripiprazole, the active metabolite, represents about 40% of aripiprazole AUC in plasma. 

Following a single oral dose of aripiprazole, approximately 25% and 55% of the administered radioactivity was recovered in the urine and feces, respectively. Less than 1% of unchanged aripiprazole was excreted in the urine and approximately 18% of the oral dose was recovered unchanged in the feces.

INDICATIONS

Schizophrenia, Acute Treatment of Manic and Mixed Episodes associated with Bipolar I Disorder, Bipolar Disorder in Pediatric patients ( 13 to 17 years), Adjunctive Treatment of Major Depressive Disorder,   Irritability Associated with Autistic Disorder,  Treatment of Tourette’s disorder.

 DOSAGE 

OD at Bed time with or without food. If you miss a dose of ARIPRO , take the missed dose as soon as you remember. If it is almost time for the next dose, just skip the missed dose and take your next dose at the regular. time.Maximum dose is  30 mg / Day.

COMMON SIDE EFFECTS 

  Dizziness, Nausea   Anxiety, Vomiting , Insomnia Constipation  Restlessness,  Headache . Do not take ARIPRO if you are  allergic to Aripiprazole or any of the ingredients in ARIPRO. 

PREGNANCY CATEGORY :  C

PRESENTATION 

ARIPRO-10 : Each Box contains 
5 catch covers with 3 strips of 10 Tablets 

ARIPRO -15 : Each Box contains 
5 catch covers with 3 strips of 10 Tablets