| Indication |
For the treatment of schizophrenia and related psychotic disorders. |
| 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. |
| 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. |
| Absorption |
Not Available |
| Volume of distribution |
|
| Protein binding |
>99% |
| Metabolism |
Hepatic. |
| Route of 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 |
