Aripen® 10 mg Tablet: Each tablet contains Aripiprazole INN 10 mg.
Aripen® 15 mg Tablet: Each tablet contains Aripiprazole INN 15 mg.
Indications: Aripiprazole is indicated for the treatment of schizophrenia, schizoaffective disorder, acute manic and mixed episodes associated with bipolar I disorder.
Aripiprazole (Aripen ) is an atypical antipsychotic drug that exhibits high affinity for dopamine D2 and Dg, serotonin and 5-HT5, receptors, moderate affinity for dopamine D4, serotonin 5-HT,, and and histamine Hi receptors and moderate affinity for the serotonin reuptake site. Aripiprazole has no appreciable affinity for cholinergic muscarinic receptors.
Mode of action:
The mechanism of action of Aripiprazole (Aripen ) as with other drugs having efficacy in schizophrenia, is unknown. However, it has been proposed that the activity of aripiprazole in schizophrenia is mediated through a combination of partial agonist activity at D2 and 5-HT,, receptors and antagonist activity at receptors. This is associated with improvement of depressive, cognitive and negative symptoms.
Pharmacokinetics:
Aripiprazole (Aripen ) is well absorbed, with peak plasma concentrations occurring within 3-5 hours after dosing. Aripiprazole undergoes minimal pre-systemic metabolism. The absolute oral bioavailability of the tablet formulation is 87%. There is no effect of a high fat meal on the pharmacokinetics of aripiprazole. Aripiprazole is widely distributed throughout the body with an apparent volume of distribution of 4.9 L/kg, indicating extensive extravascular distribution. At therapeutic concentrations, aripiprazole and dehydro-aripiprazole are greater than 99% bound to serum proteins, binding primarily to Aripiprazole is extensively metabolised by the liver primarily by three biotransformation pathways: dehydrogenation, hydroxylation and N-dealkylation. The mean elimination half-life for aripiprazole is approximately 75 hours.
Aripiprazole is indicated for the treatment of schizophrenia, schizoaffective disorder, acute manic and mixed episodes associated with bipolar I disorder.
Caution should be exercised when aripiprazole is taken in combination with centrally acting drugs and alcohol. Carbamazepine could cause an increase in aripiprazole clearance and lower blood levels. Ketoconazole, quinidine, fluoxetine or paroxetine can inhibit aripiprazole elimination and cause increased blood levels.
Overdosage: The reported sign and symptoms with aripiprazole overdose are nausea, vomiting, asthenia, diarrhoea and somnolence. specific information is available on the treatment of overdose with aripiprazole. An electrocardiogram should be obtained in case of over dosage and, if QTc interval prolongation present, cardiac monitoring should be instituted. Otherwise, management of overdose should concentrate on supportive therapy, maintaining an adequate airway, oxygenation and ventilation, and management of symptoms. Close medical supervision and monitoring should continue until the patient recovers.
Pregnancy: * No information is available. It should be used only if potential benefit outweighs risk.
Lactation: * Aripiprazole is distributed into milk in rats. It is not known whether aripiprazole is distributed into milk in humans. Women who receives aripiprazole should not breast-feed.
Aripiprazole should be used with caution in patients with known cardiovascular or cerebrovascular disease and/or conditions with history of seizure and/or conditions that would predispose patients to hypotension (e.g. dehydration, hypovolemia, concomitant antihypertensive therapy). Aripiprazole should be used with caution when administered in patients exposed to conditions that may contribute to an elevation in core body temperature (e.g., dehydration, extreme heat, strenuous exercise, concomitant use of anticholinergic agents), in patients at risk for aspiration pneumonia, in patient with neuroleptic malignant syndrome and tardive dyskinesia.
Store in a cool and dry place, protected from light.