Index of drugs

Treatment of schizophrenia in adults and adolescents aged ≥15 years. Treatment of moderate to severe manic episodes in the course of bipolar I disorder and the prevention of new manic episodes in adults with predominantly manic episodes who respond to aripiprazole treatment. Treatment of moderate to severe manic episodes in the course of bipolar I disorder in adolescents aged ≥13 years, for up to 12 weeks of treatment.

1 tabl contains either 10 mg or 15 mg of aripiprazole; drug contains lactose.

An antipsychotic drug. It has high affinity for Dopamine D receptors₂ and D₃serotonin 5HT_1a and 5HT_2a and moderate affinity for dopamine D receptors₄serotonin 5HT_2c and 5HT₇as well as adrenergic α₁ and histamine H₁. Aripiprazole also shows moderate affinity for serotonin reuptake sites, but does not have significant affinity for muscarinic receptors. Clinical efficacy of the drug associated with a combined partly agonistic action on the dopamine D receptor₂ and serotonin 5HT_1a and antagonistic to the serotonin 5HT receptor_2a. Aripiprazole is well absorbed from the digestive tract (bioavailability 87%), it reaches C_max during 3-5 h. In over 99% it is associated with proteins, mainly albumin. It is extensively metabolised in the liver (dehydrogenation, hydroxylation and N-dealkylation); CYP3A4 and CYP2D6 enzymes are involved in metabolism. It is excreted in urine (27%) and faeces (60%), mainly in the form of metabolites. T_0,5 aripiprazole in the elimination phase is about 75 h in people with increased CYP2D6 activity and about 146 h in people with decreased CYP2D6 activity.

Hypersensitivity to aripiprazole or to any of the excipients.

When using antipsychotics, improvement of the clinical condition may occur after a few days or weeks; during this time the patient should be carefully monitored, including for the occurrence of suicidal thoughts and behaviors. The antipsychotic treatment of high-risk patients should be strictly supervised. The drug is not indicated for the treatment of dementia-related psychosis; in elderly patients with psychosis associated with Alzheimer's disease treated with aripiprazole, increased mortality and an increased incidence of cerebrovascular accidents were observed. Use with caution in patients with cardiovascular disease (myocardial infarction or ischemic disease, history of heart failure or conduction abnormalities), cerebrovascular disease, states predisposed to hypotension (dehydration, reduction of circulating blood volume and antihypertensive therapy) or hypertension, including progressive or malicious; with a family history of QT prolongation; with a history of seizures or diseases that may predispose to convulsions; with diabetes or risk factors for the development of diabetes (regularly control glycaemia); with significant risk factors for the development of obesity (eg diabetes, thyroid disorders or pituitary adenoma); with the risk of aspiration pneumonia. All possible risk factors for venous thromboembolism should be identified and appropriate preventive measures should be taken before initiating aripiprazole and during treatment. Patients who were previously addicted to gambling may be at greater risk of this side effect and should be closely monitored. All patients treated with aripiprazole should be monitored for symptoms of hyperglycaemia such as excessive thirst, polyuria, excessive appetite and weakness. In adolescents, weight gain should be monitored; if it is clinically significant, a dose reduction should be considered.The safety data for the concomitant administration of aripiprazole and the stimulants used to treat ADHD are very limited - extreme caution should be exercised when administering these drugs simultaneously. If you have symptoms of a neuroleptic malignant syndrome (NMS) or a high fever with an unexplained reason, all other antipsychotics, including aripiprazole, should be discontinued without other clinical symptoms of RH. If tardive dyskinesia occurs, consideration should be given to reducing the dose or stopping treatment with aripiprazole. In the presence of other extrapyramidal disorders, reduction of aripiprazole dose and introduction of close clinical control should be considered. Due to the lactose content, the drug should not be used in patients with inherited galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.

Do not use during pregnancy unless the expected benefit clearly outweighs the risk to the fetus (congenital malformations have been reported, however, causal association with aripiprazole could not be established, the potential for toxic effects of aripiprazole on the fetus can not be excluded). In neonates exposed in the third trimester of pregnancy to the action of antipsychotics (including aripiprazole), side effects of varying severity and time of onset, including extrapyramidal syndrome and / or withdrawal syndrome may occur; have been described as agitation, hypertension, hypotonia, tremor, drowsiness, breathing disorders, and sucking disorders - newborns should be carefully observed. Aripiprazole is excreted in human milk - do not breast-feed while taking the medicine.

Common: anxiety (especially motor), insomnia, anxiety, extrapyramidal disorder, akathisia, tremor, dizziness, drowsiness, sedation, headache, blurred vision, indigestion, vomiting, nausea, constipation, increased salivation, fatigue. Uncommon: depression, hypersexuality, diplopia, tachycardia, orthostatic hypotension. Not known (post-marketing observations of aripiprazole): leucopenia, neutropenia, thrombocytopenia, allergic reactions (eg pruritus, urticaria, anaphylactic reaction, angioedema - including swelling of the tongue, swelling of the tongue, swelling of the face), hyperglycemia, diabetes, ketoacidosis in the course of diabetes mellitus, diabetic coma, weight gain, weight loss, anorexia, hyponatraemia, excessive agitation, nervousness, pathological gambling addiction, suicide attempts, suicidal thoughts and suicides, speech disorders, neuroleptic malignant syndrome, grand mal convulsions, serotonin syndrome, QT prolongation, ventricular arrhythmias, sudden unexplained death, cardiac arrest,torsades de pointes, bradycardia, fainting, hypertension, venous thromboembolism (including pulmonary embolism and deep vein thrombosis), oropharyngeal spasm, laryngeal spasm, aspiration pneumonia, pancreatitis, dysphagia, abdominal discomfort, stomach discomfort , diarrhea, hepatic failure, jaundice, hepatitis, increased ALT, AST, GGTP, ALP, rash, photoallergic reactions, alopecia, hyperhidrosis, rhabdomyolysis, muscle pain, stiffness, incontinence, urinary retention, neonatal withdrawal syndrome, priapism, disorders of the body temperature regulation (eg hypothermia, fever), chest pain, peripheral edema, increased CPK activity, increased blood Glucose, fluctuations in blood glucose, increased glycosylated hemoglobin. There may be dystonia, tardive dyskinesia, side effects on the cerebral circulation and increased mortality in elderly patients with dementia. The drug causes both increases and decreases in the concentration of prolactin in the blood.Children and youth: Schizophrenia in adolescents ≥15 years of age - the incidence and type of adverse reactions were similar to those seen in adults, except for the following, which were reported more frequently: somnolence, sedation and extrapyramidal disorders (very common); dry mouth, increased appetite, orthostatic hypotension (often); low levels of prolactin in the blood were also observed.Manic episodes in bipolar I disorder in adolescents aged ≥13 years - the incidence and type of adverse reactions were similar to those seen in adults, except for the following: drowsiness, extrapyramidal disorder, akathisia, fatigue (very common); upper abdominal pain, increased heart rate, weight gain, increased appetite, muscle tremor, dyskinesia (common); low levels of prolactin in the blood and weight gain were also observed.

Orally.Adults. Schizophrenia. Starting dose: 10 or 15 mg / day; Maintenance dose: 15 mg / day. Aripiprazole is effective at doses of 10-30 mg / day. No higher efficacy of doses> 15 mg / day has been confirmed, however, a higher dose may be beneficial for individual patients. The maximum dose is 30 mg / day.Manic episodes in bipolar I disorder. Starting dose: 15 mg / day, as monotherapy or combination therapy. Some patients may benefit from a higher dose. The maximum dose is 30 mg / day.Prevention of relapse of manic episodes in bipolar I disorder. For patients who use aripiprazole alone or in combination therapy, the treatment should be continued at a fixed dose. Adjusting the daily dose, including its reduction, should be considered based on the clinical condition.Children and youth. Schizophrenia in adolescents aged ≥15 years. Initially 2 mg / day for 2 days, then 5 mg / day for the Next 2 days, until reaching the recommended target dose - 10 mg / day. In cases where the dose increase is appropriate, further doses should be given at once increased by 5 mg, not exceeding the maximum daily dose of 30 mg. Aripiprazole is effective at doses of 10-30 mg / day. No higher efficacy of doses> 10 mg / day has been confirmed, however, a higher dose may be beneficial for individual patients. The drug is not recommended for use in children with schizophrenia <15 years of age (no sufficient data on safety and efficacy).Manic episodes in bipolar I disorder in adolescents aged ≥13 years. Initially 2 mg / day for 2 days, then 5 mg / day for the next 2 days, until reaching the recommended target dose - 10 mg / day. Treatment should be as short as possible to obtain symptom control; can not be longer than 12 weeks. Treatment efficacy at doses> 10 mg / day has not been demonstrated and a daily dose of 30 mg is associated with a significantly higher incidence of serious adverse events, including events associated with extrapyramidal symptoms, somnolence, fatigue and weight gain. For this reason, doses> 10 mg / day should be used only in exceptional cases and with strict clinical control. The drug is not recommended for use in children aged <13 years. The safety and efficacy of the preparation in the treatment of irritability associated with autistic disorders in children and adolescents <18 years has not yet been established; no recommendation on a dosage. The safety and efficacy of the preparation in the treatment of Tics associated with Tourette's syndrome in children and adolescents aged 6-18 have not yet been established; no recommendation on a dosage.Special groups of patients. No dose adjustment is required based on sex, in smokers, in patients with impaired renal function, or in patients with mild or moderate hepatic impairment. In patients with severe hepatic impairment, the dose should be carefully adjusted and the highest daily dose - 30 mg should be used with extreme caution. In elderly patients, a lower starting dose should be considered if clinical circumstances allow it. The dose of aripiprazole should be reduced if a strong CYP3A4 or CYP2D6 inhibitor is co-administered, but increased when co-administered with a strong CYP3A4 inducer (see interactions).Way of giving. The drug should be administered once a day at a constant time; can be taken regardless of meals.