Zylaxera, 10mg pills, 28pcs

Composition

1 tablet 5 mg / 10 mg / 15 mg / 30 mg contains:

Active ingredient:

Aripiprazole fumarate semi-finished granules 74.25 mg / 148.50 mg / 222.75 mg/445.50 mg

[Active ingredient of semi-finished product-granules:

Aripiprazole fumarate (in the form of aripiprazole hemifumarate) 5,647 mg/11,293 mg/16,940 mg/33,880 mg, equivalent to aripiprazole 5 mg/10 mg/15 mg/30 mg

Excipients semi-granules: lactose monohydrate, corn starch, microcrystalline cellulose, hyprolose, a blue dye – [dye patented blue (E131), dye black diamond (E 151)] (for tablets 5 mg), dye iron oxide yellow (E 172) (for tablets 15 mg), dye iron oxide red (E 172) (for tablets of 10 mg and 30 mg)]

Auxiliary substances: magnesium stearate

Pharmacological action

antipsychotic agent (neuroleptic)

Clinical pharmacology

It is assumed that the therapeutic effect of aripiprazole in schizophrenia and type I bipolar disorder is due to a combination of partial agonistic activity against_D2-dopamine and_5HT1A-serotonin receptors and antagonistic activity against 5HT2A-serotonin receptors.

Pharmacodynamics

Aripiprazole has high affinity in vitro for_D2-andD3-dopamine receptors,5HT_1a– and 5HT_2a-serotonin receptors, and moderate affinity for_D4-dopamine,5HT_2c-and 5HT₇-serotonin, alpha_-1-adrenergic_{receptors, and H1}-histamine receptors. Aripiprazole is also characterized by moderate affinity for serotonin reuptake sites and lack of affinity for muscarinic cholinergic receptors. Aripiprazole in animal experiments showed antagonism with respect to dopaminergic hyperactivity and agonism with respect to dopaminergic hypoactivity. Some of the clinical effects of aripiprazole can be attributed to interactions with other receptors besides dopamine and serotonin.

Oral use of aripiprazole in doses from 0.5 mg to 30 mg once a day in healthy volunteers for 2 weeks leads to a dose-dependent decrease in binding of 11C-racloprid, a ligand_{of D2/}D3-dopamine receptors, to the caudate nucleus and fence (according to positron emission tomography).

Pharmacokinetics

The activity of Zilaxera is mainly due to the presence of aripiprazole. The average elimination half-life (T_1/2) of aripiprazole is approximately 75 hours. The equilibrium concentration is reached after 14 days. Accumulation of aripiprazole with repeated use is predictable. The pharmacokinetics of aripiprazole at steady state are dose-proportional. There were no diurnal fluctuations in the distribution of aripiprazole and its metabolite, dehydroaripiprazole. It was found that the main metabolite of the drug in human blood plasma, dehydroaripiprazole, has the same affinity for_D2-dopamine receptors as aripiprazole.

Suction

Aripiprazole is rapidly absorbed after oral use of Zilaxera tablets, and the maximum concentration (with_max) of aripiprazole in blood plasma is reached after 3-5 hours. Oral bioavailability of Zilaxera tablets is 87%. Food intake does not affect the bioavailability of aripiprazole.

Distribution

Aripiprazole is well distributed in tissues, with an apparent volume of distribution of 4.9 l / kg, which indicates an intense extravascular distribution. At a therapeutic concentration of more than 99% of aripiprazole binds to serum proteins, mainly albumin.

Metabolism

Aripiprazole undergoes only minimal presystemic metabolism. Aripiprazole is metabolized in the liver in three ways: dehydrogenation, hydroxylation, and N-dealkylation. According to the study, in vitro dehydrogenation and hydroxylation of aripiprazole occurs under the action of CYP3A4 and CYP2D6 isoenzymes, and N-dealkylation is catalyzed by the CYP3A4 isoenzyme. Aripiprazole is the main component of the drug in the blood plasma. At steady state, the area under the concentration-time curve (AUC) of dehydroaripiprazole, the active metabolite, is approximately 40% of the AUC of aripiprazole in blood plasma.

Deduction

The average T_1/2 of aripiprazole is about 75 hours in patients with high activity of the CYP2D6 isoenzyme and 146 hours in patients with low activity. After a single oral dose of labeled [14C] aripiprazole, approximately 27% and 60% of radioactivity is detected in the urine and feces, respectively. Less than 1% of unchanged aripiprazole is detected in the urine and approximately 18% of the dose taken unchanged is excreted through the intestine with bile. The total clearance of aripiprazole is 0.7 ml / min / kg, mainly due to hepatic excretion.

Pharmacokinetics in special patient groups

Older patients

There were no age-related differences in the pharmacokinetics of aripiprazole in adult patients with schizophrenia, as well as in healthy volunteers.

Gender specific feature

There were no gender-related differences in the pharmacokinetics of aripiprazole in adult patients with schizophrenia, as well as in healthy volunteers.

Racial background

There were no clinically significant differences in the pharmacokinetics of aripiprazole depending on race.

Smoking

Smoking does not affect the pharmacokinetics of aripiprazole.

Impaired renal function

The pharmacokinetic parameters of aripiprazole and dehydroaripiprazole in patients with severe kidney disease do not differ from those in healthy volunteers.

Impaired liver function

After a single dose of aripiprazole in patients with varying degrees of cirrhosis, there was no significant effect of impaired liver function on the pharmacokinetics of aripiprazole and dehydroaripiprazole. However, the study involved only 3 patients with decompensated cirrhosis of the liver (Child-Pugh class C), and therefore it is impossible to draw definitive conclusions about the metabolic activity of the liver in patients with decompensated cirrhosis of the liver.

Indications

* Schizophrenia: acute attacks and maintenance therapy.

* Type I bipolar disorder: manic episodes and maintenance therapy to prevent relapse in patients with type I bipolar disorder who have recently had a manic or mixed episode.

* Adjunct therapy with lithium or valproic acid to treat manic or mixed episodes in the context of type I bipolar disorder, with or without psychotic symptoms, and maintenance therapy to prevent relapse in patients with type I bipolar disorder.

* An adjunct to antidepressant therapy for major depressive disorder.

Use during pregnancy and lactation

Pregnancy

No adequate and well-controlled studies have been conducted in pregnant women. It is not known whether the use of aripiprazole in a pregnant woman can have a harmful effect on the fetus or cause a violation of reproductive function. It is known that newborns whose mothers took antipsychotics during the third trimester of pregnancy are at risk of developing extrapyramidal disorders and/or withdrawal symptoms in the postpartum period. Newborns experienced agitation, muscle hypertension or hypotension, tremor, drowsiness, respiratory distress syndrome, and feeding disorders. These symptoms were of varying severity, sometimes they went away without treatment, while in other cases newborns needed intensive care and prolonged hospitalization. When using aripiprazole, the development of such symptoms in newborns was very rare.

Patients should be warned that they should immediately inform the doctor about the onset of pregnancy during treatment, and they should also inform the doctor about the planned pregnancy.

Zilaxera may be taken during pregnancy only if the potential benefit to the mother outweighs the potential risk to the fetus.

Breast-feeding period

Aripiprazole passes into breast milk. When using Zilaxera®, breast-feeding should be discontinued.

Contraindications

·  Hypersensitivity to aripiprazole or other components of the drug.

·  Age up to 18 years (efficacy and safety have not been established).

* Breast-feeding period.

* Lactase deficiency, lactose intolerance, glucose-galactose malabsorption syndrome (because Zilaxera contains lactose).

Interaction

Due to the alpha-1-adrenergic antagonism of aripiprazole, there is a possibility of enhancing the effect of some antihypertensive drugs.

Since aripiprazole has an effect on the central nervous system( CNS), you should be wary of taking alcohol or other drugs that affect the central nervous system at the same time, as this can lead to increased side effects, such as sedation. Caution should be exercised when using aripiprazole with medications that may cause prolongation of the QT interval or electrolyte imbalance.

Likelihood of other medications affecting aripiprazole

There was no clinically significant effect of the histamine_H2-receptor blocker famotidine, which causes inhibition of hydrochloric acid secretion in the stomach, on aripiprazole, despite a decrease in the rate of absorption of aripiprazole.

Various pathways of aripiprazole metabolism are known, including those involving the CYP2D6 and CYP3A4 isoenzymes, with the exception of the CYP1A isoenzyme. Therefore, no dose adjustment is required for smokers.

Quinidine and other inhibitors of the CYP2D6 isoenzyme

In studies in healthy volunteers, a potent inhibitor of the CYP2D6 isoenzyme (quinidine) increased the AUC of aripiprazole by 107%, while C_max remained unchanged. The AUC and_cmax of dehydroaripiprazole, the active metabolite, decreased by 32% and 47%, respectively. In this regard, it is necessary to reduce the dose of Zilaxer® approximately 2 times when it is used simultaneously with quinidine. Other potent inhibitors of the CYP2D6 isoenzyme, such as fluoxetine and paroxetine, may have similar effects, so a similar dose reduction is necessary.

Ketoconazole and other inhibitors of the CYP3A4 isoenzyme

In clinical trials in healthy volunteers, a potent inhibitor of the CYP3A4 isoenzyme (ketoconazole) increased the AUC and cmax of aripiprazole by 63% and 37%, respectively. AUC and_cmax of dehydroaripiprazole increased by 77% and 43%, respectively. In slow metabolizers of the CYP2D6 isoenzyme, the combined use of powerful inhibitors of the CYP3A4 isoenzyme can lead to an increase in plasma concentrations of aripiprazole compared to “fast” metabolizers of the CYP2D6 isoenzyme. If the combined use of ketoconazole and other potent inhibitors of the CYP3A4 isoenzyme and Zilaxer® is necessary, it is necessary to assess whether the risk of use does not exceed the possible benefit. When combined with ketoconazole, the prescribed dose of Zilaxer should be approximately halved. It is expected that other potent inhibitors of the CYP3A4 isoenzyme, such as itraconazole and HIV protease inhibitors, may have similar effects, therefore, in this case, a dose reduction is also recommended.

If a CYP2D6 or CYP3A4 inhibitor is discontinued, it is necessary to increase the dose of Zilaxer® to that used by the patient before prescribing concomitant therapy.

When using weak inhibitors of the CYP3A4 isoenzyme (for example, diltiazem or escitalopram) or CYP2D6 in combination with Zilaxer®, a slight increase in aripiprazole concentrations should be expected.

Carbamazepine and other inducers of the CYP3A4 isoenzyme

When combined with carbamazepine, a potent inducer of the CYP3A4 isoenzyme, the geometric mean values with_max and AUC of aripiprazole were 68% and 73% lower, respectively, compared with aripiprazole monotherapy at a dose of 30 mg. Geometric mean values with_max and AUC of dehydroaripiprazole when combined with carbamazepine decreased by 69% and 71%, respectively, compared with aripiprazole monotherapy. The dose of Zilaxer should be doubled when combined with carbamazepine. It can be expected that other potent inducers of the CYP3A4 isoenzyme (such as rifampicin, rifabutin, phenytoin, phenobarbital, primidone, efavirenz, nevirapine and St. John’s wort preparations) have similar effects, therefore, the exact same dose increase is recommended. When a powerful inducer of the CYP3A4 isoenzyme is discontinued, the dose of Zilaxer® should be reduced to the recommended level.

Valproate and Lithium

No clinically significant changes in aripiprazole concentrations were observed with the combined use of valproate or lithium.

Serotonin syndrome

Serotonin syndrome has been reported in patients taking aripiprazole. Possible manifestations of this condition are particularly common when used concomitantly with other serotonergic drugs, such as selective serotonin reuptake inhibitors (SSRIs) and selective serotonin and norepinephrine reuptake inhibitors (SSRIs), or drugs that may increase the concentration of aripiprazole (see section “Side effects”).

Probability of aripiprazole’s effect on other medications

In clinical studies of aripiprazole at a dose of 10-30 mg / day, there was no significant effect on the metabolism of substrates of the isoenzymes CYP2D6 (dextromethorphan/3-methoximorphinan ratio), CYP2C9 (warfarin), CYP2C19 (omeprazole) and CYP3A4 (dextromethorphan). In addition, aripiprazole and dehydroaripiprazole have not been shown to affect CYP1A2-mediated metabolism in vitro. Thus, it is unlikely that aripiprazole has a clinically significant effect on drugs metabolized by this isoenzyme.

Concomitant use of lithium, lamotrigine, or valproate with aripiprazole did not result in clinically significant changes in lithium, lamotrigine, or valproate concentrations.

How to take, course of use and dosage

of Schizophrenia

The recommended starting dose is 10 mg to 15 mg once a day, regardless of the meal time. The maintenance dose is usually 15 mg per day. Clinical studies have shown the effectiveness of the drug in doses from 10 mg to 30 mg per day.

Manic episodes in bipolar disorder

Monotherapy

The recommended starting dose is 15 mg once a day, regardless of the meal time. If necessary, the dose should be changed at intervals of at least 24 hours. In clinical studies for manic episodes, the effectiveness of the drug in doses of 15-30 mg / day when taken for 3-12 weeks has been demonstrated. The safety of doses above 30 mg / day has not been evaluated in clinical trials.

When monitoring patients with type I bipolar disorder who have had a manic or mixed episode, who have experienced stabilization of symptoms against the background of taking Zilaxera® (15 mg/day or 30 mg/day at an initial dose of 30 mg/day) for 6 weeks, then for 6 months and then for 17 months, a favorable effect of such maintenance therapy was established. Patients should be periodically evaluated to determine whether maintenance therapy should be continued.

Adjunct therapy with lithium or valproic acid for the treatment of manic or mixed episodes in type I bipolar disorder

The recommended starting dose is 10 mg to 15 mg once a day, and the maintenance dose is 15 mg / day. The dose can be increased to 30 mg / day depending on the clinical indications. When monitoring patients with type I bipolar disorder, a favorable effect of maintenance therapy with aripiprazole at a dose of 10 mg to 30 mg per day as an adjunct to therapy with lithium or valproic acid was established. Patients should be periodically evaluated to determine whether maintenance therapy should be continued.

Complementary therapy for major depressive disorder

As an adjunct to treatment with antidepressants, it is recommended to prescribe Zilaxera® at an initial dose of 5 mg per day, if necessary and well tolerated therapy, the daily dose of Zilaxera® can be increased weekly by 5 mg to a maximum of no more than 15 mg per day.

The duration of therapy with Zilaxera® for all the above indications has not been established, it is necessary to regularly examine the patient for the possibility of discontinuing therapy.

In patients with hepatic insufficiency, a dose of 30 mg is prescribed with caution.

Use in special patient groups

Patients with renal insufficiency

No dose adjustment is required when Zilaxer is prescribed to patients with renal insufficiency.

Patients with hepatic insufficiency

No dose adjustment is required for patients with hepatic insufficiency when Zilaxer is prescribed.

Use in patients over 65 years of age

No dose adjustment is usually required. However, due to hypersensitivity in patients in this population, the use of lower initial doses should be considered.

Influence of the patient’s gender on the dosage regimen

The dosage regimen of Zilaxer® is the same for patients of both sexes.

Effect of smoking on the dosage regimen

The dosage regimen of Zilaxera® for smokers and non-smokers is the same.

Dosage regimen for concomitant therapy

Concomitant use of Zylaxera and potent CYP3A4 inhibitors (ketoconazole, clarithromycin) should reduce the dose of Zylaxera by half.If CYP3A4 inhibitors are discontinued, the dose of Zilaxer should be increased.

Concomitant use of Zylaxera and potent inhibitors of the CYP2D6 isoenzyme (quinidine, fluoxetine, paroxetine) should reduce the dose of Zylaxera by at least half. When inhibitors of the CYP2D6 isoenzyme are discontinued, the dose of Zilaxer® should be increased.

Zilaxera should be used without changing the dosage regimen if it is prescribed as an adjunct therapy in patients with major depressive disorder.

When Zylaxera is co-administered with potent inhibitors of the CYP2D6 isoenzymes (quinidine, fluoxetine, paroxetine) and CYP3A4 (ketoconazole, clarithromycin), the dose of Zylaxera should be reduced by three-quarters (i. e. up to 25% of the usual dose). When inhibitors of the CYP2D6 and/or CYP3A4 isoenzymes are discontinued, the dose of Zilaxer® should be increased.

When Zylaxera is co-administered with potent, moderate or mild inhibitors of the CYP2D6 and CYP3A4 isoenzymes, the dose of Zylaxera may initially be reduced by three-quarters (i. e. up to 25% of the usual dose), and then increased to achieve an optimal clinical result.

When prescribing Zylaxera® to patients with low CYP2D6 isoenzyme activity, the initial dose of Zylaxera® should be reduced by half, and then increased to achieve an optimal clinical result. When Zylaxera® is co-administered with a potent inhibitor of the CYP3A4 isoenzyme in patients with low activity of the CYP2D6 isoenzyme, the dose of Zylaxera® should be reduced by ¾ (i. e., up to 25% of the usual dose).

When Zylaxera® is co-administered with potential inducers of the CYP3A4 isoenzyme (carbamazepine), the dose of Zylaxera® should be increased 2-fold. If the inducers of the CYP3A4 isoenzyme are discontinued, the dose of Zilaxer® should be reduced to 10-15 mg.

Overdose

Symptoms

Clinical studies and post-marketing observations have described accidental or intentional overdoses of aripiprazole in adult patients with a single dose of up to 1260 mg, not accompanied by a fatal outcome. Potentially clinically significant symptoms include lethargy, high blood pressure, drowsiness, tachycardia, nausea, vomiting, and diarrhea. Cases of overdose of aripiprazole in children (taking up to 195 mg), not accompanied by a fatal outcome, are described. Potentially clinically significant symptoms included: drowsiness, temporary loss of consciousness, and extrapyramidal symptoms.

Treatment

Maintenance and symptomatic therapy, airway patency, ventilation and oxygenation. You should take into account the need to prescribe several medications. To detect arrhythmias, you should immediately start monitoring the state of the cardiovascular system, including constant ECG monitoring. In cases of confirmed or suspected overdose with aripiprazole, careful monitoring is indicated until all symptoms disappear.

Activated carbon in a dose of 50 g, administered 1 h after taking aripiprazole, resulted in a decrease in AUC and cmax of aripiprazole by 51% and 41%, respectively, which indicates that activated carbon can be effective in the treatment of overdose.

Hemodialysis

Despite the lack of information on the effectiveness of hemodialysis in the treatment of overdose with aripiprazole, the effectiveness of hemodialysis is unlikely, since aripiprazole is largely bound to plasma proteins.

Description

5 mg tablets: capsule-shaped, slightly biconvex tablets, light blue in color with marbling and possible dark inclusions.

Tablets 10 mg: capsule-shaped, slightly biconvex tablets, pale pink in color with marbling and dark flecks.

Tablets 15 mg: round, slightly biconvex tablets with a chamfer, pale yellow color with marbling and possible dark inclusions.

Tablets 30 mg: round, slightly biconvex tablets with a chamfer, pale pink color with marbling and dark flecks.

Special instructions

Cardiovascular diseases (coronary heart disease [CHD] or previous myocardial infarction, chronic heart failure [CHF] or conduction disorders), cerebrovascular diseases, conditions predisposing to the development of arterial hypotension (dehydration, hypovolemia, use of antihypertensive drugs) due to the possibility of developing orthostatic hypotension, seizures or diseases that may cause seizures, an increased risk of hyperthermia (for example, intense physical activity use of m-holinoblockers, dehydration, because neuroleptics can disrupt thermoregulation), in patients with an increased risk of aspiration pneumonia due to the risk of developing impaired esophageal motor function and aspiration, obesity or diabetes mellitus in the family history, in patients with a high risk of suicide (psychotic diseases, bipolar disorders, major depressive disorder), in persons aged 18-24 years due to the risk of suicidal behavior.

Contraindicated in persons under 18 years of age (efficacy and safety have not been established).

Patients with renal insufficiency

No dose adjustment is required when Zilaxer is prescribed to patients with renal insufficiency.

Patients with hepatic insufficiency

No dose adjustment is required for patients with hepatic insufficiency when Zilaxer is prescribed.

Use in patients over 65 years of age

No dose adjustment is usually required. However, due to hypersensitivity in patients in this population, the use of lower initial doses should be considered.

When using antipsychotic drugs (neuroleptics), the therapeutic effect develops from several days to several weeks. During this period, it is necessary to monitor the patient’s condition.

Suicidal behavior

Suicidal behavior is often seen in psychotic disorders and mood disorders. In some cases, suicidal behavior occurs at the beginning of treatment or when changing an antipsychotic drug, including when using aripiprazole. Antipsychotic treatment in high-risk patients should be carried out under close supervision. Epidemiological studies have shown that there is no increased risk of suicidal behavior when using aripiprazole compared to other antipsychotics in adult patients with schizophrenia or bipolar disorder. There are insufficient data to assess the risk in younger patients (under 18 years of age), but it is known that the risk of suicide persists during the first 4 weeks of treatment with atypical antipsychotics, including aripiprazole.

Cardiovascular diseases

Aripiprazole should be used with caution in patients with diseases of the cardiovascular system (myocardial infarction or a history of coronary heart disease, heart failure, conduction disorders), cerebrovascular disorders, risk factors for hypotension (dehydration, hypovolemia, use of antihypertensive drugs) or arterial hypertension, including progressive and malignant.

When using antipsychotics, venous thrombosis may develop. Since patients receiving such drugs may have predisposing factors for venous thromboembolism, patients should be carefully evaluated before starting treatment with aripiprazole to identify all possible risk factors and take preventive measures during treatment.

Prolongation of the QT interval

In clinical trials, the incidence of QT prolongation in patients treated with aripiprazole was comparable to that in the placebo group. However, as with other antipsychotics, caution should be exercised when prescribing aripiprazole in patients with a family history of QT prolongation.

Tardive dyskinesia

In clinical trials lasting 1 year or less, infrequent cases of tardive dyskinesia were observed during treatment with aripiprazole. If the patient develops objective or subjective symptoms of tardive dyskinesia during treatment with Zilaxera®, a dose reduction or discontinuation of the drug is indicated. These symptoms may persist for a certain period of time or even worsen after treatment is discontinued.

Neuroleptic malignant syndrome

(NMS) is a potentially lethal complex of symptoms that develops with the use of antipsychotics. In clinical trials of aripiprazole, cases of NMS were rare. NMS is manifested by increased body temperature, muscle rigidity, mental disorders, and instability of the autonomic nervous system (instability of pulse and blood pressure, tachycardia, sweating, and arrhythmias). In addition, increased creatine phosphokinase activity, myoglobinuria (rhabdomyolysis) and acute renal failure may occur. However, increased creatine phosphokinase and rhabdomyolysis do not necessarily indicate the development of NMS.

If symptoms of NMS or unexplained fever occur without additional clinical manifestations of NMS, all antipsychotics, including Zilaxera, should be discontinued.

Convulsions

Seizures were infrequent in clinical trials of aripiprazole. Aripiprazole should be used with caution in patients with a history of convulsive disorders or in the presence of conditions leading to the development of convulsive seizures.

Elderly patients with psychosis on the background of dementia

Increased mortality

According to the results of three placebo-controlled studies, elderly patients (56-99 years, mean age 82.4 years) with Alzheimer’s-related psychoses had an increased risk of death with aripiprazole compared to the placebo group.

Mortality in the aripiprazole-treated group compared to the placebo group was 3.5% and 1.7%, respectively. Although the causes of death varied, most of them were cardiovascular (for example, heart failure, sudden cardiac death) or infectious (for example, pneumonia).

Cerebrovascular adverse reactions

In the same studies in patients (mean age: 84 years; age range: 78-88 years) the development of cerebrovascular adverse reactions (for example, stroke, transient ischemic attack), including those with fatal outcomes, was noted. Overall,1.3% of patients in the aripiprazole group experienced cerebrovascular adverse reactions, compared to 0.6% in the placebo group. The differences did not reach statistical significance. However, in one fixed-dose study, there was a statistically significant dose-dependent relationship between the frequency of cerebrovascular adverse reactions in patients in the aripiprazole group.

Zilaxera is not indicated for the treatment of psychosis in patients with dementia.

Hyperglycemia and diabetes mellitus

Hyperglycemia, in some cases severe and accompanied by ketoacidosis or hyperosmolar coma with a fatal outcome, was observed in patients taking atypical antipsychotics. Risk factors such as obesity and a hereditary history of diabetes may have contributed to the development of severe complications. There were no significant differences in the incidence of hyperglycemic adverse reactions (including diabetes mellitus)in clinical trials of aripiprazole or hyperglycemia compared to placebo. Based on the available data, it is impossible to directly compare the frequency of hyperglycemic adverse reactions with the use of aripiprazole and other atypical antipsychotics. All patients taking atypical antipsychotics, including aripiprazole, should be carefully monitored for symptoms of hyperglycemia (increased thirst, frequent urination, polyphagia, weakness). In patients with diabetes mellitus or risk factors for diabetes mellitus, the blood glucose concentration should be monitored regularly.

Hypersensitivity

As with the use of other medications, hypersensitivity reactions may develop during treatment with aripiprazole, which are manifested by allergic symptoms.

Weight gain

Patients with schizophrenia or bipolar mania often experience an increase in body weight associated with comorbid disorders, taking antipsychotics that cause an increase in body weight, and insufficient motor activity. Weight gain can lead to serious complications. In post-marketing studies of aripiprazole, an increase in body weight of patients was noted. However, it was usually observed against a background of significant risk factors, such as diabetes mellitus, thyroid disease or pituitary adenoma in a history of adult patients. In clinical studies involving adolescent patients suffering from bipolar mania, an increase in body weight after 4 weeks was shown during treatment with aripiprazole. It is necessary to monitor body weight in adolescents with bipolar mania. With a significant increase in body weight, a dose reduction may be indicated.

Dysphagia

When using neuroleptics, cases of esophageal peristalsis and aspiration disorders have been reported.

Caution should be exercised when using in patients with risk factors for aspiration pneumonia.

Pathological gambling addiction and other impulse control disorders

When taking aripiprazole, patients may experience an increased craving, especially for gambling, and an inability to control these urges.

There have also been reports of increased sex drive, an overwhelming urge to shop, overeating or compulsive eating, and other impulsive and compulsive behavioral disorders. Patients and their caregivers should be informed about the development of previously unobserved urges or about the increase in gambling, sexual desire, irresistible shopping, overeating or compulsive eating, or other urges during treatment with aripiprazole. It should be noted that the symptoms of impaired impulse control may be related to the underlying disease, but cases of cessation of symptoms have been reported when the dose is reduced or the drug is discontinued. Untimely diagnosis of the development of impulse control disorders can cause harm to the patient and others. In cases of impulse control disorders, the decision should be made to reduce the dose of the drug or cancel it.

Patients with Attention Deficit Hyperactivity disorder (ADHD)

Despite the high incidence of co-morbidity of type I bipolar disorder and ADHD, there are limited data on the safety of concomitant use of aripiprazole and psychostimulants. Therefore, special care should be taken when using them simultaneously.

Falls

The use of aripiprazole can cause drowsiness, orthostatic hypotension, motor and sensory disorders, which can lead to a fall. Caution should be exercised when treating high-risk patients (for example, elderly or debilitated patients) and the use of lower initial doses should be considered (see the section “Dosage and use”).

Caution should be exercised when using Zilaxera until patients are satisfied that aripiprazole does not adversely affect them.

Form of production

Tablets,5 mg,10 mg,15 mg,30 mg.

14 tablets each in a contour cell package made of combined PVC material/PVDH and aluminum foil.

2 or 4 contour cell packages together with the instructions for use are placed in a pack of cardboard.

Storage conditions

At a temperature not exceeding 25 ° C, in the original packaging.

Keep out of reach of children.

Expiration date

For tablets 10 mg,15 mg,30 mg: 5 years.

For 5 mg tablets: 2 years.

Do not use the drug after the expiration date.

Active ingredient

Aripiprazole

Conditions of release from pharmacies

By prescription

Dosage form

Tablets