DR. DOPING

Instructions

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Instructions / Instruction for use: Alepbik Pipzol

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Dosage form: tablets

Active substance: Aripiprazole *

Composition

One 5 mg tablet contains:

active ingredient: aripiprazole 5 mg;

auxiliary substances: lactose monohydrate 42.84 mg, microcrystalline cellulose 32.78 mg, giprolose 2.85 mg, corn starch 4.75 mg, crospovidone 2.85 mg, silicon dioxide colloid 0.48 mg, indigocarmine 2.50 mg, magnesium stearate 0.95 mg.

One 10 mg tablet contains: active ingredient: aripiprazole 10 mg;

Excipients: lactose monohydrate 39.51 mg, microcrystalline cellulose 32.78 mg, giprolose 2.85 mg, corn starch 4.75 mg, crospovidone 2.85 mg, silicon dioxide colloid 0.48 mg, pigment mixture PB-24880 pink * 0.83 mg, magnesium stearate 0.95 mg.

One 15 mg tablet contains:

active ingredient: aripiprazole 15 mg;

auxiliary substances: lactose monohydrate 58.01 mg, cellulose microcrystalline 49.17 mg, giprolose 4,275 mg, corn starch 7,125 mg, crospovidone 4,275 mg, silicon dioxide colloid 0.72 mg, pigment mixture PB-52290 yellow ** 2.50 mg , magnesium stearate 1.425 mg.

One 30 mg tablet contains:

active ingredient: aripiprazole 30 mg;

auxiliary substances: lactose monohydrate 118.52 mg, cellulose microcrystalline 98.34 mg, giprolose 8.55 mg, corn starch 14.25 mg, crospovidone 8.55 mg, silicon dioxide colloid 1.44 mg, a mixture of pigments PB-24880 pink * 2.50 mg, magnesium stearate 2.85 mg.

* Mixture of pigments –¬-24880 pink: lactose monohydrate 90.0%, iron dye red oxide (E172) 10.0%.

** Pigment mixture PB-52290 yellow: lactose monohydrate 25.0%, iron dye oxide yellow (E172) 75.0%.

Description of dosage form

Dosage of 5 mg: rectangular flat with rounded edges of a tablet of blue color with impregnations, on one side an engraving "250".

Dosage of 10 mg: rectangular flat with rounded edges of a tablet of light pink color with impregnations, on one side an engraving "252".

Dosage of 15 mg: round planocylindrical with a bevel of yellow tablets with impregnations, on one side engraving "253".

Dosage of 30 mg: round planocylindrical with a bevel of a tablet of light pink color with impregnations, on one side an engraving "L255".

Taking aripiprazole orally at doses of 0.5 to 30 mg once a day by healthy volunteers for 2 weeks results in a dose-dependent decrease in the binding of 11C-raclopride, the D 2 / D d-dopamine receptor ligand, with the caudate nucleus and the fence according to data positron emission tomography.

Pharmacokinetics

Suction

Aripiprazole is rapidly absorbed after ingestion, while its maximum concentration in the blood plasma is reached in 3-5 hours. Aripiprazole is minimally exposed to pre-systemic metabolism. Absolute bioavailability of tablets is 87%. Foods high in fat do not affect the pharmacokinetics of aripiprazole.

Distribution

Aripiprazole is intensively distributed in tissues, the apparent volume of distribution is 4.9 l / kg, indicating a significant extravascular distribution. At therapeutic concentrations aripiprazole and dehydroaripiprazole bind more than 99% to blood plasma proteins, mainly with albumins.

Metabolism

Aripiprazole is largely metabolized in the liver in three ways: dehydrogenation, hydroxylation and N-dealkylation. According to in vitro experiments, the dehydrogenation and hydroxylation of aripiprazole occurs under the action of the CYP3 A4 and CYP2 D6 isoenzymes, and N-dealkylation is catalyzed by the CYP3 A4 isoenzyme. Aripiprazole is the main active substance in the blood. In the equilibrium state, the area under the concentration-time curve (AUC) of dehydroaripiprazole, the main metabolite, is approximately 40% of aripiprazole AUC in the blood plasma.

Excretion

The mean half-life (T 1/2) of aripiprazole is approximately 75 hours in patients with high CYP2 D6 isoenzyme activity and about 146 hours in patients with low CYP2 D6 isoenzyme activity. The total clearance of aripiprazole is 0.7 ml / min / kg, mainly due to excretion by the liver.

After a single oral administration of labeled [14C] aripiprazole, approximately 27% of radioactivity is detected in urine and about 60% in feces. Less than 1% of unchanged aripiprazole is excreted in the urine, and approximately 18% of the accepted dose is excreted unchanged from the faeces.

Pharmacokinetics in specific patient groups

Use in children

The pharmacokinetics of aripiprazole and dehydroaripiprazole in children aged 10 to 17 years was the same as in adults after adjusting the difference in body weight.

Elderly patients

Differences in the parameters of aripiprazole pharmacokinetics in healthy elderly and adult volunteers have not been revealed. Population pharmacokinetics analysis also showed no significant effect of age in patients with schizophrenia.

Floor

Differences in the parameters of aripiprazole pharmacokinetics in healthy men and women have not been revealed. Population analysis of pharmacokinetics also did not reveal a significant effect of sex in patients with schizophrenia.

Smoking

Population analysis of pharmacokinetics showed no clinically significant effects of smoking on the parameters of aripiprazole pharmacokinetics.

Race

Population analysis of pharmacokinetics showed no effect of racial differences on the pharmacokinetics of aripiprazole.

Patients with impaired renal function

Parameters of pharmacokinetics of aripiprazole and dehydroaripiprazole in patients with severe kidney diseases do not differ from those of healthy volunteers.

Patients with impaired hepatic function

In a single dose study in patients with varying severity of liver cirrhosis (class A, B and C according to the Child-Pugh classification), there was no significant effect of liver dysfunction on the pharmacokinetics of aripiprazole and dehydroaripiprazole, however, only three patients with cirrhosis class C according to the Child-Pugh classification, in connection with which it is impossible to draw definitive conclusions on their metabolic activity.

Indications

schizophrenia: acute attacks and maintenance therapy;

manic episodes in type I bipolar disorder of moderate to severe severity and prophylaxis of a new manic episode in adults who develop predominantly manic episodes that are treatable with aripiprazole;

supplementation with lithium or valproic acid therapy for the treatment of manic or mixed episodes in type I bipolar disorder with or without psychotic symptoms and maintenance therapy to prevent relapse in patients with type I bipolar disorder;

addition to antidepressant therapy for major depressive disorder.

Contraindications

hypersensitivity to aripiprazole or any other component included in the formulation;

hereditary galactosemia, lactase deficiency, glucose-galactose malabsorption;

age 18 years (efficacy and safety not established);

the period of breastfeeding.

Carefully

Cardiovascular diseases (coronary heart disease (CHD) or previous myocardial infarction, chronic heart failure (CHF) or conduction disorders); cerebrovascular diseases and conditions predisposing to the development of arterial hypotension (dehydration, hypovolemia, use of antihypertensive drugs) in connection with the possibility of developing orthostatic hypotension; patients with convulsions or with diseases in which cramps are possible; increased risk of hyperthermia (eg, intense physical exertion, overheating, use of m-cholinergic blockers, dehydration, since antipsychotics are able to disrupt thermoregulation); patients with an increased risk of aspiration pneumonia because of the risk of developing a violation of the motor function of the esophagus and aspiration; obesity or diabetes in a family history; patients with a high risk of suicide (psychotic diseases, bipolar disorders, major depressive disorder); persons aged 18-24 years due to the risk of developing suicidal behavior.

Application in pregnancy and lactation

Adequate and well-controlled studies in pregnant women have not been conducted. It is not known whether the use of the drug by a pregnant woman can have a harmful effect on the fetus or cause reproductive harm. It is known that in newborns, whose mothers took neuroleptics during the III trimester of pregnancy, in the postpartum period there is a risk of developing extrapyramidal disorders and / or withdrawal syndrome. They had excitement, increased or decreased blood pressure, tremor, drowsiness, respiratory distress syndrome, eating disorders. These symptoms were of varying severity, sometimes they were treated without treatment, while in other cases the newborns needed intensive therapy and continued hospitalization. When using aripiprazole, development in newborns of such a symptomatology was very rare.

It is necessary to warn patients that they should immediately inform the doctor about the onset of pregnancy against the background of treatment, should also inform the doctor about the planned pregnancy.

The drug can be taken during pregnancy only if the potential benefit to the mother is greater than the potential risk to the fetus.

Aripiprazole penetrates into breast milk. When applying the drug, breastfeeding should be discontinued.

Dosing and Administration

Inside, 1 time per day, regardless of food intake.

Schizophrenia

The recommended initial dose is 10-15 mg once daily.

The maintenance dose is usually 15 mg / day.

The effectiveness of the drug is confirmed in the dose range from 10 to 30 mg / day. Increasing the dose more than 15 mg / day does not increase the effectiveness of the drug. The dose is increased not earlier than in 2 weeks.

The maximum daily dose is 30 mg.

Manic episodes with type I bipolar disorder

Monotherapy

The recommended initial dose is 15 mg once a day.

The dose change, if necessary, is carried out with an interval of at least 24 hours. In manic episodes, the effectiveness of the drug in doses of 15-30 mg / day with a dose of 3-12 weeks was demonstrated. The maximum daily dose is 30 mg.

When observing patients with type I bipolar disorder who have had a manic or mixed episode, who had a symptom stabilization against the background of taking the drug 15 or 30 mg / day at an initial dose of 30 mg / day for 6 weeks, and then for 6 months and beyond - within 17 months, the favorable effect of such maintenance therapy has been established.

Periodically, patients should be examined to determine whether to continue supporting therapy.

As an adjunct to therapy with lithium or valproic acid

The recommended starting dose is 10 mg to 15 mg once a day, regardless of food intake. The maintenance dose is usually 15 mg / day. The dose can be increased to 30 mg / day, depending on the clinical indications.

When observing patients with type I bipolar disorder, a favorable effect of maintenance therapy with a drug from 10 mg to 30 mg per day was added as a supplement to therapy with lithium or valproic acid. Periodically, patients should be examined to determine whether to continue supporting therapy.

Additional therapy for major depressive disorder

As an additional therapy to treatment with antidepressants, it is recommended to prescribe the drug in an initial dose of 5 mg / day. If necessary and good tolerability of therapy, the daily dose of the drug can be increased every week by 5 mg to a maximum of no more than 15 mg per day.

The duration of drug therapy for all of the above indications is not established; It is necessary to conduct a regular examination of the patient for the possibility of canceling therapy.

Use in special patient groups

Patients with renal insufficiency

Correction of the dose is not required.

Patients with hepatic insufficiency

Patients with mild and moderate hepatic insufficiency do not need dose adjustment. Patients with severe hepatic impairment should be dosed with caution. In patients with severe hepatic insufficiency, a maximum daily dose of 30 mg should be administered with caution.

Patients over 65 years of age

Correction of the dose is not required.

Effect of the patient's sex on the dosing regimen

Dosage regimen for patients of both sexes is the same.

Smoking

Dosage regimen for smoking and non-smoking patients is the same.

Dosing regimen with concomitant therapy

With the simultaneous use of aripiprazole and potent inhibitors of the isoenzyme CYP3 A4 (ketoconazole, clarithromycin), the dose of aripiprazole should be reduced by a factor of 2. With the cancellation of inhibitors of the isoenzyme CYP3 A4, the dose of aripiprazole should be increased.

With the simultaneous use of aripiprazole and potent inhibitors of the isoenzyme CYP2 D6 (quinidine, fluoxetine, paroxetine), the dose of aripiprazole should be reduced by a factor of 2. With the cancellation of CYP2 D6 isoenzyme inhibitors, the dose of aripiprazole should be increased.

The drug should be used without changing the dosage regimen if it is prescribed as an adjunctive therapy in patients with major depressive disorder. With the simultaneous use of aripiprazole and potent inhibitors of CYP2 D6 isoenzymes (quinidine, fluoxetine, paroxetine) and CYP3 A4 (ketoconazole, clarithromycin), the dose of aripiprazole should be reduced

by ¾ (that is, up to 25% of the usual dose). With the cancellation of inhibitors of CYP2 D6 and / or CYP3 A4 isoenzymes, the dose of aripiprazole should be increased.

With the simultaneous use of aripiprazole and powerful, moderate and weak inhibitors of CYP2 D6 and / or CYP3 A4 isozymes, the dose of aripiprazole can initially be reduced by ¾ (i.e., up to 25% of the usual dose) and then increased to achieve the optimal clinical outcome.

Patients with a low activity of the isoenzyme CYP2 D6 initially dose of aripiprazole should be reduced 2 times, and then increased to achieve the optimal clinical result. With the simultaneous use of aripiprazole and a potent inhibitor of the CYP3 A4 isoenzyme, in patients with a low CYP2 D60 isoenzyme activity, the dose of aripiprazole should be reduced by ¾ (that is, up to 25% of the usual dose).

With the simultaneous use of aripiprazole and potential inducers of the isoenzyme CYP3 A4 (carbamazepine), the dose of aripiprazole should be doubled. When cannabis inducers cancellation CYP3 A4, the dose of aripiprazole should be reduced to 10-15 mg.

Side effects

The most common side effects in placebo-controlled clinical trials are akathisia and nausea, each of which was observed in more than 3% of patients taking aripiprazole.

Undesirable reactions are classified according to organ and organ damage and the frequency of development as follows: very often (e1 / 10), often (from e1 / 100 to <1/10), infrequently (from e1 / 1000 to <1/100) , rarely (from e1 / 10000 to <1/1000), very rarely (<1/10000) and the frequency is unknown (can not be estimated based on available data). Within the limits of each group, isolated depending on the frequency of occurrence of the undesired reaction, undesirable reactions are presented in order of decreasing severity.

The incidence of adverse reactions in post-marketing studies can not be determined, since reports of adverse reactions were spontaneous. Therefore, the frequency of these unwanted reactions is indicated as "frequency unknown".

Often Infrequently Frequency unknown
Violations of the blood and lymphatic system Leukopenia
Immune system disorders Neutropenia
Disorders from the endocrine system Hyperprolactinemia Thrombocytopenia
Disorders of metabolism and nutrition Diabetes Hyperglycaemia Allergic reactions (eg, anaphylactic reactions, angioedema, including swelling of the tongue, swelling of the tongue, face swelling, itching, or urticaria)
Mental disturbance Insomnia Depression Diabetic hyperosmolar coma
Disturbances from the nervous system Anxiety Increased sexuality Diabetic ketoacidosis
Disturbances on the part of the organ of sight Anxiety Late dyskinesia Hyperglycaemia
Heart Disease Akathisia Dystonia Hyponatremia
Vascular disorders Extrapyramidal disorders Diplopia Anorexia
Disturbances from the respiratory system, chest and mediastinal organs Tremor Tachycardia Decreased body weight
Disorders from the gastrointestinal tract Headache Orthostatic hypotension Weight gain
Disturbances from the liver and bile ducts Sedation effect Hiccups Attempted suicide, suicidal thoughts and perfect suicide Pathological predilection for gambling
Disturbances from the skin and subcutaneous tissues Drowsiness Frequency unknown Aggression
Disturbances from musculoskeletal and connective tissue Dizziness Excitation
Disorders from the kidneys and urinary tract Blurred vision Nervousness
Pregnancy, postpartum and perinatal conditions Hyperprolactinemia Malignant
Violations of the genitals and mammary gland Hyperglycaemia neuroleptic syndrome (CNS)
General disorders and disorders at the site of administration Depression Great seizure
Laboratory and instrumental data Constipation Increased sexuality Serotonin syndrome

Overdose

Symptoms: lethargy, increased blood pressure, drowsiness, tachycardia, nausea, vomiting, loss of consciousness. Hospitalized patients showed no clinically significant changes in the basic physiological parameters, laboratory parameters and electrocardiogram (ECG).

Potentially dangerous symptoms of overdose include drowsiness, extrapyramidal disorders and transient loss of consciousness.

Treatment: monitoring of vital functions, ECG (to detect possible arrhythmia), maintenance therapy, airway patency, oxygenation, effective ventilation, activated charcoal, symptomatic treatment, careful medical observation until all symptoms disappear.

Drug reactions should be considered.

Activated charcoal (50 g), administered 1 hour after taking aripiprazole, reduced AUC and C max aripiprazole by 51 and 41%, respectively, which allows recommending its use in overdose.

Data on the use of hemodialysis in case of an overdose of aripiprazole are absent; a favorable effect of this method is unlikely, since aripiprazole is not excreted by the kidneys in an unchanged form and is largely associated with plasma proteins.

Interaction

Aripiprazole may enhance the effect of certain antihypertensive drugs, since it has antagonistic action against α1-adrenergic receptors.

The mechanism of action of aripiprazole is associated with influence on the central nervous system (CNS), therefore caution should be exercised when aripiprazole is used together with alcohol or drugs having a central effect, as this may exacerbate a side effect such as sedation. Caution should be exercised with the simultaneous use of aripiprazole and medications that cause prolongation of the QT interval or disturb the electrolyte balance.

Effect of the use of other drugs on aripiprazole

The H2-histamine receptor blocker famotidine reduces the rate of absorption of aripiprazole, however, it is believed that this has no clinically significant effect. Aripiprazole is metabolized in various ways, including with the participation of isoenzymes CYP 2 D 6 and CYP 3 A 4, but it is not metabolized with the participation of the CYP 1 A isoenzyme. Therefore, the adjustment of the dose to smoking patients is not required.

Quinidine and other inhibitors of the isoenzyme CYP 2 D 6

Results from a clinical study involving healthy patients showed that a potent inhibitor of the CYP 2 D 6 isoenzyme (quinidine) increases aripiprazole AUC by 107%, while the C max index remains unchanged. The values of AUC and C max dehydroaripiprazole, the active metabolite, were reduced by 32% and 47%, respectively. It is necessary to reduce the dose of aripiprazole by approximately half of the prescribed dose while using aripiprazole with quinidine. Other potent inhibitors of the CYP 2 D 6 isoenzyme, such as fluoxetine and paroxetine, can have similar effects, so a similar reduction in the dose of aripiprazole is recommended if they are used simultaneously.

Ketoconazole and other inhibitors of the CYP 3 A 4 isoenzyme

The results of a clinical trial involving healthy patients showed that a potent inhibitor of the isoenzyme CYP 3 A 4 (ketoconazole) increases aripiprazole AUC and C max values by 63% and 37%, respectively. The values of AUC and C max dehydroaripiprazole increased by 77% and 43%, respectively. In slow metabolizers of the CYP 2 D 6 isoenzyme, the simultaneous use of potent inhibitors of the CYP 3 A 4 isoenzyme may lead to a higher concentration of aripiprazole in the blood plasma compared to the fast metabolizers of the CYP 2 D 6 isoenzyme.

When considering the simultaneous use of ketoconazole or other potent inhibitors of the CYP 3 A 4 isoenzyme with aripiprazole, the potential benefit should exceed the possible risk to the patient. With the simultaneous use of ketoconazole and aripiprazole, the dose of aripiprazole should be reduced by approximately half the prescribed dose. When a joint application of aripiprazole with other potent inhibitors of the CYP 3 A 4 isoenzyme, such as itraconazole and HIV protease inhibitors, a similar effect can be expected, so the dose of aripiprazole should also be reduced.

If the CYP 2 D 6 or CYP 3 A 4 isoenzyme inhibitor is discontinued, the dose of aripiprazole should be increased to the level appropriate for the level before the start of the joint application.

With the simultaneous use of aripiprazole and weak inhibitors of CYP 3 A 4 isoenzymes (such as diltiazem or escitalopram) or CYP 2 D 6, a slight increase in the aripiprazole concentration in the blood plasma can be expected.

Carbamazepine and other inducers of the isoenzyme CYP 3 A 4

With the simultaneous use of carbamazepine, a powerful inducer of the CYP 3 A 4 isozyme, the geometric mean values of C max and AUC of aripiprazole decreased by 68% and 73%, respectively, compared with aripiprazole (30 mg) as monotherapy. Similarly, with the simultaneous use of dehydroaripiprazole and carbamazepine, the geometric mean C max and AUC were reduced by 69% and 71%, respectively, compared with the use of aripiprazole as monotherapy.

When combined with carbamazepine, the dose of aripiprazole should be increased 2-fold. When the joint application of aripiprazole with other potent inducers of CYP isoenzyme 3 A 4 (such as rifampin, rifabutin, phenytoin, phenobarbital, primidone, efavirenz, nevirapine and St. John's wort) can expect a similar effect, however aripiprazole dose should be increased. If the CYP 3 A 4 isoenzyme is stopped, the dose of aripiprazole should be reduced to the recommended one.

Valproic acid and lithium preparations

With the simultaneous use of aripiprazole with preparations of valproic acid or lithium, there were no significant clinical changes in the concentration of aripiprazole in the blood plasma.

Serotonin syndrome

Cases serotonin syndrome were reported in patients taking aripiprazole, and possible signs and symptoms of this condition may occur especially when applied to other serotonergic drugs such as selective serotonin reuptake inhibitor (SSRI) and a selective serotonin reuptake inhibitor, norepinephrine (SNRIs) , or drugs that increase the concentration of aripiprazole in the blood plasma.

Effect of aripiprazole on other drugs

In clinical studies, aripiprazole at doses of 10-30 mg / day had no significant effect on the metabolism of substrates isozymes CYP 2 D 6 (dektrometorfan / 3- methoxymorphinan), CYP 2 9 C (warfarin), CYP 2 C 19 (omeprazole) and CYP 3 A 4 (dextromethorphan). In addition, aripiprazole and dehydroaripiprazole did not alter the biotransformation of drugs metabolized by the CYP 1 A 2 isoenzyme in vitro. Thus, it is unlikely that aripiprazole may cause a clinically significant effect on the interaction of drugs metabolized with the participation of these isoenzymes.

With the simultaneous use of aripiprazole with valproic acid, lithium or lamotrigine, there was no clinically significant change in the concentration of valproic acid, lithium or lamotrigine in blood plasma.

Special instructions

With the use of antipsychotic drugs, the therapeutic effect develops from several days to several weeks. During this period, it is necessary to carefully monitor the patient's condition.

Suicide attempts

The phenomenon of suicidal behavior is characteristic for psychoses and mood disorders, in some cases it is observed immediately after the beginning or change of treatment with antipsychotics, including treatment with aripiprazole. When treating with antipsychotic drugs, it is necessary to carefully monitor patients who are at high risk.

The results of the epidemiological study showed that patients with schizophrenia or bipolar disorder did not have an increased risk of suicidality when treated with aripiprazole, compared to other antipsychotics. There is insufficient clinical data to estimate this risk in younger patients (under the age of 18), but there is reason to believe that the risk persists after 4 weeks of treatment with antipsychotics, including aripiprazole.

Cardiovascular diseases

Aripiprazole should be used with caution in patients with cardiovascular disease (myocardial infarction or ischemic heart disease, heart failure, or cardiac conduction disease), cerebrovascular disease, conditions that predispose to hypotension (dehydration, hypovolemia and antihypertensive drugs therapy) or hypertension, including essential or malignant. When using antipsychotic drugs, cases of venous thromboembolism (VTE) have been reported. Since patients undergoing antipsychotic medications often have acquired risk factors for the development of VTE, it is necessary to identify all possible risk factors for developing VTE before and during treatment with aripiprazole with preventive measures.

The elongation of the OT interval

In clinical studies of aripiprazole, the incidence of QT prolongation was comparable to the placebo group. Aripiprazole, like other antipsychotics, should be used with caution in patients who have a family history of prolonging the QT interval.

Late dyskinesia

In clinical studies lasting 1 year or less, during the treatment with aripiprazole, infrequent cases of dyskinesia requiring urgent treatment were observed. If the patient is treated with aripipra

Malignant neuroleptic syndrome (CNS)

Malignant neuroleptic syndrome is a potentially life-threatening combination of symptoms associated with the use of antipsychotics. In clinical studies during the treatment with aripiprazole, rare cases of CNS were observed. Clinical manifestations of CNS are hyperpyrexia, muscle rigidity, mental disorders and instability of the autonomic nervous system (irregular pulse or arterial pressure, tachycardia, increased sweating and cardiac arrhythmia). Additional signs may include an increase in the activity of creatine phosphokinase, myoglobinuria (rhabdomyolysis), and acute renal failure. Nevertheless, there have been cases of an increase in the activity of creatine phosphokinase and rhabdomyolysis, not associated with the NSA. In the case of signs and symptoms of NSA or unexplained fever without additional clinical manifestations of NSA, all antipsychotics, including aripiprazole, should be discarded.

Convulsions

In clinical studies during the treatment with aripiprazole, infrequent cases of seizures were observed. Therefore, aripiprazole should be used with caution in patients with a history of seizures or the risk of their development.

Psychoses associated with senile demenia

Increased mortality

In three placebo-controlled clinical trials of aripiprazole in elderly patients (938 patients, mean age 82.4 years, age range 56-99 years) with psychosis due to Alzheimer's disease, there was an increased risk of death compared to the placebo group. Mortality with aripiprazole was 3.5% compared with 1.7% in the placebo group. Although the causes of death varied, the main causes of most deaths were either cardiovascular disorders (including heart failure, sudden death), or the development of infection (including pneumonia).

Cerebrovascular undesirable reactions

In the same clinical trials, elderly patients (mean age 84 years, age range 78-88 years) reported the development of cerebrovascular unwanted reactions (including stroke, transient ischemic attack), including fatal outcome. In general, in 1.3% of patients with aripiprazole treatment, cerebrovascular unwanted reactions were observed compared with 0.6% of patients receiving placebo. This difference was not statistically significant. However, in one of these studies a fixed dose of aripiprazole revealed a significant dose-to-cerebrovascular undesirable reactions. Aripiprazole is not recommended for use in patients with psychoses due to dementia.

Hyperglycemia and diabetes mellitus

Hyperglycemia, sometimes expressed and accompanied by ketoacidosis or hyperosmolar coma with a fatal outcome, was noted in patients taking atypical antipsychotics, including aripiprazole. The risk factors for serious complications in patients include obesity and diabetes in the family history. In clinical trials of aripiprazole, there was no significant difference in the incidence of adverse events associated with hyperglycemia (including diabetes) or in changing laboratory glucose values compared to the placebo group. There is no accurate comparative assessment of the risks of developing adverse reactions associated with hyperglycemia in patients taking aripiprazole and other atypical antipsychotics. Patients taking atypical antipsychotics, including aripiprazole, need constant monitoring of symptoms of hyperglycemia (increased thirst, frequent urination, polyphagia, and weakness). Patients with diabetes mellitus or with risk factors for developing diabetes should regularly be assessed for blood glucose.

Hypersensitivity

As with other medications, hypersensitivity reactions may develop in the form of allergic symptoms when taking aripiprazole.

Weight gain

An increase in body weight is usually observed in patients with schizophrenia and bipolar mania due to the development of concomitant diseases, the use of antipsychotics that cause weight gain, unhealthy lifestyles, and can lead to serious complications. Reports of cases of weight gain were obtained in the postmarketing period in patients who took aripiprazole. Usually, these adverse reactions were observed in patients with significant risk factors, such as diabetes mellitus, thyroid disease or pituitary adenoma. In clinical trials, the administration of aripiprazole did not produce a clinically significant increase in body weight in adult patients. In clinical studies of adolescent patients with bipolar mania, when receiving aripiprazole, body weight increased after 4 weeks of treatment. It is necessary to continuously monitor body weight in adolescent patients with bipolar mania. If the increase in body weight is clinically significant, it is necessary to reduce the dose of aripiprazole.

Dysphagia

With the use of neuroleptics, including aripiprazole, cases of peristalsis of the esophagus and aspiration were noted. Aripiprazole and other antipsychotics should be used with caution in patients at risk of developing aspiration pneumonia.

Pathological attraction to gambling

In the post-registration period, there were reports of pathological attraction to gambling in patients taking aripiprazole, regardless of whether they had a pathological attraction to gambling in the anamnesis. Patients with an anamnesis pathological attraction to gambling may be at increased risk for developing this disorder and should be carefully monitored.

Lactose

The drug contains lactose, therefore it is not recommended for patients who have rare hereditary diseases associated with intolerance to galactose, deficiency of lactase or glucose-galactose malabsorption.

Patents with concomitant attention deficit hyperactivity disorder (ADHD)

Despite the high frequency of combination of type I bipolar disorder and ADHD, there are very limited data on the safety of simultaneous use of aripiprazole and psychostimulants, so caution should be exercised in the joint use of these drugs.

Influence on ability to drive vehicles, mechanisms

During the treatment period, care must be taken when driving vehicles and engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

Relase form

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

For 10 tablets per blister of OPA / Al / PVC film and aluminum foil. 1 blister with instructions for use in a cardboard box.

Shelf life

2 years.

Do not use at the expiration date.

Conditions of leave from pharmacies

Letting go by prescription.

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