Abilifay - instructions for use, dose, side effects, contraindications

Excipients: lactose monohydrate 67 mg, microcrystalline cellulose 10 mg, corn starch 10 mg, giprolose 2 mg, magnesium stearate 0.80 mg, indigocarmine aluminum varnish 0.20 mg.

Each 10 mg tablet contains:

Active substance: aripiprazole 10 mg.

Excipients: lactose monohydrate 62.18 mg, cellulose microcrystalline 10 mg, corn starch 10 mg, giprolose 2 mg, magnesium stearate 0.80 mg, iron oxide dye red 0.02 mg.

Each 15 mg tablet contains:

Active substance: aripiprazole 15 mg.

Excipients: lactose monohydrate 57 mg, cellulose microcrystalline 10 mg, corn starch 10 mg, giprolase 2 mg, magnesium stearate 0.80 mg, iron oxide dye yellow 0.2 mg.

Each 30 mg tablet contains:

Active substance: aripiprazole 30 mg.

Excipients: lactose monohydrate 186.45 mg, microcrystalline cellulose 30 mg, corn starch 30 mg, giprolase 6 mg, magnesium stearate 2.40 mg, ferric oxide red oxide 0.06 mg.

Description:

Tablets 5 mg: rectangular tablets with rounded edges, blue, marked "A-007" and "5" on one side.

Tablets 10 mg: rectangular tablets with rounded edges, pink,. with the marking "A-008" and "10" on one side.

Tablets 15 mg: round tablets of yellow color, with a bevel, marked "A-009" and "15" on one side.

Tablets 30 mg: round tablets of pink color, with a bevel, marked "A-011" and "30" on one side.

Pharmacotherapeutic group:Antipsychotic agent (antipsychotic)

ATX: & nbsp

N.05.A.X Other antipsychotics

N.05.A.X.12 Aripiprazole

Pharmacodynamics:

It is assumed that the therapeutic effect of aripiprazole in schizophrenia bipolar disorder Itype is due to a combination of partial agonistic activity in relation to D2- Dopamine and 5HT1_a-serotonin receptors and antagonistic activity against 5HT2-serotonin receptors.

Pharmacodynamics

Aripiprazole has a high affinity iP vitro to D2- and D3-dopamine receptors, 5HT1_a- and 5HT2_aserotonin receptors and moderate affinity for D4dopamine, 5HT2_FROM- and 5HT₇-serotonin, α1-adrenoreceptors and H1-ghistamine receptors.

Aripiprazole is also characterized by moderate affinity for the sites of serotonin reuptake and lack of affinity for m-holinoretseptoram. Aripiprazole in animal experiments, showed antagonism with respect to dopaminergic hyperactivity and agonism with respect to dopaminergic hypoactivity. Some clinical effects of aripiprazole can be explained by interaction with other types of receptors (notdopamine and serotonin).

Pharmacokinetics:

The activity of Abilifay® is mainly due to the presence of the initial substance, aripiprazole. The average half-life of aripiprazole is approximately 75 hours.The equilibrium concentration is achieved after 14 days. Cumulation of aripiprazole with multiple admission is predictable. The pharmacokinetics of aripiprazole in the equilibrium state are proportional to the dose. There were no daily fluctuations in the distribution of aripiprazole and its metabolite dehydroaripiprazole. It was found that the main metabolite of aripiprazole in human plasma, dehydroaripiprazole, has the same affinity for D2- dopamine receptors, as well as aripiprazole.

Aripiprazole is rapidly absorbed after ingestion of Abilifay®, with the maximum concentration of the drug in the plasma achieved in 3-5 hours. Absolute; the bioavailability of the tablets of the drug Abilifay® is 87%. Food intake for the bioavailability of aripiprazole is not affected.

Aripiprazole is intensively distributed in tissues, with an apparent volume of distribution of 4.9 l / kg. At a therapeutic concentration of more than 99%, aripiprazole binds to serum proteins, mainly with albumin. Aripiprazole is subjected to presystemic metabolism only to a minimal extent. Aripiprazole metabolized in the liver in three ways: dehydrogenation, hydroxylation and N-dealkylation. According to experiments in vitro, dehydrogenation and hydroxylation of aripiprazole occurs under the action of isoenzymes CYP3A4 and CYP2D6, a N-dealkylation is catalyzed by isoenzyme CYP3A4. Aripiprazole is the main component of the drug in the blood. In the equilibrium state, the area under the curve, "drug concentration-time" (AUC) dehydroaripiprazole is about 39% AUC aripiprazole in plasma.

The mean half-life of aripiprazole is about 75 hours in patients with a high metabolic rate through isoenzyme CYP2D6 and about 146 hours in patients with a low metabolic rate with the participation of this isoenzyme. 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% and 60% of radioactivity is determined in urine and feces, respectively. Less than 1% of unchanged aripiprazole is detected in the urine and approximately 18% of the dose taken is unchanged with feces.

Pharmacokinetics in specific patient groups

Children 13 - 17 years old

Parameters of pharmacokinetics of aripiprazole and dehydroaripiprazole in children 13-17 years old do not differ from those in adults,therefore dose adjustment is not required.

Patients of the older age group

Age differences in the parameters of aripiprazole pharmacokinetics in adult patients with schizophrenia, as well as in healthy volunteers, have not been revealed.

Floor

The sex differences in the parameters of aripiprazole pharmacokinetics in adult patients with schizophrenia, as well as in healthy volunteers, were not detected.

Race

Clinically significant differences in the pharmacokinetics of aripiprazole, depending on race, were not observed.

Smoking

Smoking does not affect the pharmacokinetics of aripiprazole.

Impaired renal function

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

Violation of the function necheni

After a single administration of aripiprazole by persons with varying severity of liver cirrhosis, there was no significant effect of liver dysfunction on the pharmacokinetics of aripiprazole and dehydroaripiprazole. However, the study involved only 3 patients with decompensated liver cirrhosis (Class C according to the Child-Pugh classification),in connection with which 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;

- bipolar disorder type I: manic episodes and maintenance therapy to prevent relapse in patients with type I bipolar disorder who have recently undergone a manic or mixed episode;

- 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 1 bipolar disorder;

- addition to antidepressant therapy for major depressive disorder.

Contraindications:Hypersensitivity to aripiprazole or any other component in the formulation;
Rare hereditary galactosemia, lactase deficiency, glucose-galactose malabsorption;
Age to 18 years;
Breastfeeding period.

Carefully:

Use in patients with cardiovascular diseases (with coronary heart disease or with myocardial infarction, with heart failure and conduction disorders), cerebrovascular diseases and conditions predisposing to arterial hypotension (dehydration, hypovolemia and taking antihypertensive drugs) in connection with the possibility of orthostatic development hypotension, in patients with convulsive seizures or with diseases in which convulsions are possible; in patients with an increased risk of hyperthermia, for example, with intense physical exertion, overheating, m-holinoblokatorov, dehydration due to the ability of neuroleptics to disrupt thermoregulation; in patients with an increased risk of aspiration pneumonia due to the risk of impaired motor function of the esophagus and aspiration; in patients with obesity and in the presence of diabetes in the family; in patients with high risk of suicide (psychotic diseases, bipolar disorders, major depressive disorder); at persons in the age of 18-24 years in connection with risk of development of suicidal behavior.

If you have any of these diseases, consult a doctor before taking the drug.

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 3rd trimester of pregnancy, there is a risk of developing extrapyramidal disorders and / or withdrawal syndrome in the postpartum period. They showed 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, whereas 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.Abilifay® may be taken during pregnancy only if the potential benefit to the mother is greater than the potential risk to the fetus.
Aripiprazole penetrates into the human breast milk. Breastfeeding when using the drug is not recommended.

Dosing and Administration:

Schizophrenia

The recommended starting dose is 10 to 15 mg once a day, regardless of food intake. The maintenance dose is usually 15 mg per day.

In clinical trials, the effectiveness of the drug in doses of 10 to 30 mg / day is shown.

Manic episodes with bipolar disorder

Monotherapy

The recommended initial dose is 15 mg once a day, regardless of food intake. The dose change, if necessary, is carried out with an interval of at least 24 hours.

In clinical studies in manic episodes, the drug was shown to be effective at doses of 15-30 mg / day when taken for 3-12 weeks. Safety of doses above 30 mg / day in clinical trials was not evaluated.

When observing patients with bipolar disorder type I who have had a manic or mixed episode who had a stabilized symptom against the background of taking Abilifay® (15 mg / day or 30 mg / day at an initial dose of 30 mg / day) for 6 weeks,then - 6 months and further - within 17 months, the favorable effect of such maintenance therapy is established. Periodically, patients should be examined to determine whether to continue supporting therapy

Supplementary Therapy

As an adjunct to therapy with lithium or valproic acid in bipolar disorderve

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

When observing patients with type I bipolar disorder, a favorable effect of maintenance therapy with Abilifay® (10 mg / day to 30 mg / day) as a supplement to therapy with lithium or valproic acid was established. Periodically, patients should be examined to determine whether to continue supporting therapy.

Additional therapy for major depressive disorder

As an adjunct to the treatment with antidepressants, it is recommended to prescribe Abilifay® in an initial dose of 5 mg per day; if necessary and good tolerability of therapy, the daily dose of Abilifay® can be weekly increase by 5 mg to a maximum of 15 mg per day.

The duration of therapy with Abilifay® for all of the above indications is not established; It is necessary to regularly conduct a patient the possibility of canceling therapy.

For patients with hepatic insufficiency, a dose of 30 mg is given with caution.

Use in special groups patients

Patients with renal insufficiency

Dose adjustments for prescribing patients with renal insufficiency are not required.

Patients with hepatic insufficiency

Dose adjustments for prescribing patients with hepatic insufficiency are not required.

Use in 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.

Effect of smoking on the dosing regimen

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

Dosing regimen with concomitant therapy

With the simultaneous use of Abilifay® and powerful isoenzyme inhibitors CYP3A4 (ketoconazole, clarithromycin), the dose of Abilifay® should be reduced by half. When cancellation of isoenzyme inhibitors CYP3A4, the dose of Abilifay® should be increased.

With the simultaneous use of Abilifay® and powerful isoenzyme inhibitors CYP2D6 (quinidine, fluoxetine, paroxetine) the dose of Abilifay® should be reduced at least half. When cancellation of isoenzyme inhibitors CYP2D6 the dose of Abilifay® should be increased.

Abilafay® should be used without changes in the dosing regimen if it is prescribed as an adjunctive therapy in patients with major depressive disorder.

With the simultaneous use of Abilifay® and powerful isozyme inhibitors CYP2D6 (quinidine, fluoxetine, paroxetine) and CYP3A4 (ketoconazole, clarithromycin), the dose of Abilifai® should be reduced by 3/4% (that is, up to 25% of the usual dose). When cancellation of isozyme inhibitors CYP2D6 and / or CYP3A4, the dose of Abilifay® should be increased.

With the simultaneous use of Abilifay® and powerful, moderate or weak inhibitors of isoenzymes CYP2D6 and CYP3A4, the dose of Abilifai® can be initially reduced by 3/4% (that is, up to 25% of the usual dose), and then increased to achieve the optimal clinical outcome.

When Abilafia® is prescribed for patients with low isoenzyme activity CYP2D6 Initially, the dose of Abilifai® should be reduced by half, and then increased to achieve optimalclinical result. With the simultaneous use of Abilifay® and a potent inhibitor of isoenzyme CYP3A4 patients with low isoenzyme activity CYP2D60 The dose of Abilafia® should be reduced by 3/4% (that is, up to 25% of the usual dose.

With the simultaneous use of Abilifay® and potential isozyme inducers CYP3A4 (carbamazepine), the dose of Abilifay® should be increased 2-fold. When cancellation of isoenzyme inducers CYP3A4, The dose of Abilifai® should be reduced to 10-15 mg.

Side effects:

The frequency of side effects is shown in accordance with the following scale:

Very often:> 10%

Often:> 1% and <10%

Uncommon:> 0.1% and <1%

Rarely:> 0.01% and <0.1%

Very rarely: <0.01%

The frequency is unknown (can not be estimated with the help of available data).

The cardiovascular system

Often: orthostatic hypotension, tachycardia;

Infrequently: bradycardia, palpitations, myocardial infarction, lengthening of the interval QT, heart failure, hemorrhage, atrial fibrillation, heart failure, AV blockade, myocardial ischemia, deep vein thrombosis, phlebitis, extrasystole;

Rarely: vasovagal syndrome, atrial flutter, thrombophlebitis, intracranial hemorrhage, cerebral ischemia;

Rarely: fainting, increased blood pressure.

Frequency unknown: thromboembolism (including pulmonary embolism and deep vein thrombosis).

Digestive system

Often: nausea, loss of appetite;

Often: increased appetite *, indigestion, vomiting, constipation, hypersecretion of saliva, dry mouth, heaviness in the abdomen, diarrhea;

* in the treatment of depression in combination with antidepressants

Infrequently: gastroenteritis, difficulty swallowing, flatulence, gastritis, dental caries, gingivitis, hemorrhoids, gastroesophageal reflux, gastrointestinal hemorrhages, periodontal abscess, edema of the tongue, incontinence of feces, colitis, rectal hemorrhage, stomatitis, ulceration of the oral mucosa, cholecystitis, fecaloma, candidiasis of the oral mucosa, belching, stomach ulcer;

Rarely: esophagitis, gum bleeding, inflammation of the tongue, bloody vomiting, intestinal bleeding, duodenal ulcer, cheilitis, enlarged liver, perforation of the intestine;

Rarely: increased activity of alanine aminotransferase (ALT), and aspartate aminotransferase (ACT), hepatitis, jaundice, pancreatitis, dysphagia.

The immune system

Rarely: allergic reactions (anaphylaxis, angioedema, itching and urticaria), laryngospasm.

Musculoskeletal system

Often: arthralgia, rigidity of muscles;

Infrequently: myasthenia gravis, arthritis, arthrosis, muscle weakness, muscle spasms, bursitis;

Rarely: an increase in the activity of creatine phosphokinase, rhabdomyolysis, tendonitis, tenobursitis, myalgia.

Nervous system

Often: Insomnia, drowsiness, headache, akathisia;

Often: dizziness, tremor, extrapyramidal syndrome, psychomotor agitation, depression, nervousness, hostility, suicidal thoughts, manic thoughts, confusion, resistance to passive movements ("cogwheel syndrome"), lethargy, decreased concentration, sedation;

Infrequently: dystonia, muscle twitching, paresthesia, limb tremor, impotence, bradykinesia, decreased / increased libido, panic reactions, apathy, memory loss, stupor, amnesia, stroke, hyperactivity, depersonalization, dyskinesia,syndrome of restless legs, myoclonus, depressed mood, increased reflexes, slowing of mental function, increased sensitivity to irritants, violation of oculomotor reaction;

Rarely: delirium, euphoria, bucco-glossal syndrome, akinesia, depression of consciousness down to loss of consciousness, decreased reflexes, obsessive thoughts, malignant neuroleptic syndrome;

Rarely: speech disorder, convulsions.

Respiratory system

Often: shortness of breath, pneumonia;

Infrequently: nosebleeds, hiccoughs, laryngitis;

Rarely: hemoptysis, increased sputum discharge, dry nasal mucosa, pulmonary edema, pulmonary embolism, hypoxia, respiratory insufficiency, apnea.

Rarely: aspiration pneumonia.

Skin and subcutaneous tissue

Often: dry skin, itching, skin ulceration;

Infrequently: acne, vesicle-bullous (blister) rash, eczema, alopecia (alopecia), psoriasis, seborrhea;

Rarely: Maculopapular rash, exfoliative dermatitis, urticaria, hyperhidrosis.

Sense organs

Often: blurred vision, photophobia, pain in the ears;

Infrequently: dry eyes, eye pain, ringing in the ears, inflammation of the middle ear, cataracts, loss of taste, blepharitis;

Rarely: increased lacrimation, frequent blinking, external otitis media, amblyopia, deafness, diplopia, intraocular hemorrhages.

Genitourinary system

Infrequently: cystitis, frequent urination, leukorrhea, hematuria, dysuria, amenorrhea, premature ejaculation, vaginal bleeding, vaginal candidiasis, renal failure, uterine bleeding, menorrhagia, albuminuria, kidney stones, nocturia, polyuria, false urges to urinate;

Rarely: pain in the mammary gland, cervicitis, galactorrhea, anorgasmia, burning in the urethra and external genitalia, glucosuria, gynecomastia (enlargement of the mammary glands in men), painful erection;

Rarely: urinary incontinence, urinary retention, priapism.

Organism as a whole

Often: asthenia, fatigue, flu-like syndrome, sensation of trembling in the body;

Infrequently: peripheral edema, edema of the face, malaise, photosensitivity, maxillary pains, chills, stiffness of the jaws, bloating, tension in the chest;

Rarely: pain in the throat, stiffness in the back, heaviness in the head, candidiasis, sensation. compression in the throat, Mendelssohn's syndrome, heat stroke;

Rarely: leukopenia, neutropenia, thrombocytopenia, violations temperature regulation, pyrexia, pain in the chest, in the neck.

Metabolic disorders and disorders associated with diet

Often: decreased body weight;

Infrequently: dehydration, edema, hypercholesterolemia, hypokalemia, hyperlipidemia, hypoglycemia, thirst, increased urea in the blood, increased activity of alkaline phosphatase, iron deficiency anemia, increased lactate dehydrogenase activity, obesity;

Rarely: hyperkalemia, gout, hypernatremia, cyanosis, urine acidification;

Rarely: hyponatremia, increased activity of alanine aminotransferase, increased activity of aspartate aminotransferase, increased activity of creatine phosphokinase, anorexia, hyperglycemia, diabetic ketoacidosis, diabetic hyperosmolar coma.

Additional information on the side effects of the drug

Adverse events occurring during treatment with neuroleptics have also been observed with Abilifay®, including rare cases of malignant neuroleptic syndrome, as well as infrequent cases of development of tardive dyskinesia and convulsive seizures.

Sensitive patients in the first days of treatment may have symptoms of dystonia - prolonged pathological muscle spasms.

Symptoms of dystonia are: spasm of the neck muscles, sometimes with a feeling of constriction in the throat; difficulty in swallowing, shortness of breath and / or protrusion of the tongue. These symptoms may appear with the appointment of low doses of the drug, but they are more pronounced and more often the appointment of high doses of antipsychotics of the first generation.

Patients at high risk for developing dystonia are men and young people.

Overdose:

In clinical studies, a random or deliberate overdose of aripiprazole with a single dose of up to 1260 mg, not accompanied by a fatal outcome, has been described. Symptoms of an overdose: lethargy, increased blood pressure, drowsiness, tachycardia, loss of consciousness. In hospitalized patients, there were no clinically significant changes in the main physiological parameters, laboratory parameters and ECG.

Cases of overdose of aripiprazole in children (intake up to 195 mg) are described. Potentially dangerous symptoms of overdose include 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 carbon, symptomatic treatment, close medical supervision until all symptoms disappear.

Data on the use of hemodialysis in case of an overdose of aripiprazole are absent; The 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:

The mechanism of action of aripiprazole is associated with an effect on the central nervous system, which must be taken into account when combined with other drugs that have a central effect.

Having antagonistic action against alpha 1-adrenergic receptors, aripiprazole can enhance the effect of antihypertensive drugs.

Caution should be exercised with the simultaneous use of aripiprazole and drugs that cause lengthening of the interval QT - or violating the electrolyte balance.

Aripiprazole does not affect the pharmacokinetics and pharmacodynamics of warfarin, it does not displace warfarin from the connection with blood proteins.

The H2-histamine receptor blocker famotidine, causing a powerful oppression of the secretion of hydrochloric acid in the stomach, reduces the rate of absorption of aripiprazole, but this does not affect the clinical effect of aripiprazole.

Various routes of metabolism of aripiprazole are known; including with the participation of isoenzymes CYP2D6 and CYP3A4. In studies in healthy volunteers, potent inhibitors of isoenzymes CYP2D6 (quinidine) and CYP3A4 (ketoconazole) had an effect on the pharmacokinetics of aripiprazole, therefore, doses of aripiprazole should be reduced when used in various combinations with inhibitors - isoenzymes CYP3A4 and CYP2D6 (see section "Method of administration and dose"). With the simultaneous use of aripiprazole and weak inhibitors of isoenzymes CYP3A4 (diltiazem, escitalopram) or CYP2D6 we can expect a small increase in the concentration of aripiprazole in the blood.

Due to the fact that the isoenzyme CYP1A does not participate in the metabolism of aripiprazole, Smoking does not affect the pharmacokinetics and effect of aripiprazole.

When taking aripiprazole together with carbamazepine, a powerful inducer of "isoenzyme CYP3A4, the metabolism of aripiprazole is enhanced, so the dose of aripiprazole should be adjusted (see section "Method of administration and dose"). It is possible to expect a similar effect on other powerful inductors of isoenzymes CYP3A4 and CYP2D6.

In the metabolism of aripiprazole in vitro does not participate isoenzymes CYP1A1, CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19 and CYP2E1, in connection with which it is unlikely that it interacts with drugs and other factors (for example, smoking), capable of inhibiting or activating these enzymes.

Simultaneous administration of lithium or valproic acid with 30 mg of aripiprazole did not have a clinically significant effect on the pharmacokinetics of aripiprazole.

In clinical trials aripiprazole in doses of 10-30 mg / day had no significant effect on the metabolism of substrates of isoenzymes CYP2D6 (dextromethorphan), CYP2C9 (warfarin), CYP2C19 (omeprazole, warfarin) and CYP3A4 (dextromethorphan). Besides, aripiprazole and its main metabolite dehydroaripiprazole did not change the metabolism involving isoenzyme CYP1A2 in vitro. The clinically significant effect of aripiprazole on drugs metabolized with the participation of these isoenzymes is unlikely.

At simultaneous application of aripiprazole (10-30 mg / day) and lamotrigine (100-400 mg / day) in patients with bipolar disorder there were no changes in the pharmacokinetics of lamotrigine,therefore correction of its dose is not required. Aripiprazole had no effect on the pharmacokinetics of escitalopram and venlafaxine in healthy volunteers, therefore no dosage adjustments for these drugs are required while using aripiprazole at the same time.

When using aripiprazole in patients with major depressive disorder, no significant changes in the concentrations of antidepressants in plasma were detected simultaneously with fluoxetine (20-40 mg / day), paroxetine (37.5-50 mg / day) and sertraline (2-20 mg / day) .

The use of alcohol during treatment with aripiprazole may increase the sedative effect of the drug, so it should be avoided.

Special instructions:

Suicide attempts

The tendency to suicidal thoughts and attempts is typical for patients with psychosis, bipolar disorder and major depressive disorder, therefore, drug therapy should be combined with a thorough medical observation. The drug Abilifay® should be prescribed in a minimal amount sufficient to treat the patient; this will reduce the risk of overdose.

Admission of antidepressants, according to clinical studies, increases the risk emergence of suicidal thoughts and attempts in children, adolescents and young patients with depression and other mental disorders. Concerning should be especially careful when using antidepressants, including in the form of combination therapy with antidepressants and drug

Abilafay®, for the treatment of children, adolescents and young patients. Patients over 24 did not have an increase in suicidal thoughts and behavior under the influence of antidepressants, and in patients older than 65 there was a decrease in the incidence of this side effect.

Late dyskinesia

The risk of developing tardive dyskinesia increases with the duration of therapy with antipsychotics, therefore, if the symptoms of tardive dyskinesia appear on the background of Abilafia®, reduce the dose of this drug or cancel it. After the withdrawal of therapy, these symptoms may temporarily increase or even appear for the first time.

Malignant neuroleptic syndrome

In the treatment of neuroleptics, including aripiprazole, a life-threatening symptom complex is described,known as malignant neuroleptic syndrome (CNS). This syndrome manifests itself as hyperpyrexia, Muscular rigidity, mental disorders and instability of the vegetative nervous system (irregular pulse and arterial pressure, tachycardia, sweating and cardiac arrhythmias). In addition, sometimes there is an increase in the activity of creatine phosphokinase, myoglobinuria (rhabdomyolysis), and acute renal failure. In the case of symptoms of NSA or unexplained fever, all antipsychotics, including Abilifay®, should be withdrawn.

Convulsions

Like other antipsychotics, aripiprazole should be used with caution in patients with a history of seizures and the risk of their development.

Psychoses associated with senile dementia and Alzheimer's disease

In patients with psychoses due to senile dementia, the risk of a lethal outcome increases with the treatment of atypical neuroleptics. At psychoses in patients older than 65 years with Alzheimer's disease there were violations of the cardiovascular system: infarction, transient ischemic disturbance of cerebral circulation, including fatal outcome. The use of Abilfai® in psychoses due to senile dementia and in elderly patients with Alzheimer's disease is not recommended.

Hyperglycemia and diabetes mellitus

Hyperglycemia, in some cases expressed and accompanied by ketoacidosis or hyperosmolar coma with a fatal outcome, was noted in patients taking atypical antipsychotics. Although the association between the administration of atypical antipsychotics and hyperglycemic disorders remains unclear, patients who have diabetes mellitus should regularly determine the blood glucose concentration when taking atypical antipsychotics. Patients who have risk factors for diabetes (obesity, the presence of diabetes in the family history) with the admission of atypical antipsychotics should determine the concentration of glucose in the blood at the beginning of the course and periodically in the process of taking the drug. Patients taking atypical antipsychotics need constant monitoring of symptoms of hyperglycemia, including increased thirst, frequent urination, polyphagia, weakness; special attention should be given to patients with diabetes mellitus and risk factors for its development.

Leukopenia, neutropenia, agranulocytosis

It is known that neuroleptics, including Abilifay®, can cause temporary changes in the blood picture- leukopenia, neutropenia, as well as agranulocytosis. Risk factors are the low concentration of white blood cells in a patient prior to treatment, as well as those caused by other drugs; leukopenia and neutropenia. It is necessary to regularly monitor the blood picture in these patients, especially in the first months of treatment with Abilifay®. With a clinically significant decrease in the concentration of white blood cells of unclear etiology, consideration should be given to abolishing Abilifay®.

Careful monitoring of the condition of patients with clinically significant neutropenia should be undertaken to detect elevated temperature or other signs of infection in order to initiate appropriate treatment immediately. In severe neutropenia (the number of neutrophils is less than 1000 / mm³) treatment with Abilifay® is interrupted until the blood picture is normalized.

Cardiovascular diseases

In connection with the risk of development of orthostatic "hypotension aripiprazole should be apply with caution in patients with cardiovascular diseases (myocardial infarction, ischemic heart disease, heart failure, cardiac conduction disorders in the anamnesis),disorders of cerebral circulation or conditions predisposing. to arterial hypotension (dehydration, hypovolemia, antihypertensive therapy).

Cognitive and motor disorders

Like other antipsychotics, Abilifay® can cause cognitive and motor disorders. In particular, in clinical studies of the drug Abilifay ® there were cases of drowsiness and retardation. During treatment, patients should refrain from driving and dangerous mechanisms.

Violation of thermoregulation

It is known that neuroleptics can cause a violation of thermoregulation. This should be taken into account when prescribing Abilifai® to patients who have an increased risk of overheating due to intense physical load, high ambient temperature, the intake of drugs with m-cholinoblocking activity, dehydration.

Dysphagia

When using neuroleptics, cases of peristalsis of the esophagus and, as a consequence, aspiration pneumonia were noted.

Caution should be exercised when prescribing to patients with risk factors for the development of aspiration pneumonia.

The risk of developing venous thromboembolism

The use of neuroleptics, including Abilifay®, may be associated with a risk of venous thromboembolism. In this regard, the risk factors for the development of this complication should be identified before the appointment of Abilifay®, as well as during treatment with this drug. If necessary, measures should be taken to prevent the development of venous thromboembolism.

Effect on the ability to drive transp. cf. and fur:

As with the appointment of other neuroleptics, with the appointment of aripiprazole the patient should be warned about the dangers of working with moving machinery and driving.

Form release / dosage:Tablets 5 mg, 10 mg, 15 mg, 30 mg.

Packaging:

7 tablets per blister AI/A1, laminated with polyamide film and PVC.

For 4 blisters together with instructions for use in a pack of cardboard.

Storage conditions:

At a temperature of 15 to 30 ° C in a dry place.

Keep out of the reach of children.

Shelf life:

3 years

Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-001812

Date of registration:06.08.2010/21.01.2014

Date of cancellation:2016-12-09

The owner of the registration certificate:Bristol-Myers Squibb CompanyBristol-Myers Squibb Company USA

Manufacturer: & nbsp

BRISTOL-MYERS SQUIBB Manufacturing Company Puerto Rico

Representation: & nbspBRISTOL-Majers SKVIBB, LLCBRISTOL-Majers SKVIBB, LLCRussia

Information update date: & nbsp16.01.2017

Illustrated instructions

Instructions

Abilifay® (Abilify®)