Amdoal

Amdoal – drug with antipsychotic, antipsychotic action.

Form of release and structure

Amdoal release in the form of tablets: almost white or white color, round, biconvex, on one party an engraving (depending on a dosage of 10/15/20/30 mg) "N74", "N75", "N76" or "N77" (on 15 pieces in blister strip packagings, on 1-2 packagings in a cardboard pack).

Structure of 1 tablet:

• Active agent: арипипразол – 10, 15, 20 or 30 mg;
• Auxiliary components (10/15/20/30 mg respectively): microcrystallic cellulose – 10/15/20/30 mg, monohydrate of lactose – 63,077/94,615/126,153/189,23 mg, a hypro rod – 3,8/5,7/7,6/11,4 mg, corn starch – 6,983/10,475/13,967/20,95 mg, magnesium stearate – 1,14/1,71/2,28/3,42 mg.

Indications to use

• Schizophrenia at adults (treatment);
• Maniacal episodes within bipolar disorder of the I type (treatment) and maniacal episodes at patients who have instructions in anamnestic data on maniacal episodes and the clinical response to therapy aripiprazoly (prevention).

Contraindications

Absolute:

• Senile dementia;
• Lactose intolerance, deficit of lactase, glyukozo-galaktozny malabsorption;
• Period of chest feeding;
• Age up to 18 years;
• Hypersensitivity to drug components.

Relative (Amdoal appoint with care in the presence of the following diseases / states):

• States which contribute to a lowering of arterial pressure, including dehydration, a hypovolemia, reception of hypotensive drugs (because of probability of developing of orthostatic hypotension);
• Diseases of cardiovascular system (coronary heart disease, including the postponed myocardial infarction, chronic heart failure, conductivity disturbances);
• Epilepsy;
• Diseases at which development of spasms is possible;
• Cerebrovascular diseases;
• The increased risk of development of a hyperthermia, for example, during the overheating, dehydration, intensive exercise stresses, reception of funds from m-holinoblokiruyushchey activity (because of probability of disturbance of thermal control);
• The increased risk of development of aspiration pneumonia (because of probability of disturbance of motor function of a gullet and aspiration);
• Diabetes mellitus in the anamnesis;
• Obesity;
• Pregnancy (due to the lack of well controlled and adequate researches; Amdoal's appointment is possible in cases when the expected advantage for health of mother is higher than possible risk for a fruit; about pregnancy approach, and also it is necessary to notify the doctor on its planning).

Route of administration and dosage

Amdoal accept inside. Does not accord meal on efficiency of drug of influence.

Frequency rate of reception – once a day.

The recommended mode of dosing (daily dose):

• Schizophrenia (treatment): an initial dose – 10-15 mg, supporting – 15 mg, maximum – 30 mg. Amdoal is effective in doses of 10-30 mg. Use over 15 mg a day can be required by some patients though increase in efficiency of a dose more than 15 mg a day is not proved;
• Maniacal episodes at bipolar disorder (treatment): an initial dose – 15 mg, maximum – 30 mg. In certain cases purpose of higher doses can be required. Drug is appointed as monotherapy or along with other medicines;
• Maniacal episodes at bipolar disorder of the I type (prevention): Amdoal appoint in the same doses which were applied at treatment. Carrying out dose adjustment is defined by a condition of the patient.

The patient with a renal/liver failure, and also to patients of advanced age the mode of dosing is not adjusted.

At a renal failure in heavy degree it is necessary to appoint a daily dose of 30 mg with care.

When carrying out a combination therapy it is necessary to consider:

• Powerful inhibitors of isoenzymes of CYP2D6 or CYP3A4: Amdoal's dose needs to be reduced twice; after their cancellation the dose needs to be increased. Change of the mode of dosing is not required at purpose of drug as auxiliary treatment at big depressive frustration;
• CYP3A4 isoenzyme inductors: Amdoal's dose needs to be increased twice; further increase is possible on the basis of clinical indications; after their cancellation the dose is reduced.

At purpose of several medicines inhibiting isoenzymes of CYP2D6 and CYP3A4 it is necessary to consider the possibility of reduction of a daily dose of Amdoal.

Side effects

Nausea and akathisia belong to number of the most often registered side effects (at more than 3% of patients).

Other possible disturbances (> 10% – are very frequent;> 1% and <10% – is frequent;> 0,1% and <1% – infrequently;> 0,01% and <0,1% – are rare; <0,01% – are very rare):

• Cardiovascular system: infrequently – orthostatic hypotension, tachycardia;
• Nervous system: often – sedation, a tremor, extrapyramidal frustration, an akathisia, drowsiness, dizziness, a headache;
• Alimentary system: often – vomiting, dyspepsia, a lock, nausea, hypersalivation;
• Organ of sight: often – a sight illegibility;
• Mentality: often – sleeplessness, alarm, concern; infrequently – a depression;
• Others: often – fatigue.

At treatment of schizophrenia, maniacal episodes and bipolar disorder of the I type by Amdoal the frequency of emergence of extrapyramidal symptoms (EPS) is less, than at the patients receiving a haloperidol, and same, as at the patients receiving olanzapine. Frequency of development of EPS in the patients receiving арипипразол at therapy of bipolar disorder of the I type and maniacal episodes is higher in comparison with group of treatment with use of drugs of lithium.

By results of carrying out post-marketing observations the following side reactions were recorded (with an unspecified frequency of development):

• Nervous system: malignant antipsychotic syndrome, disturbance of the speech, epileptic seizures;
• Endocrine system: diabetic ketoosmolyarny coma, diabetes mellitus, hypercalcemia, diabetic ketoacidosis;
• Cardiovascular system: ventricular arrhythmia, increase in arterial pressure, lengthening of an interval of QT, a stenocardia attack, sudden death for the unknown reason, polymorphic ventricular tachycardia like "pirouette", a faint, bradycardia, a thrombembolia of veins (including a deep vein thrombosis and a thromboembolism of branches of a pulmonary artery);
• Gepatobiliarny system: hepatitis, jaundice, increase in activity gamma глутамилтрансферазы, aspartate aminotransferases, alaninaminotranspherases, alkaline phosphatase;
• Urinary system: urination delay, urine incontience;
• Hemopoietic system: neutropenia, leukopenia, thrombocytopenia;
• Alimentary system: pancreatitis, discomfort in a stomach/stomach, a dysphagy, diarrhea;
• Reproductive system and mammary glands: priapism;
• Skeletal and muscular system and connecting fabric: mialgiya, рабдомиолиз, rigidity;
• Respiratory system: laryngospasm, oropharyngeal spasm, aspiration pneumonia;
• Immune system: allergic reactions (puffiness of the person, urticaria, a skin itch, anaphylactic reactions, a Quincke's disease, including hypostasis and inflation of language);
• Skin and hypodermic cellulose: rash, alopecia, photodermatosis, hyperhidrosis;
• Metabolism and food: anorexia, hyponatremia, change (increase/decrease) of body weight;
• Mentality: nervousness, agitation, suicide thoughts / attempts, perfect suicide;
• Laboratory researches: increase in activity of a kreatinfosfokinaza, fluctuation/increase in concentration of glucose of blood, increase in concentration of glikozilirovanny hemoglobin;
• Pregnancy, puerperal period, perinatal states: Amdoal withdrawal at newborns;
• Others: disorders of temperature regulation (pyrexia, hypothermia), stethalgias, peripheral hypostases.

Special instructions

Improvement of a state at Amdoal's use can demand several days in this connection patients have to be under fixed observation.

Tendency, characteristic of psychoses, to suicide attempts / thoughts can arise in short terms after the beginning of therapy or change of drug. The condition of such patients demands careful observation.

In the presence of disturbances from cardiovascular system performing therapy demands care. Because of probability of development of vein thromboses, at the contributing factors to developing of a thrombembolia of veins before Amdoal's appointment it is necessary to conduct careful examination of patients, and also to carry out preventive measures during therapy. In the presence of instructions in the family anamnesis on lengthening of an interval of QT it is necessary to be careful.

The probability of developing of late dyskinesia increases with the drug use duration therefore at emergence during therapy of symptoms of late dyskinesia it is necessary to lower a dose or to cancel treatment. After Amdoal's cancellation these symptoms can is passing to amplify or even for the first time to appear.

At treatment by Amdoal the life-threatening malignant antipsychotic syndrome can develop (the main symptoms: disturbances of mentality, muscular rigidity, a hyper pyrexia, instability of the autonomic nervous system, including instability of arterial pressure / pulse, arrhythmia, perspiration, tachycardia). At emergence of signs of a malignant antipsychotic syndrome or inexplicable fever therapy is cancelled.

At Amdoal's appointment patients in the anamnesis or in the presence of frustration at which they can develop need to be careful with convulsive attacks.

It is not necessary to use drug at treatment of neurosis tardas as at the same time the risk of development of cerebrovascular complications and mortality increases.

Patients with a diabetes mellitus during therapy need to define regularly concentration of glucose in blood. With risk factors of development of a diabetes mellitus (the diabetes mellitus in the family anamnesis, obesity) should be defined concentration of glucose in blood at the beginning of a course, and also periodically in the course of Amdoal's reception. During treatment it is necessary to control constantly hyperglycemia symptoms, including weakness, the speeded-up urination, the increased thirst, a polyphagia.

Administration of drug can lead to aspiration and disturbance of motility of a gullet. With risk of development of aspiration pneumonia Amdoal appoint with care.

During therapy it is necessary to be careful when working, demanding from sick bystry psychomotor reactions and high concentration of attention.

Medicinal interaction

At the combined use of Amdoal with some medicinal means / substances the following effects can be observed:

• Some anti-hypertensive means: strengthening of their effect (because of antagonism of an aripiprazol to α1-адренорецепторам);
• The alcohol, drugs influencing the central nervous system: strengthening of side effects (the combination demands care);
• Drugs which can cause lengthening of an interval of QT: strengthening of side effects (the combination demands care);
• Inhibitors of isoenzymes CYP3A4 (итраконазол and HIV protease inhibitors) and CYP2D6: decrease in clearance of an aripiprazol (reduction of a dose of Amdoal is required, after cancellation of a combination therapy the dose is increased to initial);
• Carbamazepine and other powerful inductors of isoenzymes CYP3A4 (phenobarbital, rifampicin, Phenytoinum, рифабутин, Primidonum, not Virapinum, эфавиренз, the St. John's Wort which is made a hole) and CYP2D6: decrease in the maximum and total concentration of an aripiprazol in blood (Amdoal's dose needs to be increased twice, after cancellation of a combination therapy to lower a dose to recommended).

Terms and storage conditions

To store in protected from light, the place, dry, unavailable to children, at a temperature up to 30 °C.

Period of validity – 3 years.