Абилифай

Абилифай – antipsychotic means (neuroleptic).

Form of release and structure

• Tablets of 5 mg: blue color, a rectangular shape with the rounded edges, on one of the parties of marking of "A-007" and "5", with a facet (on 7 pieces in blisters, in a pack of cardboard 2, 4, 7, 8 or 14 blisters);
• Tablets of 10 mg: pink color, a rectangular shape with the rounded edges, on one of the parties of marking of "A-008" and "10", with a facet (on 7 pieces in blisters, in a pack of cardboard 2, 4, 7, 8 or 14 blisters);
• Tablets of 15 mg: yellow color, a round form, on one of the parties of marking of "A-009" and "15", with a facet (on 7 pieces in blisters, in a pack of cardboard 2, 4, 7, 8 or 14 blisters);
• Tablets of 20 mg: color, white or white with a yellowish shade, a round form, on one of the parties of marking of "A-010" and "20", with a facet (on 7 pieces in blisters, in a pack of cardboard 2, 4, 7, 8 or 14 blisters);
• Tablets of 30 mg: pink color, a round form, on one of the parties of marking of "A-011" and "30", with a facet (on 7 pieces in blisters, in a pack of cardboard 2, 4, 7, 8 or 14 blisters);
• Solution for intramuscular introduction: transparent, colourless, without visible mechanical inclusions (on 1,69 ml in the colourless glass bottles corked by a rubber bung and an aluminum cap under a running in and a protective plastic cover in a pack a cardboard 1 bottle).

Active agent – арипипразол:

• 1 tablet – 5, 10, 15, 20 or 30 mg;
• 1 bottle – 10 mg (this amount of active ingredient contains in 1,33 ml of solution, however the full volume of solution in 1 bottle makes 1,69 ml – such packing is made taking into account a rebookmark that is required for the guaranteed receiving a necessary dose after solution extraction).

Excipients of tablets: magnesium stearate, corn starch, cellulose microcrystallic, lactoses monohydrate, hydroxypropyl cellulose, and also dyes: in tablets of 5 mg – a varnish aluminum blue, in mg tablets 10 and 30 – ferrous oxide red, in tablets of 15 mg – ferrous oxide yellow.

Solution excipients: water for injections, sodium hydroxide, the tartaric acid granulated R-tsiklodekstrina sulfobutyl ether (Каптисол®).

Indications to use

For tablets:

• Bad attacks of schizophrenia and maintenance therapy;
• Acute maniacal episodes of bipolar disorder of the I type and maintenance therapy at the patients with this disease who recently transferred the maniacal or mixed episode.

In the form of solution of Abilifay it is applied to bystry stopping of acute conditions of excitement and behavioural disturbances at patients with schizophrenia and maniacal episodes at bipolar disorder of the I type when there is no impossibility of administration of drug inside.

Contraindications

• Age up to 18 years;
• Lactation;
• Hypersensitivity to any component of drug.

With care:

• Cardiovascular diseases (coronary heart disease, heart failure, conductivity disturbances, the postponed myocardial infarction);
• The cerebrovascular diseases and states contributing to development of hypotension (a hypovolemia, dehydration, reception of anti-hypertensive drugs);
• Convulsive attacks and diseases at which spasms are possible;
• The increased risk of a hyperthermia (for example, overheating, dehydration, intensive exercise stresses, reception of anticholinergic drugs);
• Existence of risk of development of aspiration pneumonia;
• Obesity and diabetes at close relatives;
• Pregnancy (during this period drug is appointed only in extreme cases if the potential advantage exceeds possible risks).

Route of administration and dosage

Tablets
In this dosage form drug should be accepted inside regardless of meal.

The recommended doses:

• Schizophrenia: an initial dose – 10 or 15 mg of 1 times a day, a maintenance dose – 15 mg of 1 times a day. According to data of clinical trials, drug is effective in daily doses from 10 to 30 mg;
• Maniacal episodes at bipolar disorder: an initial dose – 15 or 30 mg of 1 times a day. If necessary the dose is changed with the minimum intervals of 24 hours. According to data of clinical trials, drug is effective in daily doses from 15 to 30 mg at reception within 3-12 weeks.

Solution for intramuscular introduction in oil
In this dosage form of Abilifay apply a short course at impossibility of administration of drug inside.

Solution is entered intramusculary – deeply into a big buttock or deltoid muscle, avoiding zones with the expressed hypodermic fatty tissue.

The initial dose makes 10 mg (contents of 1 bottle) in the form of a single injection. Effective single doses depending on circumstances are in range from 5,25 to 15 mg. The doctor can appoint the reduced dose (5,25 mg) on the basis of assessment of the general clinical condition of the patient taking into account the drugs which are already appointed to it for the supporting or emergency treatment. If necessary in 2 hours do the second injection. Within 24 hours it is not necessary to appoint more than 3 injections.

As soon as becomes possible, the patient is transferred to the tableted form of Abilifaya.

The most admissible daily dose makes 30 mg, at the same time it is necessary to consider all applied dosage forms of drug – solution and tablets.

At patients 65 years are more senior there is an increased risk of development of side effects therefore the doctor has to consider a question of decrease in an initial dose.

Dose adjustment of drug is required at simultaneous use of some other drugs. In case of the combined appointment with powerful inhibitors of isoenzymes of CYP3A4 and CYP2D6 the dose of an aripiprazol is reduced, after their cancellation – again increased. At the combined use with powerful inductors of an isoenzyme CYP3A4 the dose of an aripiprazol is increased, after cancellation of the inductor the dose is reduced.

Side effects

Classification of side effects:

• Very often:> 10%;
• Often:> 1% and <10%;
• Infrequently:> 0,1% and <1%;
• Seldom:> 0,01% and <0,1%;
• Very seldom: <0,01%.

Possible side effects:

• From cardiovascular system: often – tachycardia, orthostatic hypotension; infrequently – heartbeat, bradycardia, myocardium ischemia, AV blockade, heart failure, hemorrhages, lengthening of QT of an interval, fibrillation of auricles, premature ventricular contraction, phlebitis, a deep vein thrombosis, a myocardial infarction, a cardiac standstill; seldom – an atrial flutter, a cardiomegaly, intracranial bleeding, thrombophlebitis, a vazovagalny syndrome, brain ischemia; very seldom – faints;
• From the alimentary system: very often – appetite loss, nausea; often – dyspepsia, a lock, vomiting; infrequently – an ulitis, tooth caries, the complicated swallowing, a paraglossa, stomatitis, candidiasis of a mucous membrane of a mouth, an ulceration in a mouth, increase in appetite, gastritis, a meteorism, an eructation, a gastroenteritis, an incontience a calla, a gastroesophagal reflux, colitis, cholecystitis, periodontal abscess, stomach ulcer, a fekaloma, gastrointestinal hemorrhages, rectal hemorrhages, hemorrhoids, cholelithiasis; seldom – a language inflammation, bleeding of gums, a cheilitis, pancreatitis, an esophagitis, intestinal bleedings, an intestines perforation, a hematemesis, a duodenum ulcer, increase in a liver, hepatitis; very seldom – increase in activity of aspartate aminotransferase (nuclear heating plant) and alaninaminotranspherase (ALT);
• From immune system: very seldom – allergic reactions (an itch, urticaria, a Quincke's disease, an anaphylaxis);
• From a musculoskeletal system: often – spasms, a mialgiya; infrequently – a joint pain and bones, spasms, muscular weakness, arthritis, a bursitis, arthrosis, a myasthenia; very seldom – the tendinitis, a myopathy, a pseudorheumatism, tendobursit, рабдомиолиз, increase in activity of a kreatinfosfokinaza;
• From a nervous system: very often – drowsiness or sleeplessness; often – an extrapyramidal syndrome, a cogwheel syndrome (resistance to performance of passive movements), nervousness, psychomotor excitement, hostility, a tremor, dizziness, maniacal thoughts, confusion of consciousness, the increased salivation, a depression, staggering gait, suicide thoughts; infrequently – a bradykinesia, easing of concentration of attention, muscular twitchings, paresthesia, dystonia, a tremor of extremities, a stupor, memory easing, dyskinesia, apathy, amnesia, panic reactions, an akathisia (a syndrome of "uneasy legs"), the suppressed mood, dyskinesia, depersonalization, a myoclonus, delay of cogitative function, a hyperactivity, hypotonia, reinforced reflexes, disturbance of oculomotor reaction, hypersensitivity to irritants, the lowered/raised libido, impotence, a stroke; seldom – reduced reflexes, an akineziya, a bukkoglossalny syndrome, nonsense, the notions of compulsion, euphoria, a malignant antipsychotic syndrome, oppression of consciousness up to a loss of consciousness;
• From respiratory system: often – short wind, pneumonia; infrequently – a hiccups, nasal bleeding, laryngitis, asthma; seldom – the strengthened expectoration, a pneumorrhagia, a xeromycteria, respiratory insufficiency, a hypoxia, aspiration pneumonia, a pulmonary embolism, a fluid lungs, an apnoea;
• From urinogenital system: often – an urine incontience; infrequently – desires to an urination, a delay of an urination or the speeded-up urination, cystitis, a dysuria, a renal failure, a polyuria, a nocturia, stones in kidneys, an albuminuria, a hamaturia, a leukorrhea, a menorrhagia, an amenorrhea, vaginal candidiasis, vulval bleeding, uterine bleeding, a premature ejaculation; seldom – burning in the field of urinogenital system, a cervicitis, an urolithiasis, a galactorrhoea, a mammary gland pains, a glycosuria, an anorgazmiya, a painful erection, a gynecomastia at men;
• From integuments: often – the increased perspiration, an itch, a xeroderma, skin ulcerations; infrequently – vezikulobullezny rash, psoriasis, an alopecia, eczema, an acne, seborrhea; seldom – urticaria, exfoliative dermatitis, makulopapulezny rash;
• From sense bodys: often – ear pain, conjunctivitis; infrequently – eye pain, a xerophthalmus, a cataract, a blepharitis, an inflammation of a middle ear, a ring in ears, taste loss; seldom – outside otitis, deafness, the strengthened dacryagogue, a diplopia, an amblyopia, photophobia, a frequent blinking, eye hemorrhages;
• From a metabolism and food: often – increase in level of a kreatinfosfokinaza, loss of weight; infrequently – a hyperglycemia, a hypercholesterolemia, a hypopotassemia, hypostasis, dehydration, thirst, a hypoglycemia, a diabetes mellitus, an iron deficiency anemia, a hyponatremia, a lipidemia, obesity, increase in an alkaline phosphatase, creatinine, a lactate dehydrogenase, level of nuclear heating plant and ALT, urea in blood; seldom – a hypernatremia, hypoglycemic reaction, a hyperpotassemia, urine acidulation, cyanosis, gout;
• Others: often – a grippopodobny syndrome, thorax pains and/or in a neck, peripheral hypostasis; infrequently – an indisposition, a fever, constraint of jaws, maxillary pains, a face edema, abdominal distention, pains in the field of a basin, a photosensitivity, tension in a breast; seldom – weight in the head, a pharyngalgia, constraint in spin and in a throat, heatstroke, Mendelssohn's syndrome, candidiasis.

Special instructions

Solution of Abilifay is not intended for hypodermic and intravenous administration.

During treatment it is necessary to refrain from alcohol intake, driving and performance of potentially dangerous types of works.

Medicinal interaction

Powerful CYP2D6 inhibitors (for example, quinidine) and CYP3A4 (for example, кетоконазол) reduce clearance of an aripiprazol at intake respectively by 52% and 38%. For this reason in need of use of a similar combination it is necessary to lower a dose of Abilifaya.

Carbamazepine – the powerful inductor CYP3A4 – reduces concentration of an aripiprazol and its active metabolite of a degidroaripiprazol. Similar reaction can be expected at simultaneous use of other powerful inductors CYP2D6 and CYP3A4.

Aripiprazol shows antagonism to _{alfa1-adrenoceptors} therefore it is supposed that it can strengthen effect of hypotensive drugs.

It is necessary to be careful at simultaneous use of drugs which can break electrolytic balance or extend QT interval, and also with other medicines influencing the central nervous system.

At the combined use with benzodiazepines (for example, lorazepam) the risk of strengthening of sedation and development of orthostatic hypotension increases.

Terms and storage conditions

To store at a temperature of 15-25 ºС in dry, protected from light and the place, unavailable to children.

Period of validity:

• Tablets – 3 years;
• Solution – 2 years.