Abilify tablets 15 mg №28

Description for the ABILIFY 15 mg tablets:

General Characteristics:

International name: aripiprazole (aripiprozole) 7 - [4 - [4 - (2,3-dihlorofenil)-1-piperazinyl] butoxy] -3,4-dihydro-2 (1H)-hinolinon;

basic physical and chemical properties:

- 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 and marked "A-008" and "10" on one side;

- Tablets 15 mg: round yellow pill with beveled, labeled "A-009" and "15" on one side;

- Tablets 30 mg: round pink tablets, with a facet, labeled "A-011" and "30" on one side.

Ingredients 1 tablet contains 5 mg or 10 mg or 15 mg or 30 mg of aripiprazole;

Excipients: lactose, microcrystalline cellulose, corn starch, gidroksipropiltselyuloza, magnesium stearate, colors: yellow iron oxide (tablet 15 mg), iron oxide red (tablet 10 mg and 30 mg), lacquer aluminum blue (5 mg tablets).

Tablets.

Pharmacotherapeutic group.

Antipsychotic (neuroleptic). ATC code N05AX12

Pharmacological properties.

Pharmacological

The therapeutic effect of aripiprazole in schizophrenia due to a combination of partial agonist activity on D2 dopamine and serotonin 5HT1a receptors and antagonist activity on 5HT2 serotonin receptor.

Aripiprazole has a high affinity in vitro to the D2 and D3 dopamine receptors, 5HT1a 5HT2a and serotonin receptors and moderate affinity for dopamine D4, 5HT2c and 5HT7 serotonin receptor, alpha 1-adrenergic receptors and H1 histamine receptors. Aripiprazole is also characterized by a moderate affinity for serotonin reuptake sites and the lack of affinity for muscarinic receptors. Aripiprazole in animal experiments showed antagonism against dopaminergic hyperactivity and agonism for dofaminergichenoi gipoaktivnosti. Interaction not only with dopamine and serotonin receptors may explain some of the clinical effects of aripiprazole.

Pharmacokinetics

Activity Abilifayu due to active substance - aripiprazola.Sredny half-life of aripiprazole is about 75 chasov.Ravnovesnaya concentration is reached after 14 days. Cumulation of the drug after repeated admission to predict. Indicators of the pharmacokinetics of aripiprazole at steady state are proportional to dose. There was no diurnal variation of distribution of aripiprazole and its metabolite degidroaripiprazolu. Established that the main metabolite of the drug in human plasma degidroaripiprazola has the same affinity for D2 dopamine receptors, as aripiprazole.

Aripiprazole is rapidly absorbed after ingestion Abilifayu, with maximum plasma concentrations achieved within 3-5 hours. The absolute bioavailability of tablets Abilifayu is 87%. Meal on the bioavailability of aripiprazole is not affected.

At therapeutic concentrations, more than 99% of aripiprazole binds to serum proteins, primarily albumin. Aripiprazole undergoes presystemic metabolism only minimally. Aripiprazole is metabolized by the liver in three ways: dehydrogenation, hydroxylation, and N-dezalkiliruvannyam. According to the experiments in vitro, dehydrogenation and hydroxylation of aripiprazole occurs under the action of enzymes CYP3A4 and CYP2D6, and N-dezalkilyuvannya catalyzed by the enzyme CYP3A4. Aripiprazole is a major component of the drug in the blood. At the equilibrium state of the area under the curve "concentration of the drug - the time» (AUC) degidroaripiprazola is approximately 39% AUC of aripiprazole in plasma.

After a single dose of labeled [14C] aripiprazole about 27% and 60% of the radioactivity is determined in the urine and feces, respectively. Less than 1% of unchanged aripiprazole is determined in the urine and approximately 18% of the dose in unchanged form excreted in the feces. The total clearance of aripiprazole is 0.7 ml / min / kg, mainly due to liver removal.

Indications Treatment of acute episodes of schizophrenia and for maintenance therapy in patients with schizophrenia.

Treatment of acute manic episodes of bipolar disorder type I and for maintenance therapy in patients with bipolar disorder type I, which before that suffered a manic or mixed episode.

Dosing and Administration

Schizophrenia

It is recommended that Abilifay the initial dose of 10 or 15 mg once a day, regardless of the meal. Maintenance dose is 15 mg / day. In clinical studies, the effectiveness of the drug in doses ranging from 10 to 30 mg / day.

Manic episodes in bipolar disorder

Abilifay should be taken once a day regardless of the meal, beginning with a dose of 15 or 30 mg / day. Changing the dose, if necessary, should be conducted at intervals of not less than 24 hours. In clinical studies demonstrated efficacy at doses of 15-30 mg / day with a manic episode at the reception for 3-12 weeks. Safety of doses above 30 mg / day in clinical trials has not been evaluated.

When monitoring patients with bipolar disorder type I manic or mixed episodes in which no symptoms while taking Abilifayu (15 mg or 30 mg / d at an initial dose of 30 mg / day) for 6 weeks, a maintenance therapy should be considered effective. You should periodically examine the patient to determine the need for continued maintenance therapy.

Do not want to change the dosage of the drug in the appointment of his patients with renal / hepatic failure (class A, B and C by Child-Pugh classification).

Although the experience of the drug in patients over 65 years is limited, dose adjustment for these patients is required.

Side effects.

The frequency of side effects is given in accordance with the following scale: very rare (≤ 0,01%), rare (≥ 0,01% and <0.1%): Rare (≥ 0,1% and <1%), frequent ( ≥ 1% and <10%), very frequently (≥ 10%)

Circulatory system

Very rare - a faint, rarely - vasovagal syndrome, the expansion of the heart, atrial flutter, thrombophlebitis, intracranial hemorrhage, cerebral ischemia, rarely - bradycardia, palpitations, myocardial infarction, QT interval prolongation, cardiac arrest, hemorrhage, atrial fibrillation, heart failure, AV blockade, myocardial ischemia, deep vein thrombosis, phlebitis, premature beats frequent: orthostatic hypotension, tachycardia.

Digestive

Very rare: increased activity of alanine aminotransferase (ALT) and aspartate aminotransferase (AST), rarely - esophagitis, bleeding gums, glossitis, hematemesis, intestinal bleeding, duodenal ulcer, cheilitis, hepatitis, liver enlargement, pancreatitis, intestinal perforation, rare - increased appetite, gastroenteritis, difficulty swallowing, flatulence, gastritis, dental caries, gingivitis, hemorrhoids, gastroesophageal reflux, gastrointestinal hemorrhage, periodontal abscess, swelling tongue, fecal incontinence, colitis, rectal hemorrhage, stomatitis, mouth ulcers, cholecystitis , fekaloma, candidiasis of the mucous membranes of the mouth, gallstone disease, flatulence, gastric ulcer, frequent: dyspepsia, vomiting, constipation, very often - nausea, loss of appetite.

Immune system

Very rare - allergic reactions (anaphylaxis, angioedema, pruritus and urticaria).

Musculoskeletal system

Very rarely - increased activity of creatine kinase, rhabdomyolysis, tendonitis, tendobursit, rheumatoid arthritis, myopathy, rarely - a pain in the joints and bones, myasthenia gravis, arthritis, arthrosis, muscle weakness, cramps, bursitis, and often - myalgia, muscle cramps.

Nervous system

Rare: delirium, euphoria, bukkoglossalny syndrome, akinesia, depression of consciousness until he lost consciousness, decreased reflexes, obsessive thoughts, neuroleptic malignant syndrome, infrequent: dystonia, muscle twitching, weakening of concentration, paresthesia, tremor of limbs, impotence, bradykinesia, reduced / increased libido, panic reaction, apathy, dyskinesia, weakening of memory, stupor, amnesia, stroke, hyperactivity, depersonalization, the syndrome of "restless legs (akathisia), myoclonus, depressed mood, increased reflexes, slowing of mental function, increased sensitivity to stimuli, hypotension , violations of the oculomotor response, frequent: dizziness, tremor, extrapyramidal symptoms, psychomotor agitation, depression, nervousness, excessive salivation, hostility, suicidal thoughts, manic thoughts, staggering, confusion, resistance to the implementation of passive motion (cogwheel sign) is very frequent : insomnia, somnolence, akathisia.

Respiratory System

Rare: hemoptysis, aspiration pneumonia, increased sputum, dryness of the nasal mucosa, pulmonary edema, pulmonary embolism, hypoxia, respiratory failure, sleep apnea; infrequently - asthma, epistaxis, hiccup, laryngitis, frequent: dyspnea, pneumonia.

Skin

Rare: maculopapular rash, exfoliative dermatitis, urticaria; infrequent: acne, vezikulobulozni (bubbly), rashes, eczema, alopecia (hair loss), psoriasis, seborrhea, and often - dry skin, itching, sweating, skin ulcer.

Sense organs

Rare: increased lacrimation, frequent blinking, otitis externa, amblyopia, deafness, diplopia, eye hemorrhage, photophobia, rarely - dry eyes, eye pain, tinnitus, otitis media, cataracts, loss of taste, blepharitis; frequent: con ' conjunctivitis, ear pain.

Genitourinary System

Rare: breast pain, cervicitis, galactorrhea, anorgasmia, burning sensation in the urinary system, glycosuria, gynecomastia (breast enlargement in men), urolithiasis, painful erections; infrequent: cystitis, frequent urination, Leucorrhoea, urinary retention, hematuria, dysuria, amenorrhea, premature ejaculation, vaginal bleeding, vaginal candidiasis, renal failure, uterine bleeding, menorrhagia, albuminuria, kidney stones, nocturia, polyuria, urge to urinate, often - incontinence.

Organ