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Pharmacokinetics

Activity due to the active substance Abilifayu - aripiprazole. Average half-life of aripiprazole is approximately 75 hours. The equilibrium concentration is reached after 14 days. Drug accumulation with repeated admission predictable. Indicators pharmacokinetics of aripiprazole at steady state is proportional to dose. There was no diurnal variation of distribution of aripiprazole and its metabolite degidroaripiprazolu. Found that the main metabolite of the drug in human plasma degidroaripiprazola, has the same affinity for the D2 dopamine receptor, as aripiprazole.

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Aripiprazole is rapidly absorbed after oral Abilifayu, with maximum plasma concentrations achieved within 3-5 hours. The absolute bioavailability of tablets Abilifayu 87%. Meal on the bioavailability of aripiprazole does not affect. At therapeutic concentrations of more than 99% of aripiprazole bound to serum proteins, mainly to albumin. Aripiprazole undergoes first-pass metabolism only minimally. Aripiprazole is metabolized in 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 drug in the blood. At steady state area under the curve "drug concentration - time´┐Ż (AUC) degidroaripiprazola is approximately 39% AUC of aripiprazole in plasma. After a single dose of labeled [14C] aripiprazole 27% and 60% of the radioactivity determined in the urine and feces, respectively. Less than 1% of unchanged aripiprazole determined in the urine and about 18% of the dose in unchanged form excreted in the feces. Total clearance of aripiprazole is 0.7 ml / min / kg, mainly due to launch liver.

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Indications. Treatment of acute episodes of schizophrenia and for maintenance therapy in patients with schizophrenia.
Treatment of acute manic episodes of bipolar I disorder and for maintenance therapy in patients with bipolar I disorder, which before it was moved a manic or mixed episode.

Dosage and administration.

Schizophrenia

Recommended for use in Abilifay initial dose of 10 or 15 mg once a day with or without food. The maintenance dose is 15 mg / day. In clinical trials, the effectiveness of the drug in doses of 10 to 30 mg / day.

Manic episodes in bipolar disorder

Abilifay should be taken once a day with or without food, starting with a dose of 15 or 30 mg / day. Changing the dose, if necessary, should be performed at least 24 hours. In clinical studies demonstrated the effectiveness of the drug in doses of 15-30 mg / day in manic episodes when administered within 3-12 weeks. Safety of doses above 30 mg / day in clinical studies has not been evaluated.

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In the observation of patients with bipolar I disorder and manic or mixed episodes in which no symptoms while taking Abilifayu (15 mg / day or 30 mg / day at an initial dose of 30 mg / day) for 6 weeks, a maintenance therapy should be considered as effective. Periodically examine patients to determine the need for continued maintenance. Do not want to change the dosage of the drug in the appointment of his patients with renal / hepatic insufficiency (class A, B and C according to Child-Pugh classification). Although experience with the drug in patients older than 65 years is limited, dose adjustment for these patients is needed.

Side effect. generic abilify

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%), common ( 1% and <10%), very common ( 10%)

Circulatory system

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

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

Immune system

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

Musculoskeletal

Very rarely - increased activity of creatine phosphokinase, rhabdomyolysis, tendonitis, tendobursit, rheumatoid arthritis, myopathy, rarely - pain in the joints and bones, myasthenia gravis, arthritis, arthritis, 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, intrusive thoughts, neuroleptic malignant syndrome, infrequent: dystonia, muscle twitching, a weakening of concentration, paresthesia, tremor of limbs, impotence, bradykinesia, low / increased libido, panic reactions, lethargy, dyskinesia, memory loss, stupor, amnesia, stroke, hyperactivity, depersonalization, a syndrome of "restless legs" (akathisia), myoclonus, depressed mood, increased reflexes, slowing of mental function, increased sensitivity to irritants, hypotension , violations of the oculomotor response, frequent dizziness, tremor, extrapyramidal symptoms, agitation, depression, nervousness, excessive salivation, hostility, suicidal thoughts, manic thoughts, unsteady gait, confusion, resistance to passive movements implementation syndrome (gear), very frequent : insomnia, somnolence, akathisia.

Respiratory System

Rare: hemoptysis, aspiration pneumonia, increased sputum production, dryness of the nasal mucosa, pulmonary edema, pulmonary embolism, hypoxia, respiratory distress, apnea, rarely - asthma, epistaxis, hiccup, laryngitis, frequent shortness of breath, pneumonia.

Integuments

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

The 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.

Urogenital

Rare: pain in the breast, cervicitis, galactorrhea, anorgasmia, burning sensation in the urinary tract, glycosuria, gynecomastia (breast enlargement in men), kidney stones, painful erection; Infrequent: cystitis, urinary frequency, 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.

Body as a Whole

Rarely - sore throat, stiffness in the back, heaviness in the head, candidiasis, throat tightness, Mendelson's syndrome, heat stroke, rarely - pelvic pain, swelling of the face, nausea, light sensitivity, jaw pain, fever, stiff jaw, bloating , the feeling of tension in the chest, frequent: flu-like symptoms, peripheral edema, pain in the chest, in the neck.

Metabolic disorders and nutrition-related

Rare: hyperkalemia, gout, hypernatremia, cyanosis, acidification of urine, hypoglycemic reaction, rarely - dehydration, edema, hypercholesterolemia, hyperglycemia, hypokalemia, diabetes, elevated ALT, hyperlipidemia, hypoglycemia, thirst, elevated levels of blood urea, hyponatremia, elevated AST levels, increased alkaline phosphatase, iron deficiency anemia, elevated creatinine, bilirubinemia, elevated lactate dehydrogenase, obesity, frequent: weight loss, increased CK levels.

Contraindications.
- Hypersensitivity to aripiprazole or any other components of the drug.
- Age 18 years.

Overdose. Abilify online cheap.

In clinical studies described cases of accidental or intentional overdose of aripiprazole with a single dose up to 1080 mg, followed by death. Symptoms of an overdose of aripiprazole were nausea, vomiting, fatigue, diarrhea and lethargy. In hospitalized patients, no clinically significant changes in vital signs, laboratory parameters and ECG. Post-marketing experience of a single dose of adult patients and 450 mg of aripiprazole suggests the possible development of arrhythmias. In addition, the described cases overdose of aripiprazole in children (receiving up to 195 mg). Potentially dangerous overdose symptoms include extrapyramidal disorder, and transient loss of consciousness.

In overdose require maintenance therapy to ensure adequate airway, oxygenation, ventilation and effective symptomatic treatment. It should be drug reactions. Should be started immediately monitoringuvannya performance of the heart with ECG recordings to detect arrhythmias. After confirmed or suspected overdose of aripiprazole need close medical supervision to the disappearance of all symptoms. Activated charcoal (50 g), introduced an hour after taking aripiprazole decreases the AUC and Cmax (length of stay and the level of the maximum concentration in the blood) of aripiprazole by 51 and 41%, respectively, which allows us to recommend its use in overdose.

Although reliable data on the use of hemodialysis for overdose of aripiprazole no beneficial effect of this method is unlikely, since aripiprazole is not excreted by the kidneys in unchanged form and is largely bound to plasma proteins.

Features of the application. Pharmacy online abilify.

Suicide attempts - a tendency to suicidal thoughts and attempts characteristic of psychosis, so drug therapy should be combined with careful medical supervision. Abilifay should prescribe the minimum amount sufficient to treat the patient, this will reduce the risk of overdose.

Tardive dyskinesia - the risk of tardive dyskinesia increases with the duration of neuroleptic therapy, so when you see the intake Abilifayu symptoms of tardive dyskinesia should reduce the dose of the drug or to cancel it. After discontinuation of therapy, these symptoms may temporarily worsen or appear for the first time. Neuroleptic malignant syndrome - in the treatment of antipsychotic drugs, including aripiprazole, described a life-threatening syndrome, known as "neuroleptic malignant syndrome" (NMS). This syndrome is hyperpyrexia, muscle rigidity, mental disorders and autonomic instability (irregular pulse or blood pressure, tachycardia, sweating, and heart arrhythmias). In addition, sometimes there is an increase in the activity of creatine phosphokinase, myoglobinuria (rhabdomyolysis) and acute renal failure. In the event of symptoms of NMS, or unexplained fever all antipsychotics, including Abilify, should be abolished.

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Hyperglycemia and Diabetes Mellitus - Hyperglycemia, in some cases severe and associated with ketoacidosis, which can lead to hyperosmolar coma or death, has been observed in patients treated with atypical antipsychotics. Although the association between atypical antipsychotics and impaired hyperglycemic type remains unclear, patients found to have diabetes, should regularly determine the level of glucose in the blood when taking atypical antipsychotics. Patients who present risk factors for diabetes (obesity, diabetes in the family) when taking atypical antipsychotics should conduct glucose in the blood at the beginning of the course and periodically during treatment. In all patients treated with atypical antipsychotics, need constant monitoring of the development of symptoms of hyperglycemia including increased thirst, frequent urination, polyphagia and weakness).

With care - for patients with cardiovascular disease (with coronary heart disease or myocardial infarction, heart failure and conduction disorders), cerebrovascular diseases and conditions that lead to hypotension (dehydration, hypovolemia, and antihypertensive drugs) because of the possibility of orthostatic hypotension in patients with seizure disorders, or, if where possible convulsions, patients with an increased risk of hyperthermia, such as intense exercise, overheating, taking anticholinergics, dehydration due to the ability of neuroleptics disrupt thermoregulation, in patients with an increased risk of aspiration pneumonia because of the risk of violating the motor function of the esophagus and aspiration, in patients suffering from obesity and the presence of diabetes in the family.