Table of content:
- Indications for use
- Results of clinical trials
- Possible adverse reactions
- Special instruction
Abilify refers to a class of neuroleptics, medications often referred to in modern medicine as "antipsychotics". Experts position pharmaceutical medicine as an advanced development of the latest generation, the specific impact of which is many times more powerful than previously used analogs.
In psychiatry, atypical antipsychotics are regarded as the optimal solution in the fight against several serious mental disorders. The first time Abilify was launched in the pharmaceutical market in the heyday of the second Millennium. In our country, the neuroleptic drug received official recognition only by the end of 2007. Initially, the drug was approved by the Food & Drug Administration as the optimal solution for the treatment of schizophrenia. But in the course of clinical studies and practical application, it was revealed that the number of indications for use of the drug is much more extensive.
Since 2004, Abilify has been actively used for the treatment of episodic manic bipolar disorders. Since 2007, it has been prescribed to patients with dangerous depressive injuries of consciousness. In the fall of 2009, the drug was officially included in the comprehensive treatment of autism among children and adolescents.
From several advantages of the drug, many patients and doctors are attracted by the variety of its dosage forms: tablets, oral liquid, injectable solution. The use of the latter guarantees the maximum effectiveness of therapy, due to the high bioavailability of the drug.
Manufacturing company, Abilify development history
Initially, the development of aripiprazole — the active substance of a neuroleptic, was carried out by scientists of a large pharmaceutical holding in Japan, Otsuka Pharmaceuticals. The chemical compound derived in the course of research was called ORS-14597.
At the end of the last century, thanks to the undeniable evidence of the effectiveness of the derived drug, the Japanese company managed to unite with the largest pharmaceutical Corporation in America, Bristol-Myers Squibb.
Thus, the antipsychotic Abilify is the result of a collaboration between two manufacturers, who have conducted repeated large-scale clinical studies and delivered the neuroleptic to the pharmaceutical market.
Today, the chemical compound goes on sale under the officially recognized trade name "Abilify".
Results of clinical trials
In the course of clinical studies, it was found that the effectiveness of therapy with Abilify was detected in 94% of cases. Already in the first few weeks of use, the severity of symptoms was reduced by 30%.
Negative effects on appetite and weight were not recorded. Approximately 15% of patients developed nausea and other minor side effects. Due to complications, treatment had to be canceled in 0.8 — 1% of cases.
Abilify: Indications for Use
The pharmaceutical substance is indicated for people suffering from acute schizophrenia and episodic, sometimes mixed, manic bipolar disorders. Also, the drug is prescribed to maintain the effect of therapeutic therapy.
Instruction for use
The drug differs from its analogs with a high level of safety, but this does not exclude the risk of very severe adverse reactions during its use. This tolerance of complications makes an individual selection of dosage and dosage form mandatory.
Important: the original drug, delivered from abroad, must be accompanied by instructions that help the patient to thoroughly familiarize themselves with the characteristics of the drug, including contraindications. But in any case, the principle of dosing and other important aspects are recommended to coordinate with your doctor.
Among the contraindications of a neuroleptic, we can note:
- increased susceptibility to an active agent or another component.
Treatment for pregnancy and lactation
To date, no clinical trials have been conducted about the harmlessness of antipsychotics during pregnancy. But based on the point of view of doctors, a neuroleptic is allowed to treat pregnant women if the health benefits of the future mother outweigh the possible harm to the fetus.
Whether the active component gets into breast milk-it is impossible to say for sure. But doctors strongly recommend against antipsychotic treatment during lactation.
Possible adverse reactions
As a result of numerous clinical trials and tests, several potential side effects provoked by taking Abilify have been identified:
- heart tachycardia;
- drop in blood pressure;
- nausea and vomiting;
- absence of appetite;
- asthenic condition;
- erectile dysfunction;
- sudden mood swings;
- memory loss, General confusion, low concentration;
- loss of sleep;
- frequent shortness of breath;
- damage to the lower respiratory tract;
- increased sweating;
- irritation, skin rash;
- weakening of auditory and visual functions;
- failure of the urinary system;
There is a small probability:
- abnormal liver function;
- acute pain in the body;
- excessive dryness of the conjunctiva;
- the appearance of fungal infections;
- failures in the optimal functioning of the kidneys.
Less common is a violation of blood clotting, heart arrhythmia failure. In rare cases, there are symptoms of diabetes and acid-base imbalance.
Neuroleptic is recommended to include in therapeutic therapy with special care if the patient has cardiovascular diseases, cerebrovascular diseases, as well as frequent conditions, the impact of which predisposes to arterial hypotension — dehydration, a decrease in blood volume in the body.
The drug is not indicated for people who are prone to seizures, as well as carriers of diseases that provoke these seizures.
With special caution, include in therapy with an increased risk of hyperthermia, - manifested for example in the process of intense physical activity, overheating or dehydration — - because of the peculiarity of antipsychotics to provoke failures of thermoregulation. Also-with aspiration pneumonia, which is due to an increased risk of disorders of the motor functions of the digestive tract and aspiration.
The drug is not recommended for patients with obesity and hereditary diabetes.
For psychoses, suicidal thoughts and actions are characteristic, so the inclusion of a neuroleptic in treatment should be accompanied by careful monitoring by a doctor.
To reduce the risk of intentional overdose, the drug should be prescribed in a minimum amount, but sufficient for a full course of treatment.
It is necessary to reduce the dose or completely cancel treatment with the drug, in case of symptoms typical for tardive dyskinesia during treatment. The fact is that long-term therapy, including neuroleptics, can provoke the development of a neuroleptic syndrome. After discontinuation of the medication, symptoms may briefly worsen, or even appear for the first time.
In isolated cases, treatment with neuroleptic drugs is fraught with the development of a deadly malignant neuroleptic syndrome, manifested by fever, extremely high body temperature-above 41, muscle rigidity, mental disorders, confusion, the variability of the Autonomous nervous system, as well as instability of blood pressure and pulse, tachycardia, arrhythmia and increased sweating. Sometimes, the symptoms are added to the increased energy of CPK, acute kidney failure, and myoglobinuria. If the patient has symptoms of a malignant syndrome or has developed an unexplained fever, the drug should be excluded from therapy.
Although the relationship between atypical neuroleptics and hyperglycemia remains unexplained, in some patients whose therapy included neuroleptics, a hyperglycemic condition was detected, rarely accompanied by ketoacidosis, which is dangerous hyperosmolar coma to the point of death. Patients with a high predisposition to diabetes mellitus, when the drug is included in the treatment, should detect the concentration of glucose in the blood at the very beginning of the treatment course, and, cyclically in its process.
When taking anti-psychotics, patients with a diagnosis of diabetes requires systematic identification of the level of glucose in the blood. All patients taking neuroleptic medications need regular monitoring of hyperglycemia symptoms. This includes increased thirst, frequent urination, polyphagia, and General weakness.
During therapy with Abilify, you should be careful to engage in activities that require increased concentration and accelerated psychomotor reactions.
Medicinal form of release
The original Abilify is available in tablet form. Depending on the dose, tablets differ in color, shape, and engraving:
- from 2 to 10 mg-rectangular tablets, green, blue, and pink shades. Marked by the inscription — A-006, A-007 A-008;
- from 15 to 30 mg-round pills, white, yellow, and pink. There are markings on the surface: A-009, A-010, and A-011.
Neuroleptic is also released in a dispersible form:
- 10 mg — pink-tinted tablets, engraved-A, 640;
- 15 mg-yellow dragees, marked with the inscription-A, 641.
The volume of the original bottle with the medicinal oral substance is 150 ml. The optimal amount for use is 1 mg/ml.
An antipsychotic drug available in injectable form. The volume of the bottle with the solution is 1.3 ml. The dose of the active substance is 9.75. The optimal concentration is 7.5 mg / ml).
Each Abilify tablet contains a certain concentration of the main component — aripiprazole.
In addition to the active agent, the medication contains a number of secondary:
- lactose monohydrate;
- corn starch;
- magnesium compounds;
- oxides: yellow/red;
- aluminum blue lacquer.
The active component-aripiprazole refers to partial, that is, partial agonists, whose interaction occurs with receptors that are susceptible to certain natural neurotransmitters in the human body — dopamine and serotonin. Thus, the effect of the active substance directly depends on the concentration of neurotransmitters, which are released under the influence of CNS structures.
If the concentration of natural neurotransmitters arrives in excess, the neuroleptic acts as a highly functional opponent. It binds to the corresponding receptors, calming their activity. If there is a lack of neurotransmitters, the component produces the opposite effect, that is, it has a stimulating effect on the receptors.
The drug exerts a hostile dynamism in the mesolimbic pathway of the brain and an increased concentration of dopamine in which leads to symptoms of psychiatric abnormalities. But a decrease in the probability of complications that target the nigrostriatal and tuberoinfundibular pathways provokes the formation of neuroleptic extrapyramidal disorders and an increase in the concentration of prolactin.
In the course of clinical studies and in vitro tests, minor differences were found between oral dispersible tablets and conventional ones.
Regarding absorption: after taking the tablets, aripiprazole is immediately absorbed from the gastrointestinal tract. The bioavailability is about 92%. Limit values are marked in the period from 3 to 5 hours. Speaking of the oral form, we can note higher plasma concentrations. So, comparing the bioavailability of tablets and solutions, the first differ in speed by 10%.
From the distribution when injected into the vein, a measure of the distribution reaches up to 5L/kg. The degree of binding to plasma proteins is 100%, while the active drug substance interacts mainly with albumins. By nature, the effectiveness of therapy is considered dose-dependent.
Regarding biotransformation and elimination: chemical-biological transformations of the active component are performed by detaching the hydroxy group, hydroxylation, and N-dealkylation. Laboratory studies have shown that the isoenzymes CYP3A4 and CYP2D6 are responsible for regulating the metabolism. aripiprazole accounts for the Largest amount of medication circulating with the bloodstream, and the remaining amount — about 40% - is dehydro-aripiprazole. More than 50% is excreted from the body with fecal masses, about 30% - with urine. The half-life can reach 3 or more days.
Speaking of intramuscular administration of neuroleptic fluid, peak levels were observed as early as 1-3 hours after administration. The bioavailability is 100%. At first, higher concentrations of aripiprazole were recorded in the blood than when administered orally. However, after a day, the indicators are leveled.
In the course of clinical studies, there was a direct interaction to a small extent between the patient's gender and age and the pharmacokinetic characteristics of the drug. But a significant influence on the level of metabolism and the stage of partial elimination of aripiprazole from the body has the presence of affected liver and kidney cells.
Abilify: the procedure for use and dosage
The dosage of the active component is selected taking into account the type of disease and the age category of the patient. An equally important role is played by the pharmaceutical form of the drug. So, the tablet drug is prescribed at a dosage of 10-30 mg, oral-2-25 mg, and in the case of injection-5.25-15 mg.
Standard therapy begins with a minimum dosage, which is proportionally increased to therapeutically rational. Taking into account the pharmacokinetic features of the substance, namely the period required to balance the concentration of the medicinal component in the bloodstream, a two-week interval is maintained between the dosage changes.
When the initial inclusion of the solution in therapy, after normalization of the General condition and well-being of the patient, it is replaced with a tablet dosage form. Switching to Abilify from other neuroleptics should be done with extreme caution. Doctors follow an individual approach, but the duration of taking a neuroleptic in a minimum dosage is minimized.
The treatment regimen Abilities taking into account age and diagnosed characteristics
Doctors note the following recommended dosage and system of use of the tablet preparation, taking into account the age category and diagnosis of the disease:
- Schizophrenia in adults. The initial volume of the daily dose is 10-15 mg. If necessary, a methodical increase of up to 30 mg is acceptable.
- Schizophrenia in adolescents. The initial daily dosage is 10 mg. In the course of laboratory studies, it was found that a dose of 30 mg is not therapeutically appropriate.
- Bipolar disorders in adults. In the case of monotherapy, 15 mg per day is prescribed (if necessary, an increase in the dose to 0.003 g is acceptable). When combined with Lithium or Valproates, the optimal daily dosage is 10 mg.
- Bipolar disorders in adolescents. The recommended daily dose is 2 mg. The target dosage can reach up to 10 mg. Treatment schematics are not important.
- Depressive disorders in adults. When combined with antidepressants, the daily dosage does not exceed 2 — 5 mg. At the discretion of the doctor, it is permissible to increase the dosage to 15 mg per day.
- Autism in children and adolescents. The recommended daily dose is 2 mg. If necessary, an increase to 15 mg is allowed (by 5 mg every two weeks).
- Tourette's syndrome in children and adolescents. The dosage is selected based on the patient's body weight. Up to 50 kg of therapy begins with 2 mg per day. Methodically, the dose is increased to 10 mg. If the weight exceeds 50 kg, the initial dose remains unchanged, but the target can reach up to 20 mg per day.
Speaking of the injectable form, for schizophrenia and bipolar disorders in adults, the recommended daily dose is 9.75 mg.
The principle of dosage of the oral solution, regardless of the nature of the pathology, remains the same as with the tablet medication, but instead of 30 mg, 25 mg of the active substance in the solution is prescribed.
The principle of taking Abilify
Preformed shape — inside, drinking plenty of water. Before or after a meal-it doesn't matter.
Oral liquid-mixed into drinks.
Injection solution-slowly and carefully inserted into the muscle.
Overdose with an excess volume of the drug does not cause death but can cause a malfunction of the cardiovascular system. In case of overdose, special absorbents are prescribed and supportive therapy is prescribed.
When used simultaneously with powerful inhibitors of CYP2D6 and CYP3A4 isoenzymes, the dosage of the active substance decreases. With extreme caution, include in therapy containing antidepressants, antihypertensive substances, anticonvulsants.
ATTENTION! During treatment with a neuroleptic agent, alcohol intake is not allowed!
Abilify cost, where to buy, the differences from a fake
The drug has long been registered in the United States and Europe, but you can not buy Abilify in all pharmacies in the country, because not everywhere it is available. The drug is released only on the order of a psychiatrist.
You can order Abilify without a prescription in online pharmaceutical stores that specialize in selling the drug from Europe. Transportation is carried out in the shortest possible time. You only need to contact the supplier and confirm the order.
One pack of the drug, which includes 98 tablets of 15 mg, will cost 350 euros. The cost of other medicinal forms is indicated in the online pharmacy.
How to distinguish it from a fake
It is recommended to purchase a neuroleptic strictly from trusted suppliers, which helps to avoid a collision with a counterfeit. Of course, you can buy Abilify with your hands, but doctors are extremely disapproving of various ads from forums. It is important to understand that the medicine purchased from third parties may be of low quality and even safety.
The intermediary must necessarily have all the necessary quality certificates or receipts confirming the transport of the drug from licensed pharmacies in Europe. These documents serve as a guarantee of the quality of the medicinal product.
What do the doctors say
"Among patients whose therapeutic therapy includes the neuroleptic drug Abilify, quite impressive results were noted. Side effects are almost not observed. We can confirm that this drug is safe even with long-term use, both for adults and for patients in the age category up to 18 years" - Steven Dubovsky, a psychiatrist with 24 years of experience.
Patients who have been treated with Abilify, note the absence of any complications in the course of therapy. Reviews from various forums confirm the effectiveness of the drug, which allows us to call the neuroleptic the optimal solution in the fight against mental illnesses.
"On the recommendation of a psychiatrist ordered Abilify mother. We have been struggling with the symptoms of bipolar disorder for several years. I was afraid that there would be any complications, side effects because the instructions say that there may be general weakness and a bunch of different violations. I was pleasantly surprised, but the treatment went smoothly, a complete absence of any disorders and side effects. After therapy, my mother felt much better. Now the drug is used to maintain the effect" - Alex, 29 years old.
The drug should be stored in a dry place, protected from sunlight, at a temperature of 15 to 30C. The shelf life of the drug is 3 years.