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Aripiprazole

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2019-09-19
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Clinical Pharmacology

Pharmacodynamics

The therapeutic effect of aripiprazole in schizophrenia and type 1 bipolar disorder is assumed to be due to a combination of partial agonistic activity against D2-dopamine and 5HT1a-serotonin receptors and antagonistic activity against 5HT2a-serotonin receptors. Aripiprazole in animal experiments showed antagonism in relation to dopaminergic hyperactivity and agonism in relation to dopaminergic hypoactivity. Aripiprazole possesses high in vitro affinity for D2 and D3 dopamine receptors, 5HT1a and 5HT2a serotonin receptors, and moderate affinity for D4 dopamine, 5HT2c and 5HT7 serotonin receptors, and α1 adrenoreceptrs, and I and adrenoreceptors, and I and adrenoreceptors. Aripiprazole is also characterized by moderate affinity for serotonin reuptake sites and lack of affinity for m-cholinergic receptors. Some of the clinical effects of aripiprazole may be attributed to the interaction with receptors other than dopamine and serotonin.

When used inside aripiprazole in healthy volunteers at a dose of 0.5 to 30 mg once a day for 2 weeks, a dose-dependent decrease in the binding of 11C-racloprid, D2 / D3-dopamine receptor ligand, to the caudate nucleus and the fence according to positron emission data is observed. tomography.

Pharmacokinetics

Suction
After oral administration, aripiprazole is rapidly absorbed, while its maximum concentration in the blood plasma is reached in 3-5 hours. Aripiprazole is minimally subjected to a systemic metabolism. Absolute bioavailability of pills is 87%. High fat foods do not affect the pharmacokinetics of aripiprazole.

Distribution
Aripiprazole is intensively distributed in the tissues, the apparent volume of distribution is 4.9 l / kg, which indicates a significant extravascular distribution. At therapeutic concentrations in the blood, aripiprazole and its main metabolite dehydroaripiprazole are more than 99% bound to plasma proteins, mainly albumin.

Metabolism
Aripiprazole is metabolized in the liver in three ways: dehydrogenation, hydroxylation and N-dealkylation. According to in vitro studies, dehydrogenation and hydroxylation of aripiprazole occurs under the action of CYP3A4 and CYP2D6 isoenzymes, and N-dealkylation is catalyzed by CYP3A4 isoenzyme. Aripiprazole is the main active ingredient in the blood. In the equilibrium state, the area under the concentration-time curve (AUC) of dehydroaripiprazole is about 40% of the plasma aripiprazole AUC.

Removal
Mean half-life (T1/2aripiprazole - approximately 75 hours in patients with a high activity of the isoenzyme CYP2D6 and approximately 146 hours in patients with a low activity of this isoenzyme. The total clearance of aripiprazole is 0.7 ml / min / kg, mainly due to the elimination of the liver
After a single ingestion of labeled [14C] aripiprazole approximately 27% of radioactivity is determined in the urine and approximately 60% in the feces. Less than 1% of unchanged aripiprazole is detected in the urine, and about 18% of the dose taken is excreted unchanged with feces.

Pharmacokinetics in Special Patient Groups

Use in children
The pharmacokinetics of aripiprazole and dehydroaripiprazole in children aged 10 to 17 years was the same as in adults after correcting the difference in body weight.

Elderly patients
There were no differences in pharmacokinetic parameters of aripiprazole in adult patients with schizophrenia and in healthy volunteers due to age.

Floor
There were no differences in pharmacokinetic parameters of aripiprazole in adult patients with schizophrenia and in healthy volunteers due to gender.

Smoking and Race
There were no clinically significant differences in the pharmacokinetics of aripiprazole depending on race and smoking.

Renal dysfunction
Pharmacokinetic parameters of aripiprazole and dehydroaripiprazole in patients with severe kidney disease do not differ from those in healthy volunteers.

Liver dysfunction
After a single dose of aripiprazole by persons with varying degrees of severity of liver cirrhosis (Class A, B and C according to Child-Pugh classification), no significant impairment of liver function on the pharmacokinetics of aripiprazole and dehydroaripiprazole was detected, however, only three patients with decompensated liver cirrhosis participated in the study (Class C according to the Child-Pugh classification), in connection with which it is impossible to draw final conclusions about the metabolic activity of the liver in patients with decompensated liver cirrhosis.

Indications

Composition

Active ingredient: aripiprazole 10.00 / 15.00 / 30.00 mg.
Excipients: lactose monohydrate - 61.23 / 91.53 / 183.69 mg, corn starch - 10.45 / 15.675 / 31.35 mg, microcrystalline cellulose - 10.45 / 15.675 / 31.35 mg, hyprolosis - 1 , 90 / 2.85 / 5.70 mg, magnesium stearate - 0.95 / 1.425 / 2.85 mg, iron dye red oxide (E172) (for dosages of 10 mg and 30 mg) - 0.02 / 0.06 mg, iron dye yellow oxide (E172) (for a dosage of 15 mg) - 0.345 mg.

Aripiprazole is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Ariprisole Belupo Croatia pills
Zylaxera Krka dd Novo mesto AO Slovenia pills

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Aripiprazole

Dosage and Administration

Schizophrenia
The recommended starting dose is from 10 mg to 15 mg once a day, regardless of the meal. Maintenance dose - 15 mg per day. In clinical studies showed the effectiveness of the drug in doses of 10 mg to 30 mg per day. The maximum daily dose should not exceed 30 mg.

Manic episodes in bipolar disorder
As a monotherapy, the recommended initial dose is 15 mg once a day, regardless of the meal. If necessary, the dose change should be carried out with an interval of at least 24 hours. Clinical studies have shown the effectiveness of the drug in doses from 15 mg to 30 mg per day for 3-12 weeks. The safety of the drug in doses of more than 30 mg per day has not been evaluated in clinical studies.
When monitoring patients with type I bipolar disorder after a manic or mixed episode, symptoms of symptoms stabilized with aripiprazole for 6 weeks at a dose of 15 mg per day or 30 mg per day at an initial dose of 30 mg per day, then 6 months and beyond - for 17 months, the beneficial effect of such maintenance therapy has been established. Patients should be examined periodically to determine the need for continued maintenance therapy.

Supplement to therapy with lithium or valproic acid in case of bipolar I disorder
The recommended starting dose is from 10 mg to 15 mg once a day, regardless of the meal. Maintenance dose - 15 mg per day. The dose may be increased to 30 mg per day, depending on the clinical indications.
When monitoring patients with type I bipolar disorder, the beneficial effect of maintenance therapy with aripiprazole in a dose of 10 mg to 30 mg per day was established as an adjunct to therapy with lithium or valproic acid.
Patients should be examined periodically to determine the need for continued maintenance therapy.

Supplementary Therapy for Major Depressive Disorder
The recommended starting dose is 5 mg per day, regardless of the meal.
If necessary and well tolerated, the daily dose can be weekly increased by 5 mg to the maximum - no more than 15 mg per day.
The duration of therapy for all the above indications has not been established. Patients should be regularly examined for the possibility of cancellation of therapy.

Use of the drug in special patient groups

Patients with impaired renal function. Dose adjustment of the drug is not required.

Patients with impaired liver function.
Dose adjustment of the drug is not required.
Patients with severely impaired liver function, a dose of 30 mg is prescribed with caution.

Patients over the age of 65 years.
Dose adjustment of the drug is not required.

The influence of the patient's gender on the dosing regimen.
Dosage regimen for patients of both sexes is the same.

The effect of smoking on the dosing regimen.
The dosage regimen for smoking and non-smoking patients is the same.

Dosing regimen with concomitant therapy
With simultaneous use of aripiprazole and potent inhibitors of the CYP3A4 isoenzyme (ketoconazole, clarithromycin), the dose should be reduced by 2 times; when canceling CYP3A4 isoenzyme inhibitors, the dose should be increased.

With the simultaneous use of aripiprazole and powerful inhibitors of the isoenzyme CYP2D6 (quinidine, fluoxetine, paroxetine), the dose should be reduced by 2 times; when canceling CYP2D6 isoenzyme inhibitors, the dose should be increased.
If the drug is prescribed as an additional therapy for major depressive disorder, the drug should be used without changing the dosing regimen.

With simultaneous use of the drug and potent inhibitors of CYP2D6 isoenzymes (quinidine, fluoxetine, paroxetine) and CYP3A4 (ketoconazole, clarithromycin), the dose of the drug should be reduced to 25% of the usual dose. When canceling inhibitors of isoenzymes CYP3A4 and / or CYP2D6, the dose of the drug should be increased.

With simultaneous use of the drug and powerful, moderate or weak inhibitors of CYP3A4 and CYP2D6 isoenzymes, the dose of the drug can be initially reduced to 25% of the usual dose, and then increased to achieve an optimal clinical result.

When prescribing the drug to patients with low activity of the CYP2D6 isoenzyme, the initial dose of the drug should be reduced by half and then increased to achieve an optimal clinical result. With simultaneous use of the drug and a potent inhibitor of the CYP3A4 isoenzyme in patients with low activity of the CYP2D6 isoenzyme, the dose of the drug should be reduced to 25% of the usual dose.

With simultaneous use of the drug and potential inducers of the CYP3A4 isoenzyme (carbamazepine), the dose of the drug should be increased by 2 times. After discontinuation of CYP3A4 isoenzyme inducers, the dose should be reduced to the recommended dose.

Adverse reactions

The most common side effects in placebo-controlled clinical trials are akathisia and nausea, each of which was observed in more than 3% of patients taking aripiprazole.

The following side effects are more common (≥ 1/100) compared with placebo or identified as possible clinically significant side effects (*).
To indicate the frequency of side effects, the following classification is used: often (? 1/100 and? 1/10) and infrequently (? 1/1000 and? 1/100):

Mental disorders:
often - anxiety, insomnia, anxiety;
infrequently - depression *, heightened sexuality.

Nervous system disorders:
often - extrapyramidal disorders, akathisia, tremor, dizziness, drowsiness, sedation, headache.

Violations by the organ of vision:
often - blurred vision; infrequently - diplopia.

Violations of the cardiovascular system:
infrequently - tachycardia *, orthostatic hypotension *.

Disorders of the gastrointestinal tract:
often - dyspepsia, vomiting, nausea, constipation, salivary hypersecretion.

General violations:
often - fatigue.

Contraindications

Hypersensitivity to aripiprazole or to any component of the drug;
age up to 18 years;
lactase deficiency, rare hereditary galactosemia, glucose-galactose malabsorption.

Carefully

In patients with cardiovascular diseases (ischemic heart disease or myocardial infarction, heart failure and conduction disturbances), cerebrovascular diseases and conditions that predispose to arterial hypotension (dehydration, hypovolemia and hypotensive drugs) due to the possibility of orthostatic hypotension; in patients with convulsive seizures or suffering from diseases that may cause convulsions; in patients with an increased risk of hyperthermia (for example, with intense physical exertion, overheating, taking m-cholinoblockers, with dehydration due to the ability of neuroleptics to interfere with thermoregulation); in patients with an increased risk of aspiration pneumonia due to the risk of impaired motor function of the esophagus and aspiration; in patients with obesity, and in the presence of diabetes mellitus in family history; in patients with a high risk of suicide (psychotic illness, bipolar disorder, major depressive disorder); in persons aged 18-24 years due to the risk of suicidal behavior.

Drug interactions

Aripiprazole may enhance the effect of antihypertensive drugs, since it has an antagonistic effect on alpha1-adrenoreceptors.

The mechanism of action of aripiprazole is associated with an effect on the central nervous system; this must be taken into account when used together with other drugs that have a central action.

Caution should be exercised with the simultaneous use of aripiprazole and drugs that cause prolongation of the QT interval or disrupt the electrolyte balance.

Pregnancy and Lactation

Pregnancy.Adequate and strictly controlled clinical studies of the safety of use in pregnant women have not been conducted. It is not known whether the use of the drug Priprizol® a pregnant woman can have a harmful effect on the fetus or cause reproductive disorders. In newborns whose mothers took antipsychotics during the last trimester of pregnancy, in the postpartum period there is a risk of developing extrapyramidal disorders and "withdrawal" syndrome. Cases of excitement, muscle hypertension or hypotension, tremor, drowsiness, respiratory distress syndrome, and feeding disorders have been reported. These symptoms were of varying severity, sometimes they passed without treatment, in other cases, newborns needed intensive therapy and prolonged hospitalization. When using aripiprazole, the development of new symptoms in newborns was very rare.

Patients should be warned that they should immediately inform the doctor about the occurrence of pregnancy during treatment, and also should inform the doctor about the planned pregnancy.

Drug Ariprizol® can be used during pregnancy only if the potential benefit to the mother exceeds the potential risk to the fetus.

Breast-feeding. Aripiprazole passes into breast milk. If necessary, use of the drug breastfeeding canceled.

Special instructions

The therapeutic effect of antipsychotic drugs develops within a few days to several weeks. During this period, it is necessary to monitor the patient's condition.

Suicidal attempts.
The phenomenon of suicidal behavior is characteristic of psychosis and mood changes, in some cases it is observed immediately after the start or change of treatment with antipsychotic drugs, including treatment with aripiprazole. When treating with antipsychotic drugs, it is necessary to monitor patients at higher risk. The results of one epidemiological study showed that patients with schizophrenia or bipolar disorder did not have an increased risk of suicidality with aripiprazole compared with other antipsychotic drugs. There is not enough clinical evidence to evaluate this risk in younger patients (under the age of 18), but there is reason to assume that the risk persists after 4 weeks of treatment with antipsychotics, including aripiprazole.

Cardiovascular diseases.
Aripiprazole should be used with caution in patients with cardiovascular diseases (myocardial infarction, ischemic heart disease, heart failure, a history of cardiac conduction disturbances), cerebral circulation disorders, conditions predisposing to arterial hypotension (dehydration, hypovolemia, antihypertensive therapy. hypertension, including essential or malignant.

When using antipsychotic drugs, cases of venous thromboembolism have been reported. Since patients undergoing treatment with antipsychotic drugs often have acquired risk factors for the development of venous thromboembolism, it is necessary to identify all possible risk factors for the development of venous thromboembolism before and during the treatment with Ariprizol® with preventive measures.

Conduction disturbances.
In aripiprazole clinical studies, the incidence of prolongation of the QT interval was comparable to the placebo group. Aripiprazole, like other antipsychotics, should be used with caution in patients with a family history of lengthening the QT interval.

Late dyskinesia.
In clinical studies that lasted less than 1 year, infrequent cases of dyskinesia requiring urgent treatment were observed during aripiprazole treatment. If the patient is treated with drug Prizizol® Signs and symptoms of tardive dyskinesia appear, the possibility of lowering the dose or stopping treatment should be considered.

Symptoms of dyskinesia may temporarily worsen or even appear for the first time after discontinuation of therapy.

Other extrapyramidal disorders.
In clinical studies of aripiprazole in children, akathisia and parkinsonism were observed. In the event of signs and symptoms of other extrapyramidal disorders, consideration should be given to reducing the dose of aripiprazole with subsequent observation of the patient.

Malignant neuroleptic syndrome (SNS).
Malignant neuroleptic syndrome is a potentially life-threatening combination of symptoms associated with the use of antipsychotic drugs. In clinical studies during treatment with aripiprazole, rare cases of NNS were observed, which manifests itself as hyperpyrexia, muscle rigidity, mental disorders and instability of the autonomic nervous system (irregular pulse and blood pressure, tachycardia, sweating, cardiac arrhythmia). In addition, in some cases there is an increase in the activity of CPK, myoglobinuria (rhabdomyolysis) and acute renal failure. In the event of symptoms of ZNS or unexplained fever, all neuroleptics, including the drug Priprizol®should be canceled.

Cramps.
In clinical studies during the treatment with aripiprazole, infrequent cases of seizures have been observed. Therefore, aripiprazole should be used with caution in patients with a history of seizures and risk of their development.

Psychoses associated with senile dementia.
Three placebo-controlled clinical trials for the use of aripiprazole in elderly patients (mean age 82.4 years, age range 56-99 years) with Alzheimer's disease psychosis showed an increased risk of death compared with the placebo group. Aripiprazole mortality was 3.5% compared with 1.7% in the placebo group. Although the causes of death differed, the main causes of most deaths were either disorders of the cardiovascular system (including heart failure, sudden death), or the development of infection (including pneumonia).

In the course of these same clinical studies in elderly patients (mean age 84 years, age range 78–88 years), cerebrovascular unwanted reactions (including stroke, transient ischemic attack), including fatal, were reported. In general, cerebrovascular adverse reactions were observed in 1.3% of patients treated with aripiprazole compared with 0.6% of patients receiving placebo. This difference was not statistically significant. However, in one of these fixed-dose studies of aripiprazole, a significant dose-response relationship with cerebrovascular unwanted reactions was detected.

Arisipole® not recommended for use in patients with dementia-related psychosis.

Hyperglycemia and diabetes.
Hyperglycemia, in some cases severe and accompanied by ketoacidosis or hyperosmolar coma with a fatal outcome, was noted in patients taking atypical antipsychotics. The relationship between taking atypical antipsychotics and hyperglycemic type disorders remains unclear. In clinical studies using aripiprazole, there was no significant difference in the incidence of adverse reactions involving hyperglycemia (including diabetes) or in changes in laboratory values ​​of glycemia compared with the placebo group.
Patients who are diagnosed with diabetes mellitus, when taking atypical antipsychotics should regularly determine the concentration of glucose in the blood.
Patients who have risk factors for diabetes (obesity, the presence of diabetes in the family history), while taking atypical neuroleptics should determine the concentration of glucose in the blood at the beginning of the course and periodically in the process of taking the drug. In patients taking atypical antipsychotics, constant monitoring of symptoms of hyperglycemia (increased thirst, frequent urination, polyphagia, weakness) is necessary. Particular attention should be paid to patients with diabetes and risk factors for its development.

Hypersensitivity.
As with the use of other drugs, while taking aripiprazole, hypersensitivity reactions may develop in the form of allergic symptoms.

Weight gain
An increase in body weight is usually observed in patients with schizophrenia and bipolar mania due to the development of comorbidities, the use of antipsychotic drugs that cause an increase in body weight, an unhealthy lifestyle, which can lead to acute complications. Reports of weight gain have been reported in the post-marketing period in patients who took aripiprazole. Usually, these adverse reactions were observed in patients with significant risk factors, such as diabetes, thyroid disease, or pituitary adenoma. In the framework of clinical studies, aripiprazole did not cause a clinically significant increase in body weight.
In clinical studies of adolescent patients with bipolar mania while taking aripiprazole, body weight increased after 4 weeks of treatment. Constant monitoring of body weight in adolescent patients with bipolar mania is needed. If an increase in body weight is clinically significant, it is necessary to reduce the dose of aripiprazole.

Dysphagia.
When using neuroleptics, there were cases of violations of the motility of the esophagus and, as a result, aspiration pneumonia. The drug should be administered with caution to patients with risk factors for the development of aspiration pneumonia.

Pathological attraction to gambling.
During the post-registration period, reports of a pathological attraction to gambling in patients taking aripiprazole were recorded, regardless of whether these patients had a pathological attraction to gambling in history. Patients with a history of craving for gambling may be at increased risk of developing this disorder and should be carefully monitored when using aripiprazole.

Lactose.
Drug Ariprizol® contains lactose in the composition, so it is not recommended for patients who have rare hereditary diseases associated with intolerance to galactose, lactase deficiency or glucose-galactose malabsorption.

Patients with concomitant attention deficit hyperactivity disorder (ADHD).
Despite the high frequency of combination of bipolar disorder type I and ADHD, there are very limited data on the safety of the simultaneous use of aripiprazole and psychostimulants, so caution should be exercised in the case of their combined use.

Impact on the ability to drive vehicles and mechanisms

As with the use of other antipsychotics, when prescribing aripiprazole, the patient must be warned about the dangers of working with moving machinery and driving.

Overdosage

In clinical studies described cases of accidental or deliberate overdose of aripiprazole with a single dose of up to 1260 mg, not accompanied by a fatal outcome.

Symptoms: lethargy, increased blood pressure, drowsiness, tachycardia, loss of consciousness, nausea, vomiting, diarrhea. In hospitalized patients, there were no clinically significant changes in the main physiological parameters, laboratory parameters and ECG.

The cases of aripiprazole overdose in children (up to 195 mg) without death are described. Potentially dangerous symptoms of overdose are drowsiness, extrapyramidal disorders, and transient loss of consciousness.

Treatment: monitoring of vital functions, ECG to detect possible arrhythmias, supportive therapy, airway management, oxygenation, effective ventilation of the lungs, activated carbon, symptomatic treatment, careful medical observation until all symptoms disappear. There are no data on the use of hemodialysis in overdose of aripiprazole; the favorable effect of this method is unlikely, since aripiprazole is not excreted by the kidneys unchanged and is largely bound to plasma proteins.

  • Brand name: Arisipole
  • Active ingredient: Aripiprazole
  • Manufacturer: Belupo
  • Country of Origin: Croatia

Studies and clinical trials of Aripiprazole (Click to expand)

  1. An Efficient Synthesis of Aripiprazole, Buspirone and NAN-190 by the Reductive Alkylation of Amines Procedure
  2. Synthetic Study on the Unique Dimeric Arylpiperazine: Access to the Minor Contaminant of Aripiprazole (I).
  3. Synthesis and Bioactivity of Aripiprazole Derivatives.
  4. Aripiprazole augmentation for treatment of patients with inadequate antidepressants response
  5. Aripiprazole augmentation of incomplete treatment response in an adolescent male with obsessive-compulsive disorder
  6. Reversal of trichotillomania with aripiprazole
  7. Aripiprazole in anorexia nervosa and low-weight bulimia nervosa: Case reports
  8. High dosage of aripiprazole-induced dysphagia
  9. Simultaneous determination of aripiprazole and its active metabolite, dehydroaripiprazole, in plasma by capillary electrophoresis combining on-column field-amplified sample injection and application in schizophrenia
  10. An open trial of aripiprazole augmentation for SSRI non-remitters with late-life depression
  11. Efficacy and safety of adjunctive aripiprazole in major depressive disorder in older patients: a pooled subpopulation analysis
  12. A safety and tolerability laboratory study of the combination of aripiprazole and topiramate in volunteers who drink alcohol
  13. Aripiprazole as adjunct to a mood stabilizer and citalopram in bipolar depression: a randomized placebo-controlled pilot study
  14. Neurocognition and its influencing factors in the treatment of schizophrenia—effects of aripiprazole, olanzapine, quetiapine and risperidone
  15. The comparison of aripiprazole and risperidone augmentation in selective serotonin reuptake inhibitor-refractory obsessive-compulsive disorder: a single-blind, randomised study
  16. Aripiprazole plus divalproex for recently manic or mixed patients with bipolar I disorder: a 6-month, randomized, placebo-controlled, double-blind maintenance trial
  17. Aripiprazole altered plasma levels of brain-derived neurotrophic factor and catecholamine metabolites in first-episode untreated Japanese schizophrenia patients
  18. A case series of patients with Tourette's syndrome in the United Kingdom treated with aripiprazole
  19. Effects of DRD2 and CYP2D6 genotypes on delta EEG power response to aripiprazole in healthy male volunteers: a preliminary study
  20. A non-randomized study to investigate the effects of the atypical antipsychotic aripiprazole on the steady-state pharmacokinetics of lamotrigine in patients with bipolar I disorder
  21. Synthesis of multi-labeled [14C]Aripiprazole
  22. Conformational polymorphism in aripiprazole: Preparation, stability and structure of five modifications
  23. A sensitive column-switching HPLC method for aripiprazole and dehydroaripiprazole and its application to human pharmacokinetic studies
  24. Aripiprazole associated with severe exacerbation of Parkinson's disease

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