Zilaxera - Instructions For Use, Reviews, Price, Analogues, 10 Mg

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Zilaxera

Zilaxera: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. Drug interactions
12. 12. Analogs
13. 13. Terms and conditions of storage
14. 14. Terms of dispensing from pharmacies
15. 15. Reviews
16. 16. Price in pharmacies

Latin name: Zylaksera

ATX code: N05AX12

Active ingredient: aripiprazole (Aripiprazole)

Manufacturer: LLC "KRKA-RUS" (Russia)

Description and photo update: 2019-11-07

Prices in pharmacies: from 3089 rubles.

Buy

Zilaxera is an antipsychotic drug (neuroleptic).

Release form and composition

Zilaxera is available in tablet form:

• dosage 5 mg: slightly biconvex, capsular, light blue with marbling, inclusions of a darker color are possible;
• dosage 10 mg: slightly biconvex, capsular, light pink with marbling and interspersed with a darker color;
• dosage 15 mg: slightly biconvex, round, light yellow with marbling, inclusions of a darker color are possible, with a bevel;
• dosage of 30 mg: slightly biconvex, round, light pink with marbling and interspersed with a darker color, with a bevel.

Tablets, regardless of dosage, are packaged in 14 pieces. in blister strip packaging made of polyvinyl chloride (polyvinylidene chloride) film and aluminum foil, in a cardboard box 2 or 4 packages and instructions for use of Zilaxer.

Composition for 1 tablet:

• active substance: aripiprazole fumarate (in the form of a semi-finished product-granules) - 5.65; 11.3; 16.95 or 33.90 mg, which corresponds to the content of aripiprazole - 5, 10, 15 or 30 mg;
• auxiliary components of semi-finished granules: corn starch, hyprolose, microcrystalline cellulose, lactose monohydrate; additionally for 5 mg tablets - blue dye (diamond black dye, patented blue dye); additionally for tablets 10 mg and 30 mg - dye iron oxide red; additionally for tablets 15 mg - dye iron oxide yellow;
• tablet auxiliary components: magnesium stearate.

Pharmacological properties

Pharmacodynamics

The therapeutic effect of Zilaxera in bipolar I disorder and schizophrenia is likely due to a combination of antagonistic activity against 5HT2a-serotonin receptors and partial agonist activity against 5HT1a-serotonin receptors and D2-dopamine receptors.

Under in vitro conditions, aripiprazole has a high affinity for 5HT1- and 5HT2a-serotonin receptors, D2- and D3-dopamine receptors and a moderate affinity for 5HT2c- and 5HT7-serotonin receptors, D4-dopamine receptors, H1-histamine receptor and alpha-1 receptors.

In addition, aripiprazole is characterized by moderate affinity for the sites responsible for serotonin reuptake, and a complete lack of affinity for muscarinic cholinergic receptors. In experiments carried out on animals, it has been proven that aripiprazole exhibits agonism with respect to dopaminergic hypoactivity and antagonism with respect to dopaminergic hyperactivity. Some of the therapeutic effects of Zilaxera are due to its interaction with receptors other than serotonin and dopamine.

Pharmacokinetics

Aripiprazole is rapidly absorbed from the gastrointestinal tract after taking Zilaxera inside. The maximum plasma concentration is observed in 3-5 hours. Bioavailability is about 87%. It should be noted that food intake does not alter the bioavailability of aripiprazole in any way.

The drug spreads well in tissues, and the apparent volume of distribution (4.9 l / kg) indicates an active extravascular distribution of the substance. In therapeutic doses, more than 99% binds to serum proteins, mainly albumin.

The pre-systemic metabolism of aripiprazole is negligible. It undergoes predominantly hepatic metabolism in three main pathways: hydroxylation, dehydrogenation, and N-dealkylation. Hydroxylation and dehydrogenation of the drug occurs with the participation of isoenzymes CYP2D6 and CYP3A4. The isoenzyme CYP3A4 also catalyzes the N-dealkylation process. The major component in plasma is the parent aripiprazole. When an equilibrium state is reached, the AUC (area under the concentration-time curve) of the active metabolite of the drug (dihydroaripiprazole) is about 40% of the AUC of the active substance.

The average elimination half-life of aripiprazole is 75 hours. An equilibrium concentration of the substance is reached after 14 days. With repeated administration, its cumulation is quite predictable.

Equilibrium pharmacokinetic parameters are proportional to the dose taken. Daily fluctuations in the distribution of the substance and its main metabolite were not observed. Dihydroaripiprazole has the same affinity for D2-dopamine receptors as the parent active ingredient.

Aripiprazole is excreted in urine, feces and bile. The total clearance is 0.7 ml / min / kg, which is mainly due to the excretion of the drug by the liver.

There were no differences in pharmacokinetic parameters in patients of the older age group, patients of different sex and race, smokers, people with severe renal impairment and decompensated liver cirrhosis compared with healthy volunteers.

Indications for use

• schizophrenia;
• manic episodes in bipolar I disorder of moderate to severe degree;
• prevention of new manic episodes in adult patients with predominantly manic episodes responsive to aripiprazole therapy;
• major depressive disorder (in addition to antidepressant medication).

Contraindications

Absolute:

• lactose intolerance, glucose-galactose malabsorption, deficiency of the enzyme lactase (since the tablets contain lactose);
• lactation period;
• children and adolescents up to 18 years old;
• hypersensitivity to aripiprazole or excipients of the drug.

Relative (Zilaksera is used with caution):

• diseases of the cardiovascular system (chronic heart failure, ischemic heart disease, conduction disturbances, myocardial infarction);
• conditions that can lead to arterial hypotension (hypovolemia, dehydration, use of antihypertensive drugs);
• cerebrovascular diseases;
• seizures or conditions that may be accompanied by seizures;
• family history of diabetes or obesity;
• increased risk of hyperthermia (overheating, intense physical activity);
• dehydration (since antipsychotics can disrupt thermoregulation);
• an increased risk of aspiration pneumonia (as this can lead to impaired motor function of the esophagus and further aspiration);
• the presence of a high risk of suicide, especially in patients aged 18 to 24 years.

Zilaxer, instructions for use: method and dosage

Zilaxer tablets are taken orally, once a day, regardless of food.

In schizophrenia, an initial dose of Zilaxera of 10 mg or 15 mg once a day is recommended, a maintenance dose of 15 mg once a day. The maximum dose is 30 mg per day.

In patients with manic episodes with bipolar I disorder, the starting dose of aripiprazole is 15 to 30 mg per day. If necessary, the dose is adjusted, but at intervals of at least 24 hours. The effectiveness of Zilaxera in daily doses of 15-30 mg has been demonstrated in clinical studies when the drug is taken by patients with manic episodes for 3-12 weeks. The safety of higher doses has not been evaluated.

Observations of patients with bipolar I disorder who underwent a mixed or manic episode, in whom the symptoms of the disease stabilized while taking Zilaxera at doses of 15 mg or 30 mg per day for 6 weeks, 6 months and then for 17 months, showed the beneficial effect of such supportive treatment.

The need for further supportive therapy is determined through periodic examination of patients.

In case of major depressive disorder, Zilaxera is used as an additional agent simultaneously with antidepressants. The initial dose of the drug is 5 mg per day. If the patient tolerates the treatment well, the dose can be increased by 5 mg per week until a maximum daily dose of 15 mg is reached. The duration of therapy is set individually.

In renal failure, mild to moderate hepatic failure, in the elderly and in smoking patients, dose adjustment is not required. In severe hepatic impairment, Zilaxer dosing is carried out with caution.

Side effects

• digestive system: very often - loss of appetite, nausea; often - vomiting, dyspeptic disorders, increased saliva secretion, increased appetite, dry mouth, constipation or diarrhea, a feeling of heaviness in the abdomen; infrequently - difficulty swallowing, dental caries, tongue edema, belching, ulceration and candidiasis of the oral mucosa, gingivitis, gastroesophageal reflux, stomatitis, periodontal abscess, loss of taste, gastroenteritis, gastritis, gastrointestinal hemorrhage, colitis, stomach ulcer, flatulence, rectal hemorrhage, fecaloma, fecal incontinence, hemorrhoids; rarely - inflammation of the tongue and red border of the lips, esophagitis, duodenal ulcer, bleeding of the gums, bloody vomiting, intestinal perforation, intestinal bleeding; very rarely - dysphagia, pancreatitis;
• hepatobiliary system: infrequently - cholecystitis; rarely - an increase in the size of the liver; very rarely - jaundice, hepatitis, increased activity of liver enzymes;
• metabolism and nutrition: often - weight loss; infrequently - thirst, edema, obesity, dehydration, hypokalemia, hypercholesterolemia, increased activity of lactate dehydrogenase and alkaline phosphatase, hyperlipidemia, increased blood urea; rarely - cyanosis, gout, acidification of urine, hypernatremia; very rarely - anorexia, hyponatremia;
• cardiovascular system: often - orthostatic hypotension, tachycardia; infrequently - palpitations, decreased blood pressure, bradycardia, phlebitis, deep vein thrombosis, prolongation of the QT interval on an electrocardiogram (ECG), hemorrhages, atrial fibrillation, AV blockade, extrasystole, myocardial infarction, myocardial ischemia, sudden cardiac arrest; rarely - atrial flutter, intracranial hemorrhage, expansion of the heart, cerebral ischemia, thrombophlebitis, vasovagal (Lewis) syndrome; very rarely - increased blood pressure, fainting; frequency unknown - thromboembolism;
• respiratory system: often - pneumonia, shortness of breath; infrequently - hiccups, nosebleeds, laryngitis; rarely - increased sputum secretion, hypoxia, hemoptysis, apnea, dryness of the nasal mucosa, respiratory failure, pulmonary edema; very rarely - aspiration pneumonia;
• lymphatic system and blood: infrequently - iron deficiency anemia; very rarely - a decrease in the number of platelets, leukocytes and neutrophils;
• nervous system: very often - headache, drowsiness, pathological restlessness; often - tremor, decreased concentration, dizziness, resistance to passive movements, confusion, sedation, extrapyramidal syndrome, lethargy; infrequently - tremor of the limbs, weakening of memory, amnesia, dyskinesia, muscle twitching, erectile dysfunction, increased or decreased libido, stupor, myoclonus, slowing down of mental function, impaired oculomotor reaction, dystonia, paresthesia, general slowness of movements, stroke, restless legs syndrome, increased sensitivity to stimuli, increased reflexes, depressed mood; rarely - euphoria, akinesia, decreased reflexes, delirium, depression of consciousness, neuroleptic malignant syndrome, buccoglossal syndrome; very rarely - convulsions,speech disorder;
• psyche: very often - insomnia; often - depression, hostility, manic thoughts, psychomotor agitation, nervousness, suicidal thoughts; infrequently - hyperactivity, panic reactions, self-perception disorder; rarely - obsessive thoughts;
• sense organs: often - photophobia, ear pain, blurred vision; infrequently - eye pain, dry eyes, inflammation of the middle ear, blepharitis, ringing in the ears; rarely - frequent blinking, diplopia, otitis externa, increased lacrimation, intraocular hemorrhage, decreased vision in one eye, deafness;
• musculoskeletal system and connective tissue: often - muscle stiffness, joint pain; infrequently - arthritis, muscle weakness, bursitis, myasthenia gravis, arthrosis, muscle spasms; very rarely - myalgia, tendon inflammation, rhabdomyolysis, degenerative changes in the tendon and inflammation of its synovial bag;
• urinary system: infrequently - frequent urination, dysuria, cystitis, polyuria, hematuria, albuminuria, false urge to urinate, predominance of nocturnal urine output over daytime, mucous discharge of white or yellowish color, renal failure, kidney stones; rarely - glucosuria, burning sensation in the external genitalia and urethra; very rarely - urinary retention or incontinence;
• genitals and mammary gland: infrequently - vaginal or uterine bleeding, vaginal candidiasis, amenorrhea, heavy menstruation, premature ejaculation; rarely - gynecomastia, cervicitis, pain in the mammary gland, complete or partial absence of orgasm, painful erection, galactorrhea; very rarely - long and painful erection;
• endocrine system: infrequently - diabetes mellitus, hypoglycemia; very rarely - diabetic ketoacidosis or coma, hyperglycemia;
• immune system: very rarely - laryngospasm, itching, nettle rash, anaphylactic reactions, Quincke's edema;
• skin and subcutaneous fat: often - itching and ulceration of the skin, dry skin; infrequently - eczema, seborrhea, blistering rash, acne, photosensitivity, pathological baldness; rarely - urticaria, excessive sweating, exfoliative dermatitis, maculopapular rash;
• laboratory data: very rarely - an increase in the activity of the enzyme creatine phosphokinase;
• other reactions: often - increased fatigue, asthenia, trembling, flu-like symptoms; infrequently - malaise, chills, chest pain, jaw pain, facial edema, jaw stiffness, peripheral edema; rarely - heaviness in the head, a feeling of squeezing and sore throat, heatstroke, a feeling of stiffness in the back, acid-aspiration pneumonitis, candidiasis; very rarely - pain in the neck and chest, impaired thermoregulation, increased body temperature.

Overdose

Described are individual cases of deliberate or accidental overdose of aripiprazole with a single dose of up to 1260 mg, which did not lead to death. Signs of substance intoxication include: increased blood pressure, tachycardia, lethargy, drowsiness, loss of consciousness. The main physiological parameters, as well as laboratory parameters and ECG parameters in patients hospitalized due to an overdose did not change significantly. Potentially dangerous symptoms of poisoning include transient loss of consciousness and extrapyramidal disorders.

The patient is given activated charcoal, good airway patency and effective ventilation of the lungs are provided, vital functions and ECG are monitored, and other supportive and symptomatic therapy is prescribed. The patient should be closely monitored until symptoms disappear completely. Hemodialysis is most likely ineffective, since aripiprazole is almost completely bound to plasma proteins.

special instructions

When using Zilaxera, the therapeutic effect develops gradually - over several days and even weeks. During this period, the patient should be monitored.

For patients with a tendency to suicidal attempts and thoughts, Zilaksera is prescribed in the minimum doses sufficient for treatment. Particularly careful monitoring is required for such patients.

If symptoms of tardive dyskinesia appear, it is necessary to reduce the dose of Zilaxera or completely cancel the drug.

Treatment with antipsychotics can lead to the onset of NMS (neuroleptic malignant syndrome), manifested by mental disorders, muscle rigidity, instability of the autonomic nervous system, rhabdomyolysis, acute renal failure, and an increase in creatine phosphokinase activity. All antipsychotics should be discontinued if unexplained fever or NMS symptoms develop.

Elderly patients (aged 56 to 99 years) with psychoses due to Alzheimer's disease are at increased risk of mortality during treatment with aripiprazole compared to patients in the placebo group.

In patients with diabetes mellitus, it is necessary to monitor the blood sugar level before starting therapy and periodically during treatment, as well as pay attention to possible symptoms of hyperglycemia (thirst, polyphagia, urinary frequency and weakness).

Weight gain is usually observed in individuals with severe risk factors (pituitary adenoma, thyroid disease, history of diabetes mellitus).

Antipsychotics can change the blood picture, causing neutropenia, agranulocytosis and leukopenia, therefore it is recommended to regularly monitor the corresponding parameters in patients at risk (especially in the first months of therapy).

Zilaxera, like other antipsychotics, can cause disturbances in thermoregulation. This feature should be taken into account in the case of prescribing the drug to patients with an increased risk of overheating as a result of physical exertion, dehydration, high temperature indoors or outdoors, as well as taking drugs with m-anticholinergic activity.

Aripiprazole may cause pathological gambling, regardless of whether the patient has gambled before.

Influence on the ability to drive vehicles and complex mechanisms

Before driving a car or other vehicles, the patient's individual sensitivity to Zilaxer should be established. In the absence of a negative effect on psychomotor functions, it is possible to perform work that requires a high concentration of attention and a quick reaction.

Application during pregnancy and lactation

Well-controlled scientific studies of the use of Zilaxer for the treatment of pregnant women have not been conducted. There are no data on the effect of the drug on reproductive function or the developing fetus. Newborns whose mothers took antipsychotic drugs in the third trimester are at risk of withdrawal and / or extrapyramidal disorders in the postpartum period. Patients should immediately inform the doctor about the pregnancy that has occurred during treatment or planned. During pregnancy, taking Zilaxera is possible only if the expected benefit from treatment outweighs the possible risk of side effects for the fetus.

Aripiprazole passes into breast milk, therefore, its use is contraindicated during lactation.

Pediatric use

In children and adolescents under the age of 18, Zilaksera is not used.

Drug interactions

Aripiprazole can enhance the therapeutic effect of antihypertensive drugs.

Zilaksera is used with caution in conjunction with medications that disturb the electrolyte balance or prolong the QT interval.

Famotidine (a blocker of H2-histamine receptors) reduces the rate of absorption of aripiprazole, but this does not affect the therapeutic effect of Zilaxera.

Zilaxer does not affect the pharmacodynamics and pharmacokinetics of warfarin and does not displace it from its association with proteins.

When using aripiprazole simultaneously with potent inhibitors of CYP2D6 and CYP3A4 isoenzymes (for example, ketoconazole and quinidine), the dose of Zilaxera should be reduced. Weak inhibitors of CYP2D6 or CYP3A4 isoenzymes (for example, escitalopram and diltiazem) slightly increase the plasma concentration of aripiprazole.

When used together with powerful inducers of isoenzymes CYP2D6 and CYP3A4, the metabolism of the drug increases, therefore it is necessary to adjust the dose of aripiprazole.

A clinically significant effect of Zilaxera on drugs that are metabolized with the participation of cytochrome isoenzymes CYP2D6, CYP2C19, CYP3A4 and CYP1A2 is unlikely.

Aripiprazole does not alter or slightly alter the pharmacokinetics of lamotrigine, venlafaxine, escitalopram, paroxetine, fluoxetine, and sertraline.

Ethanol can increase sedation, so drinking alcoholic beverages during treatment is not recommended.

Analogs

Zilaxer analogs are Alembic Pipzol, Aripiprazole-Teva, Aripiprazole OD-Teva, Amdoal, Abilify, Ariprizol, Mirium, etc.

Terms and conditions of storage

Store in original packaging at a temperature not exceeding 30 ° C. Keep out of the reach of children.

The shelf life of the tablets is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Zilaxer

Reviews about Zilaxer, like other neuroleptics, are rarely left by patients themselves. Most often, reviews of a drug are shared by doctors or relatives of patients receiving therapy with this drug. They note that aripiprazole is good at eliminating psychotic symptoms, evens mood, and does not cause drowsiness. The drug does not affect the patient's sleep and weight; adverse reactions are rare. It is convenient to take the tablets, since a single dose is required per day.

Zilaxer can only be prescribed by a doctor, since aripiprazole is not suitable for all patients. Another disadvantage is the high cost of the tablets.

The price of Zilaksera in pharmacies

The price of Zilaxer depends on the dosage and package size:

• tablets 10 mg (28 pcs. in a package) - 2880–3430 rubles;
• tablets 15 mg (28 pcs. in a package) - 3380-3900 rubles;
• tablets 30 mg (28 pcs. in a package) - 5590-6400 rubles.

Zilaxera: prices in online pharmacies

Drug name Price Pharmacy

Zilaxera 10 mg tablets 28 pcs. RUB 3089 Buy

Zilaxera 15 mg tablets 28 pcs. RUB 3715 Buy

Zilaxera tablets 15mg 28 pcs. RUB 4572 Buy

Zilaxera 30mg tablets 28 pcs. RUB 5766 Buy

Zilaxera 30 mg tablets 28 pcs. RUB 5766 Buy

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!