Zairis

The manufacturer of the drug Zairis (Zayris) is the Indian pharmaceutical corporation Kadila Heltker Ltd. Risperidone is its international name, risperidone is also the main active substance of this drug.

Indications Zairis

The main indications for the use of Zairis are reduced to blocking and eliminating acute attacks, as well as prolonged maintenance therapy:

• In acute or chronic schizophrenia, including primary attacks of psychosis.
• Other mental disorders both with productive symptoms:
  • The patient is aggressive.
  • Differs suspicion.
  • The pathology of thinking is clearly expressed.
  • Occurrence of hallucinations.
  • The patient is delirious.
• Disorders with negative symptoms:
  • Emotional decline and retardation.
  • Social alienation.
  • Emotional complication.
  • Low speech fullness.
• Coping of affective abnormalities, such as:
  • Depressive state.
  • Anxious excitement.
  • Fear.
• The indication for the use of Zairis is the violation of the patient's behavior with the diagnosis of dementia (acquired dementia, characterized by a persistent decline in the cognitive abilities of the patient's brain).
  • Manifestation of aggressive symptoms.
  • Fits of anger.
  • Violence of the physical plane.
  • Agitation (strong emotional excitement, accompanied by a sense of anxiety and fear and turning into motor anxiety).
• Treatment of manic attacks in the case of manic-depressive psychosis.
• Elimination of the causes of all kinds of manifestations, both aggressive and apathetic, if they fit into the clinical picture of the disease.

[1], [2], [3]

Release form

Form release - a tablet coated.

The active substance is risperidone. The pharmacological market produces Zairis tablets of various quantitative content - risperidone in the preparation:

• One tablet contains 1 mg of active ingredient, as well as ya 7000 white.
• One tablet contains 2 mg of active ingredient, as well as 02H84915 pinkish opadri.
• One tablet contains 4 mg of active ingredient, as well as 02H51441 green.

Additional constituent elements included in the tablet: lactose monohydrate, sodium lauryl sulfate, silicon dioxide, anhydrous colloid, hypromelose, corn starch, magnesium stearate.

Pharmacodynamics

According to the mechanism of action, the active substance Zairis (risperidone) is an irreconcilable opponent of monoamines, which have high rates of kinship with D2-dopaminin and 5-TN ₂ -serotonin receptors. Pharmacodynamics Zayris also manifests itself in connection with α1 - adrenoreceptors and has a slight affinity with α2 - adrenovye and H1 - histamine receptors, without affecting the cholinergic receptors that participate in the transfer of electrical impulses from one cell to another neurons.

 Despite the fact that the active substance is the strongest antagonist (this allows him to work effectively at the relief of the symptomatology that accompanies such a mental disorder as schizophrenia), Zairis does not have a significant inhibition of motility of the movement. Even when compared with the already familiar neuroleptics, it lessens catalepsy to a lesser extent (a state resembling a dream, during which there is a decrease in sensitivity, both to external stimuli and to internal stimuli).

Zairis is an effective remedy, both with productive and negative symptoms of schizophrenia.

[4], [5], [6],

Pharmacokinetics

Suction. With closer examination, the pharmacokinetics of Zayris are drawn rather brightly. The active substance of the preparation is perfectly absorbed into the intestine after oral administration of the tablet. After one or two hours, the blood plasma analysis shows its maximum concentration. At the same time, the time of taking the medicine does not need to be combined with the ingestion of food.

Metabolism and excretion. The half-life of risperidone is approximately three hours. To derive its derivative (9-hydroxyrisperidone) takes about a day. Zairis is excellent and fairly quickly distributed in the tissues of the patient's body. Volumes of distribution approximately correspond to 1 - 2 liters per one kilogram of the patient's weight.

The process of connecting risperidone with plasma proteins is 88%, and 9-hydroxyrisperidone - 77%. The balance of the quantitative component of risperidone in the blood of the vast majority of patients is achieved within 24 hours, 9-hydroxyrisperidone - for four to five days.

At oral intake (through the mouth), 70% of the dosage of the drug is excreted through the kidneys with urine, 14% - goes along with the feces.

In patients who suffer from impaired renal function, as well as in elderly people, the concentration of the drug in the blood is much higher, while the withdrawal time from the body also increases. If the patient suffers from abnormalities in the liver, the concentration of active substance Zairis in the blood plasma corresponds to the concentration noted during normal liver function. Prolongation of the output, in this case, is not observed.

[7], [8], [9]

Dosing and administration

Zayris take inwards. The necessary dosage should be swallowed and filled with a glass of water. The method of application and dose of the drug depends on the diagnosis, the severity of the symptoms and the patient's condition.

Schizophrenia

Adults take this medication once or twice a day. The starting daily dose of the drug is equal to 2 mg, for the next day the dosage is increased to 4 mg and then kept at this level. If necessary, it can be adjusted, bringing up to 6 mg. The use of large doses - 10 mg daily - does not bring high efficacy (it is proved by clinical observations). But they can cause the development of extrapyramidal symptoms. Studies of dosages above 16 mg daily were not carried out, so this amount of the drug can not be used.

For elderly people, it is recommended to prescribe a starting dosage - 0.5 mg twice a day. If necessary, a single dose can be raised to 1-2 mg.

The initial dosage for adolescents is recommended from 0.5 mg per diem, which is drunk once in the morning or in the evening. With medical necessity, the amount of the drug can be increased by 0.5 or 1 mg per day, but not more often than every other day, until it reaches a figure of 3 mg / day. The expected effect is observed at daily doses from 1 to 6 mg, dosages above these figures have not been studied.

Patients who are constantly drowsy and apathy, the dosage can be reduced by half, divided into two doses. It is difficult to talk about a specific number for children under the age of 13 suffering from schizophrenia, since Zairis does not have a lot of experience.

Manic-depressive syndrome (bipolar disorder)

With this diagnosis, the recommended dosage for adults is 2 mg - 3 mg of the drug taken once a day. On an individual basis, if necessary, this number can be increased by 1 mg daily and no more than a day later. The required positive result is usually obtained at a daily dosage of 1-6 mg.

To children and adolescents, the starting dosage is prescribed from the figure - 0.5 mg, which is administered once during the day in the morning and in the evening. If there is a medical need, individually add the dose can be calculated at 0.5 or 1 mg. It is necessary to raise the dosage every other day, until the amount of 2.5 mg per day is reached. Therapeutic treatment is effective at daily doses of 0.5 to 6 mg. With a persistent manifestation of such a side effect as drowsiness, the dose of the drug should be reduced by half.

As in the case of many other drugs, the way of using and dosing Zairis should be adjusted throughout the treatment course. With this pathology, the experience of using this remedy in children under the age of ten is practically nonexistent.

Dementia

The starting daily dosage for adults is 0.25 mg divided into two doses. If there is a need, the dosage of the drug can be increased by 0.25 mg twice a day, but not more than every other day. The optimal single dose for most patients is 0.5 mg, taking twice a day, but there are cases of the need to increase to 1 mg twice a day.

After obtaining the desired effect, the patient can be transferred to a single daily dose of 1 mg Zaisis. As with other medications, in this case, the treating physician should keep the patient under constant observation and adjust the amount of the drug taken.

[14], [15], [16], [17], [18], [19]

Other psychiatric disorders

For patients who weigh more than 50 kg. The recommended starting dosage is 0.5 mg once a day. Within the treatment course, it is allowed to adjust the dose of Zairis by adding 0.5 mg of the drug, but not more often than every other day. The effective dosage of most patients is 0.5 mg once a day during the day. However, in some cases, in order to achieve a positive effect, it is enough for patients to take no more than 0.25 mg once a day, while others may need 0.75 mg per diem.

For patients with body weight does not exceed 50 kg. The recommended starting dosage is 0.25 mg once a day. Within the treatment course, it is allowed to adjust the dose of Zairis by adding 0.25 mg of the drug, but not more often than every other day. The effective dosage of most patients is 0.5 mg once a day during the day. However, in some cases, in order to achieve a positive effect, it is enough for patients to take no more than 0.5 mg once a day, while others need 1.5 mg per diem.

With prolonged use of Zairis, a constant adjustment of the doses of the drug is necessary. Experiences in taking this medication by children under the age of 5 years are not available.

If a history of the patient has a functional pathology of the liver and kidneys. The suggested starting dosage is 0.5 mg twice a day. If necessary, individually, the dose can be raised by 0.5 mg twice a day, bringing it to 1-2 mg two meals per day. Therapeutic course of Zairis should be performed with caution, under the constant supervision of a specialist, especially patients of this group.

Use Zairis during pregnancy

Both clinical and laboratory observations in women during pregnancy were not conducted. Therefore, the use of Zairis during pregnancy is justified only if the expected necessary positive effect for the expectant mother exceeds the potential risk for the fetus, since the use of antipsychotics during the third trimester of pregnancy can negatively affect the psychosomatic development of the child. After birth, babies who received a dose of Zairis in their mother's womb are more likely to acquire such abnormalities: agitation (severe emotional arousal), drowsiness, hypertension (high blood pressure), hypotension (low blood pressure), tremors, and feeding disorders. Therefore, these babies need to be looked after more carefully.

A similar approach to prescribing Zairis is also needed when a woman feeds her newborn baby with a breast. Animal studies have shown that the active substance of the drug is excreted into breast milk. Therefore, if you can not do without a medicine, then it is desirable to stop feeding.

 

Contraindications

Hypersensitivity to the active substance or to any component of the drug is, perhaps, the only thing that can be attributed to the category of contraindications to the use of Zaisis.

[10], [11]

Side effects Zairis

After using the drug, Zairis side effects are characterized by moderate or severe manifestations. You can distribute them both in the direction, and in the manner of the action.

• Infections and the ability of cells to divide and penetrate into surrounding tissues.
  • Infectious diseases of the upper respiratory and urinary tract (pharyngitis, tonsillitis, bronchitis, cystitis and others).
  • Otitis and cellulite.
  • Flu.
  • And many others.
• The system of hematopoiesis:
  • Anemia.
  • Decreased platelet count.
  • Neutropenia (reduction of the neutrophil count in the blood).
  • And others.
• The immune system:
  • Acute anaphylactic reactions.
  • Puffiness.
  • Allergic reactions.
• System of metabolism and metabolism.
  • Anorexia.
  • Diabetes.
  • Water intoxication.
  • The growth of cholesterol in the blood.
  • Increase or decrease in appetite.
• Psychological aspects:
  • Anxiety and nervousness.
  • Insomnia.
  • Decrease in the general tone of the body.
  • Decreased emotionality.
  • Confusion of consciousness.
  • Depressive state.
  • The appearance of all kinds of manias.
  • And others.
• Nervous system:
  • Parkinsonism.
  • Dizziness, headache.
  • Lethargic cases.
  • Loss of consciousness.
  • Cerebrovascular disorders.
  • Involuntary contraction of muscles.
  • Spasms of facial muscles.
  • And many other manifestations.
• Organs of vision:
  • Conjunctivitis.
  • Swelling and itching.
  • Decreased vision.
  • Dry eyes and tear.
  • Fear of light.
  • And others.
• The organs of hearing are ringing in the ears.
• The cardiovascular system:
  • Tachycardia.
  • Arterial hypotension.
  • Hyperemia.
  • Sudden death.
  • Venous thromboembolism.
  • Abnormal ECG.
• Respiratory system:
  • Nasal congestion and nasal bleeding.
  • Pneumonia.
  • Shortness of breath and wheezing.
  • Congestive events in the respiratory tract.
  • Sinusitis and swelling of the nasal cavity.
  • Productive cough.
• Side effects of Zairis in the digestive system:
  • Nausea, vomiting and diarrhea.
  • Dryness in the mouth.
  • Constipation and indigestion or fecal incontinence.
  • Pain in the stomach.
  • Distortion of taste.
  • Intestinal obstruction.
  • Toothache.
  • And others.
• The endocrine system is hyperprolactinaemia.
• Skin:
  • Rash, dandruff.
  • Seborrheic dermatitis.
  • Eczema and itching.
  • And others.
• Musculoskeletal system:
  • Pain in the back and extremities.
  • Muscle weakness.
• Urinary system:
  • Urinary incontinence.
  • Retention of urine.
  • And others.
• Reproductive system:
  • Malfunctions of the menstrual cycle.
  • Increased mammary glands.
  • Impotence.
  • Retrograde ejaculation.
  • And others.

[12], [13]

Overdose

When taking significant doses of Zairis, it is possible to overdose it, which begins to manifest itself with such symptoms:

• Significant sedation.
• Drowsiness.
• Arterial hypotension.
• Tachycardia.
• Extrapyramidal disorders.
• Convulsions.
• Atrial flutter-atrial fibrillation.
• Hypersomnia.
• And some others.

A single-valued antidote does not exist in this case. In severe, acute overdose, it is necessary, as soon as possible, to start measures for deintoxication of the body, introduce adequate ventilation and oxygenation.

Such patients are shown gastric lavage, reception of activated carbon and laxatives. Throughout the process, continuous cardiac monitoring is required, including a permanent ECG recording to prevent the acute development of arrhythmia.

With hypotension and collapse, adequate measures should be taken by administering intravenous infusions and / or administering sympathomimetics. In severe extrapyramidal disorders, anticholinergic drugs are prescribed. The patient should be under constant medical supervision until the symptoms of an overdose disappear completely.

[20], [21], [22]

Interactions with other drugs

If Zairis interacts with other drugs, extreme caution is necessary. This is especially true for drugs that in pharmacodynamics have a predisposition for lengthening the QT interval of the cardiogram, since risperidone, the active substance of Zairis, also has the same properties.

Such medicines, for example, include:

• antiarrhythmic drugs Ia class: disopyramide, quinidine, procainamide.
• antiarrhythmic drugs of the III class: amiodarone, sotalol.
• tricyclic antidepressants, for example, amitriptyline.
• tetracyclic antidepressants, for example, maprotiline.
• some antiarrhythmic drugs.
• a number of antipsychotic drugs.
• some antimalarials: quinine and mefloquine.
• drugs that cause an imbalance of electrolytes.
• and some others. This list is not complete.

Zairis should be used with caution in combination with other drugs that can affect the central nervous system, including alcohol, opiates (opiate addiction alkaloids), antihistamines (drugs blocking the release of histamines into the bloodstream), and benzodiazepines (medications of psychoactive substances with hypnotic, sedative and anticonvulsant effects).

Risperidone may be an antagonist of levodopa (an antiparkinsonian agent). In the case where such a combination is necessary, especially at a severe stage of Parkinson's disease, the minimum effective doses of Zaisis should be given. With the simultaneous use of risperidone and antihypertensive drugs, clinically significant arterial hypotension was observed.

This drug has no significant effect on the pharmacokinetics of valproate, lithium, digoxin or topiramate.

If risperidone is used in conjunction with other drugs that are largely associated with the dynamics of the protein in the blood plasma, there is no apparent visible displacement of one of the drugs from the protein fraction of the blood in the clinical picture.

Fluoxetine and paroxetine (inhibitors of hepatic enzymes) - increase the concentration of risperidone in blood plasma. But this factor is less than the increase in antipsychotic fractions. It is believed that other inhibitors of hepatic enzymes (such as quinidine) directly affect the concentration of risperidone in the blood plasma. With any change in the dosage of fluoxetine or paroxetine, the quantitative component of Zayris should be reviewed.

In the application of Zaisis, in combination with carbamazepines, a decrease in the concentration of the active antipsychotic fraction of risperidone in the blood plasma was noted. A similar result can be observed with the use of other inducers of hepatic enzymes (rifampicin, phenytoin, phenobarbital and others). If carbamazepine (or a similar drug) is canceled, the dosage of Zayris should be reviewed and reduced.

Amitriptyline does not introduce any correction into the actions of the drug Zairis or active antipsychotic fractions. Cimetidine and ranitidine increase the biological penetration of risperidone, but minimally activate antipsychotic fractions. Erythromycin does not change the pharmacokinetics of risperidone and the activity of antipsychotic fractions.

Galantamine and doonezepil, do not have a particular effect on the pharmacokinetics of risperidone and the active antipsychotic fraction. Phenothiazines and some antidepressants can increase the percentage of risperidone in the blood plasma.

[23], [24]

Storage conditions

Do not differ from the conditions of many other preparations and the storage conditions of Zairis. The temperature of the room in which this medical product is stored should not exceed 25 ° C. The storage location of Zairis must not be accessible to children.

[25], [26]

Shelf life

The shelf life of the drug is mandatory indicated on the package and is 36 months (or three years). In case the storage time of Zairis has come to an end, it is not recommended to use the drug. After the drug has been opened and started to be applied, having removed the seal from the bottle, the shelf life is sharply reduced and is only one month.

[27]