Zairis

The manufacturer of the drug Zayris is the Indian pharmaceutical corporation Cadila Healthcare 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 to block and eliminate acute attacks, as well as to conduct long-term maintenance therapy:

• In acute or chronic schizophrenia, including primary attacks of psychosis.
• Other mental disorders with productive symptoms:
  • The patient is showing aggressiveness.
  • Characterized by suspiciousness.
  • Pathology of thinking is clearly expressed.
  • The appearance of hallucinations.
  • The patient is delirious.
• Disorders with negative symptoms:
  • Emotional decline and inhibition.
  • Social alienation.
  • Emotional complexes.
  • Low speech content.
• Relief of affective deviations such as:
  • Depressive state.
  • Anxious excitement.
  • Fear.
• An indication for the use of Zairis is also a behavioral disorder in a patient diagnosed with dementia (acquired dementia, characterized by a persistent decrease in the cognitive abilities of the patient’s brain).
  • Manifestation of aggressive symptoms.
  • Outbursts of anger.
  • Physical violence.
  • Agitation (strong emotional excitement, accompanied by a feeling of anxiety and fear and turning into motor restlessness).
• Treatment of manic episodes in case of manic-depressive psychosis.
• Elimination of the causes of various manifestations of both an aggressive and apathetic nature, if they fit into the clinical picture of the disease.

[ 1 ], [ 2 ], [ 3 ]

Release form

Release form: film-coated tablet.

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

• One tablet contains 1 mg of active substance, as well as opadry Y1 7000 white.
• One tablet contains 2 mg of the active substance, as well as opadry 02N84915 pink.
• One tablet contains 4 mg of active substance, as well as opadry 02N51441 green.

Additional ingredients included in the tablet: lactose monohydrate, sodium lauryl sulfate, colloidal silicon dioxide anhydrous, hypromellose, 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 affinity with D2-dopamine and 5-TH2 _- serotonin receptors. The pharmacodynamics of Zairis also manifests itself in connection with α1-adrenoreceptors and has a slight affinity with α2-adrenal and H1-histamine receptors, without affecting cholinergic receptors, which are involved in the transmission of electrical impulses from one neuronal cell to another.

Despite the fact that the active substance is a very strong antagonist (this allows it to work effectively in relieving symptoms that accompany such a mental disorder as schizophrenia), Zairis does not significantly inhibit motor skills. Even when compared with the already familiar neuroleptics, it increases catalepsy to a lesser extent (a state resembling sleep, during which there is a decrease in sensitivity to both external and internal stimuli).

Zairis is an effective medicine for both productive and negative symptoms of schizophrenia.

[ 4 ], [ 5 ], [ 6 ]

Pharmacokinetics

Absorption. Upon closer examination, the pharmacokinetics of Zairis appear quite rosy. The active substance of the drug is perfectly absorbed into the intestine after oral administration of the tablet. After one to two hours, a blood plasma analysis shows its maximum concentration. At the same time, the time of taking the drug does not need to be matched with food intake.

Metabolism and excretion. The half-life of risperidone is approximately three hours. Its derivative (9-hydroxyrisperidone) takes about a day to be excreted. Zairis is distributed well and fairly quickly in the patient's body tissues. The distribution volumes are approximately 1-2 liters per kilogram of the patient's weight.

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

When taken orally (by mouth), 70% of the drug dosage is excreted through the kidneys in the urine, 14% is excreted in the feces.

In patients with impaired renal function, as well as in elderly people, the concentration of the drug in the blood is significantly higher, while the period of drug elimination from the body also increases. If the patient suffers from liver dysfunction, the concentration of the active substance of the drug Zairis in the blood plasma corresponds to the concentration observed with normal liver function. Prolongation of elimination, in this case, is not observed.

[ 7 ], [ 8 ], [ 9 ]

Dosing and administration

Zairis is taken orally. The required dosage should be swallowed and washed down with a glass of water. The method of administration and dosage of the drug depend on the diagnosis, the severity of the symptoms and the patient's condition.

Schizophrenia

Adults are prescribed this medicine once or twice a day. The starting daily dose of the drug is 2 mg, the next day the dosage is increased to 4 mg and then maintained at this level. If necessary, it can be adjusted, bringing it to 6 mg. The use of large doses - 10 mg daily - does not bring high efficiency (proven by clinical observations). But they can cause the development of extrapyramidal symptoms. Doses higher than 16 mg daily have not been studied, so this amount of the drug cannot be used.

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

The initial dosage for adolescents is recommended to be 0.5 mg per day, taken once in the morning or evening. If medically necessary, 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 3 mg/day. The expected effect is observed with daily doses from 1 to 6 mg, dosages above these figures have not been studied.

For patients who experience constant drowsiness and apathy, the dosage can be reduced by half, divided into two doses. It is difficult to talk about a specific amount for children under 13 suffering from schizophrenia, since there is no extensive experience with the use of Zairis.

Manic-depressive syndrome (bipolar disorder)

For 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 per day and not more often than every other day. The required positive result is usually obtained with a daily dosage of 1-6 mg.

For children and adolescents, the starting dosage is 0.5 mg, administered once a day in the morning and evening. If there is a therapeutic need, the dose can be individually increased at the rate of 0.5 or 1 mg. The dosage must be increased every other day, until reaching 2.5 mg daily. Therapeutic treatment is effective with daily doses from 0.5 to 6 mg. If such a side effect as drowsiness persists, the dose of the drug must be halved.

As with many other medications, the method of administration and dosage of Zairis must be adjusted throughout the course of treatment. There is virtually no experience with this medication in children under ten years of age for this pathology.

Dementia

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

After achieving the desired effect, the patient can be transferred to a single daily dose of 1 mg of Zairis. As with other medications, in this case the attending physician must keep the patient under constant supervision and adjust the amount of the drug taken.

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

Other psychiatric diseases

For patients weighing over 50 kg. The recommended starting dose is 0.5 mg once daily. During 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 dose for most patients is 0.5 mg once daily. However, in some cases, to achieve a positive effect, it is enough for patients to take no more than 0.25 mg once daily, while others may need 0.75 mg daily.

For patients weighing less than 50 kg. The recommended starting dose is 0.25 mg once daily. During 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 dose for most patients is 0.5 mg once daily. However, in some cases, to achieve a positive effect, it is enough for patients to take no more than 0.5 mg once daily, while others need 1.5 mg daily.

With prolonged use of Zairis, constant adjustment of the doses of the drug taken is necessary. There is no experience in taking this medicine by children under 5 years of age.

If the patient has a history of functional liver and kidney pathology. The suggested starting dosage is 0.5 mg twice a day. If necessary, on an individual basis, the dosage can be increased by 0.5 mg twice a day, bringing it to 1-2 mg twice a day. The treatment course of Zairis should be carried out with sufficient caution, under the constant supervision of a specialist, especially for patients in this group.

Use Zairis during pregnancy

Neither clinical nor laboratory observations have been conducted in women during pregnancy. Therefore, the use of Zairis during pregnancy is justified only if the expected necessary positive effect for the expectant mother exceeds the potential risk to the fetus, since taking antipsychotic drugs during the third trimester of pregnancy can have a rather negative effect on the psychosomatic development of the child. After birth, babies who received a dose of Zairis in the womb have an increased likelihood of acquiring the following deviations: agitation (strong emotional arousal), drowsiness, hypertension (high blood pressure), hypotension (low blood pressure), tremor, feeding disorders. Therefore, such babies need to be monitored more carefully.

A similar approach to prescribing the drug Zairis is necessary when a woman is breastfeeding her newborn child. Animal studies have shown that the active substance of the drug is excreted in breast milk. Therefore, if you cannot do without the drug, then it is advisable to stop breastfeeding.

Contraindications

Hypersensitivity to the active substance or to any component of the drug is perhaps the only thing that can be classified as a contraindication to the use of Zairis.

[ 10 ], [ 11 ]

Side effects Zairis

After using the drug, the side effects of Zairis are moderate or severe. They can be divided both by direction and by mode of action.

• Infections and the ability of cells to divide and invade surrounding tissues.
  • Infectious diseases of the upper respiratory and urinary tract (pharyngitis, tonsillitis, bronchitis, cystitis and others).
  • Otitis and cellulitis.
  • Flu.
  • And many others.
• Hematopoietic system:
  • Anemia.
  • Decreased platelet levels.
  • Neutropenia (decreased neutrophil levels in the blood).
  • And others.
• Immune system:
  • Acute anaphylactic reactions.
  • Swelling.
  • Allergic reactions.
• The system of exchange and metabolism.
  • Anorexia.
  • Diabetes mellitus.
  • Water intoxication.
  • Increased cholesterol in the blood.
  • Increase or decrease in appetite.
• Psychological aspects:
  • Anxiety and nervousness.
  • Insomnia.
  • Decreased overall tone of the body.
  • Decreased emotionality.
  • Confusion of consciousness.
  • Depressive state.
  • The emergence of all sorts of manias.
  • And others.
• Nervous system:
  • Parkinsonism.
  • Dizziness, headache.
  • Lethargic cases.
  • Loss of consciousness.
  • Cerebrovascular disorders.
  • Involuntary muscle contraction.
  • Spasms of facial muscles.
  • And many other manifestations.
• Organs of vision:
  • Conjunctivitis.
  • Swelling and itching.
  • Decreased vision.
  • Dry eyes and watery eyes.
  • Fear of light.
  • And others.
• Hearing organs – ringing in the ears.
• Cardiovascular system:
  • Tachycardia.
  • Arterial hypotension.
  • Hyperemia.
  • Sudden death.
  • Venous thromboembolism.
  • Abnormal ECG.
• Respiratory system:
  • Nasal congestion and nosebleeds.
  • Pneumonia.
  • Shortness of breath and wheezing.
  • Congestion 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.
  • Dry mouth.
  • Constipation and dyspepsia or fecal incontinence.
  • Stomach pain.
  • Distortion of taste.
  • Intestinal obstruction.
  • Toothache.
  • And others.
• Endocrine system - hyperprolactinemia.
• Skin:
  • Rash, dandruff.
  • Seborrheic dermatitis.
  • Eczema and itching.
  • And others.
• Musculoskeletal system:
  • Pain in the back and limbs.
  • Muscle weakness.
• Urinary system:
  • Urinary incontinence.
  • Urinary retention.
  • And others.
• Reproductive system:
  • Menstrual cycle disorders.
  • Enlargement of the mammary glands.
  • Impotence.
  • Retrograde ejaculation.
  • And others.

[ 12 ], [ 13 ]

Overdose

When taking significant doses of the drug Zairis, an overdose is possible, which begins to manifest itself with the following symptoms:

• Pronounced sedative effect.
• Drowsiness.
• Arterial hypotension.
• Tachycardia.
• Extrapyramidal disorders.
• Cramps.
• Atrial fibrillation.
• Hypersomnia.
• And some others.

There is no clear antidote in this case. In severe, acute overdose cases, it is necessary to begin detoxification measures as soon as possible, introduce adequate ventilation and oxygenation.

Such patients are recommended to undergo gastric lavage, take activated charcoal and laxatives. Throughout the process, continuous monitoring of the heart is necessary, including continuous ECG recording, to prevent acute development of arrhythmia.

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

[ 20 ], [ 21 ], [ 22 ]

Interactions with other drugs

In case of necessity of interaction of Zairis with other drugs, it is necessary to exercise extreme caution. This especially concerns drugs that in pharmacodynamics have a predisposition to prolongation of the QT interval of the cardiogram, since risperidone, the active substance of Zairis, has the same properties.

Such medications include, for example:

• antiarrhythmic drugs of class Ia: disopyramide, quinidine, procainamide.
• antiarrhythmic drugs of class III: amiodarone, sotalol.
• tricyclic antidepressants, such as amitriptyline.
• tetracyclic antidepressants, such as maprotiline.
• some antiarrhythmic drugs.
• a number of antipsychotic drugs.
• some antimalarial drugs: quinine and mefloquine.
• drugs that cause electrolyte imbalance.
• 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 (narcotic opium alkaloids), antihistamines (medicines that block the release of histamines into the human blood) and benzodiazepines (medicines of psychoactive substances with hypnotic, sedative and anticonvulsant effects).

Risperidone may be an antagonist of levodopa (an antiparkinsonian drug). When such a combination is necessary, especially in severe stages of Parkinson's disease, the minimum effective doses of Zairis should be prescribed. Clinically significant arterial hypotension has been observed with the simultaneous use of risperidone and antihypertensive drugs.

This drug does not significantly affect the pharmacokinetics of valproate, lithium, digoxin, or topiramate.

When risperidone is used in combination with other drugs that are significantly associated with plasma protein dynamics, there is no obvious displacement of one of the drugs from the protein fraction of the blood in the clinical picture.

Fluoxetine and paroxetine (inhibitors of liver enzymes) - increase the concentration of risperidone in the blood plasma. But this factor is less than the increase in antipsychotic fractions. It is believed that other inhibitors of liver 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 Zairis should be reviewed.

When using Zairis 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 when using other liver enzyme inducers (rifampicin, phenytoin, phenobarbital, and others). If carbamazepine (or a similar drug) is discontinued, the dosage of Zairis should be reviewed and reduced.

Amitriptyline does not modify the action of 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 or the activity of antipsychotic fractions.

Galantamine and donezepil do not significantly affect the pharmacokinetics of risperidone and the active antipsychotic fraction. Phenothiazines and some antidepressants can increase the percentage of risperidone in blood plasma.

[ 23 ], [ 24 ]

Storage conditions

The storage conditions for Zairis are no different from those of many other drugs. The temperature of the room in which this medicine is stored should not exceed 25 °C. The storage location for Zairis should not be inaccessible to children.

[ 25 ], [ 26 ]

Shelf life

The expiration date of the drug is necessarily indicated on the packaging and is 36 months (or three years). In the event that the shelf life of Zairis has expired, it is not recommended to use the drug. After the drug has been opened and used, removing the seal from the bottle, the expiration date is sharply reduced and is only one month.

[ 27 ]