Risperidone drops instructions for use. When is the drug needed? Side effects of risperidone

LSR-004845/10-270510

Tradename: Risperidone

International non-proprietary name:

risperidone

Dosage form:

film-coated tablets

Compound:

1 film-coated tablet contains:
active substances: risperidone 1 mg, 2 mg and 4 mg;
Excipients: calcium hydrogen phosphate dihydrate, povidone (plasdon K 29/32 or collidon 30), pregelatinized starch (C*Pharm starch), magnesium stearate, microcrystalline cellulose;
film composition: Selecoat AQ-02003 (Hypromellose 2910 (Hydroxypropyl Methylcellulose 2910), Macrogol-6000 (Polyethylene Glycol 6000), Titanium Dioxide).

Description: Tablets, film-coated white or almost white, round, biconvex. On a cross section - almost white color.

Pharmacotherapeutic group:

antipsychotic (neuroleptic)

ATX code:[N05AX08]

Pharmacological properties

Pharmacodynamics.
Antipsychotic agent (neuroleptic), a derivative of benzisoxazole. It also has a sedative,. antiemetic and hypothermic action. Selective monoaminergic antagonist, has a high tropism for serotonergic 5-HT 2 and dopaminergic D 2 receptors. It also binds to alpha1-adrenergic receptors with a slightly lower affinity for H1-histaminergic and alpha2-adrenergic receptors. It does not have tropism for cholinergic receptors.
The antipsychotic effect is due to the blockade of dopamine D 2 receptors of the mesolimbic and mesocortical systems. The sedative effect is due to the blockade of adrenoreceptors of the reticular formation of the brain stem; antiemetic effect - blockade of dopamine D 2 receptors in the trine zone of the vomiting center; hypothermic action - blockade of dopamine receptors of the hypothalamus.
Suppresses productive symptoms (delusions, hallucinations, aggressiveness), automatism. Causes less suppression of motor activity and induces catalepsy to a lesser extent than classical antipsychotic drugs (neuroleptics). Balanced central antagonism to serotonin and dopamine can reduce the propensity for extrapyramidal side effects and extend the therapeutic effect of the drug to cover the negative and affective symptoms of schizophrenia.
May induce a dose-dependent increase in plasma prolactin concentration.

Pharmacokinetics
Absorption is fast and complete. Food does not affect the completeness and speed of absorption. TS max risperidone - 1 h, 9-hydroxyrisperidone - 3 h (with high activity of the CYP2D6 isoenzyme) and 17 h (with low activity of the CYP2D6 isoenzyme). Plasma concentrations of risperidone are dose-proportional. The equilibrium concentration of risperidone in most patients is achieved within 1 day, 9-hydroxy-risperidone - after 4-5 days.
Risperidone is rapidly distributed in the body. Penetrates into the central nervous system (CNS), breast milk. The volume of distribution is 1-2 l/kg. Plasma protein binding (with alpha1-acid glycoprotein and albumin) of risperidone is 90%, 9-hydroxyrisperidone is 77%.
It is metabolized by the CYP2D6 isoenzyme to the active metabolite, 9-hydroxyrisperidone (risperidone and 9-hydroxyrisperidone constitute the active antipsychotic fraction). Another route of metabolism of risperidone is N-dealkylation.
The half-life of risperidone is 3 hours; 9-hydroxyrisperidone and active antipsychotic fraction - 20-24 hours.
It is excreted by the kidneys (70%: 35-45% of them - in the form of a pharmacologically active fraction) and intestines (14%).
A single dose study of the drug revealed higher plasma concentrations and slower elimination in elderly patients and in patients with renal insufficiency. Excretion is slowed down in elderly patients and in patients with renal insufficiency.
In hepatic insufficiency, plasma levels of risperidone are increased by 35%.

Indications for use

• schizophrenia (acute and chronic) and other psychotic conditions with productive and/or negative symptoms;
• affective disorders in various mental illnesses;
• behavioral disorders in patients with dementia with symptoms of aggressiveness (outbursts of anger, physical violence), mental disorders (arousal, delirium) or psychotic symptoms;
• as adjuvant therapy in the treatment of mania in bipolar disorders;
• as an adjunct therapy for behavioral disorders in adolescents from 15 years of age and adult patients with a reduced intellectual level or mental retardation, in cases where destructive behavior (aggressiveness, impulsivity, auto-aggression) is leading in the clinical picture of the disease.

Contraindications

• hypersensitivity;
• lactation period;
• children's age (up to 15 years) - efficacy and safety have not been established.

Carefully used for brain tumors, intestinal obstruction, drug overdose, Reye's syndrome (the antiemetic effect of risperidone may mask the symptoms of these conditions), diseases of the cardiovascular system (chronic heart failure, atrioventricular blockade, myocardial infarction), dehydration, cerebrovascular accident, hypovolemia, Parkinson's disease , convulsions (including history), drug abuse, drug dependence, severe renal failure, severe liver failure, conditions predisposing to the development of pirouette-type tachycardia (bradycardia, electrolyte imbalance, concomitant medication prolonging the QT interval), pregnancy.

Dosage and administration
Applied inside. Adults and children over 15 years of age are prescribed 1 or 2 times a day.
Schizophrenia. The initial dose is 2 mg / day. On day 2 - up to 4 mg / day. From this point on, if necessary, the dose can either be kept at the same level, or individually adjusted in the range of 4-6 mg / day.
Doses above 10 mg/day have not been shown to be more effective than lower doses and may cause extrapyramidal symptoms. The maximum daily dose is 16 mg.
Behavioral disorders in patients with dementia: The optimal dose is 1 mg 1 time per day.
Bipolar disorders in mania: initial dose - 2 mg / day for 1 dose. Increasing the dose (by 2 mg / day) - no more than every other day. The optimal dose is 2-6 mg / day.
Behavioral disorders in patients with mental retardation or with the dominance of destructive tendencies in the clinical picture. Patients weighing 50 kg or more. The optimal dose is 1 mg / day.
It is recommended to reduce both the initial dose and subsequent dose increases by 2 times in elderly patients and in patients with renal or hepatic insufficiency (if necessary, use an adequate dosage form).

Side effect
From the side of the central nervous system: insomnia, agitation, anxiety, headache, drowsiness, fatigue, dizziness, decreased ability to concentrate, blurred vision, extrapyramidal symptoms (tremor, rigidity, hypersalivation, bradykinesia, akathisia, acute dystonia), mania or hypomania, stroke (in the elderly patients with predisposing factors). In patients with schizophrenia, hypervolemia (either due to polydipsia or due to a syndrome of inappropriate secretion of antidiuretic hormone), tardive dyskinesia (involuntary rhythmic movements, mainly of the tongue and / or face), neuroleptic malignant syndrome (hyperthermia, muscle rigidity, instability of autonomic functions , disturbance of consciousness and increased activity of creaginphosphokinase), thermoregulation disorders, epileptic seizures.
From the digestive system: constipation, dyspepsia, nausea or vomiting, abdominal pain, increased activity of "liver" transaminases, dry mouth, hyposalivation or hypersalivation, anorexia.
From the side of the cardiovascular system: orthostatic hypotension, reflex tachycardia or increased blood pressure (BP).
From the side of the hematopoietic organs: neutropenia, thrombocytopenia.
From the endocrine system: galactorrhea, gynecomastia, menstrual irregularities, amenorrhea, weight gain or loss, hyperglycemia, or exacerbation of pre-existing diabetes mellitus.
From the genitourinary system: priapism, erectile dysfunction, ejaculation disorders, orgasm disorders, including anorgasmia, urinary incontinence.
Allergic reactions: itching, rash, angioedema.
From the side of the skin: dry skin, hyperpigmentation, seborrhea, photosensitivity.
Others: arthralgia, rhinitis.

Overdose
Symptoms: drowsiness, sedation, tachycardia, decreased blood pressure, extrapyramidal disorders, rarely - prolongation of the QT interval.
Treatment: ensure free airway patency to ensure adequate oxygen supply and ventilation, gastric lavage (after intubation if the patient is unconscious) and administration of activated charcoal along with a laxative. Start ECG monitoring immediately to detect possible arrhythmias. There is no specific antidote. It is necessary to carry out symptomatic therapy aimed at maintaining the vital functions of the body. With a decrease in blood pressure and vascular collapse - intravenously inject infusion solutions and / or adrenostimulants. In case of development of acute extrapyramidal symptoms, anticholinergic drugs. Constant medical supervision and monitoring should be continued until the symptoms of intoxication disappear.

Interaction with other drugs
Risperidone reduces the effectiveness of levodopa and dopamine agonists. Phenothiazines, tricyclic antidepressants and beta-blockers increase the plasma concentration of risperidone (do not affect the concentration of the active antipsychotic fraction).
With the simultaneous administration of carbamazepine and other inducers of microsomal enzymes, a decrease in the concentration of the active antipsychotic fraction of risperidone in plasma is noted. Clozapine reduces the clearance of risperidone.
With simultaneous use of ethanol with risperidone, drugs that depress the central nervous system (CNS) lead to additive depression of CNS function.
Antihypertensive drugs increase the severity of blood pressure reduction against the background of the use of risperidone.
Fluoxetine may increase the plasma concentration of risperidone (to a lesser extent, its active antipsychotic fraction).

special instructions
In schizophrenia, at the beginning of treatment with risperidone, it is recommended to gradually withdraw previous therapy if clinically warranted. If patients are transferred from therapy with depot antipsychotic drugs, it is recommended to start taking instead of the next scheduled injection. The need to continue ongoing antiparkinsonian therapy should be periodically assessed.
The risk of developing mania or hypomania can be significantly reduced by using low doses of risperidone or by gradually increasing them.
If orthostatic hypotension occurs, especially in the initial period of dose selection, dose reduction should be considered. In patients with diseases of the cardiovascular system, as well as dehydration, hypovolemia or cerebrovascular disorders, the dose of risperidone should be increased gradually. If signs and symptoms of tardive dyskinesia occur, consideration should be given to discontinuing all antipsychotic drugs. In neuroleptic malignant syndrome, all antipsychotic drugs, including risperidone, should be discontinued.
With the abolition of carbamazepine and other inducers of microsomal enzymes, the dose of risperidone should be reduced.
Patients should be advised to refrain from overeating due to the possibility of weight gain.
During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

Release form:

Film-coated tablets, 1 mg, 2 mg and 4 mg.
10, 20 or 30 tablets in a blister pack made of PVC film and printed lacquered aluminum foil. 1,2, 3, 5, 6, 10 blister packs of 10 tablets each or 1, 3, 5 blister packs of 20 tablets each, or 1, 2, 3 blister packs of 30 tablets each with instructions for use placed in a cardboard box.

Storage conditions
List B. In a dry, dark place at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Best before date:

2 years.
Do not use after the expiration date. Leave conditions: prescription.

Manufacturer:

CJSC "Canonpharma production" Address: 141100 Schelkovo, Moscow region, st. Zarechnaya, 105

Compound

One tablet contains: active ingredient - risperidone - 1 mg and 2 mg; excipients - lactose monohydrate, starch 1500, anhydrous colloidal silicon dioxide, magnesium stearate, opadry II (including polyvinyl alcohol, talc, macrogol 3350, pink coloring pigment (contains titanium dioxide E 171, iron oxide red E 172, iron oxide black E 172) or a green coloring pigment (contains aluminum lacquer based on quinoline yellow E 104, aluminum lacquer based on sunset yellow E 110, aluminum lacquer based on indigo carmine E 132)).

Description

Film-coated tablets, dosage of 1 mg - light green color and dosage of 2 mg - pink, with a biconvex surface, with a score.

Indications for use

Risperidone is indicated for the treatment of schizophrenia, moderate to severe manic episodes in bipolar disorder, for the short-term treatment (up to 6 weeks) of persistent aggression in patients with moderate to severe Alzheimer's disease dementia who fail to respond to non-pharmacological treatments at risk of harm to yourself or those around you.

Contraindications

Hypersensitivity to risperidone or to any of the excipients. Patients with hereditary galactose intolerance, lactase deficiency or malabsorption of glucose-galactose.

Carefully

Brain tumor, intestinal obstruction, drug overdose, Reye's syndrome, diseases of the cardiovascular system (chronic heart failure, previous myocardial infarction, AV blockade), dehydration, cerebrovascular accident, hypovolemia, Parkinson's disease, seizures (including a history of ), drug dependence, severe renal / hepatic insufficiency, conditions predisposing to the development of pirouette-type tachycardia (bradycardia, electrolyte imbalance, concomitant use of drugs that lengthen the QT interval), pregnancy.

Dosage and administration

inside. It is unacceptable to divide a 1 mg tablet. If it is necessary to use doses less than 1 mg, other dosage forms of risperidone should be prescribed.

Schizophrenia Adults: The starting dose for all patients is 2 mg once or twice daily. The dose may be increased to 4 mg per day on the second day of use. Subsequently, the dose can be individually adjusted if necessary.

The usual optimal dose is 4-6 mg per day. Doses above 10 mg do not increase the effect, but may increase the risk of extrapyramidal symptoms. It is not recommended to use doses of more than 16 mg / day.

Elderly patients:

Manic phases in bipolar disorder.

Adults: The initial dose is 2 mg once a day. The increase in dose should be carried out no more than 24 hours later and be 1 mg per day. The recommended dose range is from 1 to 6 mg per day, depending on the degree of effectiveness and individual tolerance. It is necessary to regularly evaluate the feasibility of further use of risperidone.

Elderly patients: For initial treatment, other dosage forms should be used that allow dosing of risperidone in 0.5 mg increments. This form is used for maintenance treatment at 1-2 mg twice a day.

Persistent aggression in patients with moderate to severe dementia in Alzheimer's disease For initial treatment, other dosage forms should be used that allow dosing of risperidone in 0.5 mg increments. This form is used for maintenance treatment at 1 mg twice a day. The use of risperidone for more than 6 weeks is not recommended. During treatment, it is necessary to monitor the condition of patients and assess the feasibility of further use of the drug.

Renal and liver failure Regardless of severity, the initial and subsequent doses should be halved and titration should be slower.

Food intake does not affect the absorption of risperidone. Gradual discontinuation of the drug is recommended. Acute manifestations of the withdrawal syndrome, including nausea, vomiting, sweating, insomnia, were observed very rarely. Reappearance of psychotic symptoms is possible. Cases of involuntary movement disorders (such as akathisia, dystonia and dyskinesia) have been reported.

Switching from other antipsychotics to risperidone treatment. Gradual discontinuation of the other drug is recommended when switching to risperidone treatment. When switching from depot neuroleptics, it is recommended to start risperidone therapy instead of the next scheduled injection.

Side effect

The most common adverse drug reactions (AEs) (incidence > 10%) are: parkinsonism, headache and insomnia. The following are AEs that have been reported in medical practice. In this case, the following classification of AEs is applied according to the frequency of occurrence: very often (> 1/10); often (>1/100 to<1 / 10); нечасто (от >1 /1000 up to<1/ 100), редко (от >1/10000 to<1 / 1000); очень редко (<1 / 10000), неизвестно (не может быть оценена исходя из имеющихся данных). Внутри каждой группы, нежелательные явления представлены в порядке уменьшения степени тяжести.

From the side of laboratory data:

Common: Elevated blood prolactin, weight gain.

Infrequently: Prolongation of the QT interval and other changes on the electrocardiogram, increased blood glucose, transaminases, eosinophils, reduced numbers of leukocytes, hemoglobin, blood creatine phosphokinase, fever.

Rare: Decreased body temperature.

Heart disorders:

Common: Tachycardia.

Uncommon: Atrioventricular block, His bundle block, atrial fibrillation, sinus bradycardia, palpitations.

Hematopoietic and lymphatic system disorders:

Uncommon: Anemia, thrombocytopenia.

Rare: Granulocytopenia.

Not known: Agranulocytosis.

Immune system disorders:

Rare: Hypersensitivity to the drug.

Not known: Anaphylactic reaction.

Metabolic and nutritional disorders:

Common: Increased appetite, decreased appetite.

Uncommon: Anorexia, polydipsia.

Very rare: Diabetic ketoacidosis.

Not known: Water intoxication.

Mental disorders:

Very common: Insomnia.

Common: Restlessness, agitation, sleep disturbances.

Uncommon: Confusion, mania, decreased libido, apathy, irritability.

Rare: Anorgasmia, emotional flattening.

Nervous system disorders:

Very common: Parkinsonism, headache.

Often: Akathisia 2 , dizziness, tremor 2 , dystonia 2 , drowsiness, sedation, lethargy, dyskinesia.

Uncommon: Lack of response to stimuli, loss of consciousness, syncope, depression of consciousness, transient ischemic attack, dysarthria, attention disturbances, increased drowsiness, postural dizziness, balance disturbance, tardive dyskinesia, incoordination of movements, hypoesthesia.

Rare: Neuroleptic malignant syndrome, diabetic coma, cerebrovascular disorders, cerebral ischemia, movement disorders.

Violations of the organ of vision:

Common: Blurred vision.

Uncommon: Conjunctivitis, ocular hyperemia, discharge, oedema, dry eyes, increased lacrimation, photophobia.

Rare: Decreased visual acuity, eye rolling, glaucoma.

Hearing and inner ear disorders:

Uncommon: Ear pain, tinnitus

Respiratory, thoracic and mediastinal disorders:

Common: Dyspnea, epistaxis, cough, nasal congestion, pharyngo-laryngeal pain.

Uncommon: Wheezing, aspiration pneumonia, pulmonary edema, respiratory distress, wheezing, airway obstruction, dysphonia.

Rare: Sleep apnea syndrome, hyperventilation

Gastrointestinal disorders:

Common: Vomiting, diarrhea, constipation, nausea, abdominal pain, dyspepsia, dry mouth, stomach discomfort.

Uncommon: Difficulty swallowing, gastritis, fecal incontinence, coprolit.

Rare: Bowel obstruction, pancreatitis, lip edema, cheilitis.

Renal and urinary tract disorders:

Common: Enuresis.

Uncommon: Dysuria, stress incontinence, pollakiuria.

Reproductive system and mammary gland disorders:

Uncommon: Amenorrhea, sexual dysfunction, erectile dysfunction, ejaculation disorders, galactorrhea, gynecomastia, menstrual disorders, vaginal discharge.

Not known: Priapism.

Skin and subcutaneous tissue disorders:

Common: Rash, erythema.

Uncommon: Angioedema, skin lesions, skin inflammation, pruritus, acne, discoloration of the skin, alopecia, seborrheic dermatitis, dry skin, hyperkeratosis.

Rare: Dandruff.

Musculoskeletal, connective tissue and bone disorders:

Common: Arthralgia, back pain, pain in extremities.

Uncommon: Muscle weakness, myalgia, neck pain, joint swelling, posture disorders, joint stiffness, musculoskeletal chest pain.

Rare: Rhabdomyolysis.

Endocrine system disorders:

Rare: Disturbances in secretion of antidiuretic hormone.

Liver and biliary tract disorders:

Rare: Jaundice.

Common: Pneumonia, influenza, bronchitis, upper respiratory infections, urinary tract infections.

Uncommon: Sinusitis, viral infection, ear infection, tonsillitis, panniculitis, otitis media, ocular inflammation, local infection, acarodermatitis, respiratory infections, bladder inflammation, onychomycosis.

Rare: Chronic otitis media.

Vascular disorders:

Uncommon: Hypotension, orthostatic hypotension, flushing.

Complications of a general nature and reactions at the injection site

Often: Hyperthermia, fatigue, peripheral edema, general weakness, chest pain.

Uncommon: Facial swelling, gait disturbance, discomfort, sluggishness, flu-like illness, thirst, chest discomfort, chills.

Rare: Generalized edema, hypothermia, withdrawal syndrome, cold extremities.

Weight gain

Weight gain (> 7% of body weight) has been found in patients with schizophrenia treated with risperidone.

Additional information on the use of the drug in special groups of patients

In elderly patients with dementia or children, compared with adult patients, the following were more often observed: transient ischemic attack and stroke in 1.4% and 1.5% of cases, respectively. The following AEs have been reported in >5% of cases: urinary tract infections, peripheral edema, drowsiness, cough.

The use of atypical antipsychotics in elderly patients with dementia has been associated with increased mortality.

Overdose

Symptoms Drowsiness/lethargy, tachycardia, arterial hypotension and extrapyramidal symptoms. In rare cases, prolongation of the QT interval, ventricular arrhythmias and convulsions.

Treatment Providing and maintaining airway patency, as well as the necessary oxygenation and ventilation. Gastric lavage (after intubation, if the patient is unconscious) and the use of activated charcoal together with a laxative no more than one hour after the use of the drug. Monitoring of the state of the cardiovascular system, including continuous electrocardiographic monitoring. There is no specific antidote. With hypotension and vascular collapse, intravenous fluids and / or sympathomimetics, in case of severe extrapyramidal symptoms, the use of anticholinergic drugs.

Interaction with other drugs

Caution is advised when prescribing risperidone with drugs that prolong the QT interval, such as class 1a antiarrhythmics (quinidine, disopyramide, procainamide), class III (amiodarone, sotalol), tricyclic antidepressants (amitriptyline), tetracyclic antidepressants (maprotiline), some antihistamines, other antipsychotic drugs, certain antimalarial drugs (quinocide and mefloquine), and drugs that cause electrolyte disturbances (hypokalemia, hypomagnesemia), bradycardia, or suppress the hepatic metabolism of risperidone.

Risperidone should be used with caution in combination with other centrally acting drugs: alcohol, opiates, antihistamines and benzodiazepines.

Risperidone may block the effect of levodopa and other antiparkinsonian drugs.

Hypotension is possible with the concomitant use of risperidone with antihypertensive drugs.

Risperidone has no clinically significant effect on the pharmacokinetics of lithium, valproate, digoxin, or topiramate.

Carbamazepine, rifampicin, phenytoin and phenobarbital reduce plasma concentrations of the active antipsychotic fraction of risperidone.

Fluoxetine, paroxetine, quinidine, verapamil, phenothiazines, tricyclic antidepressants and beta-blockers, cimetidine and ranitidine increase the plasma concentration of risperidone (to a lesser extent or insignificantly the concentration of the active antipsychotic fraction).

Galantamine and donepezil do not have a clinically significant effect on the pharmacokinetics of risperidone and the active antipsychotic fraction.

Amitriptyline, erythromycin do not affect the pharmacokinetics of risperidone or the active antipsychotic fraction.

Erythromycin does not affect the pharmacokinetics of risperidone and the active antipsychotic fraction.

Precautionary measures

Simultaneous use with Furosemide There was an increase in mortality in patients taking furosemide with risperidone. Concomitant use of risperidone with other diuretics (mainly low-dose thiazide diuretics) has not been associated with increased mortality. Caution should be exercised and the benefit / risk ratio should be assessed when using the drug in the above combination. In the treatment of elderly patients with dementia, dehydration should be avoided, because. it was a common risk factor for death.

Cerebrovascular adverse events (CV AEs) There was a significant increase (approximately 3-fold) in the incidence of CV AEs, such as stroke (including fatal) and transient ischemic attack. Risperidone should be used with caution in patients with risk factors for stroke. Patients or caregivers should be advised to immediately notify their healthcare provider of signs and symptoms of potential CV AEs, such as sudden weakness or numbness of the face, arms or legs, speech or vision problems. All treatment options should be considered without delay, including discontinuation of risperidone.

orthostatic hypotension(Orthostatic) hypotension may develop, especially during initial dose titration. Clinically significant hypotension has been observed with concomitant use of risperidone with antihypertensive drugs. Risperidone should be used with caution in patients with cardiovascular disease (eg, heart failure, myocardial infarction, conduction disturbances, dehydration, hypovolemia, or cerebrovascular disease) and the dose should be titrated gradually as recommended. With the development of hypotension, the dose of the drug should be reduced.

Tardive dyskinesia / extrapyramidal symptoms The use of risperidone is associated with the induction of tardive dyskinesia characterized by rhythmic involuntary movements, predominantly of the tongue and/or face. The occurrence of extrapyramidal symptoms is a risk factor for the development of tardive dyskinesia. If signs appear, all antipsychotics should be discontinued.

Malignant neuroleptic syndrome Neuroleptic malignant syndrome characterized by hyperthermia, muscle rigidity, autonomic nervous system disorders, altered states of consciousness, and elevated creatine phosphokinase levels have been reported with antipsychotic medications. Additional signs may include myoglobinuria (rhabdomyolysis) and acute renal failure. All antipsychotics, including risperidone, should be discontinued.

Parkinson's disease and dementia with Lewy bodies Parkinson's disease and dementia may worsen with risperidone. Manifestations of hypersensitivity may include confusion, dullness of pain sensitivity, postural instability with frequent falls in addition to extrapyramidal symptoms.

hyperglycemia Very rare cases of hyperglycemia or exacerbation of pre-existing diabetes have been reported. It is advisable to conduct appropriate clinical monitoring of the condition of patients.

Hyperprolactinemia Risperidone should be used with caution in patients with hyperprolactinemia and in patients with prolactin-dependent tumours.

OT interval prolongation Very rare cases of QT prolongation have been reported. Caution should be exercised when prescribing risperidone to patients with cardiovascular disease or a family history of QT prolongation, bradycardia, or electrolyte disturbances (hypokalemia, hypomagnesemia).

convulsions Risperidone should be used with caution in patients with a history of seizures and other factors that lower the seizure threshold.

Priapism Priapism may develop with risperidone.

Body temperature regulation Caution is advised when prescribing to patients who may experience an increase in body temperature with increased physical activity, exposure to heat, concomitant use of anticholinergic drugs, dehydration.

Patients with hereditary problems of galactose intolerance, the Lapp-lactase deficiency or glucose-galactose malabsorption should not take risperidone.

Pregnancy and lactation

Pregnancy When administered, the development of extrapyramidal disorders and / or withdrawal syndrome in newborns whose mothers took Risperidone during the third trimester of pregnancy is possible.

Lactation

Risperidone and 9-hydroxy-risperidone may be excreted in breast milk in small amounts. The benefits of breastfeeding and the potential risks to the baby should be assessed on a case-by-case basis.

Best before date

2 years. Do not use after the expiration date.

Risperidone is a drug that helps to normalize the general mental state of the body.

The drug is available in the form of round-shaped tablets, which are film-coated and placed in a blister-type blister pack of 10 pieces. The contour packaging is placed in a pack of cardboard base. One pack may contain 1, 2, 3, 5, 6, 10 contour packs.

Constituent components:

• active element- risperidone;
• additional components- povidone, starch, calcium hydrogen phosphate dihydrate, magnesium stearate, cellulose, as excipients.

Pharmacological properties

Risperidone is an atypical drug that has an anxiolytic effect. It belongs to the group of antipsychotic drugs.

The active substance of the drug causes selective blocking of serotonin 5-HT2 and dopamine D2 receptors. Also it binds to alpha1 and alpha2 adrenergic receptors. Does not affect cholinergic receptors.

Despite the fact that the main constituent of the drug causes blocking of D2 receptors, it does not have a depressing effect on motor activity compared to other antipsychotics, it causes the least.

The antipsychotic effect is associated with the blocking of D2 receptors, the sedative effect is associated with the blocking of the adrenoreceptors of the brain stem of the head, and the antiemetic effect is associated with the blocking of the D2 receptors responsible for the vomiting center.

As a result of the use of the drug, hallucinations, automatism, the state of aggressiveness, and delirium are eliminated. Depending on the dosage, it can cause an increase in the level of prolactin in the blood.

Pharmacokinetics of the drug

The drug has a rapid and complete absorption. Eating does not affect the degree of absorption. The maximum concentration level can be determined 60 minutes after taking the medicine.

The drug is distributed throughout the body, most of it penetrates the central nervous system, the level of concentration in the body is directly proportional to the dosage. Almost 90% binds to proteins. The half-life is about 3 hours. Approximately 14% of the drug is excreted through the intestines, almost 70% is excreted through the kidneys.

In what situations is the drug prescribed

Risperidone is taken for the following indications:

Restrictions and contraindications for use

• during severe liver and kidney disorders;
• hypersensitivity or intolerance to the constituent components of the drug;
• lactation;
• at ;
• during prostate adenoma;
• if there is glaucoma;
• age up to 15 years.

With caution, the drug is used for the following disorders and conditions:

• if available ;
• with heart failure with a chronic course;
• if there is a prolongation of the QT interval;
• with myocardial infarction;
• in the event of seizures;
• during myocardial infarction;
• if there are convulsions;
• during dehydration;
• pregnant women;
• during intestinal obstruction.

How to take your medicine safely and effectively

The drug is taken orally. Adults and children over the age of 15 should take the medication twice a day. You should start taking 2 mg per day with a further transition to 4-6 mg. Elderly patients should take 0.5 mg twice a day.

During mania, which are accompanied by bipolar disorder, you need to take 2 mg per day, after a day the dose is increased by 2 mg and then increased by 4-6 mg per day.

During dementia, which is accompanied by behavioral disorders, you need to take 0.25 mg of the drug 2 times a day. In the future, the dose is increased by 0.25 mg to 0.5 mg per day or 1 mg 2 times a day.

Use during pregnancy and lactation

During pregnancy, the drug can be prescribed only by a doctor and in case of urgent need, only in cases where the expected benefit to the mother is higher than the expected risk to the child.

Since the constituent components of the drug enter the composition of breast milk, it is best to stop breastfeeding for the period of treatment.

The drug can be dangerous: overdose and "side effects"

• state of tachycardia;
• increased sedation;
• the occurrence of increased drowsiness;
• hypotension;
• violations .

When the above symptoms appear, gastric lavage is performed, the use of sorbents and laxatives is prescribed. If the patient is unconscious, then intubation is scheduled. ECG monitoring is done, as arrhythmia is possible.

During the use of the drug Risperidone, the following side effects may occur:

Special instructions are important!

During the use of the drug, you must pay attention to the following instructions:

1. With extreme caution, the drug is used by patients with problems with the functioning of the heart and blood vessels, as well as with dehydration, with cerebrovascular disorders, hypovolemia. When taken, the dosage increases gradually.
2. If a state of hypotension occurs, the dosage should be reduced.
3. With caution, a remedy is used to treat patients with, because the drug may worsen the patient's condition.
4. Do not use in conjunction with drugs of central action.
5. During the treatment period, it is best not to overeat, because the drug can cause a sharp increase in weight.
6. During treatment, you should refrain from driving a car, as well as from performing work that requires increased attention.

Risperidone Organika is a domestic replacement for foreign analogues

• Round biconvex tablets, film-coated white or almost white. In cross section, the nucleus is white or almost white. film-coated tablets Tablets, film-coated white or almost white, round, biconvex, scored on one side. Tablets, film-coated white or almost white, round, biconvex. On a cross section - almost white color. Tablets, film-coated, yellow, round, biconvex (dosage 2 mg). Tablets on a break of white or almost white color. Tablets, film-coated yellow, round, biconvex; on a break of white or almost white color. Film-coated tablets from light green to green, round, biconvex; on a break of white or almost white color. Light green to green film-coated tablets, round, biconvex (dosage 4 mg). Tablets on a break of white or almost white color. Pink or pale pink film-coated tablets, round, biconvex, scored on one side.

pharmachologic effect

Risperidone is an antipsychotic drug, a derivative of benzisoxazole, also has a sedative, antiemetic and hypothermic effect. Risperidone is a selective monoaminergic antagonist with high affinity for serotonergic 5-HT2 and dopaminergic D2 receptors. Risperidone also binds to ?1-adrenergic receptors and, somewhat weaker, to H1-histaminergic and ?2-adrenergic receptors. Risperidone has no affinity for cholinergic receptors. The antipsychotic effect is due to the blockade of D2-dopaminergic receptors of the mesolimbic and mesocortical systems. Risperidone reduces the productive symptoms of schizophrenia (delusions, hallucinations), aggressiveness, automatism, induces catalepsy to a lesser extent than typical antipsychotics. Balanced central antagonism to serotonin and dopamine can reduce the propensity for extrapyramidal side effects and extend the therapeutic effect of the drug to cover the negative and affective symptoms of schizophrenia. Clinical Data Schizophrenia The efficacy of risperidone in the short-term treatment of schizophrenia was demonstrated in four studies lasting 4 to 8 weeks, which included 2500 patients who met DSM-IV criteria for schizophrenia. In a 6-week placebo-controlled study, when titrated to a dose of 10 mg/day twice daily, risperidone was superior to placebo on the Brief Psychiatric Rating Scale (BPRS). In a 6-week, placebo-controlled study using four fixed doses of risperidone (2, 6, 10, and 16 mg/day, twice daily), risperidone was superior to placebo in Group 4 on the Positive and Negative Syndromes Rating Scale ( PANSS). In an 8-week comparative study of five fixed doses of risperidone (1, 4, 8, 12, and 16 mg/day twice daily), risperidone in the 4, 8, and 16 mg/day groups was superior to risperidone 1 mg/day on a scale PANSS. In a 4-week comparative placebo-controlled study of two fixed doses of risperidone (4 and 8 mg/day, once daily), risperidone was superior to placebo in both groups on several PANSS items. Manic Episodes in Bipolar Disorder The efficacy of risperidone as monotherapy for acute manic episodes in bipolar I disorder has been demonstrated in three double-blind, placebo-controlled studies in approximately 820 patients with bipolar I disorder, according to the DSM-IV scale. In these three studies, risperidone at doses of 1-6 mg/day (initial dose of 3 mg in two studies and 2 mg in one study) was statistically superior to placebo in the primary endpoint, i.e. change in Young's Mania Rating Scale (YMRS) scores. 3 weeks from baseline. The results for the secondary efficacy endpoints were broadly consistent with the results for the primary endpoint. The percentage of patients with >50% decrease in YMRS score at 3 weeks from baseline was significantly higher for risperidone than for placebo. The efficacy of risperidone in combination with mood regulators in the treatment of mania has been demonstrated in two three-week, double-blind studies in approximately 300 patients who meet DSM-IV criteria for bipolar I disorder. In a 3-week study, risperidone at doses of 1 to 6 mg/day, starting at 2 mg/day, in combination with lithium or valproate was only superior to lithium or valproate at the end of the study on the primary outcome measure, i.e., change in total score for YMRS scale compared to baseline at the third week. Long-term aggression in dementia The effectiveness of risperidone in the treatment of psycho-behavioral symptoms of dementia, including behavioral problems such as aggression, agitation, psychosis, activity and affective disorders, was demonstrated in three double-blind, placebo-controlled studies in 1150 patients with moderate and severe dementia. One study was conducted at fixed doses of 0.5, 1 and 2 mg/day. Two studies have studied non-fixed doses, including groups with doses of 0.5 to 4 mg/day and 0.5 to 2 mg/day of risperidone, respectively. Risperidone has been shown to be clinically and statistically highly effective in the treatment of aggression and, to a lesser extent, agitation and psychosis in elderly patients with dementia (as measured by the Alzheimer's Behavioral Pathology Scale (BEHAVE-AD) and the Cohen Mansfield Arousal Inventory (CMAI)). Conduct disorders The efficacy of risperidone in the short-term treatment of aggressive behavior has been demonstrated in placebo-controlled trials in approximately 240 patients aged 5 to 12 years with DSM-IV disruptive conduct disorder and below average intellectual functioning or mild to moderate mental retardation. learning disorders. In both studies, risperidone at doses of 0.02 to 0.06 mg/kg/day was significantly more effective than placebo in the pre-specified primary efficacy endpoint.

Pharmacokinetics

Absorption Risperidone after oral administration is completely absorbed, reaching the maximum concentration in the blood plasma after 1-2 hours. Food does not affect the absorption of risperidone, so it can be given with or without food. Distribution Risperidone is rapidly distributed in the body, penetrates into the central nervous system and breast milk. The volume of distribution is 1-2 l/kg. In plasma, risperidone binds to albumin and ?1-acid glycoprotein. Risperidone is 88% bound to plasma proteins, 9-hydroxyrisperidone is 77%. The equilibrium concentration of risperidone in the body in most patients is reached within one day. The equilibrium concentration of 9-hydroxyrisperidone is reached after 4-5 days. The concentration of risperidone in plasma is proportional to the dose of the drug (within therapeutic doses). Metabolism Risperidone is metabolized by the CYP2D6 isoenzyme to 9-hydroxy risperidone, which has similar pharmacological effects to risperidone. Risperidone and 9-hydroxyrisperidone constitute the active antipsychotic fraction. The CYP2D6 isoenzyme is subject to genetic polymorphism. In CYP2D6 heavily metabolized patients, risperidone is rapidly converted to 9-hydroxyrisperidone, while in patients with poor metabolism, this transformation is much slower. Although heavily metabolizing patients have lower risperidone concentrations and higher 9-hydroxyrisperidone concentrations than poor metabolizing patients, the net pharmacokinetics of risperidone and 9-hydroxyrisperidone (the active antipsychotic fraction) after single or multiple doses are similar in heavily metabolizing and poor metabolizing patients. metabolism by the CYP2D6 isoenzyme. Another route of metabolism of risperidone is N-dealkylation. Withdrawal The half-life (T1 / 2) of risperidone after oral administration in patients with psychosis is about 3 hours. T1 / 2 of 9-hydroxyrisperidone and the active antipsychotic fraction is 24 hours. After a week of taking the drug, 70% of the dose taken is excreted by the kidneys, 14% - through the intestines. In urine, risperidone and 9-hydroxyrisperidone account for 35-45% of the administered dose. The rest is inactive metabolites. A single dose study of risperidone showed higher plasma concentrations and slower elimination in elderly patients and in patients with renal insufficiency. The concentration of risperidone in blood plasma in patients with chronic liver failure did not change, however, the average concentration of the free fraction of risperidone increased by 35%.

Special conditions

Switching from therapy with other antipsychotics At the beginning of treatment with Risperidone, it is recommended to gradually withdraw the previous therapy, if clinically warranted. In this case, if patients are transferred from therapy with depot forms of antipsychotic drugs, then it is recommended to start therapy with Risperidone instead of the next scheduled injection. The need to continue current antiparkinsonian therapy should be periodically assessed. Use in Elderly Patients with Dementia Elderly patients with dementia treated with atypical antipsychotics have experienced increased mortality compared with placebo in studies of atypical antipsychotics, including risperidone. When using risperidone for this population, the incidence of deaths was 4.0% for patients taking risperidone, compared with 3.1% for placebo. The reason for this increased risk is currently unknown. The causes of death were varied, the main causes being cardiovascular (rhythm disturbances, sudden cardiac death, increased risk of strokes, thromboembolism) and infectious diseases (pneumonia). The median age of deceased patients is 86 years (range 67–100 years). For elderly patients with dementia, increased mortality was observed with concomitant use of furosemide and risperidone (7.3%, mean age 89 years, range 75-97 years) compared with the group taking only risperidone (4.1%, mean age 84 years, range 75-96 years) and the furosemide-only group (3.1%, mean age 80 years, range 67-90 years). No pathophysiological mechanisms have been established to explain this observation. However, special care should be taken when prescribing the drug in such cases. There was no increase in mortality in patients taking other diuretics concomitantly with risperidone. Regardless of treatment, dehydration is a common risk factor for mortality and should be carefully monitored in elderly patients with dementia. Cerebrovascular disorders In elderly patients with dementia treated with atypical antipsychotics, there has been an increased risk of cerebrovascular adverse reactions in randomized, placebo-controlled clinical trials. A pooled analysis of the results of six placebo-controlled studies of risperidone, mainly in elderly patients (over 65 years of age) with dementia, showed that cerebrovascular adverse reactions (serious and non-serious, combined) occurred in 3.3% (33/1009) of patients treated with risperidone and 1.2% (8/712) of patients receiving placebo. Odds ratio 2.96 (95% confidence interval). The mechanism of this risk has not been studied. An increased risk cannot be excluded for other antipsychotics and other patient groups. Risperidone should be used with caution in patients with risk factors for stroke. The risk of adverse cerebrovascular reactions is significantly higher in patients with mixed or vascular dementia than in those with Alzheimer's dementia. Therefore, patients with mixed or vascular dementia are not recommended to prescribe risperidone. The risks and therapeutic benefits of the use of risperidone in elderly patients with dementia should be assessed, taking into account the predictive risk factors for stroke in an individual patient. The patient and his environment should be warned about the need for urgent medical attention if there are signs of cerebrovascular accident, such as sudden weakness or numbness of the face, arms or legs, impaired speech or vision. In this case, all therapeutic options are urgently considered, including the withdrawal of risperidone. Risperidone should only be used in the short-term treatment of persistent aggression in patients with moderate to severe Alzheimer's dementia, as an add-on treatment for non-pharmacological treatments that have failed, or where there is a potential risk of harm to self and/or others. During treatment with risperidone, frequent and regular assessment of the patient's condition is necessary to decide whether to continue treatment. Orthostatic hypotension In connection with the?-adrenergic blocking effect of risperidone, a pronounced decrease in blood pressure (hypotension, including orthostatic), especially during the initial dose selection, may occur. A clinically significant decrease in blood pressure is observed with the joint appointment of risperidone with antihypertensive drugs. If a decrease in blood pressure occurs, dose reduction should be considered. In patients with diseases of the cardiovascular system, as well as dehydration, hypovolemia or cerebrovascular disorders, the dose should be increased gradually, according to the recommendations. QT interval prolongation As with other antipsychotic drugs, caution should be exercised when prescribing risperidone to patients with a history of arrhythmias, with congenital prolongation of the QT interval, and when used together with drugs that increase the QT interval. And also with bradycardia or electrolyte disorders (hypokalemia, hypomagnesemia), as this may increase the risk of developing arrhythmias. Tardive dyskinesia and extrapyramidal disorders The use of drugs that can block dopamine receptors may be accompanied by the induction of tardive dyskinesia (involuntary rhythmic movements, mainly of the tongue and / or face). There are reports that the occurrence of extrapyramidal symptoms is a risk factor for tardive dyskinesia. If signs and symptoms of tardive dyskinesia occur, discontinuation of all antipsychotics should be considered. Neuroleptic Malignant Syndrome If neuroleptic malignant syndrome occurs, characterized by hyperthermia, muscle rigidity, autonomic instability, altered consciousness, and increased creatine phosphokinase activity (myoglobinuria (due to rhabdomyolysis) and acute renal failure may also occur), all antipsychotic drugs, including risperidone, should be discontinued. Parkinson's disease and dementia with Lewy bodies When using antipsychotics, including risperidone, in patients with Parkinson's disease or dementia with Lewy bodies, the physician must evaluate the benefit/risk ratio. The course of Parkinson's disease may worsen with the use of risperidone. Both groups of patients are at risk of developing neuroleptic malignant syndrome, as well as hypersensitivity to neuroleptic drugs. Manifestations of hypersensitivity, in addition to extrapyramidal symptoms, may be confusion, dullness of sensitivity, postural instability with frequent falls. Seizure Threshold In patients with a low seizure threshold, Risperidone should be used with caution as the risk of seizures is increased. Hyperglycemia and Diabetes Mellitus During treatment with Risperidone, hyperglycemia, diabetes mellitus or an exacerbation of pre-existing diabetes mellitus may occur. In rare cases, ketoacidosis and diabetic coma may develop. A family history of diabetes mellitus and obesity are predisposing factors for the onset of hyperglycemia and diabetes mellitus. In all patients, it is necessary during the period of treatment with Risperidone to conduct clinical monitoring for the presence of symptoms of hyperglycemia and diabetes mellitus, and control of body weight. Regulation of body temperature When using antipsychotic drugs, there may be a violation of the central regulation of body temperature. It is recommended to monitor patients while using risperidone, especially in the event of conditions that contribute to an increase in body temperature (for example, exercise, visiting a bath / sauna), while using drugs with anticholinergic action or in patients with dehydration. Antiemetic effect Risperidone has an antiemetic effect in preclinical studies. This effect, if it occurs in humans, can mask the objective and subjective symptoms of overdose of certain antipsychotic drugs, as well as diseases such as intestinal obstruction, Reye's syndrome and brain tumor. Venous thromboembolism Cases of venous thromboembolism have been described with the use of antipsychotic drugs. Since patients taking antipsychotics are often at risk of developing venous thromboembolism, all possible risk factors should be identified before and during treatment with risperidone and preventive measures should be taken. Hyperprolactinemia Tissue culture studies have shown that cell growth in breast tumors can be stimulated by prolactin. Risperidone should be used with caution in patients with hyperprolactinemia and in patients with potentially prolactin-dependent tumours. Intraoperative flabby iris syndrome Intraoperative flabby iris syndrome (ISDR) was observed during surgery for the presence of cataracts in patients receiving therapy with α1-adrenergic antagonists. ISDR increases the risk of complications associated with the organ of vision during and after surgery. The doctor performing such an operation should be informed in advance that the patient has taken or is currently taking drugs that have ?1-adrenergic agonist activity. The potential benefit of discontinuing β1-adrenergic antagonist therapy before surgery has not been established and should be weighed against the risks associated with discontinuing antipsychotic therapy. During treatment with Risperidone, regular examination of CNS function for extrapyramidal and other movement disorders is recommended. Priapism Due to the blocking effect of risperidone on β-adrenergic receptors, priapism may occur during drug treatment. Leukopenia, neuropenia, agranulocytosis When using antipsychotic drugs, incl. Risperidone, leukopenia/neutropenia and agranulocytosis may occur. Therefore, before using the drug Risperidone, especially in patients with risk factors for the development of leukopenia / neutropenia, it is necessary to perform a clinical blood test with a leukocyte count. Patients with a clinically significant decrease in the number of leukocytes in the blood or drug-induced leukopenia / neutropenia should be observed during the first few months of treatment. If a patient has severe neutropenia, fever or other symptoms of infection should be carefully monitored. In patients with severe neutropenia (absolute neutrophil count less than 1000/mm3), in the absence of other causes, treatment with Risperidone is recommended to be discontinued until the leukocyte count is fully restored. Drowsiness Drowsiness is the most common side effect with risperidone and its severity depends on the dose. Aspiration pneumonia When using antipsychotic drugs, incl. risperidone, esophageal dysmotility and aspiration have been reported. Aspiration pneumonia is the most common cause of morbidity and mortality in patients with Alzheimer's dementia. Risperidone should be used with caution in patients at risk of developing aspiration pneumonia. Weight gain Due to the fact that the use of the drug Risperidone can lead to a significant increase in body weight, it is necessary to monitor the body weight of patients during therapy with Risperidone and give recommendations to the patient on the diet during the treatment period. If orthostatic hypotension occurs, especially at the beginning of treatment, consideration should be given to reducing the dose of the drug. In patients with diseases of the cardiovascular system, as well as dehydration, hypovolemia or cerebrovascular disorders, the dose of the drug should be increased gradually. With the abolition of carbamazepine and other inducers of "liver" enzymes, the dose of risperidone should be reduced. Withdrawal syndrome Gradual withdrawal of risperidone is recommended because after a sharp cessation of treatment with high doses of antipsychotics, the development of a “withdrawal” syndrome is possible. Symptoms of the "withdrawal" syndrome: very rarely described nausea, vomiting, sweating, insomnia. Children and adolescents Before risperidone is prescribed to a child or adolescent with a behavioral disorder, it is necessary to fully assess the causes of aggressive behavior, exclude pain, social problems. The sedative effect of risperidone should be closely monitored in children and adolescents due to possible decreased learning ability. Changing the timing of risperidone use may increase sedation and reduce attention in children and adolescents. Due to the possible effects of long-term hyperprolactinemia on growth and puberty in children and adolescents, regular clinical and laboratory evaluation of endocrinological status is necessary: ​​height, weight, puberty, menstrual cycle control, as well as other potential effects of prolactin. Influence on the ability to drive vehicles and mechanisms During the period of treatment with risperidone, care should be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions. Overdose Symptoms Drowsiness, sedation, tachycardia, decreased blood pressure, extrapyramidal symptoms, depression of consciousness. Rarely - prolongation of the QT interval, convulsions. Bidirectional ventricular tachycardia has been reported with co-administration of an elevated dose of risperidone and paroxetine. In case of overdose, the possibility of overdose from taking multiple drugs should be considered. Treatment In acute overdose, it is necessary to ensure free airway patency to ensure adequate oxygen supply and ventilation, ECG monitoring, symptomatic therapy aimed at maintaining vital body functions, gastric lavage. The appointment of activated charcoal and laxatives should be carried out only if no more than one hour has passed since the drug was taken. With a pronounced decrease in blood pressure or vascular collapse, intravenous infusion solutions should be administered and / or sympathomimetic drugs should be used. With the development of extrapyramidal symptoms, anticholinergic drugs (eg, trihexyphenidyl) are prescribed. Constant medical supervision should be continued until the symptoms of intoxication completely disappear. There is no specific antidote.

Compound

• 1 tab. risperidone 2 mg Excipients: lactose monohydrate 155 mg, microcrystalline cellulose 30 mg, povidone 7 mg, magnesium stearate 2 mg, colloidal silicon dioxide 4 mg. 1 tab. risperidone 2 mg 1 tab. risperidone 2 mg Excipients: lactose monohydrate 82 mg, microcrystalline cellulose 12 mg, pregelatinized corn starch 2 mg, magnesium stearate 1 mg, potato starch 7 mg, povidone 4 mg. 1 tab. risperidone 4 mg 1 tab. risperidone 4 mg Excipients: lactose monohydrate 153 mg, microcrystalline cellulose 30 mg, povidone 7 mg, magnesium stearate 2 mg, colloidal silicon dioxide 4 mg. The composition of the film shell: Opadry II 85F240012 Pink 6 mg, including polyvinyl alcohol 2.4 mg, macrogol 3350 1.463 mg, iron dye red oxide 0.024 mg, iron dye yellow oxide 0.013 mg, talc 0.888 mg, titanium dioxide 1.212 mg. 1 film-coated tablet contains: active substances: risperidone 4 mg; excipients: calcium hydrogen phosphate dihydrate, povidone (plasdon K 29/32 or collidon 30), pregelatinized starch (C * Pharm starch), magnesium stearate, microcrystalline cellulose; composition of the film shell: selecoat AQ-02003 (hypromellose 2910 (hydroxypropyl-methylcellulose 2910), macrogol-6000 (polyethylene glycol 6000), titanium dioxide). active substance risperidone - 2 mg Excipients (core): lactose monohydrate (milk sugar) - 82.0 mg; microcrystalline cellulose - 12.0 mg; pregelatinized corn starch (Starch 1500) - 2.0 mg; magnesium stearate - 1.0 mg; potato starch - 7.0 mg; povidone (medium molecular weight polyvinylpyrrolidone) - 4.0 mg. Shell composition: Opadry II - 3 mg (polyvinyl alcohol, partially hydrolyzed - 1.2000 mg; talc - 0.4440 mg; macrogol (polyethylene glycol 3350) - 0.6060 mg; titanium dioxide E 171 - 0.6561 mg; aluminum varnish based on quinoline yellow - 0.0903 mg; aluminum varnish based on sunset yellow - 0.0021 mg; iron dye oxide (II) yellow E 172 - 0.0009 mg; aluminum varnish based on indigo carmine - 0.0006 mg). active substance risperidone - 4 mg Excipients (core): lactose monohydrate (milk sugar) - 114.0 mg; microcrystalline cellulose - 19.7 mg; pregelatinized corn starch (Starch 1500) - 3.0 mg; magnesium stearate - 1.0 mg; potato starch - 11.0 mg; povidone (medium molecular weight polyvinylpyrrolidone) - 7.3 mg. Shell composition: Opadry II - 5 mg (polyvinyl alcohol, partially hydrolyzed - 2.2000 mg; talc - 1.0000 mg; macrogol (polyethylene glycol 3350) - 0.6175 mg; titanium dioxide E 171 - 0.6545 mg; soy lecithin E 322 - 0.1750 mg; aluminum varnish based on yellow quinoline - 0.1010 mg; aluminum varnish based on indigo carmine - 0.2520 mg) active substance: risperidone - 2.000 mg; excipients: lactose monohydrate - 145,000 mg; microcrystalline cellulose - 40,000 mg; corn starch - 10,000 mg; colloidal silicon dioxide - 1,000 mg; magnesium stearate - 2,000 mg; film coating: [hypromellose - 3.600 mg, talc - 1.200 mg, titanium dioxide - 0.660 mg, macrogol 4000 (polyethylene glycol 4000) - 0.540 mg] or [dry mix for film coating containing hypromellose (60%), talc (20%) , titanium dioxide (11%), macrogol 4000 (polyethylene glycol 4000) (9%)] - 6,000 mg. active substance: risperidone - 4,000 mg; excipients: lactose monohydrate - 290,000 mg; microcrystalline cellulose - 80,000 mg; corn starch - 20,000 mg; colloidal silicon dioxide - 2,000 mg; magnesium stearate - 4,000 mg; risperidone 2 mg excipients: pregelatinized corn starch (starch 1500) - 43.3 mg; colloidal silicon dioxide (aerosil) - 0.5 mg; magnesium stearate monohydrate - 0.3 mg; stearic acid - 0.6 mg; MCC - 43.3 mg; Opadry II white (polyvinyl alcohol - 2 mg, talc - 0.74 mg, macrogol (polyethylene glycol) - 1.01 mg, titanium dioxide - 1.25 mg) - 5 mg Risperidone 2 mg; Auxiliary substances: MCC, lactose monohydrate, povidone, sodium carboxymethyl starch, colloidal silicon dioxide, magnesium stearate risperidone 4 mg 11 mg, povidone 7.3 mg. The composition of the film shell: Opadry II 5 mg (polyvinyl alcohol, partially hydrolyzed 2.2 mg, talc 1 mg, macrogol 0.6175 mg, titanium dioxide 0.6545 mg, soy lecithin 0.175 mg, aluminum varnish based on yellow quinoline 0.101 mg, aluminum varnish based on indigo carmine 0.252 mg). risperidone 4 mg excipients: pregelatinized corn starch (starch 1500) - 86.6 mg; colloidal silicon dioxide (aerosil) - 1 mg; magnesium stearate monohydrate - 0.6 mg; stearic acid - 1.2 mg; MCC - 86.6 mg; Opadry II white (polyvinyl alcohol - 4 mg, talc - 1.48 mg, macrogol (polyethylene glycol) - 2.02 mg, titanium dioxide - 2.5 mg) - 10 mg Risperidone 4 mg; Auxiliary substances: MCC, lactose monohydrate, povidone, sodium carboxymethyl starch, colloidal silicon dioxide, risperidone magnesium stearate 2 mg Excipients: calcium hydrogen phosphate dihydrate, povidone (plasdon K 29/32 or collidone 30), pregelatinized starch (C * Pharm starch ), magnesium stearate, cellulose microcrystalline composition of the film shell: selecoat AQ-02003 (hypromellose 2910 (hydroxypropyl-methylcellulose 2910), macrogol-6000 (polyethylene glycol 6000), titanium dioxide). risperidone 4 mg excipients: calcium hydrogen phosphate dihydrate, povidone (plasdon K 29/32 or collidon 30), pregelatinized starch (C * Pharm starch), magnesium stearate, cellulose methylcellulose 2910), macrogol-6000 (polyethylene glycol 6000), titanium dioxide).

Risperidone indications for use

• treatment of schizophrenia in adults and children aged 13 to 17; treatment of manic episodes associated with bipolar disorder, moderate and severe severity in adults and children over 10 years of age; short-term (up to 6 weeks) treatment of persistent aggression in patients with dementia due to Alzheimer's disease, moderate to severe, not amenable to non-pharmacological methods of correction, and if there is a risk of harm by the patient to himself and / or others; short-term (up to 6 weeks) symptomatic treatment of persistent aggression in the structure of conduct disorder in children aged 5 years and older and adolescents with mental retardation, diagnosed in accordance with DSM-IV, in which, due to the severity of aggression or other destructive behavior, medical treatment is required . Pharmacotherapy should be part of a broader treatment program, including psychological and educational interventions. Risperidone should be prescribed by a pediatric neurologist

Risperidone contraindications

• Hypersensitivity to risperidone. Hypersensitivity to risperidone. Application during pregnancy and lactation Application during pregnancy is possible if the expected benefit of therapy for the mother outweighs the potential risk to the fetus. If necessary, use during lactation, breastfeeding should be discontinued. Application for violations of liver function In schizophrenia with concomitant liver diseases, an initial dose of 500 mcg 2 times / day is recommended. If necessary, the dose can be increased to 1-2 mg 2 times / day. Application for violations of kidney function In schizophrenia with concomitant kidney diseases, an initial dose of 500 mcg 2 times / day is recommended. If necessary, the dose can be increased to 1-2 mg 2 times / day. Use in children There are no data on the safety of risperidone in children under 15 years of age. Use in elderly patients In schizophrenia for elderly patients, an initial dose of 500 mcg 2 times / day is recommended. At

Risperidone dosage

• 2 mg 4 mg

Risperidone side effects

• Side effects of the drug Risperidone in therapeutic doses are given with distribution by frequency and system organ classes. The frequency of side effects was classified as follows: very common (?1/10 cases), frequent (?1/100 and

  drug interaction

  Given that risperidone primarily affects the central nervous system, it should be used with caution with alcohol, opiates, antihistamines and benzodiazepines due to an increased risk of sedation. Risperidone reduces the effectiveness of levodopa and other dopamine receptor agonists. However, if concomitant use is necessary, especially in end-stage Parkinson's disease, the minimum effective dose of each treatment should be prescribed. Caution should be exercised when Risperidone is co-administered with drugs that prolong the QT interval, e.g. class Ia antiarrhythmics (e.g. quinidine, disopyramide, procainamide), class III antiarrhythmics (e.g. amiodarone, sotalol), tricyclic antidepressants (amitriptyline), tetracyclic antidepressants (maprotiline), some antihistamines, other antipsychotics, some antimalarial drugs (quinine and mefloquine), and some drugs that cause electrolyte disturbances (hypokalemia, hypomagnesemia), bradycardia, or suppress the hepatic metabolism of risperidone. Clozapine reduces the clearance of risperidone. When using carbamazepine, there was a decrease in the concentration of the active antipsychotic fraction of risperidone in plasma. Similar effects can be observed with the use of other inducers of the CYP3A4 isoenzyme and P-glycoprotein. When prescribing and after discontinuation of carbamazepine or other inducers of the CYP3A4 / P-glycoprotein isoenzyme, the dose of Risperidone should be adjusted. Fluoxetine and paroxetine, inhibitors of the CYP2D6 isoenzyme, increase the plasma concentration of risperidone, but to a lesser extent the concentration of the active antipsychotic fraction. When prescribing and after discontinuation of fluoxetine or paroxetine, the dose of risperidone should be adjusted. Other inhibitors of the CYP2D6 isoenzyme, such as quinidine, can change the plasma concentration of risperidone in the same way. Verapamil, an inhibitor of the CYP3A4 isoenzyme and P-glycoprotein, increases the plasma concentration of risperidone. Topiramate moderately reduces the bioavailability of risperidone, but not the active antipsychotic fraction. This interaction is not considered clinically significant. Phenothiazine derivatives, tricyclic antidepressants and some ?-blockers can increase plasma concentrations of risperidone, but this does not affect the concentration of the active antipsychotic fraction. Amitriptyline does not affect the pharmacokinetics of risperidone and the active antipsychotic fraction. Cimetidine and ranitidine increase the bioavailability of risperidone, but minimally affect the concentration of the active antipsychotic fraction. Erythromycin, an inhibitor of the CYP3A4 isoenzyme, does not affect the pharmacokinetics of risperidone and the active antipsychotic fraction. Cholinesterase inhibitors (galantamine and donepezil) do not have a clinically significant effect on the pharmacokinetics of risperidone and the active antipsychotic fraction. When using the drug Risperidone together with other drugs that are highly bound to plasma proteins, there is no clinically significant displacement of any drug from the plasma protein fraction. Antihypertensive drugs increase the degree of blood pressure reduction against the background of risperidone. Risperidone has no clinically significant effect on the pharmacokinetics of lithium, valproic acid, digoxin, or topiramate. Eating does not affect the absorption of risperidone.

  Overdose

  Symptoms: drowsiness, sedation, tachycardia, decreased blood pressure, extrapyramidal symptoms. QT interval prolongation and convulsions have been observed. Bidirectional ventricular tachycardia has been reported with co-administration of elevated doses of risperidone and paroxetine. In case of overdose, the possibility of overdose from taking multiple drugs should be considered. Treatment. An open airway should be achieved and maintained to ensure adequate oxygen supply and ventilation, gastric lavage should be done (after intubation if the patient is unconscious) and activated charcoal should be given along with a laxative. ECG monitoring should be started immediately to detect possible arrhythmias. There is no specific antidote; appropriate symptomatic therapy should be carried out. Decreased blood pressure and collapse should be treated with intravenous fluid infusions and/or sympathomimetic drugs. In the event of the development of acute extrapyramidal symptoms,

  Storage conditions

  • store in a dry place
  • store at room temperature 15-25 degrees
  • keep away from children
  • store in a place protected from light
  Information provided

The atypical drug Risperidone (from Latin risperidonum) is an antipsychotic drug, i.e., intended for the treatment of psychotic disorders. This group of medicines is also called neuroleptics. The mechanism of action of such drugs is aimed at stopping the symptoms of psychosis. Risperidone has been widely used among patients with dementia and excessive aggression, delusional syndrome and schizophrenia.

The neuroleptic is prescribed for adults, the elderly and children from the age of 15.

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Release form and composition of Risperidone

The manufacturer of the drug in Russia is Canonpharma Production. The antipsychotic is available in tablet form of 1, 2, 3 and 4 mg. All of them differ in color and shape:

• magnesium stearate;
• lactose;
• silicon dioxide colloidal;
• microcrystalline cellulose;
• sodium lauryl sulfate;
• corn starch;
• sodium croscarmellose.



Indications

A 2006 U.S. study of children and adolescents showed that the neuroleptic is effective in relieving irritability associated with autism and can be used as a symptomatic treatment. Risperidone is prescribed for patients with acute psychosis, new onset, sudden onset of schizophrenia, or a chronic type of schizophrenia.

Other indications for the use of neuroleptics:

• mania associated with bipolar disorders (the drug acts as an auxiliary and is a mood stabilizer);
• depression, anxiety, guilt in patients with schizophrenia;
• behavioral disorders in patients with dementia (physical abuse, aggressiveness, outbursts of anger);
• mental disorders (excessive arousal, delirium);
• prevention of recurrence of chronic schizophrenia.

An antipsychotic drug is suitable for the treatment of psychotic conditions with overt productive or negative symptoms. The first ones include:

• suspicion;
• hallucinations;
• hostility;
• thought disorders.

Among the negative symptoms are:

• paucity of speech;
• blunted affect;
• social detachment;
• emotional closeness.



Dosages and method of application

Risperidone is a drug with many side effects, so the doses indicated in the instructions for use must be strictly observed. In elderly patients, the amount of the drug is halved. Tablets are taken by children over 15 years of age and adults twice a day according to the following scheme: they start taking 2 mg with the transition to 6 mg.

Elderly people are shown 0.5 mg 2 times a day. In the case of mania with bipolar disorders, the dose is 2 mg per day, gradually increasing by 2 mg every other day. The maximum amount is 4-6 mg per day.

Patients with dementia accompanied by behavioral disorders are prescribed 0.25 mg twice with an increase of 0.25 mg every other day to 0.5-2 mg per day. If the weight of patients is not more than 50 kg, then the dosage is 0.25 mg once a day, rising to 0.5 mg.



Side effects

After taking Risperidone, skin problems such as dryness, hyperpigmentation, itching, rash, angioedema may occur. Elderly patients had a stroke, hypotension. As side effects, rhinitis, urinary incontinence, uncontrolled erection, and ejaculation disorders occur. In women, failures of the menstrual cycle begin.

Other side effects include:

• obesity;
• galactorrhea;
• increased blood sugar levels;
• hypersalivation (salivation);
• nausea;
• constipation;
• loss of appetite;
• abdominal pain;
• dryness of the oral mucosa.

On the part of the psyche, the following disorders are noted:

• anxiety;
• drowsiness;
• insomnia;
• fatigue;
• acute dystonia;
• tremor;
• decrease in concentration.

Patients with schizophrenia are more likely to experience consequences in the form of epileptic seizures, involuntary movements of the tongue, muscle rigidity, impaired thermoregulation and hyperthermia.

Overdose

If the amount of the drug is exceeded, an overdose occurs, which is manifested by extrapyramidal disorders, palpitations, hypotension, excessive drowsiness and sedation. Treatment involves washing the stomach, taking laxatives and sorbents.

If the patient is unconscious, then intubation is indicated. The patient needs to do an ECG, as arrhythmias are possible. Taking anticholinergic drugs is indicated in the event of acute extrapyramidal disorders.

Contraindications

Do not use the medicine if hypersensitivity to the active or auxiliary component of Risperidone is observed. Antipsychotics should be used with caution in the presence of diseases of the heart muscle and vascular system: cardiac conduction disorders, chronic heart failure, a history of myocardial infarction.

It is forbidden to use the drug without prior consultation with a doctor for a brain tumor, Reye's syndrome (acute liver failure), intestinal obstruction, drug overdose. Risperidone has an antiemetic effect and may mask the symptoms of the above conditions, making it difficult to diagnose each of them.

With caution, the drug is prescribed in the following situations:

• hypovolemia (reduction in the volume of circulating blood);
• dehydration;
• conditions that increase the risk of developing tachycardia, the type of "pirouette" (when the pulse rate is increased and reaches 150-250 beats per minute); this is facilitated by taking drugs that lengthen the QT interval, bradycardia, electrolyte imbalance;
• Parkinson's disease;
• drug dependence or drug abuse;
• cerebrovascular accident;
• epilepsy in the history of the disease;
• history of seizures;
• severe liver and kidney failure.

Use in pediatrics and during pregnancy

The antipsychotic should not be taken by children under 18 years of age due to the fact that there is no data on the safety of the effect of drug components on the body at this age. Use in pregnant women is justified if the intended benefit to the mother is greater than the potential risk to the fetus. There are no official data on the safety of taking Risperidone. During the experiments, no toxic effects on reproductive function were revealed, however, it was noticed that the drug affects prolactin and the central nervous system. Risperidone is not teratogenic (does not interfere with proper embryonic development).

If a woman takes antipsychotics in the third trimester, then the newborn may experience withdrawal syndrome or extrapyramidal disorders (motor disorders):

• agitation;
• violation of feeding;
• hypertension;
• respiratory disorders;
• drowsiness;
• hypotension;
• tremor.

Before use, you should consult your doctor. If you need to take the medicine during lactation, then breastfeeding should be stopped.

Interaction with other drugs

The active component of Risperidone reduces the effect of Dopamine antagonists (Levodopa). The amount of drug in the blood is increased by phenothiazines and tricyclic antidepressants. The content of the antipsychotic fraction of the drug reduces Carbamazepine - a remedy for epileptics.

The plasma concentration of risperidone is increased by the antidepressant fluoxetine. Antihypertensive drugs enhance their effect when taken simultaneously with this antipsychotic. Depression of the central nervous system is caused by drugs that act on it, and ethanol.

Release from pharmacies and storage conditions

The drug is sold by prescription. In a carton box there are 2-5 blisters, each of which contains 10 tablets. The cost of the drug is about 170 rubles.