Rispolept - instructions for use, ratings, analogs and release forms (tablets 1 mg, 2 mg, 3 mg and 4 mg, Kviklet, drops or solution injections in ampoules for injection Konst suspension) drug for treating schizophrenia in adults, children and of pregnancy

In this article, you can read the instructions for using the drug Rispolept. It is comments of visitors - users of the drug, as well as opinions of doctors skilled in the use Rispolept in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Rispolept analogues in the presence of existing structural analogues.Use for the treatment of schizophrenia, Alzheimer's disease in adults, children, as well as during pregnancy and lactation.

Rispolept - antipsychotic drug (antipsychotic).

Risperidone is a selective monoaminergic antagonist with a high affinity for serotonin 5-HT2 and dopamine D2 receptors. It also binds to alpha1-adrenergic receptors and somewhat weaker - to histamine H1 receptors and alpha2-adrenoreceptors. Has no tropism for cholinergic receptors.

Risperidone reduces productive symptomatology of schizophrenia, causes less inhibition of motor activity and to a lesser degree induces catalepsy than classical antipsychotics. A balanced central antagonism to serotonin and dopamine probably reduces the propensity to extrapyramidal side effects and expands the therapeutic effect of the drug on the negative and affective symptoms of schizophrenia.

Composition

Risperidone + excipients.

Pharmacokinetics

After ingestion, Risperidone is completely absorbed from the digestive tract. The relative bioavailability after oral administration of risperidone in the form of tablets is 94% when compared with risperidone in formsolution. Food does not affect the absorption of the drug, so Rispolept can be administered regardless of food intake.

Risperidone is rapidly distributed in the body. In plasma, risperidone binds to albumin and alpha1-glycoprotein. Risperidone binds 90% to plasma proteins, 9-hydroxyrisperidone - by 77%. The concentration of risperidone in plasma is directly proportional to the dose taken in the therapeutic dose range.

Risperidone is metabolized with the participation of the isoenzyme CYP2D6 to form 9-hydroxyrisperidone, which has a pharmacological action similar to risperidone. Risperidone and 9-hydroxyrisperidone constitute the active antipsychotic fraction. The CYP2D6 isozyme is susceptible to genetic polymorphism. In patients with intensive metabolism by the CYP2D6 isoenzyme, risperidone is rapidly converted to 9-hydroxyrisperidone, while in patients with weak metabolism this transformation occurs much more slowly. Although patients with intensive metabolism have a lower concentration of risperidone and a higher concentration of 9-hydroxyrisperidone than patients with poor metabolism,the total pharmacokinetics of risperidone and 9-hydroxyrisperidone (active antipsychotic fraction) after taking one or more doses is similar in patients with intensive and weak metabolism of CYP2D6.

Another way of metabolizing risperidone is N-dealkylation. Studies on human liver microsomes show that risperidone at clinically significant concentrations does not, in general, inhibit the metabolism of drugs that undergo biotransformation with P450 isoenzymes, including CYP1A2, CYP2A6, CYP2C8 / 9/10, CYP2D6, CYP2E1, CYP3A4 and CYP3A5.

A week after the start of the drug, 70% of the dose is excreted in the urine, 14% - with feces. In the urine risperidone together with 9-hydroxyrisperidone constitute 35-45% of the dose. The rest is made up of inactive metabolites.

Pharmacokinetics in special clinical cases

After a single dose of risperidone in elderly patients, the concentration of the active antipsychotic fraction in plasma was 43% higher on average, T1 / 2 lasted 38% longer, and the clearance decreased by 30%.

The pharmacokinetics of risperidone, 9-hydroxyrisperidone and the active antipsychotic fraction in children are comparable to that of adult patients.

Indications

• treatment of schizophrenia in adults and children from 13 years;
• treatment of manic episodes associated with bipolar disorder, moderate to severe in adults and children 10 years of age;
• short-term (up to 6 weeks) treatment of persistent aggression in patients with dementia due to Alzheimer's disease, medium and severe, not amenable to non-pharmacological correction methods, and when there is a risk of harm to the patient or others;
• short-term (up to 6 weeks) symptomatic treatment of incessant aggression in the structure of behavioral disorder in children from 5 years 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 wider treatment program, incl. psychological and educational activities. Risperidone should be prescribed by a specialist in the field of pediatric neurology and child psychiatry or a physician familiar with the treatment of behavioral disorders in children and adolescents.

Forms of release

Tablets coated with 1 mg, 2 mg, 3 mg and 4 mg.

Tablets for resorption of 1 mg and 2 mg (Rispolept Quiklet).

Solution for ingestion 1 mg (sometimes mistakenly called drops).

Powder for the preparation of suspension for intramuscular administration of prolonged action 25 mg, 37.5 mg and 50 mg (injections in injections) (Rispoleptus Konsta).

Instructions for use and dosage

Pills

The drug is taken orally. Eating does not affect the absorption of the drug.

When prescribing the drug in doses less than 1 mg, it is recommended to use Rispolept, a solution for oral administration.

Schizophrenia

Adults Rispolept can be prescribed 1 or 2 times a day. The initial dose of Rispolept is 2 mg per day. On the second day, the dose should be increased to 4 mg per day. From this moment the dose can either be kept at the same level, or individually adjusted if necessary. Usually the optimal dose is 4-6 mg per day. In some cases, a slower dose increase and lower initial and maintenance doses may be justified.

Doses above 10 mg per day did not show a higher efficacy compared with smaller doses and may cause extrapyramidal symptoms. Due to the fact that safety of doses above 16 mg per day has not been studied, doses above this level can not be used.

Patients who have sustained drowsiness, it is recommended to take half the daily dose 2 times a day.

For elderly patients, the drug is prescribed in an initial dose of 0.5 mg 2 times a day. The dose can be individually increased by 0.5 mg 2 times a day to 1-2 mg 2 times a day.

Children from 13 years of age are recommended to take an initial dose of 0.5 mg once a day in the morning or evening. If necessary, the dose can be increased at least after 24 hours at 0.5-1 mg per day to a recommended dose of 3 mg per day with good tolerability. Despite the efficacy shown in the treatment of schizophrenia in adolescents with a drug in doses of 1-6 mg per day, no additional efficacy was observed when the drug was used at doses above 3 mg / day, and higher doses caused more side effects. The use of the drug in doses above 6 mg per day has not been studied.

Manic episodes associated with bipolar disorder

The recommended initial dose of the drug for adults is 2 mg per day at one time. If necessary, this dose can be increased at least 24 hours per 1 mg per day. For most patients, the optimal dose is 1-6 mg per day. The use of the drug in doses above 6 mg per day in patients with manic episodes has not been studied.

As for any other symptomatic therapy, the appropriateness of continuing treatment with Rispolept should be regularly evaluated and confirmed.

Patients who have sustained drowsiness, it is recommended to take half the daily dose 2 times a day.

For elderly patients, the initial dose is 0.5 mg twice a day. The dose can be individually increased by 0.5 mg twice a day to 1-2 mg twice a day. Care should be taken in connection with the limited experience of the drug in elderly patients.

Children from 10 years of age are recommended to take an initial dose of 0.5 mg once a day in the morning or evening. If necessary, the dose can be increased at least after 24 hours at 0.5-1 mg per day to a recommended dose of 1-2.5 mg per day with good tolerability. Despite the efficacy shown in the treatment of manic episodes associated with bipolar disorder in children, the drug at doses of 0.5-6 mg per day showed no additional efficacy when administered at doses above 2.5 mg / day, and higher doses caused more side effects. The use of the drug in doses above 6 mg per day has not been studied.

Continuous aggression in patients with dementia due to Alzheimer's disease

The initial dose of 0.25 mg 2 times a day is recommended. If necessary, the dose can be individually increased by 0.25 mg 2 times a day, not more often than every other day. For most patients, the optimal dose is 0.5 mg 2 times a day. However, some patients receive 1 mg twice daily.

Rispolept should not be used for more than 6 weeks in patients with persistent aggression in patients with dementia due to Alzheimer's disease. During treatment, the condition of patients should be evaluated on a regular basis, as well as the need to continue therapy.

Continuous aggression in the structure of conduct disorder

Children from 5 to 18 years (with a body weight of 50 kg or more) are recommended an initial dose of 0.5 mg once a day. If necessary, this dose can be increased by 0.5 mg per day, not more often than every other day. For most patients, the optimal dose is 1 mg per day. However, for some patients it is preferable to take 0.5 mg per day, while some require an increase in the dose to 1.5 mg per day.

Children from 5 to 18 years (with a body weight of less than 50 kg) are recommended an initial dose of 0.25 mg once a day.If necessary, this dose can be increased by 0.25 mg per day, not more often than every other day. For most patients, the optimal dose is 0.5 mg per day. However, for some patients it is preferable to take 0.25 mg per day, while some require an increase in the dose to 0.75 mg per day.

As for any other symptomatic therapy, the appropriateness of continuing treatment with Rispolept should be regularly evaluated and confirmed.

Use in children under 5 years of age is not recommended due to lack of data.

Special patient groups

In patients with impaired renal function, the ability to excrete an active antipsychotic fraction is reduced compared to other patients.

In patients with impaired liver function, an elevated concentration of free fraction of risperidone in the blood plasma is observed.

The initial and maintenance dose in accordance with the indications should be reduced 2 times, increasing the dose in patients with liver and kidney disease should be slower. Rispolept should be administered with caution in this category of patients.

Abolition of the drug

Stopping the drug is recommended to be carried out gradually.Acute withdrawal symptoms, including nausea, vomiting, sweating and insomnia, were very rare after a sharp discontinuation of antipsychotics in high doses.

Transition from therapy with other antipsychotic drugs

At the beginning of treatment with Rispolept, it is recommended to gradually abolish previous therapy, if it is clinically justified. In this case, if patients are transferred from the therapy of depot forms of antipsychotics, then Rispolept therapy should be started instead of the next scheduled injection. Periodically, the need to continue the current therapy with antiparkinsonian drugs should be evaluated.

Quiquette Absorption Tablets

Individual. When administered orally, the initial dose for adults is 0.25-2 mg per day, on the second day - 4 mg per day. Then the dose can either be kept at the same level, or, if necessary, corrected. Usually the optimal therapeutic dose, depending on the indications, is in the range of 0.5-6 mg per day. In some cases, a slower dose increase and lower initial and maintenance doses may be justified.

In schizophrenia for elderly patients, as well as with concomitant diseases of the liver and kidneys, an initial dose of 500 micrograms 2 times a day is recommended. If necessary, the dose can be increased to 1-2 mg 2 times a day.

Maximum dose: at application in a dose of risperidone 10 mg per day is not observed increase efficiency compared with lower doses, but increases the risk for extrapyramidal symptoms. The safety of the use of risperidone in doses exceeding 16 mg per day has not been studied, therefore further excess of the dose is not allowed.

Solution or drops for oral administration

Schizophrenia

Adults

Rispolept can be given once or twice a day.

The initial dose of Rispolept is 2 mg per day. On the second day, the dose can be increased to 4 mg per day. From this moment the dose can either be kept at the same level, or individually adjusted if necessary. Usually the optimal dose is 4-6 mg per day. In some cases, a slower dose increase and a lower initial and maintenance dose may be justified.

Doses above 10 mg per day did not show a higher efficacy compared with smaller doses and may cause extrapyramidal symptoms.Due to the fact that safety of doses above 16 mg per day has not been studied, doses above this level should not be used.

Elderly patients

Recommended initial dose of 0.5 mg per reception twice a day. Dosage can individually increase by 0.5 mg twice a day to 1-2 mg twice a day.

Children from 13 years old

Recommended initial dose of 0.5 mg per reception once a day in the morning or evening. If necessary, the dosage can be increased at least after 24 hours at 0.5-1 mg per day to a recommended dose of 3 mg per day with good tolerability. Despite the efficacy shown in the treatment of schizophrenia in adolescents at doses of 1-6 mg per day, no additional efficacy was observed at doses above 3 mg per day, and higher doses caused more side effects. The use of doses above 6 mg per day has not been studied.

Patients who have sustained drowsiness, it is recommended to take half the daily dose 2 times a day.

Manic episodes associated with bipolar disorder

Adults

The recommended initial dose of the drug is 2 mg per day at a time. If necessary, this dose can be increased at least 24 hours per 1 mg per day. For most patients, the optimal dose is 1-6 mg per day.The use of doses above 6 mg per day in patients with manic episodes has not been studied.

As for any other symptomatic therapy, the appropriateness of continuing treatment with Rispolept should be regularly evaluated and confirmed.

Elderly patients

Recommended initial dose of 0.5 mg per reception twice a day. Dosage can individually increase by 0.5 mg twice a day to 1-2 mg twice a day. Care should be taken in connection with the limited experience of the drug in elderly patients.

Children from 10 years

Recommended initial dose of 0.5 mg per reception once a day in the morning or evening. If necessary, the dosage can be increased at least in 24 hours by 0.5-1 mg per day to a recommended dose of 1-2.5 mg per day with good tolerability. Despite the efficacy shown in the treatment of manic episodes associated with bipolar disorder in children with doses of 0.5-6 mg per day, no additional efficacy was observed at doses above 2.5 mg / day, and higher doses caused more side effects. The use of doses above 6 mg per day has not been studied.

Patients who have sustained drowsiness, it is recommended to take half the daily dose 2 times a day.

Continuous aggression in patients with dementia due to Alzheimer's disease

Recommended initial dose of 0.25 mg per reception twice a day. Dosage, if necessary, can individually increase by 0.25 mg 2 times a day, not more often than every other day. For most patients, the optimal dose is 0.5 mg twice daily. However, some patients receive 1 mg 2 times a day.

Rispolept should not be used for more than 6 weeks in patients with persistent aggression in patients with dementia due to Alzheimer's disease. During treatment, the condition of patients should be assessed on a regular basis, as well as the need to continue therapy.

Continuous aggression in the structure of conduct disorder

Children from 5 to 18 years old

Patients with a body weight of 50 kg or more - the recommended initial dose of the drug - 0.5 mg once a day. If necessary, this dose can be increased by 0.5 mg per day, not more often than every other day. For most patients, the optimal dose is a dose of 1 mg per day. However, for some patients it is preferable to take 0.5 mg per day, while some require an increase in the dose to 1.5 mg per day.

Patients weighing less than 50 kg - the recommended initial dose of the drug - 0.25 mg once a day.If necessary, this dose can be increased by 0.25 mg per day, not more often than every other day. For most patients, the optimal dose is a dose of 0.5 mg per day. However, for some patients it is preferable to take 0.25 mg per day, while some require an increase in the dose to 0.75 mg per day.

As for any other symptomatic therapy, the appropriateness of continuing treatment with Rispolept should be regularly evaluated and confirmed.

Use in children under 5 years is not recommended due to lack of data.

Diseases of the liver and kidneys

In patients with kidney disease, the ability to excrete the active antipsychotic fraction is reduced compared to other patients. In patients with liver disease, there is an increased concentration of free fraction of risperidone in the blood plasma.

The initial and maintenance dose in accordance with the indications should be reduced 2 times, increasing the dose in patients with liver and kidney disease should be slower.

Rispolept should be administered with caution in this category of patients.

Mode of application

Inside. Eating does not affect the absorption of the drug.

Termination of the drug is recommended to be carried out gradually. Acute withdrawal symptoms, including nausea, vomiting, sweating and insomnia, were very rare after abrupt discontinuation of high doses of antipsychotics.

Transition from therapy with other antipsychotic drugs

At the beginning of treatment with Rispolept, it is recommended to gradually abolish previous therapy, if it is clinically justified. In this case, if patients are transferred from the therapy of depot forms of antipsychotics, then Rispolept therapy should be started instead of the next scheduled injection. Periodically, the need to continue the current therapy with antiparkinsonian drugs should be evaluated.

Injections in ampoules for injection of Konsta

Ryspolept Konsta is injected 1 time in 2 weeks deeply intramuscularly, using a sterile needle attached to the syringe. Injections should be done alternately in the right and left buttocks. The drug can not be administered iv.

For adults, the recommended dose is 25 mg IM once every 2 weeks. Some patients require higher doses - 37.5 mg or 50 mg.In clinical studies, there was no increase in efficacy with 75 mg. The maximum dose should not exceed 50 mg once every 2 weeks.

Within 3 weeks after the first administration of the preparation, the patient should take an effective antipsychotic.

The dose of the drug can be increased no more than once in 4 weeks. The effect of such a dose increase should be expected not earlier than 3 weeks after the first injection of the increased dose.

For elderly patients, the recommended dose is 25 mg IM once every 2 weeks. Within 3 weeks after the first administration of the preparation, the patient should take an effective antipsychotic.

At present, there is no data on the use of Rispolept Konsta in patients with impaired hepatic or renal function. If it is still necessary to use Rispolept Consta in this category of patients, then in the first week it is recommended to take risperidone inside at a dose of 500 mcg 2 times a day in the form of tablets or a solution for ingestion. During the second week the patient can take 1 mg 2 times a day or 2 mg 1 time per day.If the patient tolerates an oral dose of at least 2 mg, then he can inject Rispolept Konsta IM in a dose of 25 mg once every 2 weeks.

Rules for the preparation of solution

The use of the preparation Rispolept of Consta requires strict adherence to the instructions for the preparation of the suspension in order to ensure the precise administration of the preparation and avoid possible errors.

To prepare a suspension from the Ripolept Constant micro-granules in the vial of the prolonged action, only the solvent in the pre-filled syringe can be used. Ready suspension is injected in / m only in the gluteal region. Do not replace the components in the packaging with any other products. To ensure the use of a full dose of risperidone, the entire contents of the vial should be administered. The introduction of part of the contents of the vial can not ensure that the patient receives the correct dose of the drug. The drug should be administered immediately after the preparation of the suspension.

Pack a preparation of Rispolept's preparation Konsta from the refrigerator and allow it to warm up for 30 minutes to room temperature before preparing the suspension.

1. Remove the colored plastic cover from the bottle.Do not remove the gray rubber stopper. Wipe unopened vial with alcohol wipe and allow to dry.

2. Unfold the blister pack and remove the Alaris Smart Site without the needles, holding it between the white luer cap and the "skirt". Never touch the sharp tip of the device.

3. It is very important that the SmartSite needleless device is correctly installed on the vial, otherwise the solvent may leak when it enters the vial.

Place the vial on a hard surface.

Hold the bottom of the vial. Point the needleless SmartSite device onto the bottle vertically so that the sharp tip is located in the center of the vial of the vial.

Pushing down from the top, push the sharp tip of the needleless device SmartSite through the center of the rubber bottle stopper until the device is securely attached to the top of the bottle.

4. Before attaching the syringe to the needleless device SmartSite, holding the base of the bottle, wipe the place of attachment of the device with a syringe (blue circle) with an alcoholic cloth and allow to dry.

5. The pre-filled syringe has a white tip consisting of two parts: a white collar and a glossy white cap.In order to open the syringe, hold the syringe by the white collar and break off the glossy white cap (the white cap can not be unscrewed or cut off). Remove the white cap with the rubber tip inside.

At all stages of assembly, the syringe should only be held by the white collar located on the tip of the syringe. Fixing the white collar will help to protect the collar from separation and ensures a good connection with the syringe. Do not twist the components during assembly, because while parts of the syringe can come off of it.

6. While holding the syringe by the white collar, insert the syringe into the blue circle of the needleless device, press and turn clockwise to ensure that the syringe is firmly connected to the needleless device (avoid twisting). To prevent rotation of the needleless device during the connection with the syringe, you must firmly hold the "skirt". The syringe and the needleless device must be on the same line.

7. Insert the contents of the syringe with the solvent into the vial.

8. While holding the piston of the syringe with your thumb, shake the contents of the vial vigorously for at least 10 seconds until a homogeneous suspension forms.After proper mixing, the suspension becomes homogeneous, thick, milky in color. The microgranules can be seen in the liquid, but should not remain dry by the solvent of the dry microgranules.

Do not store the vial after the suspension has been prepared, since the suspension may be exfoliated.

9. Turn the bottle upside down and slowly draw all the contents of the vial into the syringe. Separate part of the label from the vial along the perforation line and glue it to the syringe (for identification).

10. Holding the syringe by the white collar, disconnect the syringe from the needleless device. Dispose of the bottle and needleless device in accordance with local regulations for the destruction of this kind of waste.

11. Open the blister pack of Needle-Pro needle. Do not touch the part of the needle that joins the syringe. Remove the needle from the package, holding it by the transparent case.

12. To prevent germs from entering, do not touch the luer tip of the orange needle safety device Needle-Pro. Holding the syringe by the white collar, attach the Luer cannula of the orange Needle-Pro needle safety device to the syringe by slightly turning it clockwise.

13.Continuing to hold the syringe by the white collar, clamp the transparent case of the needle and tighten the needle firmly in the Needle-Pro protective device by pressing and turning it clockwise. Securing the needle can guarantee a secure connection between the needle and the Needle-Pro needle guard during the following steps.

14. Immediately prior to the administration, the preparation Rispolept Consta should be resuspended, since after the preparation of the suspension in the vial, some of the microgranules may settle. To resuspend the microgranules, vigorously shake the syringe.

15. Holding the syringe by the white collar, remove the transparent case from the needle. Do not bend the case; the connection of the luer tip can be violated.

16. Lightly tap with your finger on the syringe so that the air bubbles in it go up. Slightly pushing the piston upward, remove air bubbles from the syringe and needle, holding the syringe so that the needle is directed vertically upwards. Enter the entire contents of the syringe into the upper outer quadrant of the gluteal region. Suspension can not be administered intravenously!

Warning! To avoid injury to medical personnel using a needle:

• Do not touch the needle protection device Needle-Pro while pressing it against a flat surface;
• Do not disassemble needle protection device Needle-Pro;
• Do not attempt to straighten the needle and do not touch the needle protection device Needle-Pro if the needle is bent or damaged;
• Needle-Pro needles should only be used as intended, otherwise the needle may protrude from the protective cap.

17. After the injection is complete, insert the needle into the orange Needle-Pro needle guard with one hand. To do this, carefully press the orange needle protection device Needle-Pro against a flat surface. Once the orange Needle-Pro needle protection device is pressed, the needle must fit tightly into the needle protection device Needle-Pro. Before you eject the needle, make sure that the needle is firmly attached to the orange needle protection device Needle-Pro. Disposal is carried out in accordance with local regulations for the destruction of such waste.

Do not reuse: this device is intended for single use only. Any attempt at subsequent reuse may adversely affect the integrity of the device itself or lead to a deterioration in its performance.

Side effect

• upper respiratory tract infection;
• nasopharyngitis;
• influenza-like infections;
• bronchitis;
• urinary tract infections;
• rhinitis;
• ear infections;
• pneumonia;
• pharyngitis;
• sinusitis;
• viral infections;
• localized infections;
• cystitis;
• gastroenteritis;
• subcutaneous abscess;
• neutropenia, anemia, agranulocytosis, thrombocytopenia;
• hypersensitivity;
• Quincke's edema (including perioral edema, edema of the eyelids, edema of the face, hereditary edema of the Quincke, edema of the larynx and pharynx, oculo-respiratory syndrome, edema of the mouth, periglacial edema, edema of the small intestine, edema of the tongue);
• anaphylactic shock;
• hyperprolactinemia;
• increased appetite;
• decreased appetite;
• anorexia;
• diabetes;
• water intoxication;
• headache;
• Parkinsonism (including extrapyramidal disorders, muscle rigidity, hypokinesia, rigidity as a "cogwheel", bradykinesia, muscle cramps);
• dizziness;
• tremor;
• drowsiness;
• sedative effect;
• fainting;
• violation of attention;
• lack of coordination;
• dystonia;
• salivation;
• postural dizziness;
• convulsions;
• insomnia;
• anxiety;
• excitation;
• depression;
• sleep disturbance;
• violation of falling asleep;
• decreased libido;
• nervousness;
• blurred vision;
• conjunctivitis;
• decreased visual acuity;
• earache;
• vertigo;
• occlusion of the retinal artery (observed with an intracardiac defect predisposing to the shunt from right to left, for example, an "oval window");
• arterial hypertension;
• disturbance of balance;
• lack of response to stimuli;
• decreased consciousness;
• Parkinsonian tremor;
• transient ischemic attack;
• myocardial infarction;
• stroke;
• speech impairment;
• loss of consciousness;
• involuntary muscle contractions;
• diabetic coma;
• rhythmic nodding;
• atrial fibrillation;
• cough;
• nasal congestion;
• nasal congestion;
• pain in the pharynx and in the larynx;
• dyspnea;
• sleep apnea syndrome;
• constipation, diarrhea;
• dry mouth;
• dyspepsia;
• nausea, vomiting;
• hypersecretion of saliva;
• pain in the abdomen (including in the upper abdomen);
• discomfort in the stomach;
• gastritis;
• pancreatitis;
• jaundice;
• acne;
• dry skin;
• rashes;
• eczema;
• itching (including generalized);
• alopecia;
• pain in the limbs;
• arthralgia;
• back pain;
• myalgia;
• muscle pain in the chest;
• pain in the buttocks;
• muscle weakness;
• pain in the neck;
• urinary incontinence;
• urinary retention;
• violation of menstruation;
• slow ejaculation;
• priapism;
• withdrawal syndrome in newborns;
• pain during injection;
• pain at the injection site, compaction, swelling and other reactions at the injection site;
• reactions at the site of injection, such as abscess, phlegmon, cyst, hematoma, necrosis, nodules, ulcer (these side effects were noted as serious, in some cases required surgical intervention).

Contraindications

• lactation period (breastfeeding);
• phenylketonuria;
• children and adolescents under the age of 18 (for injections);
• hypersensitivity to the components of the drug.

Application in pregnancy and lactation

There are no data on the safety of Rispolept's use in pregnant women.

In experimental animal studies, risperidone had no direct toxic effect on the reproductive system, but caused some indirect effects mediated through prolactin and the central nervous system. In none of the studies did risperidone have a teratogenic effect.

In the case of a woman taking antipsychotic medications (including Rispolept) in the third trimester of pregnancy, newborns are at risk of extrapyramidal disorders and / or withdrawal syndrome of varying severity.These symptoms may include agitation, hypertension, hypotension, tremor, drowsiness, respiratory disorders, and breast-feeding disorders.

Ryspolept can be used during pregnancy only if the expected benefit of therapy for the mother exceeds the potential risk to the fetus.

Contraindicated in the period of lactation (breastfeeding).

Use in children

Rispolept in the form of injections is contraindicated in children and adolescents under the age of 18 years.

It is possible to use other forms of the drug in children according to the dosage regimen.

Application in elderly patients

In schizophrenia, an initial dose of 500 micrograms 2 times a day is recommended for elderly patients. If necessary, the dose can be increased to 1-2 mg 2 times a day.

For elderly patients, the recommended dose is 25 mg IM once every 2 weeks. Within 3 weeks after the first administration of the preparation, Rispolept Konsta (ie prior to the onset of the drug), the patient should take an effective antipsychotic.

special instructions

Increased mortality in elderly patients with dementia

In elderly patients with dementia in the treatment of atypical antipsychoticmeans there is an increased mortality compared with placebo in studies of atypical antipsychotics, including risperidone. When using risperidone for a given population, the rate of death was 4.0% for patients taking risperidone, compared with 3.1% for placebo. The average age of the deceased patients is 86 years (range 67-100 years). The data collected from two extensive observational studies show that elderly patients with dementia who are treated with typical antipsychotics also have a slightly increased risk of death compared to patients who do not receive treatment. At the moment, there is insufficient data to accurately assess this risk. The cause of this risk increase is also unknown. Also, the extent to which an increase in mortality may not be applicable to antipsychotics, nor to the characteristics of this group of patients, has been determined.

Co-administration with furosemide

In elderly patients with dementia, an increased mortality was observed with simultaneous application of Furosemide and risperidone by oral route (7.3%, mean age 89 years,the range of 75-97 years) compared with the group taking only risperidone (3.1%, mean age 84 years, range 70-96 years) and the group taking only furosemide (4.1%, mean age 80 years, range 67-90 years) . Increased mortality of patients taking risperidone with furosemide was observed in 2 of 4 clinical trials. Joint use of risperidone with other diuretics (mainly with thiazide diuretics in small doses) was not accompanied by an increase in mortality.

There are no pathophysiological mechanisms that explain this observation. Nevertheless, special care should be taken when prescribing the drug in such cases. Before appointment, the risk / benefit ratio must be carefully assessed. There was no increase in mortality in patients taking other diuretics simultaneously with risperidone. Regardless of treatment, dehydration is a common risk factor for mortality and should be carefully monitored in elderly patients with dementia.

In elderly patients with dementia, there was an increase in side effects from the cerebrovascular system (acute and transient disorders of cerebral circulation), incl.deaths in patients (mean age 85 years, range 73-97 years) with risperidone compared with placebo.

Cardiovascular effects

In placebo-controlled clinical trials in patients with dementia, taking some atypical antipsychotics, an increased risk of cerebrovascular side effects was approximately 3-fold. Combined data from six placebo-controlled trials, mainly elderly patients with dementia (age greater than 65 years), demonstrated that cerebrovascular side effects (serious and non-serious) occurred in 3.3% (33/1009) of patients taking risperidone and in 1.2 % (8/712) of patients taking placebo. The risk ratio was 2.96 (1.34, 7.50) with a confidence interval of 95%. The mechanism of increasing the risk is unknown. Increased risk is not excluded for other antipsychotics, as well as for other patient populations. Rispolept should be used with caution in patients with risk factors for stroke.

The risk of cerebrovascular side effects is much higher in patients with mixed or vascular dementia, compared with patients with Alzheimer's dementia.Therefore, patients with dementia of any type other than Alzheimer's should not take risperidone.

Doctors should evaluate the risk / benefit ratio of using Rispolept in elderly patients with dementia, taking into account the precursors of stroke risk individually for each patient. Patients and caregivers should be warned that it is necessary to immediately report the signs and symptoms of cardiovascular events such as sudden weakness or immobility / insensitivity in the face, legs, hands, as well as speech difficulties and vision problems. All possible treatment options should be considered, including discontinuation of risperidone.

Rispolept can be used only for short-term treatment of persistent aggression in patients with dementia due to Alzheimer's disease, moderate and severe, as a supplement to non-pharmacological correction methods, in case of their inefficiency or limited effectiveness, and when there is a risk of harming the patient to himself or others persons.

It is necessary to constantly assess the condition of patients and the need to continue therapy with risperidone.

Orthostatic hypotension

Risperidone has alpha-blocking activity, and therefore can cause orthostatic hypotension in some patients, especially during the initial dose selection. Clinically significant hypotension was observed in the postmarketing period when combined with antihypertensive drugs. Rispolept should be used with caution in patients with known cardiovascular diseases (eg, heart failure, myocardial infarction, cardiac muscle conduction disorders, dehydration of hypovolemia or cerebrovascular disease). Corresponding dose adjustment is also necessary. It is recommended to evaluate the possibility of reducing the dose in the event of hypotension.

Late dyskinesia and extrapyramidal disorders

Drugs that have the properties of dopamine receptor antagonists can cause tardive dyskinesia, which is characterized by rhythmic involuntary movements, predominantly of the tongue and / or facial musculature.The occurrence of extrapyramidal symptoms is a risk factor for the development of tardive dyskinesia. If the patient has objective or subjective symptoms indicating tardive dyskinesia, consideration should be given to the desirability of abolishing all antipsychotics, including Rispolept.

Malignant neuroleptic syndrome (CNS)

Antipsychotic drugs, including risperidone, can cause malignant neuroleptic syndrome (CNS), which is characterized by hyperthermia, rigidity of muscles, instability of the autonomic nervous system function, depression of consciousness, and an increase in serum concentrations of CK. In patients with ZNS, myoglobinuria (rhabdomyolysis) and acute renal failure may also occur. If a patient develops objective or subjective symptoms of the NSA, all antipsychotics, including Rispolept, should be immediately discontinued.

Parkinson's disease and dementia with Levi bodies

The administration of antipsychotics, including Rispolept, to patients with Parkinson's disease or dementia with Levy bodies should be done with caution, sincein both groups of patients, the risk of neuroleptic malignant syndrome increased and sensitivity to antipsychotics increased (including blunting of pain sensitivity, confusion, postural instability with frequent falls and extrapyramidal symptoms). When taking risperidone, there may be a worsening of the course of Parkinson's disease.

Hyperglycemia and diabetes mellitus

When treating the drug Rispolept, hyperglycemia, diabetes mellitus and exacerbation of already existing diabetes mellitus were observed. It is likely that the previous increase in body weight is also predisposing to this factor. It is very rare to have ketoacidosis and rarely - a diabetic coma. All patients need to be clinically monitored for symptoms of hyperglycemia (such as polydipsia, polyuria, polyphagia, and weakness). Patients with diabetes should be monitored regularly for impaired glucose control.

Weight gain

When treated with Rispolept, a significant increase in body weight was observed. It is necessary to monitor the body weight of patients.

Hyperprolactinemia

Based on the results of studies on tissue cultures, it has been suggested that the growth of breast tumor cells can be stimulated by prolactin. Although clinical and epidemiological studies have not revealed a clear association between hyperprolactinaemia and antipsychotic medications, caution should be exercised in prescribing risperidone to patients with a history of history. The drug Rispolept should be used with caution in patients with existing hyperprolactinemia and in patients with possible prolactin-dependent tumors.

QT interval extension

The prolongation of the QT interval was very rare in the post-marketing period. As with other antipsychotics, caution should be exercised when prescribing Rispolept for patients with known cardiovascular disease, prolonged QT interval in a family history, bradycardia, electrolyte balance disorders (hypokalemia, hypomagnesemia), because this may increase the risk of arrhythmogenic effect; and when combined with drugs that extend the QT interval.

Convulsions

Rispolept should be used with caution in patients with a history of seizures or with other medical conditions in which the convulsive threshold may be reduced.

Priapism

Priapism may occur when taking risperidone due to alpha-adrenergic blocking effects.

Regulation of body temperature

Antipsychotic drugs attributed to such an undesirable effect as a violation of the ability of the body to regulate the temperature. Caution should be exercised when prescribing Rispolept to patients with conditions that may contribute to an increase in internal body temperature, such as intense physical activity, dehydration, exposure to high external temperatures, or simultaneous use of drugs with anticholinergic activity.

Venous thromboembolism

When using antipsychotic drugs, cases of venous thromboembolism were noted. Because patients who take antipsychotics often have a risk of developing venous thromboembolism, all possible risk factors should be identified before and during treatment with Rispolept, and precautionary measures should be taken.

Excipients

The drug Rispolept, tablets coated with a film coat, contains lactose. Patients with rare hereditary diseases associated with intolerance to galactose, deficiency of lactase lapp or glucose-galactose malabsorption should not be prescribed Rispolept preparation, film-coated tablets.

Tablets of 2 mg contain a dye sunset yellow sunset (E110), which can cause allergic reactions.

Use in Pediatrics

Before prescribing Rispolept, children or adolescents with mental retardation should carefully assess their condition for physical or social causes of aggressive behavior, such as pain or inadequate demands of the social environment.

The sedative effect of risperidone should be carefully monitored in this population because of the possible effect on learning ability. The change in the time of risperidone intake can improve the control of the effect of sedation on the attention of adolescents and children.

The use of risperidone was associated with an average increase in body weight and body mass index.Changes in growth during long-term studies were within the expected age norms. The long-term effect of risperidone on sexual development and growth has not been fully studied.

In connection with the possible impact of prolonged hyperprolactinemia on the growth and sexual development in children and adolescents, regular clinical evaluation of the hormonal status should be carried out, incl. measurement of height, weight, monitoring of sexual development, menstrual cycle and other possible prolactin-dependent effects.

During treatment with risperidone, regular monitoring of the presence of extrapyramidal symptoms and other movement disorders should be performed.

Impact on the ability to drive vehicles and manage mechanisms

Rispolepts may have a slight or moderate effect on the ability to drive vehicles and mechanisms. Patients should be advised not to drive the car and from working with the mechanisms to determine their individual sensitivity to the drug.

Drug Interactions

As in the case of other antipsychotic drugs,caution should be exercised when co-prescribing the drug Rispolept with drugs that increase the QT interval, for example, with antiarrhythmic drugs of class 1a (quinidine, disopyramide, procainamide, etc.), 3 classes (amiodarone, sotalol, etc.), tricyclic antidepressants (amitriptyline and others .), tetracyclic antidepressants (maprotiline, etc.), some antihistamines, other antipsychotics, some antimalarial drugs (quinine, mefloquine, etc.), drugs that cause electrolytes ny imbalance (hypokalemia, hypomagnesemia), bradycardia or inhibit hepatic metabolism of risperidone. This list is not exhaustive.

Influence of the drug Rispolept on other drugs

Rispolept should be used with caution in combination with other drugs and substances of central action, especially with ethanol, opiates, antihistamines and benzodiazepines because of the increased risk of sedation.

Rispolept may decrease the effectiveness of levodopa and other dopamine agonists. If this combination is necessary, especially in the terminal phase of Parkinson's disease, the lowest effective dose of each drug should be given.

When using risperidone together with antihypertensive drugs in the postmarketing period, clinically significant arterial hypotension was observed.

Risperidone does not have a clinically significant effect on the pharmacokinetics of lithium, valproate, digoxin, or topiramate.

The effect of other drugs on the drug Rispolept

When Carbamazepine was used, a decrease in the concentration of the active antipsychotic fraction of risperidone in plasma was noted. Similar effects can be observed with the use of other inducers of hepatic enzymes and P-glycoprotein (for example, rifampicin, phenytoin, phenobarbital). With the appointment and after withdrawal of carbamazepine or other inducers of hepatic enzymes and P-glycoprotein, the dose of Rispolept should be adjusted.

Fluoxetine and paroxetine, which are inhibitors of the CYP 2D6 isoenzyme, increase the concentration of risperidone in plasma, to a lesser extent, the concentration of the active antipsychotic fraction. It is assumed that other inhibitors of the CYP2D6 isoenzyme (eg, quinidine) affect the concentration of risperidone in the same way.When appointing and after the abolition of Fluoxetine or paroxetine, the dose of Rispolept should be adjusted.

Verapamil, an inhibitor of the isoenzyme CYP3A4 and P-glycoprotein, increases the concentration of risperidone in plasma.

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

Phenothiazines, tricyclic antidepressants, and some beta-blockers may 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 have a minimal effect on 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.

Joint use of psychostimulants (eg, methylphenidate) and the drug Rispolept in children does not change the pharmacokinetic parameters and the effectiveness of risperidone.

It is not recommended to use risperidone together with paliperidone because paliperidone is an active metabolite of risperidone, and the use of this combination may lead to an increase in the concentration of the active antipsychotic fraction.

Analogues of the drug Rispolept

Structural analogs for the active substance:

• Leptinorm;
• It is resilient;
• Ridonex;
• Rilept;
• Rileptid;
• Ridonal;
• Ryspaksol;
• Rispen;
• Risperidone;
• Rispeplet of Konsta;
• Rispolept Quicklet;
• Rispolux;
• Risset;
• Risseth Kwitab;
• Sizodon-san;
• Speridan;
• Torendo.

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