Risperon

General characteristics. Structure:

Active agent: рисперидон 2,0 mg,

Excipients: lactoses monohydrate, starch corn, cellulose microcrystallic, a gipromelloza, magnesium stearate, silicon dioxide colloid anhydrous, sodium lauryl sulfate, a covering for drawing a cover.

Pharmacological properties:

Pharmacodynamics. Risperidon is the selection antagonist 5-HT2-serotoninergicheskikh and D2-dofaminergichesky receptors in TsNS; it blocks also? 1-adrenergic, to a lesser extent — histamine N1-and? 1-adrenergic, without exerting impacts on cholinergic receptors. Though рисперидон is powerful D2 antagonist that is connected with its efficiency of rather productive symptomatology of schizophrenia, it does not cause considerable oppression of motor activity and, in comparison with classical neuroleptics, to a lesser extent induces a katalepsy. The balanced central antagonism to serotonin and dopamine reduces tendency to extrapyramidal side effects and expands therapeutic influence of drug with coverage of negative and affective symptoms of schizophrenia.

Pharmacokinetics. After oral administration active component of drug рисперидон is completely absorbed and reaches Cmax in a blood plasma for 1–2 h. Meal does not influence drug absorption. Risperidon is metabolized by means of P450 2D6 cytochrome to a 9-gidroksirisperidon having pharmacological action similar to a risperidon. Risperidon and 9-gidroksirisperidon form active antipsychotic fraction. Some other way metabolism of a risperidon N-dealkylation is.
At oral administration of T1/2 of a risperidon makes about 3 h, T1/2 of a 9-gidroksirisperidon reaches 24 h.
Risperidon is quickly distributed in an organism. The volume of distribution makes 1–2 l/kg.
Linkng of a risperidon with proteins of a blood plasma (albumine and? a 1-acid glycoprotein) makes 88%, a 9-gidroksirisperidon — 77%.
Equilibrium concentration of a risperidon in a blood plasma at most of patients is reached for 1 days, a 9-gidroksirisperidon — 4–5 days. Concentration of a risperidon in a blood plasma are proportional to a drug dose (within the range of therapeutic doses).
In a week after the beginning of administration of drug of 70% of a dose 14% — with a stake are removed with urine. The summary contents of a risperidon and 9-gidroksirisperidon in urine reaches 35–45% of size of the accepted drug dose, other part is made by inactive metabolites.
At patients of advanced age, and also at patients with the expressed renal failure after a single dose of drug note higher, than usually, concentration of active agent and the slowed-down its removal.
At patients with the expressed abnormal liver function concentration of a risperidon in a blood plasma does not differ from that at patients with normal function of a liver.

Indications to use:

Treatment of an acute psychotic state at schizophrenia and a long maintenance therapy at the chronic course of schizophrenia for prevention of a recurrence.
Monotherapy or the combined treatment of the acute maniacal and mixed episodes at bipolar disorders.

Route of administration and doses:

Schizophrenia
The adult in most cases drug appoint in an initial dose 2 mg/days in 1 or 2 receptions, if necessary raise a dose on 1–2 mg in a day. For most of patients the recommended dose makes 4–6 mg/days.
The dose exceeding 10 mg/days in most cases has no additional benefits of efficiency, can lead to increase in number of side reactions therefore it is recommended with restriction.
At a maintenance therapy of schizophrenia (prevention of a recurrence) Risperon in a dose of 2-6 mg/days is applied. The patients who are on a maintenance therapy need periodic inspection as the dose of drug can change.
For patients of advanced age and patients with the expressed abnormal liver function and/or kidneys initial and the subsequent doses of drug reduce twice.
Bipolar disorders
The recommended initial dose of Risperon makes 2–3 mg/days. If necessary the dose is changed, adding 1 mg/days every other day to 6 mg of drug a day or reduction by 1 mg/days. Efficiency of the doses exceeding 6 mg at bipolar disorders was not studied.
Recommendations for selection of doses of drug
Schizophrenia
Initial dose — 2 mg/days.
Dose for titration — 1–2 mg/days.
Target dose — 4–6 mg/days.
Range of effective doses — 4–16 mg/days.
Bipolar disorders
Initial dose — 2–3 mg/days.
Dose for titration — 1 mg/days.
Target dose — 1–6 mg/days.
Range of effective doses — 1–6 mg/days.

Features of use:

 Because Risperon is a blocker? - adrenoceptors, at its use there can be orthostatic hypotension, especially in an initiation of treatment during selection of a dose.
Risperon it is necessary to apply with care at patients with diseases of cardiovascular system (heart failure, a myocardial infarction, conductivity disturbance), and also at dehydration, a hypovolemia and cerebrovascular disturbances; at the same time the dose of drug needs to be raised gradually, according to recommendations. When developing hypotonia it is necessary to consider a question concerning a dose decline.
At use of drugs with properties of antagonists of dopamine receptors developing of late dyskinesia was noted that is characterized by the involuntary rhythmic movements (preferential language and/or the person). There are messages that emergence of extrapyramidal symptoms is risk factor for development of late dyskinesia. As Risperon in much smaller degree provokes development of extrapyramidal collateral symptoms, in comparison with classical neuroleptics, risk of development of late dyskinesia in comparison with other neuroleptics much less. If there are signs and symptoms of late dyskinesia, it is necessary to consider a question concerning cancellation of all antipsychotic drugs.
At use of classical neuroleptics cases of emergence of an antipsychotic syndrome which is characterized by a hyperthermia, muscle tension, instability of vegetative functions, disturbance of consciousness and increase in level of a kreatinfosfokinaza are described. In case of development of an antipsychotic syndrome it is necessary to cancel all antipsychotic drugs.
It is also necessary to be careful at Risperon's appointment to patients with Parkinson's disease as theoretically it can cause deterioration in a course of a disease.
Rather classical neuroleptics it is known that they reduce a threshold of development of an epileptic attack. Risperon at patients with epilepsy is recommended to apply with care.
Patients should recommend to refrain from an overeating in connection with a possibility of increase in body weight.
Drug contains lactose therefore patients with hereditary intolerance of a galactose are not recommended to apply Risperon.
During treatment by drug emergence of a hyperglycemia or an aggravation of the existing diabetes mellitus is possible.
Risperon, as well as other antipsychotic means, it is necessary to apply with care at patients with an inborn syndrome of lengthening of an interval of Q-T and at a combination therapy the drugs extending Q–T interval.
Use during pregnancy and feeding by a breast. Risperon it is possible to use at pregnancy only in that case when the positive effect justifies potential risk for a fruit.
Women who apply Risperon should stop feeding by a breast.
Children. Experience of use of drug for treatment of children aged up to 15 years is limited.
Ability to influence speed of response at control of vehicles or work with other mechanisms. In the course of treatment it is recommended to refrain from performance of work which demands the increased concentration of attention, bystry mental and motor reactions.

Side effects:

From a nervous system and sense bodys: a sleep disorder, including sleeplessness or drowsiness, hypererethism, fatigue, disturbance of attention, concern, alarm, a headache, dizziness, extrapyramidal frustration (a tremor, rigidity, a bradykinesia, a hypokinesia, hypersalivation, an akathisia, acute dystonia), late dyskinesia, an antipsychotic malignant syndrome, thermal control disturbance, convulsive attacks, a stroke (at predisposed patients of advanced age), confusion of consciousness, a loss of consciousness, a lethargy, orthostatic dizziness, the tranzitorny ischemic attack, cerebrovascular disturbances, a dysarthtia, disorder of the movements, a hypersomnia, a mania, parkinsonism, lack of reaction to an irritant.
From an organ of sight: a vision disorder, a sight illegibility, conjunctivitis, a conjunctiva hyperemia, allocation from eyes, rolling of eyes, the century, a swelling of eyes, a blepharitis, a xerophthalmus, lachrymation, photophobia, glaucoma, decrease in visual acuity swelled.
From an acoustic organ and vestibular mechanism: a ring in ears, ear pain, balance disturbance.
Endocrine frustration: a giperprolaktinemiya, a galactorrhoea, a gynecomastia, a syndrome of inadequate secretion of antidiuretic hormone (ADG), increase in level of glucose of blood, a hyperglycemia (at patients with a diabetes mellitus), a diabetic coma.
Cardial disturbances: orthostatic hypotension, reflex tachycardia, AG, a heart consciousness, a sinus bradycardia, sinus tachycardia, AV blockade of the I degree, blockade of the left branch of a ventriculonector, blockade of the right branch of a ventriculonector, fibrillation of auricles, lengthening of an interval of Q-T on an ECG.
From respiratory system, bodies of a thorax: a nose congestion, nasal bleeding, throat and drink pain, a nasopharyngitis, tonsillitis, tracheitis, bronchitis, pneumonia, cough, диспноэ, goose breathing, a dysphonia, productive cough, developments of stagnation in respiratory tracts, wet rattles, a hyperventilation, an apnoea syndrome in a dream, sinusitis, a grippopodobny syndrome.
Infections and invasions: ear infections (average otitis, including chronic), viral infections, infections of an eye, infection of urinary tract (including cystitis).
From a GIT: anorexia, dyspepsia, hypersalivation, nausea, vomiting, dryness in a mouth, abdominal discomfort, an incontience a calla, gastritis, a swelling of lips, a cheilitis, intestinal impassability, pancreatitis, jaundice, an abdominal pain, a lock, increase in level of hepatic transaminases.
From an urinary system: enuresis, dysuria, polyuria, urine incontience.
From reproductive system and mammary glands: increase in mammary glands, dysmenorrhea, amenorrhea, impotence, disturbance of an erection and ejaculation, anorgazmiya, decrease libido, priapism, sexual dysfunction, retrograde ejaculation, vaginal allocations.
From skin and hypodermic cellulose: cellulitis, an onychomycosis, an acariasis, rash on skin (erythematic, papular, makulopapulezny, generalized character), skin discoloration, a xeroderma, dandruff, seborrheal dermatitis, a hyperkeratosis, an itch, an alopecia, a hyperemia.
From system of blood and lymphatic system: neytro-and thrombocytopenia, a Werlhof's disease, anemia, decrease in hemoglobin, decrease in a hematocrit, a granulocytopenia, an agranulocytosis, thrombocytopenia (including reduction of quantity of thrombocytes, decrease in formation of thrombocytes).
From immune system: a Quincke's disease (including a Quincke's disease, perioral hypostasis, an eye, periorbital hypostasis, a face edema, a mouth, language, a throat, laryngotracheal hypostasis, an okulo-respiratory syndrome, acute hypostasis of a small bowel swelled).
From a musculoskeletal system and connecting fabric: arthralgia, extremity pain, disturbance of a bearing, constraint of joints, mialgiya, muscular weakness, рабдомиолиз.
Others: slackness, rhinitis, a dorsodynia, neck pain, increase in body weight, hypostases, a hypervolemia, a polydipsia, decrease in body temperature, thirst, an indisposition, discomfort, a fever, a cryesthesia in extremities, a drug withdrawal.

Interaction with other medicines:

Taking into account that Risperon exerts impact first of all on TsNS, it should be applied with care along with other drugs of the central action.
At simultaneous use Risperon reduces effect of a levodopa and other agonists of dopamine.
When using carbamazepine and other inductors of liver enzymes decrease in concentration of active antipsychotic fraction of a risperidon in a blood plasma is possible. Therefore at their cancellation Risperon's dose needs to be reconsidered and, if necessary, to lower.
Fluoxetine, fenotiazina, tricyclic antidepressants and some blockers? - adrenoceptors can increase concentration of a risperidon in a blood plasma. Fluoxetine can increase concentration of a risperidon in a blood plasma. It to a lesser extent concerns antipsychotic fraction.
At Risperon's use along with other medicines which substantially contact proteins of a blood plasma clinically expressed replacement of any drug from protein fraction of a blood plasma is not revealed.
Topiramat moderately reduces bioavailability of a risperidon, but not active antipsychotic fraction. However the clinical importance of this interaction is improbable.
Fenotiazina, tricyclic antidepressants and some blockers? - adrenoceptors can increase concentration of a risperidon in a blood plasma.
Amitriptyline does not influence pharmacokinetics of a risperidon or active antipsychotic fraction.
Cimetidinum and ranitidine increase bioavailability of a risperidon, but only the minimum active antipsychotic fraction.
Erythromycin, inhibitors of ZA4 liver enzymes do not change pharmacokinetics of a risperidon and active antipsychotic fraction.
Also donezepit cholinesterase inhibitors, Galantaminum do not render clinically significant effects on pharmacokinetics of a risperidon and active antipsychotic fraction.
It is necessary to be careful at use of drug along with the medicines extending Q–T interval.
Risperon does not reveal clinically significant effects on pharmacokinetics of lithium, Valproatum, digoxin or a topiramat.
Meal does not influence drug absorption Risperon.

Contraindications:

Hypersensitivity to drug.

Overdose:

In the general plan the revealed signs and symptoms of overdose are the known pharmacological effects of drug in more expressed form.
Symptoms: drowsiness, excessive sedation, tachycardia; arterial hypotension, extrapyramidal disturbances; in isolated cases — lengthening of an interval of Q-T.
Treatment: Risperon has no specific antidote therefore at overdose it is necessary to carry out a symptomatic and maintenance therapy: a gastric lavage (after an intubation, if the patient in unconsciousness), purpose of absorbent carbon together with a purgative, ensuring passability of respiratory tracts, constant medical observation and monitoring of function of cardiovascular system. At arterial hypotension and a vascular collapse it is necessary to carry out to infusions and/or to appoint sympathomimetic drugs. In case of development of acute extrapyramidal symptoms appoint anticholinergic drugs. It is necessary to continue constant medical observation and monitoring before recovery of the patient.

Storage conditions:

At a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

Tab. п / captivity. cover of 2 mg, No. 10, No. 20.