Eridanum

General characteristics. Structure:

Active ingredient: risperidona of 4 mg;

Excipients: lactoses monohydrate, starch corn, cellulose microcrystallic, a gipromeloza, magnesium stearate, silicon dioxide colloid anhydrous, sodium lauryl sulfate, a covering for drawing a cover of Opadry II Pink (ferrous oxide red (Е 172), ferrous oxide yellow (Е 172), ferrous oxide black (Е 172), polyethyleneglycol, polyvinyl alcohol, talc, titanium dioxine (Е 171).

Pharmacological properties:

Pharmacodynamics. Risperidon is the selection antagonist 5-HT2-serotoninergicheskikh and D2-dofaminergichesky receptors; it blocks also a1-adrenergic and to a lesser extent - histamine N1-and a1-adrenergic receptors, without showing influence on cholinergic receptors. Though рисперидон is powerful D2 antagonist that connect with its efficiency in relation to 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 Eridon - рисперидон - is completely absorbed and reaches the maximum concentration in plasma within 1-2 hours. Meal does not influence drug absorption. Risperidon is metabolized through R-450 IID6 cytochrome to a 9-gidroksirisperidon who has pharmacological effect 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 the elimination half-life of a risperidon makes about 3 hours, the elimination half-life of a 9-gidroksirisperidon reaches 24 hours.
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 α1-кислым a glycoprotein) makes 88%, a 9-gidroksirisperidon - 77%.
Equilibrium concentration of a risperidon in a blood plasma at most of patients is reached within 1 days, a 9-gidroksirisperidon - within 4-5 days.
Concentration of a risperidon in plasma is proportional to a drug dose (within 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 quantity is made by inactive metabolites.
At patients of advanced age, and also at patients with the expressed renal failures after one-time administration of drug higher concentration of active agent and the slowed-down its removal is noted.
At patients with the expressed abnormal liver functions concentration of a risperidon in a blood plasma does not differ from concentration which is observed at patients with normal function of a liver.

Indications to use:

Stoppings of bad attacks and a long maintenance therapy at a chronic current:
- at acute and chronic schizophrenia (including the first episode of psychosis) and other psychotic frustration with productive (hallucinations, nonsense, disorders of thinking, hostility, suspiciousness) and negative (block of emotions, emotional and social estrangement, poverty of the speech) symptomatology;
- at affective frustration at schizophrenia (alarm, fear, a depression);
Monotherapy or the combined treatment of the acute maniacal and mixed episodes at bipolar disorders.

Route of administration and doses:

Schizophrenia.
Transition from therapy by other antipsychotic drugs.
If it is clinically justified, during therapy by drug Eridon is recommended to stop gradually previous therapy by other drugs. At the same time, if the patient is transferred from antipsychotic therapy in the form of "depot", drug Eridon is recommended to begin treatment instead of the following planned injection. Periodically it is necessary to estimate need for extension of the current therapy by antiparkinsonichesky drugs.

Adults.
In most cases drug appoint in an initial dose 2 mg a day in 1 or 2 receptions, if necessary increase a dose by 1-2 mg a day. For most of patients the recommended dose makes 4-6 mg a day.
The dose exceeding 10 mg a day in most cases has no additional benefits of efficiency, can lead to increase in number of side reactions therefore it is recommended with restrictions.
Safety of doses more than 16 mg a day was not studied therefore these doses cannot be applied.
The maintenance therapy of schizophrenia (prevention of a recurrence) assumes use of 2-6 mg of Eridon a day. The patients receiving a maintenance therapy need periodic inspection since the dose of drug can change.

Patients of advanced age.
The recommended initial dose - 0,5 mg two times a day. In case of need it is possible to increase a dose to 1-2 mg two times a day.

Bipolar disorders.
Adults.
The recommended initial dose of Eridon makes 2-3 mg a day. If necessary the dose is changed addition of 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.

Patients of advanced age.
The recommended initial dose - 0,5 mg two times a day. In case of need it is possible to increase a dose to 1-2 mg two times a day.
Recommendations concerning selection of doses of drug

Indications to use	Initial dose	Dose for titration	Target dose	Range of effective doses
Schizophrenia	2 mg/days	1-2 mg/days	4-6 mg/days	4-16 mg/days
Bipolar disorders	2-3 mg/days	1 mg/days	1-6 mg/days	1-6 mg/days

Patients with diseases of a liver and kidneys.
The recommended initial dose - 0,5 mg two times a day. It is possible to increase the specified dose individually to 1-2 mg two times a day. At treatment of patients of this group Eridon it is necessary to apply with care before obtaining additional information.

Features of use:

Use during pregnancy and feeding by a breast.
Pregnancy.
Eridanum can be accepted at pregnancy only in that case when the positive effect justifies potential risk for a fruit.
Feeding by a breast.
Women who apply Eridon should not nurse.

Children.
Risperidon is not recommended at children up to 18 years with schizophrenia and bipolar disorders in connection with limited experience of use of drug.

the α-blocking activity.
Because Eridon is a α-blocker, at its use there can be orthostatic hypotension, especially in an initiation of treatment during selection of a dose.
Eridanum should be applied with care to patients with diseases of cardiovascular system (heart failure, a myocardial infarction, conductivity disturbances), and also at dehydration, a hypovolemia and cerebrovascular disturbances; at the same time the dose of drug should be increased gradually, according to recommendations. When developing hypotonia it is necessary to consider a question of a dose decline.

Late dyskinesia / extrapyramidal symptoms.
At use of drugs with properties of antagonists of dopamine receptors developing of late dyskinesia which is characterized by the involuntary rhythmical movements was noted (preferential language and/or the person). It was reported about emergence of extrapyramidal symptoms which are risk factor of developing of late dyskinesia. As Eridanum in much smaller degree provokes development of EPS in comparison with classical neuroleptics, the risk of development of late dyskinesia in comparison with other neuroleptics is much less. If there are signs and symptoms of late dyskinesia, it is necessary to consider a question of cancellation of all antipsychotic drugs.

Antipsychotic syndrome.
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.

Hyperglycemia.
During treatment by drug emergence of a hyperglycemia or an aggravation of the existing diabetes mellitus is possible.

QT interval.
Eridanum, as well as other antipsychotic means, patients should apply with care with an inborn syndrome of lengthening of an interval of QT and at joint therapy by drugs which extend QT interval.

Giperprolaktinemiya.
Eridanum should be applied with care at patients with already existing giperprolaktinemiya and at patients with possible prolactin - dependent tumors.

Others.
Rather classical neuroleptics it is known that they reduce a threshold of development of an epileptic seizure. Eridon the patient with epilepsy is recommended to apply with care.
It is also necessary to be to patients, careful at Eridon's appointment, with Parkinson's disease as theoretically it can cause deterioration in course of a disease.
Patients should recommend to abstain 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 Eridon.

Ability to influence speed of response at control of motor transport or work with other mechanisms. In the course of treatment it is recommended to abstain from performance of work which demands the increased concentration of attention, bystry mental and motor reactions.

Side effects:

Side reactions which are observed at Eridon's use are listed below.
From a nervous system and sense bodys: sleep disorders, 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 disturbances, 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 frustration, a dysarthtia, disturbances of movements, a hypersomnia, a mania, parkinsonism, lack of reaction to an irritant.

From organs of sight: vision disorders, a sight illegibility, conjunctivitis, an eye hyperemia, allocations from eyes, rolling of eyes, swell a century, a swelling of eyes, a crust on the edge of a century, a xerophthalmus, lachrymation, photophobia, glaucoma, decrease in visual acuity.

From acoustic organs and vestibular mechanism: a ring in ears, ear pain, balance disturbance.

From endocrine system: a giperprolaktinemiya, a galactorrhoea, a gynecomastia, a syndrome of inadequate secretion of antidiuretic hormone (ADG), increase in level of glucose in blood, a hyperglycemia (at patients with a diabetes mellitus), a diabetic coma.

From cardiovascular system: orthostatic hypotension, reflex tachycardia, arterial hypertension, feeling of heartbeat, a sinus bradycardia, sinus tachycardia, an atrioventricular block of the first 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 QT on the cardiogram.

From respiratory system, bodies of a thorax: a nose congestion, nasal bleeding, faringolaringichesky 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 the alimentary system: 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, disturbances of an erection and ejaculation, anorgazmiya, decrease libido, priapism, sexual dysfunction, retrograde ejaculation, vaginal allocations.

From skin and hypodermic cellulose: cellulitis, onychomycosis, acariasis, enanthesis (erythematic, papular, makulopapulezny, generalized), skin discoloration, xeroderma, dandruff, seborrheal dermatitis, hyperkeratosis, itch, alopecia, 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 decrease in quantity of thrombocytes, decrease in formation of thrombocytes).

From immune system: a Quincke's disease (the term includes a Quincke's disease, circumoral hypostasis, an eye, periorbital hypostasis, a face edema, a mouth, language, a throat, laryngotracheal hypostasis, a hereditary Quincke's disease, an okulo-respiratory syndrome, acute hypostasis of a small bowel swelled).

From a musculoskeletal system and connecting fabric: arthralgia, extremity pain, disturbances 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, cold sense in extremities, a drug withdrawal.

Interaction with other medicines:

Taking into account that Eridon has influence first of all on the central nervous system, it should be applied with care along with other drugs of the central action.

At simultaneous use Eridon reduces effect of a levodopa and other agonists of dopamine.

At use of 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 Eridon's dose needs to be reconsidered and if necessary to lower.

Fluoxetine, fenotiazina, tricyclic antidepressants and some β-blockers can increase concentration of a risperidon in plasma. Fluoxetine can increase concentration of a risperidon in plasma. It concerns antipsychotic fraction less. When Eridanum is applied together with other medicines which substantially contact proteins of plasma, clinically expressed replacement of any drug from protein fraction of plasma is not observed.

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 ß adrenoblockers can increase concentration of a risperidon in 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 medicines which extend QT interval.

Eridanum does not render clinically significant effects on pharmacokinetics of lithium, Valproatum, digoxin or a topiramat.

Clinically significant arterial hypotension was observed at simultaneous use of a risperidon and anti-hypertensive drugs.

Meal does not influence drug absorption Eridon.

Contraindications:

Eridanum is contraindicated to patients with the established hypersensitivity to drug.

Overdose:

In the general plan signs and symptoms of overdose which were observed are the known pharmacological effects of drug in the strengthened form.

Symptoms.
Drowsiness, excessive sedation, tachycardia; arterial hypotension, extrapyramidal disturbances; in isolated cases - lengthening of an interval of QT.

Treatment.
Eridanum 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 unconscious patient), 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 intravenous injections and/or to appoint sympathomimetic drugs. In case of development of acute extrapyramidal symptoms it is necessary to appoint anticholinergic drugs. It is necessary to continue constant medical observation and monitoring till the moment when the patient recovers.

Storage conditions:

To store in the place, unavailable to children, in original packaging, at a temperature not over 25 ºС.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in the blister; on 3 or 6 blisters in a pack cardboard.