Рисполепт

Рисполепт – derivative a benzizoksazola, antipsychotic drug (neuroleptic) with sedative, hypothermal and antiemetic action.

Form of release and structure

• tablets, film coated: oblong, from two parties convex, from risky: 1 mg – white color, with texts "1" and "Ris" on one party, 2 mg – light orange color, with texts "2" and "Ris" on one party, 3 mg – yellow color, with texts "3" and "Ris" on one party, 4 mg – green color, with texts "4" and "Ris" on one party (on 10 pieces in blisters, in a cardboard box of 2 or 6 blisters);
• solution for intake: colourless, transparent (on 30 or 100 ml in dark glass bottles, in a cardboard pack 1 bottles and the graduated pipette).

Active agent – рисперидон:

• 1 tablet – 1, 2, 3 or 4 mg;
• 1 ml of solution – 1 mg.

Additional components of tablets:

• excipients: starch corn, cellulose microcrystallic, gipromelloza 2910, lactoses monohydrate, magnesium stearate, sodium lauryl sulfate, silicon dioxide colloid;
• structure of a cover: propylene glycol, a gipromelloza 2910, besides in mg tablets 2, 3 and 4 – titanium dioxide, talc, dyes (in tablets of 2 mg – a sunset yellow (E110), in tablets of 3 mg – quinolinic yellow (E104), in tablets of 4 mg – quinolinic yellow (E104) and indigo carmine (E132)).

Solution excipients for intake: water the purified, tartaric acid, sodium hydroxide and the benzoic acid.

Indications to use

In tablets of Rispolept it is applied to stopping of bad attacks and a long maintenance therapy of the following states / diseases:

• the acute and chronic schizophrenia and other psychotic frustration which are followed by productive and negative symptomatology;
• behavioural frustration at patients with dementia – at activity disturbances (nonsense, excitement), emergence of psychotic symptoms or signs of aggression (physical abuse, fits of anger);
• affective frustration at various mental diseases;
• disorders of behavior at patients (15 years are more senior) with the reduced intellectual level or a delay of intellectual development in cases when in a clinical picture destructive tendencies dominate (an autoaggression, impulsiveness, aggression);
• manias at bipolar disorders (as means of auxiliary therapy for stabilization of mood).

In the form of solution for intake of Rispolept appoint in the following cases:

• schizophrenia at adults and teenagers of 13 years;
• the maniacal episodes of average and heavy degree connected with bipolar disorder at adults and children of 10 years;
• short-term (up to 6 weeks) therapy of continuous aggression at patients with dementia accompanying Alzheimer's disease, average and heavy degree which does not give in to non-drug methods of correction, and in cases when there is a risk that the patient can do harm to himself or other persons;
• short-term (up to 6 weeks) symptomatic therapy of continuous aggression in the structure of disorder of behavior at children of 5 mentally retarded years (established according to the Guide to diagnosis and statistics of mental disorders of DSM-IV) demanding drug treatment because of weight of aggression or other destructive behavior (Rispolept is applied as a part of the complex treatment including educational and psychological actions).

Contraindications

• fenilketonuriya;
• lactation period;
• children's age up to 5 years (for peroral solution);
• hypersensitivity to any component of Rispolept.

With care:

• spasms, in the anamnesis including;
• Parkinson's disease;
• disturbances of cerebral circulation;
• acute overdose of medicines;
• intestinal impassability;
• disease of diffusion little bodies of Levi;
• dehydration and hypovolemia;
• brain tumor;
• heavy renal/liver failure;
• syndrome to Reja;
• diseases of cardiovascular system (disturbance of conductivity of a cardiac muscle, the postponed myocardial infarction, chronic heart failure);
• states owing to which development of tachycardia in the pirouette type is possible (disturbance of electrolytic balance, bradycardia, the accompanying use of the medicines capable to extend QT interval);
• risk factors of development of a thromboembolism of venous vessels;
• abuse of medicines or medicinal dependence;
• cerebrovascular dementia at patients of advanced age;
• pregnancy;
• age up to 15 years (for tablets).

Route of administration and dosage

Both dosage forms of Rispolept are intended for oral administration. Meal does not influence efficiency of drug.

Tablets, film coated
At schizophrenia to adults and children 15 years are more senior appoint: in the first day – 2 mg, for the second day – 4 mg, leave further a dose or adjust if in it there is a need (frequency rate of use – 1 or 2 times a day). An optimum daily dose – 4-6 mg. In some cases reasonablly slower increase in a dose, and also use of lower in the initial and supporting doses.

In need of receiving additional sedation in addition to Rispolept appoint benzodiazepines.

The recommended initial dose for elderly people, patients with renal failures and a liver makes on 0,5 mg 2 times a day, further it is possible to increase a dose by 0,5 mg 2 times a day before achievement of the most admissible dose of 1-2 mg 2 times a day.

At treatment of a mania at bipolar disorders at the beginning of therapy appoint 2 mg of 1 times a day, if necessary further raise a dose on 2 mg of 1 times in 2 days or is more rare. The daily dose of 2-6 mg in most cases is optimum.

To patients with medicinal dependence and to the people abusing medicines appoint 2-4 mg a day.

At behavioural frustration at patients with dementia the initial dose makes on 0,25 mg 2 times a day. If necessary further the dose is raised on 0,25 mg of 1 times in 2 days or is more rare. The daily dose on 0,5 mg 2 times a day in most cases is optimum, but use on 1 mg 2 times a day sometimes is required. After achievement of necessary effect frequency rate of reception can be reduced to 1 time a day.

At disorders of behavior at patients with a delay of intellectual development and in cases when the destructive behavior is the leader in a clinical picture of a disease, appoint:

• patients with body weight from 50 kg: the initial dose – 0,5 mg of 1 times a day, further is not more often than 1 time in 2 days if there is a need, the dose is raised on 0,5 mg a day. A daily dose, optimum for most of patients, – 1 mg though in some cases more preferable welcome of 0,5 mg a day can be accorded, and for some patients – 1,5 mg a day;
• patients with body weight to 50 kg: the initial dose – 0,25 mg of 1 times a day, further is not more often than 1 time in 2 days if there is a need, the dose is raised on 0,25 mg a day. A daily dose optimum in most cases – 0,5 mg though in some cases more preferable welcome of 0,25 mg a day can be accorded, and for some patients – 0,75 mg a day.

Solution for intake
The recommended doses at schizophrenia:

• adults: in the first day – 2 mg, for the second day – 4 mg, leave further a dose or adjust if in it there is a need. An optimum daily dose – 4-6 mg. In some cases reasonablly slower increase in a dose, and also use of lower in the initial and supporting doses;
• patients of advanced age: an initial dose – on 0,5 mg 2 times a day, if necessary further increase a dose by 0,5 mg 2 times a day to the maximum dose of 1-2 mg 2 times a day;
• teenagers of 13 years: the initial dose makes 0,5 mg of 1 times a day (in the morning or in the evening). If the effect is not enough, a dose gradually – is not more often than 1 time a day – increase by 0,5-1 mg a day (on condition of good tolerance of drug). The maximum daily dose – 3 mg.

The recommended dosing modes at the maniacal episodes connected with bipolar disorder:

• adults: an initial dose – 2 mg of 1 times a day, in need of 1 times a day increase it by 1 mg. The optimum dose is selected individually and can vary ranging from 1 to 6 mg;
• elderly patients: an initial dose – on 0,5 mg 2 times a day, if necessary further a dose gradually – 2 times a day – increase by 0,5 mg before achievement of a daily dose on 1-2 mg 2 times a day;
• children of 10 years: an initial dose – 0,5 mg of 1 times a day (in the morning or in the evening). If the effect is not enough, a dose gradually – is not more often than 1 time a day – increase by 0,5-1 mg a day (on condition of good tolerance of drug). The maximum recommended daily dose – 1-2,5 mg.

At continuous aggression at patients with dementia owing to Alzheimer's disease in an initiation of treatment appoint 0,25 mg 2 times a day. If necessary a dose gradually – is not more often than 1 time in 2 days – is increased by 0,25 mg by 2 times a day. In most cases an optimum dose are about 0,5 mg 2 times a day, however increase in a dose up to 1 mg 2 times a day can be required by certain patients. Duration of treatment of these patients should not exceed 6 weeks.

The recommended dosages at continuous aggression in structure of disorder of behavior at children of 5-18 years:

• patients with body weight from 50 kg: an initial dose – 0,5 mg of 1 times a day, if necessary gradually – on a thicket than 1 time in 2 days – a dose raise on 0,5 mg a day. In most cases an optimum daily dose is 1 mg, however some patients have enough 0,5 mg a day, and 1,5 mg a day can be required by certain patients;
• patients with body weight to 50 kg: the initial dose – 0,25 mg of 1 times a day, further is not more often than 1 time in 2 days if there is a need, the dose is raised on 0,25 mg a day. A daily dose optimum in most cases – 0,5 mg though in some cases more preferable welcome of 0,25 mg a day can be accorded, and for some patients – 0,75 mg a day.

To patients with diseases of kidneys the initial and supporting doses are reduced twice, and increase in a dosage is carried out with big intervals.

Patients in whom Rispolept causes steady drowsiness are recommended to divide a daily dose into 2 receptions.

Side effects

• from a nervous system: very often (> 1/10 cases) – parkinsonism, drowsiness, a headache, sedation; often (> 1/100 and <1/10 cases) – a tremor, dizziness, an akathisia, dyskinesia, dystonia, a lethargy; infrequently (> 1/1000 and <1/100 cases) – disturbance of movements, balance disturbance, the tranzitorny ischemic attack, a syncope, a loss of consciousness, lack of reaction to irritants, a hypersomnia, disturbance of the speech, a food faddism, a hypesthesia, an incoordination, disturbance of attention, a dysarthtia, postural dizziness, disturbance of consciousness, frustration of flavoring feelings, cerebral ischemia, spasms, late dyskinesia, a stroke; seldom (> 1/10 000 and <1/1000 cases) – a head tremor, a diabetic coma, a malignant antipsychotic syndrome, cerebrovascular disturbances;
• mental disturbances: very often – sleeplessness; often – excitement, alarm, sleep disorders, concern; infrequently – slackness, manias, nervousness, decrease in a libido, confusion of consciousness; seldom – affect flattening, an anorgazmiya;
• from skin and hypodermic fabrics: often – rash, an erythema; infrequently – acne rash, an acne, an alopecia, skin discoloration, an itch, disturbance of integuments, a xeroderma, damage of skin, a hyperkeratosis, seborrheal dermatitis; seldom – dandruff; very seldom (<1/10 000 cases) – a Quincke's edema;
• disturbances of laboratory and tool indicators: often – increase in body weight, increase in level of prolactin; infrequently – fervescence, increase in concentration of cholesterol, reduction of level of hemoglobin and quantity of leukocytes in blood, rejections of the electrocardiogram (including lengthening of an interval of QT), increase in level of a kreatinfosfokinaza, quantity of eosinophils in blood, the level of transaminases; seldom – increase in concentration of triglycerides, fall of temperature of a body;
• from cardiovascular system: often – arterial hypertension, tachycardia; infrequently – blockade of a ventriculonector, disturbance of conductivity of heart, heartbeat, fibrillation of auricles, an atrioventricular block; seldom – an embolism of a pulmonary artery, a sinus bradycardia, a deep vein thrombosis;
• from digestive tract: often – hypersalivation, dryness in a mouth, pain in a stomach, discomfort in a stomach, a diarrhea/lock, dyspepsia, vomiting, nausea; infrequently – a meteorism, gastritis, a fekaloma, an incontience a calla, a dysphagy, a gastroenteritis; seldom – a cheilitis, hypostasis of lips, pancreatitis, impassability of intestines;
• from an acoustic organ: infrequently – pain and a sonitus;
• from a musculoskeletal system and connecting fabric: often – an arthralgia, dorsodynias, extremity pains; infrequently – muscular stethalgias, neck pains, constraint in joints, swelling of joints, a mialgiya, muscular weakness, disturbance of a bearing; seldom – рабдомиолиз;
• disturbances of a mediastinum, respiratory and thoracic disturbances: often – pain in a throat and drinks, cough, short wind, a nose congestion, nasal bleeding; infrequently – a dysphonia, breath disturbance, aspiration pneumonia, disturbance of passability of respiratory tracts, stagnation in lungs, goose breathing, wet rattles; seldom – a hyperventilation, an apnoea syndrome in a dream;
• vascular disorders: infrequently – inflows, hypotension, orthostatic hypotension;
• gepatobiliarny disturbances: seldom – jaundice;
• from endocrine system: seldom – disturbance of production of antidiuretic hormone;
• from kidneys and urinary tract: often – enuresis; infrequently – a dysuria, a pollakiuria, an urine incontience, an urination delay;
• from reproductive system and mammary glands: infrequently – a gynecomastia, a galactorrhoea, an amenorrhea, allocations from a vagina, frustration of a menstrual cycle, sexual dysfunction, disturbance of an ejaculation, erectile dysfunction; seldom – a priapism;
• hematologic disturbances and disturbances of lymphatic system: infrequently – thrombocytopenia, anemia; seldom – an agranulocytosis, a granulocytopenia;
• disturbances of metabolism and food: often – decrease/increase in appetite; infrequently – a hyperglycemia, a diabetes mellitus, a polydipsia, anorexia; seldom – water intoxication, a hypoglycemia; very seldom – diabetic ketoacidosis;
• from immune system: infrequently – hypersensitivity; seldom – anaphylactic reaction, medicinal hypersensitivity;
• infections: often – ear infections, sinusitis, upper respiratory tract infections, bronchitis, flu, pneumonia, infections of urinary tract; infrequently – the localized infections, average otitis, tonsillitis, an acrodermatitis, viral infections, infections of eyes, an inflammation of a hypodermic fatty tissue, an onychomycosis, cystitis; seldom – chronic average otitis;
• ophthalmologic disturbances: often – conjunctivitis, indistinct sight; infrequently – a photophobia, area hypostasis around eyes, allocations from eyes, the strengthened dacryagogue, a vision disorder, reddenings of eyes, a xerophthalmus; seldom – glaucoma, decrease in visual acuity, an intraoperative syndrome of a flabby iris, involuntary rotations of eyeglobes;
• general disturbances: often – an adynamy, fatigue, pains in a thorax, a pyrexia, generalized hypostasis, peripheral hypostasis; infrequently – a fever, sluggishness, feeling sick, gait disturbance, thirst, a face edema, discomfort in a thorax, a grippopodobny state; seldom – a withdrawal, a hypothermia, a cold snap of extremities.

Special instructions

Before Rispolept's appointment children and mentally retarded teenagers need to carry out careful assessment of their state to exclude the social or physical reasons of their agressive behavior, such as pain or inadequate requirements of the social environment.

At schizophrenia at the initial stage of treatment by Rispolept it is recommended to cancel gradually previous used medicines if it is clinically justified. Patients who are transferred from depot of forms of antipsychotic means of Rispolept are recommended to begin to accept instead of the following planned injection. The patients receiving protivoparkinsonichesky drugs should estimate need of their use periodically.

In case of development of orthostatic hypotension it is necessary to lower Rispolept's dose.

During treatment it is recommended to refrain from an overeating in connection with probability of increase in body weight.

Before establishment of individual sensitivity to a risperidon it is necessary to avoid driving of the car and performance of other potentially dangerous types of activity demanding the speed of reactions and high concentration of attention.

Medicinal interaction

With care of Rispolept it is necessary to apply in a combination with other drugs of the central action and ethanol.

Carbamazepine and, presumably, other inductors of liver enzymes promote decrease in concentration of active antipsychotic fraction of a risperidon in plasma.

Fluoxetine can increase concentration of a risperidon in plasma, however exerts impact on concentration of active antipsychotic fraction to a lesser extent.

At simultaneous use of anti-hypertensive drugs expressiveness of a lowering of arterial pressure amplifies.

Clozapine reduces clearance of a risperidon.

Рисполепт reduces efficiency of a levodopa and other agonists of a dopamine.

Terms and storage conditions

To store in the place, unavailable to children, at a temperature 15-30ºС.

Period of validity – 3 years.