SPERIDAN

Active material: Risperidone
When ATH: N05AX08
CCF: Antipsychotic drug (anxiolytic)
ICD-10 codes (testimony): F20, F21, F22, F23, F25, F29, F30, F31
When CSF: 02.01.02.03
Manufacturer: You are active GROUP PTC ehf. (Iceland)

Pharmaceutical form, composition and packaging

Pills, coated white, Oval, lenticular, scored, size 8 × 5 mm.

[Ring] microcrystalline cellulose, lactose bezvodnaya, magnesium stearate, pregelatinized starch, gipromelloza, macrogol 600, Titanium dioxide.

10 PC. – blisters (2) – packs cardboard.

Pills, coated white, Oval, lenticular, scored, size 10 × 5 mm.

Excipients: microcrystalline cellulose, lactose bezvodnaya, magnesium stearate, pre-gelatinized starch, gipromelloza, macrogol 6000, Titanium dioxide.

10 PC. – blisters (2) – packs cardboard.

Pills, coated white, Oval, lenticular, scored, size 14 × 7.5 mm.

Excipients: microcrystalline cellulose, lactose bezvodnaya, magnesium stearate, pre-gelatinized starch, gipromelloza, macrogol 6000, Titanium dioxide.

10 PC. – blisters (2) – packs cardboard.

Pharmacological action

Antipsychotic drug (anxiolytic), benzisoxazole derivative. It has also a sedative, antiemetic and hypothermic effect. Selective monoaminergic antagonist. It has a high affinity for serotonin 5-HT₂-Receptor, dopaminovыm D₂-Receptor; also binds to α₁-adrenoceptors and at slightly lower affinity histamine H₁-рецепторами и a₂-adrenoreceptor. It does not have affinity for holinoretseptorami. Antipsychotic effect due to blockade of dopamine D₂-receptors and the mesolimbic system Mesocortical. Sedative effect due to blockade of adrenergic receptors of the reticular formation of the brain stem; antiemetic effect – blockade of dopamine D₂-receptor trigger zone of the vomiting center; hypothermic effect – blockade of dopamine receptors of the hypothalamus. Reduces productive symptoms (delirium, hallucinations), automatism. It causes minimal suppression of motor activity and to a lesser extent induces catalepsy, than classical antipsychotics (neuroleptics).

Balanced central antagonism of serotonin and dopamine can reduce the risk of extrapyramidal symptoms.

Risperidone may cause a dose-dependent increase in the concentration of prolactin in plasma.

Pharmacokinetics

Absorption

When ingestion rapidly and completely absorbed, wherein the food has no effect on the absorption rate and completeness. C_max plasma achieved through 1-2 no.

C_ss Risperidone in the body is achieved in most patients for 1 day, 9-hydroxy-risperidone – through 4-5 days. Risperidone plasma concentrations are proportional to the dose of the drug (within the therapeutic dose).

Distribution

The drug is rapidly distributed, CNS penetration, breast milk. V_d -1.1 l / kg. Plasma protein binding (alpha₁-glycoprotein and albumin) risperidone – 90%, 9-hydroxy-risperidone – 77%.

Metabolism

Metaboliziruetsya izofermentom CYP2D6 to metabolites aktivnogo – 9-hydroxy-risperidone (risperidone and 9-hydroxy-risperidone constitute active antipsychotic fraction). Another way of metabolism is N-dealkylation.

Deduction

T_1/2 risperidone is 3 no, T_1/2 9-hydroxy-risperidone – 21 no. 70% the drug is excreted by the kidneys, of them 35-45% – in the form of a pharmacologically active fraction; the bile output 14% of the dose of the drug.

In single dose have high levels of the active plasma concentrations and a slow elimination in elderly patients and in patients with renal insufficiency.

Testimony

- Acute and chronic schizophrenia and other psychotic states with productive and / or negative symptoms;

- Affective disorders in a variety of mental disorders;

- Behavioral disorders in patients with dementia when symptoms persist aggression (outburst, physical abuse), for violations of activity (excitation, delirium) or psychotic symptoms;

- As adjunctive therapy (as a mood stabilizer) – behavioral disorders in adolescents over the age of 15 years and adult patients with reduced intellectual level or mental retardation, in cases, if the destructive behavior (aggression, impulsiveness, autoagressiâ) It is leading the clinical picture of the disease;

- As an adjuvant therapy in the treatment of mania in bipolar disorder.

Dosage regimen

At Schizophrenia Adults and adolescents over the age of 15 years drug prescribed 1-2 times / day. The initial daily dose is 2 mg. On the 2nd day, the daily dose should be increased to 4 mg. Then the dose can either remain the same, or if necessary, be adjusted individually. The optimum daily dose – 4-6 mg. In some cases it can be justified by a slow increase in the dose and lower initial and maintenance doses.

When you assign a daily dose 10 mg were observed higher efficiency compared with lower doses. At the same time there may be extrapyramidal symptoms. Because, that the safety of doses over 16 mg / day has not been studied, doses above this level can not be used.

Elderly patients The recommended starting dose is 500 g 2 times / day. The dose may be increased to individually 500 ug per day to 1-2 mg 2 times / day.

In patients with diseases of the liver and kidneys The recommended starting dose is 500 g 2 times / day. The dose can be gradually increased to 1-2 mg 2 times / day.

For information on the use of the drug for schizophrenia in children under 15 years no.

At drug abuse or drug addiction The recommended daily dose is 2-4 mg.

At behavioral disorders in patients with dementia The recommended starting dose is on 250 g 2 times / day (you should use the proper dosage form). Dose if necessary individually to increase 250 ug per day (no more than a day). For most patients, the optimal dose is 500 g 2 times / day. However, some patients shows the drug in a dose of 1 mg 2 times / day. After achieving the optimal dose can be recommended to the drug 1 time / day.

At mania in bipolar disorders recommended starting dose is 2 mg 1 time / day. If necessary, the dose may be increased by 2 mg per day, no more than a day. For most patients, the optimal daily dose is 2-6 mg.

At behavioral disorders in patients with mental retardation patients with a body weight 50 kg or more The recommended initial dose - 500 g 1 time / day. If necessary, the dose may be increased by 500 ug per day, no more than a day. For most patients, the optimal daily dose – 1 mg.

However, for some patients, preferably in a dose of the drug 500 mg / day, While some patients require an increase in dose to 1.5 mg / day.

Patients weighing less than 50 kg The recommended starting dose – 250 g 1 time / day. If necessary, this dose may be increased by 250 ug per day, no more than a day. For most patients, the optimal dose is 500 mg / day. However, for some patients, preferably in a dose of the drug 250 mg / day, While some want to increase the dose to 750 mg / day.

Long-term use Speridana^® teenagers should be under the constant supervision of a doctor.

Use in children under 15 years not recommended.

Side effect

From the central and peripheral nervous system: insomnia, ažitaciâ, alarm, headache; sometimes drowsy, fatigue, dizziness, impaired concentration, blurred vision; rarely – extrapyramidal symptoms (tremor, rigidity, hyperptyalism, bradikineziâ, akathisia, acute dystonia), mania or gipomaniya, stroke (in older patients with predraspolagatmi factors), and hypervolemia (either due to polydipsia, either because the syndrome of inappropriate secretion of ADH), pozdnyaya dyskinesia (involuntary rhythmic movements mainly language and / or the person), neuroleptic malignant syndrome (hyperthermia, muscle rigidity, instability of autonomous functions, impairment of consciousness and increased CPK), violation of thermoregulation and seizures.

From the digestive system: constipation, dyspepsia, nausea or vomiting, abdominal pain, increase in liver transaminases, dry mouth, Hypo- or hypersalivation, anorexia and / or increased appetite, increase or reduction of body weight.

Cardio-vascular system: sometimes orthostatic hypotension, reflex tachycardia, or increased blood pressure.

From the side of hematopoiesis: neutropenia, thrombocytopenia.

On the part of the endocrine system: galactorrhea, gynecomastia, menstrual disorders, amenorrhea, weight gain, Hyperglycemia and exacerbation of preexisting diabetes mellitus.

With the genitourinary system: priapism, erectile dysfunction, abnormal ejaculation, anorgazmija, urinary incontinence.

Allergic reactions: rhinitis, rash, angioedema, photosensitivity.

Dermatological reactions: xerosis, giperpigmentatsiya, itch, seborrhea.

Other: arthralgia.

Contraindications

- Lactation (breast-feeding);

- Hypersensitivity to the drug.

FROM caution It should be prescribed for diseases of the cardiovascular system (congestive heart failure, myocardial infarction, conduction disorders), Dehydration and hypovolemia, cerebrovascular disorders, Parkinson's disease, convulsions (incl. history), severe renal or hepatic insufficiency, drug abuse or drug addiction, states, predisposing to the development of the type of tachycardia “pirouette” (bradycardia, electrolyte imbalance, concomitant drugs, prolonging the QT interval), brain tumors, bowel obstruction, cases of acute overdose of drugs, Reye's syndrome (antiemetic effect of risperidone may mask the symptoms of these conditions), pregnancy, childhood to 15 years (efficacy and safety have not been established).

Pregnancy and lactation

Safety of risperidone in pregnant women has not been studied. In pregnancy, the use is possible only in cases, when the expected benefit of therapy for the mother outweighs the potential risk to the fetus.

Since risperidone and 9-hydroxy-risperidone is excreted in breast milk, If necessary, use during lactation should stop breastfeeding.

Cautions

Transition from other antipsychotic therapy. In schizophrenia the beginning of treatment Speridanom^® It recommended phased previous therapy, if clinically warranted. If patients are transferred from the depot forms of therapy antipsychotics, the reception Speridana^® recommended to start in place of the next scheduled injection. Periodically assess the need for continued therapy antiparkinsonian drugs. In connection with the alpha-adrenoceptor blocking action may occur risperidone orthostatic hypotension, especially during the initial titration. In the event of hypotension should consider lowering the dose. In patients with diseases of the cardiovascular system, as well as dehydration, hypovolemia, or cerebrovascular disorders, the dose should be increased gradually, according to the recommendations.

The occurrence of extrapyramidal symptoms is a risk factor for tardive dyskinesia. In case of signs and symptoms of tardive dyskinesia should consider abolishing all antipsychotics. In the event of neuroleptic malignant syndrome, characterized by hyperthermia, muscle rigidity, instability of autonomous functions, impairment of consciousness and increased levels of creatine kinase is necessary to abolish all antipsychotic drugs, including risperidone.

In case of cancellation of carbamazepine and other hepatic enzyme inducers a dose of risperidone should be reduced.

Patients should be advised to refrain from eating because of the possibility of weight gain.

During treatment should refrain from drinking alcohol.

Effects on ability to drive vehicles and management mechanisms

During treatment should refrain from activities potentially hazardous activities, require high concentration and speed of psychomotor reactions.

Overdose

Symptoms: drowsiness, sedation, depression of consciousness, tachycardia, hypotension, extrapyramidal disorder, rarely – QT prolongation.

Treatment: necessary to ensure a free airway to ensure adequate oxygenation and ventilation, gastric lavage (after intubation, if the patient is unconscious) and assigning the activated carbon in combination with laxatives. Symptomatic therapy, is to maintain vital body functions. The specific antidote is absent.

For early diagnosis of possible disturbances of cardiac rhythm as quickly as possible to begin ECG monitoring. Careful medical supervision and ECG monitoring is carried out to complete disappearance of symptoms of intoxication.

Drug Interactions

Considering, that Speridan^® It has an effect primarily on the central nervous system, It should be used with caution in combination with other drugs and with central action akogolem.

Speridan^® reduces the effectiveness of levodopa and other dopamine agonists.

Clozapine reduces the clearance of risperidone.

In the application of carbamazepine, a decrease of concentration of the active antipsychotic fraction of risperidone in plasma. Similar effects can be observed in the application of other hepatic enzyme inducers.

Fenotiazinы, tricyclic antidepressants and some beta-blockers may increase the plasma concentrations of risperidone, however, this does not affect the concentration of the active antipsychotic fraction.

Fluoxetine can increase plasma concentrations of risperidone, but to a lesser extent the concentration of the active antipsychotic fraction, therefore the dose of risperidone should be adjusted.

In applying Speridana^® together with other drugs, highly bound to plasma proteins, symptomatic displacement of a drug from the plasma protein fraction is observed.

Antihypertensive medicines increase the severity of BP reduction, while the application with Speridanom^®.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 3 year.