Speridan - instructions for use, doses, side effects, contraindications

Composition:1 tablet 1 mg of co-content:
active substance: risperidone 1 mg; Excipients: lactose anhydrous 61.25 mg, microcrystalline cellulose 8.75 mg, magnesium stearate 0.5 mg, pregelatinized starch 18.5 mg; film coating: hypromellose 1.646 mg, macrogol 6000 0.402 mg, titanium dioxide 0.201 mg.
1 tablet 2 mg contains:
active substance: risperidone 2 mg; Excipients: lactose anhydrous 122.5 mg, microcrystalline cellulose 17.5 mg, magnesium stearate 1 mg, pregelatinized starch 37 mg; film coating: hypromellose 3.293 mg, macrogol 6000 0.805 mg, titanium dioxide 0.402 mg.
1 tablet of 4 mg contains:
active substance: risperidone 4 mg; Excipients: lactose anhydrous 245 mg, microcrystalline cellulose 35 mg, magnesium stearate 2 mg, pregelatinized starch 74 mg; film coating: hypromellose 6,586 mg, macrogol 6000 1.61 mg, titanium dioxide 0.804 mg.

Description:Tablets 1 mg
White, oval, biconvex tablets, covered with a shell, with a risk on one side of the tablet and engravings "T" on the one side of the risks and "1" on the other side of the risks, in the fracture core of white.
Tablets 2 mg
White, oval, biconvex tablets covered with a coating, with risk from one side of the tablet and engravings "T" on one side.of risks and "2" on the other side of the risks, in the fracture core of white.
Tablets 4 mg
White, oval, biconvex tablets, covered with a shell, with a risk on one side of the tablet and the engraving "T" on the one hand of the risks and "4" on the other side of the risks, in the fracture core of white.

Pharmacotherapeutic group:Antipsychotic agent (antipsychotic).

ATX: & nbsp

N.05.A.X Other antipsychotics

N.05.A.X.08 Risperidone

Pharmacodynamics:Antipsychotic agent (antipsychotic), benzisoxazole derivative; also has a sedative, anti-rheumatic and hypothermic effect. Selective monoaminergic antagonist, has a high tropism for serotonergic 5-HT2 and dopaminergic B2 receptors, also binds to alpha 1-adrenoreceptors and with a slightly lower affinity for H₁-gistaminergic and alpha-adrenergic receptors. Has no tropism for cholinergic receptors Antipsychotic action is due to blockade of dopamine H2-receptors of the mesolimbic and mesocortical system. Sedative action is due to blockade of adrenoreceptors of the reticular formation of the brainstem; antiemetic effect - blockade of dopamine D2 receptors in the trigger zone of the vomiting center; hypothermic action - blockade of dopamine receptors of the hypothalamus.
Reduces productive symptoms (delirium, hallucinations), automatism. It causes less inhibition of motor activity and to a lesser degree induces catalepsy than classical antipsychotics (antipsychotics).
A balanced central antagonism to serotonin and dopamine may reduce the risk ofextrapyramidal symptoms.
Risperidone can cause a dose-dependent increase in prolactin concentration in the plasma.

Pharmacokinetics:Absorption. When ingested, the drug is absorbed quickly and completely, while the food does not affect the completeness and absorption rate. The maximum concentration in the plasma is achieved in 1-2 hours. The equilibrium concentration of risperidone in the body in most patients is reached within 1 day, 9-hydroxy-risperidone - after 4-5 days. The concentrations of risperidone in plasma are proportional to the dose of the drug (within therapeutic doses).
Distribution. The drug is quickly distributed, penetrates the central nervous system, breast milk. The volume of distribution is 1.1 l / kg. The connection with plasma proteins (with alpha 1-glycoprotein and albumin) risperidone - 90%, 9-hydroxy-risperidone - 77%.
Metabolism. Metabolized by the enzyme cytochrome CYP2D6 to the active metabolite - 9-hydroxy-risperidone (risperidone and 9-hydroxy-risperidone constitute the active antipsychotic fraction). Another way of metabolism is N-dealkylation.
Excretion. The half-life of risperidone is 3 hours, the half-life of 9-hydroxy-risperidone is 21 hours.70% of the drug is excreted by the kidneys, of which - 35-45% - in the form of a pharmacologically active fraction; with bile 14% of the drug is excreted.
With a single admission, high levels of active plasma concentrations and slow excretion in elderly patients and in patients with renal insufficiency are noted.

Indications:Schizophrenia (acute and chronic) and other psychotic conditions with productive and / or negative symptoms.
Affective disorders in various mental illnesses.
Behavioral disorders in patients with dementia in the manifestation of symptoms of aggression (outbursts of anger, physical abuse), with violations of activity (agitation, delirium) or psychotic symptoms.
As an adjuvant therapy (as a mood stabilizer), behavioral disorders in adolescents with 15 years of age and adult patients with reduced intellectual level or mental retardation, in cases where destructive behavior (aggressiveness, impulsivity, autoaggression) is leading in the clinical picture of the disease.
As an auxiliary therapy in the treatment of mania in bipolar disorders.

Contraindications:Hypersensitivity to the components of the drug; lactation period.

Carefully:Diseases of the cardiovascular system (chronic heart failure, suffered myocardial infarction, cardiac muscle conduction disorders) dehydration and hypovolemia of cerebral circulation disorder Parkinson's disease convulsions (including in history) severe renal or hepatic insufficiency (see recommendations for dosing) drug abuse or drug dependence (see recommendations for dosing), conditions predisposing to the development of tachycardia such as "pirouette" (bradycardia, on electrolyte balance, concomitant medication prolonging QT interval) brain tumor, intestinal obstruction, cases of acute drug overdose, Reye syndrome (antiemetic effect of risperidone may mask the symptoms of these conditions) pregnancy, children under 15 years of age (efficacy and safety not established) .

Pregnancy and lactation:The safety of risperidone in pregnant women has not been studied. When pregnancy can be used only if the positive effect justifies the possible risk.
Because the risperidone and 9-hydroxy-risperidone penetrate into breast milk, women who use the drug should not be breast-fed.

Dosing and Administration:Schizophrenia.
Adults and children over 15 years. Speridane can be administered once or twice a day. The initial dose 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.
Information on use for the treatment of schizophrenia in children under the age of 15 is not available.
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.
Diseases of the liver and kidneys. Recommended initial dose of 0.5 mg per reception 2 times a day. This dose can be gradually increased to 1-2 mg per reception twice a day.
Abuse of medicines or drug dependence - the recommended daily dose of the drug is 2-4 mg.
Behavioral disorders in patients with dementia.
An initial dose of 0.25 mg per reception is recommended twice a day (an adequate dosage form should be used). 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.
Once the optimal dose is reached, the drug may be recommended once a day.
Mania in bipolar disorders
The recommended initial dose of the drug is 2 mg per day at a time. If necessary, this dose may be increased by 2 mg per day, not more often than every other day. For most patients, the optimal dose is 2-6 mg per day.
Behavioral disorders in patients with mental retardation
Patients weighing 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 is 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.
Long-term use of Speridan in adolescents should be carried out under the constant supervision of a doctor.
Use in children younger than 15 years is not recommended.

Side effects:From the nervous system: insomnia, agitation, anxiety, headache, sometimes drowsiness, increased fatigue, dizziness, impaired concentration, blurred vision, rarely - extrapyramidal symptoms (tremor, stiffness, hypersalivation, bradykinesia, akathisia,acute dystonia), mania or hypomania, stroke (in elderly patients with predisposing factors), as well as hypervolemia (either due to polydipsia or due to the syndrome of inadequate secretion of the antidiuretic hormone), tardive dyskinesia (involuntary rhythmical movements predominantly of the tongue and / or persons), neuroleptic malignant syndrome (hyperthermia, muscle rigidity, instability of autonomic functions, impaired consciousness and increased level of creatine phosphokinase), thermoregulatory disorders and epileptic seizures.
From the digestive system: constipation, dyspepsia, nausea or vomiting, abdominal pain, increased activity of "liver" transaminases, dry mouth, hypo- or hypersalivation, anorexia and / or increased appetite, weight gain or loss.
From the cardiovascular system: sometimes orthostatic hypotension, reflex tachycardia, or increased blood pressure.
From the hematopoiesis: neutropenia, thrombocytopenia.
From the endocrine system: galactorrhea, gynecomastia, menstrual irregularity, amenorrhea, weight gain, hyperglycemia and exacerbation of pre-existing diabetes.
From the genitourinary system: priapism, erectile dysfunction, ejaculation disorders, anorgasmia, urinary incontinence.
Allergic reactions: rhinitis, rash, angioedema, photosensitivity.
From the skin: dry skin, hyperpigmentation, itching, seborrhea.
Other: arthralgia.

Overdose:Symptoms: drowsiness, sedation, depression, tachycardia, arterial hypotension, extrapyramidal disorders, in rare cases, prolongation of the QT interval. Treatment: it is necessary to ensure free airway patency to ensure adequate oxygenation and ventilation, gastric lavage (after intubation, if the patient is unconscious) and the appointment of activated carbon in combination with laxatives. Symptomatic therapy aimed at maintaining vital body functions.
For timely diagnosis of possible cardiac arrhythmias, it is necessary to begin monitoring ECG as soon as possible. Careful medical observation and ECG monitoring is performed until the symptoms of intoxication disappear completely. There is no specific antidote.

Interaction:Given that risperidone has an effect primarily on the central nervous system, it should be used with caution in combination with other drugs of central action and with alcohol.
Risperidone reduces the effectiveness of levodopa and other dopamine agonists.
Clozapine reduces the clearance of risperidone.
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.
Phenothiazines, tricyclic antidepressants and some P-blockers may increase plasma concentrations of risperidone, but this does not affect the concentration of the active antipsychotic fraction.
Fluoxetine can increase the concentration of risperidone in the plasma, but to a lesser extent the concentration of the active antipsychotic fraction, so the dosage of risperidone should be adjusted.
With the use of risperidone, along with other drugs that bind highly to plasma proteins, there is no clinically significant displacement of any drug from the plasma protein fraction.
Hypotensive drugs increase the severity of lowering blood pressure in the background of risperidone.

Special instructions:Transition from therapy with other antipsychotic drugs. In schizophrenia, at the beginning of risperidone treatment, it is recommended that the previous therapy be gradually phased out if clinically justified. If patients are transferred from depot therapy to forms of antipsychotics, then risperidone should be taken instead of the next scheduled injection. Periodically, the need to continue therapy with antiparkinsonian drugs should be evaluated.
In connection with the α-adrenoblocking action of risperidone, orthostatic hypotension may occur, especially during the initial dose selection. If hypotension occurs, consider lowering the dose. In patients with diseases of the cardiovascular system, as well as with dehydration, hypovolemia or cerebrovascular
violations, the dose should be increased gradually, according to the recommendations (see Dosage and Administration).
The occurrence of extrapyramidal symptoms is a risk factor for the development of tardive dyskinesia.In case of signs and symptoms of tardive dyskinesia, consideration should be given to the abolition of all antipsychotics. If neuroleptic malignant syndrome characterized by hyperthermia, muscle rigidity, instability of autonomic functions, impaired consciousness and increased levels of creatine phosphokinase, all antipsychotic medicines should be discontinued, including risperidone.
With the withdrawal of carbamazepine and other inducers of "liver" enzymes, the dose of risperidone should be reduced.
Patients should be advised to refrain from overeating due to the possibility of weight gain.

Effect on the ability to drive transp. cf. and fur:During treatment, it is necessary to refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions, as well as on the intake of alcohol.

Form release / dosage:Tablets, film-coated, 2 mg and 4 mg.

Packaging:For 10 tablets per blister (PVC / PVDC / aluminum foil). For 1 or 2 blisters together with instructions for use in a cardboard box.

Storage conditions:At a temperature of no higher than 25 ° C.Keep out of the reach of children!

Shelf life:3 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-000313

Date of registration:07.04.2010 / 13.03.2014

Expiration Date:Unlimited

The owner of the registration certificate:Actavis PTS ehf GroupActavis PTS ehf Group Iceland

Manufacturer: & nbsp

ACTAVIS, Ltd. Iceland

Representation: & nbspACTAVIS GROUP AO ACTAVIS GROUP AO Iceland

Information update date: & nbsp2016-12-20

Illustrated instructions

Instructions

Speridan® (Speridan®)