Description
Release form
lozenges
Packing
30 pcs.
Pharmacological action
Torendo Ku-tab – antipsychotic drug (antipsychotic).
Pharmacodynamics
Risperidone is an antipsychotic, also has a sedative, antiemetic and hypothermic effect. Risperidone is a selective monoaminergic antagonist with a pronounced affinity for serotonergic 5-HT2 and dopaminergic D2 receptors, it also binds to alpha1-adrenergic receptors and, with a slightly lower affinity, to H1-histaminergic and alpha2-adrenergic receptors. It has no tropism for cholinergic receptors.
Antipsychotic effect due to blockade of dopamine D2 receptors of the mesolimbic and mesocortical system.
Sedative effect is due to blockade of adrenoreceptors of the reticular formation of the brain stem antiemetic – blockade of the dopamine receptors of the trigger zone of the vomiting center hypothermic effect – blockade of the dopamine receptors of the hypothalamus.
Reduces productive symptoms (delirium, hallucinations), automatism. It causes less suppression of motor activity and to a lesser extent induces catalepsy than classical antipsychotics (antipsychotics).
Balanced central antagonism of serotonin and dopamine may reduce the risk of extrapyramidal symptoms.
Risperidone may cause a dose-dependent increase in plasma prolactin concentrations.
Pharmacokinetics
When taken orally, risperidone is completely absorbed (regardless of food intake) and plasma Cmax levels are observed after 1 2 hours.
Risperidone is metabolized by cytochrome P450 2D6 to form 9-hydroxy risperidone, which has a similar pharmacological effect .
Risperidone and 9-hydroxy-risperidone are an effective antipsychotic fraction. Further risperidone metabolism is N-dealkylation. When ingested, risperidone is excreted with T1 / 2 for about 3 hours.
It has been found that T1 / 2 of 9-hydroxy-risperidone and the active antipsychotic fraction is 24 hours.
In most patients, an equilibrium concentration of risperidone is observed one day after the start of treatment. The equilibrium state of 9-hydroxy-risperidone in most cases is achieved 3-4 days after the start of treatment.
The concentration of risperidone in plasma is proportional to the dose of the drug (within therapeutic doses).
Risperidone is rapidly distributed in the body. The volume of distribution is 1 2 l / kg. In plasma, risperidone is bound to albumin and acidic alpha1-glycoprotein. The risperidone fraction, which is bound by the plasma protein, is 88% and, in the case of 9-hydroxy risperidone, 77%.
It is excreted by the kidneys – 70% (of which 35 45% in the form of a pharmacologically active fraction) and 14% – with bile. With a single dose, there are high levels of active plasma concentrations and slow elimination in elderly patients and patients with insufficient renal function.
Indications
– Acute and chronic schizophrenia and other psychotic conditions with productive and / or negative symptoms.
– Affective disorders in various mental illnesses.
– Behavioral disorders in patients with dementia with symptoms of aggressiveness (outbursts of anger, physical abuse), with mental disorders (agitation, delirium) or psychotic symptoms.
– As an adjunct therapy in the treatment of mania in bipolar disorders.
– As an adjunct therapy for behavioral disorders in adolescents from 15 years of age and adult patients with reduced intellectual level or mental retardation, in cases if destructive behavior (aggressiveness, impulsiveness, autoaggression) is leading in the clinical picture of the disease.
Contraindications
Lactation.
– Children and adolescents under 15 years of age (efficacy and safety not established).
– Hypersensitivity to the drug.
With caution, the drug should be used for diseases of the cardiovascular system (chronic heart failure, myocardial infarction, impaired conduction of the heart muscle), dehydration and hypovolemia, impaired cerebral circulation, Parkinson’s disease, seizures (including a history), severe renal or hepatic insufficiency, drug abuse or drug dependence, conditions predisposing to the development of pirouette type tachycardia (bradycardia, electrolyte imbalance, concomitant use of drugs that extend the QT interval), brain tumors, intestinal obstruction, in case of acute drug overdose, Reye’s syndrome (the antiemetic effect of risperidone can mask the symptoms of these conditions).
Pregnancy and lactation
The safety of risperidone during pregnancy has not been studied. The use of the drug during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus. Since risperidone and 9-hydroxy-risperidone are excreted in breast milk, if you need to use the drug during lactation, you should decide whether to stop breastfeeding.
Special instructions
With schizophrenia at the beginning of treatment with risperidone, it is recommended to gradually cancel the previous therapy, if it is clinically justified. If patients are transferred from therapy with depot forms of antipsychotic drugs, it is recommended that the use of risperidone be started instead of the next planned injection. Periodically, the need to continue therapy with potivoparkinsonian drugs should be assessed. In connection with the A-adrenergic blocking effect of risperidone, orthostatic hypotension may occur, especially during the initial dose selection. If arterial hypotension occurs, consider reducing the dose. In patients with diseases of the cardiovascular system, as well as with dehydration, hypovolemia or cerebrovascular disorders, the dose should be increased gradually, as recommended. The occurrence of extrapyramidal symptoms is a risk factor for the development of tardive dyskinesia. If signs and symptoms of tardive dyskinesia occur, consideration should be given to canceling all antipsychotic drugs. When a neuroleptic malignant syndrome occurs, characterized by hypertension, muscle rigidity, instability of autonomous functions, impaired consciousness and an increase in the level of CPK, all antipsychotic drugs, including risperidone, must be canceled. With the abolition of carbamazepine and other inducers of hepatic enzymes, the dose of risperidone should be reduced. Patients should refrain from overeating due to the possibility of increasing body weight. The use of the drug in children under the age of 15 years is not recommended. During treatment, it is necessary to refrain from engaging in potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions, as well as from drinking alcohol (ethanol).
Side effects of
From the side of the central nervous system and peripheral nervous system: insomnia, agitation, anxiety, headache sometimes – drowsiness, increased fatigue, dizziness, impaired concentration, blurred vision rarely – extrapyramidal symptoms (tremor, rigidity, hypersalivation, brachysis, hypersalivation, acute dystonia), mania or hypomania, stroke (in elderly patients with predisposing factors), as well as hypervolemia (due to polydipsia or syndrome of inadequate secretion of antidiuretic hormone), tardive dyskinesia (involuntary rhythmic movements of the tongue and / or face), neuroleptic malignant syndrome (hyperthermia, muscle rigidity, instability of autonomic functions, impaired consciousness and increased level of CPK) , thermoregulatory disorders and epileptic seizures.
From the digestive system: constipation, dyspepsia, nausea or vomiting, abdominal pain, increased activity of hepatic transaminases, dry mouth, hyposalivation or hypersalivation, anorexia and / or increased appetite, increased or decreased body weight.
From the cardiovascular system: sometimes – Orthostatic hypotension, reflex tachycardia, increased blood pressure.
From the endocrine system: galactorrhea, gynecomastia, menstrual irregularities, amenorrhea, weight gain, hyperglycemia, exacerbation of preexisting diabetes mellitus.
From the reproductive system: priapism, impaired erection, impaired ejaculation, anorgasmia.
From the hemopoietic system: neutropenia, thrombocytopenia.
Dermatological reactions: dry skin, hyperpigmentation, itching, seborrhea.
Allergic reactions: rhinitis, rash, angioedema, photosensitivity.
Other: arthralgia, urinary incontinence.
Drug Interactions
Since risperidone has an effect primarily on the central nervous system, it should be used with caution in combination with other centrally acting drugs and ethanol. Risperidone decreases the effectiveness of levodopa and other dopamine agonists. Clozapine reduces the clearance of risperidone. When using carbamazepine, a decrease in the concentration of the active antipsychotic fraction of risperidone in plasma was noted. Similar effects can be observed when using other inducers of hepatic enzymes. Phenothiazines, tricyclic antidepressants and some A-blockers can increase plasma risperidone concentrations, 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 dose of risperidone should be adjusted. With the simultaneous use of risperidone with drugs that bind to plasma proteins to a high degree, there is no clinically pronounced displacement of any drug from the protein fraction of plasma. Antihypertensive drugs increase the severity of lowering blood pressure on the background of risperidone.
Overdose
Symptoms: drowsiness, sedation, depression of consciousness, tachycardia, hypotension, extrapyramidal disorders, in rare cases prolongation of the QT interval.
Treatment: It is necessary to ensure the free passage of the respiratory tract to ensure adequate oxygenation and ventilation, gastric lavage (after intubation if the patient is unconscious) and the appointment of activated charcoal in combination with laxatives. Symptomatic therapy aimed at maintaining vital functions of the body. To timely diagnose possible heart rhythm disorders, ECG monitoring should be started as soon as possible. Careful medical monitoring and ECG monitoring are carried out until the symptoms of intoxication disappear. There is no specific antidote.
Storage conditions
The product should be stored out of the reach of children at a temperature not exceeding 30 ° C.
Shelf life
3 years.
Deystvuyushtee substance
Risperidone
Terms and conditions
prescription
Dosage Form
resorption tablets
KRKA d.d. Novo mesto AO, Slovenia
