Torendo, 1 mg 20 pcs.

Torendo is an antipsychotic (neuroleptic).

Pharmacodynamics

Risperidone is an antipsychotic and also has sedative, antiemetic and hypothermic effects. Risperidone is a selective monoaminergic antagonist with strong affinity for serotonergic 5-HT2 and dopaminergic D2 receptors, it also binds to alpha1-adrenoceptors and with some less affinity for H1-histaminergic and alpha2-adrenergic receptors. It has no tropinity to cholinoreceptors.

The antipsychotic action is caused by blockade of dopamine D2-receptors of mesolimbic and mesocortical system.

Sedative action is caused by blockade of adrenoreceptors of reticular formation of brain stem; antiemetic action – by blockade of dopamine D2-receptors of trigger zone of vomiting center; hypothermic action – by blockade of dopamine receptors of hypothalamus.

Reduces productive symptomatology (delirium, hallucinations), automatism. Causes less suppression of motor activity and is less likely to induce catalepsy than classical antipsychotics (neuroleptics).
Balanced central antagonism to serotonin and dopamine may reduce the risk of extrapyramidal symptomatology.

Risperidone may cause a dose-dependent increase in plasma prolactin concentrations.

Pharmacokinetics

In oral administration, risperidone is completely absorbed (regardless of food intake) and maximum plasma concentrations are observed after 1-2 hours.

Risperidone is metabolized by P-450 IID6 cytochrome to form 9-hydroxy-risperidone, which has similar pharmacological effects. Risperidone and 9-hydroxy-risperidone constitute an effective antipsychotic fraction. The further metabolism of risperidone consists of N-dealkylation. When administered orally, risperidone is excreted with a half-life of about 3 hours. The half-life of 9-hydroxy-risperidone and the active antipsychotic fraction has been found to be 24 hours.

In most patients the equilibrium concentration of risperidone is observed one day after the start of treatment. The equilibrium state of 9-hydroxy risperidone is in most cases reached 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 alpha-1-glycoprotein. The fraction of risperidone that is bound to plasma protein is 88% and 77%, respectively, in the case of 9-hydroxy-risperidone.

It is excreted by the kidneys – 70% (of which 35-45% as pharmacologically active fraction) and 14% with the bile. In single administration high levels of active plasma concentrations and slow excretion in elderly patients and patients with insufficient renal function are noted.

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 aggression (outbursts of anger, physical violence), mental disturbances (agitation, delirium) or psychotic symptoms.

– As adjunctive therapy in the treatment of mania in bipolar disorders.

– As adjunctive therapy for conduct disorder in adolescents from 15 years of age and adult patients with reduced intellectual level or mental retardation, in cases where disruptive behavior (aggressiveness, impulsivity, autoaggression) is leading in the clinical picture of the disease.

Active ingredient

Composition

1 film-coated tablet contains:

active ingredient:

risperidone 1 mg.

excipients:

Cellactose*,

Microcrystalline cellulose,

croscarmellose sodium,

colloidal anhydrous silica,

sodium lauryl sulfate, magnesium stearate.

coating:

Opadray OZN28785 white**, iron oxide yellow dye E 172. *Cellactose is a spray-dried compound consisting of 75% alpha lactose monohydrate and 25% cellulose powder, dry matter ** Opadray OZN28785 is a finished mixture of hypromellose, titanium dioxide, talc, propylene glycol

.

How to take, the dosage

Schizophrenia.

Adults and children over 15 years of age. Risperidone may be prescribed once or twice daily. The initial dose is 2 mg per day. On the second day, the dose should be increased to 4 mg per day. From that point on, the dose can either be maintained 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 starting and maintenance doses may be warranted.
Doses above 10 mg per day have not been shown to be more effective than lower doses and may cause extrapyramidal symptoms. Because the safety of doses above 16 mg per day has not been studied, doses above this level should not be used.

There is no information on the use of the drug for the treatment of schizophrenia in children younger than 15 years of age.

Elderly patients. A starting dose of 0.5 mg per dose twice daily is recommended. The dosage can be individually increased from 0.5 mg twice daily to 1-2 mg twice daily.

Hepatic and renal diseases. A starting dose of 0.5 mg per dose twice daily is recommended. This dose can be gradually increased to 1-2 mg per dose twice a day.

Medication abuse or drug dependence – Recommended daily dose of the drug is 2-4 mg.

Behavioral disorders in patients with dementia.

The initial dose of 0.25 mg per dose twice daily is recommended (adequate dosage form should be used). The dosage can be increased individually at 0.25 mg twice daily if necessary, no more often than every other day. For most patients, the optimal dose is 0.5 mg twice a day. However, some patients are indicated to take 1 mg twice a day.

Once the optimal dose has been reached, once daily dosing may be recommended.

Mania in bipolar disorders

The recommended starting dose of Torendo is 2 mg daily at a single dose. If necessary, this dose can be increased by 2 mg per day, no 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 starting dose of the drug is 0.5 mg once daily. If necessary, this dose may be increased by 0.5 mg daily, no more often than every other day. For most patients, the optimal dose is 1 mg daily. However, some patients prefer to take 0.5 mg daily, while some need to increase the dose to 1.5 mg daily.

Patients weighing less than 50 kg – The recommended starting dose of Torendo is 0.25 mg once daily. If necessary, this dose may be increased by 0.25 mg daily, no more often than every other day. For most patients, the optimal dose is 0.5 mg daily. However, some patients prefer to take 0.25 mg daily, while others need to increase the dose to 0.75 mg daily.

Long-term administration of Risperidone in adolescents should be conducted under constant medical supervision.
Use in children younger than 15 years is not recommended.

Interaction

As risperidone primarily affects the CNS, it should be used with caution in combination with other centrally acting drugs and ethanol. Risperidone reduces the effectiveness of levodopa and other dopamine agonists. Clozapine reduces clearance of risperidone.

When using carbamazepine a decrease in the concentration of the active antipsychotic fraction of risperidone in plasma has been observed. Similar effects may be observed with other hepatic enzyme inducers. Phenothiazines, tricyclic antidepressants and some A-adrenoblockers may increase plasma concentrations of risperidone, but this does not affect the concentration of the active antipsychotic fraction. Fluoxetine may increase plasma concentrations of risperidone, but to a lesser extent the concentration of the active antipsychotic fraction, so doses of risperidone should be adjusted.

In concomitant use of risperidone with drugs that are highly bound to plasma proteins, clinically pronounced displacement of any drug from the plasma protein fraction is not observed. Hypotensive drugs increase the severity of BP reduction against risperidone.

Special Instructions

In schizophrenia, at the beginning of risperidone treatment, it is recommended that the previous therapy be gradually withdrawn if clinically justified.

If patients are transferred from therapy with depot forms of antipsychotic drugs, it is recommended that risperidone be started instead of the next scheduled injection. The need for continuation of therapy with antiparkinsonian medications should be periodically evaluated. Due to the A-adrenoblocking action of risperidone, orthostatic hypotension may occur, especially during initial dose adjustment. If arterial hypotension occurs, dose reduction should be considered. In patients with cardiovascular disease, as well as in 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 withdrawing all antipsychotic medications.

If neuroleptic malignant syndrome occurs, characterized by hypertension, muscle rigidity, autonomic instability, impaired consciousness, and elevated CPK levels, all antipsychotic medications, including risperidone, should be discontinued. If carbamazepine and other hepatic enzyme inducers are withdrawn, the dose of risperidone should be reduced.

Patients should refrain from overeating due to the possibility of weight gain. The use of the drug in children under the age of 15 years is not recommended. During the treatment it is necessary to refrain from potentially hazardous activities requiring high concentration and quick psychomotor reactions and from taking alcohol (ethanol).

Contraindications

Lactation period.
– Child and adolescent age under 15 years (effectiveness and safety has not been established).
– Hypersensitivity to the components of the drug.

With caution the drug should be used in case of cardiovascular diseases (chronic cardiac insufficiency, myocardial infarction, cardiac conduction disorders), dehydration and hypovolemia, stroke, Parkinson’s disease, seizures (including Parkinson’s disease, seizures (including history), severe renal or hepatic insufficiency, drug abuse or addiction, conditions predisposing to development of pirouette tachycardia (bradycardia, electrolyte imbalance, concomitant use of QT prolonging drugs), brain tumor, bowel obstruction, cases of acute drug overdose, Reye syndrome (antiemetic effect of risperidone may mask the symptoms of these conditions).

Side effects

Nervous system disorders: Insomnia, agitation, anxiety, headache, sometimes drowsiness, increased fatigue, dizziness, impaired concentration, blurred vision, rarely extrapyramidal symptoms (tremor, rigidity, hypersalivation, bradykinesia, akathisia, acute dystonia), mania or hypomania, stroke (in older patients with predisposing factors), and hypervolemia (either from polydipsia or due to inadequate antidiuretic hormone secretion syndrome), tardive dyskinesia (involuntary rhythmic movements primarily of the tongue and/or face), neuroleptic malignant syndrome (hyperthermia, muscle rigidity, instability of autonomic functions, impaired consciousness and increased creatine phosphokinase levels), thermoregulation disorders and epileptic seizures.

Digestive system disorders: 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.

Cardiovascular system: sometimes orthostatic hypotension, reflex tachycardia or increased blood pressure.

Hematopoietic disorders: neutropenia, thrombocytopenia.

Endocrine system disorders: galactorrhea, gynecomastia, menstrual cycle disorders, amenorrhea, weight gain, hyperglycemia and exacerbation of pre-existing diabetes.

Urogenital system disorders: priapism, erectile dysfunction, ejaculation disorders, anorgasmia, urinary incontinence.

Allergic reactions: rhinitis, rash, angioedema, photosensitization.

Skin disorders: dry skin, hyperpigmentation, itching, seborrhea.

Other: arthralgia.

Overdose

Symptoms: drowsiness, sedation, depression of consciousness, tachycardia, arterial hypotension, extrapyramidal disorders, in rare cases QT interval prolongation.

Treatment: ensure free airway patency to ensure adequate oxygenation and ventilation, gastric lavage (after intubation if the patient is unconscious) and administration of activated charcoal in combination with laxatives. Symptomatic therapy aimed at maintaining vital body functions. For timely diagnosis of possible cardiac rhythm disturbances, ECG monitoring should be started as soon as possible. Careful medical observation and ECG monitoring is carried out until the symptoms of intoxication have completely disappeared. There is no specific antidote.

Pregnancy use

The safety of risperidone in pregnant women has not been studied. It can be used in pregnancy only if the positive effect justifies the possible risk.

Because risperidone and 9-hydroxy-risperidone penetrate into breast milk, women using the drug should not breastfeed

Pregnant women should not breastfeed.

Similarities