Risdonal, pills 2mg, 20pcs

Composition

1 film-coated tablet contains:

• active ingredients:
• risperidone 2 mg;
• excipients:
• calcium hydrophosphate dihydrate,
• povidone (plasdon K 29/32 or collidone 30),
• pregelatinized starch (C*Pharm starch),
• magnesium stearate,
• microcrystalline cellulose;
• film shell composition:  selecoate AQ-02003 (hypromellose 2910 (hydroxypropyl-methylcellulose 2910), macrogol-6000 (polyethylene glycol 6000), titanium dioxide).

Pharmacological action

Risdonal – hypothermic, sedative, antiemetic, antipsychotic.

Pharmacodynamics

It also binds to α1-adrenergic receptors and, with a slightly lower affinity, to H1-histaminergic and α2-adrenergic receptors. It has no tropicity to cholinergic receptors. The antipsychotic effect is due to the blockade_{of dopamine D2}-receptors of the mesolimbic and mesocortical systems. Sedative effect is caused by blockade of adrenoreceptors of the reticular formation of the brain stem; antiemetic effect — blockade_{of dopamine D2}-receptors of the trigger zone of the emetic center; hypothermic effect — blockade of dopamine receptors of the hypothalamus. Reduces productive symptoms (delusions, hallucinations), automatism. It causes less suppression of motor activity and induces catalepsy to a lesser extent than classical antipsychotics (neuroleptics). Balanced central antagonism to 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_cmax in blood plasma is observed after 1-2 hours. Risperidone undergoes metabolism with the participation of cytochrome P450 IID6 to form 9-hydroxyrisperidone, which has a similar pharmacological effect. Risperidone and 9-hydroxyrisperidone represent an effective antipsychotic fraction. Further metabolism of risperidone involves N-dealkylation. When taken orally, risperidone is excreted with T_1/2 at about 3 hours, it was found that the dose_{of 1/2} 9-hydroxyrisperidone is 24 hours. In most patients, the steady-state concentration of risperidone is observed 1 day after the start of treatment. In most cases, the equilibrium state of 9-hydroxyrisperidone is 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 acid alpha_-1-glycoprotein. The plasma protein bound fractions of risperidone and 9-hydroxyrisperidone are 88% and 77%, respectively. Excreted by the kidneys-70% (including 35-45% in the form of a pharmacologically active fraction) and with bile-14%. With a single dose, high levels of the active antipsychotic fraction in plasma and slow elimination are observed in elderly patients and patients with insufficient renal function.

Indications

• Schizophrenia (acute and chronic) and other psychotic states with productive and / or negative symptoms.
• Affective disorders in various mental illnesses.
• Behavioral disorders in dementia patients with aggressive symptoms (outbursts of anger, physical violence), mental disorders (agitation, delirium), or psychotic symptoms.
• As an adjunct therapy in the treatment of mania in bipolar disorders.
• As an adjunctive therapy for behavioral disorders in adolescents from 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.

Contraindications

• Hypersensitivity to the components of the drug, lactation period.

With caution:  diseases of the cardiovascular system (chronic heart failure, previous myocardial infarction, cardiac muscle conduction disorders); dehydration and hypovolemia; cerebral circulation disorders; Parkinson’s disease; seizures (including in the anamnesis); severe renal or hepatic insufficiency (see dosage recommendations); substance abuse Dosage recommendations); conditions predisposing to the development of pirouette-type tachycardia (bradycardia, electrolyte imbalance, concomitant use of drugs that prolong the QT interval); brain tumor, intestinal obstruction, cases of acute drug overdose, Reye’s syndrome (the antiemetic effect of risperidone may mask the symptoms of these conditions); pregnancy, children under 15 years of age (efficacy and safety have not been established).

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 elderly patients with predisposing factors), as well as hypervolemia (either due to polydipsia or due to-for the syndrome of inadequate secretion ADH), tardive dyskinesia (involuntary rhythmic movements mainly of the tongue and/or face), neuroleptic malignant syndrome (hyperthermia, muscle rigidity, instability of autonomous functions, impaired consciousness and increased creatine phosphokinase levels), thermoregulation disorders and epileptic seizures.

From the digestive system:  constipation, dyspepsia, nausea or vomiting, abdominal pain, increased activity of hepatic transaminases, dry mouth, hypo – or hypersalivation, anorexia and / or increased appetite, increased or decreased body weight.

From the cardiovascular system:  sometimes-orthostatic hypotension, reflex tachycardia or increased blood pressure.

From the side of hematopoietic organs:  neutropenia, thrombocytopenia.

From the endocrine system:  galactorrhea, gynecomastia, menstrual disorders, amenorrhea, weight gain, hyperglycemia, and exacerbation of pre-existing diabetes mellitus.

From the genitourinary system:  priapism, erectile dysfunction, ejaculation disorder, anorgasmia, urinary incontinence.

From the side of the skin:  dry skin, hyperpigmentation, itching, seborrhea.

Allergic reactions:  rhinitis, rash, angioedema, photosensitivity.

Other services:  arthralgia.

Interaction

Taking into account the fact 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 using carbamazepine, there was a decrease in the concentration of the active antipsychotic fraction in plasma (similar effects can be observed when using other inducers of liver enzymes).

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

Fluoxetine may increase the plasma concentration of risperidone and, to a lesser extent, the concentration of the active antipsychotic fraction, so risperidone doses should be adjusted.

When using risperidone together with other drugs that are highly bound to plasma proteins, clinically expressed displacement of any drug from the plasma protein fraction is not observed.

Antihypertensive drugs Drugs increase the severity of the decrease HELL on the background of risperidone.

How to take, course of use and dosage

Inside.

Schizophrenia. Adults and children over 15 years of age: 1 or 2 times a day. The initial dose is 2 mg / day, on the second day the dose should be increased to 4 mg / day. From this point on, the dose can either be kept at the same level, or individually adjusted if necessary. Usually the optimal dose is 4-6 mg / day. In some cases, a slower increase in the dose and lower initial and maintenance doses may be justified. Doses higher than 10 mg / day have not been shown to be more effective than lower doses and may cause extrapyramidal symptoms. Due to the fact that the safety of doses above 16 mg/day has not been studied, doses above this level should not be used. There is no information on use for the treatment of schizophrenia in children under 15 years of age.

Elderly patients and patients with liver and kidney diseases: the initial dose is 0.5 mg taken 2 times a day. The dosage can be individually increased to 1-2 mg 2 times a day.

Abuse Drugs or drug dependence: the recommended daily dose is 2-4 mg.

Behavioral disorders in patients with dementia:  the initial dose is 0.25 mg 2 times a day. If necessary, the dosage can be individually increased by 0.25 mg 2 times a day, no more than every other day. For most patients, the optimal dose is 0.5 mg 2 times a day. However, some patients are shown to take 1 mg 2 times a day. When the optimal dose is reached, it may be recommended to take the drug 1 time a day.

Mania in bipolar disorders: The recommended starting dose is 2 mg per day in 1 dose. If necessary, this dose can be increased by 2 mg per day, no more than every other day. For most patients, the optimal dose is 2-6 mg / day.

Behavioral disorders in patients with mental retardation. Patients with a body weight of 50 kg or more: the recommended initial dose is 0.5 mg once a day. If necessary, this dose can be increased by 0.5 mg per day, no more than every other day. For most patients, the optimal dose is 1 mg per day. However, some patients prefer to take 0.5 mg per day, while others need to increase the dose to 1.5 mg per day.

Patients with a body weight of less than 50 kg: the recommended initial dose is 0.25 mg once a day. If necessary, this dose can be increased by 0.25 mg per day, no more than every other day. For most patients, the optimal dose is 0.5 mg per day. However, for some patients, a dose of 0.25 mg per day is preferable, while some require an increase in the dose to 0.75 mg per day.

Long-term use of Risdonal in adolescents should be carried out under the constant supervision of a doctor.

Use in children under 15 years of age is not recommended.

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 free airway patency for 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 body functions.

For timely diagnosis of possible cardiac arrhythmias, it is necessary to start ECG monitoring as soon as possible. Careful medical monitoring and ECG monitoring are performed until the symptoms of intoxication completely disappear. There is no specific antidote.

Special instructions

Transition from therapy with other antipsychotic drugs. In schizophrenia, at the beginning of treatment with risperidone, it is recommended to gradually cancel the previous therapy, if this is clinically justified. If patients are being transferred from depot therapy with forms of antipsychotic drugs, it is recommended to start taking risperidone instead of the next scheduled injection. Periodically, the need to continue therapy with Antiparkinsonian drugs should be evaluated.

Due to the alpha-blocking effect of risperidone, orthostatic hypotension may occur, especially during the initial dose selection period. If hypotension occurs, a dose reduction should be considered. In patients with diseases of the cardiovascular system, as well as with dehydration, hypovolemia or cerebrovascular disorders, the dose should be increased gradually, according to the recommendations (see “Dosage and use”).

The occurrence of extrapyramidal symptoms is a risk factor for the development of tardive dyskinesia. If signs and symptoms of tardive dyskinesia occur, discontinuation of all antipsychotic medications should be considered. If a neuroleptic malignant syndrome occurs, characterized by hyperthermia, muscle rigidity, instability of autonomous functions, impaired consciousness, and increased creatine phosphokinase levels, all antipsychotic drugs, including risperidone, should be discontinued.

When carbamazepine and other inducers of liver enzymes are discontinued, the risperidone dose should be reduced.

Patients should refrain from overeating due to the possibility of weight gain.

During treatment, it is necessary to refrain from engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions, as well as from taking alcohol.

Composition

Tablet Form of production

Storage conditions

In a dark place, at a temperature of 15-25 °C

Shelf life

3 years

Active ingredient

Risperidone

Conditions of release from pharmacies

By prescription

Dosage form

Tablets