Risperidone, pills 2mg, 20pcs

Composition

Active ingredient:  

risperidone 2 mg;

Excipients:

calcium hydrophosphate dihydrate,

povidone (plasdon K 29/32 or collidone 30),

pregelatinized starch (C*Pharm starch),

magnesium stearate,

microcrystalline cellulose;

Composition of the film shell:

selecoate AQ-02003 (hypromellose 2910 (hydroxypropyl-methylcellulose 2910), macrogol-6000 (polyethylene glycol 6000), titanium dioxide).

Pharmacological action

Risperidone is an antipsychotic (neuroleptic) drug derived from benzisoxazole. It also has a sedative effect. antiemetic and hypothermic effects. Selective monoaminergic antagonist, has a high tropicity to serotonergic 5-HT2 and dopaminergic D2 receptors. It also binds to alpha-1-adrenergic receptors with a slightly lower affinity for H1-histaminergic and alpha-2-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 emetic center’s trestern zone; hypothermic effect – blockade of dopamine receptors of the hypothalamus.

Suppresses productive symptoms (delusions, hallucinations, aggressiveness), automatism. It causes less suppression of motor activity and induces catalepsy to a lesser extent than classical antipsychotic drugs (neuroleptics). Balanced central antagonism to serotonin and dopamine can reduce the tendency to extrapyramidal side effects and expand the therapeutic effect of the drug to cover the negative and affective symptoms of schizophrenia. May induce a dose-dependent increase in plasma prolactin concentrations.

Pharmacokinetics

Absorption is fast and complete. Food does not affect the fullness and speed of absorption. TCmax of risperidone is 1 h,9-hydroxyrisperidone is 3 h (with high activity of the CYP2D6 isoenzyme) and 17 h (with low activity of the CYP2D6 isoenzyme). Plasma concentrations of risperidone are proportional to the dose of the drug. The equilibrium concentration of risperidone in most patients is reached within 1 day,9-hydroxy-risperidone-after 4-5 days.

Risperidone is rapidly distributed in the body. Penetrates the central nervous system (CNS), breast milk. The volume of distribution is 1-2 l / kg. The binding to plasma proteins (alpha-1-acid glycoprotein and albumin) of risperidone is 90%, and that of 9-hydroxyrisperidone is 77%.

It is metabolized by the CYP2D6 isoenzyme to the active metabolite-9-hydroxyrisperidone (risperidone and 9-hydroxyrisperidone make up the active antipsychotic fraction). Another route of risperidone metabolism is N-dealkylation. The elimination half-life of risperidone is 3 hours; that of 9-hydroxyrisperidone and the active antipsychotic fraction is 20-24 hours. It is excreted by the kidneys (70%: 35-45% of them-in the form of a pharmacologically active fraction) and by the intestines (14%).

The study of a single dose of the drug revealed a higher concentration in blood plasma and slower elimination in elderly patients and in patients with renal insufficiency. Elimination is delayed in elderly patients and in patients with renal insufficiency.

In patients with hepatic insufficiency, the content of risperidone in plasma increases by 35%.

Indications

• schizophrenia (acute and chronic) and other psychotic States with productive and/or negative symptoms;
• affective disorders with various mental disorders,
• behavioral disorders in patients with dementia in the manifestation of symptoms of aggression (angry outbursts, physical violence), disorders of mental activity (agitation, delirium) or psychotic symptoms;
• as adjunctive therapy in the treatment of mania in bipolar disorders;
• as adjunctive therapy for behavioral disorders in adolescents 15 years and adult patients with reduced intellectual level or retardation, in cases if destructive behavior (aggressiveness, impulsivity, autoaggression) is leading to the clinical picture of the disease.

Contraindications

• hypersensitivity;
• lactation period;
• children’s age (up to 15 years) – efficacy and safety have not been established.

With caution:  it is used for brain tumors, intestinal obstruction, drug overdose, Reye’s syndrome (the antiemetic effect of risperidone can mask the symptoms of these conditions), diseases of the cardiovascular system (chronic heart failure, atrioventricular block, myocardial infarction), dehydration, circulatory disorders, hypovolemia, Parkinson’s disease, seizures (including in the anamnesis), drug abuse, drug dependence, severe renal failure severe hepatic insufficiency, conditions predisposing to the development of pirouette-type tachycardia (bradycardia, electrolyte imbalance, concomitant use of drugs that prolong the QT interval), pregnancy.

Side effects

From the central nervous system:  insomnia, restlessness, anxiety, headache, drowsiness, increased fatigue, dizziness, decreased ability to concentrate, blurred vision, extrapyramidal symptoms (tremor, rigidity, hypersalivation, bradykinesia, akathisia, acute dystonia), mania or hypomania, stroke (in elderly patients with predisposing factors). In patients with schizophrenia-hypervolemia (either due to polydipsia or due to the syndrome of inadequate secretion of antidiuretic hormone), 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 activity of creagine phosphokinase), thermoregulation disorders, epileptic seizures.

From the digestive system:  constipation, dyspepsia, nausea or vomiting, abdominal pain, increased activity of “liver” transaminases, dry mouth, hyposalivation or hypersalivation, anorexia.

From the cardiovascular system:  orthostatic hypotension, reflex tachycardia, or increased blood pressure (BP ).

From the side of hematopoietic organs:  neutropenia, thrombocytopenia.

From the endocrine system:  galactorrhea, gynecomastia, menstrual disorders, amenorrhea, increased or decreased body weight, hyperglycemia, or exacerbation of pre-existing diabetes mellitus.

From the genitourinary system:  priapism, erectile dysfunction, ejaculation disorders, orgasmic disorders, including anorgasmia, urinary incontinence.

Allergic reactions:  pruritus, rash, angioedema.

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

Other services:  arthralgia, rhinitis.

Interaction

Risperidone reduces the effectiveness of levodopa and dopamine agonists. Phenothiazines, tricyclic antidepressants and beta-blockers increase the concentration of risperidone in plasma (do not affect the concentration of the active antipsychotic fraction).

Concomitant use of carbamazepine and other inducers of microsomal enzymes is associated with a decrease in the concentration of the active antipsychotic fraction of risperidone in plasma. Clozapine reduces the clearance of risperidone.

When used concomitantly with risperidone ethanol, drugs that depress the central nervous system (CNS) lead to additive suppression of CNS function.

Antihypertensive drugs increase the severity of the decrease in blood pressure against the background of the use of risperidone.

Fluoxetine may increase the concentration of risperidone in plasma (to a lesser extent-its active antipsychotic fraction).

How to take, course of use and dosage

It is applied inside. Adults and children over 15 years of age are prescribed 1 or 2 times a day.

Schizophrenia. The initial dose is 2 mg per day. On day 2 – up to 4 mg per day. From this point on, if necessary, the dose can either be kept at the same level, or individually adjusted in the range of 4-6 mg per day.

Doses higher than 10 mg / day have not been shown to be more effective than lower doses and may cause extrapyramidal symptoms. The maximum daily dose is 16 mg.

Behavioral disorders in patients with dementia:  The optimal dose is 1 mg once a day.

Bipolar disorders in mania:  the initial dose is 2 mg per day for 1 reception. Increase the dose (by 2 mg per day) – no more than every other day. The optimal dose is 2-6 mg per day. Behavioral disorders in patients with mental retardation or with the predominance of destructive tendencies in the clinical picture. Patients with a body weight of 50 kg or more. The optimal dose is 1 mg per day.

It is recommended to reduce both the initial dose and subsequent dose increases by 2 times in elderly patients and in patients with renal or hepatic insufficiency (if necessary, use an adequate dosage form).

Overdose

Symptoms:  drowsiness, sedation, tachycardia, decreased blood pressure, extrapyramidal disorders, rarely-prolongation of the QT interval.

Treatment: ensure free airway patency to ensure adequate oxygen supply and ventilation, gastric lavage (after intubation, if the patient is unconscious) and taking activated charcoal along with a laxative. Start ECG monitoring immediately to detect possible arrhythmias.

There is no specific antidote. It is necessary to conduct symptomatic therapy aimed at maintaining the vital functions of the body. With a decrease in blood pressure and vascular collapse, intravenous infusion solutions and/or adrenostimulants should be administered. In case of acute extrapyramidal symptoms-anticholinergic drugs.

Continuous medical supervision and monitoring should be continued until the symptoms of intoxication disappear.

Special instructions

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 therapy with depo-forms of antipsychotic drugs, then it is recommended to start taking them instead of the next scheduled injection. Periodically, the need to continue current therapy with Antiparkinsonian drugs should be evaluated.

The risk of developing mania or hypomania can be significantly reduced by using low doses of risperidone or gradually increasing them. If orthostatic hypotension occurs, especially during the initial dose adjustment period, 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 of risperidone should be increased gradually. If signs and symptoms of tardive dyskinesia occur, discontinuation of all antipsychotic medications should be considered. In neuroleptic malignant syndrome, all antipsychotic medications, including risperidone, should be discontinued.

When carbamazepine and other microsomal enzyme inducers are discontinued, the risperidone dose should be reduced.

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

During the treatment period, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Composition

Tablet Form of production

Storage conditions

Store in a dry place protected from light at a temperature not exceeding 25°C.

Shelf life

2 years

Active ingredient

Risperidone

Conditions of release from pharmacies

By prescription

Dosage form

Tablets