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Risperidone is an antipsychotic, also has a sedative, antiemetic and hypothermic effect. Risperidone is a selective monoaminergic antagonist with a pronounced affinity for 5-HT2 serotonergic and dopaminergic D2-receptor, also binds to a1-adrenoceptors and at slightly lower affinity H1-histaminergic and a2-adrenergic receptors. It has no affinity for holinoretseptorami.

Antipsychotic buy equipoise effect due to blockade of dopamine D2-receptor and Mesocortical mesolimbic system.

Sedative effect due to blockade of adrenergic receptors of the reticular formation of the brain; antiemetic action – blockade of dopamine D2-receptor trigger zone of the vomiting center; hypothermic action – blockade of dopamine receptors of the hypothalamus.

Reduces productive symptoms (delusions, hallucinations), automatism. It causes minimal suppression of motor activity and to a lesser extent induces catalepsy than classic antipsychotics (neuroleptics).

Balanced central antagonism of serotonin and dopamine may reduce the risk of extrapyramidal symptoms.

Risperidone can cause dose-dependent increase in plasma prolactin concentrations.

Pharmacokinetics
Ingestion risperidone completely absorbed (regardless of the meal) and the maximum levels in the blood plasma concentrations are observed within 1-2 hours. Risperidone buy equipoise is metabolized involving cytochrome P450 IID6 to form a 9-hydroxyrisperidone which has a similar pharmacological action. Risperidone and 9-hydroxyrisperidone is an effective antipsychotic fraction. Subsequent metabolism of risperidone is N-dealkylation. Ingestion risperidone is excreted in the period poluvy.chedeniya about 3 hours.

It is found that the half-life of 9-hydroxyrisperidone and the active antipsychotic fraction is 24 hours.

In most patients, the equilibrium concentration of risperidone is observed one day after the start of treatment. The equilibrium state of 9-hydroxyrisperidone in most cases is achieved after 3-4 days of treatment.

The concentration of risperidone in the plasma is proportional to the dose of the drug (in the range of therapeutic doses).

Risperidone is rapidly distributed in the body. volume of distribution is 1 to 2 L / kg. The risperidone plasma associated with albumin and alpha-1-acid glycoprotein. Fraction risperidone is associated plasma protein of 88% and 77%, respectively, in the case of 9-hydroxyrisperidone.

Excreted by the kidneys – 70% (35-45% of them as a pharmacologically active fraction) and 14% in the bile. In single dose have high levels of the active plasma concentrations and a slower elimination in elderly patients and patients with poor kidney function.

Indications

  • schizophrenia (acute and chronic) and other psychotic states with productive and / or negative symptoms;
  • affective disorders in a variety of mental disorders;
  • behavioral disturbances in patients with dementia with symptoms manifestation of aggressiveness (anger, physical abuse), disorders of mental activity (agitation, delirium) or psychotic symptoms;
  • as adjuvant therapy in the treatment of mania in bipolar disorder;
  • as adjunctive therapy of behavior disorders in adolescents from 15 years and adult patients with reduced intellectual level or mental retardation, in cases where destructive behavior (aggressiveness, impulsivity, autoaggression) is leading the clinical picture of the disease.

Contraindications
: Hypersensitivity to the drug; lactation.

Carefully:

  • Diseases of the buy equipoise cardiovascular system (chronic heart failure, myocardial infarction, conduction disorders of the heart muscle)
  • Dehydration and hypovolemia
  • cerebrovascular accidents
  • Parkinson’s disease
  • seizures (including history)
  • severe renal or hepatic insufficiency (see. dosing recommendations)
  • drug abuse or drug dependency (see. for dosage recommendations)
  • conditions that predispose to the development of tachycardia type “pirouette” (bradycardia, electrolyte imbalance, concomitant drugs prolonging the QT interval)
  • brain tumor, intestinal obstruction, acute cases of drug overdose, Reye’s syndrome (an antiemetic effect of risperidone may mask the symptoms of these conditions), pregnancy, children under 15 years (effectiveness and safety have been established).

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