Risperidone is an antipsychotic, also has a sedative, antiemetic and hypothermic effect. Risperidone is a selective monoaminergic antagonist with a pronounced affinity serotonergic and dopaminergic, also binds to alpha s and at slightly lower affinity and turinbol adrenergic receptors. It has no affinity for holinoretseptorami. Antipsychotic effect due to blockade of dopamine and Mesocortical mesolimbic system. Sedative effect due to blockade of adrenergic receptors of the reticular formation of the brain;antiemetic action – blockade of dopamine 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 serotonin antagonism of dopamine and may reduce the risk of extrapyramidal symptoms. Risperidone can cause dose-dependent increase in plasma prolactin concentrations.
Ingestion risperidone completely absorbed (regardless of the meal) and maximum levels of plasma concentration observed after 1-2 hours.
Risperidone is metabolized with cytochrome , which has a similar pharmacological action . Risperidone and 9-hydroxy-risperidone are effective antipsychotic fraction. Subsequent metabolism of risperidone . Ingestion risperidone is excreted in the half-life of about 3 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 in most cases achieved 3-4 days after initiation of treatment.
Risperidone plasma concentration of the drug dose proportional (within therapeutic doses).
Risperidone is distributed quickly in the body. The volume of distribution is 1-2 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-hydroxy-risperidone.
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.
- schizophrenia turinbol (acute and chronic) and other psychotic states with productive and / or negative symptoms;
- affective disorders in a variety of mental illnesses;
- behavioral disturbances in patients with dementia with aggressive manifestation of symptoms (angry outbursts, physical violence), 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.
: Hypersensitivity to the drug; lactation, children under 15 years of age (efficacy and safety have not been established). Precautions:
- Diseases of the 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 turinbol 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 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 and lactation. Risperidone safety in pregnant women has not been studied. If pregnancy can only be used if a positive effect justifies the potential risk.
Because risperidone and 9-hydroxy-risperidone passes into breast milk, women using the drug should not breast-feed.
Dosing and Administration Schizophrenia. Adults turinbol and children over 15 years. Risperidone can be administered once or twice a day. Initial dose – 2 mg per day. On the second day, the dose should be increased to 4 mg per day. From this point the dose can either maintain the same level, either individually adjusted if necessary. Typically, the optimal dose is 4.6 mg per day. In some cases it may be justified by a slower increase in the dose and lower initial and maintenance doses. Doses greater than 10 mg per day did not show a higher efficiency compared to lower doses and may cause the appearance of extrapyramidal symptoms. Due to the fact that the safety of doses above 16 mg per day has not been studied, doses above this level can not be used. For information on the use of a drug for the treatment of schizophrenia in children younger than 15 years no. Elderly patients. It is recommended initial dose of 0.5 mg per administration twice a day .