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, aggressiveness), automatism. It causes minimal suppression of motor activity and to a lesser extent induces catalepsy than classic antipsychotics (neuroleptics). Balanced andriol cycle 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 a P-450 cytochrome to form a 9-hydroxyrisperidone which has a similar pharmacological action. Risperidone and 9-hydroxyrisperidone is an effective antipsychotic fraction.
Ingestion risperidone derived from a half-life of 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 (the therapeutic dose within).
Risperidone is distributed quickly in the body. Volume of distribution is 1 to 2 L / kg. The risperidone binds to plasma albumin and a-1-glycoprotein. Risperidone Plasma protein binding is 88%, 9-hydroxyrisperidone -77%.
Displayed buds – 70% (of which 35 – 45% as the pharmacologically active fraction) and 14% – with bile. The balance of the account for inactive metabolites.
Elderly patients after a single dose andriol cycle of the drug inside the observed increase in the concentration of the active fraction in the plasma of up to 30%, and in patients with renal failure – up to 60%, and reduced clearance of antipsychotic fraction.
The presence of hepatic insufficiency is not affected maintenance of plasma concentrations of risperidone, but the average number of patients free fraction was 35% higher than in plasma.
- schizophrenia (acute and chronic) and other psychotic states with a predominance of positive symptoms (delusions, hallucinations, aggressiveness), negative symptoms (poverty of speech, emotional and social detachment);
- affective disorders in a variety of mental disorders;
- behavioral disturbances in patients with dementia with aggressive manifestation of symptoms (angry outbursts, physical violence), activity in disorders (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. Precautions :
- disease cardiovascular (chronic heart failure, myocardial infarction, conduction disorders of the heart muscle);
- Dehydration and hypovolemia;
- cerebrovascular accident;
- Parkinson’s disease;
- seizures (including history);
- severe renal or hepatic insufficiency (see dosing recommendations.);
- the abuse of drugs or drug dependence (see dosing recommendations.);
- conditions that predispose to the development of tachycardia type “pirouette” (bradycardia, electrolyte imbalance, concomitant andriol cycle drugs, prolonging the interval QT);
- 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).
Application of pregnancy and lactation.
The safety of risperidone 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-hydroxyrisperidone into breast milk, women using the drug should not breast-feed.
DOSAGE AND ADMINISTRATION
Rispaksol can be taken during meals or between meals; Tablets can be washed down with a little water. Schizophrenia Adults 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 for the treatment of schizophrenia in children younger than 15 years, no. Elderly patients . It is recommended initial dose of 0.5 mg twice a reception day.The dosage can be individually increased by 0.5 mg twice a day for 1 -. 2 mg twice daily, liver and kidney disease . It is recommended initial dose of 0.5 mg to receiving two times a day. This dose can be gradually increased to 1 -. 2 mg for administration twice a day drug abuse or drug dependency -Recommended daily dose -. 2.4 mg . Behavioral disturbances in patients with dementia recommended starting dose of 0.25 mg per reception twice daily (adequate dosage form should be used). If necessary dosage can be individually increased by 0.25 mg 2 times a day, no more than a day. For most patients, the optimal dose is 0.5 mg twice a day. However, some patients are shown receiving 1 mg 2 times a day. On reaching the optimum dose of the drug can be recommended once daily.
Mania in bipolar disorderrecommended initial dose – 2 mg per day in one portion. If necessary, this dose may be increased to 2 mg per day, no more than a day. For most patients the optimal dose is 2 – 6 mg per day. Conduct disorders in patients with mental retardation patients weighing 50 kg or more – the recommended initial dose – 0.5 mg once daily. If necessary, this dose may be increased to 0.5 mg per day, no more than a day. For most patients, the optimal dose is 1 mg per day. However, andriol cycle preferred for some patients receiving 0.5 mg per day, whereas some require increasing doses up to 1.5 mg per day. Patients weighing less than 50 kg – recommended initial dose – 0.25 mg once daily. If necessary, this dose may be increased by 0.25 mg per day, no more than a day. For most patients, the optimal dose is 0.5 mg per day.However, for some patients preferred receiving 0.25 mg daily, whereas some require increasing the dose to 0.75 mg per day. Long-term use of risperidone in adolescents should be carried out under the constant supervision of a doctor. Use in children under 15 years is not recommended. Running low dose t3 clen cycle trying to lose bodyfat isn’t a real hot idea imo.