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Active ingredients
Risperidone
Release form
Pills
Composition
Risperidone 4 mg; Excipients: Cellactose (75% alpha-lactose monohydrate, 25% cellulose powder) - 152.2 mg, microcrystalline cellulose - 41 mg, croscarmellose sodium - 8.4 mg, colloidal silicon dioxide - 0.7 mg, sodium lauryl sulfate - 2.1 mg, magnesium stearate - 1.6 mg; shell composition: Opadry 03Н28758 white - 6.99 mg (hypromellose 72%, titanium dioxide (E171) 16%, talc 7%, propylene glycol 5%), dye quinoline yellow (E104) - 0.008 mg, indigo carmine dye (E132) - 0.002 mg.
Pharmacological effect
An antipsychotic drug (neuroleptic); Risperidone is a selective monoaminergic antagonist with α-β affinity for serotonin 5-HT2 receptors and dopamine D2-receptors, also binds with 1-adrenergic receptors and, with slightly less affinity for histamine γ-β-β-α-adrenoreceptors, β-β-γ-receptor i -α-α-α-2 receptors. . Does not possess tropnost to cholinergic receptors. It also has a sedative, antiemetic and hypothermic effect. The antipsychotic effect is due to the blockade of the dopamine D2 receptors of the mesolimbic and mesocortical system. The sedative effect is due to the blockade of the adrenergic receptors of the reticular formation of the brain stem.; Hypothermic effect due to blockade of the dopamine receptors of the hypothalamus.; Reduces productive symptoms (delusions, hallucinac ii) automatism. It causes less suppression of motor activity and to a lesser extent induces catalepsy than classical antipsychotics (neuroleptics) .; Balanced central antagonism of serotonin and dopamine may reduce the risk of extrapyramidal symptoms.; Risperidone may cause a dose-dependent increase in plasma prolactin concentration.
Pharmacokinetics
Absorption; When ingestion, risperidone is completely absorbed (regardless of food intake) and Cmax in plasma is observed after 1-2 hours; Distribution; The concentration of risperidone in plasma is proportional to the dose of the drug (within therapeutic doses); Risperidone is rapidly distributed in the body. Vd is 1-2 l / kg. In plasma, risperidone binds to albumin and an acidic -1-glycoprotein.The plasma protein-bound fractions of risperidone and 9-hydroxy risperidone are 88% and 77%, respectively.; Metabolism; Risperidone undergoes metabolism with the participation of the CYP2D6 isoenzyme with the formation of 9-hydroxy-risperidone, which has similar pharmacological effects.; Risperidone and 9 -Hydroxy-risperidone is an effective antipsychotic fraction. The further metabolism of risperidone is N-dealkylation. When administered, risperidone is eliminated with a T1 / 2 of about 3 hours. T1 / 2 of 9-hydroxy-risperidone and the active antipsychotic fraction is 24 hours. In most patients, Css of risperidone is observed 1 day after the start of treatment. Css 9-hydroxy-risperidone in most cases is achieved 3-4 days after the start of treatment.; Excretion; Excreted in the urine -70% (of which 35-45% in the pharmacologically active fraction) and 14% in the bile. Pharmacokinetics in special clinical situations; Elderly patients or patients with insufficient kidney function with a single use of the drug have high levels of active substances in the plasma and their slow excretion.
Indications
- acute and chronic schizophrenia and other psychotic states with productive and / or negative symptoms; - affective disorders in various mental illnesses; - behavioral disorders in patients with dementia with symptoms of aggressiveness (outbreak of anger, physical violence), with mental disorders (agitation, delusions) or psychotic symptoms; - as an adjuvant therapy in the treatment of mania with bipolar disorders; - as an adjuvant therapy of behavioral disorders in adolescents from 15 years and adult patients with reduced intellectual level or mental retardation, in cases where destructive behavior (aggressiveness, impulsivity, auto-aggression) is leading in the clinical picture of the disease.
Contraindications
- lactation period; - children's and teenage age up to 15 years (efficiency and safety are not established); - Hypersensitivity to the components of the drug.; The drug should be used with caution in diseases of the cardiovascular system (chronic heart failure, myocardial infarction, conduction disturbances of the cardiac muscle), dehydration and hypovolemia, cerebral circulation disturbance, Parkinson's disease, convulsions (in t. ha history of severe renal or hepatic insufficiency, drug abuse or drug dependence, conditions predisposing to the development of pirouette type tachycardia (bradycardia, electrolyte imbalance, concomitant medication that prolong the QT interval), brain tumors, intestinal obstruction , in cases of acute drug overdose, Reye's syndrome (the antiemetic effect of risperidone may mask the symptoms of these conditions).
Use during pregnancy and lactation
The safety of using risperidone during pregnancy has not been studied.; Use of the drug in pregnancy is possible only when the intended benefit to the mother outweighs the potential risk to the fetus. Since risperidone and 9-hydroxy-risperidone are excreted in breast milk, if necessary, use the drug during lactation should decide whether to stop breastfeeding.
Dosage and administration
In schizophrenia; Adults and children over the age of 15 years, risperidone can be administered 1-2 times / day.; Initial dose - 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 maintained at the same level, or individually adjusted if necessary. Usually the optimal dose is 4-6 mg / day. In some cases, a slower dose increase and lower initial and maintenance doses may be justified. Doses> 10 mg / day did not show a higher efficacy compared to lower doses and may cause extrapyramidal symptoms. Due to the fact that the safety of the drug in doses> 16 mg / day has not been studied, doses above this level should not be used.; There is no information on the use of the drug for the treatment of schizophrenia in children under the age of 15 years old.; Elderly patients are recommended drug in the initial dose of 0.5 mg 2 times / day. The dose can be individually increased by 0.5 mg 2 times / day to 1-2 mg 2 times / day. For patients with liver and kidney diseases, it is recommended to use the drug in the initial dose of 0.5 mg 2 times / day. This dose can be gradually increased up to 1-2 mg 2 times / day; With drug abuse or drug dependence; The recommended daily dose is 2-4 mg. With behavioral disorders in patients with dementia; The recommended initial dose of the drug is 0.25 mg 2 times / day (in adequate dosage form).If necessary, the dose can be individually increased by 0.25 mg 2 times / day, not more often than every other day. For most patients, the optimal dose is 0.5 mg 2 times / day. Some patients showed the use of the drug in 1 mg 2 times / day. Once the optimal dose has been reached, the drug can be recommended once a day; Manias for bipolar disorders; The recommended initial dose of the drug is 2 mg / day at a time. If necessary, this dose can be increased by 2 mg / day, no more than a day. For most patients, the optimal dose is 2-6 mg / day; For behavioral disorders in patients with mental retardation; Patients with a body weight of ≥50 kg are recommended to use the drug in the initial dose of 0.5 mg 1 time / day. If necessary, this dose can be increased by 0.5 mg / day, no more than a day. For most patients, the optimal dose is 1 mg / day. However, for some patients, it is preferable to use 0.5 mg / day or increase the dose to 1.5 mg / day. For patients weighing ≤50 kg, use of the drug in the initial dose of 0.25 mg 1 time / day is recommended. If necessary, this dose can be increased by 0.25 mg / day, no more than every other day. For most patients, the optimal dose is 0.5 mg / day. However, for some patients, it is preferable to use 0.25 mg / day, or increase the dose to 0.75 mg / day; Long-term use of the drug Torendo; in adolescents should be under the constant supervision of a physician.; Use of the drug in children under the age of 15 years is not recommended.
Side effects
On the part of the central nervous system and peripheral nervous system: insomnia, agitation, anxiety, headache; sometimes - drowsiness, 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 (due to polydipsia or inadequate secretion of antidiuretic) tardive dyskinesia (involuntary rhythmic movements mainly of the tongue and / or face), ZNS (hyperthermia, muscle rigidity,autonomic instability, impaired consciousness and increased CPK), impaired thermoregulation and epileptic seizures. On the part of the digestive system: constipation, dyspepsia, nausea or vomiting, abdominal pain, increased liver transaminase activity, dry mouth, hypo-salivation or hypersalivation, anorexia and / or increased appetite, increase or decrease in body weight. From the side of the cardiovascular system: sometimes - orthostatic hypotension, reflex tachycardia, increased blood pressure. From the endocrine system: galactor I, gynecomastia, menstrual disorders, amenorrhea, weight gain, hyperglycemia, exacerbation of pre-existing diabetes mellitus. From the reproductive system: priapism, erectile dysfunction, impaired ejaculation, anorgasmia. Reactions: dry skin, hyperpigmentation, pruritus, seborrhea. Allergic reactions: rhinitis, rash, angioedema, photosensitization.; Other: arthralgia, urinary incontinence.
Overdose
Symptoms: drowsiness, sedation, depression of consciousness, tachycardia, arterial hypotension, extrapyramidal disorders, in rare cases lengthening of the QT interval. Treatment: it is necessary to provide free airway to ensure adequate oxygenation and ventilation, gastric lavage (after intubation, if the patient is without consciousness) and the appointment of activated carbon in combination with laxatives. Symptomatic therapy aimed at maintaining the vital functions of the body. To timely diagnose possible arrhythmias, it is necessary to start ECG monitoring as soon as possible. Careful medical observation and ECG monitoring is carried out until the symptoms of intoxication disappear. The specific antidote is absent.
Interaction with other drugs
Since risperidone has an effect primarily on the central nervous system, it should be used with caution in combination with other centrally acting drugs and ethanol.; Risperidone reduces the effectiveness of levodopa and other dopamine agonists. Clozapine reduces the clearance of risperidone. When using carbamazepine, a decrease in the concentration of active antipsychotic plasma fractions of risperidone.Similar effects can be observed with other hepatic enzyme inducers.; Phenothiazines, tricyclic antidepressants and some β-adrenergic blockers may increase plasma concentrations of risperidone, but this does not affect the concentration of active antipsychotic fraction.; Fluoxetine may increase plasma concentrations of risperidone, however the degree of concentration of the active antipsychotic fraction, so the dose of risperidone should be adjusted. With the simultaneous use of risperidone with drugs, highly associated with plasma proteins, there is no clinically pronounced displacement of any drug from the plasma protein fraction.; Antihypertensive drugs increase the severity of blood pressure reduction against the background of risperidone.
special instructions
For schizophrenia at the beginning of treatment with risperidone, it is recommended to gradually cancel the previous therapy, if it is clinically justified. If patients are transferred from treatment with depot forms of antipsychotic drugs, then it is recommended to start the use of risperidone instead of the next scheduled injection. Periodically, the need to continue therapy with antiparkinsonian drugs should be assessed.; In connection with the β-adreno-blocking effect of risperidone, orthostatic hypotension may occur, especially during the initial dose selection period. If arterial hypotension occurs, a dose reduction should be considered. In patients with diseases of the cardiovascular system, as well as dehydration, hypovolemia, or cerebrovascular disorders, the dose should be increased gradually, according to the recommendations. The occurrence of extrapyramidal symptoms is a risk factor for the development of tardive dyskinesia. When the signs and symptoms of tardive dyskinesia occur, the issue of abolishing all antipsychotic drugs should be considered. cancellation of carbamazepine and other hepatic enzyme inducers should lower the dose of risperidone.; Patients shouldrefrain from overeating due to the possibility of increasing body weight.; Use in pediatrics; Use of the drug in children under the age of 15 is not recommended.; Impact on ability to drive vehicles and control mechanisms; During treatment, it is necessary to refrain from practicing potentially hazardous activities , requiring increased concentration of attention and speed of psychomotor reactions, as well as alcohol intake (ethanol).