Description
Latin name
Rispolept
packaging 20 pcs
Pharmacological action
Rispolept is an antipsychotic drug derived from benzisoxazole. It also has a sedative, antiemetic and hypothermic effect.
Risperidone is a selective monoaminergic antagonist with high affinity for serotonin 5-HT2 and dopamine D2 receptors. It binds to β1-adrenergic receptors and is somewhat weaker – to histamine H1 receptors and β2-adrenergic receptors. It has no tropism for cholinergic receptors.
Antipsychotic effect due to blockade of dopamine D2 receptors of the mesolimbic and mesocortical system. Sedative effect is due to blockade of adrenoreceptors of the reticular formation of the brain stem antiemetic effect – blockade of the dopamine D2 receptors of the trigger zone of the vomiting center hypothermic effect – blockade of the dopamine receptors of the hypothalamus.
Risperidone reduces the productive symptoms of schizophrenia (delirium, hallucinations), aggressiveness, automatism, to a lesser extent, suppresses motor activity and induces catalepsy to a lesser extent than classical antipsychotics. Balanced central antagonism of serotonin and dopamine can reduce the tendency to extrapyramidal side effects and expand the therapeutic effect of the drug on the negative and affective symptoms of schizophrenia.
Risperidone may cause a dose-dependent increase in plasma prolactin concentrations.
Pharmacokinetics
Absorption
After oral administration, risperidone is completely absorbed from the gastrointestinal tract. Cmax in plasma is reached after 1-2 hours. Food does not affect absorption
Pharmacokinetics
Absorption
After oral administration, risperidone is completely absorbed from the gastrointestinal tract. Cmax in plasma is reached after 1-2 hours. Food does not affect absorption
Pharmacokinetics
Absorption
After oral administration, risperidone is completely absorbed from the gastrointestinal tract. Cmax in plasma is reached after 1-2 hours. Food does not affect absorptionyu drug, so Rispolept can be prescribed regardless of food intake.
Distribution
Risperidone is rapidly distributed in the body. Vd is 1-2 l / kg. In plasma, risperidone binds to albumin and alpha-1-glycoprotein. Risperidone is 88% bound to plasma proteins, 9-hydroxy-risperidone – 77%.
Css risperidone in the body in most patients is achieved within 1 day.
Css 9-hydroxy-risperidone is achieved within 4-5 days. The concentration of risperidone in plasma is proportional to the dose of the drug (within therapeutic doses).
Metabolism
Risperidone is metabolized in the liver with the participation of the CYP2D6 isoenzyme to form 9-hydroxy risperidone, which has a pharmacological effect similar to risperidone. Risperidone and 9-hydroxy-risperidone constitute the active antipsychotic fraction. Another route of risperidone metabolism is N-dealkylation.
Excretion of
After oral administration in patients with psychosis, T1 / 2 of risperidone from plasma is about 3 hours. T1 / 2 of 9-hydroxy-risperidone and the active antipsychotic fraction is 24 hours.
After a week of taking the drug, 70% of the dose is excreted in urine, 14 % – with feces. In urine, risperidone plus 9-hydroxy-risperidone make up 35-45% of the dose. The remaining amount is inactive metabolites.
Pharmacokinetics in special clinical cases
In elderly patients and in patients with renal failure after a single oral administration, higher plasma concentrations and delayed excretion of risperidone were observed.
In patients with hepatic insufficiency, the concentration of risperidone in the plasma did not change.
Indications
Acute seizure relief and long-term maintenance therapy: acute and chronic schizophrenia and other psychotic disorders with productive and negative symptoms of
affective disorders in various mental diseases
behavioral disorders in patients with dementia with symptoms of aggressiveness , impaired activity (agitation, delirium) or psychotic symptoms of
behavior disorders in adolescents from 15 years old and adult patient in a reduced intellectual level or mental retardation, in cases where destructive behavior (aggressiveness, impulsivity, autoaggression) is leading the clinical picture of the disease.
To stabilize mood in the treatment of mania in bipolar disorders – as a means of adjuvant therapy.
Contraindications
lactation (breastfeeding)
hypersensitivity to the components of the drug.
Caution is advised to use the drug in patients with diseases of the cardiovascular system (including those with chronic heart failure, myocardial infarction, conduction disturbances), with dehydration, hypovolemia, cerebrovascular accident, Parkinson s disease, seizures (i.e. hours in history), severe renal or hepatic insufficiency, with drug abuse or drug dependence, with conditions predisposing to the development of pirouette type tachycardia (bradycardia, electrolyte imbalance, concomitant use of drugs that extend the QT interval), with brain tumors, intestinal obstruction, in cases of acute drug overdose, with Reye syndrome (since the antiemetic effect of risperidone can mask the symptoms of these conditions), during pregnancy, to patients under the age of 15 years (because the safety and effectiveness of use I have not established the drug).
Use in pregnancy and lactation
Safety Pregnancy has not been studied. Risolept can be used during pregnancy only if the positive effect justifies the possible risk. Since risperidone and 9-hydroxy-risperidone pass into breast milk, women using Rispolept should not breast-feed.
Composition
Active ingredient: risperidone 4 mg.
Excipients: lactose monohydrate corn starch hypromellose 2910 (15 mPa · s) sodium lauryl sulfate MCC magnesium stearate silicon dioxide colloidal
Film sheath: hypromellose 2910 (5 mPa · s) propylene glycol dye talc yellow t1 titanium dioxide1 quinoline yellow (E104) indigo carmine (E132)
Dosage and administration of
A. Schizophrenia
Adults and children over 15 years of age. Risolept can be appointed once or twice a day.
The initial dose of Rispolept is 2 mg per day. On the second day, the dose should be increased to 4 mg per 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 per day. In some cases, a slower dose increase and lower initial and maintenance doses may be warranted.
Doses above 10 mg per day have not shown higher efficacy compared to lower doses and may cause extrapyramidal symptoms. Due to the fact that the safety of doses above 16 mg per day has not been studied, doses above this level cannot be used.
Benzodiazepines can be added to Rispolept therapy if additional sedation is required.
Information on the use for the treatment of schizophrenia in children under 15 years of age is not available.
Elderly patients. An initial dose of 0.5 mg twice daily is recommended. The dosage can be individually increased by 0.5 mg twice a day to 1-2 mg twice a day.
Diseases of the liver and kidneys. An initial dose of 0.5 mg per dose 2 times a day is recommended. This dose can gradually be increased to 1-2 mg per dose twice a day.
Drug abuse or drug dependence – the recommended daily dose of the drug is 2-4 mg.
B. Behavioral disorders in patients with dementia
An initial dose of 0.25 mg twice daily is recommended. If necessary, the dosage can be individually increased by 0.25 mg 2 times a day, not more often than every other day. For most patients, the optimal dose is 0.5 mg twice daily. However, some patients are shown taking 1 mg 2 times a day.
Once an optimal dose is reached, a once-daily dose may be recommended.
B. Bipolar disorder with mania
The recommended initial dose of the drug is 2 mg per day at a time. If necessary, this dose can be increased by 2 mg per day, not more often than every other day. For most patients, the optimal dose is 2-6 mg per day.
D. Behavioral disorders in patients with mental retardation or with a predominant destructive tendency in the clinical picture
Patients weighing 50 kg or more – the recommended initial dose of the drug is 0.5 mg once a day. If necessary, this dose can be increased by 0.5 mg per day, not more often than every other day. For most patients, the optimal dose is 1 mg per day. However, for some patients, 0.5 mg per day is preferable, while some require an increase in dose to 1.5 mg per day.
Patients weighing less than 50 kg – The recommended starting dose is 0.25 mg once daily. If necessary, this dose can be increased by 0.25 mg per day, not more often than every other day. For most patients, the optimal dose is a dose of 0.5 mg per day. However, for some patients, 0.25 mg per day is preferable, while some require an increase in dose to 0.75 mg per day.
Long-term administration of Rispolepta in adolescents should be carried out under the constant supervision of a physician.
Use in children under 15 years of age is not recommended.
Side effects of the
From the nervous system: insomnia, agitation, anxiety, headache, sometimes drowsiness, fatigue, dizziness, impaired attention, blurred vision, rarely – extrapyramidal symptoms: tremor, rigidity, hypersalivation, bradykinesia, acute bradykinesia, dystonia.
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 of the tongue and / or face), neuroleptic malignant syndrome (hyperthermia, muscle rigidity, instability of autonomous functions, impaired consciousness and an increase in the level of creatine phosphokinase), disturbances in thermoregulation and epileptic seizures.
From the digestive system: constipation, dyspepsia, nausea or vomiting, abdominal pain, increased activity of liver enzymes, dry mouth, hypo-or hypersalivation, anorexia, increased appetite, increased or decreased body weight.
From the cardiovascular system: orthostatic hypotension, reflex tachycardia, increased blood pressure. Against the background of Rispolept therapy, the development of strokes is described, mainly in elderly patients with predisposing factors.
From the hemopoietic organs: neutropenia, thrombocytopenia.
From the endocrine system: galactorrhea, gynecomastia, menstrual irregularities and amenorrhea. In very rare cases, hyperglycemia and exacerbation of preexisting diabetes mellitus have been reported in patients.
From the genitourinary system: priapism, erectile dysfunction, ejaculation disorders, anorgasmia, urinary incontinence.
Allergic reactions: rhinitis, rash, angioedema, photosensitivity.
From the skin: dry skin, hyperpigmentation, itching, seborrhea.
Other: arthralgia
Drug Interaction
No specific studies on the interaction of Risolept with other drugs have been performed.
Risolept may act as a levodopa antagonist and a dopamine agonist.
A decrease in the concentration of the active antipsychotic fraction of risperidone in plasma was observed with the concomitant use of Rispolept and carbamazepine. Similar effects can be observed with other inducers of hepatic enzymes. If carbamazepine and other inducers of hepatic enzymes are abolished, the dose of Rispolept should be revised and, if necessary, reduced.
When co-administered with Risolept, phenothiazines, tricyclic antidepressants and some beta-blockers may increase plasma risperidone concentrations, but this does not affect the concentration of the active antipsychotic fraction.
Fluoxetine may increase plasma concentrations of risperidone when co-administered with Risolept, but to a lesser extent the concentration of the active antipsychotic fraction.
When co-administered with Risolept with other drugs with a high degree of plasma protein binding, there is no marked displacement of any drug from the plasma protein fraction, which is manifested clinically.
Overdose
Symptoms: drowsiness, manifestations of sedation, tachycardia, arterial hypotension, extrapyramidal symptoms in rare cases – increase in QT interval.
In the case of acute overdose with combination therapy, the possibility of multiple drugs should be analyzed.
Treatment: The airway should be kept open to maintain adequate oxygen supply and ventilation. The gastric lavage (after intubation, if unconscious) and the appointment of activated charcoal with laxative are shown. ECG monitoring should be started immediately to identify possible cardiac arrhythmias.
The specific antidote is unknown. It is necessary to conduct symptomatic therapy aimed at maintaining the vital functions of the body. At arterial hypotension and vascular collapse it is necessary to enter in / in infusion solutions and / or to use sympathomimetic preparations. In case of acute extrapyramidal symptoms, anticholinergic drugs should be prescribed. Continuous medical monitoring and monitoring should continue until the symptoms of intoxication have disappeared.
Storage conditions
The drug should be stored at a temperature of 15 ° to 30 ° C.
Expiration
3 years.
Active ingredient
risperidone
Pharmacy
Prescription
Dosage form
Dosage form
Tablets
