Risperidone Verte film coated pills 4mg N20
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Active ingredients
Risperidone
Release form
Pills
Composition
Risperidone 4 mg Auxiliary substances: lactose monohydrate 114 mg, microcrystalline cellulose 19.7 mg, corn starch pregelatinized 3 mg, magnesium stearate 1 mg, potato starch 11 mg, povidone 7.3 mg. Film coating composition: Opadry II 5 mg (polyvinyl alcohol, partially hydrolyzed 2.2 mg, talc 1 mg, macrogol 0.6175 mg, titanium dioxide 0.6545 mg, soy lecithin 0.175 mg, aluminum varnish based on yellow quinoline 0.101 mg, aluminum varnish based on indigo carmine 0.252 mg).
Pharmacological effect
Antipsychotic (neuroleptic), benzisoxazole derivative. It has a high affinity for serotonin 5-HT2 and dopamine D2 receptors. It binds to α1-adrenergic receptors and, with somewhat lower affinity, to histamine H1 receptors and α2-adrenergic receptors. It has no affinity for cholinergic receptors. Although risperidone is a potent D2 antagonist (which is thought to be the main mechanism for improving the productive symptoms of schizophrenia), it causes less pronounced inhibition of motor activity and to a lesser extent induces catalepsy than classical antipsychotics. Due to a balanced antagonism to serotonin and dopamine receptors in the central nervous system, the likelihood of extrapyramidal side effects is reduced. Risperidone may induce a dose-dependent increase in plasma prolactin concentration.
Pharmacokinetics
After ingestion, risperidone is completely absorbed from the gastrointestinal tract, Cmax in plasma is reached within 1-2 hours. Food does not affect the absorption of risperidone. Css risperidone in the body in most patients is achieved within 1 day. Css 9-hydroxyrisperidone is achieved within 4-5 days. The plasma concentrations of risperidone are proportional to the dose (in the range of therapeutic doses). Risperidone is rapidly distributed in the body, Vd is 1-2 l / kg. In plasma, risperidone binds to albumin and alpha1 glycoprotein. The binding of risperidone to plasma proteins is 88%, 9-hydroxyrisperidone - 77%. Risperidone is metabolized in the liver with the participation of CYP2D6 isoenzyme with the formation of 9-hydroxyrisperidone, which has a pharmacological effect similar to risperidone.The antipsychotic effect is due to the pharmacological activity of risperidone and 9-hydroxyrisperidone. Another route of metabolism of risperidone is N-dealkylation. After ingestion in patients with psychosis T1 / 2 risperidone from plasma is 3 hours. T1 / 2 of 9-hydroxyrisperidone and the active antipsychotic fraction is 24 hours. After 1 week, 70% is excreted in the urine, 14% in feces. In urine, the total content of risperidone and 9-hydroxyrisperidone is 35-45%. The remaining amount falls on inactive metabolites. In elderly patients and in patients with renal insufficiency, after a single oral administration, elevated plasma concentrations and delayed elimination of risperidone were observed.
Indications
Treatment of schizophrenia (including first-time acute psychosis, acute attack of schizophrenia, chronic schizophrenia); psychotic states with pronounced productive (hallucinations, delusions, mental disorders, hostility, suspicion) and / or negative (dulled affect, emotional and social detachment, speech scarcity) symptoms; to reduce affective symptoms (depression, guilt, anxiety) in patients with schizophrenia; prevention of recurrence (acute psychotic states) in chronic schizophrenia; treatment of behavioral disorders in patients with dementia with symptoms of aggressiveness (outbreak of anger, physical abuse), mental disorders (agitation, delirium) or psychotic symptoms; treatment of mania in bipolar disorders (as a mood stabilizer as a means of adjuvant therapy).
Contraindications
Hypersensitivity to risperidone.
Use during pregnancy and lactation
Use during pregnancy is possible if the expected benefit of therapy for the mother outweighs the potential risk to the fetus. If necessary, use during lactation breastfeeding should be discontinued.
Dosage and administration
Individual. When administered, the initial dose for adults is 0.25-2 mg / day, on the 2nd day - 4 mg / day. Further, the dose can either be maintained at the same level, or, if necessary, adjusted. Typically, the optimal therapeutic dose, depending on the evidence, is in the range of 0.5-6 mg / day. In some cases, a slower dose increase and lower initial and maintenance doses may be justified.For schizophrenia, for patients of advanced age, as well as for concomitant diseases of the liver and kidneys, an initial dose of 500 mcg 2 times / day is recommended. If necessary, the dose can be increased to 1-2 mg 2 times / day. Maximum dose: when risperidone is used in a dose of more than 10 mg / day, there is no increase in efficacy compared with smaller doses, but the risk of extrapyramidal symptoms increases. The safety of the use of risperidone in doses of more than 16 mg / day has not been studied, therefore, a further dose excess is not allowed.
Side effects
From the side of the central nervous system: often - insomnia, agitation, anxiety, headache; possible - drowsiness, fatigue, dizziness, impaired ability to concentrate, blurred vision; rarely, extrapyramidal symptoms (including tremor, rigidity, hypersalivation, bradykinesia, akathisia, acute dystonia). In patients with schizophrenia, tardive dyskinesia, MNS, impaired thermoregulation, and seizures may occur. On the part of the digestive system: constipation, dyspepsia, nausea, vomiting, abdominal pain, increased activity of liver enzymes. On the part of the reproductive system: priapism, erectile dysfunction, ejaculation disorders, orgasm disorders. Since the cardiovascular system: rarely - orthostatic hypotension and reflex tachycardia, arterial hypertension. On the part of the endocrine system: galactorrhea, gynecomastia, menstrual disorders, amenorrhea, weight gain. On the part of the hematopoietic system: a slight decrease in the number of neutrophils and / or platelets. Allergic reactions: rhinitis, skin rash, angioedema. Other: urinary incontinence.
Overdose
Symptoms: drowsiness, sedation, tachycardia, decrease in blood pressure, extrapyramidal disorders, rarely - prolongation of the QT interval. Treatment: provide free airway to ensure adequate supply of oxygen and ventilation, gastric lavage (after intubation, if the patient is unconscious) and taking activated carbon with laxatives. Immediately start ECG monitoring to detect possible arrhythmias. There is no specific antidote. It is necessary to conduct symptomatic therapy aimed at maintaining the vital functions of the body.With a decrease in blood pressure and vascular collapse - intravenous infusion solutions and / or adrenostimulyatory. In the case of acute extrapyramidal symptoms, anticholinergic drugs. Constant medical observation and monitoring should be continued until the symptoms of intoxication disappear.
Interaction with other drugs
With the simultaneous use of inducers of microsomal liver enzymes, a decrease in the concentration of risperidone in the blood plasma is possible. With simultaneous use with phenothiazine derivatives, tricyclic antidepressants and beta-blockers, it is possible to increase the concentration of risperidone in plasma. With simultaneous use with carbamazepine, the concentration of risperidone in the blood plasma significantly decreases. With simultaneous use, risperidone reduces the effects of levodopa and other dopamine receptor agonists. With simultaneous use with fluoxetine may increase the concentration of risperidone in the blood plasma.
special instructions
Use with caution in patients with diseases of the cardiovascular system (including heart failure, myocardial infarction, cardiac muscle conduction disturbances), as well as dehydration, hypovolemia, or cerebrovascular disorders. In this category of patients, the dose should be increased gradually. The risk of developing orthostatic hypotension is especially increased in the initial period of dose selection. If hypotension occurs, a dose reduction should be considered. When using drugs with antagonistic properties of dopamine receptors, the occurrence of tardive dyskinesia, characterized by involuntary rhythmic movements (mainly of the tongue and / or face), was noted. There are reports that the occurrence of extrapyramidal symptoms is a risk factor for the development of tardive dyskinesia. Risperidone causes extrapyramidal symptoms to a lesser extent than classical antipsychotics. If symptoms of tardive dyskinesia appear, the abolition of all antipsychotics should be considered. In the case of the development of NMS, it is necessary to cancel all antipsychotics, including risperidone.Risperidone should be used with caution in patients with Parkinson's disease, since it is theoretically possible that the disease will worsen. It is known that classic neuroleptics reduce the threshold of convulsive readiness. Given this, risperidone is recommended to be used with caution in patients with epilepsy. Risperidone should be used with caution in combination with other drugs of central action. When canceling carbamazepine and other hepatic enzyme inducers, the dose of risperidone should be reconsidered and, if necessary, reduced. During treatment, patients should be advised to refrain from overeating due to the possibility of an increase in body weight. Data on the safety of risperidone in children under the age of 15 years are not available. Impact on the ability to drive vehicles and control mechanisms During the period of treatment, until the individual sensitivity to risperidone is ascertained, patients should avoid driving vehicles and other activities requiring high concentration of attention and psychomotor speed.