Rispolept solution for oral administration 30 ml
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Active ingredients
Risperidone
Release form
Solution
Composition
1 ml of oral solution Rispolept contains: Risperidone - 1 mg.
Pharmacological effect
Rispolept is an antipsychotic drug. Rispolept contains the active ingredient risperidone, a selective monoaminergic antagonist with high affinity for dopaminergic D2 receptors and serotonergic 5-HT 2 receptors. Risperidone also binds to alpha1-adrenergic receptors and has some affinity for alpha2-adrenergic and H1-histamine receptors. Risperidone has no effect on cholinergic receptors. Risperidone is a strong D2-receptor antagonist, but it does not cause an inhibition of motor activity and, compared to classical neuroleptics, induces catalepsy much less to a lesser extent. extrapyramidal disorders. Rispolept has a wide spectrum of therapeutic action that covers the affective and negative symptoms of schizophrenia.
Pharmacokinetics
When oral administration of the drug Rispolept the active ingredient is well absorbed in the digestive tract, reaching peak concentrations within 1-2 hours after ingestion. Meal does not affect the rate and extent of absorption of risperidone. The active ingredient of the drug Rispolept in the liver is metabolized with the participation of cytochrome P-450 with the formation of a pharmacologically active metabolite, 9-hydroxyrisperidone. 9-hydroxyrisperidone and unchanged risperidone form an active antipsychotic fraction. Risperidone is also metabolized by N-dealkylation. The half-life of unchanged risperidone in patients with psychosis is about 3 hours. The half-life of the active metabolite and antipsychotic fraction reaches 24 hours. Equilibrium concentrations of unchanged risperidone are reached on day 1-2 of therapy, of the active metabolite on day 4-5 of therapy. Within therapeutic doses, plasma concentrations of risperidone are directly proportional to the dose taken. About 88% of the unchanged substance and 77% of the active metabolite binds to plasma proteins. Within 7 days about 70% of the taken dose are excreted by the kidneys, and about 14% of the received dose by the intestines.About 35-45% of the dose of risperidone determined unchanged and as an active metabolite in the urine. Elderly patients with impaired renal function and patients with renal insufficiency did not show clinically significant changes in the pharmacokinetic profile of risperidone.
Indications
Rispolept is used to treat patients with various forms of schizophrenia, including the first episode of psychosis, an acute attack of schizophrenia and a chronic form of schizophrenia, as well as other psychotic conditions that are accompanied by pronounced productive or negative symptoms (including hostility, mental disorders, hallucinations, suspicion, emotional and social exclusion, dulled affect and speech poverty). The Rispolept drug can also be used in patients with schizoaffective disorders and isophrenia with severe affective symptoms (depression, anxiety, fear). Dispel use as a means of maintenance therapy in patients with chronic schizophrenia to prevent the development of acute psychotic conditions. Tablets and Rispolept solution are prescribed to treat behavioral disorders in patients with dementia with symptoms of aggressiveness (including physical abuse and verbal outbreaks), behavioral disorders (including agitation and anxiety), and severe psychotic symptoms. The drug Rispolept may s recommended as a means for additional therapy in patients with manic episodes in bipolar disorders (these episodes are characterized by expansive, or irritable elevated mood, decreased need for sleep, inflated self-esteem, poor concentration, rapid speech, rejection of criticism and aggressive or antisocial behavior).
Contraindications
Rispolept is not prescribed to patients with personal intolerance to risperidone or additional components of the drug. The coated pills, Rispolept are not prescribed to patients with rare forms of lactose intolerance (including glucose-galactose malabsorption syndrome, galactosemia, and lactase deficiency). In pediatric practice, Rispolept pills are used only for treating patients over 15 years of age. apply with caution and only in children older than 5 years. Care should be taken when prescribing Rispolept to patients suffering from diseases of the cardiovascular system. s (including heart failure,conduction disorders and myocardial infarction), cerebrovascular disorders, epilepsy and Parkinson's disease, as well as elderly patients and patients with impaired renal function. Use a hypoprotectant with hypovolemia and dehydration.
Use during pregnancy and lactation
There are no data on the safety of risperidone during pregnancy. In animal studies, no teratogenic effect of risperidone was found, however, only indirect indirect prolactin and CNS-mediated effects were noted. The disposit can be used during pregnancy only under the supervision of a physician, and taking into account possible risks. lactation period should complete breastfeeding.
Dosage and administration
Solution for oral administration Rispolept: The drug is intended for oral administration. The vial caps of the drug Rispolept are protected from children. The kit includes a pipette that allows you to measure from 0.25 to 3 ml of solution (a bottle of 30 ml of the preparation), or a pipette to measure from 0.25 to 4 ml with an accuracy of 0.05 ml (a bottle of 100 ml of the preparation). The divisions of 0.05 ml are applied in the range from 0.5 to 3 or 4 ml, respectively. For accurate dosing of the drug, the required amount of solution should be pipetted, pulling the piston to the mark in milliliters or milligrams. While supporting the lower rim, the pipette is removed from the vial and the contents of the pipette are poured into any soft drink, excluding tea. It is recommended to rinse the pipette with running water after each use. Dosage: The duration of therapy and doses of the drug Rispolept is determined by the doctor individually, taking into account the concomitant therapy, the nature of the disease and the patient’s personal characteristics. During therapy, the patient’s condition should be monitored and, if necessary, the dose of the drug Rispolept should be adjusted. Schizophrenia: In schizophrenia, as a rule, 2 mg risperidone per day is prescribed. If necessary, on the second day of therapy, the dose is increased to 4 mg of risperidone per day. Further, the dose is adjusted individually, the average therapeutic dose is 2-8 mg risperidone per day. In some patients, it may be advisable to administer more than 8 mg of risperidone per day.It should be borne in mind that when taking more than 10 mg of the drug per day, there was no increase in the effectiveness of risperidone compared to lower doses, however, the risk of extrapyramidal disorders increased. drugs on rispolept recommended to gradually cancel the previous therapy. If a patient received antipsychotic drugs in the form of a “depot,” risperidone therapy should be started on the day when the next injection was planned (and the injection is not performed). It is recommended to periodically assess the need for further anti-parkinsonian therapy. reduce the initial dose of the drug Rispolept to 0.5 mg twice a day. Behavioral disorders in patients with dementia: For patients with dementia that is accompanied behavioral disorders usually prescribers Rispolept at an initial dose of 0.25 mg twice a day. If necessary, the dose is adjusted by increasing with an interval of at least 48 hours by 0.25 mg of risperidone twice a day. The average therapeutic dose is 0.5 mg twice a day, for some patients 1 mg of risperidone twice a day. After establishing an individual dose, it is allowed to switch to a daily dose once a day. Bipolar disorders: As an additional therapy, patients with bipolar disorders, as a rule, are prescribed 2 mg risperidone per day. The dose can be adjusted individually at intervals of at least 48 hours by adding up to 2 mg of risperidone to the current dose. The optimal therapeutic dose for most patients is 2-6 mg risperidone per day. Dosing for patients with a body weight less than 50 kg: For patients with a body weight less than 50 kg, it is recommended to use only Rispolept solution. The recommended initial dose for these patients is 0.25 mg risperidone 1 time per day. Dose adjustment, if necessary, is carried out by increasing the current by 0.25 mg with an interval of at least 48 hours. The average therapeutic dose is 0.25-0.75 mg per day.
Side effects
Rispolept is usually well tolerated by patients, in some cases it is quite difficult to distinguish the undesirable effects of risperidone from the symptoms of the underlying disease. When taking the drug Rispolept, patients developed the following side effects: From the nervous system: sleep disorders, anxiety, agitation, headache. Possible short-term sedation, which is more common in adolescents. In addition, the development of dizziness, impaired coordination of movements, and increased fatigue are possible. One cannot exclude the possibility of the development of extrapyramidal manifestations, including tremor, hypersalivation, rigidity, akathisia, acute dystonia and bradykinesia, while taking risperidone. Extrapyramidal symptoms when taking the drug Rispolept were observed much less frequently than with other antipsychotics, and were also less pronounced and passed when the dose was reduced. On the digestive system: abdominal pain, vomiting, nausea, dyspeptic symptoms, abnormal stool, increased liver activity enzymes. From the urogenital system: erectile dysfunction, anorgasmia, urinary incontinence, ejaculation disorder, priapism. From the heart, blood vessels and blood system: the development of a reflex was rarely observed tachycardia, hypotension or hypertension, and a decrease in the number of neutrophils and platelets. Allergic reactions: allergic rhinitis, urticaria, skin rash, Quincke's edema. Others: reduced visual acuity, increased prolactin in plasma (symptoms of which are gynecomastia, galactorrhea, menstrual disorders cycle and amenorrhea), weight gain, tardive dyskinesia (with involuntary rhythmic movements of the tongue and muscles of the face). In elderly patients with several risk factors when taking risperidone during development of cerebrovascular phenomena is possible. In addition, when taking the drug Rispolept (less often than taking classical neuroleptics), patients with schizophrenia may develop seizures, neuroleptic malignant syndrome, tardive dyskinesia, impaired thermoregulation, as well as aquatic intoxication. syndrome of inadequate secretion of antidiuretic hormone). In isolated cases, when taking the drug Rispolept, patients developed hyperglycemia and exacerbations of the existing sugar diabetes
Overdose
When receiving excessive doses of the drug Rispolept, patients developed drowsiness, tachycardia, sedation, hypotension, and extrapyramidal symptoms. In some cases, patients with an overdose of risperidone had a prolonged Q-T interval. There is evidence of a happy outcome after taking 360 mg of risperidone. The specific antidote is unknown. In case of overdose, gastric lavage is performed (after intubation, if the patient is unconscious), the appointment of enterosorbents and laxatives. It is necessary to ensure airway patency for normal ventilation and oxygenation, as well as to monitor the function of the cardiovascular system to detect arrhythmias. In case of hypotension and vascular collapse, sympathomimetic drugs and / or intravenous fluids are prescribed. For acute extrapyramidal symptoms, anticholinergics are prescribed. Monitoring the patient’s condition is necessary until the state is fully normalized.
Interaction with other drugs
It should be used with caution the drug Rispolept combined with drugs of central action. Disposal can reduce the effectiveness of levodopa and dopamine antagonists. Carbamazepine reduces the concentration of the active antipsychotic fraction of the drug Rispolept. Similar effects are also possible when taking other hepatic enzyme inducers. When combined, use of risperidone and hepatic enzyme inducers requires dose adjustment of the drug Rispolept. Fluoxetine, phenothiazines, some beta-blockers and tricyclic antidepressants can increase the plasma concentrations of risperidone. degrees bound to plasma proteins.
special instructions
During the period of drug therapy, Rispolept should not be controlled by potentially unsafe mechanisms.