Risperidone

Brand Vertex

In stock 1656 Items

Available since: 2019-09-19

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Clinical Pharmacology

Rileptide - antipsychotic drug, benzisoxazole derivative. It also has a sedative, antiemetic and hypothermic effects.

Risperidone is a selective monoaminergic antagonist, has a high affinity for serotonin 5-HT 2 - and dopamine D 2 -receptors. It binds to A 1 -adrenoreceptors and somewhat weaker - with histamine H 1 -receptors and A 2 -adrenoreceptors. Does not possess tropnost to cholinergic receptors.

The antipsychotic action is due to the blockade of the dopamine D 2 receptors of the mesolimbic and mesocortical system. Sedative effect due to blockade of adrenergic receptors of the reticular formation of the brain stem; antiemetic effect - blockade of dopamine D2-receptors of the trigger zone of the vomiting center; hypothermic action - blockade of dopamine receptors of the hypothalamus.

Rileptide reduces the productive symptoms of schizophrenia (delirium, hallucinations), automatism, to a lesser extent causes the suppression of motor activity and to a lesser extent induces catalepsy than classical antipsychotics. Balanced central antagonism of serotonin and dopamine may reduce the propensity for extrapyramidal side effects. Risperidone may cause a dose-dependent increase in plasma prolactin concentration.

Indications

- Acute and chronic schizophrenia and other psychotic disorders 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 abuse), mental disorders (agitation, delusions) or psychotic symptoms.
- As a means of adjuvant therapy in the treatment of mania with bipolar disorders.
- As a means of 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.

Risperidone is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Risperidone	Vertex	Russia	pills
Risperidone	Canonpharma	Russia	pills
Torendo	Krka dd Novo mesto AO	Slovenia	pills
Rispaxol	Grindex	Latvia	pills
Torendo Q-Tab	Krka dd Novo mesto AO	Slovenia	lozenges
Rileptide	Egis	Hungary	pills
Risdonal	Alkaloid	Macedonia	pills
Risset	Pliva Hrvatska doo	Croatia	pills
Rispolept consta	Janssen Pharmaceuticals N.V	Belgium	bottle
Rispolept	Janssen Pharmaceuticals N.V	Belgium	pills

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Dosage and Administration

It is applied inside. Adults and children over 15 years old are prescribed 1 or 2 times a day.
Schizophrenia. The initial dose is 2 mg / day. On day 2 - up to 4 mg / day. From this point on, if necessary, the dose can either be maintained at the same level, or individually adjusted in the range of 4–6 mg / day.
Doses above 10 mg / day did not show higher efficacy compared with lower doses and may cause the appearance of extrapyramidal symptoms. The maximum daily dose is 16 mg.
Behavioral disorders in patients with dementia: The optimal dose is 1 mg once a day.
Bipolar disorder in mania: initial dose - 2 mg / day for 1 reception. Increasing the dose (2 mg / day) - no more than a day. The optimal dose is 2-6 mg / day.
Behavioral disorders in patients with mental retardation or with predominantly destructive tendencies in the clinical picture. Patients weighing 50 kg or more. The optimal dose is 1 mg / day.
It is recommended to halve both the initial dose and subsequent dose increases in elderly patients and in patients with renal or hepatic insufficiency (if necessary, use an adequate dosage form).

Adverse reactions

From the side of the central nervous system: insomnia, agitation, anxiety, headache, drowsiness, fatigue, dizziness, decreased ability to concentrate, blurred vision, extrapyramidal symptoms (tremor, rigidity, hypersalivation, bradykinesia, akathisia, acute dystonia), mania or hypomania, stroke (elderly patients with predisposing factors).
Patients with schizophrenia - hypervolemia (either due to polydipsia, either due to the syndrome of inappropriate secretion of antidiuretic hormone), tardive dyskinesia (involuntary rhythmic movements mainly language and / or persons), neuroleptic malignant syndrome (hyperthermia, muscle stiffness, instability autonomous functions , impaired consciousness and increased activity of creatine phosphokinase), impaired thermoregulation, epileptic seizures.
From the digestive system: constipation, dyspepsia, nausea or vomiting, abdominal pain, increased activity of liver transaminases, dry mouth, hypo-salivation or hypersalivation, anorexia.
Since the cardiovascular system: orthostatic hypotension, reflex tachycardia, or increased blood pressure (BP).
From the side of blood-forming organs: neutropenia, thrombocytopenia.
On the part of the endocrine system: galactorrhea, gynecomastia, menstrual disorders, amenorrhea, increase or decrease in body weight, hyperglycemia, or exacerbation of pre-existing diabetes mellitus.
From the genitourinary system: priapism, erectile dysfunction, ejaculatory disorders, orgasm disorders, including anorgasmia, urinary incontinence.
Allergic reactions: itching, rash, angioedema.
On the part of the skin: dry skin, hyperpigmentation, seborrhea, photosensitization.
Other: arthralgia, rhinitis.

Contraindications

Carefully: used in brain tumor, intestinal obstruction, overdose drugs syndrome Reye (antiemetic effect of risperidone may mask symptoms of these conditions), disorders of the cardiovascular system (chronic heart failure, atrioventricular block, myocardial infarction), dehydration, cerebral circulatory disorders, hypovolemia, Parkinson's disease , convulsions (including history), drug abuse, drug dependence, kidney failure is difficult degree, liver failure severe, conditions predisposing to the development of tachycardia type "pirouette" (bradycardia, electrolyte imbalance, concomitant medication, prolonged QT interval), pregnancy.

Drug interactions

Risperidone reduces the effectiveness of levodopa and dopamine agonists.
Phenothiazines, tricyclic antidepressants, and beta-blockers increase plasma concentration of risperidone (they do not affect the concentration of the active antipsychotic fraction).
While taking carbamazepine and other microsomal enzyme inducers at the same time, there is a decrease in plasma active antipsychotic fraction of risperidone.
Clozapine reduces the clearance of risperidone.
With simultaneous use with risperidone ethanol, drugs that inhibit the central nervous system (CNS), lead to additive inhibition of the function of the central nervous system.
Antihypertensive drugs increase the severity of blood pressure reduction in the background of the use of risperidone.
Fluoxetine can increase the concentration of risperidone in plasma (to a lesser extent - its active antipsychotic fraction).

Special instructions

In 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, it is recommended to begin the procedure instead of the next scheduled injection. Periodically, the need to continue current antiparkinsonian therapy should be assessed.
The risk of developing mania or hypomania can be significantly reduced by using low doses of risperidone or by gradually increasing them.
At occurrence of orthostatic hypotension, especially in the initial period of dose selection, the issue of dose reduction should be considered. In patients with diseases of the cardiovascular system, as well as with dehydration, hypovolemia, or cerebrovascular disorders, the dose of risperidone should be increased gradually.
If signs and symptoms of tardive dyskinesia occur, the abolition of all antipsychotic drugs should be considered. In malignant neuroleptic syndrome, all antipsychotic drugs, including risperidone, must be canceled.
When canceling carbamazepine and other inductors of microsomal enzymes, the dose of risperidone should be reduced.
Patients should be advised to refrain from overeating due to the possibility of an increase in body weight.
During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and psychomotor reactions.

Overdosage

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 charcoal along 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 the development of acute extrapyramidal symptoms - anticholinergic drugs. Constant medical observation and monitoring should be continued until the symptoms of intoxication disappear.