Rispetril (risperidone) coated tablets 2 mg. №60 vial

Description

Rispetril (risperidone) coated tablets 2 mg. №60 vial

Composition

active substance: risperidone (risperidone);

1 tablet contains risperidone 1 mg; 2 mg; 4 mg;

excipients: lactose monohydrate, sodium lauryl sulfate, microcrystalline cellulose, corn starch, magnesium stearate, colloidal anhydrous silicon dioxide;

shell composition:

• 1 mg – titanium dioxide (E 171), polydextrose (E 1200), hypromellose (E 464), triethyl citrate (E 1505), macrogol.
• 2 mg: – polyvinyl alcohol, macrogol, titanium dioxide (E 171), talc, FCF sunset yellow dye (E 110).
• 4 mg – polyvinyl alcohol, titanium dioxide (E 171), macrogol, talc; dyes: quinoline yellow (E 104), indigo carmine (E 132).

Medicinal form

Coated tablets.

The main physical and chemical properties:

• tablets 1 mg: white, oblong tablets, covered with a shell with an imprint of “R 1” on both sides of the tablet;
• tablets 2 mg: pink-orange, oblong tablets, covered with a shell, on both sides of the imprint “R” and “2” with a dividing line between them;
• tablets 4 mg: light green, oblong tablets, covered with a shell, on one side the imprint “R” and “4” with a dividing line between them, the other side is smooth;

Pharmacotherapeutic group

Antipsychotic drugs. Risperidone.
ATX code N05A X08.

Pharmacological properties

Risperidone is a selective monoaminergic antagonist with unique properties. It shows high affinity for serotonergic 5-HT2 and dopaminergic D2 receptors. Risperidone also binds to α1-adrenergic receptors and, with less affinity, to H1-histaminergic and α2-adrenergic receptors. Risperidone does not show affinity for cholinergic receptors. Although risperidone is a potent D2 antagonist associated with its efficacy in productive symptoms of schizophrenia, it does not significantly inhibit motor activity and is less inducing of catalepsy than conventional neuroleptics. Balanced central antagonism of serotonin and dopamine reduces the susceptibility to extrapyramidal side effects and expands the therapeutic effect of the drug to cover the negative and affective symptoms of schizophrenia.

Indication:

• treatment of schizophrenia and other mental disorders, including maintenance therapy, in patients who respond to therapy to prevent recurrence;
• temporary treatment of manic episodes in bipolar disorder (adjuvant therapy in combination with normothymics as initial treatment or as monotherapy for up to 12 weeks). For patients who do not respond to treatment, other treatment options should be considered, including discontinuation of Rispetril.

Treatment can be continued for up to 12 weeks if risperidone is not used in combination with normothymics. This prolonged treatment is used to consolidate the patient’s response. In combination with normothymics, treatment with Rispetril coated tablets can be discontinued more quickly, as the therapeutic effect of normothymics in combination with risperidone is manifested in the first few weeks of treatment.
No relapse prevention studies have been performed.
Due to the nature of the disease and the drugs used for treatment, including rispetril, attention should be paid to the occurrence of symptoms of depression after the initial response to treatment.

• short-term treatment (up to 12 weeks) of severe aggression or severe mental symptoms in patients with Alzheimer’s dementia in the presence of a threat of harm to themselves or others and in the absence of response to non-pharmacological treatments;
• symptomatic treatment of provocative oppositional disorders or other disorders of social behavior in children, adolescents and adults with mental development below average or mental retardation, which have manifestations of destructive behavior (impulsivity, autoaggression);
• symptomatic treatment of autistic disorders in children over 5 years of age, in which symptoms range from hyperactivity to irritability (including aggression, self-harm, anxiety and pathological cyclic actions). Treatment should be initiated and performed under the supervision of an experienced physician. The use of medicines should be part of an integrated approach to treatment, including social and psychotherapeutic treatments.

Contraindication

Hypersensitivity to the active ingredient or to any of the excipients.
Dementia and symptoms of Parkinson’s disease (rigidity, bradykinesia and parkinsonic posture disorders).
Dementia and suspected dementia with Lewy bodies (in addition to dementia symptoms, at least two of the following symptoms: parkinsonism, visual hallucinations, gait instability).

Use during pregnancy or breastfeeding

Rispetril coated tablets is not recommended for use during pregnancy, except in cases of vital necessity. If it is necessary to stop treatment with Rispetril during pregnancy, it should not be done suddenly. If it is necessary to take the drug, breastfeeding should be stopped.

Method of application and dosage

Usual dose

Rispetril coated tablets can be used once or twice a day. Doses greater than 8 mg should be divided into two doses (morning and evening). Eating does not affect the absorption of Rispetril.

Gradual discontinuation of treatment is recommended. Acute withdrawal symptoms, including nausea, vomiting, sweating, and insomnia, have been observed very rarely after abrupt discontinuation of high-dose antipsychotic drugs. Relapse of psychotic symptoms is also possible, and involuntary movements (eg, akathisia, dystonia, and dyskinesia) have been reported.

To achieve a dose of 0.25–2.5 mg, it is recommended to use Rispetril, an oral solution.

Schizophrenia and other mental disorders

Adults (up to 65 years old)
Rispetril coated tablets can be prescribed once or twice a day.

You should start taking Rispetril coated tablets 2 mg per day, on the second day the dose can be increased to 4 mg. After that, the dose can be maintained unchanged or, if necessary, individual dose correction can be continued. For most patients, the recommended dose is 4–6 mg per day. For some patients, a gradual increase in dose or a reduced starting dose may be indicated.

The maximum daily dose of the drug is 10 mg.

Doses greater than 10 mg per day have not been shown to be more effective than lower doses, but may cause extrapyramidal symptoms. Since the safety of doses exceeding 16 mg per day has not been studied, doses exceeding this level should not be used.

If additional sedation is needed, benzodiazepine can be used at the same time.

Elderly patients (over 65 years of age)
The recommended starting dose is 0.5 mg twice a day. If necessary, the dose can be increased to 1-2 mg twice a day in increments of 0.5 mg twice a day.

Manic episodes in bipolar disorders

Adults and children over 15 years old
The recommended initial dose of Rispetril coated tablets is 2 mg once a day, in the evening. The dose can be individually increased by adding 1 mg/day no more often than every 24 hours. The recommended dose range is from 2 to 6 mg per day.

As with other types of symptomatic treatment, with long-term use of Rispetril, it is necessary to periodically review the doses and adjust them during the entire therapy. There are no data on the effectiveness of Rispetril in the treatment of acute bipolar mania lasting more than 12 weeks. If Rispetril is used in combination with normotimic drugs, therapy can be stopped earlier, since the onset of the treatment effect can be expected in the first weeks of therapy. Even after the appearance of the first response to treatment, the possibility of re-emergence of depressive symptoms should be taken into account due to the peculiarities of the course of the disease and side effects of the drugs used for treatment, including Rispetril.

Elderly patients (over 65 years old)
The recommended starting dose is 0.5 mg twice a day. If necessary, the dose can be increased to 1-2 mg twice a day, increasing by 0.5 mg twice a day. Since the experience of use in elderly patients is limited, caution is recommended.

Short-term therapy of marked aggression or severe mental symptoms in patients with dementia of the Alzheimer type

The recommended starting dose is 0.25 mg twice a day. If necessary, the dose can be increased by increasing the dose by 0.25 mg twice a day no more than every other day. For most patients, the optimal dose is 0.5 mg twice a day. However, for some patients, the effective dose can be increased to 1 mg twice daily. Once the optimal dose is reached, a once-a-day daily dose can be considered. As with other types of symptomatic treatment, with long-term use of Rispetril, it is necessary to periodically review the doses and adjust them during the entire therapy.

Discontinuation of treatment with Rispetril coated tablets should occur no later than three months after the start of therapy, therapy can be resumed only if behavioral disorders reappear.

Symptomatic treatment of disorders of social behavior or aggressive behavior.

Patients with body weight > 50 kg
The recommended starting dose is 0.5 mg once daily. If necessary, the dose should be adjusted by adding 0.5 mg once a day no more than every other day. The optimal dose for most patients is 1 mg once a day. However, for some patients, no more than 0.5 mg once a day is enough to achieve a positive effect, while others may need 1.5 mg once a day.

Patients with body weight < 50 kg
The recommended starting dose is 0.25 mg once a day. If necessary, the dose can be adjusted by adding 0.25 mg once a day no more than every other day. The optimal dose for most patients is 0.5 mg once a day. However, for some patients, no more than 0.25 mg once a day is enough to achieve a positive effect, while others may need 0.75 mg once a day.

As with other types of symptomatic treatment, long-term use of Rispetril must be periodically reviewed and adjusted throughout the therapy.

There is no experience using Rispetril coated tablets for the symptomatic treatment of social behavior disorders or aggressive behavior in children under 5 years of age.

Autism (children aged 5 and over)
The dose should be selected individually, depending on the patient’s condition and clinical response.

Patients with body weight < 50 kg
The recommended starting dose is 0.25 mg once daily. From the 4th day, the dose can be increased by 0.25 mg. A dose of 0.5 mg should be maintained and clinical response evaluated on day 14. Dose increases of 0.25 mg at 2-week intervals may only be considered for patients with insufficient clinical response.

Patients with body weight ≥ 50 kg
The recommended starting dose is 0.5 mg once a day. From the 4th day, the dose can be increased by 0.5 mg. A dose of 1 mg should be maintained and clinical response evaluated on day 14. Dose increases of 0.5 mg at 2-week intervals may only be considered for patients with insufficient clinical response.

Children

Risperidone is used to treat disorders of social behavior or aggressive behavior, as well as autistic disorders in children over 5 years of age; for the treatment of manic episodes in bipolar disorder – in children over 15 years of age.

Overdose

Signs and symptoms of overdose observed are known side effects of the drug, which are manifested in an increased form: drowsiness and sedation, tachycardia and hypotension, as well as extrapyramidal symptoms. QT prolongation and convulsions have been reported with overdose. Flicker-flicker associated with risperidone overdose in combination with paroxetine has been reported.
In case of acute overdose, the possibility of drug interaction of several drugs should be analyzed.

Side effects:

• Infections and invasions: pneumonia, bronchitis, upper respiratory tract infections, sinusitis, urinary tract infections, ear infections, influenza, respiratory infections, cystitis, eye infections, tonsillitis, onychomycosis, inflammation of the subcutaneous tissue, viral infection, localized infection;
• From the blood and lymphatic system: neutropenia, decreased white blood cell count, thrombocytopenia, anemia, decreased hematocrit, increased eosinophils;
• From the immune system: hypersensitivity;
• From the endocrine system: hyperprolactinemia;
• From the metabolism and digestion: weight gain, increased appetite, decreased appetite, diabetes, hyperglycemia, polydipsia, weight loss, anorexia, high cholesterol;
• From the psyche: insomnia, sleep disorders, agitation, depression, anxiety,
  mania, confusion, decreased libido, nervousness, night terrors;
• From the nervous system: sedation / drowsiness, parkinsonism, headache, akathisia, dystonia, dizziness, dyskinesia, tremor, tardive dyskinesia, cerebral ischemia, lack of response to stimuli, loss of consciousness, depressed consciousness, convulsions, syncope, psychomotor hyperactivity disorder balance, incoordination, postural dizziness, attention deficit, dysarthria, taste disturbances, hypoesthesia, paresthesia;
• From the eyes: blurred vision, conjunctivitis, photophobia, dry eyes, increased tearing, redness of the eyes;
• From the hearing organs: vertigo, tinnitus, ear pain;
• From the cardiac activity: tachycardia, atrial fibrillation, atrioventricular block, cardiac conduction disorders, prolongation of the QT interval on the electrocardiogram, bradycardia, abnormalities on the electrocardiogram, palpitations;
• From the vascular system: hypertension, hypotension, orthostatic hypotension, hot flashes;
• From the respiratory system: dyspnea, pharyngolaryngeal pain, cough, epistaxis, nasal congestion, aspiration pneumonia, pulmonary congestion, impaired airway patency, wheezing, wheezing, dysphonia, respiratory disorders;
• From the digestive system: abdominal pain, abdominal discomfort, vomiting, nausea, constipation, diarrhea, dyspepsia, dry mouth, toothache, fecal incontinence, feces, gastroenteritis, dysphagia, bloating, pancreatitis, gastrointestinal obstruction, swelling of the tongue, cheilitis;
• From the hepatobiliary system: increased levels of transaminases, increased levels of gamma-glutamyl transferase, increased levels of liver enzymes, jaundice;
• From the skin and subcutaneous tissue: rash, erythema.