Risperidone - instructions for use, doses, side effects, contraindications

Absorption is fast, complete. F 70%. VD 1.1 l / kg. Relationship with plasma proteins of risperidone 90%, 9-hydroxyrisperidone 77%. Biotransformation in the liver (CYP2D6) with the formation of an active metabolite - 9-hydroxyrisperidone. Half-life 20-24 hours Elimination by the kidneys (70%) and with feces (15%).

Indications:

Treatment of schizophrenia (including the first acute acute psychosis, acute attack of schizophrenia, chronic schizophrenia); psychotic states with pronounced productive (hallucinations, delusions, thinking disorders, hostility, suspicion) and / or negative (dull affect, emotional and social detachment, speech scarcity) symptomatology; to reduce affective symptoms (depression, guilt, anxiety) in patients with schizophrenia; prevention of recurrences (acute psychotic conditions) in the chronic course of schizophrenia; treatment of behavioral disorders in patients with dementia with symptoms of aggression (outbursts 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 supporting therapy).

ICD-10

V.F20-F29.F20 Schizophrenia

V.F20-F29.F21 Chrysotile disorder

V.F20-F29.F22 Chronic delusional disorders

V Mental and behavioral disorders

V.F20-F29.F25 Schizoaffective disorder

V.F20-F29.F29 Inorganic psychosis, unspecified

V.F30-F39.F30 Manic episode

V.F30-F39.F31 Bipolar affective disorder

Contraindications:

Hypersensitivity, breast-feeding.

Carefully:

Brain tumor, intestinal obstruction, drug overdose, Reye syndrome (antiemetic effect of risperidone can mask the symptoms of these conditions), diseases of the cardiovascular system (chronic heart failure, myocardial infarction, AV blockade), dehydration, cerebral circulation, hypovolemia, Parkinson's disease, seizures (including history), drug abuse or drug dependence, severe renal / hepatic insufficiency, conditions predisposing to the development of pirouette tachycardia (bradycardia, electrolyte imbalance, concomitant use of funds extending the Q-T interval), pregnancy, children under 15 years of age (efficacy and safety of use not studied).

Pregnancy and lactation:

Category by FDA - C.

Animal studies have shown an increase in the death rate of newborns. Do not apply! There is no information about the penetration into human milk of a man, but penetrates into the milk of animals. Do not apply!

Dosing and Administration:

Individual. When administered orally, the initial dose for adults is 0.25-2 mg / day, on the second day - 4 mg / day. Further, the dose can either be kept at the same level, or, if necessary, corrected. Usually the optimal therapeutic dose, depending on the indications, 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.

Maximum dose: when risperidone is administered at a dose of more than 10 mg / day, there is no increase in efficacy compared with lower doses, but the risk of developing extrapyramidal symptoms increases. The safety of the use of risperidone in doses greater than 16 mg / day has not been studied, therefore further excess of the dose 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, violating the clarity of vision; rarely - extrapyramidal symptoms (including tremor, rigidity, hypersalivation, bradykinesia, akathisia, acute dystonia).In patients with schizophrenia, tardive dyskinesia, malignant neuroleptic syndrome, thermoregulatory disorders and convulsive seizures are possible.

From the digestive system: constipation, dyspeptic phenomena, nausea, vomiting, abdominal pain, increased activity of hepatic enzymes.

On the part of the reproductive system: priapism, erectile dysfunction, ejaculation disorders, violations of orgasm.

From the cardiovascular system: rarely - orthostatic hypotension and reflex tachycardia, arterial hypertension.

From the endocrine system: galactorrhea, gynecomastia, menstrual irregularities, amenorrhea, weight gain.

On the part of the hematopoiesis system: a small decrease in the number of neutrophils and / or platelets.

Allergic reactions: rhinitis, skin rash, angioedema.

Other: urinary incontinence.

Overdose:

Symptoms: drowsiness, prolongation of the Q-T interval, electrolyte disorders, hypotension, convulsions, tachycardia.

Treatment: symptomatic. There is no specific antidote. ECG monitoring is mandatory! Dizopyramide, procainamide, quinidine, brethil tosylate, epinephrine, dopamine apply strictly prohibited!

Interaction:

Alcohol and other drugs that cause CNS depression - increased oppression of the central nervous system.

Antihypertensive drugs - strengthening the hypotensive effect.

Bromocriptine, levodopa, pergolide - a decrease in their therapeutic effect.

Carbamazepine - increased clearance of risperidone and a weakening effect.

Clozapine is a decrease in clearance of risperidone.

Special instructions:

In the treatment of resistant schizophrenia risperidone, olanzapine, amisulpride and clozapine (short-term use) seem to be equal in effectiveness, but long-term studies evaluating different outcomes and quality of life (9 CI, 1417 patients) are required to judge the comparative efficacy of atypical antipsychotics.

Instructions

Risperidone (Risperidonum)