Description overdue on 10/22/2014

• Composition
• Product form
• Pharmacological action
• Pharmacodynamics and pharmacokinetics
• Indications rispolept
• Contraindications
• Side effects
• Instructions for use rispolept
• Overdose
• Cooperation
• Terms of sale
• Storage conditions
• Shelf life
• Cautions
• Analogs
• Synonyms
• Babies
• With alcohol
• During pregnancy (and lactation)
• Reviews
• Price, where to buy

Composition

Tablets Rispolept (Rispolept)

1 tablet contains 1 mg, 2 mg, 3 mg or 4 mg risperidone - Active substance.

Additional ingredients: corn starch, lactose, microcrystalline cellulose, magnesium stearate, hypromellose, colloidal silicon dioxide, anhydrous, propylene glycol, sodium lauryl sulfate, titanium dioxide, talc.

Oral solution Rispolept (Rispolept)

1 ml of a solution comprising 1 mg risperidone   - Active substance.

Additional ingredients: tartaric acid, sodium hydroxide, benzoic acid, purified water.

Powder / m slurry Rispolept Consta (Rispolept Sonsta)

1 vial contains 25 mg; 37, 5 mg or 50 mg R isperidona   - Active substance in the form of microgranules (381 mg risperidone 1 g of microgranules).

Additional ingredients: a copolymer of glycolic and lactic acids.

Solvent: Polysorbate 20, sodium carmellose, sodium hydrogen phosphate dihydrate, anhydrous citric acid, sodium hydroxide, sodium chloride, water for injection.

Product form

The drug is produced in the form of Rispolept oral tablets   №20 and №60 and oral solution   30 or 100 ml.

Medicine Rispolept Consta   It is marketed in the form of powder / m on the suspension 25; 37, 5 and 50 mg per vial. Attached to the powder 2 ml syringe with a solvent safe needle and needleless device for producing the slurry.

Pharmacological action

Antipsychotic.

Pharmacodynamics and pharmacokinetics

Rispolept   and Rispolept Consta   They are antipsychotic drugs and comprise, as active ingredient, risperidone - Monoaminergic antagonist selective. Risperidone has a relatively high affinity for D2-dopaminergic receptors and 5-HT 2 serotonergic .   It has the ability to bind to alpha-1-receptors adrenergichekimi and exhibits some affinity for the alpha 2 adrenergic receptors and H1-histamine .   Effect on the cholinergic receptors were observed.

Risperidone shows strong antagonism D2-receptors and do not cause, in this case, inhibition of motor activity And compared with other neuroleptics, weaker inducts   catalepsy.   Shows balanced antagonism to the central action   dopamine   and serotonin, It reduces the tendency for extrapyramidal disorders character. Therapeutic effect rispolept includes negative and affective symptoms schizophrenia.

When applied orally (by mouth) is well absorbed in GI to achieve peak concentrations for 60-120 minutes after administration. Food does not affect the extent and rate of absorption.

Metabolism   It occurs by N-dealkylation as well as in the liver, with the assistance   Cytochrome P-450 which ultimately leads to the formation of a metabolite - 9-hydroxyrisperidone (pharmacologically active). This metabolite of risperidone and unchanging form antipsychotic active fraction.

T1 / 2 of unchanged drug in patients with psychosis occurs in about 3 hours, and the antipsychotic fraction and the active metabolite per day. Equilibrium concentrations, respectively, are observed for 1-2 days and 4-5 days. Within the accepted therapeutic doses risperidone   its plasma concentration directly proportional to its dose.

FROM plasma proteins   It binds approximately 88% of unchanged drug and 77% of the metabolite.

Throughout the week, excreted by the kidneys approximately 70%, approximately 14% of the intestines of the dose. As an active metabolite, and unchanged in the urine is determined by the order of 35-45% of the dose.

Patients in the elderly, and patients with abnormalities of the kidneys   No significant deviations pharmacokinetic profile .

Rispolept Consta   (extended-release formulation) once after the / m, it shows a slight release of the active ingredient (less than 1%) with an interval of 21 days. Significant release was observed 3 weeks after injection and monitored for 4 to 6 weeks. Release risperidone 7 week decreased. In connection with a small drug release in the first week, parallel recommended to take oral form of the drug.

Carrying a single injection of 14 days confirming providing therapeutic levels plasma concentrations of risperidone   4-6 weeks after the last injection. When carrying out treatment on this circuit was not observed accumulation of risperidone   even when used over a year.

FROM plasma proteins   It binds about 90% risperidone   and 77% of its active metabolite.

It is metabolized by cytochrome P450, with the assistance and forms a 9-hydroxyrisperidone, which exhibits similar, with the same drug pharmacodynamic profile.

After the last application rispolept Consta its excretion continues for 7-8 weeks.

Patients in the elderly, and patients with abnormalities of the kidneys We observed an increase in the plasma content unchanged risperidone and its active metabolite .

Indications rispolept

Indications for use of tablets and oral solution

Rispolept drug used for long-term maintenance treatment and prevention of acute episodes:

• affective disorders, manifested in various mental disease states;
• chronic and acute Schizophrenia   and other psychotic pathologies with negative and positive symptoms;
• behavioral disorders in patients with scope dementia   under the supervision of aggression ( physical abuse . outburst   etc.), psychotic symptoms , Disorders of the (delirium, excitement, etc.);
• behavioral disorders scope   adolescents from 15 years of age and patients of adult age with a reduced level of intelligence or inhibition of mental development when destructive behavior ( autoaggression . impulsiveness . aggression ) Is dominant in the clinical course of the disease.

Also Rispolept prescribed for the treatment of mania at different bipolar disorder   (as an adjuvant) and to stabilize mood.

Indications for rispolept Consta is:

• prevention and therapy schizoaffective disorder   and exacerbations Schizophrenia .

Contraindications

Absolute contraindications to receiving oral solution and tablets rispolept are hypersensitivity to the ingredients of the formulation and lactation.

For rispolept Consta, except the above, the age of 18 years.

With caution is prescribed:

• in diseases of the cardiovascular system ( CHF . the loss of conductivity of the heart muscle , Postinfarction period);
• at circulatory disorders of the brain ;
• at hypovolemia   and Dehydration ;
• at convulsions   (even in history) and epilepsy ;
• at Parkinson's disease ;
• at renal and / or hepatic pathologies, severe;
• when drug dependence or abuse of drugs;
• at bowel obstruction . brain tumors Acute drug overdose, Reye's syndrome ;
• under conditions which may lead to tachycardia   type "pirouette" (electrolyte imbalance, bradycardia Parallel medications increase the interval QT);
• at pregnancy ;
• in childhood and adolescence up to 15 years for the tablets, and up to 4 years for the oral solution.

Side effects

Negative effects are described by the frequency of their occurrence, from the frequent to rare.

Oral forms rispolept

Very common: infections of the urinary system in elderly patients with dementia .

Common: respiratory tract infections (upper) nasopharyngitis , Urinary tract infections, phlegmon . sinusitis . pneumonia   (elderly patients with dementia ), Flu-like state, and   rhinitis   (in children).

Rare: ear infections, pharyngitis , Viral infections, eye infections, tonsillitis . bronchitis Localized infection onychomycosis . cystitis , Respiratory tract infection, acrodermatitis . bronchopneumonia . tracheobronchitis .

• The immune system : Hypersensitivity, anaphylactic shock .
• Endocrine system : Kussmaul's coma . hyperprolactinemia , Violation of antidiuretic hormone secretion.
• Violations power mode   and metabolism : decreased appetite   (elderly patients with dementia ) increased appetite   (in children), anorexia . polydipsia . diabetic ketoacidosis . hypoglycemia . diabetes , Water intoxication.
• Mental Disorders : insomnia . nervousness . anxiety . confusion   (elderly patients with dementia ), Weakness (in children), agitation, sleep disturbances, flattening of affect . anorgasmia , Weakening of libido, mania.
• Nervous system : Parkinsonism   (including extrapyramidal disorder . akinesia . syndrome "gear" . bradykinesia . muscle rigidity . hypokinesia ), Sedation, headache . drowsiness   (in children); akathisia   (also a concern), dizziness, drowsiness . sedation . dystonia   (including muscle spasm or involuntary contraction, contraction of muscles, paralysis of the tongue, involuntary motions of the eyeballs); lethargy , Postural dizziness, tremor . dyskinesia   (including chorea   and choreoathetosis , Muscle twitching), fainting, impaired attention and gait, depressed (in elderly patients with dementia) ataxophemia   (in children); poor coordination, lack of response to external stimuli, dizziness to his loss, hypoesthesia , Speech impairment, movement disorders cerebral ischemia . tardive dyskinesia , Neuroleptic malignant syndrome, character, cerebrovascular disorders.
• Government of : A disorder of visual acuity, conjunctivitis   (elderly patients with dementia), conjunctival hyperemia, involuntary rotational movement of the eyeballs, blurred vision, swelling of the eyelids, crusting on the eyelids, periorbital edema , Dry eye, photophobia, lacrimation increased, increasing Intraocular pressure .
• Cardiovascular system : tachycardia , Lowering blood pressure, orthostatic hypotension , Transient ischemic attack (in elderly patients with dementia) stroke . myocardial infarction , Palpitations (in children); sinus bradycardia . atrioventricular block , Palpitations, sinus tachycardia "Tides" of blood, the blockade of legs (left and right) bundle branch block, Atrial fibrillation .
• Gastrointestinal tract Nausea, dyspepsia . constipation . vomiting , Salivation, diarrhea , Sensation of dryness in the mouth, abdominal pain, stomach discomfort, fekaloma   (elderly patients with dementia) encopresis . swelling of the lips . gastritis . aptializm . cheilitis . pancreatitis , Ileus.
• The kidneys and urinary tract : thamuria . urinary incontinence   and enuresis   (in children), pain during urination, urinary retention.
• Skin   and subcutaneous tissue : rash . dandruff , Dry skin, hyperkeratosis . seborrheic dermatitis . erythema   (elderly patients with dementia) itch   and acne   (in children), violation of skin pigmentation, papular rash . erythematous rash . generalized rash . maculopapular rash . alopecia . angioedema .
• Musculo-skeletal system : Back pain, joint swelling, pain in the limbs, arthralgia , Gait disturbance (in elderly patients with dementia), and pain in the neck myalgia   (in children), chest pain, muscle weakness, stiffness in the joints, rhabdomyolysis .
• Reproductive system and breast : Lack of ejaculation, galactorrhea   (in children), violation of menstruation, gynecomastia . amenorrhea , Vaginal discharge, abnormal ejaculation And sexy erectile dysfunction , Breast enlargement, retrograde ejaculation . priapism .
• Thoracic and respiratory disorders As well as complications from mediastinum : breathlessness , Nasal congestion, cough, and rhinorrhea   (elderly patients with dementia and children), nosebleeds, pain in the throat and larynx, pulmonary congestion, inhalation pneumonia . wheezing . dysphonia , Obstructive airways disease, productive cough, crackles, edema of the nose, hyperventilation , Respiratory failure syndrome apnea   in a dream.
• Lymphatic System   and hematology : anemia . granulocytopenia . agranulocytosis . thrombocytopenia .
• Liver: jaundice .
• Hearing : Tinnitus, ear pain.
• General disorders : Fatigue, fever . asthenia , Chest pain, gait disturbance, and peripheral edema (in elderly patients with dementia), chest discomfort and slow (for children) thirst , Swelling, flu-like symptoms, malaise, general edema, chills, cold extremities, swelling of the face, the syndrome of "cancellation" hypothermia .
• Laboratory findings : Acceleration of heart rate, increase in creatine , Increase in body temperature (elderly patients with dementia), weight gain (in children), the growth of content prolactin . Increased activity aspartate aminotransferase   and alanine aminotransferase , The increase in eosinophils   and leukocytes   blood, impaired ECG, increase of blood glucose, lowering the concentration Hemoglobin , Reduction of body temperature, reduction hematocrit , Lowering blood pressure, lengthening the interval on the electrocardiogram QT.

Rispolept Consta

Common: respiratory tract infections (upper).

Rare: flu-like infection nasopharyngitis . bronchitis . rhinitis , Urinary tract infections, ear infections, and respiratory tract, pneumonia . pharyngitis Viral infections, sinusitis Localized infection gastroenteritis . cystitis . subcutaneous abscess .

• The immune system : Hypersensitivity, anaphylactic shock .
• Endocrine system : hyperprolactinemia , Violation of antidiuretic hormone secretion.
• Violations power mode   and metabolism : High or low appetite . hyperglycemia . anorexia . diabetic ketoacidosis . hypoglycemia . diabetes , Water intoxication.
• Nervous system : headache, Parkinsonism   (including muscle rigidity, extrapyramidal disorders, hypokinesia . bradykinesia , Rigidity of the "gear" muscle cramps ); akathisia . dizziness . tremor . sedation . drowsiness , Fainting, impaired attention, hypoesthesia ; loss of coordination, tardive dyskinesia . dystonia . lethargy . paresthesia . drooling , Postural dizziness, convulsions, drowsiness, ataxophemia . akinesia .
• Mental Disorders : Anxiety, insomnia, agitation, sleep disturbances, depression , Violation of sleep, nervousness, decrease in libido, mania.
• Government of : Blurred vision, decreased visual acuity, conjunctivitis , Retinal artery occlusion (shown at the intracardiac defect that has to right to left shunt).
• Cardiovascular system : arterial hypertension . atrioventricular block   (I degree) tachycardia , Palpitations, bundle-branch block (left and right), sinus bradycardia, low blood pressure, sinus tachycardia, orthostatic hypotension . atrial fibrillation .
• Respiratory system : Nasal sinuses, cough, shortness of breath, rhinorrhea Pain in the larynx and pharynx, sleep apnea syndrome .
• Gastrointestinal tract : Dryness of the mouth, constipation . dyspepsia , Dental pain, nausea, hypersecretion of saliva , Vomiting, abdominal pain, diarrhea . gastritis , Discomfort in the stomach, pancreatitis . bowel obstruction .
• Skin and subcutaneous tissue : Dry skin, acne . rashes . itch . eczema . angioedema (Including swelling of the eyelids, perioral edema, swelling of the face, swelling of the pharynx and larynx, hereditary angioedema, oculo-respiratory syndrome, periorbital edema, swelling of the tongue, mouth, small intestine) alopecia .
• Musculo-skeletal system : myalgia . arthralgia , Violation of posture, pain in the extremities and back pain, muscle pain in the chest, muscular weakness Pain in the buttocks, neck pain.
• Kidneys   and urinary tract : Urinary incontinence, urinary retention.
• Reproductive system   and mammary gland : amenorrhea . spanomenorrhea . galactorrhea And sexy erectile dysfunction , Chest discomfort, abnormal ejaculation or deceleration, gynecomastia , Violation of menstruation, priapism .
• Liver : jaundice .
• Hearing : vertigo , earache.
• Lymphatic System   and hematology : anemia . neutropenia . thrombocytopenia . agranulocytosis .
• General disorders and complications at the injection site : asthenia . fatigue , Peripheral edema, hyperthermia Pain, injection site pain, pain during injection, flu-like condition, pain and discomfort in the chest, malaise, sluggishness, compaction, swelling and other reactions at the injection site; hypothermia . phlegmon . abscess . cyst . necrosis . hematoma . ulcer , Nodules (these events were reported as serious and sometimes require surgery).
• Laboratory findings : Abnormalities in body weight, increase in the concentration of prolactin in the blood, increasing activity alanine aminotransferase . aspartate aminotransferase   and GGT , Violations of the ECG, increase the amount of glucose and liver microsomal enzymes, lengthening the interval QT, monitoring glucose in urine.

Instructions for use rispolept

Tablets and solution rispolepta administered orally, regardless of the meal.

When treating   Schizophrenia to adults and children under 15 years old can assign rispolepta both in tablet form and in the form of an oral solution, in one or two steps in a starting daily dose of 2 mg.

On the second day of therapy should increase the daily dose of 4 mg and continue treatment while maintaining dosage at this level, or adjust it individually. Typically, the optimal daily dose ranges from 4-6 mg. In some cases, it may be correct more gradual increase in the dose and decrease in initial and maintenance doses.

The daily dosage of 10 mg of the above does not affect the effectiveness of treatment and may lead to extrapyramidal symptoms . Due unexplored effect dose Rispolept above 16 mg per day, the drug in large doses can not be taken.

In case of need for sedation in the therapy rispolepta be added benzodiazepines.

Data on the carrying out of treatment Schizophrenia   rispolept tablets for patients under 15 years, as well as an oral solution for patients under 13 years are not available.

When the possibility of treatment at doses less than 1 mg is prescribed oral solution.

Patients older than 13 years should start treatment with daily doses of 0, 5 mg with the reception the morning or evening. After every 24 hours may increase the dose by half, up to the recommended daily dose of 3 mg (for portability). Safety of treatment with a daily dose of 6 mg are not studied. When stable drowsiness, recommend acceptance 0, 25 mg twice a day.

For therapy behavioral disorders   patients with dementia   shows a starting daily dose of 0, 5 mg, with the possibility of an increase of 0, 25 mg every 48 hours until the maximum tolerated dose of 2 mg. In general, the optimal therapeutic dose is receiving 0, 5 mg 2 times per day. After reaching the optimal dose of the drug can be applied 1 time a day.

Treatment bipolar disorder at mania adults start with a daily dose of 2 mg or 3 mg per once. May increase the dose of 1 mg every day. The optimal daily dose for most patients is a dose of from 1 mg to 6 mg.

Patients over 10 years Rispolept prescribed in the starting daily dose of 0, 5 mg in the morning or in the evening. Every day the dose can be increased to 0, 5 mg - 1 mg per day, to achieve the recommended dose of 2, 5 mg (for portability). The optimal daily dose of 0, 5 mg to 6 mg. There is no information on the safety of the drug in a daily dose greater than 6 mg.

With Sustainable sleepiness I recommend to divide the daily dose into two doses.

There is no reliable information on the use of rispolept therapy bipolar disorder   in patients up to 10 years.

With behavioral disorders   recommend that patients weighing more than 50 kg, receiving daily doses of 0, 5 mg. Every two days, the dose can be increased to 0, 5 mg. The optimal dose for a larger number of patients - 1 mg per day, but may be at 0, 5 mg, or 1, 5 mg. Weighing 50 kg patient receiving the dose more preferably 0 to 25 mg per day, with possible increase of 0, 25 mg in 24 hours. The optimal daily dose usually equals 0, 5 mg, although some patients must take 0, 25 0 mg or 75 mg. Long-term treatment rispolept adolescence is conducted under strict medical supervision.
Use in pediatric patients under 5 years of age has not been studied.

In therapy autism   in children and adolescents, the daily dose picked individually. Initially, treatment administered in a dose of 0, 25 mg a day, with a weight up to 20 kg, and 0 5 mg per day with a weight of 20 kg and more.

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Terms of sale

Prescription.

Storage conditions

Shelf life

Cautions

 

  placebo

Furosemide   When combined reception and Furosemide With Furosemide dehydration    

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orthostatic hypotension antihypertensive agents .   Patients with   and dehydration

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Analogs

Synonyms

•   etc.

Babies

With alcohol

During pregnancy and lactation

pregnancy  

lactation.

neuroleptics

  schizophrenia  

Nervous System

Price  

Oral Solution  

Cost