Chlorprotine 15 mg Instructions for use. Chlorprotine - instructions for use

Chlorprotine Zentiva is a drug with an antipsychotic, moderate antidepressive and pronounced sedative effect.

Release form and composition

Dosage form Zentiva chlorproticsena - tablets coated with film shell: a round two-way form, orange (15 mg) or from light brown to light yellow (50 mg); The kernel color on the break - from almost white to white (in a carton 3 or 5 contour cellular packs of 10 pcs.).

1 tablet composition:

• active substance: hydrochloride chlorproticine - 15 or 50 mg;
• auxiliary components (15/50 mg): corn starch - 10 / 37.5 mg; Lactose monohydrate - 92/135 mg; sucrose - 10/20 mg; Calcium stearate - 1.5 / 3.75 mg; Talc - 1.5 / 3.75 mg;
• shell (15/50 mg): Gipromellos 2910/5 - 2.011 / 3,659 4 mg; Macroogol 6000 - 0.069 / 0.133 3 mg; Macroogol 300 - 0.49 / 0.916 6 mg; Talc - 1.43 / 2.419 4 mg; Aluminum varnish on the basis of the yellow sunset yellow dye (E110) - 1/0 mg; Titanium dioxide - 0.342 3 mg.

Pharmacological properties

Pharmacodynamics

Chlorprotine - Neuroleptic, Tioksanthen derivative. It has an antipsychotic, moderate antidepressive and pronounced sedative effect. The antipsychotic effect is associated with the blocking effect of chlorprotine on dopamine receptors. Also with blockade of these receptors are associated with analgesic and anti-metic properties of the drug. Chlorprotine is capable of blocking A1-adrenoreceptors, 5-HT2 receptors, as well as H1-histamine receptors, which determines its adrenoblocking hypotensive and antihistamine effect.

Pharmacokinetics

When orally admission, the biological accessibility of chlorprotic is about 12%. After taking inside, it is absorbed well and quickly. In the liver and intestinal walls is subject to preserved metabolism. It has the effect of the first passing through the liver.

Chloroprietary penetrates through a placental barrier and in breast milk.

The removal is carried out by intestines and kidneys: chlorprotine - 29%, chloroprotine sulfoxide - 41%.

The half-life is ranging from 8 to 12 hours.

Indications for use

The following states and diseases are indications of chlorproticsene:

• insomnia;
• psychosis, including manic states and schizophrenia, accompanied by psychomotor excitation, anxiety and award;
• depressive states, neurosis, psychosomatic disorders;
• abstineent syndrome with alcoholism and drug addiction;
• violation of behavior in children;
• confusion of consciousness, hyperactivity, excitement, irritability in elderly patients;
• pain (combined with analgesics).

Contraindications

Absolute:

• bone marrow oppression;
• pathological blood changes;
• feochromocytoma;
• lactose intolerance or fructose, glucose-galactose malabsorption or lactase deficiency, the deficiency of isomaltase / sacraise (the lactose and sucrose) are included in the chlorprichnysen);
• depression Central nervous system any origin (including associated with the admission of alcohol, opiates or barbiturates);
• vascular collapse;
• comatous states;
• age up to 6 years;
• individual intolerance to the components of the drug, including phenothiazines.

Relative (chlorprotine zentiv is appointed under medical control):

• a tendency to collapsam;
• diabetes;
• glaucoma (including predisposition to its occurrence);
• urine delay and risk of its development clinical manifestations prostate hyperplasia;
• renal / liver failure;
• ray's syndrome;
• parkinson's disease (associated with the enhancement of extrapyramidal disorders);
• pronounced cardiovascular and respiratory failure associated with acute infectious diseases, asthma or emphysemic lungs (there is a high risk of transient increase arterial pressure);
• pronounced atherosclerosis of brain vessels;
• ulcerative disease of the stomach and duodenum;
• epilepsy (associated with the probability of participating attacks as a result of a decrease in a convulsive threshold);
• pregnancy and lactation period.

Instructions for the use of chlorprotine Zentiva: method and dosage

Chlorprotine Zentiv is designed for oral reception. Perhaps long-term therapy is possible, since the drug of the development of addiction or drug dependence does not cause.

• psychoses, including manic states and schizophrenia: the initial daily dose - 50-100 mg. Gradually, the dose increases to the achievement of the optimal effect, usually 300 mg. The average supporting dose is from 100 to 200 mg per day. Maximum - 600 mg per day. Usually, a daily dose is divided into 2-3 receptions, a smaller part should be taken in the daytime, in the evening;
• an abstitent syndrome in drug addiction and alcoholism: a daily dose - 500 mg in 2-3 reception. The duration of application is 7 days. After improving the state, the dose is gradually reduced. Supporting daily dose is in range from 15 to 45 mg. Reception of chlorprotine zentiv allows to stabilize the state, reduce the likelihood of the development of the next binge;
• hyperactivity, irritability, excitation, confusion of consciousness in elderly patients: from 15 to 90 mg per day in 3 receptions;
• violation of behavior in children: 0.5-2 mg / kg;
• neurosis, depressive states, psychosomatic disorders: daily dose - 90 mg in 2-3 receptions;
• insomnia: 15-30 mg 60 minutes before sleep;
• pain (in combination with analgesics): 15-300 mg per day.

Side effects

Possible adverse reactions (\u003e 10% - very often;\u003e 1% and< 10% – часто; > 0.1% I.< 1% – нечасто; > 0.01% I.< 0,1% – редко; < 0,01% – очень редко):

• cardiovascular system: Ortostatic hypotension (especially when applying high doses of chloroprotine zentiv), transient changes q-T interval on electrocardiogram and tachycardia;
• nervous system: dizziness, increased fatigue, drowsiness, psychomotor inhibition, lightweight extrapyramidal hypokinetic-hypertonic syndrome, acactic (for the first 6 hours after taking), dystonic reactions persistent late dyskinesia (violations usually appear at the beginning of therapy and often as it continues independently disappear); rarely - late dystonia, malignant neuroleptic syndrome;
• endocrine system: rarely dysmenorrhea; With prolonged use of high doses of chlorprotine zentiv - Galaconteo, diabetes mellitus, gynecomastia, potency / libido reduction, increased sweating, a change in carbohydrate exchange, an increase in appetite, an increase in body weight;
• digestive system: xerostomy (wearing a transit character); rarely - constipation, cholestatic jaundice (with a long course in particular with the use of high doses, the most likely development of the violation between 2 and 4 weeks of therapy);
• blood formation organs: rarely - agranulocytosis (violation is most often evolving for 4-10 weeks of treatment); In isolated cases - transient benign leukopenia and hemolytic anemia;
• feeling organs: clouding of lens / cornea with a possible impairment of vision, paresis accommodation (arises at the beginning of treatment and disappears as the chloroprotic session of Zentiva continues);
• others: skin rash, urine delay, dermatitis, blood tides to face, cancellation syndrome, photosensitization.

Overdose

Basic symptoms: drowsiness, hyper- or hypothermia, cramps, coma, shock, extrapyramidal symptoms.

Overdose is usually assigned symptomatic and supporting therapy. As possible in a shorter time, stomach washing, reception activated coal. Events aimed at maintaining the work of cardiovascular and respiratory systems are also shown. Apply epinephrine should not be applied, as this may cause a subsequent decrease in blood pressure. Extrapyramidal disorders can be stopped by bieperid, seizures - diazepam.

special instructions

Reception of the drug can lead to false hyperbilirubinemia indicators, false positive results When conducting an immunobiological urine test for pregnancy, changing the Qt interval on an electrocardiogram.

Alcohol abuse enhances the oppression of the central nervous system.

Most often, the development of dystonic reactions is observed in children and young patients. As a rule, they appear at the beginning of therapy and can weaken within 24-48 hours after the cessation of taking chlorprotic sewage.

In the first few days of treatment, parquinsonic extrapyramidal effects may be occurred, but usually their frequency increases as the dose increases; More often, their appearance is celebrated in older patients and older children.

Late dyskinesia at the beginning of treatment is dose-dependent, but the frequency of it can increase with a long course and as the total dose is achieved. After cancellation of the chlorprotine zentiv, the violation can persist.

The risk of developing extrapyramidal and hypotensive reactions in adolescents is higher than in adult patients.

During the application of chlorproticsena, Zentiv requires a blood test and definition leukocyte formula, control of the indicators of the hepatic function, conducting an ophthalmological research, as well as careful observation in order to identify early signs Late dystonia and disconesia.

The occurrence of malignant neuroleptic syndrome is possible at any time of therapy, but more often its development is noted shortly after the start of reception of the chlorproticsena of Zentiv or after the patient's translation from the other neuroleptic, during combined application With other psychoactive preparations or after a dose increases.

From taking ethanol, as well as exposure to insolation and extreme high temperatures It is recommended to refrain.

Cancel therapy should be gradually, it will reduce the likelihood of cancellation syndrome.

Impact on the ability to control vehicles and complex mechanisms

During the reception of the chlorproticsena, the patients must be careful when managing motor vehicles.

Application during pregnancy and lactation

According to the instructions, chlorprotine zentiv during pregnancy / lactation to apply, if possible, should not be applied.

Childcare

Therapy chlorprichny zentiva patients under 6 years old is contraindicated.

With violations of the kidney function

Chlorprotine Zentiv according to the testimony with accompanying renal failure should be applied under medical supervision.

When violations of the liver function

Chlorprotine Zentiva Ply liver failure should be applied under medical supervision.

Medicinal interaction

• ethanol and ethanol-containing drugs, anesthetics, opioid analgesics, sedatives, sleeping pills, neuroleptic agents: the inhibitory effect of chlorprotine on the central nervous system is amplified;
• antiepileptic means (in patients with epilepsy): the threshold of convulsive activity is reduced (additional dose correction is required);
• m-cholinoblocators, antiforms and anti-parkinsonic drugs: the anticholinergic effect of chloroprotic is intensified;
• phenothiazines, metoclopramide, haloperidol, reserpine: An extrapyramidal disorders may be noted;
• levodopa: its effectiveness is reduced;
• phenylephrine: a vasoconstrictor action can decrease;
• dopamine (in high doses), epinephrine and ephedrine: peripheral vesseloring effect can be perverted;
• epinephrine: arterial hypotension and tachycardia may develop;
• hypotensive means: their action is enhanced;
• county: Risk of development adverse Reactions from the side of the heart increases;
• guanethidine: hypotensive effect decreases;
• bromocriptine: hyperprolactinemia may develop, which requires the correction of the dosing mode;
• overtoxic medicinal products (Especially antibiotics): chlorprotine can mask the symptoms of the isotoxicity (in the form of noise in the ears, dizziness).

Analogs

Analogue of chlorproticsena Zentiv is Trucal.

Terms and conditions of storage

Store at temperatures up to 25 ° C. Take care of children.

Shelf life - 3 years.

One tablet covered with film shell, 15 mg contains:

active substance: chlorprotine hydrochloride - 15 mg;

corn starch - 10 mg, monohydrate lactose - 92 mg, sucrose - 10 mg, calcium stearate - 1.5 mg, talc - 1.5 mg; film sheath: Hyprocellose 2910/5 - 2.011 mg, macrogol 6000 - 0.069 mg, macrogol 300 - 0.49 mg, talc - 1.43 mg, aluminum varnish based on the yellow sunset (E 110) dye - 1 mg.

One tablet covered with film shell, 50 mg contains :

active substance: chloroprotic hydrochloride - 50 mg;

auxiliary substances: kernel: Corn starch - 37.5 mg, monohydrate lactose - 135 mg, sucrose - 20 mg, calcium stearate - 3.75 mg, talc - 3.75 mg; film sheath: Hyprocellose 2910/5 - 3,6594 mg, macrogol 6000 - 0.1333 mg, macrogol 300 - 0.9166 mg, Talc - 2,4194 mg, titanium dioxide - 0.3423 mg, iron dye yellow - 0,0290 mg .

Tablets 15 mg: Round, double-screw tablets covered with a film shell of orange. Flaw view: core from white to almost white.

Tablets 50 mg: Round, double-screw tablets covered with film shell from light brown to light yellow. Flaw view: core from white to almost white.

Chloroprietic is a neuroleptic, Tioksanten derivative. It has an antipsychotic, pronounced sedative and moderate antidepressive effect.

Pharmacodynamics

The antipsychotic effect of chloroprotine is associated with its blocking effect on dopamine receptors.

Unlike other thiocantenans, has pronounced sedative effectsince he suppresses stimulation reticular formation The trunk of the brain, and also acts as a controversial means by inhibiting chemoreceptors in the spinal cord. Analgesic effect of the drug is also associated with the blockade of these receptors.

In rare cases, the development of malignant neuroleptic syndrome (hyperthermia, rigidity, akinesia, coma) is possible, in this situation it is necessary to immediately stop taking chlorproticsena and begin symptomatic treatment in the intensive care unit or branch of anesthesiology and resuscitation.

The so-called late (chronic - late) discsion may occur during a long-term reception of the drug (especially in patients over 65 years old) as a symptom increased sensitivity Dopaminergic system (unconscious choreoaththyoid movements are prognostically unfavorable). An additional reception of neuroleptic drugs masks symptoms, so it is necessary to closely monitor patients.

There is also a fairly high risk of epileptiform seizures.

In rare cases, anxiety enhancement can be observed, especially in patients with manic and schizoaffective disorders (in these cases it is better to go to treatment with neuroleptics with a rapidly developing effect, such as haloperidol).

The frequency of adverse reactions below was determined according to the classification of the World Health Organization: very often (≥ 1/10); Often (≥ 1/100 and< 1/10); нечасто (≥ 1/1000 и < 1/100); редко (≥ 1/10000 и < 1/1000); очень редко (< 1/10000), частота неизвестна (не может быть подсчитана на основании имеющихся данных).

Violations from the nervous system: Very often - drowsiness, dizziness; often - headache, dystonia; Infrequently - acatisia, late dyskinesia, Parkinsonism, convulsions; seldom - epileptic seizures; Very rarely - malignant neuroleptic syndrome (hyperthermia, rigidity, akinesia, coma).

Psyche violations: often - insomnia, nervousness, assessment, decline in libido.

Disorders of the respiratory system, organs chest and mediastinum: rarely - nasal congestion, shortness of breath; rarely - bronchial asthma, Maudan's swelling.

Heart disorders: Often - tachycardia (especially after sudden cessation of treatment), heartbeat; Rarely - the elongation of the Qt interval on the ECG, ventricular arrhythmia (including ventricular fibrillation, ventricular tachycardia, pyruette ventricular tachycardia ( torsade de Pointes.) and sudden death); Very rarely - bradycardia, heart stop.

Vessel violations: often - orthostatic hypotension; Infrequently - decrease in blood pressure (blood pressure), "tides" blood to skin cover; very rare - venous thromboembolism; Frequency of unknown - thromboembolism pulmonary artery, deep veins thrombosis.

Disorders from the gastrointestinal tract: very often - dryness of the oral mucosa, increased salivation; Often - constipation, dyspepsia, nausea; Infrequently - vomiting, diarrhea.

Violations by the liver and biliary tract: Very rarely - jaundice, cholestatic jaundice (based on an immunopathological reaction).

Disorders from the skin and subcutaneous fabrics: Often - increased sweating, infrequently skin rash, skin itch, dermatitis, photosensitivity reactions; Rarely erythema, eczema.

Disorders of the skeletal muscular and connective tissue : often - Malgy; infrequently muscular rigidity; Very rarely - a lupus-like syndrome.

Kidney violations and urinary tract: Infrequently - impaired urination, urine delay; Very rarely - hyperikozuria.

Pregnancy, postpartum and perinatal states: The frequency is unknown - the "cancel" syndrome in newborns (see section "Application during pregnancy and in breastfeeding period").

Disorders from the genital organs and breasts: infrequently - ejaculation disorder, erectile dysfunction; rarely - gynecomastia, galathery, amenorrhea; The frequency is unknown - Priapism.

Disorders from the endocrine system: rarely hyperprolactinemia.

Disturbance of metabolism and nutrition: often - elevated appetite, increase in body weight; infrequently - decreased appetite, decrease in body weight; Rarely - hyperglycemia, violation of glucose tolerance.

Violations of the organ of vision: Often - violation of accommodation, violation of vision; Infrequently - Okulo-boil crisis (seizures of the gaze); Very rarely (after long-term treatment with high doses) - pigment retinit, clouding of lens, corneal deposits (precipitates).

Blood violations and lymphatic system: rarely - thrombocytopenia, leukopenia, neutropenia, agranulocytosis; Very rarely - hemolytic anemia, thrombocytopenic purpura, pancytopenia, eosinophilia.

Violations from immune system : rarely - hypersensitivity reactions, anaphylactic reactions.

General disorders and disorders at the injection site: often - asthenia, increased fatigue; Rarely - violation of thermoregulation.

Laboratory and instrumental data: Infrequently - deviation from the normlaboratory liver function indicators.

Syndrome "Cancellation": A sharp cessation of treatment with chlorproticine may be accompanied by the "cancellation" syndrome. The most common symptoms are nausea, vomiting, anorexia, diarrhea, rhinora, sweating, Malgy, parrestzia, insomnia, anxiety, anxiety and excitement. Patients may also be observed vertigo, changing the sensations of heat and cold, tremor limbs. Symptoms usually occur within 1-4 days after cancellation and decrease after 7-14 days.

Symptoms : drowsiness, coma, cramps, shock, extrapyramidal disorders, hyperthermia / hypothermia, inhibition of breathing, resistant decrease in blood pressure (may occur in a few hours and continue 2-3 days), tachycardia, myiosis. In severe cases - a violation of the kidney function. Changes to ECG parameters, Qt interval lengthening, pyruette stomatricular Tachycardia (Torsade de Pointes), stopping the heart and ventricular arrhythmias were observed with simultaneous overdose with drugs affecting the heart.

Treatment : symptomatic and supportive. As early after the reception, stomach washed must be made, the use of activated carbon is recommended. Must be taken aimed at maintaining respiratory activities and cardiovascular systems. Do not use (adrenaline), because This may lead to a subsequent decrease in blood pressure. Corps can be stopped with diazepam, and extrapyramidal disorders bieperid.

Dose from 2.5 to 4 g can be lethal (in infants approximately 4 mg / kg). Some adults survived after receiving 10 g, a three-year-old child survived after receiving 1 g.

Combinations requiring compliance with precautions

Chloroprietary can enhance the sedative effect of alcohol and the effects of barbiturates and other substances depressing the CNS (such as antidepressants, anti-epileptic preparations, analgesics, muscle relaxants, neuroleptics, antihistamines of the first generations, etc.).

Neuroleptics can increase or reduce the effect of antihypertensive drugs; The anti-hypertensive effect of guanetidine and is similar to the acting drugs.

The simultaneous use of neuroleptics and lithium preparations increases the risk of neurotoxicity.

Tricyclic antidepressants and neuroleptics mutually inhibit each other's metabolism.

Chloroprietary can reduce the effect of levodopes and adrenergic drugs and enhance the effect of anticholinergic agents.

With the simultaneous use of metoclopramid, piperazine, phenothiazines, haloperidol and reserpine increases the risk of extrapyramidal symptoms.

The antihistamine effect of chlorprotine can reduce or eliminate the symptoms of disulfiram-ethanol reaction.

The increase in the Qt interval to the ECG associated with the treatment of neuroleptics may be exacerbated by simultaneously receiving other drugs that significantly increase the Qt interval.

The simultaneous use of chlorprotic is contraindicated with the following drugs (See "Contraindications" section):

Antiarrhythmic agents I and III class (for example, dfethylide)

Some antipsychotic drugs (for example,)

Some antibiotics from the group of macrolides (for example,)

Some antihistamines (for example, terphelanadine,)

Some antibiotics from the quinolon group (for example,)

Cypris and drugs lithium

Also, drugs should not be used, which cause electrolyte disorders, such as tiazide diuretics (hypokalemia), and drugs that increase the concentration of chlorprotine in the blood plasma, as this may increase the risk of elongation of the Qt interval and the occurrence of malignant arrhythmias (see Contraindications section) .

Neuroleptics are metabolized by the isoenzymes of the cytochrome R450 system in the liver. Preparations that inhibit CYP 2D 6 isoenzymes (for example, Mao inhibitors, oral contraceptives, to a lesser extent, or), can increase the concentration of chlorprotine in the blood plasma.

The simultaneous use of chlorofriter with cholin bockers enhances the anticholinergic effect.

Chloroprietary can block α -adrenergic effects of epinephrine (adrenaline), which can lead to a decrease in blood pressure and tachycardia during co-use.

Chloroprietary also reduces the threshold of convulsive readiness, which may cause the need to correct the dose of anti-epileptic drugs.

In the treatment of chlorproticsene, the concentration of prolactin in the blood plasma can increase - when applied, a dose correction may be needed in combination with bromocriptine.

Thioxanthenes can mask the isotoxic effect of other drugs (noise in the ears, Vertigo TP).

Patients receiving long-term therapy by the drug, especially in high doses, should be carefully observed by a specialist, while periodically it is necessary to assess the possibility of reducing the maintenance dose.

Malignant neuroleptic syndrome

The possibility of the development of malignant neuroleptic syndrome (hyperthermia, muscle rigidity, an unstable level of consciousness, instability of the vegetative nervous system) exists when using any neuroleptics. In patients with already existing syndrome of organic brain damage, mental retardation, abuse of opiates and alcohol, are more often observed fatal outcomes.

Treatment : Termination of treatment with neuroleptics. Symptomatic treatment and carrying out general supportive events. May be useful application Danterlena and bromocriptine.

Symptoms can be maintained during the week and more after taking neuroleptics.

Glaucoma

The sharp seizures of glaucoma due to the expansion of the pupil can occur in patients with rare fine-chamber syndrome and in patients with a narrow corner of the chamber.

Interlining intervalQt.

Due to the risk of the emergence of malignant arrhythmias, the drug should be used in patients with cardiovascular diseases in history or with cases of elongation of the Qt interval in a family history.

Before the start of treatment, an ECG study should be carried out.

The use of the drug is contraindicated in case the QTC interval exceeds 450 ms in men or 470 ms in women at the beginning of treatment (see Contraindications section). During treatment, the need for ECG monitoring should be assessed on an individual basis. During the treatment period, a dose should be reduced if the Qt interval will increase, and should stop therapy if the QTC interval is\u003e 500 ms.

Like others psychotropic means, the drug may influence PA indicators of glycemia in patients with diabetesthat may require the correction of antidiabetic therapy (insulin or hypoglycemic drugs for intake).

Increased sensitivity to phenothiazins can mean the presence of high sensitivity to thiocaanthen.

Venous thromboembolia

When applying antipsychotic drugs, cases of venous thromboembolism (VTE) were noted. Since patients gaining treatment for neuroleptics often have acquired risk factors for the development of venous thromboembolism, all possible RISE risk factors must be identified before and during treatment, as well as carrying out preventive measures.

Patients older than 65 years

According to randomized placebo-controlled studies in the population of patients with dementia, the purpose of some atypical neuroleptics was accompanied by approximately 3-fold increase in the risk of cerebrovascular undesirable phenomena.

The risk increase mechanism is unknown. Such risk increase cannot be excluded for other neuroleptics and other groups of patients. In patients with risk factors, a stroke drug should be used with caution.

The use of the drug can lead to a false-positive result during the immunobiological dough urine for pregnancy, false hyperbilirubinemia indicators, as well as a change in the Qt interval on an electrocardiogram.

Priapism

With the use of antipsychotic drugs that block α-adrenoreceptors, cases of prioxy were observed, and this phenomenon is possible when applying the drug. Heavy cases of priapism may require medical intervention. Patients need to inform about the need to apply for medical help In case of signs and symptoms of priapism.

During treatment, it is necessary to refrain from the reception of substances containing, the effects of extremely high temperatures (risk of development heat strike), excess insolation.

In order to avoid the development of the "Cancellation" syndrome, cease treatment with the drug must be gradually.

Lactose and Sakhares

Tablets of the drug chloroprotic Sanofi contain lactose and sucrose. Patients with rare hereditary lactose intolerance or fructose, lactase deficiency or glucose-galactose malabsorption, a deficiency of sacrase / isomaltase Reception of the drug is contraindicated.

The drug chlorophoticine sanofi in 15 mg dosage contains aluminum varnish based on the yellow sunset yellow (E 110) dye, which can cause allergic reactions.

Chlorproticsene has a sedative effect, so during treatment, caution should be taken when driving and occupying other potentially hazardous species Activities requiring increased concentration of attention and speed of psychomotor reactions. Patients should be prevented in advance about the possible violation of the ability to manage vehicles and working with mechanisms.

Tablets coated with film shell, 15 mg and 50 mg.

10 tablets in a PVC blister / AL.

3 or 5 blisters along with instructions for use in a cardboard pack.

At a temperature not higher than 25 ° C.

Keep out of the reach of children.

Do not apply after the expiration date indicated on the package.