Klopiksol tablets p / o 2mg, No. 50

Acute and chronic schizophrenia and other psychotic disorders, especially with hallucinations, paranoid delusions and impaired thinking, as well as states of agitation, increased anxiety, hostility or aggressiveness.

Manic phase of manic-depressive psychosis.

Agitation and other conduct disorders in mentally retarded patients.

The tablets are taken orally: swallowed with water.

Doses of the drug should be selected individually, depending on the patient's condition. As a rule, initially small doses should be used (from 2-10 mg and more, depending on the indication), which are then rapidly increased to optimal, depending on the clinical effect. A maintenance dose can be administered once daily at bedtime.

Acute attack of schizophrenia, other acute psychotic disorders, severe agitation and mania.

Usually 10-50 mg / day.

In severe disorders and conditions of moderate severity, the initial dose of 20 mg / day may, if necessary, be increased by 10-20 mg after 2-3 days to 75 mg per day or more. The maximum single dose is 40 mg. The maximum daily dose is 150 mg.

Chronic psychotic conditions in schizophrenia and other chronic psychoses.

The maintenance dose is 20-40 mg / day.

Agitation in mentally retarded patients.

Usually 6-20 mg / day. If necessary, the dose can be increased to 25-40 mg / day.

Elderly patients:

Elderly patients should be prescribed the minimum dose from the possible dose range (2-6 mg and higher).

Decreased liver function:

Clopixol should be used with caution in patients with hepatic impairment. Patients with impaired liver function should be prescribed half of the recommended doses, and, if possible, monitor the level of the drug in the blood serum.

Reduced kidney function:

Clopixol can be administered in normal doses to patients with reduced renal function.

The active substance is zuclopenthixol dihydrochloride 2.364 mg / 11.82 mg / 29.55 mg, which corresponds to 2 mg / 10 mg / 25 mg of zuclopenthixol;

excipients - potato starch 22.2 mg / 29.2 mg / 31.6 mg, lactose monohydrate 17.4 mg / 21.6 mg / 22.0 mg, microcrystalline cellulose 9.0 mg / 13.5 mg / 18 , 0 mg, copovidone 3.0 mg / 4.5 mg / 6.0 mg, glycerol 85% 1.2 mg / 1.8 mg / 2.4 mg, talc 4.2 mg / 6.3 mg / 8 , 4 mg, hydrogenated castor oil 0.48 mg / 0.72 mg / 0.96 mg, magnesium stearate 0.42 mg / 0.63 mg / 0.84 mg.

Sheath: hypromellose 5 1.37 mg / 2.05 mg / 2.74 mg, macrogol 6000 0.274 mg / 0.411 mg / 0.548 mg, titanium dioxide (E171) 0.445 mg / 0.479 mg / 0.091 mg, iron oxide red (E172) 0.011 mg / 0.205 mg / 0.822 mg.

Hypersensitivity to zuclopenthixol or any of the excipients.

Known hypersensitivity to drugs of the thixanthene group. Acute intoxication with ethanol, barbiturates and opiates.

Collapse, depression of consciousness of any origin, coma, suspected or established subcortical brain damage.

Hereditary galactose intolerance, lactase deficiency or impaired absorption of glucose and galactose.

Carefully:

Organic brain diseases, mental retardation, seizure disorders, liver failure, history of cardiovascular disease, including prolongation of the QT interval, bradycardia <50 beats per minute, recent acute myocardial infarction, decompensated heart failure, arrhythmia, hypokalemia, hypomagnesemia and genetic predisposition to such conditions, the presence of risk factors for stroke (including acute arteriosclerosis), parkinsonism, opioid and alcohol dependence; pregnancy, breastfeeding period; children and adolescents up to 18 years of age (due to insufficient clinical data).

Dosage form:

Film-coated tablets.

Composition:

The active substance is zuclopenthixol dihydrochloride 2.364 mg / 11.82 mg / 29.55 mg, which corresponds to 2 mg / 10 mg / 25 mg of zuclopenthixol;

excipients - potato starch 22.2 mg / 29.2 mg / 31.6 mg, lactose monohydrate 17.4 mg / 21.6 mg / 22.0 mg, microcrystalline cellulose 9.0 mg / 13.5 mg / 18 , 0 mg, copovidone 3.0 mg / 4.5 mg / 6.0 mg, glycerol 85% 1.2 mg / 1.8 mg / 2.4 mg, talc 4.2 mg / 6.3 mg / 8 , 4 mg, hydrogenated castor oil 0.48 mg / 0.72 mg / 0.96 mg, magnesium stearate 0.42 mg / 0.63 mg / 0.84 mg.

Sheath: hypromellose 5 1.37 mg / 2.05 mg / 2.74 mg, macrogol 6000 0.274 mg / 0.411 mg / 0.548 mg, titanium dioxide (E171) 0.445 mg / 0.479 mg / 0.091 mg, iron oxide red (E172) 0.011 mg / 0.205 mg / 0.822 mg.

Description:

2 mg - pale pink, round, biconvex film-coated tablets. Cross-sectional color - white;

10 mg - round, biconvex, pinkish-brown film-coated tablets. Cross-sectional color - white;

25 mg - round, biconvex, red-brown film-coated tablets. The cross-sectional color is white.

Pharmacotherapeutic group:

Antipsychotic (neuroleptic)

Pharmacodynamics:

Clopixol is an antipsychotic drug (neuroleptic) of the thioxanthene group.

The antipsychotic effect of neuroleptics is associated with blockade of dopamine receptors, and possibly also blockade of 5-HT (5-hydroxytryptamine) receptors.

In vitro,
zuclopenthixol has a high affinity for dopamine D1 and D2 receptors, as well as alpha1-adrenergic receptors and serotonin 5-HT2 receptors, but does not have an affinity for muscarinic cholinergic receptors. The drug has a weak affinity for the H1 histamine receptors, and does not have alpha2-adrenergic blocking activity. In vivo, affinity for D2 receptors predominates over affinity for D1 receptors.

Like most antipsychotics,
zuclopenthixol increases serum prolactin levels.

Zuclopenthixol is indicated for the treatment of acute and chronic psychoses and for the treatment of mentally retarded patients with hyperactive and aggressive behavior.

In addition to significantly weakening or completely eliminating the main symptoms of schizophrenia, such as hallucinations, delusions and thinking disorders,
zuclopenthixol also has a pronounced effect on the accompanying symptoms - hostility, suspicion, agitation and aggressiveness.

Zuclopenthixol has a transient, dose-dependent sedative effect. The rapid onset of sedation at the start of therapy is usually an advantage in the treatment of acute psychoses. Tolerance to the nonspecific sedative effect of the drug develops rapidly. The specific inhibitory effect of Clopixol is especially beneficial in the treatment of patients with agitation, anxiety, hostility or aggressiveness.

Pharmacokinetics:

The oral bioavailability of zuclopenthixol is about 44%. The maximum serum concentration is reached after about 4 hours.

Apparent volume of distribution (Vd)? is about 20 l / kg. Plasma protein binding is about 98-99%.

Zuclopentixol slightly penetrates the placental barrier and is excreted in small quantities in breast milk. The half-life is approximately 20 hours. Metabolites have no neuroleptic activity and are excreted mainly in the feces and, in part, in the urine.

With maintenance therapy in patients with schizophrenia with mild or moderate severity of the disease, a minimum (that is, measured immediately before administration) level of drug concentration in serum of 2.8-12 ng / ml (7-30 nmol / L) is recommended.

Indications for use:

Acute and chronic schizophrenia and other psychotic disorders, especially with hallucinations, paranoid delusions and impaired thinking, as well as states of agitation, increased anxiety, hostility or aggressiveness.

Manic phase of manic-depressive psychosis.

Agitation and other conduct disorders in mentally retarded patients.

Contraindications:

Hypersensitivity to zuclopenthixol or any of the excipients.

Known hypersensitivity to drugs of the thixanthene group. Acute intoxication with ethanol, barbiturates and opiates.

Collapse, depression of consciousness of any origin, coma, suspected or established subcortical brain damage.

Hereditary galactose intolerance, lactase deficiency or impaired absorption of glucose and galactose.

Carefully:

Organic brain diseases, mental retardation, seizure disorders, liver failure, history of cardiovascular disease, including prolongation of the QT interval, bradycardia <50 beats per minute, recent acute myocardial infarction, decompensated heart failure, arrhythmia, hypokalemia, hypomagnesemia and genetic predisposition to such conditions, the presence of risk factors for stroke (including acute arteriosclerosis), parkinsonism, opioid and alcohol dependence; pregnancy, breastfeeding period; children and adolescents up to 18 years of age (due to insufficient clinical data).

Pregnancy and lactation:

During pregnancy, Clopixol should be used only if the intended benefit to the mother outweighs the potential risk to the fetus.

Newborns whose mothers took antipsychotic drugs late in pregnancy or during labor may show signs of intoxication, such as lethargy, tremors, and hyperexcitability. In addition, these newborns have a low Apgar score.

During treatment with Clopixol, breastfeeding is allowed if it is clinically necessary. However, it is recommended that the newborn be monitored, especially in the first 4 weeks after birth.

Method of administration and dosage:

The tablets are taken orally: swallowed with water.

Doses of the drug should be selected individually, depending on the patient's condition. As a rule, initially small doses should be used (from 2-10 mg and more, depending on the indication), which are then rapidly increased to optimal, depending on the clinical effect. A maintenance dose can be administered once daily at bedtime.

Acute attack of schizophrenia, other acute psychotic disorders, severe agitation and mania.

Usually 10-50 mg / day.

In severe disorders and conditions of moderate severity, the initial dose of 20 mg / day may, if necessary, be increased by 10-20 mg after 2-3 days to 75 mg per day or more. The maximum single dose is 40 mg. The maximum daily dose is 150 mg.

Chronic psychotic conditions in schizophrenia and other chronic psychoses.

The maintenance dose is 20-40 mg / day.

Agitation in mentally retarded patients.

Usually 6-20 mg / day. If necessary, the dose can be increased to 25-40 mg / day.

Elderly patients:

Elderly patients should be prescribed the minimum dose from the possible dose range (2-6 mg and higher).

Decreased liver function:

Clopixol should be used with caution in patients with hepatic impairment. Patients with impaired liver function should be prescribed half of the recommended doses, and, if possible, monitor the level of the drug in the blood serum.

Reduced kidney function:

Clopixol can be administered in normal doses to patients with reduced renal function.

Side effect:

Most of the side effects are dose related. The incidence of side effects and their intensity are most pronounced in the early stages of treatment and decrease as therapy continues.

Information on the incidence of side effects is presented on the basis of literature data and spontaneous reports. Frequency is indicated as: very often (? 1/10), often (from? 1/100 to <1/10), infrequently (from 1/1000 to <1/100), rarely (from? 1/10000 to <1 / 1000), very rare (<1/10000), or unknown (cannot be estimated from existing data).

From the nervous system: very often - drowsiness, akathisia, hyperkinesia, hypokinesia; often - tremor, dystonia, muscle hypertonia, dizziness, headache, paresthesia, attention disorders, amnesia, gait disturbances; infrequently - tardive dyskinesia, hyperreflexia, parkinsonism, syncope, speech disorders, dyskinesia, ataxia, hypotonia, convulsive disorders, migraine; very rarely - neuroleptic malignant syndrome.

From the side of mental activity: often - insomnia, depression, anxiety, nervousness, agitation, unusual dreams, decreased libido; infrequently - apathy, increased libido, nightmares, confusion.

From the side of the cardiovascular system: often - tachycardia, palpitations; infrequently - lowering blood pressure, 'hot flashes'; rarely - an extended QT interval on the electrocardiogram; very rarely - venous thromboembolism.

From the side of the organs of vision: often - violation of accommodation, visual impairment; infrequently - mydriasis (pupil dilation), involuntary movement of the eyeballs.

From the organ of hearing and labyrinth: often - dizziness; infrequently - hyperacusis, tinnitus.

From the respiratory system: often - shortness of breath, nasal congestion.

From the digestive system: very often - dry mouth; often - increased salivation, constipation, vomiting, indigestion, diarrhea; infrequently - abdominal pain, nausea, flatulence.

Metabolic and nutritional disorders: often - increased appetite, weight gain; infrequently - decreased appetite, weight loss; rarely - hyperglycemia, impaired glucose tolerance, hyperlipidemia.

Reproductive system disorders: infrequently - ejaculation disorders, erectile dysfunction, orgasm disorders in women, vulvovaginal dryness; rarely - galactorrhea, gynecomastia, amenorrhea, priapism.

From the urinary system: often - painful urination, urinary retention, polyuria.

Hepatic and hepatobiliary disorders: infrequently - changes in laboratory parameters of liver function; very rarely - cholestatic hepatitis, jaundice.

From the endocrine system: rarely - hyperprolactinemia.

From the circulatory and lymphatic system: rarely, thrombocytopenia, neutropenia, leukopenia, agranulocytosis.

On the part of the skin and subcutaneous tissue: often - hyperhidrosis, itching; infrequently - photosensitivity, pigmentation disorders, seborrhea, skin rash, dermatitis, purpura.

From the musculoskeletal system: often - myalgia; infrequently - muscle rigidity, trismus, torticollis.

From the immune system: rarely - hypersensitivity, anaphylactic reactions.

From the side of the body as a whole: often - asthenia, fatigue, malaise, pain; infrequently - thirst, hypothermia, pyrexia.

Extrapyramidal disorders can occur, especially in the early stages of treatment. In most cases, these side effects are successfully controlled by dose reduction and / or antiparkinsonian medications. However, the routine use of antiparkinsonian drugs to prevent side effects is not recommended. They do not relieve tardive dyskinesia and may worsen them. A dose reduction or, if possible, discontinuation of zuclopenthixol therapy is recommended. For persistent akathisia, benzodiazepines or
propranolol may be helpful .

When taking zuclopenthixol, the following side effects were also reported that occur when taking other antipsychotics: in rare cases, prolongation of the QT interval, ventricular arrhythmias - tachycardia and fibrillation, sudden death, cardiac arrest and the development of paroxysms of ventricular tachycardia (torsade des pointes).

Abrupt discontinuation of zuclopenthixol may be accompanied by withdrawal reactions. The most common symptoms are nausea, vomiting, anorexia, diarrhea, rhinorrhea, sweating, myalgia, paresthesia, insomnia, nervousness, anxiety, and agitation. Patients may also experience dizziness, sensations of warmth and coldness, and tremors. Symptoms usually begin within 1-4 days after withdrawal and improve within 7-14 days.

Overdose:

Symptoms:

Drowsiness, coma, movement disorders, convulsions, shock, hyperthermia / hypothermia.

ѕри передозировке одновременно с приемом препаратов, оказывающих вли¤ние на сердечную де¤тельность, были зарегистрированы изменени¤ на Ё v, удлинение интервала QT, полиморфна¤ пируэтна¤ желудочкова¤ тахикарди¤, остановка сердца и желудочковые аритмии.

Ћечение:

—имптоматическое и поддерживающее. ?олжны быть прин¤ты меры, направленные на поддержание де¤тельности дыхательной и сердечнососудистой систем. Ќе следует использовать
эпинефрин (адреналин), т.к. это может привести к последующему понижению артериального давлени¤. —удороги можно купировать диазепамом, а двигательные расстройства бипериденом.

¬заимодействие:

 лопиксол может усилить седативное действие алкогол¤, действие барбитуратов и других угнетающих ?Ќ— веществ.

 лопиксол не следует назначать вместе с гуанетидином и аналогично действующими средствами, так как нейролептики могут повышать или понижать эффект некоторых антигипертензивных средств; антигипертензивное действие гуанетидина и аналогично действующих препаратов снижаетс¤.

ќдновременное применение нейролептиков и лити¤ повышает риск нейротоксичности.

“рициклические антидепрессанты и нейролептики взаимно ингибируют метаболизм друг друга.

 лопиксол может снижать эффективность леводопы и действие адренергических препаратов.

ќдновременное применение с метоклопрамидом и пиперазином повышает риск развити¤ экстрапирамидных нарушений.

ѕоскольку
зуклопентиксол частично метаболизируетс¤ изоферментом CYP2D6, то одновременный прием с препаратами, ингибирующими этот изофермент, может привести к снижению клиренса зуклопентиксола. ”величение интервала QT, характерное дл¤ терапии антипсихотическими средствами, может быть усилено при одновременном приеме препаратов, удлин¤ющих интервал QT: антиаритмических лекарственных средств IA и III классов (
хинидин,
амиодарон,
соталол, дофетилид), некоторых антипсихотических средств (
тиоридазин), некоторых антибиотиков- макролидов (
эритромицин) и антибиотиков хинолонового р¤да (
гатифлоксацин,
моксифлоксацин), некоторых антигистаминных средств (терфенадин,
астемизол), а также цизаприда, лити¤ и других лекарственных средств, увеличивающих интервал QT. —ледует избегать одновременного приема  лопиксола и указанных выше препаратов.

 лопиксол следует с осторожностью назначать одновременно с препаратами, вызывающими электролитные нарушени¤ (тиазидные и тиазидоподобные диуретики), и препаратами, способными повысить концентрацию зуклопентиксола в плазме крови, из-за возможного увеличени¤ риска удлинени¤ интервала QT и возникновени¤ опасных дл¤ жизни аритмий.

ќсобые указани¤:

ѕри длительной терапии, особенно большими дозами (выше 25-40 мг/сутки), необходимо проводить тщательный контроль, периодически оценива¤ состо¤ние пациентов, чтобы прин¤ть решение о возможности уменьшени¤ поддерживающей дозы.

ѕри терапии любыми нейролептиками существует возможность развити¤ злокачественного нейролептического синдрома («Ќ—). ќсновными симптомами «Ќ— ¤вл¤ютс¤ гипертерми¤, мышечна¤ ригидность и нарушение сознани¤ в сочетании с дисфункцией вегетативной нервной системы (лабильное артериальное давление, тахикарди¤, повышенное потоотделение).  роме немедленного прекращени¤ приема нейролептиков крайне необходимо использование общих поддерживающих мер и симптоматического лечени¤.

ѕри сопутствующем сахарном диабете назначение  лопиксола может изменить содержание инсулина и глюкозы в крови, что может потребовать коррекции дозы гипогликемических препаратов.

 ак и другие препараты, принадлежащие к терапевтическому классу нейролептиков,  лопиксол может вызвать удлинение интервала QT. ѕосто¤нно удлиненные интервалы QT могут повысить риск возникновени¤ злокачественных аритмий.

—ообщалось о случа¤х развити¤ венозной тромбоэмболии на фоне приема нейролептиков. ¬ св¤зи с тем, что пациенты, наход¤щиес¤ на лечении нейролептиками, часто вход¤т в группу риска развити¤ венозной тромбоэмболии, до начала и во врем¤ лечени¤  лопиксолом необходимо определить факторы риска развити¤ венозной тромбоэмболии и предприн¤ть меры предосторожности.

¬ ходе рандомизированных плацебо-контролируемых клинических исследований применени¤ некоторых атипичных антипсихотических препаратов у пациентов с деменцией наблюдалось 3-кратное увеличение риска возникновени¤ цереброваскул¤рных побочных реакций. ћеханизм такого повышени¤ риска неизвестен. Ќельз¤ исключать повышени¤ риска и при применении других антипсихотических средств у других групп пациентов. ” пациентов с риском развити¤ инсульта следует примен¤ть  лопиксол с осторожностью.

?анные двух больших наблюдательных исследований показали, что у пожилых пациентов с деменцией, принимавших антипсихотические препараты, отмечалось незначительное повышение риска смерти, по сравнению с пациентами, не принимавшими нейролептики. ?остаточных данных дл¤ точной оценки величины риска и причин его повышени¤ нет.  лопиксол не зарегистрирован дл¤ лечени¤ поведенческих расстройств у пожилых больных с деменцией.

ѕри употреблении алкогол¤ на фоне лечени¤ зуклопентиксолом возможно усиление угнетающего действи¤ на ?Ќ—.

“аблетки содержат гидрогенизированное касторовое масло, что может вызвать расстройство желудка и диарею.

¬ли¤ние на способность управл¤ть транспортным средством:

ѕациенты должны быть предупреждены о седативном действии препарата и о возможном вли¤нии его приема на способность вождени¤ автотранспорта и управлени¤ механизмами.

Release form:

Film-coated tablets 2 mg, 10 mg, 25 mg.

Packaging:

50 or 100 tablets in a plastic container with protection against opening by children and control of the first opening. The container opening diagram is printed on the lid by embossing. Container with instructions for use in a cardboard box.

Storage conditions:

At a temperature not higher than 25 ? C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date printed on the package.

Terms of dispensing from pharmacies:

On prescription