Active substanceChlorprotixenChlorprotixen
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  • Truksal®
    pills inwards 
    H. Lundbeck A / S     Denmark
  • Chlorprotixen
    pills inwards 
  • Chlorprotixen Zentiva
    pills inwards 
    Zentiva c.s.     Czech Republic
  • Dosage form: & nbspfilm coated tablets
    Composition:

    active substance - chlorprotixen hydrochloride 25 mg / 50 mg.

    Excipients - corn starch 43.8 mg / 27.7 mg,

    lactose monohydrate 87.7 mg / 55.4 mg, copovidone 10 mg / 8.5 mg, glycerol 85% 4 mg / 3.4 mg, microcrystalline cellulose 20 mg / 17 mg, croscarmellose sodium 4 mg / 3.4 mg, talc 4 mg / 3.4 mg, magnesium stearate 1.5 mg / 1.28 mg.

    Sheath - Opadry OY-S-9478 brown 4 mg / 3.4 mg (hypromellose, macrogol 400, iron oxide black (E 172), iron oxide red (E 172), titanium dioxide (E 171)).

    Description:

    25 mg - round, biconvex tablets, film-coated, dark brown;

    50 mg - oval, biconvex tablets, film-coated, dark brown in color.

    Pharmacotherapeutic group:antipsychotic (antipsychotic) remedy.
    ATX: & nbsp

    N.05.A.F.03   Chlorprotixen

    Pharmacodynamics:

    Truksal is a neuroleptic, a derivative of thioxanthene. Has antipsychotic, pronounced sedative and moderate antidepressant effect.

    Antipsychotic action of neuroleptics is associated with blockade of dopamine receptors, and, possibly,blockade of 5-HT (5-hydroxytryptamine) receptors. In vivo chloroprotoxen has a high affinity for dopamine receptors D1 and D2. Chlorprotixen also has a high affinity for 5-HT2 receptors, a1-adrenergic receptors, histamine (H1) cholinergic muscarinic receptors. The profile of the receptor binding of chlorprotixen is very similar to that of clozapine, but it has about a 10-fold higher affinity for dopamine receptors.

    Chlorprotixen reduces the severity or eliminates anxiety, obsessions, psychomotor agitation, anxiety, insomnia, as well as hallucinations, delusions and other psychotic symptoms. A very low incidence of extrapyramidal effects (about 1%) and tardive dyskinesia (about 0.05%) suggests that Truksal can be successfully used for maintenance therapy in patients with psychotic disorders. Low doses of chlorprotixen have an antidepressant effect, which makes the use of the drug useful in mental disorders characterized by anxiety, depression and anxiety. Also, when chlorprotixen therapy is used, the severity of associatedpsychosomatic symptoms. Chlorprotixen does not cause addiction, dependence or the formation of tolerance. Besides, chloroprotoxen potentiates the action of analgesics. has its own analgesic effect, as well as antipruritic and antiemetic effects.

    Pharmacokinetics:

    The bioavailability of chlorprotixen at oral intake is about 12%. The maximum concentration in the serum is reached after about 2 hours.

    The half-life is about 16 hours. Chlorprotixen penetrates the placental barrier and in small amounts is excreted in breast milk.

    Metabolites have no neuroleptic activity.
    Indications:

    Schizophrenia and other psychoses occur with psychomotor agitation, agitation and anxiety.

    Abstinence syndrome with alcoholism and drug addiction.

    Depressive states, neuroses, psychosomatic disorders with anxiety, stress, anxiety, insomnia, sleep disorders. Epilepsy and oligophrenia, combined with mental disorders: agitation, agitation, mood lability and behavioral disorders.

    Pain syndrome (in combination with analgesics).

    Hyperactivity, agitation, irritability, confusion, anxiety, impaired behavior and sleep in the elderly.

    Behavioral and sleep disorders in children.

    Contraindications:

    Hypersensitivity to chlorprotixen or any of the excipients. Vascular collapse, depression of consciousness of any origin (including those caused by taking alcohol, barbiturates or opiates), coma. Uncorrected hypokalemia or hypomagnesemia.

    Truksal is contraindicated in the presence or in history of patients with clinically significant cardiovascular diseases (bradycardia (less than 50 beats per minute), recent myocardial infarction, decompensated heart failure, cardiac hypertrophy, arrhythmias in which antiarrhythmics of IA and III classes are prescribed), ventricular arrhythmias or development of polymorphic pirouette ventricular tachycardia (Torsade de Pointes).

    Truksal should not be given to patients with congenital syndrome of prolonged QT interval or in cases of acquired extended QT interval (over 450 ms for men and 470 ms for women).

    Simultaneous reception with drugs that extend the QT interval.

    Hereditary intolerance to galactose, deficiency of lactase

    Lappa, impaired absorption of glucose and galactose.

    Carefully:

    organic diseases of the brain, mental retardation, the presence of cardiovascular diseases in the status, the presence in the family history of cases of prolongation of the QT interval, convulsive disorders, severe hepatic and renal insufficiency, intraocular hypertension (in persons with local anatomical predisposition - narrow angle of the anterior chamber), severe pseudoparalytic myasthenia gravis, benign prostatic hypertrophy, the presence of risk factors for stroke, abuse of opiates and alcohol; pregnancy, the period of breastfeeding.

    Pregnancy and lactation:

    During pregnancy, Truksal should be used only if the intended

    The benefit to the mother exceeds the potential risk to the fetus.

    In newborns whose mothers have taken antipsychotics, in the last stages of pregnancy or during labor, signs of intoxication may appear, such as lethargy; tremor and excessive excitability.In addition, such neonates may have a low Apgar score.

    During treatment, Truksal is allowed to breast-feed, if it is recognized clinically necessary. Nevertheless, it is recommended to monitor the condition newborn, especially in the first 4 weeks after birth.

    Dosing and Administration:

    Tablets are taken orally with water.

    Dosage is selected individually depending on the patient's condition. Typically, at the beginning of treatment, small doses are prescribed that increase to the optimal effective level as quickly as possible depending on the therapeutic response.

    Schizophrenia and other psychosis.

    Manic conditions.

    Treatment begins with 50 - 100 mg / day, gradually increasing the dose to achieve the optimal effect, usually up to 300 mg / day. In some cases, the dose may be increased to 1200 mg / day.

    The maintenance dose is usually 100-200 mg / day.

    The daily dose of chlorprotixen is usually divided into 2 to 3 doses, given the expressed sedative effect of chlorprotixen, it is recommended to prescribe a smaller portion of the daily dose in the daytime, and most in the evening.

    Abstinence syndrome, with alcoholism and drug addiction.

    The daily dose divided into 2 to 3 doses is 500 mg. The course of treatment usually lasts 7 days. After the disappearance of manifestations of withdrawal, the dose gradually decreases. The maintenance dose of 25 - 75 mg / day allows to stabilize the condition, reduces the risk of developing another binge.

    Depressive states, neuroses, psychosomatic disorders. Truksal can be used for depression, especially when combined with anxiety, stress, as an adjunct to therapy with antidepressants or alone. Truksal can be prescribed for neuroses and psychosomatic disorders, accompanied by anxiety and depressive disorders, up to 75 mg / day. The daily dose, as a rule, is divided into 2-3 doses. Since the use of chlorprotixen does not cause the development of addiction or drug dependence, it can be used for a long time.

    The maximum dose for the treatment of such conditions is 150 mg / day.

    Epilepsy and oligophrenia, combined with mental disorders.

    The daily dose is 50 mg and is usually divided into 2-3 doses. The daily dose can be increased to 75-100 mg / day.

    In elderly patients, the dose is 25 - 75 mg / day.

    Children for correcting behavioral disorders chloroprotoxen is prescribed at the rate of 0.5 - 2 mg per 1 kg of body weight.

    Insomnia.

    25 mg per hour before bedtime.

    Chronic pain.

    The ability of chlorproticene to potentiate the action of analgesics can be used in the treatment of patients with pain. In these cases chloroprotoxen prescribe in doses from 75 to 300 mg, it is possible to use, together with analgesics.

    Decreased kidney function:

    Patients with reduced renal function should be given a lower dosage, and if possible, monitor the level of the drug in the blood serum.

    Decreased liver function:

    Patients with reduced liver function should be given a lower dosage, and if possible, monitor the level of the drug in the blood serum.

    Side effects:

    Most side effects depend on the dose used. The incidence of side effects and their severity are most pronounced at the beginning 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.The frequency is indicated as: very often (> or = 1/10), often (from> or = 1/100 to <1/10), infrequently (from 1/1000 to <1/100), rarely (> or = 1 / 10000 to <1/1000), very rarely (<1/10000), or unknown (can not be estimated based on existing data).

    From the nervous system:

    very often - drowsiness, dizziness

    often - dystonia, headache;

    infrequently - tardive dyskinesia, parkinsonism, convulsions, akathisia;

    very rarely - malignant neuroleptic syndrome.

    From the side of mental activity:

    often - insomnia, nervousness, agitation, decreased libido.

    From the cardiovascular system:

    often - tachycardia, palpitations;

    infrequently - hypotension, hot flashes;

    rarely - prolongation of the QT interval on the electrocardiogram;

    very rarely venous thromboembolism.

    From the hematopoiesis:

    rarely - thrombocytopenia,

    neutropenia, leukopenia, agranulocytosis.

    On the part of the organs of vision:

    often - a violation of accommodation, visual impairment;

    infrequently - movement of eyeballs

    From the respiratory system:

    rarely - shortness of breath.

    From the digestive system:

    very often - dry mouth, increased salivation;

    often - constipation, indigestion, nausea;

    infrequently - vomiting, diarrhea.

    Metabolic and nutritional disorders:

    often - increased appetite, weight gain;

    infrequent - loss of appetite, weight loss;

    rarely - hyperglycemia, impaired glucose tolerance.

    From the endocrine system:

    rarely - hyperprolactinaemia.

    From the urinary system:

    infrequently urinary retention, painful urination.

    On the part of the reproductive system:

    infrequently - violations of ejaculation, erectile dysfunction;

    rarely - gynecomastia, galactorrhea, amenorrhea.

    Hepatic and hepatobiliary disorders:

    infrequently - changes in laboratory parameters of liver function;

    very rarely - jaundice.

    From the immune system:

    rarely - hypersensitivity, anaphylactic reactions.

    Disturbances of the musculoskeletal system and connective tissue:

    Often - myalgia;

    infrequent muscle rigidity.

    From the side of the skin and subcutaneous tissue:

    often hyperhidrosis;

    infrequently - skin rash, itching, photosensitivity, dermatitis.

    On the part of the body as a whole:

    often - asthenia, fatigue.

    When taking neuroleptics, there is a possibility of developing a malignant neuroleptic syndrome (CNS). The main symptoms of the NSA are hyperthermia,Muscular rigidity and impaired consciousness in combination with dysfunction of the autonomic nervous system (labile arterial pressure, tachycardia, increased sweating). In addition to the immediate discontinuation of antipsychotics, the use of general supportive measures and symptomatic treatment is extremely important.

    Patients on long-term care may develop tardive dyskinesia. Antiparkinsonian drugs do not eliminate its symptoms and can aggravate them. It is recommended to reduce the dose or, if possible, stop treatment with chlorprotixene.

    With persistent akathisia, benzodiazepines may be useful, or propranolol.

    When taking chlorprotixen, as with other neuroleptics, the following rare side effects were also observed: lengthening of the QT interval, ventricular arrhythmias - ventricular fibrillation, ventricular tachycardia, sudden death and pirouette ventricular tachycardia (Torsade de Pointes).

    A sharp discontinuation of chlorprotrixen may be accompanied by the emergence of 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, an additional sensation of heat and cold and tremor. Symptoms usually begin within 1-4 days after cancellation and decrease within 7-14 days.

    Overdose:

    Symptoms.

    Drowsiness, coma, convulsions, shock, extrapyramidal symptoms, hyperthermia / hypothermia. In severe cases, kidney failure is possible.

    In case of an overdose and simultaneous administration with drugs that affect cardiac activity, the development of ECG changes was reported,

    lengthening of QT interval, polymorphic pirouette ventricular tachycardia, cases of cardiac arrest and ventricular arrhythmia.

    Treatment.

    Symptomatic and supportive. As soon as gastric lavage is to be performed, the use of activated charcoal is recommended. Measures should be taken to maintain the respiratory and cardiovascular systems. Do not use epinephrine, tk. this can lead to a subsequent lowering of blood pressure. Seizures can be suppressed with diazepam, and extrapyramidal disorders with biperidenum.

    Interaction:

    Truksal can strengthen the sedative effect of alcohol, the effects of barbiturates and other drugs that depress the central nervous system.

    Truksal should not be administered together with guanethidine and similarly acting agents, as antipsychotics may enhance or weaken the effect of antihypertensive drugs; The antihypertensive effect of guanethidine and similarly acting drugs is reduced.

    Simultaneous use of neuroleptics and lithium increases the risk of neurotoxicity.

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

    Truksal can reduce the effectiveness of levodopa and the effect of adrenergic drugs and enhance the action of anticholinergics.

    Simultaneous use with metoclopramide and piperazine increases the risk of extrapyramidal disorders.

    The antihistaminic effect of chlorprotixen may suppress or eliminate the reaction of alcohol / disulfiram.

    The increase in the QT interval, characteristic for therapy with antipsychotic agents, can be enhanced by simultaneous administration of drugs significantly extending the QT interval: antiarrhythmic drugs IA and III classes (quinidine, amiodarone, sotalol, dofetilide), some antipsychotics (thioridazine), some antibiotics-macrolides (erythromycin) and antibiotics of the quinolone series (gatifloxacin, moxifloxacin), some antihistamines (terfenadine, astemizole), as well as cisapride, lithium and other drugs that increase the QT interval. It should avoid simultaneous reception of Truksala and the above drugs.

    Truksal should be administered with caution at the same time with drugs that cause electrolyte disorders (thiazide and thiazide-like diuretics) and drugs that can increase the concentration of chloroprotoxen in the blood plasma, because of the possible increase in the risk of prolongation of the QT interval and the occurrence of life-threatening arrhythmias.

    Special instructions:

    With prolonged therapy, especially in large doses, careful monitoring is necessary, periodically assessing the condition of patients to decide whether to reduce the maintenance dosage.

    With the concomitant treatment of diabetes mellitus, the appointment of Truksal may require correction of the dose of insulin.

    Because of the risk of malignant arrhythmias, Truksal should be administered with caution to patients withcardiovascular diseases in the Shk. history and patients with the presence of cases of prolonged QT interval in the family history.

    Before starting treatment Truksalom it is necessary to conduct an ECG examination. At QT interval over 450 ms for men and 470 ms for women, Truksal should not be assigned.

    During therapy, the need for an ECG study is evaluated by a doctor individually based on the patient's condition.

    When extending the QT interval, smaller doses of Truksal should be used, with prolongation of the QT interval greater than 500 msec, therapy should be discontinued.

    During treatment it is recommended to carry out a periodic assessment of the electrolyte balance. It was reported about the development of venous thromboembolism in the presence of neuroleptics.

    Due to the fact that patients treated with neuroleptics are often at risk for developing venous thromboembolism, it is necessary to identify risk factors for venous thromboembolism before and during treatment, and take precautions.

    Truksal is not registered for the treatment of behavioral disorders in elderly patients with dementia.

    Effect on the ability to drive transp. cf. and fur:

    During the period of treatment it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:

    Tablets coated with a film coating of 25 and 50 mg.

    Packaging:

    For 50 or 100 tablets in a plastic container with a screw cap and first opening control.

    Container with instructions for use in a cardboard box.
    Storage conditions:

    At a temperature of no higher than 25 ° C. Keep out of the reach of children.

    Shelf life:

    5 years.

    Do not use after the expiration date printed on the package
    Terms of leave from pharmacies:On prescription
    Registration number:П N012057 / 01
    Date of registration:01.04.2011
    The owner of the registration certificate:H. Lundbeck A / SH. Lundbeck A / S Denmark
    Manufacturer: & nbsp
    Representation: & nbspLUNDBEK EXPORT A / C LUNDBEK EXPORT A / C Denmark
    Information update date: & nbsp20.10.2015
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