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Pharmacological properties

Zuclopentixol is an antipsychotic of the thioxanthene group. the antipsychotic effect is associated with blockade of dopamine receptors, as well as probable blockade of 5-nt receptors. in vitro, zuclopentixol has a high affinity for both dopamine d1 and d2 receptors, α1 adrenoreceptors, and 5 nt2 receptors, but it does not have an affinity for cholinergic muscarinic receptors. it has a weak affinity for histamine (H1) receptors and does not have a blocking effect on α2-adrenergic receptors.

Like most other antipsychotics, zuclopentixol increases serum prolactin levels.

Clopixol is prescribed in the treatment of acute and chronic psychoses, the treatment of patients with mental disabilities with hyperactive destructive behavior, as well as elderly patients with dementia and paranoid ideas, behavior disorders.

In addition to a marked reduction or complete elimination of the nuclear symptoms of schizophrenia, such as hallucinations, mania, and impaired thinking, zuclopentixol effectively reduces concomitant symptoms such as hostility, suspicion, anxiety, and aggressiveness.

Zuclopentixol causes a transient dose-dependent sedation. However, such a pronounced primary sedative effect is usually an advantage in the initial phase of the disease. Tolerance to a nonspecific sedative effect develops rapidly.

The pronounced effect after the use of the drug Clopixol-Acufaz occurs at the 4th hour after parenteral use of the oily solution of zuclopentixol acetate. A slightly more significant effect is noted in the period from 1 to 3 days after injection. Over the next days, the effect is significantly reduced.

Clopixol-Acuphase is used for the initial treatment of acute and chronic psychoses in the acute phase, as well as manic conditions. A single injection of the drug Clopixol-Akufaz provides a pronounced and rapid weakening of psychotic symptoms. The effect of the drug lasts from 2 to 3 days and, as a rule, one or two injections are enough to achieve the desired effect, after which it is possible to switch to treatment with oral or deposited forms.

Clopixol-Akufaz exhibits a transient dose-dependent sedative effect. The rapid development of a sedative effect at the beginning of therapy (before the appearance of antipsychotic action) is an advantage in the treatment of acute and subacute psychoses, as it reassures the patient before the antipsychotic effect is manifested.

Nonspecific sedative effect develops rapidly after injection, becomes pronounced after 2 hours, reaches a maximum after 8 hours, after which it decreases significantly and remains weak, despite repeated injections.

Clopixol-Akufaz is prescribed for the treatment of psychotic patients with agitation, anxiety, hostility or aggression.

The specific inhibitory effect of Clopixol Depot is especially beneficial in the treatment of psychotic patients with symptoms of arousal, anxiety, hostility and aggressiveness.

Clopixol Depot has a transient dose-dependent sedative effect. However, if the patient switches to maintenance therapy with Clopixol Depot after taking Clopixol tablets or injections of Clopixol-Acufaz, the risk of sedation is reduced. Tolerance to a nonspecific sedative effect develops rapidly.

Clopixol Depot provides the possibility of continuous treatment, which is extremely important for patients who do not follow the doctors prescription. Clopixol Depot prevents the development of frequent relapses, which are associated with interruption by patients of the use of oral medications.

Pharmacokinetics

Clopixol tablets. WITHmax in blood serum is achieved after 4 hours. Zuclopentixol is used regardless of food intake. Oral bioavailability is about 44%. Binding to plasma proteins is approximately 98–99%. T½ zuclopentixol is approximately 20 hours; systemic clearance is approximately 0.86 l / min. Zuclopentixol is eliminated mainly with feces and partially with urine. Metabolites do not have antipsychotic activity and are excreted mainly with feces and partially with urine (10%). Zuclopentixol in small quantities penetrates the placental barrier and in small amounts is excreted in breast milk. The kinetics is linear. The equilibrium concentration is established after 3-5 days.

Clopixol-Akufaz. After injection, zuclopentixol acetate is enzymatically cleaved into the active component of zuclopentixol and acetic acid. T½ Clopixol-Acuphase after IM injection is approximately 32 hours (reflects release from the depot). Cmax Zuclopentixol in blood serum is reached 24–48 hours (average 36 hours) after injection.

Clopixol Depot. After the introduction of zuclopentixol, decanoate is enzymatically digested into the active component of zuclopentixol and decanoic acid. Cmax serum zuclopentixol is reached at the end of the 1st week after injection. T½ Clopixol Depot after i / m injection - 3 weeks (reflects release from the depot), the equilibrium concentration is established with repeated use for 3 months.

Pharmacokinetically, the dose of clopixol Depot 200 mg once every 2 weeks is equivalent to a daily oral dose of 25 mg of clopixol for 2 weeks.

Indications

Clopixol tablets

  • Acute and chronic schizophrenia and other psychotic disorders, especially with symptoms such as hallucinations, mania and impaired thinking with agitation, anxiety, hostility and aggressiveness.
  • The manic phase of manic-depressive psychosis.
  • Excitation or other behavioral disorders in patients with mental retardation.
  • Symptoms of agitation and aggression in elderly patients with dementia.

Clopixol-Akufaz

  • Initial treatment of acute psychoses, manic states and chronic psychoses in the acute phase.

Clopixol Depot

  • Supportive care for schizophrenia and other psychoses, especially with symptoms such as hallucinations, mania, and impaired thinking with agitation, anxiety, hostility, and aggressiveness.

Application

Clopixol tablets

Adults The dose of the drug is selected individually depending on the condition of the patient. As a rule, at the beginning of treatment, the drug should be used in low doses, which then quickly increase to the optimal effective level, depending on the clinical effect. A maintenance dose is usually taken 1 time per day in the evening.

Acute schizophrenia and other acute psychoses. Severe acute arousal. Mania

Assign, as a rule, 10-50 mg / day. In severe disorders and conditions of moderate severity, the initial dose of 20 mg / day can be increased, if necessary, by 10–20 mg every 2-3 days to 75 mg / day or more. The maximum dose for 1 dose is 40 mg, the daily dose is 150 mg.

Chronic schizophrenia and other chronic psychoses

The maintenance dose is 20–40 mg / day.

Agitation in patients with mental retardation

Usually prescribed 6–20 mg / day, if necessary, the dose can be increased to 25–40 mg / day.

Stimulation and aggressiveness in elderly patients with dementia

Assign 2-6 mg / day (preferably taken in the evening), if necessary, the dose can be increased to 10-20 mg / day.

Dosage for impaired renal function. In patients with impaired renal function, zuclopentixol is prescribed in usual doses.

Dosage for impaired liver function. Patients with impaired liver function should be prescribed a dose half as low as usual, and if possible, determine the level of the drug in blood serum.

Clopixol-Akufaz

Adults

Doses of the drug are determined individually depending on the condition of the patient.Clopixol-Acuphase is prescribed as an intramuscular injection into the upper outer quadrant of the buttock. Local tolerance is good. Usually, adults are recommended doses in the range of 50-150 mg (1-3 ml). A 2 ml injection should be divided into two injection sites. If necessary, repeated injections are carried out with an interval of 2-3 days. For some patients, an additional injection may be given 24–48 hours after the first injection.

Zuclopentixol acetate is not intended for prolonged use, the duration of therapy should not exceed 2 weeks. The maximum total dose per course of therapy is not more than 400 mg, and the number of injections is not more than 4.

Supportive therapy should be continued with oral administration of clopixol or the administration of clopixol depot, guided by the following scheme:

1. The transition to oral administration of clopixol. 2-3 days after the final injection of Clopixol-Acuphase (100 mg), the patient should be prescribed Clopixol orally daily at a dose of 40 mg, if possible in several doses. If necessary, increase the dose by 10–20 mg every 2–3 days to 75 mg / day or more.

2. When switching to treatment with Clopixol Depot. At the same time as the final injection of Clopixol-Acuphase (100 mg), 200–400 mg (1-2 ml) of Clopixol Depot should be administered 200 mg / ml. Repeated injections of Clopixol Depot are given IM every 2 weeks. Possible use of maximum doses or shorter intervals between injections.

Clopixol Depot and Clopixol-Akufaz can be mixed in one syringe and prescribed in one injection (co-injection). Subsequent doses of clopixol Depot and the intervals between injections should be set depending on the patients condition.

Elderly patients

It is necessary to reduce the usual doses. The maximum dose of one injection should not exceed 100 mg.

Dosage for impaired renal function

In patients with impaired renal function, clopixol-Akufaz can be prescribed in usual doses.

Dosage for impaired liver function

Patients with impaired liver function should be prescribed half the usual dose, and if possible, determine the level of the drug in the blood serum.

Clopixol-Akufaz can be mixed with Clopixol Depot, which contains the same oil.

Clopixol Depot

Adults

The dose of the drug and the interval between injections are determined individually in accordance with the condition of the patient in order to achieve maximum containment of psychotic symptoms with a minimum of side effects. Clopixol Depot is injected intramuscularly into the upper outer quadrant of the buttock. Injections do not cause irritation at the injection site, slightly damaging muscle tissue. Clopixol Depot can be mixed with Clopixol-Akufaz, which contains the same Viscoleo oil (co-injection).

With supportive treatment, the dosage range is usually 200-400 mg (1-2 ml) every 2-4 weeks. Some patients may need higher doses or shorter intervals between injections. 2 ml injections should be divided into two injection sites.

When switching from oral therapy with Clopixol or Clopixol-Akufaz to maintenance treatment with Clopixol Depot, the following scheme should be followed:

Switching from oral administration of clopixol to clopixol depot v / m:

Oral daily dose of clopixol (mg) x 8 = Clopixol Depot (mg) IM once every 2 weeks.

Oral daily dose of clopixol (mg) x16 = Clopixol Depot (mg) IM once every 4 weeks.

Patients should continue to take clopixol orally for 1 week after the 1st injection, but in a reduced dose.

Dosage for impaired renal function. In patients with impaired renal function, the drug is prescribed in normal doses.

Dosage for impaired liver function. Patients with impaired liver function should be given a dose twice as low as usual, and if possible, a determination of the level of the drug in serum should be carried out.

Contraindications

Hypersensitivity to any component of the drug, circulatory collapse, depression of any etiology (e.g. alcoholic, barbiturate or opioid intoxication), coma.

Side effects

In most cases, dose-dependent. their frequency and severity are more pronounced at the beginning of therapy and decrease with further treatment.

Extrapyramidal symptoms may develop, especially in the first few days after the injection and in the initial phase of therapy. In most cases, they are adjusted by dose reduction and / or antiparkinsonian drugs. Regular prophylactic use of the latter is not recommended.

If side effects occur, a dose reduction or, if possible, discontinuation of zuclopentixol therapy is recommended. In cases of persistent akathisia, the use of benzodiazepine or propranolol is recommended.

The frequency of adverse reactions shown in the table below is defined as: very often (≥1 / 10); often (≥1 / 100, but 1/10); infrequently (≥1 / 1000, but 1/100); rarely (≥1 / 10,000, but 1/1000); very rarely (1/10 000).

Organ systems Frequency Manifestations
Disorders of the cardiovascular system Often Tachycardia, palpitations
Infrequently Arterial hypotension, blush
Rarely ECG Q-T interval extension
Violations of the blood system and lymphatic system Rarely Thrombocytopenia, neutropenia, leukopenia, agranulocytosis
Disorders of the nervous system Often Drowsiness, akathisia, hyperkinesia, hypokinesia
Often Tremor, dystonia, hypertension, dizziness, headache, paresthesia, impaired attention, amnesia, impaired gait
Infrequently Tardive dyskinesia, hyperreflexia, dyskinesia, parkinsonism, syncope, ataxia, speech disorders, hypotension, convulsions, migraine
Rarely Malignant antipsychotic syndrome
Violations of the organ of vision Often Disturbance of accommodation
Infrequently Eye movement disorder, mydriasis
Hearing organ impairment (including labyrinthine) Often Dizziness
Infrequently Hypersensitivity, tinnitus
Disorders of the respiratory system, chest and mediastinum Often Nasal congestion, shortness of breath
Gastrointestinal Disorders Often Dry mouth
Often Hypersalivation, constipation, vomiting, dyspepsia, diarrhea
Infrequently Abdominal pain, nausea, flatulence
Violations by

urinary system

Often Urination disorders, urinary retention, polyuria
Skin disorders

and subcutaneous tissue

Often Hyperhidrosis, itching
Infrequently Rash, photosensitivity reactions, pigmentation disorders, seborrhea, dermatitis, purpura
Musculoskeletal disorders Often Myalgia
Infrequently Muscular rigidity, trismus, torticollis
Disorders from the endocrine system Rarely Hyperprolactinemia
Metabolic disorders Often Increased appetite, weight gain
Infrequently Decreased appetite, weight loss
Rarely Hyperglycemia, impaired glucose tolerance, hyperlipidemia
General disorders and disorders at the injection site Often Asthenia, fatigue, malaise, pain
Infrequently Thirst, reaction at the injection site, hypothermia, pyrexia
Immune System Disorders Rarely Hypersensitivity, anaphylactic reaction
Violations of the liver and biliary tract Infrequently Functional impairment
Rarely Cholestatic hepatitis, jaundice
Disorders from the reproductive system and mammary glands Infrequently Lack of ejaculation, erectile dysfunction, orgasmic disorders in women, vulvovaginal dryness
Rarely Gynecomastia, galactorrhea, amenorrhea, priapism
Mental disorders Often Insomnia, depression, anxiety, nervousness, pathological dreams, decreased libido
Infrequently Apathy, nightmares, increased libido, confusion

There are reports of rare cases of prolongation of the Q – T interval, ventricular arrhythmias - ventricular fibrillation, ventricular tachycardia, Torsade de Pointes arrhythmias and sudden death when using drugs belonging to the antipsychotic class, including zuclopentixol.

Sudden discontinuation of zuclopentixol can cause withdrawal symptoms, the most common of which are nausea, vomiting, anorexia, diarrhea, rhinorrhea, sweating, myalgia, paresthesia, insomnia, anxiety, anxiety and agitation. Patients may also experience dizziness, tremors, and variable sensations of heat and cold. Symptoms usually appear within 1–4 days after discontinuation of the drug and decrease within 7–14 days.

special instructions

The likelihood of developing a malignant antipsychotic syndrome (hyperthermia, muscle rigidity, impaired consciousness, dysfunction of the autonomic nervous system) exists with the use of any antipsychotic. the risk is potentially higher if several agents are used. fatal cases occur mainly in patients with existing organic syndrome, mental retardation, abuse of opiates and alcohol.

Treatment: discontinuation of antipsychotics, symptomatic and general supportive measures. Dantrolene and bromocriptine can be used.

Symptoms can be noted for a week or more after stopping the administration of oral forms and slightly longer after using the deposited forms of the drug.

Like other antipsychotics, zuclopentixol should be used with caution in the treatment of patients with organic brain syndrome, seizures, and progressive liver disease.

Like other antipsychotic drugs, zuclopentixol can alter the need for insulin and glucose tolerance, which may require correction of antidiabetic therapy in patients with diabetes mellitus.

During maintenance therapy, especially when using the drug in high doses, the condition of patients should be carefully monitored and the possibility of reducing the maintenance dose periodically evaluated.

When using some atypical antipsychotic drugs in a randomized, placebo-controlled study among patients with dementia, an increase in the risk of cerebrovascular disorders by about 3 times was noted. The mechanism for this increased risk is unknown. An increased risk cannot be excluded for other antipsychotic drugs and other groups of patients. Zuclopentixol should be used with caution in patients with risk factors for stroke.

Like other antipsychotic drugs, zuclopentixol can lead to a prolongation of the Q – T interval. Existing Q – T prolongation may increase the risk of malignant arrhythmias. Therefore, zuclopentixol should be used with caution in patients with suspected hypokalemia, hypomagnesemia, or with a genetic predisposition to such conditions, as well as in patients with a history of cardiovascular diseases, for example, an extended Q – T interval, significant bradycardia (50 beats / min) recently suffered myocardial infarction, decompensated heart failure, or cardiac arrhythmia. The simultaneous use of other antipsychotic drugs should be avoided.

Excipients. Clopixol tablets contain lactose monohydrate. Patients with a rare hereditary impairment of galactose tolerance, Lapp lactase deficiency or glucose-galactose malabsorption should not be prescribed this drug.

During pregnancy and breastfeeding.Clopixol, Clopixol-Akufaz and Clopixol Depot are not prescribed during pregnancy, unless the expected benefit for the patient does not exceed the theoretical risk to the fetus.

In newborns whose mothers used antipsychotics in late pregnancy, they may show

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