Clopixol - description of the drug, instructions for use, reviews

Release form and composition

Clopixol is available in the form of film-coated tablets: biconvex, round, pale pink (2 mg), pinkish-brown (10 mg) or red-brown (25 mg); in cross section - white (in plastic containers of 50 or 100 pcs., 1 container in a cardboard pack).

1 tablet contains:

• Active substance: zuclopenthixol - 2, 10 or 25 mg (in the form of zuclopenthixol dihydrochloride - 2.364, 11.82 or 29.55 mg, respectively);
• Auxiliary components (2/10/25 mg, respectively): hydrogenated castor oil - 0.48/0.72/0.96 mg, potato starch - 22.2/29.2/31.6 mg, lactose monohydrate - 17, 4/21.6/22 mg, glycerol 85% – 1.2/1.8/2.4 mg, microcrystalline cellulose – 9/13.5/18 mg, copovidone – 3/4.5/6 mg, talc – 4.2/6.3/8.4 mg, magnesium stearate – 0.42/0.63/0.84 mg;
• Shell (2/10/25 mg, respectively): hypromellose 5 – 1.37/2.05/2.74 mg, macrogol 6000 – 0.274/0.411/0.548 mg, E172 (iron oxide red) – 0.011/0.205/0.822 mg , E171 (titanium dioxide) – 0.445/0.479/0.091 mg.

Notes

1. José Miguel Vela;
   Helmut Buschmann; Jörg Holenz; Antonio Parraga; Anthony Torrens. Antidepressants, Antipsychotics, Anxiolytics: From Chemistry and Pharmacology to Clinical Application (English). - Weinheim: Wiley-VCH (English) Russian, 2007. - P. 516. - ISBN 3-527-31058-4.
2. Green AI, Noordsy DL, Brunette MF, O'Keefe C.
   Substance abuse and schizophrenia: pharmacotherapeutic intervention (English) // Journal of substance abuse treatment. - 2008. - Vol. 34, no. 1. - P. 61–71. - doi:10.1016/j.jsat.2007.01.008. - PMID 17574793.
3. Anxiolytic Sedatives Hypnotics and Antipsychotics // Martindale: The complete drug reference (unspecified) / Sweetman, Sean C.. - 36th. - London: Pharmaceutical Press (English) Russian, 2009. - pp. 1040-1041. — ISBN 978-0-85369-840-1.
4. ↑ 1 2 3 4 5 6 7 Syropyatov O., Dzeruzhinskaya N., Aladysheva E.
   Basics of psychopharmacotherapy: a manual for doctors / Edited by corresponding member. Crimean Academy of Sciences, Doctor of Medical Sciences, Professor O. G. Syropyatov. - Kyiv: Ukrainian Military Medical Academy, Ukrainian Research Institute of Social and Forensic Psychiatry and Narcology, 2007. - 310 p.
5. ↑ 123
   Interaction of drugs and the effectiveness of pharmacotherapy / L. V. Derimedved, I. M. Pertsev, E. V. Shuvanova, I. A. Zupanets, V. N. Khomenko; edited by prof. I. M. Pertseva. - Kharkov: Megapolis Publishing House, 2001. - 784 p. — 5000 copies. — ISBN 996-96421-0-X.

Pharmacological properties

Pharmacodynamics

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

It has an antipsychotic effect due to the blockade of dopamine receptors and, possibly, 5-hydroxytryptamine (5-HT) receptors.

Zuclopenthixol in vitro has a high affinity for dopamine D2 and D1 receptors, as well as serotonin 5-HT2 receptors and alpha1 adrenergic receptors, but has no affinity for muscarinic cholinergic receptors. Clopixol has a weak affinity for histamine H1 receptors and does not exhibit alpha2-adrenergic blocking activity. In vivo, the affinity for D2 receptors prevails over the affinity for D1 receptors.

Similar to most antipsychotics, taking zuclopenthixol leads to an increase in serum prolactin levels.

Zuclopenthixol is intended for the treatment of chronic and acute psychoses, as well as for the treatment of mentally retarded patients characterized by hyperactivity and aggressive behavior. This substance significantly weakens or completely eliminates the main symptoms of schizophrenia (hallucinations, thought disorders, delusions), and also has a pronounced effect on accompanying symptoms (suspiciousness, hostility, aggressiveness, agitation).

Zuclopenthixol is characterized by a dose-dependent transient sedative effect. At the beginning of therapy, a rapid sedative effect is provided, which is considered an advantage in cases of treatment of acute psychoses. Tolerance to the nonspecific sedative effect of the drug quickly develops. The specific inhibitory effect is particularly beneficial when treating patients with agitation, hostility, aggressiveness or restlessness.

Pharmacokinetics

When taken orally, the bioavailability of zuclopenthixol is approximately 44%. The time to reach maximum serum concentration is about 4 hours.

The apparent volume of distribution is about 20 l/kg. Approximately 98-99% of the substance binds to blood plasma proteins.

Zuclopenthixol penetrates slightly through the placental barrier and is excreted in breast milk in small quantities. The half-life of the active substance is 20 hours. Metabolites of zuclopenthixol are not neuroleptically active and are excreted mainly in feces, and also in some quantities in urine.

In patients with mild or moderate severity of schizophrenia, during maintenance therapy it is recommended to maintain a minimum (that is, measured immediately before administration) serum drug levels of 2.8 to 12 ng/ml.

pharmachologic effect

Clopixol has a pronounced antipsychotic and specific inhibitory effect; the latter is especially indicated for agitation, restlessness, hostility or aggressiveness. Clopixol may also have a transient, dose-dependent nonspecific sedative effect, the rapid development of which at the beginning of therapy (before the onset of antipsychotic action) is an advantage in the treatment of acute and subacute psychoses. Tolerance to the nonspecific sedative effect of the drug occurs quickly.

A single injection of Clopixol-acuphas provides significant and rapid relief of psychotic symptoms. The duration of the antipsychotic effect of the drug after one injection is 2-3 days. The nonspecific sedative effect appears after 2 hours, reaches a maximum after about 8 hours, after which it decreases significantly and is weakly manifested with repeated injections.

The therapeutic effect of Clopixol depot is significantly more prolonged compared to Clopixol. This allows confident continuous antipsychotic treatment with Clopixol depot, which is especially important for patients who do not comply with medical prescriptions. Clopixol depot prevents the development of frequent relapses associated with arbitrary interruption of patients taking oral medications.

Indications for use

• Schizophrenia (chronic and acute) and other psychotic disorders, especially those accompanied by hallucinations, thinking disorders and paranoid delusions;
• Hostility, aggressiveness, states of increased anxiety, agitation;
• Manic-depressive psychosis in the manic phase;
• Mental retardation, occurring with agitation, psychomotor agitation and other behavioral disorders;
• Senile dementia, occurring with behavioral disturbances, disorientation, paranoid ideas, and confusion.

Instructions for use of Clopixol: method and dosage

Clopixol tablets are taken orally.

The doctor prescribes the dosage regimen individually depending on the patient’s condition; the daily dose can be divided into several doses.

At the beginning of therapy, it is recommended to take Clopixol in low doses. Depending on the response to treatment, it may rapidly increase until an optimal clinical effect is achieved.

Recommended dosage regimen (daily dose):

• Acute attacks of schizophrenia and other acute psychotic disorders, severe agitation and mania: 10-50 mg;
• Psychotic disorders with moderate and severe course: 20 mg, with an interval of 2-3 days, it is possible to increase the dose by 10-20 mg to 75 mg per day;
• Psychotic conditions in a chronic course with schizophrenia and other chronic psychoses: 20-40 mg;
• Agitation in patients with oligophrenia: 6-20 mg, if necessary, the dose can be increased to 25-40 mg;
• Senile disorders accompanied by confusion and agitation: 2-6 mg, if necessary, the dose can be increased to 10-20 mg (the drug is preferably taken in the evening).

Pharmacokinetics

Cisordinol
Pharmacokinetic and clinical trials of Clopixol depot have shown that injections of the drug are most advisable at intervals of 2-4 weeks. Pharmacokinetically, a dose of Clopixol depot 200 mg once every 2 weeks is equivalent to an oral dose of Clopixol of 25 mg/day for 2 weeks.

Suction

After taking Clopixol orally, the Cmax of zuclopenthixol in the blood plasma is achieved after 4 hours. The bioavailability of zuclopenthixol when taken orally is about 44%. After an intramuscular injection of Clopixol-acufaz, zuclopenthixol acetate undergoes enzymatic cleavage into the active component zuclopenthixol and acetic acid. Cmax of zuclopenthixol in serum is achieved 24-48 hours (on average 36 hours) after injection. The concentration then slowly decreases, reaching 1/3 of the Cmax 3 days after injection. After an intramuscular injection of Clopixol, zuclopenthixol decanoate depot undergoes enzymatic cleavage into the active component zuclopenthixol and decanoic acid. Cmax of zuclopenthixol in serum is achieved by the end of the first week after injection. The concentration curve of zuclopenthixol decreases exponentially, with T1/2 being 19 days, which reflects the rate of release of the active substance from the depot.

Distribution

Zuclopenthixol penetrates the placental barrier in small quantities and is excreted in breast milk in small quantities.

Removal

When taken orally, T1/2 is approximately 20 hours. Metabolites do not have neuroleptic activity; excreted mainly in feces and partly in urine.

Side effects

• Cardiovascular system: possible tachycardia, orthostatic dizziness; rarely – orthostatic hypotension;
• Central and peripheral nervous system: at the initial stage of therapy, extrapyramidal symptoms may occur (as a rule, they are corrected by lowering the dose and/or prescribing antiparkinsonian drugs, but regular use of the latter for preventive purposes is not recommended), drowsiness, and the development of accommodation disturbances is also possible; very rarely, with long-term therapy, some patients develop tardive dyskinesia (antiparkinsonian drugs do not eliminate the symptoms of this condition; it is recommended to reduce the dose or, if possible, discontinue therapy);
• Urinary system: urinary retention;
• Digestive system: constipation, dry mouth; rarely – transient minor changes in liver tests.

Similar drugs:

• Eglonil Oral tablets
• Finlepsin Oral tablets
• Moditen depo Solution for intramuscular administration
• Egolanza Oral tablets
• Rispaksol Oral tablets
• Thiodazine Oral tablets
• Closasten (Closastene) Oral tablets
• Clopixol Depot Solution for intramuscular administration
• Thioridazine Oral tablets
• Leponex Oral tablets

** The Drug Directory is intended for informational purposes only. For more complete information, please refer to the manufacturer's instructions. Do not self-medicate; Before starting to use the drug Clopixol, you should consult a doctor. EUROLAB is not responsible for the consequences caused by the use of information posted on the portal. Any information on the site does not replace medical advice and cannot serve as a guarantee of the positive effect of the drug.

Are you interested in the drug Clopixol? Do you want to know more detailed information or do you need a doctor's examination? Or do you need an inspection? You can make an appointment with a doctor - the Euro lab is always at your service! The best doctors will examine you, advise you, provide the necessary assistance and make a diagnosis. You can also call a doctor at home . Euro lab clinic is open for you around the clock.

** Attention! The information presented in this medication guide is intended for medical professionals and should not be used as a basis for self-medication. The description of the drug Clopixol is provided for informational purposes only and is not intended for prescribing treatment without the participation of a doctor. Patients need to consult a specialist!

If you are interested in any other drugs and medications, their descriptions and instructions for use, information about the composition and form of release, indications for use and side effects, methods of use, prices and reviews of drugs, or you have any other questions and suggestions - write to us, we will definitely try to help you.

Overdose

In case of an overdose of the drug, drowsiness, convulsions, movement disorders, shock, hyperthermia/hypothermia, and coma may occur.

In cases of overdose due to the simultaneous use of drugs that affect cardiac activity, changes in the electrocardiogram, prolongation of the QT interval, the development of polymorphic torsade de pointes ventricular tachycardia, ventricular arrhythmias, and cardiac arrest have been recorded.

Symptomatic and supportive treatment is indicated. Measures should be taken to maintain the activity of the cardiovascular and respiratory systems. Due to the possible decrease in blood pressure, the use of adrenaline (epinephrine) is not recommended. Movement disorders can be treated with biperiden, and seizures with diazepam.

Links

• Zuclopenthixol

special instructions

During long-term therapy, careful clinical monitoring of the patient's condition is periodically necessary to reduce the maintenance dose.

It must be taken into account that when using Clopixol, in rare cases, neuroleptic malignant syndrome (NMS) may develop with a fatal outcome. The main symptoms of NMS include: muscle rigidity, hyperthermia and disturbances of consciousness in combination with dysfunction of the autonomic nervous system (tachycardia, labile blood pressure, increased sweating). If these symptoms develop, it is necessary to urgently discontinue therapy and prescribe symptomatic and supportive treatment.

When using Clopixol, especially at the beginning of therapy, before determining the individual response to the treatment, care must be taken when driving vehicles and performing potentially hazardous types of work.

Use during pregnancy and lactation

During pregnancy, the drug should be used with caution and only in cases where the expected risk to the fetus is lower than the potential benefit to the mother.

There is evidence that if the mother takes antipsychotic drugs at the end of pregnancy or during childbirth, newborns may show signs of intoxication (lethargy, excessive excitability, tremor). Along with this, such children have a low Apgar score.

If clinically necessary, breastfeeding is allowed during treatment with Clopixol. It is recommended to monitor the condition of the newborn, especially during the first 4 weeks after birth.

Contraindications

The instructions for Clopixol say that this antipsychotic drug should not be used:

• If you have hypersensitivity to zuclopenthixol or any of the auxiliary components of the drug;
• Patients with acute intoxication with barbiturates, ethanol or opioid analgesics;
• In comatose states;
• Pregnant women;
• During lactation.

It is possible to use Clopixol, but with great caution and under constant medical supervision in case of epileptic syndrome, heart disease (including arrhythmias) or liver disease (including chronic hepatitis).

Drug interactions

When Clopixol is used simultaneously with certain medications, the following effects may occur:

• Ethanol, barbiturates and other drugs that have a depressant effect on the central nervous system: increased sedative effect;
• Guanethidine and drugs with similar effects: blocking their hypotensive effect (the combination is not recommended);
• Metoclopramide, piperazine: increased risk of developing extrapyramidal symptoms;
• Levodopa and other adrenergic drugs: decreased effectiveness.

Pharmaceutical incompatibility of Clopixol has not been established.