Tizercin analogs and synonyms. Medicinal reference book geotar

05.03.2020 -

Instructions for use Tizercin ®
Composition of the drug Tizercin ®
Indications for the drug Tizercin ®
Storage conditions for the drug Tizercin ®
Shelf life of the drug Tizercin ®

ATX Code: Nervous system (N) > Psycholeptics (N05) > Antipsychotics (N05A) > Phenothiazine derivatives with aliphatic structure (N05AA) > Levomepromazine (N05AA02)

Release form, composition and packaging

tab., cover coated, 25 mg: 50 pcs.
Reg. No.: RK-LS-5-No. 004387 dated 07/08/2011 - Valid

Film-coated tablets white, round, slightly biconvex, odorless.

Excipients: lactose monohydrate, potato starch, microcrystalline cellulose, povidone K-25, sodium carboxymethyl starch (type A), magnesium stearate.

Shell composition: hypromellose, titanium dioxide (E171), dimethicone (E-1049).

50 pcs. - dark glass bottles (1) - cardboard packs.

Description of the drug TIZERTSIN ® tablets created in 2013 on the basis of instructions posted on the official website of the Ministry of Health of the Republic of Kazakhstan. Date updated: 12/25/2013

Pharmacological action

Tizercin is an antipsychotic from the group of phenothiazine derivatives. Acting on dopamine receptors of the thalamus, hypothalamus, reticular formation, limbic system, levomepromazine inhibits sensory stimulation. Reduces motor activity and has a strong sedative effect. In addition, it is an antagonist of other neurotransmitter systems (noradrenergic, serotonergic, histaminergic and cholinergic). Therefore, levomepromazine has antiemetic, antihistamine, antiadrenergic and anticholinergic effects. Levomepromazine is an analogue of chlorpromazine with a more pronounced effect of inhibition of psychomotor activity compared to chlorpromazine. Extrapyramidal side effects less pronounced than with other antipsychotics. The drug is a strong alpha-adrenergic receptor antagonist, but has a weak anticholinergic effect. Levomepromazine increases pain threshold(analgesic effectiveness comparable to morphine) and has an amnestic effect. Due to its ability to enhance the effects of analgesics, this drug can be used for adjuvant therapy for severe acute and chronic pain syndrome.

Pharmacokinetics

After oral administration, Cmax in blood plasma is reached within 1-3 hours. Levomepromazine is rapidly metabolized to form sulfate and glucuronide conjugates, which are excreted in the urine. A small part of the administered dose (1%) is excreted unchanged in urine and feces. T 1/2 – 15-30 hours.

Indications for use

psychomotor agitation of various etiologies: in schizophrenia (acute and chronic), in bipolar disorders, with psychoses (senile, intoxication and others), with mental retardation, with epilepsy;
other mental disorders, occurring with agitation, anxiety, panic, phobias, persistent insomnia;
adjuvant therapy for chronic psychoses: chronic hallucinatory psychoses;
enhancing the effect of analgesics, general anesthesia, antihistamines;
pain syndrome (neuralgia trigeminal nerve, neuritis facial nerve, herpes zoster).

Dosage regimen

Use the drug strictly as prescribed by your doctor.

Treatment should begin with low doses, which can then be gradually increased depending on tolerability of the drug. After the patient’s condition improves, the dose should be reduced to a maintenance dose, the amount of which is determined individually. The duration of treatment is determined by the doctor individually, depending on clinical condition patient.

For psychosis, the initial dose is 25-50 mg (1-2 tablets) 2 times a day daily. If necessary, initial daily dose can be increased to 150-250 mg (in 2-3 doses). In patients resistant to other antipsychotics, the daily dose can be increased by 50-75 mg/day.

Side effects

Often: decreased blood pressure, tachycardia, orthostatic hypotension (with accompanying weakness, dizziness and fainting), Morgagni-Adams-Stokes syndrome, prolongation of the QT interval (proarrhythmogenic effect, pirouette-type tachycardia).

Rarely:

dry mouth, discomfort in the abdominal area, nausea, vomiting, constipation, liver damage (jaundice, cholestasis), photosensitivity, erythema, urticarial elements, pigmentation, exfoliative dermatitis, pancytopenia, agranulocytosis, leukopenia, eosinophilia, thrombocytopenia, disorientation, confusion, visual hallucinations, slurred speech, extrapyramidal symptoms (dyskinesia, dystonia, parkinsonism, opisthotonus, hyperreflexia), epileptic seizures, increased intracranial pressure, reactivation psychotic symptoms, catatonia, galactorrhea, disorders menstrual cycle, weight loss, pituitary adenoma (described in some patients taking phenothiazines, but establishing a causal relationship with these drugs requires additional research), discoloration of urine, urination problems.

Very rarely: uterine contractions, deposits in the lens and cornea, pigmentary retinopathy, asthma, laryngeal edema, peripheral edema, anaphylactoid reactions, hyperthermia, vitamin deficiency.

Contraindications for use

hypersensitivity to phenothiazines or other components of the drug;
simultaneous administration antihypertensive drugs;
overdose of drugs that cause central depression nervous system(alcohol, general anesthetics, sleeping pills);
angle-closure glaucoma;
urinary retention;
Parkinson's disease;
multiple sclerosis;
myasthenia gravis, hemiplegia;
severe cardiomyopathy (circulatory failure);
severe renal or liver dysfunction;
pronounced arterial hypotension;
spicy infectious diseases viral, fungal or bacterial nature(incl. chicken pox, herpes zoster); coma caused by intoxication with ethanol, drugs and sleeping pills;
diseases of the hematopoietic organs;
porphyria;
lactation period;
children up to 12 years of age.

Use during pregnancy and breastfeeding

The drug should not be used during pregnancy unless a careful comparison of risks and benefits has been made. Levomepromazine is excreted in breast milk. In this regard, its use in breastfeeding contraindicated.

Special instructions

The use of the drug should be discontinued immediately if any hypersensitivity reaction occurs.

Particular caution is needed when prescribing the drug to patients with renal and/or liver failure due to the risk of accumulation and toxicity.

Elderly patients (especially those with dementia) have a significant predisposition to orthostatic hypotension, as well as the anticholinergic and sedative effects of phenothiazines. In addition, they are particularly prone to extrapyramidal side effects. Therefore, in elderly patients, the drug is prescribed with low initial doses and dose increases should be gradual.

To avoid orthostatic hypotension, the patient should lie down for half an hour after the first dose. If dizziness occurs frequently after using the drug, you should remain in bed after each dose.

In case of lactose intolerance, when planning the patient's diet, the lactose content (40 mg) in each tablet should be taken into account.

Caution is recommended when treating patients with a history of cardiovascular disease, especially in the elderly, as well as those with congestive heart failure, conduction disorders, arrhythmias, congenital long QT syndrome or unstable circulatory system. Before starting the use of Tizercin, an electrocardiogram should be recorded to exclude any cardiovascular disease that may serve as a contraindication.

Cases have been reported when taking phenothiazine antipsychotics: sudden death(possibly caused by cardiac reasons).

As with other phenothiazines, levomepromazine may cause QT prolongation, arrhythmias and, very rarely, torsade de pointes (TdP).

If hyperthermia is observed during antipsychotic therapy, neuroleptic malignant syndrome (NMS) should be excluded. ZNS - fatal dangerous disease, characterized by the following symptoms: muscle rigidity, hyperthermia, confusion, dysfunction of the autonomic nervous system (unstable blood pressure, tachycardia, arrhythmia, increased sweating), catatonia. Laboratory indicators:

increased levels of creatine phosphokinase (CPK), myoglobinuria (rhabdomyolysis) and acute renal failure. All these symptoms indicate the development of NMS. If they occur, as well as if, during treatment, hyperthermia of unknown etiology occurs without pronounced clinical symptoms ZNS, administration of Tizercin should be stopped immediately. If, after recovery from NMS, the patient's condition requires further antipsychotic therapy, the choice of drug should be carefully considered.

headache, tremor, increased sweating, tachycardia, insomnia and anxiety. Therefore, discontinuation of the drug should always be done gradually.

Many antipsychotics, including levomepromazine, can lower the epileptic seizure threshold and cause epileptiform changes in the electroencephalogram (EEG). Therefore, when selecting the dose of Tizercin in patients with epilepsy, you should constantly monitor clinical indicators and EEG.

The development of cholestatic jaundice depends on the individual sensitivity of the patient and completely disappears after stopping the drug administration. Therefore, during long-term treatment, regular monitoring of liver function indicators is required.

Agranulocytosis and leukopenia have also been observed in some patients treated with phenothiazines. Therefore, during long-term therapy, regular monitoring of the blood count is recommended, despite very low frequency these phenomena.

Prohibited use alcoholic drinks during treatment and until the effects of the drug disappear (within 4-5 days after stopping the use of Tizercin).

blood pressure (especially in patients with an unstable circulatory system and a predisposition to hypotension);
liver function tests (especially in patients with liver disease);
blood count (for fever and pharyngitis, as well as suspected leukopenia and agranulocytosis, at the beginning of treatment and during long-term therapy);
electrocardiogram (for cardiovascular diseases and in elderly patients).

Impact on the ability to drive vehicles and operate machinery

Overdose

Symptoms:

changes are vital important indicators(usually arterial hypotension and hyperthermia), conduction disorders in the heart muscle (prolongation of the QT interval, ventricular tachycardia/fibrillation, tachycardia of the “pirouette” type, atrioventricular block), extrapyramidal symptoms, sedation, excitation of the central nervous system (epileptic seizures) and ZNS.

Treatment: monitoring of the following parameters: acid-base balance, water-electrolyte balance, kidney function, urine volume, liver enzyme activity, electrocardiogram. In patients with NMS, serum CPK and body temperature should be monitored. In accordance with the measurements of monitored parameters, symptomatic treatment should be prescribed. For arterial hypotension:

intravenous administration fluids, Trendelenburg position, dopamine and/or norepinephrine (due to the proarrhythmogenic effect of levomepromazine, it is necessary to have a resuscitation kit ready;
When administering dopamine and/or norepinephrine, cardiac function should be monitored). For convulsive conditions, diazepam can be administered, and if seizures recur, phenytoin or phenobarbitone can be administered. For rhabdomyolysis, mannitol should be prescribed. A specific antidote is not known. Forced diuresis, hemodialysis and hemoperfusion are not effective. It is not recommended to induce vomiting, since possible epileptic seizures and dystonic reactions of the head and neck can lead to aspiration of vomit. Gastric lavage and monitoring of vital signs should be performed even 12 hours after dosing, since gastric emptying is slowed by the anticholinergic effect of levomepromazine. To further reduce absorption, it is recommended to administer activated carbon and laxatives.

Drug interactions

The simultaneous use of Tizercin with the following drugs should be avoided: antihypertensives due to the risk of severe arterial hypotension, monoamine oxidase inhibitors, since it is possible to increase the duration of the effect of Tizercin and the severity of its side effects.

Caution should be exercised when combined with the following:

anticholinergic drugs (tricyclic antidepressants; H 1 -antihistamines; some antiparkinsonian drugs; atropine, scopolamine, succinylcholine) due to increased anticholinergic effects (paralytic intestinal obstruction, urinary retention, glaucoma); when combined with scopolamine, extrapyramidal side effects were observed;
central nervous system depressants ( narcotic drugs, general anesthesia, anxiolytics, sedatives and hypnotics, tranquilizers, tricyclic antidepressants) enhance the effect of the drug on the central nervous system;
drugs that stimulate the central nervous system (for example, amphetamine derivatives) there is a decrease in the psychostimulating effect;
levodopa weakens the effect of this drug;
oral antidiabetic drugs : their effectiveness decreases and hyperglycemia may occur;
drugs that prolong the QT interval (some antiarrhythmic drugs, macrolide antibiotics, some azole antifungals, cisapride, some antidepressants, some antihistamines, as well as the indirect effect of diuretics that reduce potassium levels); these effects may be additive and increase the risk of arrhythmia;
dilevalol: by mutual inhibition of metabolism, this drug and Tizercin enhance each other’s effects; at joint use It may be necessary to reduce the dose of one or both drugs; a similar interaction with other beta blockers is possible;
drugs that cause photosensitivity, due to the risk of increasing it;
ethanol: the inhibitory effect on the central nervous system increases and the likelihood of developing extrapyramidal side effects increases;
other: simultaneous administration with vitamin C reduces the deficiency of this vitamin associated with the use of Tizercin.

Instructions for medical use

medicine

TIZERTSIN ®

Trade name

Tizercin ®

International nonproprietary name

Levomepromazine

Dosage form

Solution for injection 25 mg/1ml

1 ml of solution contains

active substance- levomepromazine (methotrimeprazine) 25 mg,

excipients : anhydrous citric acid , monothioglycerol,

sodium chloride, water for injection

Description

Colorless or almost colorless solution with a characteristic odor

Pharmacotherapeutic group

Psychotropic drugs. Neuroleptics. Phenothiazines with a dimethylaminepropyl group. Levomepromazine

ATX code N05A A02

Pharmacological properties

Pharmacokinetics

After intramuscular injection the maximum concentration in blood plasma is reached after 30-90 minutes. The apparent volume of distribution of levomepromazine is 23-42 l/kg. Levomepromazine is rapidly metabolized to form sulfate and glucuronide conjugates, which are excreted from

urine. A small part of the administered dose (1%) is excreted unchanged in urine and feces. The half-life is 15 - 30 hours. Levomepromazine has linear kinetics in the range of 10-300 ng/ml.

Pharmacodynamics

Tizercin is an antipsychotic from the group of phenothiazine derivatives. Acting on dopamine receptors of the thalamus, hypothalamus, reticular formation, and limbic system, levomepromazine inhibits sensory stimulation. Reduces motor activity and has a strong sedative effect. In addition, it is an antagonist of other neurotransmitter systems (noradrenergic, serotonergic, histaminergic and cholinergic). Therefore, levomepromazine has antiemetic, antihistamine, antiadrenergic and anticholinergic effects. Levomepromazine is an analogue of chlorpromazine with a more pronounced effect of inhibition of psychomotor activity compared to chlorpromazine. Extrapyramidal side effects are less pronounced than with other antipsychotics. The drug is a strong alpha-adrenergic receptor antagonist, but has a weak anticholinergic effect. Levomepromazine increases the pain threshold (analgesic effectiveness is comparable to morphine) and has an amnestic effect. Due to its ability to enhance the effects of analgesics, this drug can be used for adjuvant therapy in acute and chronic pain syndrome. The maximum analgesic effect develops within 20-40 minutes after intramuscular administration and lasts approximately 4 hours.

Indications for use

Acute psychoses with psychomotor agitation and severe anxiety:

Acute attack of schizophrenia

Other acute psychotic conditions

Adjuvant therapy for chronic psychoses:

Chronic schizophrenia

Chronic hallucinatory psychoses

Directions for use and doses

The drug is administered parenterally when it is not possible to take it orally.

The usual daily dose is 75-100 mg (in 2-3 doses or injections) in bed rest under the control of blood pressure and heart rate.

When administered intramuscularly, the drug should be injected deep into the muscle.

When administered intravenously, Tizercin must be diluted (50-100 mg of the drug in 250 ml saline solution or isotonic glucose solution) and administered slowly through a dropper.

The duration of treatment is determined by the doctor individually, depending on the clinical condition of the patient.

Instructions for opening ampoules (for right-handed people):

Take the ampoule into left hand, holding it between the big and index finger so that the break point is at the top. (Fig.1). Take the tip of the ampoule with your right hand, holding it between your thumb and bent index finger, so that thumb was located above the fault point (Fig. 2). Break off the tip of the ampoule by pressing down with your thumb right hand, fixing the ampoule with your left hand. Apply the bend with a medium constant force, without moving your hands closer or further away (Fig. 3). The neck of the ampoule can break off at any time so that you may not feel it (Fig. 4).

Side effects

No frequency data available adverse reactions.

Pancytopenia, agranulocytosis, leukopenia, eosinophilia, thrombocytopenia

Anaphylactoid reactions, laryngeal edema, peripheral edema, asthma

- weight loss, vitamin deficiency, glucose intolerance, hyperglycemia, hyponatremia, syndrome of inappropriate antidiuretic hormone secretion

Reactivation of psychotic symptoms, catatonia, confusion, disorientation, visual hallucinations, slurred speech, drowsiness.

Epileptic seizures, increased intracranial pressure, extrapyramidal symptoms (dyskinesia, dystonia, parkinsonism, opisthotonus, hyperreflexia), withdrawal syndrome, confusion, delirium, convulsions

- deposits in the lens and cornea, pigmentary retinopathy

- tachycardia, Adams-Stokes syndrome, prolongation of the QT interval (proarrhythmogenic effect, spindle-shaped ventricular tachycardia).

Venous thromboembolism, including pulmonary embolism and deep vein thrombosis, (the frequency of which is unknown)

Heat stroke in hot, humid conditions

Nausea, vomiting, constipation, which can become very severe and cause paralytic ileus, abdominal discomfort, dry mouth, liver damage (jaundice, cholestasis)

Necrotizing enterocolitis, possibly fatal (in very rare cases)

- exfoliative dermatitis, urticaria, erythema, photosensitivity, hyperpigmentation

- coloration of urine, difficulty urinating

- withdrawal symptoms in newborns

Galactorrhea, menstrual irregularities, in very rare cases - impaired uterine contractility, priapism

Neuroleptic malignant syndrome, hyperpyrexia, asthenia

Often:

Orthostatic hypotension (with associated weakness, dizziness and fainting)

Individual messages:

Cases of sudden death, possibly of cardiac origin, as well as cases of unexplained sudden death in patients receiving phenothiazine antipsychotics

Pituitary adenoma has been described in some patients chronically treated with phenothiazines, but further research is needed to establish a causal relationship with these drugs.

Contraindications

Hypersensitivity to phenothiazines and other components of the drug

Concomitant use of antihypertensive drugs

Concomitant use of monoamine oxidase inhibitors

Overdose of drugs that cause depression of the central nervous system (alcohol, general anesthetics, sleeping pills)

Angle-closure glaucoma

Urinary retention

Parkinson's disease

Multiple sclerosis

Myasthenia gravis, hemiplegia

Severe cardiomyopathy (circulatory failure)

Severe renal or liver dysfunction

Clinically significant hypotension

Acute infectious diseases of a viral, fungal or bacterial nature (including chicken pox, shingles); coma caused by intoxication with ethanol, drugs and sleeping pills

Diseases of the hematopoietic organs

Porphyria

Pregnancy and lactation

Children's age up to 12 years

Drug interactions

When levomepromazine is used concomitantly with drugs that are primarily metabolized by the cytochrome P450 2D6 enzyme system, the plasma concentrations of these drugs may increase, which may prolong or increase the effect or side effects of these drugs.

The simultaneous use of Tizercin with the following drugs is prohibited:

- antihypertensive due to the risk of severe arterial hypotension

Monoamine oxidase inhibitors, since it is possible to increase the duration of the effect of Tizercin and the severity of its side effects.

Extreme caution should be exercised when combined with the following:

Anticholinergic drugs (tricyclic antidepressants; H 1 -antihistamines; some antiparkinsonian drugs; atropine, scopolamine, succinylcholine) due to increased anticholinergic effects (paralytic ileus, urinary retention, glaucoma). When combined with scopolamine, extrapyramidal side effects were observed.

Central nervous system depressants ( narcotic analgesics, general anesthesia, anxiolytics, sedatives and hypnotics, tranquilizers, tricyclic antidepressants) enhance the effect of the drug on the central nervous system.

Drugs that stimulate the central nervous system (for example, amphetamine derivatives) have a psychostimulant effect.

Levodopa weakens the effect of this drug.

Oral antidiabetic drugs: their effectiveness is reduced and hyperglycemia may occur.

Drugs that prolong the QT interval (some antiarrhythmic drugs, macrolide antibiotics, some azole antifungals, cisapride, some antidepressants, some antihistamines, and the indirect effect of potassium-lowering diuretics); these effects may be additive and increase the risk of arrhythmia.

Dilevalol: by mutual inhibition of metabolism, this drug and Tizercin enhance each other's effects. If administered together, it may be necessary to reduce the dose of one or both drugs. A similar interaction with other beta blockers is possible.

Drugs that cause photosensitivity due to the risk of increasing it.

Ethanol: the inhibitory effect on the central nervous system increases and the likelihood of developing extrapyramidal side effects increases.

Other:

- simultaneous administration with vitamin C reduces the deficiency of this vitamin associated with the use of Tizercin.

Concomitant use of desferrioxyamine with prochlorperazine causes transient metabolic encephalopathy with loss of consciousness lasting 48 to 72 hours. Such an interaction is also possible with levomepromazine, since its pharmacological activity is largely similar to that of prochlorperazine.

Adrenaline (epinephrine) should not be used in case of overdose of antipsychotics.

Special instructions

The use of the drug should be discontinued immediately if any hypersensitivity reaction occurs.

Particular caution is required when prescribing the drug to patients with renal and/or hepatic impairment due to the risk of accumulation and toxicity.

Stroke

In randomized clinical studies In a placebo-controlled study of older patients with dementia treated with certain atypical antipsychotics, there was a 3-fold increased risk of developing disorders cerebral circulation. The mechanism for this increased risk is unknown. An increased risk of developing cerebrovascular accidents cannot be excluded for other antipsychotics or other patient groups. Tizercin should be used with caution in patients with risk factors for stroke.

Increased mortality in older patients with dementia

Two observational clinical studies showed that the use of antipsychotics in older patients with dementia had a small increased risk of mortality compared with untreated patients. These data are insufficient to accurately assess the risk, and the mechanism by which the risk increases is also unknown.

The use of Tizercin for the treatment of behavioral disorders in dementia is prohibited.

Elderly patients (especially those with dementia) have a greater predisposition to orthostatic hypotension and are also more sensitive to the anticholinergic and sedative effects of phenothiazines. In addition, they are particularly prone to extrapyramidal side effects. Therefore, low initial doses and gradual dose increases are especially important in this category of patients.

To avoid orthostatic collapse, the patient should lie down for half an hour after the first dose. If dizziness occurs after administration of the drug, you should remain in bed after each dose.

Injection sites should be changed whenever possible, since the drug may have a local irritant effect.

As with other phenothiazines, levomepromazine may cause QT prolongation, arrhythmias and, very rarely, torsade de pointes (TdP).

Cases of venous thromboembolism (VTE) have been observed during antipsychotic therapy. Since patients receiving antipsychotic drugs often have risk factors for acquired VTE, all possible factors risk and take the necessary preventive measures before and during treatment with Tizercin.

Hyperglycemia or glucose intolerance has been observed in patients receiving levomepromazine. Patients with an established diagnosis diabetes mellitus or with risk factors for diabetes who are prescribed treatment with levomepromazine, appropriate glycemic monitoring should be carried out throughout treatment.

If hyperthermia is observed during antipsychotic treatment, neuroleptic malignant syndrome (NMS) should be excluded. NMS is a deadly disease characterized by the following symptoms: muscle rigidity, hyperthermia, confusion, dysfunction of the autonomic nervous system (unstable blood pressure, tachycardia, arrhythmia, increased sweating), catatonia. Laboratory findings: increased creatine phosphokinase (CPK) levels, myoglobinuria (rhabdomyolysis) and acute renal failure. All these symptoms indicate the development of NMS. If they occur, as well as if hyperthermia of unknown etiology occurs during treatment without pronounced clinical symptoms of NMS, the administration of Tizercin should be stopped immediately. If, after recovery from NMS, the patient's condition requires further antipsychotic therapy, the choice of drug should be carefully considered.

Tolerance to the sedative effects of phenothiazines and cross-tolerance to various antipsychotics have been described in the literature. Such tolerance may explain signs of functional impairment that occur after sudden withdrawal of high or long-term doses: nausea, vomiting, headache, tremor, increased sweating, tachycardia, insomnia and restlessness. Therefore, discontinuation of the drug must be done gradually.

Many antipsychotics, including levomepromazine, can lower the epileptic seizure threshold and cause epileptiform electroencephalogram (EEG) changes. Therefore, when gradually adjusting the dose of Tizercin in patients with epilepsy, clinical parameters and EEG should be constantly monitored.

It is prohibited to consume alcoholic beverages during treatment and until the effects of the drug disappear (within 4-5 days after stopping the use of Tizercin).

Blood pressure (especially in patients with an unstable circulatory system and a predisposition to hypotension)

Liver function tests (especially in patients with liver disease)

Blood count (for fever and pharyngitis, as well as signs of leukopenia and agranulocytosis, at the beginning of treatment and during long-term therapy)

Electrocardiogram (for cardiovascular diseases and elderly patients).

Potassium level in the blood (periodic monitoring and correction of the level of electrolytes in the blood, especially with prolonged chronic use drug).

Features of the effect of the drug on the ability to drive vehicle or potentially dangerous mechanisms

Tizercin may cause drowsiness, disorientation, confusion, or significant hypotension, which may affect the patient's ability to drive.

Overdose

Symptoms: changes in vital physiological indicators (usually arterial hypotension and hyperthermia), conduction disturbances in the heart muscle (prolongation of the QT interval, ventricular tachycardia/fibrillation, tachycardia of the “pirouette” type, atrioventricular block), extrapyramidal symptoms, sedation, central nervous system excitation systems (epileptic seizures) and NMS.

Treatment: resuscitation measures, symptomatic therapy V specialized department hospital.

It is recommended to monitor the following parameters: acid-base balance, water-electrolyte balance, kidney function, urine volume, liver enzyme activity, ECG. In patients with neuroleptic malignant syndrome, serum CPK and body temperature should also be monitored. In accordance with the values of the monitored parameters, symptomatic treatment should be prescribed. For hypotension: intravenous fluids, Trendelenburg position, dopamine and/or norepinephrine (due to the proarrhythmogenic effect of levomepromazine, it is necessary to have a resuscitation kit ready and monitor the ECG). In case of an overdose of antipsychotics, adrenaline should not be used. Lidocaine (lignocaine) should be avoided and, if possible, antiarrhythmic drugs long-acting. For convulsive conditions, diazepam can be administered, and if seizures resume due to diazepam, phenytoin or phenobarbital can be administered. For rhabdomyolysis, mannitol should be prescribed. A specific antidote is not known. Forced diuresis, hemodialysis and hemoperfusion are ineffective. It is not recommended to induce vomiting, because... possible epileptic seizures and dystonic reactions of the head and neck can lead to aspiration of vomit. Gastric lavage and monitoring of vital signs should be performed even 12 hours after dosing, since gastric emptying is slowed by the anticholinergic effect of levomepromazine. To further reduce absorption, the administration of activated charcoal and laxatives is recommended.

Release form and packaging

1 ml in ampoules of colorless neutral glass with a break point for opening. A red and red code ring is applied to the rim of the ampoules with indelible paint. blue. A self-adhesive paper label is placed on each ampoule. 5 ampoules are placed in a blister pack made of polyvinyl chloride film and PET/PE film. 2 blister packs together with instructions for medical use in the state and Russian languages are placed in a cardboard pack.

Storage conditions

Store at a temperature not exceeding 25°C, protected from light.

Keep out of the reach of children!

Shelf life

Do not use after expiration date.

Conditions for dispensing from pharmacies

By prescription

Manufacturer

JSC "EGIS PHARMACEUTICAL PLANT"

1106 BUDAPEST, st. Keresturi, 30-38 Hungary

Any mental disorder requires complex therapy. And often the drug “Tizercin” is included in the treatment regimen. Reviews from experts indicate that the drug really helps to cope with psychomotor agitation that develops against the background various diseases(including schizophrenia and mental retardation).

Of course, people faced with the need to take medicine look for additional information. What properties does Tizercin have? Instructions for use, reviews, prices, analogues - these are important data that should be studied before starting therapy.

Features of the composition. Release form of the drug

Unfortunately, today many people are faced with the need to take the drug Tizercin. Instructions for use, price, reviews - this important facts. But first, it’s worth studying general characteristics means.

"Tizercin" is available in the form of small round tablets, coated film-coated. Main active component is levomepromazine (1 tablet - 25 mg of substance). In addition, the composition contains magnesium stearate, lactose, potato starch, povidone. Titanium dioxide, magnesium stearate, hypromellose, and dimethicone are used to make the shell.

In addition, the drug is prepared in the form of an injection solution. This is a clear liquid, packaged in 1 ml glass ampoules. One serving (ampoule) contains 25 mg of levomepromazine. As for excipients, the composition contains anhydrous citric acid, sodium chloride, monothioglycerol, and purified water as a solvent.

How does the product affect the body?

"Tizercin" is a very effective antipsychotic drug of the phenothiazine series. This antipsychotic blocks dopamine D2 receptors of the mesocortical and mesolimbic systems, thereby exerting an antipsychotic effect.

The drug has sedative properties - it calms the nervous system, relieves anxiety and irritability, copes with anxiety and other symptoms. By the way, the medicine also acts as a sleeping pill.

Tizercin tablets also have antiemetic and hypothermic properties. They relieve pain by acting as analgesics. In addition, during therapy there is a decrease in blood pressure.

The drug is quickly absorbed by the walls digestive tract. The maximum concentration of levomepromazine in the blood is observed approximately 1 to 3 hours after administration. The substance is quickly distributed throughout tissues and organs. Metabolism occurs in the liver - as a result chemical reactions glucuronide and sulfate conjugates are formed, which are excreted by the kidneys.

The drug "Tizercin": indications for use

Reviews indicate that this is a very effective antipsychotic. So in what cases do doctors recommend taking this drug?

The drug helps relieve diseases such as schizophrenia, epilepsy, mental retardation. The tablets are effective for various types of bipolar disorders and psychoses (including intoxication and senile).

In what other cases is it advisable to take Tizercin tablets? Reviews from experts say that the drug copes well with anxiety, panic attacks, persistent forms of insomnia, various phobias, agitation. As part of complex therapy, tablets are used for herpes zoster, facial neuritis, trigeminal neuralgia - they help relieve pain and alleviate the patient’s condition.

Instructions. Approximate dosages

For various psychomotor disorders, the drug "Tizercin" is often used. Reviews indicate that the medicine is really effective. But the dosage in this case is selected individually in each case.

The initial dose is 25 - 50 mg - it should be divided into several doses, with the maximum amount taken before bedtime. The dose is increased daily by 25 - 50 mg, bringing it to 200 - 300 mg per day. As soon as the patient’s condition is stabilized, the daily amount of the drug begins to be slowly reduced. Of course, you need to monitor the patient’s condition throughout the entire period, adjusting the dose depending on the appearance or disappearance of certain symptoms.

As a rule, therapy begins with intramuscular injection of the solution. This treatment is carried out in a hospital setting, since the patient’s condition (in particular, his blood pressure) must be constantly monitored. After improvements appear, the patient is transferred to outpatient treatment and prescribe pills.

Contraindications: who should not take the medicine?

Despite the fact that the drug is considered relatively safe, not everyone can take it. There are contraindications, and their list needs to be studied.

The medicine is not prescribed to patients with hypersensitivity to some of its constituent components, as well as phenothiazines.
Contraindications include chronic heart failure, liver and kidney failure.
The drug is not used for Parkinson's disease, multiple sclerosis.
Contraindications include angle-closure glaucoma, severe forms arterial hypertension, porphyria.
Tizercin is not prescribed to children (reviews indicate that in this case it is very difficult to choose an effective and safe dose).
The medicine is not recommended to be taken during pregnancy. If there is a need for therapy during lactation, then breastfeeding needs to stop.

Information about adverse reactions

What are the dangers associated with taking Tizercin? Reviews from doctors, as well as the results of statistical surveys, confirm that adverse reactions rarely develop during therapy. But you still need to familiarize yourself with their list.

Most often, therapy provokes disorders from cardiovascular system. While taking pills, blood pressure often decreases, leading to the development of orthostatic hypotension. Tachycardia is sometimes observed.
The drug can affect hematopoietic processes, causing eosinophilia, pancytopenia, leukopenia, and agranulocytosis.
The medicine affects the central nervous system. During therapy, the development of neuroleptic malignant syndrome is sometimes observed. Sometimes intracranial pressure increases. Some patients complain of slurred speech and confusion. Epileptic seizures may occur.
Therapy sometimes negatively affects metabolic processes and causes fluctuations hormonal levels. Sudden weight loss is possible. Sometimes the development of galactorrhea is observed. Women sometimes complain about menstrual irregularities.
Adverse reactions from the excretory system are possible. Their list includes urine retention, as well as its discoloration.
Sometimes there are disorders of the digestive tract. Some patients complain of nausea, constipation, and sometimes unpleasant painful sensations in the stomach, as well as dry mouth.
If we're talking about about long-term therapy, the development of pigmentary retinopathy is possible.
The possibility of developing allergic reactions. Therapy is sometimes associated with skin rash, itching, burning, the appearance of urticaria.

What to replace the medicine with?

What should a patient do who, for one reason or another, cannot take the antipsychotic drug Tizercin (EGIS)? Pharmacological market offers quite a large selection similar drugs. For example, Haloperidol is widely used for various mental disorders. Effective analogues This drug is also “Sulpiride” and “Droperidol”.

Of course, self-medication with antipsychotics is unacceptable. These are serious medications that affect the central nervous system. Their inept use can only further complicate the situation.

How much does the drug cost?

In modern medical practice The medicine Tizercin is often used. Instructions for use, reviews, indications and contraindications - information that must be studied. But for many patients one of important factors is the cost.

Of course, it is almost impossible to give an exact figure, because a lot here depends on the pricing policy of the pharmacy. On average, the cost of one package consisting of 50 tablets ranges from 210 to 280 rubles.

Medicine "Tizercin": reviews from patients and doctors

This drug often used in medical practice. Experts say that the medicine really helps relieve various symptoms psychomotor disorders. In the right dose, the tablets help cope with anxiety, nervousness, insomnia and other problems. The drug rarely causes any complications (despite the impressive list of adverse reactions), and there are not many contraindications.

You need to understand that diseases such as schizophrenia, bipolar disorders, mental retardation require complex treatment. These pills help relieve some symptoms, but do not cope with the disease itself.

Dosage form: solution for infusion and intramuscular administration Compound:

Active substance: levomepromazine 25 mg,

excipients: anhydrous citric acid 9 mg, monothioglycerol 7.5 mg, sodium chloride 6 mg, water for injection up to 1 ml.

Description: A colorless or slightly colored transparent solution with a characteristic odor. Pharmacotherapeutic group:Antipsychotic (neuroleptic) ATX:

N.05.A.A Phenothiazine derivatives with aliphatic structure

N.05.A.A.02 Levomepromazine

Pharmacodynamics:

Antipsychotic drug, (neuroleptic) phenothiazine series. It has an antipsychotic, sedative (hypnotic), analgesic, moderate antiemetic,hypothermic, moderately blocks H1-histamine and M-cholinergic receptors. Causes a decrease in blood pressure (BP).

The antipsychotic effect is due to the blockade of dopamine D 2-receptors of the mesolimbic and mesocortical system.

The sedative effect is due to the blockade of adrenergic receptors in the reticular formation of the brain stem; antiemetic effect - blockade of dopamine D 2-receptors - trigger zone of the vomiting center; hypothermic effect - blockade of dopamine receptors of the hypothalamus.

Extrapyramidal side effects of levomepromazine are less pronounced than those of “typical” antipsychotics. increases the pain threshold. Due to its ability to enhance the effects of non-narcotic analgesics, thisthe drug can be used for adjuvant therapy for acute and chronic pain syndrome. The maximum analgesic effect develops within 20-40 minutes after intramuscular administration and lasts approximately 4 hours.

Pharmacokinetics:

After intramuscular administration, the maximum concentration in the blood plasma is reached after 30-90 minutes. Passes through histohematic barriers, including the blood-brain barrier, and is distributed in organs and tissues.

Levomepromazine is rapidly metabolized in the liver by demethylation to form conjugates with sulfuric or glucuronic acid, which are excreted in the urine. Metabolite resulting from demethylation(N -desmethylmonomethotrimeprazine), has pharmacological activity, the remaining metabolites are inactive. A small part of the administered dose (1%) is excreted unchanged in urine and feces. The half-life is 15-30 hours.

Indications:

Psychomotor agitation of various etiologies:

- for schizophrenia (acute and chronic)

- for bipolar disorders

- for senile, intoxication and other psychoses

- for oligophrenia

- for epilepsy

as well as other mental disorders occurring with:

- agitation

- anxiety

- panic

- phobias

- persistent insomnia

Strengthening the effect of analgesics, general anesthesia, H1-histamine receptor blockers.

Pain syndrome(trigeminal neuralgia, facial neuritis, herpes zoster).

Contraindications:

- simultaneous use of antihypertensive drugs,

- hypersensitivity to the components of the drug and phenothiazine derivatives,

- overdose of drugs that cause inhibition of the central nervous system (alcohol, general anesthesia, sleeping pills),

- angle-closure glaucoma,

- urinary retention,

- Parkinson's disease,

- multiple sclerosis,

- myasthenia gravis, hemiplegia,

- chronic heart failure in the stage of decompensation;

- severe renal/liver failure,

- severe arterial hypotension,

- inhibition of bone marrow hematopoiesis (granulocytopenia),

- porphyria,

- breastfeeding,

- children up to 12 years of age.

With caution:

Epilepsy, patients with a history of cardiovascular diseases, especially in old age (cardiac muscle conduction disorders, arrhythmias, congenital long interval syndrome QT).

Pregnancy and lactation:

The drug should not be used during pregnancy unless the risk to the fetus has been carefully weighed against the benefit to the mother.

Levomepromazine penetrates into breast milk. In this regard, and in the absence of controlled studies, its use during breastfeedingcontraindicated. If it is necessary to take the drug during lactation, the issue of stopping breastfeeding should be decided.

Directions for use and dosage:

Parenteraladministration is used when it is impossible to take the drug orally. The usual daily dose is 75-100 mg (for 2-3 injections) in bed rest under the control of blood pressure and pulse. If necessary, the daily dose is increased to 200-250 mg. When administered intramuscularly, the drug should be injected deep into the muscle. Intravenous drip infusions are also used, for which the drug Tizercin® should be diluted (50 - 100 mg of the drug in 250 ml of 0.9% sodium chloride solution or 5% dextrose (glucose) solution) and administered slowly through a dropper. Clinical experience in parenteral use Levomepromazine is not enough for children under 12 years of age. If there are strict indications for children over 12 years of age, doses ranging from 0.35 mg/kg/day to 3.0 mg/kg/day are recommended.

Side effects:

From the outside cardiovascular system: lowering blood pressure,orthostatic hypotension (with accompanying weakness, dizziness and loss of consciousness), Adams-Stokes syndrome, tachycardia, prolongation of the interval QT (arrhythmogenic effect, pirouette-type arrhythmia) (see section "Special instructions"). Cases of sudden death (possibly caused by cardiac causes) have been reported when taking phenothiazine antipsychotics.

From the circulatory system and lymphatic system: pancytopenia, agranulocytosis, leukopenia, thrombocytopenia, eosinophilia.

From the central nervous system: drowsiness, dizziness, increased fatigue, confusion, slurred speech, visual hallucinations, catatonia, disorientation, extrapyramidal symptoms with a predominance of akinetic-hypotonic syndrome (dyskinesia, dystonia, parkinsonism, opisthotonus, hyperreflexia), epileptic seizures, increased intracranial pressure, malignant neuroleptic syndrome (NMS) (see also section "Special instructions").

From the side of metabolism: weight loss, galactorrhea, menstrual irregularities, mastalgia. Pituitary adenomas have been reported in some patients receiving phenothiazine derivatives, but further research is needed to establish a causal relationship between the use of these drugs and tumor development.

From the reproductive and urinary system: difficulty urinating, discoloration of urine, impaired contractions of the uterine muscles.

From the gastrointestinal tract: vomiting, nausea, constipation, discomfort in the abdominal area, dry mouth, liver damage (jaundice, cholestasis).

From the outside skin: exfoliative dermatitis, urticaria, erythema, photosensitivity, hyperpigmentation.

From the organs of vision: pigmentary retinopathy, deposits in the lens and cornea.

Allergic reactions: laryngeal edema, peripheral edema, anaphylactoid reactions, bronchospasm, urticaria, exfoliative dermatitis.

Other:hyperthermia (may be the first sign of NMS), pain and swelling at the injection sites.

Overdose:

Symptoms:decreased blood pressure, hyperthermia, conduction disturbances in the heart muscle (extension of the interval QT ventricular tachycardia of the "pirouette" type,atrioventricular block), depression of consciousness varying degrees severity (up to coma), extrapyramidal symptoms, sedation, epileptic seizures, neuroleptic malignant syndrome.

Treatment:It is recommended to monitor the following indicators: acid-base balance, fluid and electrolyte balance, kidney function, urine volume, liver enzyme activity, ECG readings, and in patients with neuroleptic malignant syndrome - additionally serum CPK levels and body temperature. Symptomatic treatment should be carried out based on the results of assessing the above parameters. If blood pressure decreases, intravenous fluid replacement, Trendelenburg position, dopamine and/or norepinephrine are indicated. (Due to the pro-arrhythmogenic effect of levomepromazine, it is necessary to provide conditions for resuscitation, and when administering dopamine and/or norepinephrine, an ECG must be performed). In case of overdose of antipsychotics, it is not recommended to use (adrenaline). The use of lidocaine (lignocaine) and, if possible, long-acting arrhythmic drugs should also be avoided.

To eliminate seizures, use either, in case of relapses of seizures, or phenobarbitone. If rhabdomyolysis occurs, it is prescribed. There is no specific antidote. Forced urination, hemodialysis and hemoperfusion are ineffective.

It is not recommended to induce vomiting, since intermittent epileptic convulsions and dystonic reactions of the muscles of the head and neck can lead to vomit entering the respiratory tract. Gastric lavage, along with monitoring vital signs, is indicated even 12 hours after taking the drug, since its natural emptying is slow due to the m-anticholinergic effect of levomepromazine. An additional reduction in drug absorption is achieved by usingactivated carbon and laxatives.

Interaction:

The simultaneous use of levomepromazine and the following drugs should be avoided:

- Antihypertensive drugs due to the risk of a pronounced decrease in blood pressure.

- Monoamine oxidase inhibitors (MAO), because possible increase duration of action of levomepromazine and increasing severity of its side effects.

Caution should be exercised when used simultaneously with the following drugs:

- Drugs with m-anticholinergic activity (tricyclic antidepressants; H1-histamine receptor blockers; some antiparkinsonian drugs; scopolamine, suxamethonium) enhance the m-anticholinergic effect of levomepromazine (paralytic intestinal obstruction, urinary retention, glaucoma). When used concomitantly with scopolamine, extrapyramidal side effects were observed.

- CNS depressants (narcotic analgesics, drugs for generalanesthesia, anxiolytics, sedatives and hypnotics, tranquilizers, tricyclic antidepressants), enhance the inhibitory effect of levomepromazine on the central nervous system.

- CNS stimulants (for example, amphetamine derivatives): reduces their psychostimulant effect.

- Levodopa: Reduces the effect of levodopa.

- Oral hypoglycemic agents: when used simultaneously with levomepromazine, their effectiveness decreases, which requires dose adjustment.

- Means that extend the interval QT (some antiarrhythmic drugs, macrolide antibiotics, some azole antifungals, cisapride, some antidepressants, some antihistamines, and diuretics that reduce the concentration of potassium in the blood), increase the risk of prolonging the interval QT and therefore increase the risk of arrhythmia.

- Drugs that cause photosensitivity, when used simultaneously with levomepromazine, increase the likelihood of photosensitivity.

- Alcohol increases central nervous system inhibition and increases the likelihood of extrapyramidal side effects when used simultaneously with levomepromazine.

- Antacids reduce absorption of gastrointestinal tract (should be prescribed 1 hour before or 4 hours after taking antacids).

- Drugs that inhibit bone marrow hematopoiesis increase the risk of myelosuppression.

- Dilevalol, like levomepromazine, inhibits metabolism, which leads to a mutual enhancement of the action of both medicines. If they are used simultaneously, it may be necessary to reduce the dosage of one or both drugs. A similar interaction with other beta-blockers is possible.

- Levomepromazine and its non-hydroxylated metabolites are potent cytochrome P450 inhibitors 2 D 6. Concomitant use of levomepromazine with metabolizable drugs. mainly via cytochrome P450 2 D 6 may lead to increased concentrations of these drugs, which may increase unwanted effects these drugs.

Special instructions:

The use of the drug should be discontinued if allergic reactions occur. Concomitant use with central nervous system depressants, MAO inhibitors and m-anticholinergics requires special caution (see section "Interaction with other drugs").

The drug should be prescribed with extreme caution to patients with impaired liver and/or kidney function.

Elderly patients are predisposed to orthostatic hypotension, as well as m-anticholinergic and sedative effect phenothiazines. In addition, they are particularly prone to extrapyramidal side effects. Therefore, treatment of these patients should begin with low doses and gradually increase them.

In older people with dementia who were treated with antipsychotics, there was a small increase in the risk of mortality. There are insufficient data to determine the exact magnitude of the risk, and the reason for this increased risk is unknown. Tizercin® is not approved for use in the treatment of behavioral disorders associated with dementia.

To avoid the development of orthostatic hypotension, the patient should lie down for half an hour after the first dose. If dizziness occurs after administration of the drug, you should remain in bed after each dose until the dizziness disappears.

In cases of parenteral administration of the drug Tisercin®, the injection sites should, if necessary, be alternated, since the drug can cause local irritation and tissue damage.

It is also necessary to be careful when prescribing the drug to patients (especially the elderly) with a history of cardiovascular diseases, patients with congestionheart failure, conduction disorders, arrhythmia, congenital long interval syndrome QT. Before starting treatment with Tizercin®, an ECG must be performed to exclude any cardiovascular disorder that may contraindicate the use of the drug.

There are reports of interval prolongation QT the occurrence of arrhythmia and, very rarely, arrhythmia of the “pirouette” type during therapy with phenothiazines (see section “Side effects”).

If hyperthermia occurs during antipsychotic therapy, the possibility of neuroleptic malignant syndrome (NMS) should be excluded. This potentially life-threatening syndrome is characterized by the following symptoms: muscle rigidity, hyperthermia, confusion, dysfunction of the autonomic nervous system (unstable blood pressure, tachycardia, arrhythmia, increased sweating), catatonia, increased activity of creatine phosphokinase (CPK), myoglobinuria (rhabdomyolysis ) and acute renal failure. If they occur, as well as if hyperthermia occurs during treatment unknown etiology without other clinical symptoms of NMS, the use of Tizercin® should be stopped immediately.

After sudden withdrawal of a drug used in high doses or for a long time, the following may occur: nausea, vomiting, headache, tremor, increased sweating, tachycardia, insomnia and anxiety, as well as the development of tolerance to the sedative effects of phenothiazine derivatives and cross-tolerance to various antipsychotics. For this reason, drug withdrawal should always be done gradually.

Many antipsychotics, including, can lower the seizure threshold and cause epileptiform ECG changes. For this reason, when titrating the dose of Tizercin®, all patients with epilepsy must ensure careful clinical observation and ECG monitoring.

The development of cholestatic jaundice depends on the individual sensitivity of the patient and completely disappears after stopping the use of the drug. Therefore, during long-term treatment, regular monitoring of liver function is required.

Agranulocytosis and leukopenia have been reported in some patients receiving phenothiazines. Despite the rarity of such cases, during long-term therapy with levomepromazine it is necessary to regularly monitor the leukocyte count.

During treatment and until the drug stops working (within 4-5 days after discontinuation of the drug), alcohol consumption is prohibited.

Before and during treatment, it is recommended to regularly monitor the following indicators: blood pressure, liver function (especially in patients with liver disease), leukocyte formula blood, ECG (for cardiovascular diseases and in elderly patients), potassium concentration in blood serum. Periodic monitoring of the level of electrolytes in the blood and its correction is necessary (especially when planning long-term therapy).

Impact on the ability to drive vehicles. Wed and fur.:

At the beginning of treatment (for a period the duration of which depends on the patient’s response), driving a car and performing work associated with an increased risk of accidents is prohibited. Subsequently, the severity of the ban is determined individually for each patient.

Release form/dosage:Solution for infusion and intramuscular administration 25 mg/ml. Package:

1 ml in ampoules made of colorless hydrolytic glass type I, with red and blue code rings and with a break point. 5 ampoules per blister pack, sealed with PVC/PET/PE film. 2 blister packs in a cardboard box along with instructions for use.

Storage conditions:

In a place protected from light at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Best before date: 2 years. Do not use the drug after the expiration date indicated on the package. Conditions for dispensing from pharmacies: By prescription Registration number: P N012432/01 Registration date: 20.09.2011 Owner Registration certificate: Hungary Manufacturer: Representative office: EGIS CJSC pharmaceutical plant Hungary Information update date: 29.10.2015 Illustrated instructions