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Tizercin application. Tizercin: instructions for use, analogues and reviews, prices in Russian pharmacies

One tablet of Tizercin contains 25 mg levomepromazine. Additional substances: sodium starch glycolate, magnesium stearate, potato starch, microcrystalline cellulose, povidone, lactose. Shell composition: magnesium stearate, titanium dioxide, , hypromellose.
One milliliter of Tizercin solution contains 25 mg levomepromazine. Additional substances: sodium chloride, monothioglycerol, anhydrous citric acid, water.

Release form

White, biconvex, round, odorless tablets. 50 tablets in a brown glass bottle with an accordion shock absorber and initial opening control - one such bottle in a cardboard pack.
Colorless transparent solution with a specific odor. 1 ml of solution in a glass ampoule with a break point - five ampoules in a contour package - two packages in a cardboard box.

pharmachologic effect

Antipsychotic, antihistamine, antiemetic, sedative, hypothermic, analgesic, m-anticholinergic effect.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Phenothiazine-type neuroleptic . It has antipsychotic, antiemetic, sedative, hypothermic, antihistamine, analgesic, and anticholinergic effects. Reduces blood pressure.

Antipsychotic effect caused by blockade D2 dopamine receptors mesocortical and mesolimbic systems of the brain.

Sedative effect caused by blockade adrenaline receptors reticular formation of the brain; hypothermic - blockade hypothalamic dopamine receptors ; antiemetic - blockade D2 dopamine receptors vomiting center. Extrapyramidal side effects are less pronounced with levomepromazine than with “classical” antipsychotics.

Increases the pain threshold. Due to its ability to enhance the effect of anesthesia and antihistamines, Tizercin can be used for additional therapy for pain. The greatest analgesic effect is achieved within 40 minutes after intramuscular administration and lasts four hours.

Pharmacokinetics

After oral administration, the highest concentration is recorded on average after 2 hours, and after intramuscular administration - after 60 minutes.

Actively penetrates through any histohematic barriers and is distributed in various organs and tissues. It is rapidly transformed in the liver, undergoing demethylation with the formation of final glucuronide and sulfate conjugates, which are evacuated in the urine. N-desmethylomono-methotrimeprazine - the only one with pharmacological activity, other metabolites are inactive.

The half-life is approximately 20-25 hours. A small part of the dose taken (up to 1%) is excreted in its original form in urine and feces.

Indications for use

Psychomotor agitation at psychoses, bipolar disorders, oligophrenia, .
Other mental disorders complicated by anxiety, agitation , phobias, panic, persistence.
The need to enhance the effects analgesics , drugs for general anesthesia , inhibitors of H1-histamine receptors.
Pain syndrome (inflammation of the facial nerve, trigeminal , shingles ).

Contraindications

overdose of drugs that have a suppressive effect on the nervous system ( general anesthetics , alcohol, sleeping pills );
sharing antihypertensive drugs;
closed angle;
multiple sclerosis;
hemiplegia;
myasthenia gravis;
urinary retention;
chronic cardiac failure in the stage of decompensation;
pronounced hepatic or ;
suppression of bone marrow hematopoiesis;
heavy arterial hypotension;
lactation;
porphyria;
hypersensitivity to the components of the drug or other phenothiazines;
age less than 12 years.

The drug is used with caution in elderly patients and in people with a history of cardiac diseases.

Side effects

Phenomena from the outside blood circulation: orthostatic hypotension , pressure reduction, Adams-Stokes syndrome , increase QT interval, . Using phenothiazine antipsychotics cases of sudden death are known.
Phenomena from the outside hematopoiesis: agranulocytosis, pancytopenia, leukopenia, thrombocytopenia, eosinophilia.
Phenomena from the outside nervous activity: dizziness, drowsiness, fatigue, visual hallucinations, confusion, increased intracranial pressure, catatonia , slurred speech, extrapyramidal symptoms , orientation disorder, epileptic seizures .
Phenomena from the outside metabolism: changes in the menstrual cycle, galactorrhea , weight loss, mastalgia . Development reported pituitary adenomas in a number of patients using phenothiazine derivatives , but further research is needed to prove a cause-and-effect relationship.
Phenomena from the outside genitourinary area: discoloration of urine, difficulty urinating, impaired uterine contractions.
Phenomena from the outside digestion: abdominal discomfort, dry mouth, vomiting, nausea, liver damage.
Phenomena from the outside skin: hyperpigmentation, erythema, photosensitivity.
Phenomena from the outside vision: pigmentary retinopathy.
Allergic reactions: peripheral, laryngeal edema, bronchospasm, anaphylactoid reactions, exfoliative dermatitis.
Other phenomena: hyperthermia , pain and swelling in the injection area.

Instructions for use of Tizercin (Method and dosage)

The instructions for use of Tizercin allow the drug to be administered orally, starting from 25-50 mg per day, divided into several doses. The dose is increased by 25-50 mg daily until the condition improves. Those who are insensitive to others antipsychotics For patients, the daily dose is allowed to be increased by 50-75 mg per day. Average doses are 200-300 mg per day. After improvement and stabilization of the condition, the dose should be reduced to maintenance (determined individually).

Patients with neurotic disorders in outpatient practice, the drug is prescribed at a dose of 12.5-50 mg per day.

Parenteral use

This delivery route is used when it is not possible to take the drug orally. The daily dose is usually 75-100 mg and is divided into 2-3 injections, which are carried out in bed rest and under the control of blood pressure and pulse. If necessary, the daily dose is increased to 200-250 mg.

The solution can be administered deeply intramuscularly or intravenously. For intravenous drip infusion, 50-100 mg of the drug must be diluted in 250 ml saline solution or 5% glucose solution and inject slowly through an IV.

Overdose

Signs of overdose: decreased blood pressure, conduction disturbances, hyperthermia , depression of consciousness up to, sedation, extrapyramidal symptoms, epileptic seizures.

Treatment of overdose: monitoring and correction of fluid balance, electrolytes and acid-base balance, renal function, diuresis , concentration hepatic, ECG . Symptomatic treatment is carried out based on an assessment of the results of the above indicators. If pressure decreases, intravenous fluid administration, Trendelenburg position, injection or Norepinephrine . It is recommended to provide conditions for resuscitation due to the proarrhythmogenic effect levomepromazine.

In case of overdose antipsychotics not recommended to use , And arrhythmic drugs long-acting. For the treatment of seizures, it is prescribed or Phenytoin (with repetitions seizures ). During development rhabdomyolysis introduce . Selective is absent.

It is not recommended to induce artificial vomiting, since epileptic seizures, dystonic movements muscles of the head or neck can lead to the penetration of vomit into the respiratory tract.

Gastric lavage is performed with monitoring of vital signs. Additional suppression of drug absorption is achieved by using enterosorbents And laxatives.

Interaction

Should not be used simultaneously with Levomepromazine antihypertensive drugs and MAO inhibitors.

m-anticholinergic drugs (H1-histamine receptor inhibitors, tricyclic antidepressants);
row Aantiparkinsonian drugs;
, Suxamethonium;
drugs that suppress the nervous system (general anesthesia, opioids, sedatives And sleeping pills, anxiolytics, tricyclic antidepressants, tranquilizers );
drugs that stimulate the nervous system ( derivatives amphetamine and other drugs);
hypoglycemic oral agents;
means that increase QT interval ;
means that cause photosensitivity ;
ethanol;
antacids;
drugs that suppress bone marrow hematopoiesis;
Dilevalol (Dosages of both drugs may need to be reduced).

Levomepromazine and him non-hydroxylated derivatives are powerful blockers CYP2D6. Concomitant use with drugs metabolized by CYP2D6 , leads to an increase in their concentration and increased undesirable effects.

Terms of sale

On prescription.

Storage conditions

Keep away from children. Store at room temperature in a dark place.

Best before date

special instructions

Combined use with MAO inhibitors , drugs that depress the nervous system, and m-anticholinergics requires extreme caution.

Tizercin should be prescribed with caution to patients with liver or kidney damage.

Elderly people are predisposed to developing orthostatic hypotension , as well as a sedative and anticholinergic effect phenothiazines . They are more likely to experience side effects extrapyramidal effects .

In cases of parenteral use of the drug, the injection sites should be alternated, since local irritation and tissue changes may occur.

Caution must be exercised when using the drug in patients (especially the elderly), suffering from cardiac diseases, patients with congestive heart failure , conduction disorders, elongated QT interval.

When hyperthermia during treatment antipsychotics it is necessary to exclude the possibility of occurrence neuroleptic malignant syndrome , which poses a threat to life and is characterized by the following symptoms: confusion, hyperthermia, muscle rigidity , disruption of the autonomic system, increased activity creatine phosphokinase, catatonia, myoglobinuria And . If such symptoms occur or hyperthermia of unknown origin, the use of the drug must be stopped immediately.

After abrupt withdrawal of a drug used for a long time or in large doses, vomiting, nausea, increased sweating, , , anxiety, tolerance to sedative effects phenothiazine derivatives and cross-tolerance towards others antipsychotics . For these reasons, Tizercin should always be discontinued gradually.

Development cholestatic type jaundice depends on the individual characteristics of the patient. This symptom completely disappears after stopping use of the drug, so long-term treatment requires constant monitoring of liver parameters.

Before and during treatment, it is necessary to regularly monitor the following indicators: liver function, leukocyte count, ECG (for cardiac diseases and elderly patients), content potassium in blood. It is also necessary to periodically monitor the ratio plasma electrolytes and its correction.

During the initial period of treatment, operating mobile mechanisms is strictly prohibited. The duration of the ban is determined in each case individually.

Analogs

Level 4 ATX code matches:

For children

Not for use in children under 12 years of age. For children over 12 years of age, if indicated, dosages of 0.35-3 mg per kilogram of body weight per day are recommended.

With alcohol

It is prohibited to combine the drug with alcohol-containing drinks.

During pregnancy and lactation

During these periods, you should refrain from taking the drug.

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

pharmachologic effect

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 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: with schizophrenia (acute and chronic), with bipolar disorders, with psychoses (senile, intoxication and others), with oligophrenia, 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 (trigeminal neuralgia, facial neuritis, 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 the clinical condition of the patient.

For psychosis, the initial dose is 25-50 mg (1-2 tablets) 2 times a day daily. If necessary, the 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, abdominal discomfort, nausea, vomiting, constipation, liver damage (jaundice, cholestasis), photosensitivity, erythema, urticaria, 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 of psychotic symptoms, catatonia, galactorrhea, menstrual irregularities, weight loss, pituitary adenoma (described in some patients, taking phenothiazines, however, additional research is needed to establish its causal relationship with these drugs), discoloration of urine, and urinary disorders.

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 use of antihypertensive drugs;
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;
severe arterial 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;
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 during breastfeeding is contraindicated.

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 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 of sudden death (possibly caused by cardiac causes) have been reported when taking phenothiazine antipsychotics.

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. 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 indicators:

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 the signs of functional impairment that occur after sudden withdrawal of high or long-term doses: nausea, vomiting,

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 electroencephalogram (EEG) changes. Therefore, when selecting the dose of Tizercin in patients with epilepsy, clinical parameters and EEG should be constantly monitored.

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 the very low frequency of these phenomena.

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 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 in vital signs (usually arterial hypotension and hyperthermia), conduction disturbances in the heart muscle (prolongation of the QT interval, ventricular tachycardia/fibrillation, pirouette-type tachycardia, atrioventricular block), extrapyramidal symptoms, sedation, central nervous system excitation ( epileptic seizures) and NMS.

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 fluids, Trendelenburg position, dopamine and/or norepinephrine (due to the pro-arrhythmogenic 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, the administration of activated charcoal and laxatives is recommended.

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 ileus, urinary retention, glaucoma); when combined with scopolamine, extrapyramidal side effects were observed;
drugs that depress the central nervous system (narcotics, 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, 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; when used 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.

Tizercin is a neuroleptic drug. The effect of the drug is determined by the substance levomepromazine, which is able to block dopamine receptors (D2) in the brain. Also, Tizercin also blocks adrenergic receptors. The result of these biochemical interactions is the antipsychotic and sedative effect of the drug. In addition, the following effects are described for Tizercin: antiemetic, the ability to reduce body temperature and blood pressure. This antipsychotic drug also has the ability to raise the pain threshold and enhance the effect of analgesic drugs. Therefore, acute pain can be treated with Tizercin.

Tizercin is used for:

Psychomotor agitation, which may accompany schizophrenia, bipolar disorder, mental retardation, epilepsy, psychosis (for example, senile);
Psychomotor disorders characterized by agitation, anxiety, persistent sleep disturbances, panic;
The need to enhance the effect of painkillers or antihistamines;
Pain caused by facial neuritis, ternary neuralgia, postherpetic neuralgia, and so on.

Tizercin is produced both in solution and in tablets. Infusions and injections of this medication are carried out for those patients who are unable to take this drug orally, as well as for those whose condition requires prompt correction. The instructions for the drug Tizercin demonstrate that its dosage regimen does not differ fundamentally from the tactics of prescribing most similar drugs. Namely, the initial dose of the drug is increased to effective, and then reduced to maintenance. Since this drug reduces blood pressure, the patient must remain in bed.

Tizercin is contraindicated for:

Overdose of alcohol, sleeping pills, anesthetics;
Multiple sclerosis;
Urinary retention;
Angle-closure glaucoma;
Parkinsonism;
Porphyria;
Myasthenia gravis and many other pathological conditions;
Lactation, children under twelve years of age;

- with caution when –

Pregnancy, in old age, especially with diseases of the cardiovascular system, epilepsy, kidney and liver diseases, and so on.

Side effects and overdose of Tizercin

The cardiovascular system is susceptible to undesirable effects of Tizercin - blood pressure may decrease and heart function may be impaired. During therapy with this and drugs from the phenothiazine group, sudden pain may occur, possibly caused by cardiac dysfunction. In addition, side effects from the following systems are described: hematopoietic, nervous, endocrine, digestive, urinary, visual. Skin reactions, systemic intolerance reactions, and so on are possible.

It is not even worth describing in particular detail what symptoms accompany an overdose of Tizercin. It must be said that this can be a very serious and life-threatening condition. The patient requires resuscitation therapy.

Reviews of Tizercin

As surprising as it may sound, reviews of Tizercin are usually associated with its sedative effect. This powerful and dangerous antipsychotic is prescribed and taken for insomnia! Of course, the cases described by patients are “out of the ordinary” and the details of these situations suggest that Tizercin was prescribed not only to restore sleep, but also for direct indications, that is, for psychosis.

For example, a young man described his story, which began with taking “loading doses” (Piracetam), and then continued with Phenibut and Tizercin. Simply put, the patient stopped sleeping altogether. He fell asleep for a short time only after taking Tizercin in such an amount that it becomes strange how he survived at all.

It is unfortunate that this case is not the only one, although it is rare. Patients also describe side effects of Tizercin - decreased mood and motivation.

I constantly feel lethargic and my blood pressure is very low – I can barely crawl...

Doctors, when asked their opinion about such schemes for using Tizercin, answer:

This is an old and dangerous antipsychotic that used to treat psychosis. Take care of your health - find an adequate doctor who will select modern therapy for you.

Perhaps we should join this opinion of experts. Under no circumstances should you take Tizercin on your own. If your doctor prescribes this drug for you to use at home, it is better to be in touch with this doctor in order to discuss possible changes in your condition in a timely manner.

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General impression: (179)

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 of various diseases (including schizophrenia and mental retardation).

Of course, people faced with the need to take medication are looking 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 - these are important facts. But first, it’s worth studying the general characteristics of the product.

"Tizercin" is available in the form of small round film-coated tablets. The main active ingredient 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 the excipients, the composition contains anhydrous citric acid, sodium chloride, monothioglycerol, as well as 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 of the 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 of 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, and 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 prescribed 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 any of its components, as well as to phenothiazines.
Contraindications include chronic heart failure, liver and kidney failure.
The drug is not used for Parkinson's disease or multiple sclerosis.
Contraindications include angle-closure glaucoma, severe forms of arterial hypertension, and 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 should be stopped.

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 of the 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 hormonal fluctuations. 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, unpleasant and sometimes painful sensations in the abdomen, and dry mouth.
If we are talking about long-term therapy, then the development of pigmentary retinopathy is possible.
The possibility of developing allergic reactions should not be excluded. Therapy is sometimes associated with skin rash, itching, burning, and 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)? The pharmacological market offers a fairly large selection of such drugs. For example, Haloperidol is widely used for various mental disorders. Effective analogues of this drug are 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 drug Tizercin is often used. Instructions for use, reviews, indications and contraindications - information that must be studied. But for many patients, cost is one of the important factors.

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 is often used in medical practice. Experts say that the medicine really helps relieve various symptoms of 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.

Antipsychotic drug (neuroleptic)

Active substance

Levomepromazine

Release form, composition and packaging

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

Excipients: magnesium stearate - 1 mg, sodium starch glycolate - 2 mg, - 8 mg, microcrystalline cellulose - 10 mg, potato starch - 15.2 mg, lactose - 40 mg.

Shell composition: titanium dioxide - 0.758 mg, hypromellose - 2.632 mg, dimethicone - 0.355 mg, magnesium stearate - 0.255 mg.

50 pcs. - brown glass bottles with a PE cap, with first opening control and an accordion shock absorber (1) - cardboard packs.

Solution for infusion and intramuscular administration colorless or slightly colored, transparent, with a characteristic odor.

Excipients: anhydrous citric acid - 9 mg, monothioglycerol - 7.5 mg, - 6 mg, liquid water - up to 1 ml.

1 ml - ampoules made of colorless glass type I (5), with red and blue code rings and with a break point - contour cell packaging (2) - cardboard packs.

pharmachologic effect

Antipsychotic drug (neuroleptic) of the phenothiazine series. It has antipsychotic, sedative (hypnotic), analgesic, moderate, hypothermic, moderate antihistamine and m-anticholinergic effects. Causes a decrease in blood pressure.

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 of the 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 “classical” antipsychotics. Levomepromazine increases the pain threshold. Due to its ability to enhance the effects of general anesthesia and antihistamines, this 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

Suction

After oral administration, Cmax in the blood is reached within 1-3 hours.

After intramuscular administration, Cmax in blood plasma is reached within 30-90 minutes.

Distribution

Penetrates through histohematic barriers, including the BBB, and is distributed in organs and tissues.

Metabolism

Levomepromazine is rapidly metabolized in the liver by demethylation to form sulfate and glucuronide conjugates, which are excreted in the urine. The metabolite formed as a result of demethylation (N-desmethylomono-methotrimeprazine) has pharmacological activity, the remaining metabolites are inactive.

Removal

T 1/2 is 15-30 hours.

A small part of the administered dose (1%) is excreted unchanged in urine and feces.

Indications

psychomotor agitation of various etiologies: in schizophrenia (acute and chronic), in bipolar disorders, in psychoses (including senile and intoxication), in oligophrenia, in epilepsy;
other mental disorders occurring with agitation, anxiety, panic, phobias, persistent insomnia;
enhancing the effect of analgesics, general anesthesia, histamine H1 receptor blockers;
pain syndrome (trigeminal neuralgia, facial neuritis, herpes zoster).

Contraindications

simultaneous use of antihypertensive drugs;
overdose of drugs that have a depressant effect on the central nervous system (alcohol, general medications, 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 failure;
severe liver failure;
severe arterial hypotension;
inhibition of bone marrow hematopoiesis (granulocytopenia);
porphyria;
lactation;
children under 12 years of age;
hypersensitivity to levomepromazine and other phenothiazines.

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

Dosage

Inside prescribed starting with a dose of 25-50 mg/day in several doses (the maximum part of the daily dose should be prescribed before bedtime), increasing it daily by 25-50 mg until the patient’s condition improves. In patients resistant to other antipsychotics, the daily dose can be increased more quickly, increasing it by 50-75 mg/day. Average daily doses are 200-300 mg.

After the patient’s condition improves, the dose should be reduced to a maintenance dose, the amount of which is determined individually.

IN outpatient practice for patients with neurotic disorders the drug is prescribed in a daily dose of 12.5-50 mg (1/2-2 tablets).

Parenterally the drug is administered when it is not possible to take it orally. The daily dose is 75-100 mg, divided into 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.

Injected intramuscularly (deeply) or intravenously.

For administration as an intravenous drip infusion (50-100 mg) should be diluted in 250 ml of 0.9% sodium chloride solution or 5% dextrose (glucose) solution and administered slowly through a dropper.

Clinical experience on parenteral use of the drug in children under 12 years of age not enough. If there are strict indications, doses of 0.35-3 mg/kg body weight/day are recommended for children over 12 years of age.

Side effects

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

From the hematopoietic system: pancytopenia, agranulocytosis, leukopenia, eosinophilia, thrombocytopenia.

From the side of 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, NMS.

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 digestive system: dry mouth, abdominal discomfort, nausea, vomiting, constipation, liver damage (jaundice, cholestasis).

From the skin: photosensitivity, erythema, hyperpigmentation.

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

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

Others: 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 (prolongation of the QT interval, ventricular tachycardia of the "pirouette" type, AV block), depression of consciousness of varying severity (up to coma), extrapyramidal symptoms, sedation, epileptic seizures, NMS.

Treatment: It is recommended to monitor the acid-base balance, fluid and electrolyte balance, kidney function, urine volume, liver enzyme activity, ECG readings, and in patients with NMS, additionally serum CPK levels and body temperature. Symptomatic treatment should be carried out based on the results of the assessment of the above parameters. In case of a decrease in blood pressure, intravenous fluid administration, Trendelenburg position, and the use of dopamine and/or norepinephrine are indicated. Due to the proarrhythmogenic 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 an overdose of antipsychotics, the use of adrenaline is not recommended. The use of lidocaine and, if possible, long-acting arrhythmic drugs should also be avoided. To eliminate seizures, use diazepam or, for recurrent seizures, phenytoin. If rhabdomyolysis occurs, mannitol 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 head and neck muscles 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 elimination is slow due to the m-anticholinergic effect of levomepromazine. An additional reduction in drug absorption is achieved by using activated carbon and laxatives.

Drug interactions

Concomitant use of levomepromazine and the following drugs should be avoided:

antihypertensive drugs due to the risk of a pronounced decrease in blood pressure;
MAO inhibitors, because it is possible to increase the duration of action of levomepromazine and increase the severity of its side effects.

Caution should be exercised when used concomitantly with the following drugs

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

CNS depressants (opioid analgesics, general anesthesia, anxiolytics, sedatives and hypnotics, tranquilizers, tricyclic antidepressants) enhance the inhibitory effect of levomepromazine on the central nervous system.

CNS stimulants (eg, amphetamine derivatives): levomepromazine reduces their psychostimulant effect.

Levodopa: Levomepromazine reduces the effect of levodopa.

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

Drugs that prolong the QT interval (some antiarrhythmic drugs, macrolide antibiotics, some azole antifungals, cisapride, some antidepressants, some antihistamines, and potassium-lowering diuretics) increase the risk of QT prolongation and therefore increase risk of arrhythmia.

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

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

Antacids reduce absorption in the gastrointestinal tract (levomepromazine 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 effect of both drugs. 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 inhibitors of CYP2D6. Concomitant use of levomepromazine with drugs primarily metabolized by CYP2D6 may result in increased concentrations of these drugs, which may increase the adverse effects of these drugs.

special instructions

The use of the drug should be discontinued if allergic reactions occur.

Concomitant use with CNS depressants, MAO inhibitors and m-anticholinergics requires special caution.

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 the m-anticholinergic and sedative effects of phenothiazines. In addition, they are particularly prone to extrapyramidal side effects. Therefore, treatment of these patients should be started with low doses and gradually increased.

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 should not be used to treat 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 Tizercin, 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 congestive heart failure, conduction disorders, arrhythmia, and congenital long QT interval syndrome. Before starting treatment with Tizercin, an ECG should be performed to exclude any cardiovascular disorder that may contraindicate the use of the drug.

There have been reports of QT prolongation, arrhythmias and, very rarely, torsade de pointes (TdP) during phenothiazine therapy.

If hyperthermia occurs during antipsychotic therapy, the possibility of 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 CPK activity, myoglobinuria (rhabdomyolysis) and acute renal failure. If they occur, as well as if hyperthermia of unknown etiology occurs during treatment 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 effect of phenothiazine derivatives and cross-tolerance to various antipsychotics. For this reason, drug withdrawal should always be done gradually.

Many antipsychotics, incl. levomepromazine may lower the seizure threshold and cause epileptiform EEG changes. For this reason, when titrating the dose of Tizercin, all patients with epilepsy must ensure careful clinical observation and EEG 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 count, ECG (for cardiovascular diseases and in elderly patients), potassium concentration in the 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 and operate machinery

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.

Pregnancy and lactation

The drug should not be used during pregnancy, unless the expected benefit of therapy for the mother outweighs the potential risk to the fetus.

Adequate and strictly controlled clinical studies on the safety of Tizercin during lactation have not been conducted. Levomepromazine is excreted in breast milk. Given these facts, the use of the drug during breastfeeding is contraindicated. If it is necessary to use the drug during lactation, the issue of stopping breastfeeding should be decided.

Use in old age

WITH caution used in patients with a history of cardiovascular diseases, especially in old age (conduction disorders of the heart muscle,

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Storage conditions and periods

The drug belongs to list No. 1 of potent substances of the Standing Committee for Drug Control of the Ministry of Health of the Russian Federation.

The drug in the form of film-coated tablets should be stored out of the reach of children at a temperature of 15° to 25°C. Shelf life - 5 years.

The drug in the form of a solution for infusion and injection should be stored out of the reach of children, protected from light at a temperature not exceeding 25°C. Shelf life - 2 years.