Tisercin®

Compound

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

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

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

The antipsychotic effect is caused by blockade of D2-dopamine receptors in the mesocortical and mesolimbic systems of the brain.

The sedative effect is caused by the blockade of adrenaline receptors in the reticular formation of the brain; hypothermic – blockade of hypothalamic dopamine receptors ; antiemetic - blockade of D2-dopamine receptors of the 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 analgesics , anesthesia drugs 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 in the blood after an average of 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 is the only metabolite 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.

Pharmacological properties of the drug Tizercin

Tizercin is a phenothiazine neuroleptic that has antipsychotic, analgesic and moderate antiemetic effects. It relieves psychomotor agitation, has a sedative effect, exhibits antidepressant, adrenergic blocking, moderate anticholinergic and antihistamine activity. Causes hypotension. The maximum concentration in blood plasma is achieved 30–90 minutes after intramuscular administration. The metabolite formed as a result of demethylation has pharmacological activity, others are inactive. The half-life is 15–78 hours. Eliminated in urine and feces.

Indications for use

• Psychomotor agitation in psychosis, bipolar disorders, mental retardation, schizophrenia, epilepsy.
• Other mental disorders complicated by anxiety, agitation , phobias, panic, persistent insomnia .
• The need to enhance the effects of analgesics , drugs for general anesthesia , H1-histamine receptor inhibitors.
• Pain syndrome (inflammation of the facial nerve, trigeminal neuralgia , herpes zoster ).

Indications for use of the drug Tizercin

• psychomotor agitation of various etiologies: manic stage of manic-depressive psychosis, depressive-paranoid form of schizophrenia, catatonic agitation, reactive depression, alcoholic psychosis and other psychotonic states accompanied by symptoms of anxiety and fear;
• neurotic disorders with increased arousal, sleep disturbances;
• diseases accompanied by pain: trigeminal neuralgia, herpes zoster, etc.;
• itchy dermatoses (as a means of additional therapy);
• epilepsy, mental retardation (as part of combination therapy);
• to potentiate the action of analgesics and anesthetics.

Contraindications

• overdose of drugs that have a suppressive effect on the nervous system ( general anesthetics , alcohol, sleeping pills );
• concomitant use of antihypertensive drugs;
• angle-closure glaucoma;
• Parkinson's disease;
• multiple sclerosis;
• hemiplegia;
• myasthenia gravis;
• urinary retention;
• chronic cardiac failure in the stage of decompensation;
• severe liver or kidney failure ;
• suppression of bone marrow hematopoiesis;
• severe 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 case of epilepsy , in old age, in persons with a history of cardiac diseases.

Side effects

• Circulatory phenomena: orthostatic hypotension , decreased blood pressure, Adams-Stokes syndrome , increased QT interval, tachycardia . When using phenothiazine antipsychotics, cases of sudden death are known.
• Hematopoietic phenomena: agranulocytosis, pancytopenia, leukopenia, thrombocytopenia, eosinophilia.
• Nervous phenomena: dizziness, drowsiness, fatigue, visual hallucinations, confusion, increased intracranial pressure, catatonia , slurred speech, extrapyramidal symptoms , disorientation, epileptic seizures .
• Metabolic phenomena: changes in the menstrual cycle, galactorrhea , weight loss, mastalgia . The development of pituitary adenomas in a number of patients using phenothiazine derivatives , but more research is needed to prove a cause-and-effect relationship.
• Phenomena from the genitourinary system: discoloration of urine, difficulty urinating, impaired uterine contractions.
• Digestive symptoms: abdominal discomfort, dry mouth, vomiting, nausea, constipation , liver damage.
• Skin phenomena: hyperpigmentation, erythema, photosensitivity.
• Visual effects: pigmentary retinopathy.
• Allergic reactions: peripheral edema , laryngeal edema, bronchospasm, urticaria, anaphylactoid reactions, exfoliative dermatitis.
• Other phenomena: hyperthermia , pain and swelling in the injection area.

Side effects of the drug Tizercin

The most common side effect is postural hypotension. In this case, loss of consciousness, dizziness, drowsiness or increased fatigue may occur. In addition, side effects such as dry mouth, tachycardia, constipation and/or difficulty urinating may be noted. Cases of impotence, frigidity, and cessation of menstrual bleeding have been reported. In some cases, the composition of the blood changed and neurological symptoms occurred (extrapyramidal disorders with a predominance of akinetic-hypotonic syndrome, for example, inability to stand still, tremor, are possible). Allergic reactions and photosensitivity reactions can also sometimes develop.

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. In patients who are insensitive to other antipsychotics , 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).

For 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 of saline or 5% glucose solution and slowly administered through a dropper.

Overdose

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

Treatment of overdose: control and correction of fluid balance, electrolytes and acid-base balance, kidney function, diuresis liver enzyme concentrations . Symptomatic treatment is carried out based on an assessment of the results of the above indicators. When pressure decreases, intravenous fluid administration, Trendelenburg position, and administration of Dopamine or Norepinephrine . It is recommended to provide conditions for resuscitation due to the proarrhythmogenic effect of levomepromazine.

In case of overdose of antipsychotics , it is not recommended to use Adrenaline, Lidocaine and arrhythmic drugs . To treat seizures, Diazepam or Phenytoin (for recurrent seizures ). rhabdomyolysis develops, Mannitol is administered . selective antidote .

It is not recommended to induce artificial vomiting, since epileptic convulsions and dystonic movements of the 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

Antihypertensive drugs and MAO inhibitors should not be used simultaneously with Levomepromazine

Caution is recommended when used concomitantly with the following drugs (due to possible increased side effects):

• m-anticholinergic drugs (H1-histamine receptor inhibitors, tricyclic antidepressants);
• a number of antiparkinsonian drugs;
• Scopolamine, Atropine, Suxamethonium;
• drugs that suppress the nervous system (general anesthesia, opioid analgesics, sedatives and hypnotics, anxiolytics, tricyclic antidepressants, tranquilizers );
• drugs that stimulate the nervous system ( amphetamine derivatives and other drugs);
• Levodopa;
• hypoglycemic oral agents;
• drugs that increase the QT interval ;
• drugs that cause photosensitivity ;
• ethanol;
• antacids;
• drugs that suppress bone marrow hematopoiesis;
• Dilevalol (dosage reduction of both drugs may be required).

Levomepromazine and its non-hydroxylated derivatives are potent CYP2D6 . Concomitant use with drugs metabolized by CYP2D6 leads to increased concentrations and increased undesirable effects.

Contraindications to the use of the drug Tizercin

Tizercin tablets and solution should not be used:

• if you are allergic to phenothiazine or any ingredients included in the drug;
• during pregnancy (or planning it) or breastfeeding;
• with severe liver disease, changes in blood counts, circulatory failure;
• in case of a sudden decrease in blood pressure;
• when treated with an antidepressant belonging to MAO inhibitors;
• when treated with drugs to lower blood pressure (especially guanethidine and ACE inhibitor).

The drug should not be administered to children and persons who are unconscious, intoxicated or under the influence of drugs..

special instructions

It is recommended to stop using the drug if hypersensitivity reactions develop.

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

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

Elderly people are predisposed to the development of orthostatic hypotension , as well as to the sedative and m-anticholinergic effects of phenothiazines . They are more likely to experience extrapyramidal side 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 , arrhythmia QT syndrome

hyperthermia occurs during treatment with antipsychotics , it is necessary to exclude the possibility of 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 acute renal failure . If such symptoms or hyperthermia of unknown origin occur, use of the drug should be stopped immediately.

After abrupt withdrawal of a drug used for a long time or in large doses, vomiting, nausea, tremor , headache , increased sweating, insomnia, tachycardia , anxiety, tolerance to the sedative effect of phenothiazine derivatives and cross-tolerance to other antipsychotic drugs . For these reasons, Tizercin should always be discontinued gradually.

The development of cholestatic 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, blood pressure , ECG (for cardiac diseases and in elderly patients), potassium in the blood. It is also necessary to periodically monitor the ratio of plasma electrolytes and correct it.

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

Special instructions for the use of the drug Tizercin

If the patient has already taken MAO inhibitors, then before starting treatment with Tizercin it is necessary to take a break of at least 14 days, during which time not to take any medication. Before and during treatment, the composition of peripheral blood and the functional state of the liver, kidneys, heart, and in elderly patients, blood pressure should be regularly monitored. During treatment, drinking alcoholic beverages is prohibited. In weakened and elderly patients, it is recommended to reduce the dose. At the beginning of treatment, patients taking the drug should refrain from potentially hazardous activities that require increased attention and quick reaction. In the future, these restrictions depend on the individual response to the drug.

Reviews of Tizercin

Reviews indicate that the drug has a powerful sedative effect in case of sleep disorders and severe agitation against the background of autism, schizophrenia and other mental pathologies.

There are frequent cases of individual insensitivity to the product. Side effects are rarely reported by patients. In outpatient practice, the use of Tizercin is limited due to the difficulty of selecting doses and monitoring the patient.

Tizercin price, where to buy

The price of a package of the drug in tablets in Russia starts from 245 rubles, and in Ukraine the price of tablets approaches 114 hryvnia.

• Online pharmacies in UkraineUkraine

Pharmacy24

• Tizercin 25 mg 1 ml No. 10 injection solution ZAT FZ EGIS/VAT Pharmaceutical plant EGIS, Ugorshchina/Ugorshchina
  109 UAH.order
• Tizercin 25 mg No. 50 tablets ZAT FZ EGIS/VAT Pharmaceutical plant EGIS, Ugorshchina/Ugorshchina

  95 UAH order

Interactions of the drug Tizercin

MAO inhibitors increase the risk of extrapyramidal disorders during treatment with Tizercin due to decreased inactivation of the drug in the liver. The simultaneous administration of Tizercin and drugs that depress the central nervous system leads to an increase in the central depressive effect. Tizercin blocks dopaminergic receptors and therefore has an antagonistic effect when used simultaneously with levodopa. Under the influence of Tizercin, the antiparkinsonian effect of levodopa is sharply reduced. With the simultaneous use of Tizercin and antihypertensive drugs, the risk of orthostatic hypotension increases.