Tisercin

Tisercinum is a neuroleptic of the phenothiazine subgroup. The element levomepromazine is an analogue of chlorpromazine, showing a more powerful suppressive effect on psychomotor activity.

Levomepromazine is a strong antagonist of α-adrenergic receptors, while exerting a weak anticholinergic effect. The active ingredient increases the pain threshold (its analgesic effect is similar to morphine) and has amnestic properties. The ability to potentiate the activity of analgesics makes it possible to use levomepromazine as an adjuvant drug for severe acute or chronic pain. [1]

Indications Tisercin

It is used in the case of active forms of psychotic states, during which there is marked anxiety and psychomotor agitation (acute schizophrenic attacks and other severe mental disorders).

It is prescribed for the adjuvant treatment of chronic psychosis ( schizophrenia and psychosis of the hallucinatory type).

Release form

The release of the medication is sold in the form of tablets - 50 pieces inside a glass bottle.

Pharmacodynamics

Levomepromazine blocks the endings of dopamine inside the hypothalamus with the thalamus, as well as the limbic and reticular systems, which leads to oppression of the sensory system, weakening of motor activity and the development of a powerful sedative effect. Along with this, the drug demonstrates an antagonistic effect relative to other neurotransmitter systems (serotonin with norepinephrine, acetylcholine and histamine). The result of this activity is the development of anti-adrenergic, antihistamine and anticholinergic effects.

Extrapyramidal negative manifestations are weaker than in the case of using powerful antipsychotics. [2]

Pharmacokinetics

When administered orally, the drug is absorbed at a high rate inside the gastrointestinal tract. Indicators of plasma Cmax reaches after 1-3 hours from the moment of admission.

The substance participates in intensive metabolic processes with the formation of sulfates and conjugates together with glucuronic acid; these elements are excreted through the kidneys. [3]

A small portion of the portion (1%) is excreted unchanged along with feces and urine. The half-life is 15-30 hours.

Dosing and administration

Adults.

Therapy should be started with a small dosage, gradually increasing it (taking into account the tolerance). When there is a noticeable improvement in the patient's condition, the portion is reduced to a maintenance portion (it is personally selected by the doctor).

The size of the initial portion is in the range of 25-50 mg (1 tablet 1-2 times a day). If necessary, the initial dosage can be increased to 0.15-0.25 g (6-10 tablets 2-3 times per day). In this case, the maximum part of the daily portion should be consumed in the evening. When the condition improves, the portion is reduced to a maintenance portion. A maximum of 0.25 g of Tizercin can be taken per day.

The duration of therapy is personally selected by the doctor, taking into account the effect of the drug.

For a child from 12 years old.

Since children are more sensitive to the sedative and antihypertensive effects of levomepromazine, they can be prescribed no more than 25 mg of the drug per day.

• Application for children

The medication cannot be prescribed in pediatrics (in children under 12 years of age).

Use Tisercin during pregnancy

In some cases, when using phenothiazine during pregnancy, the child was observed to have congenital developmental anomalies, but it was not possible to establish a connection with the intake of phenothiazine. Since the drug has not been clinically tested, it is not prescribed in the 3rd trimester.

Levomepromazine is secreted with breast milk, which is why it is not used for hepatitis B.

Contraindications

The main contraindications:

• severe intolerance associated with the active ingredient, phenothiazines or other elements of the drug;
• glaucoma;
• combined use with other antihypertensive substances;
• combination with MAOI;
• administration together with CNS depressants (drugs for general anesthesia, alcohol and sleeping pills);
• Parkinson's disease;
• delay in urination processes;
• multiple form of sclerosis;
• myasthenia gravis and hemiplegia;
• severe type of cardiomyopathy (circulatory failure);
• severe liver / kidney failure;
• a decrease in blood pressure that has clinical significance;
• diseases affecting the hematopoietic organs;
• porphyria;
• elderly people (over 65 years of age).

Side effects Tisercin

Among the side signs:

• violations of the cardiovascular system: often there is the development of orthostatic collapse, in which there is dizziness, weakness, or fainting. In addition, the appearance of Adams-Stokes syndrome, NNS or tachycardia, as well as prolongation of the QT-interval (proarrhythmogenic effect, pirouette-type arrhythmia) and heart attacks, which can cause sudden death, are possible;
• problems with the activity of the hematopoietic system: leuko-, thrombocyto- or pancytopenia, agranulocytosis, venous thromboembolism (this includes pulmonary embolism and DVT), hyperglycemia and the withdrawal syndrome observed in newborns;
• disorders of the NS function: confusion, catatonia, disorientation, seizures of epilepsy, visual hallucinations, increased ICP levels, indistinct speech, reactivation of psychotic manifestations and extrapyramidal disorders (dystonia, dyskinesia, opistotonus, parkinsonism, as well as hyperreflexia);
• lesions associated with metabolic processes and the endocrine system: disorders of the menstrual cycle, galactorrhea and weight loss. Individuals using phenothiazine developed pituitary adenoma. But to identify a connection with a medication, a more detailed study is required;
• disorders of urogenital function: problems with urination, discoloration of urine and priapism. Chaotic uterine contractions are singly noted;
• disorders in the digestive tract: abdominal discomfort, vomiting, xerostomia, nausea and constipation, which can cause paralytic intestinal obstruction. In addition, hepatic lesions (cholestasis or jaundice) and necrotizing enterocolitis, which can lead to death;
• epidermal lesions: erythema, pigmentation, photosensitivity, exfoliative dermatitis and urticaria;
• problems with visual function: opacity in the cornea and lens, as well as pigmented retinopathy;
• symptoms of intolerance: peripheral edema, asthma, edema in the larynx and anaphylactoid manifestations;
• others: cardiac arrhythmia, hyperthermia, vitamin deficiency, glucose intolerance and the development of heatstroke when in a humid hot room.

Overdose

Among the signs of poisoning:

• changes in the main vital functions (hyperthermia, decrease in blood pressure);
• cardiac conduction disorders (pirouette-type tachycardia, QT prolongation, ventricular fibrillation or tachycardia and blockade);
• extrapyramidal manifestations;
• sedative effect;
• excitement of the activity of the central nervous system (epileptic seizures) and neuroleptic syndrome;
• change in ECG readings, loss of consciousness, dyskinesia and hypothermia.

Symptomatic procedures are prescribed taking into account the data from the control of basic vital functions.

In the event of a decrease in blood pressure values, it is necessary to inject liquid, transfer the patient to the Trendelenburg position, and in addition use norepinephrine or dopamine (the doctor must have a resuscitation kit with him; when norepinephrine or dopamine is administered, it is necessary to monitor the work of the heart through an ECG).

Diazepam is used for seizures; when they are repeated, phenobarbital or phenytoin is introduced.

Mannitol is used exclusively when rhabdomyolysis occurs.

Hemodialysis, forced diuresis and hemoperfusion procedures do not have the desired effect. Vomiting cannot be induced, since during transient epileptic seizures, aspiration of vomit may occur (due to spastic movements of the neck with the head).

It is allowed to carry out gastric lavage and monitor the indications of vital functions even after 12 hours from the moment of drug administration, because the anticholinergic effect of Tizercin inhibits the gastric emptying process. To weaken the absorption of the medication, they additionally take a laxative and activated charcoal.

With NMS, you should immediately stop taking antipsychotics and perform therapy with cold. Dantrolene Na can be added. If there is a need for the subsequent use of antipsychotics, they are used very carefully.

Interactions with other drugs

You can not combine the medication with antihypertensive drugs, as this increases the likelihood of a pronounced decrease in blood pressure.

It is forbidden to inject the drug together with MAOIs, because in this case there is a potentiation and prolongation of the negative manifestations of Tizercin.

It is necessary to very carefully combine the medication with anticholinergic substances (atropine, tricyclics, H1-antihistamines, succinylcholine, certain antiparkinsonian drugs and scopolamine) - due to the potentiation of anticholinergic effects (urinary retention, paralytic intestinal blockage and glaucoma). Administration together with scopolamine causes the development of extrapyramidal disorders.

In the case of using antipsychotics together with tetracyclines (for example, maprotiline), the likelihood of arrhythmias may increase.

The combination with tri- or tetracyclics can also provoke potentiation and prolongation of anticholinergic and sedative effects, and in addition, an increase in the likelihood of the appearance of ZNS.

The introduction together with CNS depressants (substances for general anesthesia, narcotic drugs, tranquilizers, sedative-hypnotic drugs, antipsychotics and tricyclics) potentiates the effect on the central nervous system.

Tisercinum lowers the activity of central nervous system stimulants (amphetamine derivatives are among those).

The use of the drug greatly weakens the antiparkinsonian effect of levodopa - due to the antagonistic interaction that develops due to the blockage of dopaminergic endings by neuroleptics.

The combination of the drug with taken orally hypoglycemic substances leads to a weakening of the effects of the latter. This can cause the development of hyperglycemia.

The combination of the drug with drugs that prolong the QT interval (macrolides, certain antiarrhythmic substances of classes IA and III, cisapride, certain antidepressants, antihistamines, certain azole antimycotics and diuretics with hypokalemic effect) can provoke an additive effect and increase the incidence of arrhythmias.

The use of a drug with dilevalol potentiates the activity of both drugs - this is due to the mutual suppression of metabolic processes. With the combined use of these drugs, the dosage of any of them (or both) must be reduced. A similar interaction cannot be excluded with the introduction of other β-blockers. 

When administered with medications that have a photosensitizing effect, photosensitivity may increase.

It is forbidden to consume alcoholic beverages or substances containing alcohol when using Tizercin. Alcohol is able to potentiate the suppressive effect on the central nervous system, and also increases the risk of extrapyramidal disorders.

The combination with C-vitamin weakens the vitamin deficiency caused by the use of the drug.

Storage conditions

Tisercin should be kept out of the reach of small children. Temperature level - no more than 25 ° C.

Shelf life

Tisercin can be used within a 5-year term from the date of manufacture of the medicinal product.

Reviews

Tizercin receives mixed reviews from patients who have used it. There is a powerful hypnotic and sedative effect of the drug, but it indicates the presence of a large number of side signs and contraindications.