Tisercin
Tizercin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Tisercin
ATX code: N05AA02
Active ingredient: levomepromazine (levomepromazine)
Producer: EGIS PHARMACEUTICALS (Hungary)
Description and photo updated: 28.08.
Prices in pharmacies: from 209 rubles.
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Tizercin is a neuroleptic (antipsychotic drug).
Release form and composition
- film-coated tablets: round, slightly biconvex, white, odorless (50 pcs. in brown glass vials with a polyethylene lid, first opening control and accordion shock absorber, in a cardboard box 1 bottle);
- solution for infusion and intramuscular administration: transparent, colorless or slightly colored, with a characteristic odor (1 ml each in colorless glass ampoules with a break point, blue and red code rings, 5 ampoules in blisters, 2 packs in a cardboard box).
Each pack also contains instructions for the use of Tizercin.
Active substance: levomepromazine (in the form of hydrogen maleate):
- 1 tablet - 25 mg;
- 1 ml of solution - 25 mg.
Additional components of the tablets:
- excipients: sodium starch glycolate, potato starch, povidone, magnesium stearate, lactose, microcrystalline cellulose;
- shell composition: hypromellose, magnesium stearate, dimethicone, titanium dioxide.
Auxiliary components of the solution: monothioglycerol, sodium chloride, anhydrous citric acid, water for injection.
Pharmacological properties
Pharmacodynamics
Tizercin is an antipsychotic drug (neuroleptic) of the phenothiazine series. It has sedative (hypnotic), antipsychotic, hypothermic, analgesic, as well as moderate antiemetic, m-anticholinergic and antihistamine effects. Causes a decrease in blood pressure.
Mechanism of action:
- sedative: associated with blockade of adrenergic receptors of the reticular formation of the brain stem;
- hypothermic: due to blockade of dopamine receptors in the hypothalamus;
- antiemetic: associated with the blockade of dopamine D 2 -receptors of the trigger zone of the vomiting center;
- antipsychotic: based on blockade of dopamine D 2 receptors of the mesocortical and mesolimbic systems.
In levomepromazine, extrapyramidal side reactions are less pronounced than in classical antipsychotics. The substance helps to increase the pain threshold. Due to its ability to enhance the effects of analgesics, antihistamines and general anesthetics, Tizercin can be used as adjunctive therapy for acute / chronic pain syndrome.
The most pronounced analgesic effect develops within 20-40 minutes after intramuscular administration, its duration is approximately 4 hours.
Pharmacokinetics
Suction:
- oral administration: time to reach C max (maximum concentration of the substance) - 1-3 hours;
- intramuscular injection: time to reach C max in blood plasma - 0.5–1.5 hours.
Levomepromazine crosses the histohematogenous barriers, including the blood-brain barrier, and is distributed in tissues and organs.
Metabolism occurs rapidly in the liver by demethylation. In this case, sulfate and glucuronide conjugates are formed, which are excreted in the urine. N-desmethylomono-methotrimeprazine, a metabolite formed as a result of demethylation, has pharmacological activity, the other metabolites do not show activity.
T 1/2 (half-life) - from 15 to 30 hours.
About 1% of the dose is excreted unchanged in feces and urine.
Indications for use
- pain syndrome (neuritis of the facial nerve, trigeminal neuralgia, shingles);
- psychomotor agitation of various etiologies: with epilepsy, oligophrenia, bipolar disorders, acute and chronic schizophrenia, psychosis (including intoxication and senile);
- mental disorders, occurring with agitation, persistent insomnia, panic, anxiety, phobias.
Tizercin is also used to enhance the action of agents for general anesthesia, analgesics and blockers of histamine H 1 receptors.
Contraindications
Absolute:
- Parkinson's disease;
- myasthenia gravis;
- multiple sclerosis;
- hemiplegia;
- angle-closure glaucoma;
- severe arterial hypotension;
- chronic heart failure in the stage of decompensation;
- porphyria;
- retention of urine;
- oppression of bone marrow hematopoiesis (granulocytopenia);
- severe hepatic / renal failure;
- overdose of drugs that have a depressing effect on the central nervous system (hypnotics, general anesthetics, alcohol);
- children under 12 years old;
- pregnancy (unless the expected benefit outweighs the potential risks);
- lactation;
- simultaneous use of antihypertensive drugs;
- hypersensitivity to the components of Tizercin or other phenothiazines.
Relative:
- history of cardiovascular disease, especially in the elderly (arrhythmia, impaired cardiac muscle conduction, congenital lengthening of the QT interval);
- epilepsy;
- impaired renal / liver function;
- elderly age.
Tizercin, instructions for use: method and dosage
Film-coated tablets
In tablet form, Tizercin should be taken orally.
The initial daily dose is 25-50 mg in divided doses, while the maximum part of the daily dose is recommended to be taken before bedtime. Then the dose is increased every day by 25-50 mg until the desired effect is achieved. For patients resistant to other antipsychotics, the dose should be increased faster - by 50–75 mg per day.
The average daily dose of Tizercin is 200-300 mg.
After improvement of the condition, the dose is reduced to a maintenance dose, which is determined individually for each patient. For neurotic disorders, 12.5-50 mg (½-2 tablets) per day is usually sufficient.
Solution for infusion and intramuscular administration
In the form of a solution, Tizercin is prescribed in the absence of the possibility of taking the drug in tablet form.
The solution is injected deeply intramuscularly or intravenously.
For intravenous drip infusion, Tizercin (50-100 mg) is diluted with 250 ml of 0.9% sodium chloride solution or 5% dextrose solution and injected slowly through a dropper.
The daily dose is 75-100 mg, divided into 2-3 injections. If necessary, increase to 200-250 mg.
The treatment is carried out in bed rest, under the control of the pulse and blood pressure.
Clinical experience with the use of Tizercin in the form of a solution in children under 12 years of age is insufficient. In case of an urgent need to prescribe the drug, the recommended daily dose is 0.35–3 mg / kg.
Side effects
- from the central nervous system: visual hallucinations, increased fatigue, disorientation, dizziness, increased intracranial pressure, confusion, catatonia, slurred speech, drowsiness, epileptic seizures, extrapyramidal symptoms with a predominance of akineto-hypotonic syndrome (parkinsonism, dystonia, opistotonia, hyperreflexia), neuroleptic malignant syndrome;
- from the cardiovascular system: tachycardia, Adams-Stokes syndrome, decreased blood pressure, prolongation of the QT interval (arrhythmogenic effect, pirouette-type arrhythmias), orthostatic hypotension (with concomitant dizziness, weakness, loss of consciousness); there are isolated cases of sudden death, presumably caused by cardiac causes;
- from the digestive system: nausea, abdominal discomfort, vomiting, liver damage (jaundice, cholestasis), constipation, dry mouth;
- on the part of the organ of vision: retinopathy pigmentosa, deposits in the lens and cornea;
- from the urinary and reproductive systems: impaired contractions of the uterine muscles, discoloration of urine, difficulty urinating;
- from the side of metabolism: menstrual irregularities, galactorrhea, mastalgia, weight loss, pituitary adenoma (however, a causal relationship with the use of Tizercin has not been proven);
- from the hematopoietic system: eosinophilia, leukopenia, thrombocytopenia, agranulocytosis, pancytopenia;
- on the part of the skin: erythema, photosensitivity, hyperpigmentation;
- allergic reactions: urticaria, bronchospasm, exfoliative dermatitis, peripheral edema, laryngeal edema, anaphylactoid reactions;
- others: hyperthermia (may be the first sign of neuroleptic malignant syndrome), edema and pain at the injection site.
In the case of abrupt withdrawal of Tizercin, used in high doses or for a long period, the following are possible: increased sweating, insomnia, anxiety, tremor, headache, nausea, vomiting, tolerance to the sedative effect of phenothiazine derivatives, cross-tolerance to various antipsychotics.
Overdose
The main symptoms: a decrease in blood pressure, conduction disturbances in the heart muscle (ventricular tachycardia of the "pirouette" type, lengthening of the QT interval, atrioventricular block), hyperthermia, depression of consciousness of varying severity (up to coma), sedation, extrapyramidal symptoms, epileptic seizures, neuroleptic malignant syndrome.
Therapy: control of acid-base balance, electrolyte and fluid balance, urine volume, renal function, liver enzyme activity, ECG readings; in patients with neuroleptic malignant syndrome, body temperature and serum creatine phosphokinase should be monitored.
Based on the results of the assessment of the above parameters, symptomatic treatment is prescribed:
- lowering blood pressure: intravenous fluid, Trendelenburg position, norepinephrine / dopamine use. Conditions for resuscitation should be provided, and with the introduction of norepinephrine / dopamine - for an ECG. It is not recommended to use adrenaline. It is also necessary to avoid the use of lidocaine and, if possible, long-acting arrhythmic drugs;
- convulsions: use of diazepam, in case of recurrence of convulsive seizures - phenytoin;
- rhabdomyolysis: use of mannitol.
Forced urination, hemoperfusion, and hemodialysis are ineffective. There is no specific antidote.
It is not recommended to induce vomiting, since dystonic reactions of the muscles of the neck and head, intermittent epileptic seizures can lead to the ingress of vomit into the respiratory tract.
Even 12 hours after taking the Tizercin tablets, it is possible to perform gastric lavage along with the control of vital signs, which is associated with the natural delayed excretion of levomepromazine (due to the m-anticholinergic action). In addition, activated charcoal and laxatives may be prescribed to reduce the absorption of the agent.
special instructions
Older people with dementia who received antipsychotic medications had a slight increase in mortality risk. There are insufficient data to determine the cause and the exact magnitude of the risk, however, Tizercin should not be prescribed for the treatment of behavioral disorders associated with dementia in elderly people.
After the introduction of the first dose of Tizercin solution for 30 minutes, the patient should be in the supine position to avoid the development of orthostatic hypotension. If dizziness occurs after the administration of the drug, bed rest is recommended after each dose.
The injection sites should be alternated if possible, since there is a possibility of local irritation and tissue damage.
Before prescribing Tizercin, an electrocardiogram must be performed to exclude the presence of cardiovascular diseases, which may be contraindications to the use of the drug.
Hyperthermia may be the first sign of neuroleptic malignant syndrome (NMS), which is a potential life-threatening disorder. Other symptoms of NMS: impaired function of the autonomic nervous system (increased sweating, tachycardia, unstable blood pressure, arrhythmia), confusion, catatonia, muscle stiffness, myoglobinuria (rhabdomyolysis), increased creatine phosphokinase activity, acute renal failure. In the event of hyperthermia of unclear etiology or any of these symptoms, you should immediately stop taking Tizercin and conduct an examination for the presence of NNS.
Due to the likelihood of a decrease in the threshold of seizure activity and the development of epileptiform changes in electroencephalography, patients with epilepsy should be carefully monitored and controlled by electroencephalography during dose titration.
Before the appointment of Tizercin and periodically during treatment, regular monitoring of the following indicators is recommended: liver function (especially in patients with concomitant diseases), electrocardiogram, blood pressure, leukocyte blood count, serum potassium concentration, electrolyte levels in the blood.
During treatment and for 4-5 days after its completion, it is prohibited to consume alcoholic beverages.
You should not abruptly stop treatment, the drug must be canceled gradually (by reducing the dose).
Influence on the ability to drive vehicles and complex mechanisms
At the beginning of taking Tizercin, you should refrain from driving and performing potentially dangerous work. Further, the degree of restriction is determined individually.
Application during pregnancy and lactation
In pregnancy, Tizercin is contraindicated. It can only be used in cases where the expected benefit from therapy is higher than the possible risk.
It is contraindicated for women during lactation to use the drug, since levomepromazine is excreted in breast milk.
Pediatric use
Patients under 12 years of age are not prescribed Tizercin.
With impaired renal function
- severe renal impairment: Tizercin is contraindicated;
- renal failure: Tizercin can be used under medical supervision (associated with the risk of drug accumulation).
For violations of liver function
- severe hepatic impairment: Tizercin is contraindicated;
- liver failure: Tizercin can be used under medical supervision (associated with the risk of drug accumulation).
Use in the elderly
In elderly patients, especially those with a history of cardiovascular disease, therapy should be performed with caution.
Drug interactions
Combinations not recommended:
- antihypertensive drugs: the risk of a pronounced decrease in blood pressure;
- monoamine oxidase inhibitors: the risk of increasing the duration of action of levomepromazine and increasing the severity of its side effects.
Combinations requiring caution:
- drugs with m-anticholinergic activity (scopolamine, atropine, suxamethonium, blockers of histamine H 1 receptors, tricyclic antidepressants, some antiparkinsonian drugs): the m-anticholinergic effect of levomepromazine is enhanced (paralytic intestinal obstruction, glaucoma may develop); urinary retention;
- scopolamine: extrapyramidal side effects occur;
- levodopa: its effect is weakened;
- drugs that stimulate the central nervous system (for example, amphetamine derivatives): their psychostimulating effect decreases;
- drugs that depress the central nervous system (anxiolytics, tranquilizers, agents for general anesthesia, opioid analgesics, tricyclic antidepressants, sedatives and hypnotics): the depressing effect of levomepromazine on the central nervous system is enhanced;
- oral hypoglycemic agents: their effectiveness decreases;
- drugs that cause photosensitization: the likelihood of photosensitization increases;
- drugs that inhibit bone marrow hematopoiesis: the risk of myelosuppression increases;
- antacids: the absorption of levomepromazine in the gastrointestinal tract decreases (it should be taken 1 hour before or 4 hours after taking antacids);
- drugs metabolized mainly by CYP2D6: an increase in their concentration is possible and, as a result, an increase in undesirable effects;
- drugs that lengthen the QT interval (antibiotics from the macrolide group, diuretics that reduce the concentration of potassium, cisapride, some antiarrhythmic, antifungal and antihistamines, some antidepressants and azole derivatives): the risk of prolongation of the QT interval and the development of arrhythmias increases;
- Dilevalol and other beta-blockers: there is a mutual enhancement of the action of both drugs;
- ethanol: increased inhibition of the central nervous system, the likelihood of extrapyramidal side effects increases.
Analogs
Tizercin analogs are: Aminazine, Chlorpromazine hydrochloride.
Terms and conditions of storage
Keep out of the reach of children, protected from light.
Shelf life:
- coated tablets - 5 years at a temperature of 15–25 ° C;
- solution for infusion and injection - 2 years at temperatures up to 25 ° C.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Tizercin
According to reviews, Tizercin is an effective hypnotic, although there are reports that the drug did not have a therapeutic effect. Some patients indicate the development of side effects.
Price for Tizercin in pharmacies
The approximate price for Tizercin (50 tablets) is 215 rubles.
Tizercin: prices in online pharmacies
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Drug name Price Pharmacy |
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Tizercin 25 mg film-coated tablets 50 pcs. 209 RUB Buy |
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Tizercin 25 mg / ml solution for infusion and intramuscular administration 1 ml 10 pcs. 225 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
