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.
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.
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.
LEVOMEPROMAZINE
Composition and release form
Levomepromazine. Dragee (25 mg); solution for injection (in 1 amp. - 25 mg).
Levomepromazine. description of the drug
It differs in structure from aminazine by the presence in position 2 of a phenothiazine ring of a methoxy group (- OCH3) instead of a chlorine atom and an additional methyl group in the alkylamine (branched) chain.
Its pharmacological properties are similar to aminazine. The ability to potentiate the effect of narcotic and analgesic substances and the hypothermic effect of levomepromazine are more pronounced; It has strong adrenolytic activity and is inferior to aminazine in its anticholinergic and antiemetic effects. Has pronounced antihistamine activity. Has an analgesic effect. Causes relatively severe hypotension.
With regard to the neurotransmitter systems of the brain, it is characterized by a significantly stronger blocking effect on noradrenergic receptors than on dopaminergic ones.
In terms of its therapeutic effect, levomepromazine is distinguished by its high activity and rapid onset of sedation, which makes it possible to use it in acute psychoses. Unlike aminazine, it does not increase depression, but itself has some antidepressant activity. The drug, however, does not have a pronounced thymoleptic effect and, in case of typical endogenous depression, cannot replace tricyclics or other modern antidepressants.
pharmachologic effect
Levomepromazine is a phenothiazine neuroleptic. It relieves psychomotor agitation, has antipsychotic, sedative (hypnotic), analgesic, moderate antiemetic, hypothermic, antihistamine and M-anticholinergic effects. Has some antidepressant activity. Causes a decrease in blood pressure. The antipsychotic effect is due to the blockade of dopamine D2 receptors in the mesolimbic and mesocortical systems.
The sedative effect is due to the blockade of adrenergic receptors of the reticular formation, the antiemetic effect is due to the blockade of dopamine D2 receptors of the trigger zone of the vomiting center, the hypothermic effect is due to the blockade of dopamine receptors of the hypothalamus. Levomepromazine increases the pain threshold and enhances the effect of analgesics.
Indications
– psychomotor agitation of various etiologies; – manic stage of manic-depressive psychosis, involutional psychosis, depressive-paranoid schizophrenia, catatonic agitation, reactive depression, alcoholic psychosis and other psychotic states occurring with symptoms of anxiety, fear, restlessness; – neurotic disorders with increased excitability, sleep disturbances; – diseases accompanied by pain: trigeminal neuralgia, facial neuritis, 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.
Application
Prescribed orally, intramuscularly, less often - intravenously. For intramuscular administration, a 2.5% solution of levomepromazine is diluted in 3-5 ml of isotonic sodium chloride solution or 0.5% novocaine solution and injected deep into the upper outer quadrant of the buttock. IV administration is done slowly; the drug solution is diluted in 10-20 ml of 40% glucose solution.
Drip infusions are also used, diluting 50-100 mg of the drug in 250 ml of isotonic sodium chloride solution or isotonic glucose solution. In patients with psychosis during agitation, treatment begins with parenteral administration of 25-75 mg of levomepromazine (1-3 ml of solution), if necessary, increase the daily dose to 200-250 mg (sometimes up to 350-500 mg) with intramuscular administration and up to 75 -100 mg with intravenous administration. As the symptoms of agitation regress, parenteral administration is gradually replaced by oral administration of the drug. Orally prescribed 50-100 mg (up to 300-400 mg/day).
For moderately severe psychopathological disorders, course treatment begins with a daily dose of 25-50 mg (1-2 ml solution or 1-2 tablets), increasing the daily dose by 25-50 mg to a daily dose of 200-300 mg orally or 75-200 mg parenterally (in rare cases - up to a daily dose of 600-800 mg orally). Towards the end of the course of treatment, the dose is gradually reduced and 25-100 mg/day is prescribed for maintenance therapy.
To relieve acute alcoholic psychosis, 50-75 mg of the drug is prescribed intravenously. According to indications, 100-150 mg is administered intramuscularly for 5-7 days. In outpatient practice, patients with neurotic disorders are prescribed levomepromazine orally in a daily dose of 12.5-50 mg (1/2-2 tablets). During treatment with levomepromazine, systematic complete blood count and assessment of liver function are recommended; in elderly patients, blood pressure control is indicated.
In order to prevent orthostatic collapse, after the first large dose of levomepromazine or after repeated administrations of the drug, the patient is prescribed bed rest for 30 minutes.
If it is impossible, according to clinical indications, to stop taking levomepromazine in pregnant women during the entire period of pregnancy, minimum maintenance doses of the drug are prescribed, reducing them towards the end of the pregnancy to prevent the development of atropine-like effects in newborns.
During the initial, individually determined period of use of levomepromazine, driving vehicles and engaging in other potentially hazardous activities that require a quick mental and motor reaction are prohibited. In the process of further treatment, the degree of restrictions is determined depending on the individual tolerability of the drug. During treatment with levomepromazine, the consumption of alcoholic beverages is not recommended.
Side effect
On the central nervous system: extrapyramidal disorders with a predominance of akinetic-hypotonic syndrome, increased fatigue, drowsiness, confusion, slurred speech. On PS: dry mouth, nausea, vomiting, constipation, impaired liver function. On the cardiovascular system: orthostatic hypotension, tachycardia. On CK: pancytopenia, agranulocytosis, leukopenia, eosinophilia, thrombocytopenia. On ES: galactorrhea, menstrual irregularities, mastalgia, pituitary adenoma. Dermatological reactions: photosensitivity, erythema, pigmentation. AR: laryngeal edema, edema, anaphylactoid reactions, bronchospasm, urticaria, dermatitis. Other: urinary disorders, hyperthermia, pain and swelling at injection sites.
Contraindications
– persistent arterial hypotension, especially in elderly patients; – liver diseases; – kidney diseases; – diseases of the hematopoietic system; – chronic cardiovascular failure in the decompensation phase; – lactation period, childhood; – angle-closure glaucoma, urinary retention, multiple sclerosis, myasthenia gravis, hemiplegia, hypersensitivity to phenothiazines.
Overdose
Symptoms. Arterial hypotension, ventricular tachycardia, extrapyramidal disorders, convulsive syndrome, coma. Treatment. Resuscitation measures and symptomatic therapy in a specialized hospital department.
Interaction with other drugs
MAO inhibitors increase the risk of extrapyramidal disorders during treatment with levomepromazine due to reduced inactivation of the drug in the liver. The simultaneous administration of levomepromazine and drugs that have a depressant effect on the central nervous system leads to an increase in the central depressive effect.
Under the influence of levomepromazine, the antiparkinsonian effect of levodopa is sharply reduced due to the antagonistic interaction caused by the blockade of dopaminergic receptors caused by neuroleptics.
With simultaneous use of levomepromazine and antihypertensive drugs, the risk of orthostatic hypotension increases. After taking antacids containing salts, oxides or hydroxides of aluminum, magnesium or calcium, the absorption of levomepromazine is reduced, therefore, if combined use of these drugs is necessary, levomepromazine should be prescribed 1 hour before or 4 hours after taking the antacid drug, unless parenteral administration is indicated neuroleptic. The combination of levomepromazine and drugs with M-anticholinergic activity leads to increased undesirable anticholinergic manifestations.
Use of the drug Tizercin
For psychotic conditions, the daily dose is 25–50 mg (1–2 tablets); if necessary, the dose can be increased to 150–250 mg/day (6–10 tablets per day). You cannot take more than 10 tablets per day. To reduce anxiety, the initial daily dose is 12.5–25 mg (1/2–1 tablet) per day. If necessary, this dose can be increased to 75–100 mg/day (3–4 tablets per day). After the condition improves, the dose can be reduced and a maintenance dose selected. Parenteral administration of the drug is indicated in cases where oral administration is not possible. The daily dose is usually 75–100 mg 1–2 times a day (3–4 ml of the drug) under the control of blood pressure and heart rate. Injections must be done deep intramuscularly. When administered intravenously, the solution should be diluted and administered only as a drip infusion (50–100 mg of the drug in 250 ml of isotonic sodium chloride solution or glucose solution).
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.
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..
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 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.
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.
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.
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.
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
